Title of Invention

MANDELIC ACID DERIVATIVES

Abstract

ABSTRACT "MANDELIC ACID DERIVATIVES" The invention is concerned with novel mandelic acid derivatives of formula (1), wherein R1 to R10, X and Y are as defined in the description and in the claims, as well as physiologicaJly acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, 1xa and thrombin induced by factor VIIa and tissue factor and can be used as medicaments. ABSTRACT "MANDELIC ACID DERIVATIVES" The invention is concerned with novel mandelic acid derivatives of formula (1), wherein R1 to R10, X and Y are as defined in the description and in the claims, as well as physiologicaJly acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, 1xa and thrombin induced by factor VIIa and tissue factor and can be used as medicaments.

Full Text

Mandelic acid derivatives The invention is concerned with novel mandelic acid derivatives of the formula (I) wherein R1 is hydrogen, OH, NH2, lower-alkoxy-carbonyl, aryi-lower-alkoxy-carbonyi, aryloxy-carbonyl, lower-alkyl-carbonyl, aryi-carbonyi, or lower-alkoxy-carbonyl which is substituted with halogen; R2, R2 and R8 independently from each other are selected from the group consisting of hydrogen, halogen, hydroxy, carboxy-lower-allqd-NH, carbamoyl-lower-alk)4-NH, lower-alkoxy-carbonyl-lower-alkyl-NH, hydroxy-cycloalkyl-oxy, dihydroxy-cydoaBcyi-oxy, aryl, aryioxy, aryl-NH, aryl-lower-alkyl-NH, aryl-lower-alkyi-S02-NH, aryl-lower-alkoxy-carbonyl-NH, aryl-lower-alkyl-NH-carbonyl-NH, heteroaryloxy, heteroaryl-lower-alkyl-NH, and lower-alkoxy, which lower-alkoxy can optionally be substituted with hydroxy, carboxy, carbamo)d, carbamimidoyl, CF3, arji, heteroaryl, lower-alkyl-carbamoyl, lower-alkoxy-carbonyl, aryl-carbamoyi, lower-alkoxy-lower-alkyl-carbanioyl, heterocyclyl-lower-alkji-carbamoyl, or N(lower-alk)d)2-Iower-aIkyi-carbamoyl; R2 is lower-aDcyl or cycloalkyl, or, if X is O or NR , R2 can also be hydrogen; R6 is hydrogen, lower-alkyl, or fluoro-lower-alkyl; CS / 02.10^003 y isNorC-R6; R , R , R1, R and R independently from each other are selected from the group consisting of hydrogen, hydroxy, halogen, amino, lower-alkyl-amino, di-lower-alkyl-amino, lower-alkyl-carbonyl-amino, NO2, fluoro-lower-alkyi, lower-alkoxy, hydroxy-Iower-alkoxy, fluoro-lower-alkoxy, lower-alkinyl, hydroxy-lower-alkinyl, aryi, aryl-Iower-alkoxy, aiyloxy, aryloxy-lower-alkoxy, heterocyclyl, heterocyclyloxy, lower-alkoxy-carbonyi-lower-alkoxy, carbamoyl-lower-allcoxy, carboxy-lower-alkoxy, cycloalkyloxy, heteroaryl, amino-lower-alkosy, lower-alkyl-amino-loweR1alkoxy, and di-lower-alkyl-amino-lower-aJkoxy, lower-alk)d-carbonyl-amino-lower-altyl, HO-N=CH, HCO, fluoro-lower-aIkyl-S02-0, (lower-alkoxy):^) CH(lower-aIkoxy)2, hydroxy-chloro-lower-alkoxy, aryl-lower-alkoxy-lower-alkoxy, aryl-NH, aryi-NH-lower-alkyl, aryl-lower-alkyl-carbonyl-NH, heterocycl^-lower-alkyi, heterocyclyj-carbonyl, heterocyclyl-lower-alkoxy, lower-alkyl-carbamoyl, fluoro-lower-alkji-carbamojd, cycloalkyl-carbamoyl, cycioalkyi-lower-aBcjd-carbamoyl, di-lower-alk)i-carbamoyl, lower-alkoxy-Iower-alkyl-carbamoyi, di-lower-aUcyl-carbamo^d-lower-alkoxy, heteroaryloxy, heteroaryl-lower-alkoxy, amino-lower-alkyl, lower-alkyl, hydroxy-lower-allcjd, cycloalkyl, and cycloalkyi-lower-alkoxy which is optionally substituted with lower-alkyl; or R2 and R2 or R2 and R2 are bound to each other to form a ring together with the carbon atoms to which they are attached and R2 and R1 together or R2 and R2 together are -O-CH2-O-, -O-CHa-CXD-NH-, -O-CH2-CH2-CH2-. or -CH=CH-CH=CH-, which can optionally be substituted with lower-allcyd or lowei-alkoxy, and R2°, R6 and R2 oi R1 respectively are as defiiide above; X is O, S, NR112 or SO2; R2^ is hydrogen, lower-alkyl, or lower-alkjd-carbonyl; and pharraaceutically acceptable salts diereof. Further, the invention is concerned with a process for the manufecture of the above compounds, pharmaceutical preparations which contain such compounds as well as the use of these compounds for the production of pharmaceutical preparations. The compounds of formula (I) are active compounds and inhibit the formation of coagulation &ctors Xa, IXa and thrombin induced by fector Vila and tissue fector or are derivatives which are converted under physiological conditions to such active compounds. These compounds consequently influence both platelet aggregation which is induced by these factors and plasmatic blood coagulation. They therefore inhibit the formation of thrombi and can be used for the treatment and/or prevention of diseases, such as arterial and venous thrombosis, deep vein thrombosis, pulmonary embolism, unstable angina pectoris, cardiac infarction, stroke due to atrial fibrillation, inflammation and arteriosclerosis. Furthermore, these compounds have an effect on tumour cells and prevent metastases. They can therefore also be used as antitumour agents. Inhibitorsof factor Vlla had previously been suggested for the inhibition of the formation of thrombi and for the treatment of related diseases (WO 00/35858). However, there is still a need for novel factor Vlla inhibitors which exhibit improved pharmacological properties. The present invention provides the novel compounds of formula (I) which are factor Vila inhibitors. The compounds of the present invention exhibit improved pharmacological properties compared to the known compounds. Unless otherwise indi In this specification the term "loweR6 is used to mean a group consisting of one to seven, preferably of one to four carbon atom{s). The term "halogen" refers to fluorine, chlorine, bromine and iodine, with fluorine, chlorine and bromine being preferred. The term "alkyl", alone or in combination with other groups, refers to a branched or straight-chain monovalent saturated aliphatic hydrocarbon radical of one to twenty carbon atoms, preferably one to sixteen carbon atoms, more preferably one to ten carbon atoms. Lower-alkyl groups as described below also are preferred alkyl groups. The term "lower-alkyl", alone or in combination with other groups, refers to a branched or straight-chain monovalent alkyl radical of one to seven carbon atoms, preferably one to four carbon atoms. This term is further exemplified by such radicals as methyl, ethyl, n-propyl, isopropyl, n-butyl, s-butyl, t-butyl and the like. The term "fluoro-lower-alkyl" refers to lower-alkyl groups which are mono- or multiply substituted with fluorine. Examples of fluoro-lower-alkyi groups are e.g. CFH2, CF2H, CF3, CF3CH2, CF3(CH2)2, (CFjjiCH and CF2H-CF2 The term "cycloalkyl" refers to a monovalent carbocydic radical of 3 to 10 carbon atoms, preferably 3 to 6 carbon atoms, such as cyclopropyl, cyclobutyi, cyclopentyl, or cydohexyl. The term "cycloalkyloxy" refers to the group cydoaIky!-0-. The term "alkoxy" refers to the group R1-O-, wherein R1 is an alkyl. The term "lower-alkoxy" refers to the group R1-O-, wherein R1 is a lower-alkyl. The term "thio-alkoxy" refers to the group R1-S-, wherein R1 is an alkyl. The term "thio-lower-alkoxy" refers to the group R1-S-, wherein R1 is a lower-alkyl. The term "fluoro-lower-alkoxy" refers to the group R6-0-, wherein R6 is fluoro-lower-alkyl. Examples of fluoro-lower-alkoxy groups are e.g. CFH2-O, CF2H-O, CF3-O, CF3CH2-O, CF3(CH2)2-0. (CF3)2CH-0, and CF2H-CF2-O, The term "alkenyl", alone or in combination with other groups, stands for a straight-chain or branched hydrocarbon residue comprising an olefinic bond and 2 to 20, preferably2 to 16 carbon atoms, more preferrabiy2 to 10 carbon atoms. Lower-alkenyl groups as described below also are preferred alkenyl groups. The term "lower-alkenyl" refers to a straight-chain or branched hydrocarbon residue comprising an olefinic bond and 2 to 7, preferably 2 to 4 carbon atoms, such as e.g. 2-propenyl. The term "alkinyl", alone or in combination with other groups, stands for a straight-chain or branched hydrocarbon residue comprising a tripple bond and up to 20, preferably up to 16 carbon atoms. The term "lower-alkinyl" refers to a straight-chain or branched hydrocarbon residue comprising a tripple bond and 2 to 7, preferably 2 to 4 carbon atoms, such as e.g. 2-propinyl. Lower-alkinyl groups can be substituted, e.g. by hydroxy. The term "alkylene" refers to a straight chain or branched divalent saturated aliphatic hydrocarbon group of 1 to 20 carbon atoms, preferably 1 to 16 carbon atoms, more preferably up to 10 carbon atoms. Lower-alkylene groups as described below also are preferred alkylene groups. The term "lower-alkylene" refers to a straight chain or branched divalent saturated aliphatic hydrocarbon group of 1 to 7, preferably 1 to 6 or 3 to 6 carbon atoms. Straight chain alkyiene or lower-alkylene groups are preferred. The term "aryl" relates to the phenyl or naphthyl group, preferably the phenyl group, which can optionally be substituted by 1 to 5 , preferably 1 to 3, substituents independently selected from the group consisting of lower-alkenjd, lower-alldnyl, dioxo-lower-alkylene {forming e.g. a benzodioxyl group), halogen, hydroxy, CN, CFa, NH;, N(H, lower-allcyl), N(lower-alk)'l)2, aminocarbonyl, carboxy, NO2, lower-alkoxy, tbio-lower-alkoxyi lower-alkylcarbonyl, lower-alkyicarbonyloKy, lower-alkoxycarbonyl, lower-alkyl-carbonyl-NH, fluoro-lower-alkyl, fluoro-lower-alkoxy, lower-alkoxy-carbonyi-lower-alkoxy, carboxy-lower-altoxy, carbamoyl-lower-alkoxy, hydroxy-lower-alkoxy, NH2-lower-alkoxy, N(H, lower-allcyl)-lower-alkoxy, N(Iower-alkyl)2-lower-alkoxy, benzyloxy-lower-alkoxy, HO-N=CH-, and lower atkyl which can optionaEy be substituted with halogen, hydroxy, NH2, N(H, lower-allcyl) or N(lower-alkyl)2. Preferred substituents are halogen, lower-alkoxy, lower-alkyl-carbamoyl-NH, CN, fluoro-lower-aHcoxy, fluoro-lower-alkyl, lower-allcyl, thio-Iower-allcoxy, lower-alkoxy-carbonyl-lower-alkoxy, carboxy-lowei-allcoxy, carbamoyl-lower-aBcoxy, hydroxy-lower-alkoxy, N(lower-alkyl)2-lower-alkoxy, benzyloxy-lower-alkoxy, lower-alkoxy-carbonyl, carboxy, hydroxy-lower-alkyl, chloro-lower-alkyl, HO-N=CH-, amino-lower-allcyl, amino, and NO;- The term "aryloxy" refers to the group aryl-0-. The term "heterocycl)^' as used herein denotes non-aromatic monocydic heterocydes with 5 or 6 ring members, which comprise 1,2 or 3 hetero atoms selected from nitrogen, oxygen and sulfiir. Examples of suitable heterocydes are pyrrolidine^, oxopyrrolidinyl, pyrrolinyl, imidazoUdinyl, imidazolinyl, pyraioUdinyl, pyrazoUnyl, piperidyl, piperazinyl, morphohn^d, pyranyl, tetrahydropyran-jd, 4,5-dihydro-oxa2olyl, 4,5-dihydro-thiazolyi. Preferred heterocydes are piperidinyl, morpholinyl, pyrrolidinyl, oxopyrroHdinyl, tefrahydrofiiranyl and tetrahydropyranyl. A heterocyd)^ group may have a substitution pattern as described earher in coimection with the term "aryl". Preferred substituents are lower-alfcjd, lower-alkj^-sulfonjd, benzenesulfonyi, lower-alkyl-carbonyl and benzoyl. The term "heterocydyloxy" refers to the group heterocydyl-O-. The term "heteroaryl" refers to an aromatic 5 to 6 membered monocycUc ring or 9 to 10 membered bicycUc ring which can comprise 1,2 or 3 atoms selected from nitrogen, oxygen and/or sulphur, such as furyl, pyridyl, oxo-pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, thienyl, isoxazolyl, oxazol^, oxadiazolyl, imidazolyl, pyrtolyl, tetiazolyl, benzoimidazolyl, indolyl. Preferred heteroaryl groups are pyridinyi, oxo-pyridinyl, thienyl, furyl, oxadiazolyi, pyiimidinyl, benzoimidazolyl, indolyl. A heteroaryl group may have a substitution pattern as described earlier in connection with the term "aryl". Preferred substituents are NO2, NH2, lower-alkoxy. The term "heteroaryloxy" refers to the group heteroaryl-O-. Compounds of fonnula (I) can form pharmaceutically acceptable add addition salts. Examples of such phannaceaticaHy acceptable salts are salts of compounds of formula (I) with physiologically compatible mineral adds, such as hydrochloric add, sulphuric add, sulphurous acid or phosphoric addi 01 with organic adds, such as methanesulphonic add, p-toluenesulphonic add, acetic add, lactic add, trifiuoroacetic add, citric add, fumaric acid, maleic add, tartaric add, sucdnic add or salicylic add. The term "pharmaceutically acceptable salts" refers to such salts. Compounds of formula (I) in which a COOH group is present can further form salts with bases. Examples of such salts are alkaline, earth-alkaline and ammonium salts such as e.g. Na-, K-, Ca- and Trimeth)^ammoniumsalt The term "pharmaceutically acceptable salts" also refers to such salts. Add addition salts as described above are preferred. In detail, the present invention relates to compounds of formula (I) wherein R2 is hydrogen, OH, NH2, lower-alkoxy-carbonyl, aryl-lower-alkoxy-carbonyl, aryloxy-carbon)d, lower-aIk)d-carbonyi, ar)d-carbon)d, or lower-aikoxy-carbonyl which is substituted with halogen; R2, R2 and R8 independently from each other are selected from the group consisting of hydrogen, halogen, hydroxy, carboxy-lower-alkyi-NH, carbamoyl-Iower-alkyl-NH, lower-alkoxy-carbonyl-lower-alkji-NH, hydrory-cycloalkyl-oxy, dihydroxy-cycloalkj^-oxy, aryl, aryloxy, aryi-NH, aryHower-alkyl-NH, aryi-lower-alkyl-SOz-NH, ar)^-lower-alkoxy-carbonyi-NH, aryl-lower-alkyl-NH-carbonyl-NH, heteroaryloKy, heteroaryl-lowet-alfcyl-NH, andlower-alkoxy, which lower-alkoxy can optionally be substituted with hydroxy, carboxy, carbamo)4, carbamimidoyi, CF3, aryl, heteroaryl, lower-aUqd-carbamoyl, lower-alkoxy-carbonyl, aryl-carbamoyl, lower-alkoxy-lower-alkyl-carbamoyi, heterocyclyl-lower-alkyl-carbamoyl, or N(lower-alkyl)2-lower-aIkyl-carbamoyl; R2 is lower-alkyl or cycioalkyl, or, if X is O 01NR12, R2 can also be hydrogen; R8 is hydrogen, lower-alkyi, or fluoro-lower-alkyi; Y isNorC-R2^ R6", R2, R1, R2*' and R6 independently from each other are selected from the group consisting of hydrogen, hydroxy, halogen, amino, lower-alkyl-amino, di-lower- alkyl-amino, lower-alkyl-carbonjd-anmio, NO2, fluoro-lower-allcyi, lower-alkoxy, hydroxy-lower-alkoxy, fluoro-lower-alkoxy, lower-aBdnyl, hydroxy-lower-aDdnyl, aryl, ar)i-lower-alkoxy, aryloxy, aryioxy-Iower-alkoxy, heterocyclyl, heterocyclyioxy, lower-aDcoxy-carbonyl-lower-alkosy, carbamoyl-lower-alkoxy, carboxy-lower-alkoxy, cycloalfcyloxy, heteroarjd, amino-lower-alkoxy, lower-alkjd-amino-lower-alkoxy, and di-lower-alkyl-amino-Iower-alkoxy, lower-alkyl-carbonyI-amino-lower-alkyl,HO-N=CH, HCO, fluoro-lower-aIkyl-S02-0, (lower-alkox7)2^, CH(lower-a]koxy)2, hydroxy-chloro-lower-alkoxy, aryl-lower-alkoxy-lower-alkoxy, aryl-NH, ar)d-NH-lower-aIkyl, ar)d-iower-alkyi-carbonyl-NH, heterocyd^-lower-alkyl, heterocydyl-carbonyl, heterocyclyl-lower-alkoxy, lower-alkyl-carbamo^, fluoro-lower-alkyl-carbamoyi, cycloalk)i-carbainoyl, cydoalkyl-lower-alkyl-carbamoyi, di-lower-alkyi-carbamoyl, lower-alkoxy-lower-alkyi-carbamoyl, di-lower-alkyl-carbamoyl-lower-alkoxy, heteroaryloxy, heteroarjd-lower-alkoxy, amino-lower-alkyl, lower-alkyl, hydroxy-lower-alkyl, q'doalkyl, and cydoalkyl-lower-alkoxy whidi is optionally substituted with lower-alkyi; or R2andR2orR2andR2 are bound to each other to form a ring together with the carbon atoms to which they are attached and R2 and R togeflier or R and R together are -O-CH2-O-, -O-CH2-CO-NH-, -O-CH2-CH2-CH2-, or -CH=CH-CH=CH-, which can optionally be substituted with lower-alkyl or lower-alkoxy, and R2°, R6 and R2 or R1 respectively are as definde above; X is O, S, NR12 or SO2; R2^ is hydrogen, lower-alkyl, or lower-allcyl-carbonyl; and pharmaceutically acceptable salts thereof. One preferred embodiment of the present invention rdates to compounds of formula (I) as defined above, wherein R2 is hydrogen, OH, NH2, lower-alkoxy-carbon)4, arjd-lower-alkoxy-carbonyl, aryloxy-carbonyl, lower-alkyl-carbonyl, aryl-carbonyl, or lower-alkoxy-carbonyi which is substituted with halogen; R2, R2 and R2 independently from each other are sdected from the group consisting of hydrogen, halogen, hydroxy, and lower-alkoxy, which lower-alkoxy can optionally be substituted witii hydroxy, carboxy or carbamoyl; R2 is iower-alkyl or cycloalkyl, or, if X is O or NR12, R2 can also be hydrogen; R is hydrogen, lower-alkyl, or fluoro-lower-altji; Y isNorC-R11; VJ, R2, R2, R10 and R6 independently from each other are selected &om the group consisting of hydrogen, hydroxy, halogen, amino, lower-alkyl-amino, di-Iower-alkyi-amino, lower-alkjd-carbonyl-amino, NO2) fluoro-lower-alkyl, lower-alkoxy, hydroxy-lower-alkoxy, fluoro-lower-alkoxy, lower-alkinyl, hydroxy-lower-alldnyi, aryl, ar}^-Iower-alkoxy, aryloxy, arjdoxy-lower-alkoxy, heterocyclyl, heteiocyclyloxy, iower-alkoxy-carbonyl-Iowar-alkoxy, carbamoyl-lower-alkoxy, carboxy-lower-aUtoxy, cycloalkyloxy, heteroaryl, amino-lower-alkoxy, lower-alkyi-amino-Iower-alkoxy, and di-Iower-alkyl-amino-lower-alkoxy, or R2 and R2 or R8 and R6" are bound to each other to form a ring together with the carbon atoms to which they are attached and R8 and R1 together or R2 and R2 together are -O-CH2-O-, -O-CH2-CO-NH-, -O-CH2-CH3-CH2-, or -CH=CH-CH=CH-, which can optionally be substituted with lower-alkyl or lower-alkoxy, and R2'*, R6 and R2 or R2 respectively are as definde above; X is O, S, NR12 or SO2; R1^ is hydrogen, lower-alkyl, or lower-alkyl-carbon^; and pharmaceutically acceptable salts thereof. The compounds of formula (I) have at least one asymmetric C atom and can therefore exist as an enantiomeric mixture, diastereomeric mixture or as optically pure compounds. Compounds of formula (I) can exist in tautomeric forms and the invention encompasses all such tautomeric forms. In particular, the substituent R can be exchanged with a hydrogen atom bound to the other nitrogen atom of the amidino (carbaniimido)d) group. Compounds of formula {I) are individually preferred and physiologically acceptable salts thereof are individually preferred, with the compounds of formula (I) being particularly preferred. Preferred compounds of formula (I) are those, wherein R1 is hydrogen, OH, NHi, or lower-alkoxy-carbon^, preferably liiose. "wherdn R1 is hydrogen, OH, or lower-alkoxy-carbonyl, more preferably those wherein R2 is hydrogen, OH, or ethoxycarbonyl, and most preferably those wherein R1 is hydrogen. Another preferred embodiment of the present invention relates to compounds as described above, wherein R2, R2 and R8 independently from each other are hydrogen or halogen, with those compounds wherein R6, R2 and R2 are hydrogen being most preferred. In another preferred embodiment of the present invention, R2 and R8 are hydrogen. Compotinds as defined above, wherein R is hydrogen, halogen, hydroxy, carboxy-lower-alkyl-NH, carbamoyl-lower-alkyl-NH, iQwer-alkoxy-caibonyl-Iower-alkyl-NH, hydroxy-cycioaliyl-oxy, dihydroxy-cycloalkyi-oxy, aryl, arjdoxy, aryl-NH, aryl-lower-alkyl-NH, aryl-lower-alkyl-S02-NH, aryl-lower-allcoxy-carbonyl-NH, aryl-Iower-alk)d-NH-carbonyl-NH, beteroaiylosy, heteroaryl-Iowei-alkyi-NH, or lower-alkoxy, vriiich lower-alkosy can optionally be substituted with hydroxy, carboxy, carbamo}d, carbamimidoyi, CFs, aR2d, heteroaryl, lower-alkyd-carbamoyl, lower-alkoxy-carbonyl, aryi-carbamoyl, lower-alkoxy-lower-alkyl-caxbamoyl, heterocydyi-lower-alkyl-carbamoyl, or N(lower-alkyl)2-lowex-alkyl-carbamoyl, are also preferred. More preferably, R2 is hydrogen, halogen, carboxy-lower-alkyl-NH, aryl-lower-alkyl-NH, heteroaryi-lower-alkyl-NH, or iower-alkoxy, which lower-alkoxy can optionally be substituted with carbamoyl, heteroaR2d, or lower-alkoxy-lower-aHcyl-carbamoyl. Even more preferably, R2 is hydrogen, fluorine, carbamoylmethoxy, (2-methoxy-ethyicarbamoyl)-methoxy, pyridin-2-yi-methoxy, benzylamino, carboxymethl-amino, or pyridin-2-ylmetiiyl-amino. In a further preferred embodiment the invention rdates to compounds as described above in which X is O. Compounds in which R2 is lower-alkyl, or, if X is O or NR12, R2 can also be hydrogen, are preferred. Compounds in which R2 is lower-alkyi are also preferred, with those compounds wherein R2 is methyl or ethyl being particularly preferred. The invention embraces especially compounds in accordance with the above definitions in which R1^ is hydrogen, methyl or CFa, preferably hydrogen. In one preferred embodiment, R2 and R2 or R2 and R1 are not bound to each other to form a ring together with the carbon atoms to which they are attached. Moreover, the invention relates especially to compounds as defined above wherein Y is C-R and R , R , R2, V}° and R2' independently from each other are selected from the group consisting of hydrogen, hydroxy, halogen, di-lowei-aUcyl-amino, lower-alkjd-carbonyl-amino, NO2, fluoro-lower-atkyl, Iower-alkoxy, hydroxy-lower-alkoxy, fiuoro-Iower-alkoxy, aryl, axyi-lower-alkoxy, aryloxy, aryioxy-lower-alkoxy, heterocyclyl, heterocyclyloxy, Iower-alkoxy- carbonyl-lower-alkoxy, carbamoyl-lower-alkoxy, carboxy-lower-allcoxy, qfcloaIk)doxy, heteroaryl, and di-lower-alkyi-amino-Iower-alkoxy. More preferably, Y is C-R2' and iC, R2 R , R and R independently from each other are selected from the group consisting of hydrogen, halogen, lower-alkoxy, and pyridji. Even more preferably, Y is C-R2^ and R2, R2 R , R and R independentiy from each other are selected from the group consisting of hydrogen, fluoro, bromo, methoxy, and pyridyl. In another preferred embodiment of the present invention, Y is C-R6, R8 and R1 or R and R2 are bound to each other to form a ring together with the carbon atoms to which they are attached and R2 and R1 together or R2 and R2 together are -O-CHz-O-, -O-CH2-CO-NH-, -O-CH2-CH2-CH2-, or -CH=CH-CH=CH-, which can optionaUy be substituted with lower-allqd or lower-alkoxy, and R2", R6 and R2 or R2 respectivdy are hydrogen. Compounds as defined above, wherein Y is C-R2^ and R2 R2, R2, R2" and R6 independently from each other are selected from the group consisting of hydrogen, halogen, lower-alkoxy and heteroaryl, are also preferred. Even more preferred are compounds as defined above, wherein Y is C-R2\ R2 is halogen, R2 is hydrogen, R1 is lower-alkoxy, heteroaryl or heteroarjd-lower-alkoxy, R2° is hydrogen and R2' is hydrogen or halogen. Most preferred are those compounds as defined above, wherein Y is C-R , R is fluorine, R8 is hydrogen, R is methoxy, pyridin-3-yI, 5-amino-pyridin-2-yi, 6-amino-pyridin-3-yl, pyTidin-2-ylmethoxy, or 2-amino-pyrimidin-5-yI, R1° is hydrogen and R is hydrogen or fluorine. In particular, preferred compounds are the compounds of formula (I) described in the examples as individual compounds as well as pharmaceutically acceptable salts thereof. Preferred compounds of formula (I) are those selected from the group consisting of (S)-N-(4-Carbaroiniidoyl-benzyl)-2-methoxy-2-phenyl-acetamide hydrochloride, {R)-N-(4-Carbamimidoyl-benzj^)-2-methoxy-2-phenyI-acetamide hydrochloride, (RS)-2- (4-Ben2yloxy-phenyi)-N-(4-carbamimido)4-benzyl)-2-methoxy- acetamide hydrochloride, (RS) -N-{4-Carbamimido)d-benzyl) -2-methoxy-2-(4-phenoxy-phenyl) -acetamide hydrochloride, {RS) -N- (4-Carbamimidoyl-benzyI)-2-methoxy-2-(3-phenoxy-phenyl)-acetaniide hydrochloride, (RS)-N-(4-Carbamimidoyl-benzyl)-2-ethoxy-2-phenyl-acetamide hydrochloride, (RS) -N- {4-Carbanumido)^-ben2yi) -2-(2-fluoro-phenyI)-2-methoxy- acetamide hydrochloride. (RS)-2-(S-Benzyloxy-phenyi)-N-(4-carbammiidoyI-benzyl}-2-inethoxy-acetar[iide hydrochloride, (RS) -N- (4-Carbamimido)d-benzj'l) -2- (S-hydroxy-phen)^) -2-methoxy-acetaiiiide hydrochloride, (RS) -N- (4-Carbamimido)4-benzyl) -2-methoxy-2-(3-mtxo-phen}d)-acetamide hydrochloride, (RS)-2-Biphenyi-4-yi-N-(4-carbamimidoyl-benzjd)-2-inethoxy-acetainide hydrochloride, (RS)-2-Benzo[l,3]dioxoI-5-yl-N-(4-carbaniiniidoyl-ben2yl)-2-methoxy-acetainide hydrochloride, (RS)-2-Benzo[13]dioxol-5-yl-N-{4-carbairiimidoyi-beiizyi)-2-ethoxy-acetarnide hydrochloride, (RS)-N-{4-Carbainiinido)4-ben2yl) -2 - [5-ethoxy-2-fluoro-3- (1 -methyi-piperidin-4-yioxy)- phenyl]-2-methosy-acetainide hydrochloride, (RS)-N-(4-CarbamirnidoyI-benzyI)-2-{2-fluorO'4-methoxy-pheii)d)-2-methoxy-acetaimde hydrochloride, (RS)-[Amino-(4-{[2-{2-fluoro-4-methoxy-phenyi}-2-methoxy-acet)dammo]-methyl}- phenyl)-methylenej-carbarDic acid ethyl ester, {RS)-2-(2-Huoro-4-methoxy-phenyl)-N-[4-(N-hydroxycarbainimidoyi)-benzyl]-2- methoxy-acetamide, RS)-2-(2-nuoro-4-metboxy-phenyl)-N- [4^(N-aminocarbamimidoyl)-benzyll -2-inethoxy- acetamide, (RS)-{5-[(4-Carbarniniidoyl-faeiiz}icarbarnoyl)-methory-inethyll-2-methoxy-pheiioxy}- acetic acid methyl ester hydrochloride, (RS)-N-(4-Carbamiinidoyi-benzyl)-2-{3-carbamoylmethoxy-4-roethoxy-phen)d)-2- methoxy-acetamide hydrochloride, (RS)-{5-[(4-Carbamiinidoyl-benzylcarbamoyl)-ethoxy-meth)d]-2-methoxy-phenoxy}- acetic add c\hyl ester hydrochloride, (RS)-N- (4-Carbaniimidoyl-benzyl) -2-{ 3-carbainoyimethoxy-4-methoxy-phenyl) -2- elhoxy-acetamide hydrochloride, (RS)-{5-[(4-Carbanii[mdoyI-benzy]carbamoyl)-ethoxy-methyl]-2-methoxy-phenoxy}- acetic acid, (RS)-N-(4-CarbainimidoyI'benzyi)-2-etho3cy-2-{4-ethoxy-phenyi)-acetaniid hydrochloride, (RS)-N-(4-Carbamimidoyl-benZ)d)-2-methoxy-2-[4-(l-methyl-piperidin-4-yIoxy)- phenylj-acetamide hydrochloride, (RS)-N-(4-Carbaraiinidoyl-benzjd)-3,3,3-trifluoro-2-metboxy-2-phenyi-propionainide hydrochloride, (RS)-N-(4-Carbaminiidoyl-benzyl)-2-{2-fluoro-4,5-dimethoxy-phenyi)-2-methoxy- acetamide hydrochloride, (RS)-N- (4-Carbaniiiiiidoyl-benz)'l) -2-{3-isopropox7-phenyl)-2 -methoxy-acetamide hydrochloride, (RS)-N- (4-Carbainimidoyi-benzyl) -2- (4-cyclopentyloxy-pheny3)-2-methoxy- acetamide hydrochloride, (RS)-N-(4-Caibamiinidoyl-benzyl) -2-(4-isopropoxy-phenj^) -2 -methoxy-acetamide hydrochloride, (RS)-i4-[(4-Carbainiinidoyi-ben2yicarbainoyl)-methoxy-niethyl]-phenoxy}-aceticadd meth)^ ester hydrochloride, (RS)-{4-E(4-Carbamimidoyl-beii2ylcarbamoyl)-metiioxy-inetiiyl]-phenoxy}-aceticacid, (RS)-N-(4-Carbaiiiimidoyl-benzyl)-2-methoxy-2-[3-(tetrahydro-pyran-4->doxy)-phenyl]- acetamide hydrochloride, (RS) -N- (4-Carbainiimdoyl-benzyl}-2- (3,5-diethoxy-2-fluoro-phenyl)-2-niethoxy- acetamide hydiocbioride, {RS)-N-(4-Carbaniiinidoyi-ben2yl)-2-[5-ethoxy-2-fluoro-4-(2-hydroxy-ethoxy)-phenyl]- 2-methoxy-acetamide hydrochloride, (RS}-N- (4-Carbainimidoyl-benzyl) -2- (3,4-diethoxy-2-fluoro-phenyl) -2-methoxy- acetamide hydrochloride, (RS) -N- (4-Cari)ainiimdoyl-2-fluoro-benzyl)-2- (2-fluoro-4-methoxy-phenyl)-2-methoxy- acetamide hydrochloride, (RS)-N-{4-Carbamiinido)d-3-fiuoro-benz)d)-2-{2-fluoro-4-methoxy-phenyi)-2-methoxy- acetamide hydrochloride, (RS)-2-(2,4-Bis-trifluoromethyl-phenyl)-N'(4-carbamiiuidoyI-benzjd)-2-methoxy- aceUmide hydrochloride, (RS)-N-[4-(N-Hydroxycarbainimido)d)-ben2yl]-2-(2-hydroxy-4-inethoxy-phenyl)-2- methoxy-acetamide, (RS)-N- (4-Carbaiiiiimdoyl-ben2yl) -2- (2-hydroxy-4-metJioxy-phen)i)-2-medioxy- acetamide actetate, (RS)-N-{4-Carbamimidoyl-ben2yl) -2- (2-fiuoro-5-niethoxy-phenyl) -2-methoxy-acetamide hydrochloride, (R.S)-N-(4-Carbaminiido)d-benzyl)-2-(2,3-difluoro-phenyl)-2-methoxy-acetamide hydrochloride, (RS)-N-(4-Carbaimniidoyl-benzyl)-2-(2,6-difiuoro-phenyl)-2-methoxy-acetaniide hydrochloride, (RS) -2- (4-Bromo-2-fluoro-phenyl) -N-(4-carbamiinidoyi-benzyl) -2-methoxy-acetamide hydrochloride, (RS)-2-(4-Bromo-2-fluoro-phenyl)-N-(4-carbarminidoj4-benz)d)-2-ethoxy-acetamide hydrochloride. (RS)-2- (4-Bromo-2-fluoro-phenyl) -N- (4-carbamiimdoyi-benzyI)~2-propoxy-acetaniide hydrochloride, (RS)-N- {4-CarbarDimidoyl-benzyI)-2- (2-fluoro-4-trifluoromethyl-phenyi) -2-methoxy-acetamide hydrochloride, (IlS)-]SI-(4'Carbamiinidoyl-benz)d)-2-[4-{2-hydroxy-ethoxy)-phenyI]-2-methoxy-acetamide hydrochloride, (RS )-N-{4-Carbamimidoyl-benzyl) -2 - (4-diinethyIainino-phenyl)-2-methoxy-acetainLde hxdrochloride, (RS) -N- (4-Carbamiimdoyl-benzyI) -2-methoxy'2- (3 -oxo-3,4-dihydro-2H- benzo[l,4]oxa2in-6-yI)-acetamide hydrochloride, (RS)-N- (4-Carbamimidoyl-benzyi)-2 -methoxy-2- (4-pyiTolidin-1 -yl-phenyl)-acetainide hydrochloride, (RS) -N-(4-Carbainiinidoyl-benzyl)-2- (2-chIoro-phenyl)-2-methoxy-acetaniide hydrochloride, (RS)-2--(4-Acetylamino-phenyl)-N-(4-carbamimidoyI-benzyI}-2-rnethoxy-acetainide hydrochloride, (RS )-N' (4-Carbaniiinidoyl-benzj^)-2-mefhoxy-2-(4-trifluoromethoiy-pheiiyl)-acetainide hydrochloride, (RS)-N-(4-Carbamimidoyl-benz)^)-2-(4-imidazol-1 -yl-phenyl)-2-methoxy-acetainide hydrochloride, (RS)-N-(4-Carbamiinidoyi-benzyI)-2-methoxy-2-(6--methoxy-naphthalen-2-yl)-acetaniide hydrochloride, (RS)-N-(4-Carbamiinidoyl-benzyi)-2-methoxy-2-(4-morphoiin-4-yl-phenyl)-acetamide hydrochloride, (RS) -N-(4-Carbamiinidoyl-benzyl)-2-methoxy-2-(2-morpholiii-4-yl-phenyI)-acetamide hydrochloride, (RS)-N-(4-Carbainimidoyl-benzyI)-2-[4-(3-dimethylaniiBo-propoxy)-phenyl]-2- methoxy-acetamide hydrochloride, {R5)-N-(4-Carbainiinidoyl-beii2yl)-2-(4'-dinieth)^amiiio--3--fluoro-biphenyi-4-yi)-2- methoxy-acetamide hydrochloride, (RS)-N-(4-CarbamiimdoyI-beii2yl)-2-(3-£Iuoro-4'-methoxy-biphenyl-4-yi)-2-methoxy- acetamide hydrochloride, (RS) -N-(4-Carbamimidoyl-benzyl)-2 - (3-fluoro-2'-metho3cy-biphenyI-4-yi)-2-methoxy- acetamide hydrochloride, (RS)-N-(4-Carbammiidoyl-benz)4) -2-(3-fluoro-biphen}d-4-^) -2-methoxy-acetamide hydrochloride, (RS) -N-{4-CarbainimidoyI-beiizyl}-2- (3-fluoro-3 '-methoxy-biphenyl-4-yI) -2-raethoxy- acetamide hydrochloride, I (RS )-N-(4-CarbamimidoyI-ben2yi)-2-(2,2-diinethyI-ciiromaii-6-yl)-2-methoxy-acetamide hydrochloride, (RS)-N-{4-CarbamiinidoyI-beiizyl)-2-ethoxy-2-(2-fiuoro-4-methoxy-pheii)^)-acetamide hydrochloride, {RS)-2-Ethoxy-2-(2-fluoro-4-methoxy-plienyl)-N-[4-(N--hydroxycarbamimidoyl)-benzyl] -acetamide, (RS)-4-[3-(3-Cyclopent>doxy-4-inethoxy-phenyl)-3-methoxy-2-oxo-prop^ainino]-benzamidine hydrochloride, {RS)-N-(4-CarbaiiiiimdoyI-benzyI}-2-C2-chloro-4-methoxy-phenyl)-2-methoxy-acetainide hydrochloride, (RS) -N- (4-Carbainimido)d-benzyl)-2-(2,6-difluoro-4-met±ioxy-phenyl)-2-methoxy- acetamide hydrochloride, (RS) -N- (4-CarbainimidoyI-benzyI )-2- (2'fluoro-4-methoxy-phen)^) -2-propoxy-acetamide hydrochloride, (RS)-N-(4-Carbaniimidoyl-benzy!)-2-methoxy-2-naphthaleii-l-yl-propionamide hydrochloride, (RS) -2- (4-Bromo- 2,6-difluoro-phen.yl) -N- (4-carbamimidoyl-ben2yl)-2-iuethQxy- acetamide hydrochloride, (RS)-N[-(4-Carbamiinido^-benzyl)-2-(2-fluoro-4-isopropoxy-phenyl)-2-metho}!y- acetamide hydrochloride, (RS)-N-(4^Carbamimidoyl-ben2yl) - 2-(2-fiuoro-4-isobu.toxy-pbenyl)-2-methoxy- acetamide hydrochloride, (RS)-N-(4-Carbainiimdoyl-beiizyl)-2-{2-fluoio-4-[2-(4-fluoro-phenyl)-ethoxy]-phenyl}- 2-methoxy-acetaniide hydrochloride, (RS) -N-(4-CaTbamimidoyl-ben2yl)-2- (2-fluDTD-4-pyridiii-3-^-phenyl)-2-mellioxy- acetamide hydrochloride, (RS) 'N-(4-Carbamiinido)^-benz)^) -2-(2-fluoro-4-pyridin-4-yl-piienyl)-2-metlioxy- acetamide hydrochloride, (RS)-2-(5-Bromo-2-fluoro-phenyl)-N-(4-carbamimido)d-ben2yl)--2-ineihoxy-acetamide hydrochloride, (RS)-N-(4-Carbamiinidoyi'ben2yl)-2-(4-fluoro-biphenyl-3-yi)-2-methoxy-3cetainide hydrochloride, (RS)-N-(4-Carbainiinidoyi'benzyl)-2-(2-fluoro-5-methyl-phenyi)-2-methoxy'acetaimde hydrochloride, (RS)-N- (4-Carbanumidoyi'ben2yl) -2 -(2-fluoro-5-trifiuoromethyl-phenyl)-2-metiioxy- acetamide hydrochloride, (RS)-N-(4-Carbamimidojd-benzyl)-2 - (2-fluoro-6-methoxy-phenyi) -2-methoxy-acetamide hydrochloride. CRS}-N-(4-Carbaminiidoyl-benzyi)-2 - (2-fluoro-6-liydroxy-phenyl)-2 -methoxy-acetamide hydrochloride, {RS)-N-(4-Carbaimmidoyl-benzyI)-2-diinethylainino-2-phenyI-acetamide hydrochloride, (RS)-N-(4-Carbaniimidoyl-beiizyi)-2-methyiamino-2-phenyl-acetamide hydrochloride, (RS)-N-(4-Carbamiimdo}d-ben2fl)-2-methylsulfanyl~2-phenyl-acetamide hydrochloride, (RS)-N-(4-Carbarnimidoyl-beiizyi)-2-ethyIsulfenyl-2-phenyl-acetainide hydrochloride, [RS)-N-(4-Carbamiinido)d-benzyl)-2-melhanesiilfonyl-2-phenyl-acetainide hydrochloride, (RS)-2-Amino-N-(4-carbaiminidoyl-benzyl)-2-phenyl-acetaniidehydiochIoride, (RS}-2-Acet7lamino-N-(4-carbainiinidoyl-ben27l)-2-phenyl-acetamide hydrochloride, (RS)-N-(4-Carbamiimdoyl-benzyl)-2-[2-fluoro-4-(2-phenoxy-ethoxy)-phenyll-2- methoxy-acetamide hydrochloride, (RS)-N-(4-Carbamimido>^-benz)d)-2-methoxy-2-pyridiii-2-jd-acetamide hydrochloride, (RS)-N-(4-Carbaminiidoyl-benzyl)-2-niethoxy-2-phenyl-propionaiiiide hydrochloride, (RS)-2-(4-Broiiio-2,6-difluoro-phenyl)-N-(4-carbaimniidoyi-benzyl)-2-ethoxy-acetamide hydrochloride, N-(4-CarbainiinidoyI-benzyl)-2-[2-fluoro-6-(2-hydroxy-ethoxy}-phenyl]-2-methoxy- acetamide hydrodiloride, and N-(4-Carbanuimdoyl-benzyi)-2-(2-carbamoylmethoxy-6-fluoro-pheDyl)-2-methoxy- acetamide hydrochloride, and pharmaceutically acceptable salts thereof. Other preferred compounds of formula (I) are those selected from the group consisting of (RS)-2-Biphenyi-4-)d-N-(4-carbamimidoyl-benzyl)-2-ethoxy-propionanude hydrochloride, (RS)-2-[3-(l-Benzenesulfonyl-piperidm-4-yloxy)-5-ethoxy-2-fluoTO-pfaenyl]-N-(4- carbamimidoyl-benzyl)-2-methoxy-acetainide hydrochloride, (RS)-N-(4-Garbamimidoyl-ben2yl)-2- [ 5-ethosy'2-fluoro-3-(l-metfaanesulfonyl-piperidin-4-)^oiy)-phenyl] -2-methoxy-acetamide hydrochloride, (RS)-2-[3-Cl-Acetyl-piperidin-4-)^oxy)-5-ethoxy-2-fluoro-phenyl]-N-(4-carbamimidoyi- benz)d)-2-methoxy-acetamide hydrochloride, (RS)-2-[3-(l-Benzoyi-piperidin-4-yloxy)-5-ethoxy-2-fluoro-phenyl]-N-(4- carbaminiidoyl-benzyl)-2-methoxy-acetamide hydrochloride, (RS)-N-(4-Carbamimidoyl-2-chloro-ben2yl)-2-{2-fluoro-4-methoxy-phenyi)-2-inethoxy' acetamide hydrochloride, (RS) -N-(4-CarbaminiidoyI-2-chIoro-ben2yl)-2 -ethoxy-2- (2-fluoro-4-methoxy-phen)i)- acetamide hydrochloride. (RS)'N-(4-CarbamiinidoyI-2-chloro-benzyl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-etiaoxy-acetamide hydrodiloride, {RS )-N- (4-CarbamimidoyI-2-chloro-benzyI) -2 -{2,6-diguoro-4-methoxy-phenyl) -2-methoxy-acetamide hydrochloride, (RS)-N-[3-Chloro-4-(N-hydroxycaibamimidoyl)-benzyl]-2-ethoxy-2-(2-fiuoro-4-methoxy-phenyl) -acetamide, (RS)-N-(4-Carbamiinidoyl-3-chloro-berizyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl) -acetamide acetate, (RS)-2 - (4-Bromo-2,6-difluoro-phenyl)-N- C4-carbamiinidoyl-2-methoxy-benzyi)-2- ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbaniimidoyl-2-methoxy-beiizyl)-2-e&oxy-2-(2-fluoro-4-methoxy-phenyi}- acetamide hydrochloride, (RS )-N- (4-CarbamirmdoyI-2-phenoxy-benzyI) -2-ethoxy-2-(2-fluoro-4-methoxy-phen)d) - acetamide hydrochloride, (RS)-N-(4-Carbamunidoy]-2-o-tolyIoxy-benzyl)-2-ethoxy-2-(2-fluoro-4-methoxy- phenji)-acetamide hydrochloride, {RS)-N-[4-Carbainiinidoyl-2-{4-fiuoro-phenoxy)-beiizyi]-2-ethoxy-2-{2-fluoro-4- methoxy-phenyl)-acetamide hydrochloride, (RS )-N- [4-Carbamimido}d-2-{pyridin-3-)doxy) -benzyl] -2-ethoxy-2- (2-fIuoro-4-methoxy- phenyl)-acetamide acetic add, (RS)-N-[4-Carbamimidoyl-2-(5-nitro-pyridin-2-yioxy)-benzyI]-2-ethoxy-2-(2-fluoro-4- methoxy-phenjd)-acetamide hydrochloride, (RS)-N-[2-(5-Amino-pyridin-2-yloxy)-4-carbamimidoyi-beii2)d]-2-ethoxy-2-(2-fluoro-4- methoxy-phenyI)-acetamide hydrochloride, (RS) -N-(5-Carbamimidoyl-biphenyl-2-ylmeth)d)-2-€thoxy-2- (2-fiuoro-4-methoxy- phen)4)-acetamide hydrochloride, (RS)-(5-Carbamimidoyl-2-{[2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetylamino]- methyl}-phenoxy)-acetic acid ethyl ester hydrochloride 1:1, (RS) -N- (4-Carbamimidoyl-2-carbamoyhnethoxy-ben2yl)-2-ethoxy-2-(2-fluoro-4- methoxy-phenyl)-acetamide hydrochloride 1:1, (RS}-N- (4-Carbamimidoyi-2-isopropoxy-benzyl) -2-ethoxy-2-(2-fluoro-4-methoxy- phenyl)-acetamide hydrochloride, (RS)-N-[4-Carbamimidoyl-2-(2-hydroxy-ethoxy)-beiizyl]-2-ethoxy-2-(2-fluoro-4- methoxy-phenyI)-acetainide hydrochloride, 2-{5-Carbamimidoyl-2-{[2-ethoxy-2-(2-fluoro-4-methoxy-phen)d)-acet>damino]-methyl}-phenoxy)-N-isopropyi-2-phenyl-acetamide hydrochloride, (RS)-(5-Carbamii]iido)d-2-{[2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetylamino]-methyl}-phenoKy)-acetic add. (IlS)-(S)-2-(5-Carbainiiiudoyi'2-{[2-ethoxy-2-(2-fluoro-4-meTiioxy-phenyl)-acetyiamino]-methyl }-phenoxy)-propionic acid ethyl ester hydrochloride, ((RS)-S)-2-C5-CarbaminiidoyI-2-{[2-ethoxy-2-(2-fluoro-4-methoxy-phenyI)-acet)'lamiiio]-methyi}-phenoxy)-propionaiiude hydrochloride, (RS)-{R)-2-(5-Carbamiinidoyl-2-[[2-ethoxy-2-(2-fluoTO-4-methoxy-phenyl)-acetylamino]-methyl}-phenoxy)-propiomc add ethyl ester hydrochloride, (RS)-(R)-2-(5-Carbamimidoyl-2-{[2-ethoxy-2-(2-fluoro-4-methoxj'-phenyl)-acetylamino] -methyl}-phenoxy)-propionamide hydrochloride, (RS)-N- (4-Carbainimidoyi-2-carbamoylmethoxy-benzyl)-2- (2-fluoro-4-Inethox)^-phenyI)-2-methoxy-acetaraidehyd^ochIoride, (RS)-N-(4-Carbainiinidoyl-2-phenoxy-beiizyi)-2- (2,6-difluoro-4-methoxy'pheii}^) -2-ethoxy-acetamide hydrochloride, (RS) -N- (4-Carbainiinidoyl-2-methoxy-ben2yl) -2- (2,6-difluoro-4-methoxy-phenyi) -2-ethoxy-acetamide hydrochloride, {RS)-N-{4-Carbamimidoyl-2-carbamoylmethoxy-benzyl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide hydrodiloride, (RS)-N-[4-Carbainiinidoyi-2-(2-fluoro-beiizyloxy)-benzyl]-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide hydrochloride, (RS)-N-[4-Carbamiiiiido)d-2-(5-chloro-2-fluoro-benz)4oxy)-benzyl]-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide hydrochloride, (RS}-N-{4-CarbamiimdoyI-2-[(2-methoxy-ethyicarbamoyl)-methoxy]-benzyi}-2-{2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetainide hydrochloride, (RS)-N-{ 4-Carbainimidoyl-2- [ (2-morpholin-4-yl-ethylcaibainoyl)-nietho3cy] -benzy!} -2-(2,6-difluoro-4-methoxy-pbenyI)-2-ethoxy-acetamide hydrochloride, (RS)-N-{4-Carbamimidoyl-2-[{2-diethyIainmo-ethylcarbainoyl)-metboxy]-ben2}i}-2-(2,6-difluoro-4-niethoxy-phenyi)-2-ethoxy-acetamide hydrochloride, (RS}-N-[4-Carbarmmidoyl-2-C[l,2,4]oxadiazol-3-ybnethoxy)-benzyl]-2-(2,6-difluoro-4- methoxy-phenyl}-2-ethoxy-acetarmde hydrochloride, (RS)-N-C4-Carbaniiinidoyl-2-carbamimido)dinethoxy-benzyl)-2-(2,6-difiuoro-4-methcixy-phenyl)-2-ethoxy-acetainidehydiochloride, (RS)-N-[2-{lH-Benzoiniida2ol-2-yhnethoxy)-4-carbamiimdoyl-benz)d]-2-(2,6-difluoro-4-niethoxy-phenyl}-2-ethoxy-acetamide hydrochloride, (RS)-N-[4-Carbamiimdoyl-2-((lS,3R,4S)-3,4-dihydroxy-cydopentyioxy)-beiizyl]-2-(2,6-difluoro-4-methosy-phenyl)-2-ethoxy-acetamide hydrochloride, amiitureof (RS) and (SR)-N-[4-Carbamimidoyl-2-((lRS,2RS)-2-hydroxy' cyclopentyloxy) -benzyl] -2- (2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetainide hydrochloride, (RS)-N-(4-Carbainiinidoyi-2-carbamoylmethoxy-benzyi)-2-(2,6-difiuoro-4-methoxy- pheiiyI)-2-methosy-acetamide hydrochloride, (RS)-N-(4-Carbaniimidoyl-2-methylcarbamoyImethoxy-beiizjd)-2-(2,6-difluoro-4- methosy-phenyl)-2-methoxy-acetainide hydrochloride, (RS)-N-[4-Carbamiinidoyl-2-(isopropylcarbanioyl-methoxy)-ben2yl]-2-(2,6-difluoro-4- methoxy-phenyI)-2-methoxy-acetainide hydrochloride, (RS)-N-{4-Carbaniimidoyl-2-[(4-fluoro-phenylcarbanioyI)-methoxy]-ben2yl}-2-(2,6- difluoro-4-methoxy-phenyl)-2-methoxy-acetaniide hydrochloride, (RS)-N-[4-Carbamimido)d-2-(pyridm-2-ylmethoxy)-beii2)d]-2-(2,6-difluoro-4-methoxy- phenyl)-2-rQethoxy-acetaimde hydrochloride, (RS)-N-[4-Carbaiminidoyl-2-(2,2J-trifluoro-ethoxy)-benz)i]-2-(2,6-(Muoro-4- methoxy-phenyi)-2-inethoxy-acetamide hydrochloride, (RS)-N- [4- Carbamiimdo)d-2 - (pyridin-3 -^methoxy)-benzyl] -2- (2,6-difluoro-4-methoxy- phenyl)-2-metiiojty-acetainide hydrochloride, (RS)-N-[4-Carbamin2idoyl-2-{pyridin-4-ylmethoxy)-benzyl]-2-(2,6-difluoro-4-methoxy- phenyl}-2-methoxy-acetamide hydrochloride, (RS) -N- (4-Carbamimidoyi-benz)d) -2-(2,6-difluoro-4-hydroxy-phenyl) -2-ethoxy- acetainide hydrochloride, (RS)-N-(4-Carbamimidoyi-benz)d)-2-[2,6-difluoro-4-C2-morpholm-4-yl-ethoxy)-phenyi]- 2-ethoxy-acetarmde dihydrochloride, (RS)-{[4-({2-[2,6-Difluoro-4-(2-morphoIin-4-)d-etiioxy)--phenyl]-2-ethoxy-acetylaimno}- metiiyl)-phenyl]-imino-methyl}-carbainic add benzyl ester> (RS)-N-{4-Carbainimidoyi-benz)d)-2- C2,6-difluoro-4-phenethyloxy-phenyi) -2-ethoxy- acetamide hydrochJoride, (RS)-N-(4-Carbainiiiiidoyi-benz)4)-2-(4-cydopTOp)dmethoxy-2,6-difluoro-pbenyl)-2- ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbaniiinidoyi-benzyl)-2-ethoxy-2-(4-ethoxy-2,6-difluoro-phenyl)-acetamide hydrochloride, (RS)-N-C4-Carbainimidoyl-ben2:>i)-2-[2,6-difluoro-4-(4-methoxy-phenoxy)-phenyl]-2- ethoxy-acetamide, (RS)-N-{4-CarbamiinidoyI-benzyl)-2-[4-(3,4-dimethoxy-phenoxy)-2,6-difluoro-pbenyl]- 2-ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbaminiidoyl-benz)i)-2-[2,6-difIuoro-4-{3-inethoxy-phenoxy)-phenyl]-2- ethory-acetamide hydrochloride, (RS)-2- [4-(3 -Acetylamino-phenoxy) -2,6-difluoro-phenyl] -N-(4-carbainimido)d-benzyl) - 2-etlioxy-acetamide hydrochloride, (RS)-N-{ 4-CarbainimidoyI-beiiz}d)-2 - [4-(4-cyano-phenoxy)-2,6-difluDro-phen)d]-2- ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbamiinido)d-beii2}d)-2- [2,6-difiuoro-4-( 3-trifliaoTomethoxy-plienoxy)- phenyl]-2-ethoxy-acetainideh7drochJoride, (RS)-(2,6-DifIuoro-4-trifluoromethanesulfonyloxy-phenyl)-ethosy-acetic acid ethyl ester, (RS)-4-(Ethoxy-ethQKycarbonyl-inethyl)-3,5-di£luoro-benzoicacid2-tiimeth.ylsUaiiyl-ethyl ester, (RS)-4-[(4-Carbamiinidoyi-benzylcarbamoyl)-ethoxy-metiiyl]-3,5-difluoTO-N-isobntyl- benzamide hydrochloride, (RS)-4-[(4-Carbamimido)^-benzylcarbaino)d)-ethoxy-me&yl]-N-ethyl-3,5-difluoro- benzamide hydrochloride, (RS)-4-[(4-Carbamimidoyl-benzylcarbamoyl)-ethoxy-methyl]-3,5-difluoro-N-(2- methoxy-ethyI)-beiizaiiude hydrochloride, (RS)-4- [ C4-Carbamiinidoyl-benzylcarbainoyl)-ethoxy-meth)d] -N-cyclopentyl-3,5- difluoro-benzamide hydrochloride, (RS)-4-[(4-CarbamiinidoyI-ben2ylcarbamoyl)-ethoxy-methyl]-3,5-difiuoro-N-(2,2,2- trifluoro-ethyl)-benzamide hydrochloride, (RS)-4-[(4-Carbainiimdoyl-benzylcarbamoyI)-ethoxy-methyl]-N-cyclopropylmethyi-3,5- difluoro-benzamide hydrochloride, (RS)-[(4-{[2-(2,6-Difluoro-3-hydrox)'-phenyl)-2-ethoxy-acetylainino]-meth}d}-phenyl)- imino-methyl]-carbamic acid benzyl ester, (RS)-N-(4-Carbaiiiiinido)d-benzyl)-2-(2,6-difluoro-3-hydroxy-phenyi)-2-ethoxy- aceUmide hydrochloride, (RS)-N-(4-CarbamiimdoyI-benzyl)-2-ethoxy-2-{3-[2-(2-ethoxy-ethoxy)-ethoxy]-2,6- difluoio-phenyl}-acetainide hydrochloride, (RS)-N-{4-Carbainiinidoyl-benzyi)-2-[3-(3-dimeth)darnino-propoxy)-2,6-dif[uoro- phenyl]-2-ethoxy-acetaniide dihydrochloride, (RS)-N-(4-Carb3niiniido)d-ben2yl)-2-(2,6-difluoro-3-{2-[2-(2-methoxy-ethoxy)-ethoxy]- ethoxy}-phenyl)-2-ethoxy-acet3mide hydrochloride, (RS)-N-(4-Carbaiiiimido)d-benzyl)-2-[2,6-difluoro-3-C3-pyridin-4-yI-propoxy)-phen>d]- 2-ethoxy-acetaniide dihydrochloride, (RS)-N-C4-Carbamiinido}4-benzyI)-2-[2,6-difluoro-3-(2-pyrroIidiii-1-yl-ethoxy)-phenyl]- 2-ethoxy-acetamide dihydrochloride, {RS)-N-(4-Carbaininiidoyl-benzyl)-2-[2,6-difluoro-3-(l-inethyI-cyclopropylmethoxy)- phen>d]~2-ethoxy-acetaniide hydrochloride, (RS)-N-{4-CarbamimidoyI-benzyl)-2-[2,6-dif[uoro-3-(2-piperidin'l-yl-ethoxy)-phenyl]- 2-ethoxy-acetaiiude dihydrochloride, (RS,RS)-N-C4-Carbamiinidoyl-ben2yl)-2-[3-(3-chloro-2-hydroxyinethyl-2-methyl- propoxy)-2,6-difiuoro-phenyi]-2-ethoxy-acetainide hydrochloride, (RS) -N-(4-Carbainirmdoyl-benzyl)-2-ethQxy-2-13- (2-ethoxy-ethoxy)-2,6-difluoro - phenyl]-acetamide hydrochloride. (RS)-N-(4-Carbamimidoyl-benzyl)-2-[2,6-di3uoro-3-(2-methoxf-ethoxy)-phenyl]-2- ethoxy-acetamide hydrochloride, (RS)-N-(4-Carfaaniiinidoyl-benzyi)-2-[3-(3-dimethylamino-2^-diinethyl-propoxy)-2,6- difIuoro-phenyl]-2-ethoxy-acetaroidedihydrochloride, (RS)-N-(4-Carbaniiniidoyl-ben2yl)-2-[2,6-difluoro-3-(2-thiophen-2-yl-ethoxy)-phenyi]- 2-eihoxy-acetamide hydrochloride, (IIS,RS)-N- (4-Carbamiinidoyl-benzyl) -2- [2,6- di&uoro-3- (tetrahydro-ftiran-2-ylinetiioxy) - phenyl]-2-ethosy-acetainide hydrochloride, (RS)-N- (4-CaTbamimidoyl-benzyi)-2- (2,6-difluoro-3-isobutoxy-phenyl)-2-etlioxy- acetamide hydrochloride, (RS,RS,RS)-N-{4-Carbainimidoyl-benzyl)-2-[2,6-difiuoro-3-(2-inethyl- cyclopropyhnethoxy)-phenyl] -2-ethoxy-acetainide hydrochloride, (RS)-N-{4-Carbamimidoyi-ben2yl)-2-[3-(2-cydopropyl-ethoxy)-2,6-difluoro-phenyl]-2- ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbainiinidoyl-ben2yl)-2-etiioxy-2-(3-ethoxy-2,6-difluoro-phen5d)-acetanude hydrochloride, (RS)-N-(4-Carbaminiidoyi-benzyl)-2-(2,6-difluoro-3-propoxy-phenyl)-2-ethoxy- acetamide hydrochloride, (RS)-N-(4-Carbamimidoyl-benz34}-2-(3-cycloprop)dmethoxy-2,6-difiuoro-phenyl)-2- ethoxy-acetamide hydrochloride, (RS) -N- (4-Carbainimido)d-ben2yl)-2- [ 3- (2-diniethyiamino-ethoxy)-2,6-difluoro-phenyl] - 2-ethoxy-acetarDide dihydrochloride, (RS)-N-(4-Carbainiinidoyl-benzyl)-2-{3-cydobut)dinethoxy-2,6-difluoro-phen)d)'2- ethoxy-acetamide hydrochloride, (RS)-N-(4-CarbamirQidoyl-ben2)d)-2-{2,6-difluoro-3-[2-(2-oxo-pyrrolidin-l-yl)-ethoxy]- phenyi}-2-ethoxy-acetainide hydrochloride, (RS)-N-(4-Carbamimido)^-benzyi}-2-[2,6-difluoro-3-(3,3,3-Qifiuoro-propoxy}-phenyl]- 2-ethoxy-acetainide hydrochloride, (RS)-N-(4-Caibamiimdo)d-benzyi)-2-[2,6-difluoro-3-(2-pyridm-3-yi-ethoxy)-phenyl]-2- ethoxy-acetamide dihydrochloride, (RS)-N-(4-CarbamimidoyI-benzyi)-2-(3-diethylcarbanioylmethoxy-2,6-difluoro-phenyl)- 2-ethoxy-acetainide hydrochloride, [RS)-N-(4-Carbamiimdoyl-benzyl)-2-[2,6-difluoro-3-(2-morpholJn-4-yl-ethoxy)-phenjd]- 2-edioxy-acetamide dihydrochloride, (RS,RS)-N-(4-Carbamiinidoyl-benzyl)-2-[2,6-difluoro-3-(l-methyl-piperidiji-3- ylmethoxy)-phenyl]-2-ethoxy-acetamide dihydrochloride, (RS JlS}-N-(4-CarbamimidoyI-benz)d)-2-[2,6-difluoro-3-{ 1-niethyl-piperidin-2- )dinethoxy)-phenyl]-2-ethoxy-acetainide dihydrochloride. CRS)-N-C4-Carbainimidoyi-benzyi)-2-[2,6-dJfluoro-3-(2-pyridin-2-yl-ethoxy')-phenyl]-2- ethoxf-acetamide dihydrochloride, {RSJlS)-N-C4-Carbaiminido)^-benzyI)-2-[2,6-difIuoro-3-(2-piperiain-2'yl-ethoxy)- phenyl]-2-ethoxy-acet3mide dihydrochloride, (RS)-N-(4-Carbaniiimdoyl-beiizyl)-2-(2,6-difluoro-3-methoxy-phenyl)-2-ethoxy- acetainide hydrochloride, (RS) -N- (4-Carbamimidoyl-ben2^)-2-(3-cydohexyloxy-Z,6-difluoro-phenyl) -2-etfaoxy- acetamide hydrochloride, (RS)-N-{4-Carbainimidoyl-benzyi)-2-[2,6-difluoro-3-(piperidin-4-yloxy)-phenyl]-2- ethoxy-acetamide dihydrochloride, (R,S) -N-(4-Carbaniiimdoyl-benzyl)-2 - [2,6-difiuoro-3-(4-fliioro-phenoxy)-phenyl] -2- ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbamiimdoyl-beii2yl)-2-[2,6-difluoro-3-(pyridin-3-')4oxy)-phenyll-2-ethoxy- acetamide dihydrochloride, (RS)-N-{4-Carbainimidoyl-benzyl)-2-[2,6-difluoro-3-{3-trifluoromethyl-phenoxy)- phenyl] -2-ethoxy-acetaniide hydrochloride, (RS) -N-(4-Carbamiinidoyl-beiiz)i) -2-(2,6-difluoro-3-m-tolyioxy-phenyl) -2-ethoxy- acetamide hydrochloride, (RS)-N-(4-Carbamiimdoyl-ben2yi)-2-ethQxy-2-[3-(3-ethoxy-phenoxy)-2,6-difluoro- phen)1]-acetamide hydrochloride, (RS)-N-(4-Carbainimidoyl-benzyl)-2-ethoxy-2-[3-{ l-ethyl-propoxy)-2,6-difluoro- phenyl]-acetamide acetate, (RS)-N-(4-Carbamimido^-benzyl)-2-(3-cydopentyloxy-2,6-dif[uoro-phen}^)-2-ethoxy- acetamide acetate, {RS)-N-(4-Carbainimidoyl-benzyi)-2-[2,6-difluoro-3-(tetrahydro-pyran-4-yioxy)- pIienyl]-2-ethoxy-acetamide acetate, (RS)-N-(4-Carbamimidoyl-beiiz)d)-2-(2,6-difiuoro-3-pyridin-2-)^-phen)d)-2-ethoKy' acetamide dihydrochloride, (RS)-N-(4-Carbamimido)i-beiiz^)-2-[2,6-difl.uoro-3-(6-methoxy-pyridin-3-yl)-pheti^]- 2-ethoxy-acetamide dihydrochloride, (RS)-N- (4-Carbamimidoyl-benzyI) -2- (2,6-difIuoro-5-pyridin-3-yl-phenyi)-2-ethoxy- aceUmide dihydrochloride, CRS)-N- (4-Carbamimidoyl-benzyi) -2 -{2,6-difluoro-3-pyrimidin-5-yl-phenyl)-2'ethoxy- acetamide dihydrochloride, (RS)-N-(4-Carbamiinidoyl-ben!yl)-2- (2,6-difiuoro- 3-pyridin-4-yI-phenyl)-2-ethoxy- acetamide dihydrochloride, (RS) -N-(4-Carbamimidoyl-benzyl) -2 -(2,4-difluoro-3'-methyl-biphenyl-3 -yl)-2-methox7- acetamide. (RS) -N- (4-Carbainimido}d-ben2yl)-2-( 2,4-difluoro-4'-methyi-biphenyl-3-)^}-2-methoxy- acetamide hydrochloride, (RS)-N-(4-Carbaininiido7l-beii2yl)-2-methoxy-2-(2,4,4'-trifluoro-bipiienyI-3-}d)- acetamide acetate, (RS) -N-(4-CaTbamiimdDyl-beiizyl) -2-(2,4-difluoro-4' -methylsulfanyi-biphenyl-3-yi) -2- methoxy-acetamide hydrochloride, CRS)-N-{4-Carbamiinidoyl-benzyl)-2-(2,4-difIuoro-3'-trifluoromethyl-biphenyI-3-yl)-2- methoxy-acetamide acetate, (RS) -N- (4-CarbamimidoyI-beiizyI) -2- (2,4-difluoro-4'-methoxy-biphen)d-3-yl) -2- methoxy-acetamide hydrochloride, (RS)-N-(4-Carbamiiiiidoyl-benzyi)-2-[2,6-difluoro-3-(morphohne-4-carbon)i)-phenjd]- 2-methoxy-acetamide acetate, (RS)-2-[2,6-difluoro-3-(morpholine-4-caibonyl)-phenyl j-N-[4-(N- hydrQxycarbamiinidQ^)-ben2yl] -2-methoxy-acetanude, CRS)-3- [ (4-Carb3niimidoyl-ben2ylcarbamoyl)-methoxy-methyl] -N-eth)4-2,4-difIuoro- benzamide acetate, (RS)-3-[(4-Carbamimido)i-beiizylcarbaino)^)-methoxy-methyl]-2,4-dif[uoro-N-(2- inethoxy-ethyI)-ben2aniide acetate, (RS)-3-[{4-Carbainiinidoyl-benzj^carbamoyi)-methoxy-meth)d]-N,N-diethyi-2,4- difluoro-benzajnide acetate, (RS)-3-[(4-CaTbainiinidoyl-benz^caibamoyl)-metiioxy-methyi]-2,4-difiuoTO~N-(2,2,2- trifluoro-ethyI)-benzamide acetate, (RS)-3-[(4-Carbamimido7i-ben2yicarbaino}d)-methoxy-methyl]-N-cyclopropyimethyl- 2,4-difluoro-benzainide acetate, (RS)-N- (4-Carbamimidojd-benz)^)-2- [2,6-difiuoro-3-(pyridin-2-yimethoxy) -phenyl] - 2- methoxy-acetamide dihydrochloride, (RS)-N-(4-Carbamimidoyl-benzyl)-2-[2,6-difluoro-3-(pyridm-3-)dmethoxy)-phen)d]-2- tnedioxy-acetamide dihydrochloride, (RS)-N-(4-Carbamiinidoyl-ben2yl)-2-[2,6-difluoro-3-(pyridin-4-ylmethoxy)-phenyi]-2- methoxy-acetamide dihydrochloride, (RS) -N- (4-Carbainimidoyl-benzyl) -2- [2,6-difluoro-3- (4-fluoro-phenoxy)-phenyi] -2- methoxy-acetamide acetate, (RS)-2-[2,6-difluoro-3-(4-fluoro-phenoxy)-phenyi]-N-[4-(N-hydroxycarbainiraidoyl)- beiiz)d] -2-methoxy-acetanude, (RS)-N-(4-Carbamimidoyi-benzyl)-2-[2,6-difluoro-3-(pyridin-3-yloxy)-plienyl]-2- methoxy-acetamide acetate, (RS}-N- (4-Carbaniimidoyl-beii2yl)-2- (3 ^-difluoro-biphen^-4-yl)-2-methoxy-acetamide hydrochloride. (RS) -N- (4-Carbamimidoyl-ben2yl)--2- (3,5-difluoro-biphenyi-4-yl)-2-ethox)'-acetamide hydrochloride, (RS)-N-(4-Carbamimidoyl-benzyl)-2-[2,6-difluoro-4-(lH-indol-5-yi)-phen)d]-2-ethoxy-acetamide acetic acid, (RS}-2~(2,6-Difluoro-4-furan-2-yl-phenyl)-2-ethoxy-N-[4-(N-hydroxycarbainimidoyl)-benzyl] -acetamide, (RS)-N-(4-Carbamimidoyi-benzyl)-2 - (2,6-difluoro-4-furan-2-yi-phenyl)-2-ethoxy-acetamide acetate, N-(4-Carbamimidoyl-benzyl)-2-[2,6-difluoro-4-(tetrahydro-furan-2-yI)-phen)d]-2-ethoxy-acetamide acetic acid, (RS)-J4'-[(4-Carbamimidoyl-ben2ylcarbamoyl)-ethoxy-methyl]-3',5'-difluoro-biphenyl-3-yloxy}-acetic add ethyl ester hydrochloride, (RS )-{4'- [ (4-Carbamimidoyl-benzylcarbamo}d) -etboxy-methyl] -3',5 '-difluoro-biphenyl-3-yloxf}-acetic add, (RS)-N-(4-Carb amiimdoyI-benz)4)-2-(3'-carbamoylmethoxy-3,5-difluoro-biphenyl-4-)i)-2-ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbainiinidoyl-benzyI)-2-[3,5-difluoro-3'-(2-hydroxy-ethoxy)-bipheiiyl~4-yl]-2-ethoxy-acetainide hydrochloride, (RS)-N-(4-Carbamiinido)d-ben2)d)-2-[3'-(3-dimethylaiiiino-propoxy)-3,5-difluoro-biphenyl-4-yl] -2-ethoxy-acetamide hydrochloride, (RS)-2-[2'-(2-Benzyloxy-ethoxy)-3,5-difluoro-biphenyl-4-)^l-N-(4-carbamimidoyl-benZ)^)-2-ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbamimidoyl-benz)d)-2-[2'-(2-dimethylamino-ethoxy)-3,5-difluoro-biphenyl-4-ylJ-2-ethoxy-acetamide hydrochloride, {RS )-N- (4-Carbainiinidoyi-ben2yI) -2- [3,5-difluoro-2'-(2-hydroxy-ethoxy)-biphenyl-4-yl] -2-ethoxy-acetamide hydrochloride, (RS)-{4'-[(4-Carbamimidoyl-benzyIcarbamoyl)-ethoxy-methyi]-3',5'-difluoro-bipheByl-2-)ioxy}-acetic add ethyi ester hydrochloride, (RS)-{4'-[(4-Carbamimidoyl-benzylcarbamoyl)-ethoxy-meth)d]-3',5'-difluoro-biphenyi-2-yloxy}-acetic add, (RS)-2-(2'-Carbamoylmethoxy-3,5-difiuoro-biphenyl-4-^)-2-ethoxy-N-[4-(N-hydroxycarbamiinido>d)-benzyl] -acetamide, (RS)-N-(4-CarbamimidoyI-benz>i)-2-(2'-carbamoylmethoxy-3,5-difluoro-biphen)d-4-yi)-2-ethoxy-acetamide acetate, (RS) -N-(4-Carbamimidoyl-benzyl)-2- (2,6-difluoro-4-pyridin-4-yl-phenyl) -2-ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbamimidoyl-benz)i) -2- (2,6-difluoro-4-pyrimidin-5-yl-phenyl) -2-ethoxy-acetamide hydrochloride. (RS)-N-(4-Carbamiimdoyi-benzy']J-2-(2,6-difluoro-4-pyriimdin-2-yl-plienyl}-2-ethoxy- acetamide hydrochloride, (RS)-N-(4-Carbamiinidoyl-benzyl)-2-(2,6-difluoro-4-pyridin-2-yl-phenyI)-2-ethoxy- acetamide hydrochloride, (liS}-2-[4-(2-Ammo-pjTimidin-5-yl}-2,6-difluoro-phenyl]-N-(4-carbamimidoyl-benzyI}- 2-ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbamiimdo>^-benzyl)-2-(2,6-difluoro-4-pyridin-3-yl-phenyi)-2-ethoxy- acetamide hydrochloride, iRS)-2- [4-(6-Amino-pyridm-2-yI)-2,6-dMuoro-phenf]] -N-(4-carbamimidoy]-beiizyI)-2- ethoxy-acetamide hydrochloride, (RS)-2-[4-(5-Amino-pyridin-2-yl)-2,6-difluoro-phenyl]-N-(4-carbamiinidoyl-benzyl)-2- ethoxy-acetamide hydrochloride, (RS) -4' -[ {4-CarbainiinidoyI-benzylcarbainoyl) -ethoxy-mefeyJ] -3 ',5' -difluoro-bipheiiyi-3- carboxyHc add methyl ester hydrochloride, (RS)-(2-[4-(6-Ammo-pyridin-3-yl)-2,6-difluoro-phen)i]-N-(4-carbainiinidoyl-benzyl)-2- ethoxy-acetamide hydrochloride, {RS)-4'-[(4-Carbarnimido)d-benzykarbanioyl)-ethoxy-iDethylJ-3'^'-difluoro-biphenyi-3- caiboxyUc add, (RS){Aimno-[4-({2-[4-(6-ainmo-pyridin-3-yl)-2,6-difluoro-phenyl]-2-ethoxy- acetylaiiuno}-meUiyl)-phenyl]-niethylenei-carbamic add ethyl ester, (RS)2-[4-(6-Amino-pyridin-3-yI)-2,6-difluoro-phenyl]-2-ethoxy-N-l4-(N- hydroxycarbaminiidoyl)-beiizyl] -acetamide, (RS)-N- (4-Carbamiiiiidoyl-benzyl)-2-(3,5-difluoro-2' -hydroxyinethyI-biphenyl-4-yl)-2- ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbainimido)d-benz)d)-2-(2'-chloromethyl-3,5-difluoro-biphenyl-4-yl)-2- ethoxy-acetamide, (RS)-2-[3,5-Difluoro-2'-(hydroxyiinino-inethyl)-biphenyl-4-yl]-2-ethoxy-N-[4-(N- hydroxycarbamiinido}4)-benzy[]-acetamide, (RS)-2-(2'-Aminomethyl-3,5-difluoro-biphenyl-4-yl)-N-{4-carbamiinidoyi-benzyl)-2- ethoxy-acetamide acetate, (RS)-N-(4-Carbamimido)4-benzyl)-2-(2-fluoro-4-methoxy-3-phenoxy-phenyl)-2- methoxy-acetamide hydrochloride, (RS) -N- (4-carbainiinidoyl-benzyi) -2- (2-ethynyl-6-fluoro-phenyl)-2-methoxy-acetamide hydrochiorideaccording, (RS) -N- (4-Carbainimidoyl-beiizyl) -2-(2-ethyl- 6-fluoro-phen)d)-2-methoxy-acetaraide hydrochloride, (RS)-N-(4-CarbaiiiiinidoyI-beii2yl}-2-[2-fluoro-6-(3-hydroxy-prop-l-ynyi)-phenyl]-2- methoxy-acetamide hydrochloride. (RS)-N-{4-Carbaminiidoyl-benzyl)-2-[2-f[uoro-6-(3-hydroxy-propyl)-pheO)^]-2-methoxy-acetamide hydrochloride, (RS) -N- (4-Carbamiinido)i-beBzyl) -2- (3-fluoro-biphenyI-2-yl)-2-methoxy-acetamide hydrochloride, i (RS)-2-(3'-Ainino-3-fIuoro-biphenyi-2-yI}-N-C4-carbainirmdoyl-benzyl)-2-methoxy-acetamide hydrochloride, (RS) - N-(4-CarbaininiidoyI-beii2yl) -2-{3- 9uoro-3 '-mtro-biphenyl-2-yl) -2-niethoxy-acetamide hydrochloride, (RS)-2-[2-{6-Ainino-pyridin-2-yl)-6-f[uorD-phen)d]-N-(4-caTbamiinidoyi-benzyi)-2-methoxy-acetamide acetate, (RS)-{2-[(4^Carbainimido}d-beiizylcarbamoyl)-methoxy-methyl]-3-fluoro-phenoxy}-acetic add meth)^ ester acetate, (RS)-{2-[(4-CarbamimidoyI-benzyIcarbamoyl}-methoxy-methyl]-3-fluoro-pbenoxy}-acetic add, (RS)-N-C4-Carbamimidoyi-benzyl)-2-[2-(3-dimediylainino-propoxy)-6-fluoro-phenyI]-2-methoxy-acetamide hydrochloride, {RS)-N- (4-Carbainiimdoyl-benzyl) -2- (2-fluoro-6-phenoxy-phenyl) -2-methoxy-acetainide hydrochloride, (RS)-N- (4-Carbaimiradoyl-beiizyl)-2-(2,6-difluoro-4-methoxy-phenyl) -2-ethoxy-acetamide hydrochloride, (RS)-2-{4-Beiizyloxy-2,6-difiuoro-phenyl)-N-(4-carbamiimdoyl-beiizyI)-2-ethoxy-acetamide hydrochloride 1:1, (RS)-N-C4-Carbainiiiiidoyl-benz)d)-2- (2,6-difluoro-4-isopropoxy-phen)d) -2-ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbainiimdoyl-ben2)d)-2-[2,6-difluoro-4-(pyridin-2-)iinethoxy)-phen)4]-2-ethoxy-acetamide hydrochloride, (RS)-2-[2,6-Difluoro-4-{pyridin-2-ylmethoxy)-phenyi]-2-ethoxy-N-[4-(N-hydroxycarbamimido^) -benzyl] -acetamide, (RS)-|Ainino-[4-({2-[2,6-difiuoro-4-(pyridin-2-yiinethoxy)-phen'jd]-2-etho3cy-acetylainino}-methyl)-phenyi]-methyleDe}-carbaimc add ethyl ester, (RS)-N-(4-CarbaininudoyI-benzyl)-2-[2,6-difluoro-4-(pyridin-3-ylmethoxy)-phenyl]-2-ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbanixinidoyl-benzyi)-2-[2,6-difluoro-4-(pyridin-4-ylmethoxy)-phenyl]-2-ethoxy-acetamide hydrochloride, (RS) -N- (4'CarbainimidoyI-benzyl)-2-(2,6-di£[uoro-4-phenoxy-phen)4)-2-ethoxy-acetamide hydrochloride, (RS)-N-(4'CarbaniiimdoyI-benzyl)-2-[2,6-difluoro-4-(pyridin-3-)doxy)-phenyl]-2-ethoxy-acetamide hydrochloride. (RS)-N-(4-Carbamimidoyl-beiizyl)-2-(2,6-difluoro-3-isopropoxy--phenyl)-2-ethoxy"- acetaraide hydrochloride, (RS)-N-(4-CarbainiinidoyI-ben2yl)-2-(3-carbamoyhnethoxy-2,6-difluoro-phenyl)-2- ethoxy-acetamide hydrochloride, (RS)-2-[3-(2-Benzyloxy-ethoxy)-2,6-difluoro-phenyl]-N-(4-carbamiinidoyl-benzy!)-2- ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbainiimdoyl-benzyl)-2-[2,6-difluoro-3-(2-hydroKy-ethoxy)-phenyl]-2- ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbamiinidoyi-benzyl)-2-(2,6-difluoro-3-phenoxy-phen)i)-2-etiioxy- acetamide acetate, (RS)-N-(4-Carbarminidoyl-benzyl)-2-(2,4-difiuoro-biphenyl-3-yl)-2-ethoxy-acetaniide hydrochloride, (RS)-2-(2,6-Difluoro-3-phenyIaimno-phenyl)-N-[4-(N-hydroxycarbainiimdoyl)-benzyl]- 2-methoxy-acetainide, (RS) -N- (4-Carbainimidoyl-benzyl) -2-(2,6-difluoro-3-phenyIaniino-phenyl)-2-methoxy- acetamide acetate, (RS)-N-(4-Carbaniimidoyl-beii27l)-2-(2,6-difluoro-3-isopropylamino-phenyI)-2- methoxy-acetamide acetate, (RS)-2-(3-AcetylamiTio-2,6-difluoro-phenyl)-N-(4-carbainiinido)4-beiizjd)-2-inethoxy- acetamide hydrochloride, (RS)-(4-Carbammiido)4-benzyl) -2-(2,6-difluoro-3-phenylacetylainino-pheiiyI) -2- methoxy-acetamide hydrochloride, (RS )-N- (4-Carbarminidoyl-beiizyl) -2- (2,6- difluoro-3-hydroxymethyl-phenyl}-2-ethox)'- acetamide hydrochloride, (RS)-2-[3-(Acet)dammo-methyl)-2,6-difluoro-phenyl]-N--(4~carbamiinidoyl-benzyl)-2- ethoxy-acetamide hydrochloride, (RS )-2- (3-Ammomethyl-2,6-difluoro-phenyl)-N- (4-carbaimimdoyI-benzyi) -2-ethoxy- acetamide acetic acid 1:4, (RS)-(4-Carbamiinidoyl-benzyl)-2-(2,6-difluoro-3-phenylairdnomethyl-pheii)d)-2-ethoxy- acetamide hydrochloride, (RS)-(4-Carbaimniidoyl-benz)i)-2-(2,6-difluoro-3-inorpholin-4-)dinethyl-phenyI)-2- ethoxy-acetamide hydrochloride, (RS)-(4-Carbamimidoyl-benz}d)-2-(2,6-difluoro-3-piperidin-1-ybiiethyl-phen)d)-2- ethoxy-acetamide hydrochloride, (RS) -2 -{3-Diethoxymethyl-2,6-dif[uoro-phenyl) -2-ethoxy-N- [4- (N- hydroxycarbaraimidojd)-benz)d] -acetamide, (RS)- (4-Caxbarmmidoyl-ben2yl) -2-(2,6-difluoro-3-formyl-phenyi)-2-ethoxy-acetamide acetic add (1:4), (RS)-N-(4-Carbamiinidoyl-2,6-difluoro-benzyl)-2-(2,6-difiuoro-4-methoxy-phen^)-2-ethoxy-acetamide; hydrochloride, (R.S)-N-(4-Carbamimidoyl-2,6-difluoro-beiizyI)-2-ethoxy-2-(2-fluoro-4-inethoxy-phenyl)-acetaimde acetate, (RS }-N- (4-Carbammudo)d-2,6-difiuoro-b enzyl)-2- (2,6- difluoro-4-methoxy-phenyl) -2-methoxy-acetamide acetate, (RS)-N-(4-Carbainimidoyl-2,6-difluoro-benzyl)-2-(2-fluoro-4-niethoxy-phen)d)-2-methoxy-acetamide acetate, (RS)-[4-Carbammiidoyl-2-(carbanioylmethyl-ainiiio)-benzyl]-2-ethoxy-2-( 2-fluoro-4-methoxy-phenyl) -acetamide hydrochloride, (RS) -N- (2-Benzylamino-4.carbainimidoyl-beiizyl}-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl}-acetamide acetate, (RS)-[4-Carbamiinido5d-2-(2-fluoro-benzylamino)-benzyl]-2-ethoxy-2-(2-fluoro-4-methoxy-phenyI}-acetainide hydrochloride, (RS)- {4-CarbamirnidoyI-2- [ (pyridin-2-yhnethyl) -amino] -benzyl}-2 -ethoxy-2- (2-fluoro-4-methoxy-phenyl)-acetamide hydrochloride, (RS)-[4-Carbamimidojd-2-(4-chloro-2-fluoro-benzylamino)-ben2)d]-2-ethoxy-2-(2-fiuoro-4-inethoxy-phenj4)-acetaimde hydrochloride, (RS)- (4-Carbamimidoyl-2-plienethylamino-beiiz:>d)-2-ethoxy-2-{ 2-fluoro-4-methoxy-phenyl)-acetamide hydrochloride, (RS)-(5-Carbamimidoyl-2-{[2-ethoxy-2-(2-fiuoro-4-methoxy-phen)d)-acet)damino]-methyl}-phenylamino)-acetic add eth}d ester hydrochloride, (RS)-(5-Carbamimidoyl-2-{[2-ethoxy-2-(2-fluoro-4-methoxy-phen)d)-acetylainino]-methyll-phenylamino)-acetic add acetate, (RS)-(4-Carbaminiidoyl-2-phenylmethanesulfonylainino-benzyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide hydrochloride, (RS)-[2-(3-Beiizyl-urddo)-4-carbaminiidoyl-benzyi]-2-ethoxy-2-(2-fluoro-4-methoxy-phenyi)-acetamide acetate, (RS)-(5-Carbamimidoyl-2-{[2-ethoxy-2-(2-fluoro-4-methoxy-phenyi)-acetylamino]-methyl}-phenyl)-carbamic add benzyl ester hydrochloride, (RS) -(4-Carbamimidoyl-2-phenylainino-benzyi) -2-ethoxy-2-(2-fiuoro-4-methoxy-pheny]}-acetamide hydrochloride, (RS)-2- [4- (6-Amino-pyridin-3-)d)-2,6-difluoro-phenyl] -N-(4-carbamimidoyl-2-carbamo)dmethoxy-benz:>d)-2-ethoxy-acetamidehydrochloride acetic add (1:1:2), (RS) - (4-Carbamimidoyl-2-carbamoyhnethoxy-benzyl) -2- [2,6-difluoro-4-(pyridin-2-yhnethoxy)-phenylj-2-ethoxy-acetamide hydrochloride, (RS)-2-[4-(6-Ainino-pyridin-3-yl)-2,6-difluoro-phenyi]-N-(4-carbarmrmdoyl-2,6-diiluoro-benzyi)-2-ethoxy-acetamide acetate. (RS)-[(4-{[2-{2,6-Difluoro-4-methoxy-phenyl)-2-methoxy-acetylamino]-methyl}-phenyl)-imino-methyi]-carbainic acid tert-butyl ester, (S)-[(4-{[2-(2,6-Difluoro-4'medioxy-phenyl)-2-niethoxy-acetylaiiimo]-methyl}-phenyl)-imino-methylj-carbamic add tert-butyl ester, (R)-[(4-{[2-(2,6-Difluoro-4-methoxy-phenyl}-2-methoxy-acetylaminoj-methyl}-phenyI)-imino-methyij-carbamic add tert-butyl ester, (S)-N- (4-Carbaiminidoyl-benzyl)-2 -(2,6-difluoro-4-methoxy-phenyi)-2-methoxy-acetaInide fortniate^ (R)-N-(4-CarbaniiinidoyI-beiizyi)-2-(2,6-difluoro-4-metboxy-phenyI)-2-raetiioxy-acetamide formiate, [l-Ainmo-l-(4-{[(R)-2-edioxy-2-(2-fiuoro-4-methoxy-phenyl)-acetylamino]-niethyl}-phenyI)-meth-(E)-)didene]-carbamic add benzyl ester, {R)-N-(4-CarbaiTiimidoyl-benzyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phen^)-acetamide acetate, (RS)-[Ammo-(4-{[2-ethoxy-2-(2-fluoro-4-methoxy-phen)d)-acetylamino]-methyl}-phenji)-methylene]-carbamic acid bemyl ester, (RS)-[(4-{[2-(2,6-Difluoro-4-inethoKy-phenyl)-2-methoxy-acetylammo]-methyl}-phenyl)-immo-methyl]-carbaniic add benzyl ester, (RS)-N-(4-Carbamimido^'benzyl)-2-[2,6-difluoro-4-(I-oxy-pyridm-4-yl)-pheny]]-2-methoxy-acetamide hydrochloride, (RS)-(4-Carbainiiiiidoyl-benz)d)-2-[2,6-di£luoro-4-(tetrafaydro-pyran-4-yl)-phenyl]-2-ethoxy-acetamide acetate, and (RS) - (4-Carbainimidoyl-benzyi) -2-(4-cydohex^-2,6-difluoro-phenyl)-2-ethoxy-acetamide acetate, and pharraaceutically acceptable salts thereof. Particularly preferred compounds of formula (I) are those selected from the group consisting of (S)-N-{4-CarbaiiiiinidoyI-ben2yl)-2-methoxy-2-phenyl-acetamide hydrochloride, {RS)-N-(4-Carbainiinidoyl-benzyl)-2-(2-fIuoro-4-methoxy-phen5d}-2-methosy-acetamide hydrochloride, (RS)-[Amino-(4-{[2-(2-fluoro-4-methoxy-phenyl)-2-methoxy-acetyiamino]-methyll-phenj^)-methylene]-carbamJc add ethyl ester, (RS)-2-(2-Fluoro-4-methoxy-phenyl)-N-[4-(N-hydroxycarbamimido)d)-benzyl]-2-methoxy-acetamide, (RS) -N-(4-Carbamimidoyi-benzyl)-2- (3-fIuoro-3 '-methoxy-biphenyl-4-}d)-2-methoxy-acetamide hydrochloride, (RS) -N- (4-Carbamimidoyl-benzyl) -2-ethoxy-2- (2-fluoro-4-methoxy-phenyI)-acetamide hydrochloride, (RS) -N-(4-Carbaininiidoyl-benzyl)-2 -(2,6-difl^^oTO-4-methc^X)'-pheIlyl)-2-^lethox7-acetaImde hydrochloride, (RS)-N- (4-CaTbarQiimdoyl-benzyl) -2-( 2-fluDro-4-pyridm-3-yl-phenyl)-2-methoxy-acetamide hydrochloride, and (RS)-2-(4-Bromo-2,6-difluoro-phenyl)-N-(4-carbainiimdoyl-benzyl)-2-ethox7'acetainide hydrochloride, and pharmaceutically acceptable salts thereof. Other particularly preferred compounds are those selected from the group consisting of (RS)-N-(4-Carbamimidoyl-2-carbamoylmethoxy-benzyl)-2-(2,6-difluoro-4-methoxy-phen^)-2-ethoxy-acetamide hydrochloride, (RS)-N-{4-Carbamimidoyl-2-[(2-methoxy-eth)dcarbamo)i)-methoxy]-benzyl}-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide hydrochloride, (RS)-N-[4-Carbainimidoyl-2-(pyridin-2-ylmethoxy)-benzyl]-2-(2,6-difluoro-4-methoxy-phen)4)-2-methox)'-acetainide hydrochloride, (RS)-2-[4-(2-Amino-pyriniidin-5-)d)-2,6-difluoro-phenyl]-N-(4-carbamimidoyl-benzyl}-2-ethoxy-acetaniide hydrochloride, (RS)-N- (4-Carbamimido)i-benzyl) -2-(2,6'difluoro-4-pyridm-3-)d-phen5d) -2-ethoxy-acetamide hydrochloride, (RS)-2-[4-(5-Amino-pyridin-2-yl)-2,6-difluoro-phen)d]-N-(4-carbamimidoyl-benzyl)-2-ethoxy-acetamide hydrochloride, (RS)-(2-[4-{6-Amino-pyridin-3-yl)-2,6-difiuoro-phenyl]-N-(4-carbamimidoyl-benzyl)-2-ethoxy-acetamide hydrochloride, (RS)-N-{4-Carbaininiidoyl-beiizyl}-2-[2,6-difluoro-4-(pyridin-2-yhnetho]cy)-phenyI]-2-ethoxy-acetamide hydrochloride, (RS)-N-(2-Beiizylanuno-4-carbamimidoyl-benzyl)-2-ethoxy-2-(2-fluDro-4-methoxy-phenyl)-acetamide acetate, (RS)-(5-Carbamimidoyl-2-{[2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetylamino]-meth)^}-phenjdamino)-acetic acid acetate, (RS)-(4-Carbaminiidoyi-2-carbamoylmethoxy-ben2yi)-2-[2,6-difluoro-4-(pyridiii-2-)dmethoxy)-phenyI]-2-ethoxy-aceta]aiide hydrochloride, (RS)-2-[4-C6-Amino-pyridin-3-yI)-2,6-difluoro-phenyl]-N-(4-carbaminudoyI-2,6-difluoro-ben2yi)-2-ethoxy-acetamide acetate, and (RS)-{4-Carbamimidoyl-2-[{pyridin-2-ylmethyI)-amino]-benzyl}-2-ethoxy-2-(2-fluoro-4-methox)'-phenyi)-acetamide hydrochloride, and pharmaceutically acceptable salts thereof. It will be appreciated that the compounds of general formula (I) in this invention maybe derivatised at ftmctional groups to provide derivatives virhich are capable of conversion back to the parent compound in vivo. The invention further relates to a process for the manufacture of conipounds of formula (I) as defined above, which process comprises converting the nitrile group in a compound of formula (H) wherein R2 R2 R2 R2 R2 R2 R2 R1, R2", X and Y have the significances given above, into a carbamimidoyl group, or into a N-hydroxy-caibamimidoyl group, or into a N-amino-carbamimidoyl group, and, if desired, converting an obtained compound of formula (I) into a phannaceutically acceptable salt. A preferred process as described above comprises the conversion of the nitrile group into a carbamamidoyl group, or into a N-hydroxy-carbamimidojd group, or into a N-amino-carbannmidoyl group. The conversion of the nitrile group in a compound of formula II into a carbamimidoyl group -C{NH)NH2 or into a N-hydroxy-carbamimidoyl group -C(NOH)NH2 or into a N-amino-carbamimidouyi group -C(N-NH2)NH2 can be carried out according to methods known per se. For example, the conversion into a N-hydroxy-carbamimidoyl group can be performed by dissolving a compound of formula n in a solvent, such as DMF, ethanol or methanol, treating the solution with hydroxylamine or a salt of hydroxylamine with an inorganic acid, such as hydroxylamine hydrochloride, and thereafter with a base, such as diisopropylethylamine or triethylamine, sodium hydride or sodium methanolate, conveniently at a temperature up to 80°C. The conversion of the nitrile group into a carbamimidoyl group can be carried out e.g. by treating a compound of formula II in a solvent, such as ethanol or methanol, or a solvent mixture, such as chloroform and methanol or chloroform and ethanol, with a dry stream of hydrogen chloride, conveniently at a temperature below 10 °C. The solution containing the iminoether can be evaporated and the residue can be treated with gaseous ammonia or an ammonium salt in methanol or ethanol. In an analogous manner, the iminoether can be converted into a N-hydroxy-carbamimidoyl compound of formula I with hydroxyiamine or a salt thereof in the presence of a base or into a N-amino-caibamimidoyl compound of formula I with hydrazine or a salt thereof in the presence of a base. In so doing, other reactive groups present in the compound of formula I and reactive towards the treatment wih hydrogen chloride or gaseous ammonia or ammonium chloride or hydroxyiamine or hydrazine can be modified. For example, in the case of treatment with hydrogen chloride a benzjdoxy group R6, R2, R2, R1, R2, R1, R1° or R6 can be converted into the hydroxy group. In the case of treatment with gaseous ammonia in methanol or ethanol a lower-alkoxy-carbonyl-lower-alkoxy group R2 R1, R6*, R2 R2 R2, R2° or R6 can be converted into a carbamo)d-lower-alkoxy group. If a carbamimidoyl compound of formula (I) is obtained from a nitrile of formula (U) by treatment with hydrogen chloride and subsequent reaction with gaseous ammonia or ammonium chloride, the carbamimidoyl product is obtained as hydrochloride salt. This salt can be converted into any other pharmaceutically acceptable salt by thromatography over an adequately charged basic ion exchange resin. Alternatively the hydrochloride salt of a carbamimidoyl compound of formula (I) can be converted into the corresponding free base by treatment with sodium ethanolate in ethanol and subsequently treated with an excess of an appropriate acid to generate any pharmaceutically acceptable salt. Any pharmaceutically acceptable salt of a carbamimidoyl compound of formula (I) can ftirthermore be obtained when a N-hydroxy-carbamimidoyl compound of formula (I) is hydrogenated in a solvent like ethanol, methanol, dioxan or THF, with hydrogen and a catalyst such as palladium, platinum or nickel in the presence of an appropriate acid. Functional groups in compounds of formula (I) can be modified. As modifications of functional groups in a compound of formula I there come into consideration especially the conversion of a N-hydroxy-carbamimidojd group into a carbamimidoyl group, the esterification of a carboxy group, the saponification of an ester group and the cleavage of an ether group, such as an arylalkyl ether group, e.g. the benzjd ether group. All of these reactions can be carried out according to methods known per se. A compound of formula (I) in which R1 represents a hydroxy group can be converted into a compound of formula (I) in which R2 represents hydrogen by hydrogenation in a solvent, such as ethanol, methanol, dioxane, THF or ^cial acetic add, or a solvent mixture, such as ethanol and glacial acetic add, with hydrogen and a catalyst, such as palladium, platinum or nickel. In so doing, other reactive groups present in the compound of formula I and reactive towards the reducing agent can be modified. A compound of formula (I) in which R2 represents benzyloxy-carbonyl can be converted into a compound of formula (I) in which R represents hydrogen by hydrogenation in a solvent, such as ethanol, methanol, dioxane, THF oi glacial acetic acid, or a solvent mixture, such as ethanol and glacial acetic acid, with hydrogen and a catalyst, such as palladiimi. The reaction can be optionally performed in the presence of an acid such as HCl in a solvent such as EtOH or MeOH. In so doing, other reactive groups present in the compound of formula I and reactive towards the reducing agent can be modified. A compound of formula (I) in which R2 represents lower-alkoxy-carbonyl or aryl-lower-alkoxy-caibonyl is obtdned by reacting a compound of formula (I) in which R2 represents hydrogen with a chlorofonnic add lower alkyl ester or a chloroformic acid aryl-lower-alkyl ester in a solvent, such as dichloromethane, dioxane or DMF, or a solvent mbcture, such as dichloromethane and water or ethyl acetate and water, in the presence of an organic base, such as pyridine or triethylamine, or an inorganic base, such as sodiimi hydroxide, sodium carbonate or potassium bicarbonate. A compound of formula (1) in which R2 represents benzyloxy-carbonyl and R6^.^ and R2 have the significance of hydrogen can be prepared according to general methods known per se, e,g. by coupling of an add of formula (III) and [{4-aminomethyI-phenyl)-imino-methyI]-carbaraic add. benzyl ester in the presence of coupling reagents as BOP or EDCI/HOBt and a organic base such as triethylamine or diisoprop)d ethyl amine in a solvent such as THF. A compound of formula (1) in which R1^ represents lower-alkyi-carbonyl or aryl-carbonyl is obtained by reacting a compound of formula (I) in which R1 represents hydrogen with a acyl chloride in a solvent, such as dichloromethane, dioxane or DMF, or a solvent mixture, such as dichloromethane and water or ethyl acete.te and water, in the presence of an organic base, such as pyridine or triethylamine, or an inorganic base, such as sodium hydroxide, sodium carbonate or potassium bicarbonate. A compound of formula (11) in which R2 R\ R8, R1, R2 R2 V}'^ or R2^ has the significance of a hydroxy group, or a compound of formula (I) in which R2 has the significance of benz>doxy-carbon)d and R2 R2Jl^, R2 R6, R1, R2" or R6 has the significance of a hydroxy group can be reacted: - with an alkylating agent such as an appropriately substituted alkyl bromide, alkyl iodide or alkyl mesylate in tib.e presence of a base such as potassium carbonate or caesium carbonate in a solvent such as DMF or acetone, or - with an alkene oxide in a solvent like EtOH, or - by a Mitsunobu reaction witli an appropriately substituted alcohol in the presence of DEAD, DIAD, or di-tert.-butyl-azodicarboxylate, and triphenjdphosphine or triphenylphosphine on sohd suppert in a solvent such as THF, dichloromethane or dioxane, or by an oxidative coupling with an ar>d boronic add or a heteroarylboronic add in the presence of a copper salt like Cu(0Ac)2, a base like pyridine or triethylamine and a solvent like dichloromethane or 1,2-dichloroethane, or with trifluorosulfonic add anhydride and an organic base Uke triettylamine or pyridine in a solvent such as THF or dichloromethane. A compound of formula (II) in which R2, R2Jl*, R2, R2 R2, R2° or R2^ has the significance of an aniline group or a compotmd of formula (I) in which R1 has the significance of benzyioxy-carbonyl and R6^, R2.R1*, R2, R2 R1, R1" or R6 has the significance of an aniline group can be reacted: - with an alkylating agent such as an appropriately substituted alkyl bromide, aUcyl iodide or alkyl mesylate in the presence of an organic base such as trieth^ amine or diisopropyl ethyi amine in a solvent such as DMF, or with an acyi or a sulfonyl chloride or a chloroformic add ester in the presence of an organic base such as triethyl amine OT diisopropyl ethyl amine in a solvent such as DMF, THF or acetonitrile, or - by reaction with isocyanate in a solvent such as dichloromethane or 1,2-dichloroethane, or - by oxidative coupling with an arylboronic add or a heteroaryi boronic add with a copper salt like Cu(0Ac)2, an organic base such as triethylamine or pyridine and an oxidant like TEMPO in a solvent like dichloromethane or 1,2-dichloroethane. A compound of formula (H) in which R2 R2 R8, R1, R2 R1, R2° or R6 has the significance of a bromide or of CF3-SO2-O-, or a compound of formula (I) in which R1 has the significance of benzyloxy-carbonjd and R2 R2,R8, R2, R2, R2, R2" or R6 has the significance of of a bromide or of CF3-SO2-O- can be reacted - with a aryl boronic add or a heteroaryi boronic add in the presence of a base such as sohd or aqueous potassium carbonate or sodium carbonate and a palladiimi catalyst such as tetrakis(triphen)4phosphin)palladium{0) or l,r-bis(diphenyi-phosphin) ferrocene-palladium dichloride in a solvent such as toluene or THF, or - with bis(pmacolato)diboron in the presence of a base sudi as potassium acetate and a palladium catalyst like bis(triphenylpliosphine)palladium(n) chloride and a solvent such as dioxane. The boronic acid ester thus obtained is fiirther converted by reaction with an arylhalogenide or a heteroaryl halogenide and a base such as sohd or aqueous potassium carbonate or sodium carbonate and a palladium catalyst such as bis(diphenylphosphin)ferrocene-paUadiuni dichloride in a solvent such as 1^-dimethoxyethane, or with carbon monoxide in the presence of a catalyst such as Pd(0Ac)2, a Ugand such as l,3-his-{diphenylphosphino)propane, an alcohol such as MeOH or 2-trimethylsilyl ethanol and a soiventsuch as DMSO, or ' with an appropriately substituted alkine in the presence of an organic base such as triethylamine and copper(I)iodide in a solvent such as DMF and a palladium catalyst such as tetrakis(triphen)4phosphin)palladiimi(0). A compound of formula {II) in which R2 R1,R8, R1, R2 R2, R1° or R6 has the s^ficance of a COOH group or a compound of formula (I) in which R has the significance of benzyloxy-carbonyl and R1, R2R2 R2 R2 R2 R2° or R6 has the significance of a COOH group can be reacted: in the presence of coupling reagents such as BOP or EDCI/HOBt and an organic base such as trieth)damine or diisopropyl ethyl amine in a solvent such as THF, DMF or dichloromethane. A compound of formula (11) in which R2, R2Jl^, R2 R8, R2, R2° or R2^ has the significance of a CHO group, or a compound of ftinnula (I) in which R2 has the significance of benzyloxy-carbonyl and R-, R2^\ R2 R2 R1, R2° or R2^ has the significance of a CHO group can be reacted: - by reduction with NaBH4 in EtOH, or by reductive amination with an amine in the presence of a reducing agent sudi as NaBH4 or NaBHsCN and a solvent such as EtOH, or - by reaction with hydroxylamine, hydrochloride in the presence of a base such as NaOAc and a solvent such as EtOH, and subsequent reduction of the intermediate oxime by Zn in HOAc. The aminomethyl derivative thus obtained can be reacted with an acyl chloride or a sulfonyl chloride in the presence of an organic base and a solvent such as THF, dichloromethane or DMF. The compounds of formula (II) in which X has the significance of an oxygen are prepared according to general methods known per se, e.g.by coupling of an acid of formula (III) and an appropriately substituted 4-aniinomethyl benzonitrile of formula (VI) in the presence of coupling reagents such as BOP or EDCI/HOBt and an organic base such as triethylamine or diisopropyl ethyl amine in a solvent such as THF. Compounds of formula (III) in which X has the significance of oxygen are known per se or can be prepared according to general methods known per se, e.g. as described hereinafter and/or as described in the Examples or in analogy to these methods. For example, a compound of formula (EI) in which X has the significance of oxygen and R2 has the significance of hydrogen can be prepared - by reaction of an aldehyde of formula (IV) with bromoform or chloroform in a mixture of solvents like dioxane/methanol or dioxane/ethanol in the presence of an inoi^anic base like sodiimi hydroxide or potassium hydroxide, or - by reaction of an aldehyde of formula (IV) with trimethylsilyl cyanide in the presence of Znl2 in a solvent such as dichloromethane. The trimetiiylsilyi cyanohydrine thus obtained is subsequently hydrolysed in concentrated hydrochloric acid to the corresponding a-hydroxy carboxylic add which is then alkylated to give a compound of formula (III) using an appropiately substituted alkyl halide in the presence of silver oxide in a solvent such as toluene. Compounds of formula (IV) are known per se or can be prepared according to general methods known per se, e.g. as described hereinafter and/or as ciescribed in the Examples or in analogy to these methods. Compounds of formula (III) can be prepared from compounds of fonnula (V) in which R2 and/or R6 have the significance of substituents which have an ortho-directing effect in a metallation reaction by reaction with a strong base like n-butyl lithium, IDA or lithium 2,2,6,6-tetramethyi piperidide, with ediyl glyoxalate as electrophile, witii N,N,N',N',N"-pentamethyldieth}dentriamine or N,N,N',N'-tetramethyiethylendiamine as additive and THF as solvent. The a-hydroxy phenyl acetic add ester thus obtained is reacted with an alkylatii^ agent such as eth)4 iodide or methyl iodide in the presence of silver oxide in toluene as solvent The G-aikoxy phenyl acetic acid ester is then hydrolysed by a base such as aqueous NaOH or LiOH in a solvent such as THF or EtOH- A compound of formula (III) in which X has the significance of oxygen and R has the significance of methyl can be prepared by reaction of an appropriately substituted acetophenone with bromoform or chloroform in a mixture of solvents like dioxane/methanol or dioxane/ethanol in the presence of an inorganic base like sodium hydroxide or potassium hydroxide. Compounds of formula (VI) can be prepared according to general methods known per se, e.g as described hereinafter and/or as described in the Examples or in analogy to these. For example, a substituted 4-aminomethyl benzonitrile of formula (VI) can be prepared from the correspondingly substituted 4^cyano-benzaldehyde by reaction with hydroxylamine hydrochloride in the presence of a base such as NaOAc in a solvent such as EtOH. Subsequently, the oxime thus obtained can be reduced by zinc in acetic acid. Alternatively, a substituted 4-aniinomethyi benzonitrile of formula (VI) can be prepared from the correspondingly substituted 4-bromoinethyl benzonitrile by reaction with hexamethylene tetramine (HMTA) in chloroform and subsequent hydrolysis of the HMTA adduct by concentrated aqueous hydrochloric add in EtOH. The compounds of formxila (II) in which X has the significance of an NR1^ and R1^ has the significance of lower-alfcyl are prepared according to general methods known per se> e.g. as described hereinafter and/or as described in the Examples or in analogy to these methods. For example, a compound of formula (VII) can be reacted with a lower-alkyl amine or a di-lower-alkjd amine or the corresponding anunonium hydrochlorides in the presence of an organic base such as triethylamine and a catalyst such as tetrabutylammonium iodide in a solvent such as THF. Compounds of formula (II) in w^ch X has the significance of NR12 and R1 has the significance of lower-alkjd-carbonyl can be obtained by coupling an appropriately substituted N-Boc-phenylglycine and an appropriately substituted 4-aminomethyl benzonitrile in the presence of coupling reagents such as BOP or EDCI/HOBt and an organic base such as triethyiamine or diisopropy] ethyl amine in a solvent such as THF. The Boc group can be cleaved by reaction with trifluoroacetic add in a solvent like dichloromethane. The amino group thus Kberated can then be reacted with an appropriately substituted acyl chloride or acyl anhydride in the presence of an organic amine like triethyiamine in a solvent lilce THF or dichloromethane. The compounds of formula (II) in which X has the significance of sulfin are prepared according to general methods known per se, e.g. as described hereinafter and/or as described in the Examples or in analogy to these methods. For example, a compound of formula (VII) can be reacted with the sodium salt of a lower-aUcyl mercaptane in the presence of a catalyst such as tetrabutylammoniimi iodide in a solvent such as methanol. Compounds of formula (11) in which X has the significance of SO2 can be obtained from compounds of formula (H) in which X has the significance of sulfiir by reaction with an oxidant such as m-chloro perbenzoic acid in a solvent like dichloromethane. Compounds of formula (VH) can be obtained by coupling an appropriately substituted a-bromo-phen)iacetic acid and an appropriately substituted 4~aniinomethyI benzonitrile in the presence of coupling reagents such as BOP or EDCI/HOBt and an organic base as triethyiamine or diisopropyl ethyl amine in a solvent such as THF. Insofer as their preparation is not described in the examples, the compounds of formulae (I), (II), (III), (IV), (V), (VI) and (VII) can be prepared according to analogous methods or according to die methods set forth above. Furthermore, the invention relates to compounds of formula (I) as defined above, when manufectured by a process as described above. In another embodiment, the invention relates to the intermediates, the compounds of formula (II) As described above, the compounds of formula (I) are active compounds and inhibit the formation of coagulation factors Xa, IXa and thrombin induced by fector Vila and tissue factor or are derivatives which are converted under physiological conditions to such active compounds. These compounds consequently influence both platelet aggregation which is induced by these factors and plasmatic blood coagulation. They therefore inhibit the formation of thrombi and can be used for the treatment and/or prevention of diseases, such as arterial and venous thrombosis, deep vein thrombosis, pulmonary embolism, unstable angina pectoris, cardiac inferction, stroke due to atrial fibrillation, inflammation and arteriosclerosis. Furthermore, these compounds have an effect on tumour cells and prevent metastases. They can therefore also be used as antitumour agents. Prevention and/or treatment thrombosis, particularly arterial or deep vein thrombosis, is tiie preferred indication. The invention therefore also relates to pharmaceutical compositions comprising a compound as defined above and a pharmaceutically acceptable carrier and/or adjuvant. The invention likewise embraces compounds as described above for use as therapeutically active substances, espedaliy as therapeutically active substances for the treatment and/or proph)daxis of diseases which are associated with the formation of clotting fectors Xa, IXa and thrombin induced by fector Vila and tissue fector, particularly as therapeutically active substances for the treatment and/or prophylaxis of arterial and venous thrombosis, deep vein thrombosis, pulmonary embolism, unstable angina pectoris, cardiac inferction, stroke due to atrial fibrillation, inflammation, arteriosclerosis and/or tumour. In another preferred embodiment, the invention relates to a method for the therapeutic and/or prophylactic treatment of diseases which are asscodated with the formation of dotting fectors Xa, IXa and thrombin induced by fector Vila and tissue fector, particularly for the therapeutic and/or prophylactic treatment of arterial and venous thrombosis, deep vein thrombosis, pulmonary embolism, unstable angina pectoris, cardiac inferction, stroke due to atrial fibrillation, inflammation, arteriosclerosis and/or tumour, which method comprises administering a compound as defined above to a human being or animal. The invention also embraces the use of compounds as defined above for tiie therapeutic and/or prophylactic treatment of diseases which are asscodated with the formation of clotting fectors Xa, IXa and thrombin induced by fector Vila and tissue fector, particularly for the therapeutic and/or prophylactic treatment of arterial and venous thrombosis, deep vein thrombosis, pulmonary embolism, unstable angina pectoris, cardiac inferction, stroke due to atrial fibrillation, inflammation, arteriosclerosis and/or tumour. The invention also relates to the use of compounds as described above for the preparation of medicaments for the therapeutic and/or proph)dactic treatment of diseases which are asscodated mdi the formation of dotting factors Xa, IXa and thrombin induced by factor Vila and tissue factor, particularly for the therapeutic and/or prophylactic treatment of arterial and venous thrombosis, deep vein thrombosis, pulmonary embolism, unstable angina pectoris, cardiac infarction, stroke due to atrial fibrillation, inflammation, arteriosclerosis and/or tmnour. Such medicaments comprise a compound as described above. Tlie inhibition of tie amidolytic acdvity of factor Vila/tissue fector complex by the compounds in accordance with the invention can be demonstrated with the aid of a chromogenic peptide substrate as described hereinafter. The measurements were carried out by an automated robotic assay on microtitre plates at room temperature. To this end, 100 pi. of a solution of 26 nM of tissue fector, 9 nM of soluble ^ctor Vila and 8 mhi of caldum chloride were added to 25 jil of a solution of the inhibitor in a buffer [pH 7.5, lOO mM, comprising O.UM NaCl, O.IM N-(2-hydroxyethyl)piperazine-N'-(2-elhanesulphomc acid) (HEPES), 0.5 mg/1 of fatty-acid-free BSA (bovine serum albumin} and 0.05% NaNj] in each well of the plate. After an incubation time of 15 minutes the reaction was started by the addition of 50 jU of chromogenic substrate Chromozym-tPA {3,5 mM, MeSOj-D-Phe-GIy-Ai^-paranitroaniHde) and the hydrolysis of the substrate was followed spectrophotometrically on a kinetic microtitre plate reader over 10 minutes. Using the plot of the inhibition curves, the Ki values were determined according to the method described in Biochem. J. 55, 1953, 170-171. The activity of the low molecular weight substances can, moreover, be characterized in the "prothrombin time" (FT) clotting test. The substances are prepared as a 10 mM solution in DMSO or DMSO/O.IM HQ (DHCl) and thereafter made up to the desbed dilution in the same solvent Thereafter, 0.25 ml of human plasma (obtained from whole blood anticoa^ulated with 1/10 volume of 108 mM Na dtrate) was placed in the instrument-specific sample container. In each case 5 ^ of each dilution of the substance-dilution series was then mixed with the plasma provided. This plasma/inhibitor mixture was incubated at 37°C for 2 minutes. Thereafter, there were pipetted to the semi-automatic device (ACL, Automated Coagulation Laboratory (Instrument Laboratory)) 50 ^il of plasma/ inhibitor mixture in the measurement container. The dotting reaction was initiated by the addition of 0.1 ml of Innovin® (recombinant human tissue factor combined with caldum buffer and synthetic phosphoHpids( Dade Behring®, Inc.). The time up to the fibrin cross-linking was determined photoopticaUy from the ACL. The inhibitor concentration, which brought about a doubling of the PT dotting time, was determined by means of a graph. The Ki value of the active compounds of the present invention preferably amounts to about O.OOI to 50 jiM.espedally about O.OOI Co I fxM. The PT values preferably amount to about 1 to 100 |iM, espedaliy to about 1 to 10 (AM. The compounds of formxJa I and/or their pharmaceutically acceptable salts can be used as medicaments, e.g. in the form of pharmaceutical preparations for enteral, parenteral or topical administration. They can be administered, for example, perorally, e.g. in the form of tablets, coated tablets, dragees, hard and soft gelatine capsules, solutions, emulsions or suspensions, rectaUy, e.g. in the form of suppositories, parenterally, e.g. in the form of injection solutions or suspensions or infusion solutions, or topically, e,g. in the form of ointments, creams or oils. Oral administration is preferred. The production of the pharmaceutical preparations can be effected in a manner which will be ^miliar to any person skilled in the art by bringing the described compounds of formula I and/or their pharmaceutically acceptable salts, optionally in combination with other therapeutically valuable substances, into a galenical administration form together with suitable, non-toxic, inert, therapeutically compatible solid or liquid carrier materials and, if desired, usual pharmaceutical adjuvants. Suitable carrier materials are not only inorganic carrier materials, but also organic carrier materials. Thus, for example, lactose, com starch or derivatives thereof, talc, stearic acid or its salts can be used as carrier materials for tablets, coated tablets, dragees and hard gelatine capsules. Suitable carrier materials for soft gelatine capsules are, for example, vegetable oils, waxes, fets and semi-solid and liquid polyols (depending on the nature of the active ingredient no carriers might, however, be required in the case of soft gelatine capsules). Suitable carrier materials for the production of solutions and syrups are, for example, water, polyols, sucrose, invert sugar and the like. Suitable carrier materials for injection solutions are, for example, water, alcohols, polyols, glycerol and vegetable oUs. Suitable carrier materials for suppositories are, for example, natural or hardened oils, waxes, fats and semi-liquid or liquid polyols. Suitable carrier materials for topical preparations are glycerides, semi-synthetic and synthetic glycerides, hydrogenated oils, hquid waxes, Hquid paraffins, liquid fatty alcohols, sterols, polyethylene glycols and cellulose derivatives. Usual stabilizers, preservatives, wetting and emulsifying agents, consistency-improving agents, flavour-improving agents, salts for varying the osmotic pressm-e, buffer substances, solubilizers, colorants and masking agents and antioxidants come into consideration as pharmaceutical adjuvants. The dosage of the compounds of formula I can vary within wide limits depending on die disease to be controlled, the age and the individual condition of the patient and the mode of administration, and will, of course, be fitted to the individual requirements in each particular case. For adult patients a daily dosage of about 1 to 1000 iR2, especially about 1 to 100 mg, comes into consideration. Dependii^ on severity of the disease and the precise pharmacokinetic profile the compound could be administered with one or several daily dosage units, eg. in J to 3 dosage units. The pharmaceutical preparations conveniently contain about 1-500 mg, preferably 1-100 mg, of a compound of formula I. The following Examples serve to illustrate the present invention in more detail. They are, however, not intended to limit its scope in any manner. Examples Abbreviations BOP = (benzotriazol-l-yloxy)-tris-(diinethylamino)-phosphomiiin-hexaflnorophosphat, CAS = Chemical Abstract Services, DEAD = diethyl azodicarboxylate, DMF = dimethyl formamide, EDCI = l-[3-(dimethylamiiio)propyl]-3-ethyicarbodiiinide hydrochloride, EtOH = ethanol, HOST = l-hydroxybenzotriazole, MS = mass spectroscopy, MeOH = methanol, r.L = room temperature, THF = tetrahydrofiiran General Procedures General Procedure A: Conversion of an aromatic aldehyde into an aryl-a-alkosyacetic acid. To a stirred solution of the aldehyde (1 eq) andbromoform (1.27 eq) in the appropriate alkohol (MeOH or EtOH, 1 ml/mmol aldehyde) and dioxane (1 ml/mmol aldehyde) is added dropwise a solution of potassium hydroxyde (5 eq) in the appropriate alkohol (MeOH or EtOH, I ml/mmol aldehyde) for 15 min. For larger amounts a slight cooling is appUed. Stirring at r.L under an argon atmosphere is then continued for 18 - 48 h. The sohd is filtered off and washed with the appropriate alkohol. The filtrate is concentrated (rotavapor). The residue is taken up in water. The resiilting solution is washed with Et20 and acidified to pH 1 by dropwise addition of 3.0 N HCl. This is extracted with BtiO, dried (MgS04), filtered and concentrated (rotavapor). The crude product can be purified by chromatography (silicagel) or by crystallization. General Procedure 6: Coupling of an aryl-a-alkoxyacetic acid widi a primary amine using EDCI as a coupling reagent To a stirred solution of the amine (1 eq) in THF is added the acid (1.2 eq), triethylamine (1.2 eq) and EDCI (1.2 eq). HOST (1.2 eq) can also be added. The mixture is then stirred at r.t. under an argon atmosphere for 16 - 24 h. The mixture is diluted with EtOAc, washed with sat KHSO4 solution / water (1:1) and water; dried (MgS04), filtered and concentrated. The crude product can be purified by chromatography (silicagel) or by crystallization. General Procedure C: Coupling of an aryl-a-alkoxyacetic acid with a primary amine using BOP as a coupiing recent To a stirred solution of die amine (1 eq) in THF is added the add (1.5 eq), N-diisopropylamine (1.5 eq) and BOP-reagent (1.5 eq). The mixture is then stiirred at r.t under an argon atmosphere for 16 - 24 h. The mixture is diluted with EtOAc, washed with water, 1.0 N NaOH and brine; dried (MgS04), filtered and concentrated. The crude produrt can be purified by chromatography (silicagel) or by crystallization. Cjenerai Procedure D: Conversion of an aromatic nitrile into an amidine (Pinner reaction). Dry HCl gas is passed over a cooled (-10°C), stirred solution of the starting material in CHCls / EtOH (or MeOH) 5:1 for 15 min. The flask is stoppered and left at 4 "C overnight If conversion is not complete, the reaction mixture is allowed to warm to r.t. The mixture is concentrated (rotavapor and high vacutmi) at r.L The residue is dissolved in EtOH and treated with a 2.0 M NH3 solution in EtOH. The resulting mixture is stirred at r.t (sensitive compounds) or 60°C for 2 -18 h. The mixture is then concentrated (rotavapor) and purified by chromatography (silicagel). Example 1 1.1 (S)-(+)-Methoxyphenyiacetic add was coupled with 4-aminoraethyi benzonitrile (CAS No: 10406-25-4) according to general procedure C to give (S)-N-(4-cyano-benzyl)-2-methoxy-2-phenyl-acetamide as an off-white soUd. MS 281.2 ([M+H]"^) 1.2 (S)-N-(4-Cyano-ben2yl)-2-methoxy-2-phenyl-acetamide was converted to (S)-N-(4-carbamimido)^-benzyi)-2-methoxy-2-phen)d-acetamide hydrochloride according to general procedure D. Colorless solid. MS 298 ([M+H]'^) Example 2 2.1 (R)-(+)-Methoxyphenylacetic acid was coupled with 4-aminomethyl benzonitrile {CAS No: 10406-25-4} according to general procedure C to give (R)-N-(4-cyano-benzyI}-2-methoiy-2-phenyl-acetamideas an off-white solid. MS 281.1 ([M+H]"*") 2.2 {R)-N-(4-Cyano-benzyl)-2-metho3cy-2-phenyl-acetamide was converted to (R)-N-(4-carbamimidoyl-benzyi)-2-methoxy-2-phenyI-acetamide hydrochloride accordic^ to general procedure D. Colorless solid. MS 298.2 ([M+H]*) Example 3 3.1 4-Benzyloxybeti2aldehyde was converted to (RS)-(4-benzyioxy-phenyl)-methoxy-acetic add according to general procedure A. Off-white solid. MS 271.1 ([M-H]') 3.2 (RS)-{4-Ben2:)ioxy-phenyl)-inetliox7-acetic acid was coupled with 4-aminomethyl benzonitrile to give {RS)-2-(4-benzyloxy-phenyI)-N-(4-cyano-benzyi)-2-methoxy-acetamide according to general procedure B. Colorless solid. MS 387.3 ([M+H]'') 3.3 (RS)-2-{4-Benzyloxy-phenyi)-N-(4-cyano-benzyl)-2-methoxy-acetamide was converted to (RS)-2- (4-benzyloxy-phenyi) -N- (4-carbaniimido)d-benzjd)-2-methoxy-acetaimde hydrochloride according to general procedure D. Colorless foam. MS 404.5 ([M+H]"^) Example 4 4.1 4-PhenoxybenzaIdehyde was converted to (RS)-methoxy-(4-phenoxy-phenyl)-acetic add according to general procedure A. Yellow oil. MS 257.0 ([M-H]') 4.2 (RS)-Methoxy-(4-phenoxy-phenyl)-acetic add was coupled with 4-aminomethyl benzonitrile according to general procedure B to give (RS)-N-(4-cyano-benzyi)-2-methoxy-2-{4-phenoxy-phenyl)-acetamide. Colorless solid. MS 373.3 ([M+H]"^) 4.3 (RS)-N-(4-Cyano-benzyi)-2-methox7-2-(4-phenoxy-phen)^)-acetamide was converted to (RS )-N- (4-carbamimidoyi-benzyl) -2 -methoxy-2-(4-phenoxy-phen)4)-acetairude hydrochloride according to general procedure D. Colorless foam. MS 390.3 ([M-f-H]"^) Example 5 5.1 3-Phenoxybenzaldehyde was converted to (RS)-methoxy-(3-phenoxy-phenyI)-acetic add according to general procedure A. Light yellow liquid. 5.2 {RS)-Methoxy-(3-phenoxy-phenyl)-acetic add was coupled with 4-arQinomethyi benzonitxile accordmg to general procedure B to give (RS)-N-(4-cyano-benz7l)-2-methoxy-2-(3-phenoxy-phenyl)-acetainide. Light yellow oil. MS 373.3 {[M+H]"^) 5.3 (RS)-N-(4-Cyano-benzyl)-2-methoxy-2-(3-phenox)'-phenyl)-acetamide was converted to (RS)-N- (4-carbamimido)i-benzyl)-2 -methoxy-2- (3-phenoxy-phenyl)-acetaimde hydrochloride according to general procedure D. Colorless amorphous soHd. MS 390.3 ([M+H]^) Example 6 6.1 Benzaldehyde was converted to (RS)-ethoxy-phenyl-acetic add according to general procedure A. Light yellow liquid. 6.2 (RS)-Ethoxy-phenyl-acetic acid was coupled with 4-aminometh5d benzonitrile according to general procedure B to give (RS)-N-(4-cyano-benzyl}-2-ethoxy-2-phenyi-acetamide. Light yellow semisolid. MS 295.3 ([M+H]"') 6.3 (RS)-N-(4-Cyano-benz)d)-2-ethoxy-2-phenyl-acetainide was converted to (RS)-N-(4-carbaniimxdoyl-benzyl}-2-ethoxy-2-phenyi-aeetamide hydrodiloride according to general procedure D. Colorless amorphous solid. MS 312.2 ([M+H]"*^) Example? 7.1 2-Fluorobenzaldehyde was converted to CRS)-(2-fluoro-phenyl)-methoxy-acetic acid according to general procedure A. Off-white amorphous solid. MS 1S2.9 ([M-H]") 7.2 (RS)-(2-Fluoro-phenyI)-methoxy-acetic add was coupled with 4-aniinometh)^ benzonitrile according to general procedure B to give {ES)-N-(4-cyano-benzjd)-2-(2-fluoro-phenyl)-2-methoxy-acetamide. Colorless oil. MS 299.2 ([M+H]"^) 73' (RS)-N-(4-Cyano-ben2yl)-2-(2-fIuoro-phenyl)-2-methoxy-acetamide was converted to (RS)-N-(4-carbami[nidoyI-benz)d)-2-(2-fluoro-phenyl)-2-methQxy-acetaniide hydrochloride according to general procedure D. Colorless foam. MS 316.2 ([M+H]"*") Examples 8.1 3-Benzyloxybeiizaldehyde was converted to (RS)-(3-ben2yloxy-phen)i)-methoxy-acetic add according to genera! procedure A. Colorless solid. 8.2 {RS)-(3-Benzyloxy-phen)d)-methoxy-acetic acid was coupled with 4-aminomethyl benzonitrile according to general procedure B to give (RS)-2-(3-ben2yloxy-phenyl)-N-(4-cyano-benzyl)-2-methoxy-acetaniide. Light yellow oil. 8.3 (RS)-2-(3-Ben2:)doxy-phenyl)-N-(4-cyano-benzyi)-2-niethoxy-acetainide was converted to (RS) -2' (3-benzyloxy-phenyi)-N- (4-carbaminiidoyl-ben2)d)-2-niethoxy-acetamide hydrochloride according to general procedure D. Colorless amorphous soUd. MS 404.5 ([M+H]") Example 9 9.1 As a side product of the synthesis of (RS)-2-(3-benzyloxy-phen)i)-N-(4-carbaininiido)^- benzyl)-2-methoxy-acetainide hydrochloride (example 8.3) there was obtained (RS)-N-(4- carbaminiidoyl-ben2;)d)-2-(3-hydroxy-phenyl)-2-methoxy-acetamide hydrochloride. Colorless amorphous solid. MS 314.2 ([M+H]^) Example 10 10.1 To a stirred solution of 3-mtrobenza!dehyde (4.043 g) at r.t. in 190 ml CH2C12 Was added Znl: (0.427 g). The mixture was purged with N2 and cooled to 0°C. Trimethylsilyl cyanide (2.92 g as a solution in 10 ml CH2CI2) was then added dropwise to the mixture for 15 min. The mixture was then allowed to warm to room temperature and stirrii^ was continued for 16 h. Water (250 ml) was then added to the mixture. The layers were separated and the aqueous phase was ractracted with CH2CI2 (125 ml). The combined organics were washed with water (125 ml) and brine (125 ml), dried (MgS04), filtered and concentrated (rotavapor) to leave the crude (RS)-(3-nitro-phenyl)-trimeth^silanyloxy-acetonitrile (6.56 g) as an orange oil which was used in the next step without further purification. 10.2 (RS)-(3-Nitro-phenyl)-trimeth)4silanyloxy-acetoiutrile (6.30 g) was dissolved in concentrated HQ with stirring. The mixture was then refluxed for 3 h. After cooling to room temperature, the yellow solution was poured into 200 g of crushed ice. This was extracted with Et20 (150 ml + 150 ml + 150 ml). The combined organics were washed with water (200 ml) and brine (200 ml), dried (MgS04), filtered and concentrated (rotavapor) to leave a yellow solid. This solid was triturated m a mixture of n-hexane (20 ml) and Et20 (2 ml), collected by filtration and washed with n-hexane to give (RS)-hydroxy-(3-nitro-phenyl)-acetic acid as a light yellow soUd (4.56 g). 103 A mixture of (RS)-hydroxy-(3-nitro-phenyl)-acetic acid (1.054 g), A&O (2.478 g) and Mel (2.304 g) was heated to reflux in toluene (10 ml). Stirring was then continued for 3 h. After cooling to r.t., the soUd was filtered off and washed with EtOAc. The filtrate was concentrated (rotavapor) to leave the crude (RS)-methoxy-(3-mtro-phen}d)-acetic acid methyl ester (1.161 g) as a light yellow oil. 10.4 A mixture of (RS)-methoxy-(3-nitro-phenyl)-acetic acid methyl ester (1.039 g) and NaOH (0.239 g) in water (0.75 ml) and methanol (10 ml) was stirred at 0°C for 4.5 h. The reaction mianjre was then concentrated (rotavapor, high vac.) and the residue (light yellow soHd) was taken in water (25 ml). The resulting solution was acidified to pH ~ 1 by dropwise addition of 3.0 N HCl. This was extracted with EtOAc (50 ml + 25 ml). The combined organics were dried (MgS04), filtered and concentrated (rotavapor) to leave the crude (RS)-methoxy-(3-nitro-phenyl)-acetic acid (0.944 g) as a Hghtyellow sohd. 10.5 (RS)-Methoxy-(3-mtro-phenyl)-acetic acid was coupled with 4-aminomethyi benzonitrile according to general procedure C to give (RS)-N-(4-cyano-benzyl)-2-methoxy-2-(3-nitro-phenyl)-acetamide. Light yellow gum. 10.6 (RS)-N-(4-Cyano-benz)d)-2-melhoxy-2-(3-mtro-phenyl)-acetaiiiide was converted to (RS )-N-(4-carbaimmidoyl-benzyl)-2-methoxy-2-(3-nitro-phen5d) -acetamide hydrochloride according to general procedure D. Off-white solid. MS 343.2 ([M+H] '^) Example 11 11.1 4-Biphenylaldehyde was converted to (RS)-biphenyl-4-yI-methoxy-acetic acid according to general procedure A. Light brown solid. 11.2 (RS)-Biphenyl-4-yl-methoxy-acetic acid was coupled with 4-aiiunometh)i benzonitrile according to general procedure C to give (RS)-2-biphenyl-4-yl-N-(4-cyano-ben2yI)-2-methoxy-acetamide. Light yellow soUd. U.3 {RS)-2-Biphen)d-4-yl-N-(4-cyano-benzyl)-2-methoxy-acetamide was converted to (RS)-2- biphenyI-4-yl-N-(4-carbaininiidoyl-benzyl)-2-raethoxy-acetanude hydrochloride according to general procedure D. Off-white soUd. MS 374.4 ([M+H]*) Example 12 12.1 Piperonal was converted to (RS)-ben2o[l,3]dioxcl-5-yl-methoxy-acetic acid according to general procedure A. Orange oil. 12.2 (RS)-Benzo[l,3]dioxol-5-yl-methoxy-acetic add was coupled with 4-aniinometh)i ben20nitrile according to general procedure C to give (RS}-2-benzo[l,3]dioxo}-5-y]-N-(4-cyano-benzyl)-2-methoxy-acetanude. Light yellow solid. 12.3 (RS)-2-Benzo[l,3]dioxoi-5-yi-N-{4-cj^no-benzyi}-2-methoxy-acetomde vras converted to (RS)-2-benzo[l,3]dioxol-5-)d-N-(4-carbainimidoyl-benz)4)-2-niethoxy-acetaimde hydrochloride according to general procedure D (Pinner reaction in EtOH/CHQg as a solvent). OfF-white soHd. MS 342.2 ([M+H]"") Example 13 13.1 As a side product of the synthesis of {RS)-2-ben2o[l,3]dioxoI-5-)d-N-(4-carbaniiinidoyl-ben2yI)-2-methoxy-acetaimde hydrochloride (example 12.3) there was obtained (RS)-2-benzo[l,3]dioxol-5-yI-N-(4-carbamiinidoyl-benz)^)-2-ethoxy-acetaniide hydrochloride. Light brown solid. MS 356.3 ([M+H]"^) Example 14 14.1 5-Ethoxy-2-fluoro-3-(l-methyl-piperidin-4-)doxy)-benzaldehyde was converted to (RS)- [5-ethoxy-2-fluoro-3-(I-methyl-piperidin-4-yloxy)-phenyl]-methoxy-acetic acid according to general procedure A. Off-white solid. MS 342.2 ([M+H]^) U.2 (RS)-[5-Ethoxy-2-fluoro-3-(l-methyl-piperidm-4-yloxy)-phenyi]-methoxy-aceticadd was coupled with 4-aminomethyt benzonitrile according to general procedure B to give (RS)-N-(4-cyano-benzyl)-2-[5-ethoxy-2-fiuoro-3-(l-inethyl-piperidin-4-yloxy)-phenyi]-2-methoxy-acetamide. Colorless foam. MS 456.5 ([M+H]'*') 14.3 (RS}-N-(4-Cyano-benz)i)-2-[5-ethoxy-2-£luoro-3-(i-methyI-piperidin-4-yloxy)-phen)d]- 2-methoxy-acet2inide was converted to (RS)-N-(4-carbamiinidoyl-benzyl)-2-[5-ethoxy-2- fluoro-3-{l-methyI-piperidin-4-yIoxy)-pfaenyi]-2-methoxy-acetamide hydTochloride according to general procedure D. Colorless foam. MS 473.5 {[M+H]"*") Example 15 15.1 2-Fluoro-4-methoxybenzaldehyde was converted to {RS)-(2-fluoro-4-methoxy-phenyl)- methoxy-aceticaddaccordingtogeneralprocedure A, Light yellow oil. MS 213.4 ([M-H]") 15.2 (RS)-(2-Fluoro-4-methoxy-phenyl)-methoxy-acetic add was coupled with 4-anunomethyl benzonitrile according to general procedure B to give (RS)-N-(4rCyano-benzyl)-2-(2-£luoro-4-methoxy-phen)4)-2-inethosy-acetamide. Colorless oil. MS 329.2 {[M+H]"^) 15.3 {RS)-N-(4-Cyano-benzyl)-2-(2-fluoro-4-methoxy-phenyl)-2-methoxy-acetanude was converted to (RS)-N-C4-carbamimidoyl-benzyi)-2-(2-fluoro-4-methoxy-phenyl)-2-methoxy-acetamide hydrochloride according to general procedure D. Colorless foam. MS 346.4 ([M+H]"") 15.4 (RS)-N- (4-CarbaniiinidoyI-benzyI) -2- (2-fluoro-4-methoxy-phenyl)-2-niethoxy-acetainide hydrochloride (example 15.3,200 mg) was dissolved in DMF (2.2 ml). The flask was placed in an ice bath. Ethyl chloroformate (58 mg) and triethylamine (160 mg) were added dropwise. The reaction mixture was stirred for 1.5 h at 0 "C. Ethyl acetate (30 ml) and ice water (40 ml) were added and the mixture was extracted with eth-jd acetate. The organic phase vtfas washed with water, dried, filtered and evaporated. The product was purified by chromatography (silic^el, ethylacetate) to give (RS)-[amino-(4-i[2-(2-fluoro-4-methoxy-phenyl)-2-niethoxy-acet)iamino]-methjd}-phenyl)-methyIene]-carbainic add ethyl ester (218 mg) as a colorless amorphous solid. MS 418.3 ([M+H]*) 15.5 (RS)-N-(4-Cyano-benzyi)-2-(2-fluoro-4-rnethoxy-phenyl)-2-inethoxy-acetamide (example 15.2, 251 mg) was dissolved in methanol (7 ml).Hydroxylaimne hydrochloride (212 mg) and triethyiamine (618 mg) were added. The mixture was stirred for 19 h at r.L The solvent was evaporated. The residue was dissolved in methylene chloride, washed with water, dried and filtered. The solvent was evaporated to give (RS)-2-(2-fluoro-4-methox7-phenyl)-N-[4-(N-hydroxycarbainimidoyl)-benzyl]-2-methoxy-acetamide (269 mg) as an off-white foam. MS 362.2 ([M+H]*) 15.6 (RS)-N-(4-Cyano-benzyl)-2-(2-fluoro-4-methoxy-phen)4)-2-methoxy-acetamide (example 15.2, 285 mg) was dissolved in methanol (0.7 ml) and chloroform (3.3 ml). The mixture was placed in an ice-NaCl bath. Dry HCl gas was passed over the reaction mixture for 15 min. The flask was stoppered and left overnight at 4 °C. The mixture was concentrated (rotavapor and high vacuum) at r.t The residue was dissolved in methanol (i.9 ml). Hydrazine hydrochloride (66 mg) and triethyiamine (264 mg) were added. The mixture was stirred ovemighL The solvent was evaporated and the product was purified by chromatography (silica gel, CH2CI2 => CH2Cl2/MeOH 4:1) to give RS)-2-(2-fluoro-4-methoxy-phenyl)-N-[4-(N-aniinocarbaniimidoyl)-benzyi]-2-methoxy-acetamide (205 mg) as an off-white foam. MS 361.2 ([M+H]^) Example 16 16.1 3-Ben2yloxy-4-methoxy-benzaldehyde was converted to (RS)-(3-benzyloxy-4-methoxy- phenyl)-raethoxy-acetic add according to general procedure A. Orange solid. 16.2 To a stirred solution of (RS)-(3-benzyloxy-4-methoxy-pheni4)-methoxy-acetic add (0.923 g) at T,t. in ethanol was added 10% Pd/C. The mixture was then stirred at i.t. under a hydrogen atmosphere for 17 h. The catalyst was filtered off and washed with dichloromethane. The filtrate was concentrated (rotavapor) to give (RS)-(3-hydroxy-4-methoxy-phen)d)-methoxy-acetJc add (0.642 g) as an orange gum. 16.3 (RS}-(3-Hydroxy-4-methoxy-phenyl)-methoxy-acetic add was coupled with 4-aminomethyl benzonitrile according to general procedure C to give (RS)-N-(4-cyano-benzyl}-2-(3-hydroxy-4-methoxy-phenyl)-2-methoxy-acetamide. White foam. 16.4 To a stirred solution of (RS)-N-(4-cyano-benzyl)-2-(3-hydroxy-4-methoxy-phenyl)-2-methoxy-acetamide (0.303 g) at r.t. in DMF {3 ml) were added KsCOs (0.14 g) and ethyl bromoacetate (0.169 g). The reaction mixture was then stirred at r.L under an argon atmosphere for 5 h 45. The mixture was diluted with EtOAc (25 ml), washed with water (25 ml) and brine (25 ml), dried (MgS04), filtered and concentrated (rotavapor) to leave the crude product as a light yellow gum. The product was purifiied by chromatography (Siiicagel (20 g) using a gradient profile: cyclohexane to cyclohexane / EtOAc 35:65) to give (RS)-(5-[(4-cyano-ben2)4carbamoyl)-methoxy-methyl]-2-methoxy-phenoxy}-acetic add ethyl ester (0.342 g) as a white solid. 16.5 (RS)-{5-[(4-Cyano-benz>dcarbarnoyI)-metboxy-methyl]-2-metiioxy-phenoxy}-acetic add ethyl ester was converted to (RS)-{5-[(4-carbamiinidoyl-ben2ylcarbamoyi)-methoxy-methyl]-2-methoxy-phenoxy}-acetic add methyl ester hydrochloride according to general procedure D. OfF-white soUd. MS 416.3 ([M+H]^) Example 17 17.1 As a side product of the synthesis of {RS)-{5-[(4-carbamimidoyi-benzy/carbamoyi)- methoxy-methyl]-2-methoxy-phenoxy}-acetic add methyl ester hydrochloride (example 16.5) there was obtained (RS)-N-(4-carbamimidoyi-ben2yl)-2-(3-carbamoj4methoxy-4- methoxy-phenyl)-2-methoxy-acetamide hydrodiloride. Off-white solid. MS 401.5 ([M+H]^) Example 18 I8.I 3-Benzyloxy-4-methoxy-ben2aldehyde was converted to (RS)-(3-benz)4oxy-4-methoxy- phenyl)-etiio]9^-acetic add according to general procedure A. Light yellow soHd. 18.2 To a stirred solution of (RS)-(3-benzyloxy-4-m^oxy-phenyl}-ethoxy-acetic acid (0.801 g) at r.t in ethanol was added 10% Pd/C (0.1 g). The mixture was then stirred at r.t. under a hydrogen atmosphere for 17 h. The catalyst was filtered off and washed with dichlorometiiane. The filtrate was concentrated (rotavapor). The residue was purified by chromatography to give (RS)-ethoxy-(3-hydroxy-4-methoxy-phenyl)-acetic acid (0.250 g) as a light yellow gum. 18.3 (RS)-Ethoxy-(3-hydroxy-4-metlioxy-plienyl)-acetic add was coupled with 4-aminomethyl benzonitrile according to genera] procedure C to give CRS)-N-(4-cyano-benzyi)-2-ethoxy-2-(3-hydroxy-4-methoxy-phenyl)-acetamide. Light yellow gum. 18.4 To a stirred solution of (RS)-N-{4-cyano-beiizyl)-2-ethoxy-2-(3-hydroxy-4-methoxy-phenyD-acetamide (0.158 g) at r.L in DMF (1.5 ml) were added K2CO3 (0.067 g) and ethyl bromoacetate (0.081 g). The reaction mixture was then stirred at r.t under an argon atmosphere for 24 h. The mixture was diluted with EtOAc (10 ml), washed with water (10 ml+10 ml) and brine (10 ml), dried (MgSO^), filtered and concentrated (rotavapor). The product was purified by chromatography (Sihcagel (20 g) using a gradient profile: cydohexane to cyclohexane / EtOAc 45:55) to give (RS)-{5-[(4-cyano-benz)dcarbamoyl)-ethoxy-methyl]-2-methoxy-phenoxy}-acetic acid eth)d ester (0.160 g) as a colorless gum. 18.5 (RS)-{5-[(4-Cyano-benzylcarbamoyl)-ethoxy-methyi]-2-methoxy-phenoxy}-acetic add ethyl ester was converted to (RS)-{5-[(4-carbaniimido)d-benzylcarbamoyl)-ethoxy-methyl]-2-methoxy-phenoxy^}-acetic add ethyl ester hydrochloride according to general procedure D. OfF-white solid. MS 444.4 ([M+Hf) Example 19 19.1 As a side product of the synthesis of (RS)-{5-[(4-carbamimidoyI-benzyIcarbamoyi}-ethoxy-methyl]-2-methoxy-phenoxy}-acetic add ethyl ester hydrochloride (example 18.5) there was obtained (RS)-N-(4-carbamimidoyl-ben2yi)-2-(3-carbamo)dmethoxy-4-methoxy-phenyi)-2-ethoxy-acetamidehydrochloride. Off-white solid. MS 415.4 ([M+H]"^) Example 20 20.1 To a stirred suspension of (RS)-{5-[(4-carbamimidoyl-benz)4carbamoyl)-ethoxy-methyl]-2-methoxy-phenoxy}-acetic add ethyl ester hydrochloride (example 18.5, 0.045 g) at r.L in THE (1 ml) and water (0.5 ml) was added 1.0 N NaOH (0.2 ml). The mixture was then stirred at r.L under an argon atmosphere for 3 h. The mixture waa addified to pH 5-6 by addition of 1.0 N HCl. The THF was removed (rotavapor) and the product predpitated out from the remaining water. It was collected by filtration, washed with water and cydohexane and dried overnight under high vacuum to give (RS)-{5-[{4-carbaniiniidoyI- benzylcarbaiaoyl)-ethoxy-methyI]-2-methosy-plienoxy}-acetic add (0.027 g) as a white powder. MS 416.3 {[M+H]"") Example 21 21.1 (RS}-(4-Benzyloxy-phenyl)-inethoxy-acetic add (example 3.1) was hydrogenated at r.t. and normal pressure using 10% Pd/C as a catalyst and EtOH as a solvent to give (RS)-(4-hydroxy-plienyl)-methoxy-acetic add as a light grey solid. MS 181.4 ([M-H]') 21.2 (RS)-(4-Hydroxy-phenyi)-methoxy-acetic add was coupled with 4-aniinometh.yl benzonitrile according to general procedure B to give (RS)-N-(4-cyano-benzy]}-2-(4-hydroxy-phenyl)-2-metlioxy-acetamide. Colorless foam. MS 295.2 ([M-H]") 21.3 In analogy to example 16.4, (RS)-N-(4-cyano-ben2yi)-2-(4-hydroxy-phenyl)-2-methoxy-acetamide was alkylated with ethyl iodide / cesium carbonate in DMF to give (RS)-N-(4-cyano-benz)^)-2-(4-ethoxy-phenyl)-2-methoxy-acetainide as a colorless soHd. MS 325.3 ([M+H]^) 21.4 (RS)-N-(4-Cyano-ben2)^)-2-(4-ethoxy-phenyl)-2-methoxy-acetamide was converted to (RS)-N-(4-carbaminiido)d-benzyl)-2-ethoxy-2-(4-ethoxy-phenyl)-acetamid hydrochloride according to general procedure D using EtOH/CHCls as a solvent. OfF-white amorphous soUd. MS 365.3 ([M+H]"^) Example 22 22.1 (RS)-N-(4-Cyano-ben2yI)-2-(4-hydroxy-phenyl)-2-methoxy-acetamide (example 21.2, 0.406 g) was dissolved in THF (12 ml). Triphenylphosphine (0.539 g) and 4-hydroxy-N-methylpiperidine (0.237 g) were added. The reaction mixture was cooled to 0 *C. Slowly, DEAD (0.384 g) was added. The reaction mixture was stirred at 0 °C for 30 min and at r.L for 5 days. The solvent was evaporated and the product vras purified by chromatography (siHcagel, mobile phase: gradient from CH2CI2 to CH2a2/MeOH 4:1) to give (RS)-N-(4-cyano-benz}d)-2-methoxy-2-[4-(l-meth)^-piperidin-4-yloxy)-phen-)4]-acetamide as a colorless foam (0.241 g). MS 394.4 (fM+H]"") 22^ (RS)-N-(4-Cyano-beDzy])-2-inethoxy-2-[4-(l-meth)d-piperidin-4-yloxj')-phenyl]- acetamide was converted to {RS)-N-(4-carbamiimdoyi-benzyl)-2-methoxy-2-[4-(l-metfayI-piperidin-4-yloxy)-phenyl]-acetarmde hydrochloride according to general procedure D. Colorless foam. MS 411.4 ([M+HJ^ Example 23 23.1 (+/-}-a-Methoxy-alpha-trifluoromethyl phenylacetic add was coupled with 4-aminometh)^ benzonitrile according to general procedure C to give (RS)-N-(4-cyano-benzyl)-3,3,3-trifluoro-2-methoxy-2-phenyl-propionamide. Off-white solid. 23.2 (RS)-N-(4-Cyano-benzyi)-3,3,3-trifluoro-2-methoxy-2-phenyi-propionainide was converted to (RS)-N-(4-carbamimidoyl-benzyl)-3,3,3-tri0.uoro-2-methoxy-2-phenyl- propionamide hydrochloride according to general procedure D. White solid. MS 366.2 ([M+H]^) Example 24 24.1 6-Fiuorveratraidehyde was converted to (RS)-(2-fIuoro-4,5-diinethoxy-phenyl)-methox)'- acetic add according to general procedure A. Light yellow oil. MS 243.1 ([M-H]"} 24.2 (RS)-(2-Fluoro-4,5-dimethoxy-phenyl)-methoxy-acetic add was coupled with 4- aminometbyl benzonitrile according to general procedure B to give (RS}-N-{4-cyano- benzyl)-2-(2-fluoro-4,5-dimethoxy-phenyl)-2-methoxy-acetamide. Red foam. MS 359.2 ([M+H]^) 24.3 (RS)-N-(4-Cyano-benzyl)-2-(2-fluoro-4,5-dimethoxy-phenyi)-2-niethoxy-acetamide was converted to (RS)-N-{4-carbamimidoyl-benz5d)-2-{2-fluoro-4,5-dimethoxy-phen)d)-2-methoxy-acetamide hydrochloride according to general procedure D. Orange solid. MS 376.4 ([M+H]"") Example 25 25.1 (RS)-(3-Beuzyloxy-phen)^)-methoxy-acetic add (example 8.1) was hydrogenated at r.t. and normal pressure using 10% Pd/C as a catalyst and EtOH as a solvent to give (RS)-(3-hydroxy-phen)d}-methoxy-acetic add as a colorless foam. 25.2 (RS)-( 3-Hydroxy-phenyl)-medioxy-acetic add was coupled -with 4-anunomethyl benzonitrile according to general procedure B to give (RS)-N-(4-cyano-benzyl)-2-(3-hydroxy-phenyl)-2-methoxy-acetamide. Colorless oil. 25.3 In analogy to example 16.4, (RS)-N-(4-c)'ano-benzyi)-2-(3-hydroxy-phenyi)-2-methpxj'-acetamide was alkylated with 2-iodopropane / cesium carbonate in DMF to give (RS)-N-(4-cyano-benzyl)-2~(3-isopropoxy-phenyl)-2-methox7-acetainide as a colorless oil. MS 339.2 {[M+H]'*') 25.4 (RS)-N-{4-Cyano-ben2yi)-2-(3-isopropoK7-phen)d)-2-methoxy-acetarmde was converted to (RSJ-N-(4-carbainimidoyl-benzyl}-2-(3-isopropoxy-p£ienyI}-2-methoxy-acetaimde hydrochloride according to general procedure D. Colorless amorphous solid. MS 356.3 ([M+H]^) Example 26 26.1 In analogy to example 22.1, (RS)-N-{4-cyano-benz)d)-2-{4-hydrQxy-phenyl)-2-methoxy-acetamide (example 21.2) was reacted with cyclopentanol, triphen)dphosphine and DEAD in THF. Further conversion according to general procedure D gave (RS)-N-(4-carbamimidoyl-benzyl)-2-(4-cyclopentyioxy-phenyI)-2-methoxy-acetamide hydrochloride as a Hght yellow sohd. MS 282.3 ([M+H]^) Example 27 27.1 In analogy to example 16.4, (RS)-N-(4-cyano-benzyI)-2-{4-hydroxy-phen)d)-2-methoxy-acetamide (example 21.2) was alkylated with 2-iodopropane / cesium carbonate in DMF to give (RS)-N-(4-cyano-benzyl)-2-(4-isopropoxy-phen>^)-2-methoxy-acetamide as a colorless solid. MS 339.2 ([M-KH]*) 27.2 (RS)-N-(4-Cyano-benzyi)-2-(4-isopropoxy-phenyi)-2-metfaoxy-acetamide was converted to (RS)-N-(4-carbamiinidoyl-benzyl)-2-(4-isopropoxy-phenyI)-2-methox7-acetamide hydrochloride according to general procedure D. Colorless foam. MS 356.3 ([M+H]"*") Example 28 28.] In analogy to example I6.4, (RS)-N-{4-cyano-benzyl)-2-(4-liydroxy-phenyl)-2-methoxy-acetamide (example 21.2) was alkylated with ethylbromoacetate / cesium carbonate in DMF to give (RS)-{4-[(4-cyano-benzylcarbamoyl)-methoxy-methyl]-phenoxy}-acetic add ethyl ester as a colorless solid. MS 383.3 {[M+H]'^) 28.2 (RS)-{4-[(4-Cyano-ben2)4carbaino)d)-metlioxy-methyI]-phenoxy}-acetic acid ethyl ester was converted to CIlS)-{4-[(4-carbamiinidoyl-benzylcarbanioyl)-methoxy-methyl]-phenoxyj-acetic acid methyl ester hydrochloride according to general procedure D using MeOH/CHCl3 as a solvent Colorless foam. MS 386.3 ([M+H]^) Example 29 29.1 In analogy to example 20.1, (RS)-|4-[(4-carbaminiidoyi-ben2ylcarbamoyI)-methoxy-methyi]-phenoxy}-acetic acid methyl ester hydrochloride (example 28.2) was hydrolyzed to (RS}-{4-[(4-carbamimidoyl-benzylcarbamoyi)-methoxy-methyl]-phenoxyl-acetic add. Colorless soUd. MS 370.2([M-H]') Example 30 30.1 In analogy to example 22.1, (RS)-N-(4-cyano-benzylJ-2-(3-hydroxy-phenyi)-2-methoxy-acetamide (example 25.2) was reacted with tetrahydro-2H-pyran-4-ol, DEAD and triphen^dphosphine in THE and subsequently converted into (RS)-N-(4-carbamimidoyl-benzyi)-2-methoxy-2-[3-(tetrahydro-pyran-4-yloxy)-phenyl]-acetamide hydrochloride according to general procedure D. Colorless amorphous solid. MS 398.4 ([M+H]"^) Example 31 31.1 3,5-Diethoxy-2-fluoro-ben2aldehyde (CAS 277324-21-7) was converted to (RS)-(3,5- diethoxy-2-fluoro-pbenyi)-methoxy-acetic add according to general procedure A Yellow oil MS 271.1 ([M-H]") 31.2 (RS)-(3,5-Diethoxy-2-fluoro-phenyi)-methoxy-acetic acid was coupled with 4- aminomethyl benzonitrile according to general procedure B to give (RS)-N-(4-cyano- benzyl)-2-{3,5-diethoxy-2-fluoro-phen)d)-2-methoxy-acetaimde. Light yellow oil. MS 387.3 ([M+H]^) 31.3 (RS}-N-(4-Cyano-benz7l)-2-(3,5-diethoxy-2-fluoro-phen^)-2-methoxy-acetamide was converted to (RS)-N~{4-carbamimidoyi-beiizyl)-2-(3,5-diethoxy-2-fluoro-phenyl)-2-methoxy-acetamide hydrocHoride according to general procedure D. Light brown foam. MS 404.5 ([M+H]"*") Example 32 32.1 5-Ethoxy-2-fiuoro-4-(2-hydroxy-ethoxy)-benzaIdehyde (CAS 376600-66-7) was converted to {RS)-[5-ethoxy-2-fiuoro-4-(2-hydroxy-ethoxy)-phenyI]-tuethoxy-acetic add according to general procedure A. Yellow oil. MS 287.0 ([M-H]") 32.2 {RS)-[5-Ethoxy-2-fluoro~4-(2-hydrojq'-ethoj^)-phenyl]-metho39'-acetic add was coupled with 4-aminoinethyl benzonitrile according to general procedure B to give (RS)-N-(4-cyano-ben2yl) -2- [ 5-ethoxy-2-fluoro-4- (2-hydroxy-ethoxy)-phenyl] -2-medioxy-acetaniide. Light yeCow oil. MS 403.4 ([M+H]"*") 32.3 (RS)-N-(4-Cyano-benzyi)~2-[5-ethoxy-2-fluoro-4-(2-hydroxy-ethoxy)-phenTd]-2-methoxy-acetamide was converted to (RS)-N-(4-carbamiinido)d-ben27l)-2-[5-ethoxy-2-fluoro-4-(2-hydroxy-ethoxy)-phenyl]-2-methoxy-acetamide hydrochloride according to general procedure D. Off-white foam. MS 420.3 ([M+H]'*') Example 33 33.1 3,4-Diethoxy-2-fluoro-ben2aldehyde was converted to (RS)-(3,4-diethoxy-2-fluoro- phenyI)-methoxy-acetic add according to general procedure A, Yellow oil. MS 27L1 {[M- H]-) 33.2 (RS)-(3,4-Diethoxy-2-fluoro-phenyl)-methoxy-acetic acid was coupled with 4- aminomethjd benzonitrile according to general procedure B to give (RS)-N-(4-cyano- ben2yl)-2-C3,4-diethoxy-2-fiuoro-phen)d)-2-methoxy-acetamide. Colorless solid. MS 387.3 ([M+H]") 33.3 (RS)-N-(4-Cyano-benzyl)-2-(3,4-diethoxy-2-fluoro-phenyl)-2-methoxy-acetainide was converted to (RS)-N-(4-carbamimidoyl-beiizyl)-2-(3,4-diethoxy-2-fIuoro-plienyi)-2-metboxy-acetamide hydrochloride according to general procedure D. Colorless foam. MS 404.5 ([M+H]-") Example 34 34.1 4-(Bromomethyl)-3-fluoroben2omtrile (CAS 105942-09-4, 21 g) was dissolved in DMF (90 ml). Phthalimide potassium salt (19.64 g) was added and the mixture was stirred for 9 h at 130 °C. After cooling to r.t., the naixture was poured on ice. The solid was filtered off. Ethyl acetate and water were added and extracted with ethyl acetate. The organic phase was washed with water, dried, filtered and evaporated to give a light brown solid (14.1 g, 42 % pure as judged by NMR). This sohd was suspended in ethanol (50 ml), A solution of hydrazine in water (24%, 15 ml) was added and the mixture was refluxed for a total of 14 h. The mixture was filtered and the solvent was evaporated. Tlie product was purified by chromatography (silica gel, CH2CI2 => CH2Cl2/MeOH 4:1) to give 4-aminomethyl-3-fluoro-benzonitrile (0.63 g) as a brown oil. 34.2 CRS)-(2-Fluoro-4-methoxy-phen)d)-methoxy-acetic acid (aample 15.1) was coupled with 4-aminomethyl-3-fluoro-benzonitrile according to general procedure B to give (RS)-N-(4-cyano-2-fluoro-benzyi)-2-(2-fiuoro-4-methoxy-phenyl)-2-metiioxy-acetamide. Yellow oil. MS 347.3 ([M+H]') 34.3 (RS) -N- (4-Cyano-2-fluoro-benz}4}-2 - (2-fluoro-4-methoxy-phen)1) -2-methoxy-acetamide was converted to (RS)-N-(4-carbanumidoyl-2-fluoro-benzyl)-2-(2-fluQro-4-methoxy-phen7])-2-inethoxy-acetajiiide hydrochloride according to general procedure D. Off-white amorphous soHd. MS 364.2 ([M+H]"") Example 35 35.1 (RS)-(2-FIuoro-4-inethoxy-phen)^)-methoxy-acetic add (example 15.1) was coupled with 4-aminomethyl-2-fluorobenzonitrile (CAS 368426-73-7) according to general procedure B to give (RS)-N-(4-cyano-3-fluoro-benzyl)-2-(2-£luoro-4-methoxy-phenyl)-2-methoxy-acetamide. Light yellow solid. MS 347.3 ( [M+HD 35.2 (RS )-N-(4- Cyano-3 -fluoro-beiizyl)-2- {2-fluoro-4-inethoxy-phenyl)-2-methoxy-acetamide was converted to (RS)-N-(4-carbaimmido-;^-3-fluoro-ben2yl)-2-(2-fluoro-4-methoxy-phenyl)-2-methoxy-acetaimde hydrochloride according to general procedure D. Off-white amorphous solid. MS 364.2 ([M+H]^) Example 36 36.1 2,4-Bis-(trifluoromelhyl)benza]dehyde was converted to (RS)-(2,4-bis-trifluoromethyl-phenyi)-methoxy-acetic acid according to general procedure A. White solid. 36.2 {RS)-(2,4-Bis-trifluoromeihyi-phenyl)-methoxy-acetic acid was coupled with 4-aminomethyl benzonitrile according to general procedure C to give (RS)-2-(2,4-bis-trifluoromethyl-phenyl)-N-{4-cyano-benzyl)-2-methoxy-acetamide. Colorless gum. 36.3 (RS)-2-(2,4-Bis-trifluoromethyI-phenyl)-N-(4-cyano-benz>i)-2-methoxy-acetaniide was converted to (RS)-2-(2,4-bis-trifluorometh)4-phenyi)-N-(4-carbainiinidoyl-benzyl)-2-methoxy-acetamide hydrochloride according to general procedure D. Off-white solid. MS 434.4 ([M+H]^) Example 37 37.1 2-BenzyIoxy-4-methoxy-benzaldehyde (CAS 32884-23-4) was converted to (RS)-(2-benzyioxy-4-metlioxy-phenyI)-methoxy-acetic add according to general procedure A. Light yeUow oil. MS 301.1 ([M-H]') 37.2 In analogy to example 16.2, (RS)-(2-ben2yloxy-4-methoxy-phenyi}-methoxy-acetic acid was hydrogenated to give (RS)-(2-hydroxy-4-inethoxy-phen^)-methoxy-acetic acid. Purple soUd. MS 211.0 ([M-H]') 37.3 (RS)-(2-Hydroxy-4-methoxy-phenyl)-metiiory-acetic acid was coupled with 4-aminomethyl benzonitrile according to general procedure B to give (RS)-N-(4-cyano-ben2yl)-2-(2-hydroxy-4^methoxy-phenyl)-2-methoxy-acetamide. Orange amorphous 5oJid. MS 327.3 ([M+H]"") 37.4 In analogy to example 15.5, (RS)-N-(4-cyano-lienzy])-2-{2-hydroxy-4-methox7-phenyl)-2-methoxy-acetamide was converted to (RS)-N-[4-CN-liydroxycarbarnimidoyl)-benzyi]-2-C2-hydrox)'-4-methoxy-phenyl)-2-methoxy-acetamide. White solid. MS 358.1 ([M-H]") 37.5 A suspension of (RS)-N-[4-(N-hydroiycarbamimidoyl)-benzyl] -2-(2-hydroxy-4-inethoxy-ph.enyl)-2-niethoxy-acetamide {240 mg) in ethanol (9 ml) and acetic acid (0.38 ml) was hydrogenated for 7.5 h using 10% Pd/C as a catalyst. The reaction mixture was filtered and the solvent was evaporated. The product was purified by chromatography (sifica gel, CH2CI2 => CH2Cl2/MeOH 4:1) to give (RS)-N-{4-carbamimidoyl-benzyl)-2-(2-hydroxy-4-methoxy-phenyI)-2-methoxy-acetanude actetate (12 mg) as an off-white, amorphous soUd. MS 344.2 ([M+H]') Example 38 38.1 2-FIuoro-3-methoxybenzaidefayde was converted to (RS)-(2-fluoro-5-methoxy-phenyi}- methoxy-acetic add according to general procedure A. Light yellow oil. 38^ (RS)-(2-Fluoro-5-methoxy-phenyl)-methoxy-acetic acid was coupled with 4-aminomethyl benzonitrile according to general procedure C to give (RS)-N-(4-cyano-benz)d)-2-(2-fluoro-5-niethoxy-phenyi)-2-methoxy-acetamide. Colorless gum. 38.3 (RS)-N-(4-Cyano-benzyl)-2-(2-fluoro-5-methoxy-phenyl)-2-methoxy-acetamide was converted to (RS)-N-(4-carbaniimido^-benz)i)-2-(2-fluoro-5-methoxy-phenyI)-2-methoxy-acetamide; hydrochloride according to general procedure D. "White solid. MS 346.2 ([M-t-H]') Example 39 39.1 2,3-Difluorobenzaldehyde was converted to (RS)-(2,3-difiuoro-phenyl)-methoxy-acetic add according to general procedure A. Off-white soUd, 39.2 (RS)-(2,3-Difluoro-phenyi)-methoxy-acetic add was coupled with 4-aminomethyl benzonitrile according to general procedure C to give (RS)-N-{4-cyano-benzyi)-2-(2^-difluoro-phenyl)-2-methoxy-acetamide. Off-white soHd. 39.3 (RS)-N-(4-C7ano-benz}'l)-2-(2,3-diiluoro-phenyl)-2-inetboxy-acetaii!ide was converted to (RS) -N- (4-carbamimidoyl-benzyl) -2-(2,3-difluoro-piienyl}-2-methoxy-acetainide; hydrochloride according to genera! procedure D. White solid. MS 334.3 ([M+H]"^) Example 40 40.1 2,6-Difluorobenzaldehyde was converted to (RS)-(2,6-difluoro-phenyl)-methoxy-acetic acid according to general procedure A. Light yellow soHd. 40.2 (RS)-(2,6-E>ifluoro-phenyl)-methoj:y-acetic add was coupled with 4-aininQmethyl benzonitrile according to general procedure C to give (RS)-N-(4-cyano-benzyi)-2-(2,6-difluoro-phenyl)-2-methoxy-acetaniide. Off-white solid. 40.3 (RS)-N-(4-Cyano-benzylJ-2-{2,6-difluoro-phenyi)-2-methoxy-acetanude was converted to (RS)-N-(4-carbaiminidoyl-benz)d)-2-{2,6-difluoro-phenyl)-2-methoxy-acetamide; hydrochloride according to general procedure D. White solid. MS 334.2 ([M+IJ]"^) Example 41 41.1 4-Bromo-2-fluorobenzaIdehyde was converted to (RS)-{4-bromo-2-fluoro-phen)d)-methoxy-acetic acid according to general procedure A using methanol / dioxane as a solvent Light yellow oil. 41.2 (RS)-(4-Bromo-2-fluoro-phenyI)-methoxy-acetic add was coupled with 4-aniinomethy! benzonitrile according to general procedure C to give (RS)-2-(4-bromo-2-fluoro-phenjd)-N-(4-c)^no-benzyl)-2-methoxy-acetamide. Light yellow gum. 41.3 (RS)-2-(4-Bromo-2-fluoro-phenyl)-N-(4-cyano-benzyi)-2-methoxy-acetamide was converted to (RS)-2-(4-bromo-2-fluoro-phenyl)-N-(4-carbamimidoyl-benzyl)-2-methoxy-acetamide hydrochloride according to general procedure D. Off-white solid. MS 394.1 ([M+H]-") Example 42 42.1 4-Bromo-2-Quorobeii2aldehyde was reacted according to general procedure A using ethanol / dioxane as a solvent. The product of this reaction was subsequentJy coupled with 4-aminomethyl benzonitrile according to general procedure B to give (RS)-2-(4-bromo-2-fluoro-phenyl)-N-(4-cyano-benzyl)-2-ethoxy-acetaimde. Light yeUow oil, MS 39U ([M+H]^) 42.2 (RS)-2-(4-Bromo-2-fluoro-phenyl)-N-(4-cyano-ben2yl)-2-ethoxy-acetamide was converted to (RS}-2-(4-bromo-2-fluoro-phenyl}-N-(4-carbainiimdoj^-benzyl)-2-erfioxy-acetamide hydrochloride according to general procedure D. Off-white foam. MS 408.2 Example 43 43.1 4-Bromo-2-fluorobenzaldehyde was converted to (RS)-(4-bromo-2-fluoro-phen)4)-propoxy-acetic acid according to general procedure A using n-propanol / dioxane as a solvent- Colorless semisolid. 43.2 (RS)-(4-Bromo-2-fluoro-phenyl)-propoxy-acetic acid was coupled with 4-aniinomethyl benzonitrile according to general procedure C to give (RS)-2-(4-bromo~2-fluoro-phenyl)-N-(4-cyano-benz)^)-2-propcixy-acetaniide. Colorless oil. MS 405.3 ([M+H]"^) 43.3 (RS)-2-C4-Bromo-2-fluoro-phen^)-N-(4-cyano-benzyl)-2-propoxy-acetarnide was converted to (RS)-2-(4-bromo-2-fluoro-pheDyl)-N-(4-carbainimidoyl-beiizyl)-2-propoxy- acetamide hydrochloride according to general procedure D. Colorless solid. MS 423.3 ([M+H]^) Example 44 44.1 2-Fluoro-4-(trifluoromeUiyI)benzaldehyde was converted to (RS)-(2-fluoro-4-trifluoromethyl-phenyl)-methoxy-acetic add according to general procedure A. Light yellow gum. 44.2 (RS)-(2-Fluoro-4-triiluorometh)i-phenyI)-methoxy-acetic acid was coupled with 4-aminomethyl benzonitrile according to general procedure C to give CRS)-N-(4-cyano-benzyl)-2-{2-fluoro-4-trifIuoroinethyI-phen>d)-2-inethox7-acetaniide. Light yellow gum. 44.3 (RS) -N- (4-Cyano-benzyI)-2 - (2-fluoro-4-trifluoromethyl-phenyI)-2-methoxy-acetamide was converted to (RS)-N-{4-carbaniii[iidoyl-benzyl)-2-(2-fluoro-4-trifluoromethyl-phenyl)-2-inethoxy-acetainide hydrochloride according to general procedure D. Off-white soUd. MS 384.2 C[M+H]*) Example 45 45.1 In analogy to example 16.4, (RS)-N-(4-cyano-benzyl)-2-(4-hydroxy-phenyl)-2-methoxy-acetamide (example 21.2) was alkylated with bromoethanol/cesium carbonate in DMF to give (RS)-N-(4-cyano-benzyl)-2-[4-{2-hydroxy-ethoxy)-phenjd]-2-methoxy-acetamide as a colorless oil. MS 363.1 ([M+Na]"") 45.2 (RS)'N-(4-Cyano-benz}d)-2-[4-(2-hydroxy-ethoxy)-phen}^]-2-methoxy-acetaniide was converted to {RS)-N-(4-carbaniimidoyl-benzyl)-2-[4-(2-hydroxy-ethoxy)-phenyl]-2-methoxy-acetamide hydrochloride according to general procedure D. Colorless foam. MS 358.2 {[M-FH]"") Example 46 46.1 4-DimethyIaniinobenzaIdehyde was converted to (RS)-(4-dimefh}damino-phen)d)- methoxy-acetic add according to general procedure A. Light brown foam. MS 208.2 ([M- 46.2 (RS)-(4-0imeth)damLno-phenyI)-methoxy-acetic add was coupled with 4-aminomethyl benzonitrile according to general procedure B to give (RS)-N-(4-cyano-benz)d)-2-(4-dimethylamino-phenyl)-2-methoxy-acetaniide. Off-white solid. MS 324.2 ([M+H]"*") 46.3 (RS)-N-(4-Cyano-benzyi)-2-{4-dimethylamino-phenyl)-2-methoxy-acetamide . was converted to (RS)-N-(4-carbamimidoyl-benzyi)-2-(4-diniethylamino-phenyl)-2-methoxy- acetamide hxdrochloride according to general procedure D. Colorless solid. MS 341.2 ([M+H]") Example 47 47.1 3-Oxo-3,4-dihydro-2H-ben2o[l,4]oxaziiie-6-carba]dehyde (CAS 200195-15-9) was reacted according to general procedure A using methanol / dioxane as a solvent. The product of this reaction was subsequendy coupled with 4-aminomethyl benzonitrile according to general procedure C to give (RS)-N-(4-cpno-beiizyl)-2-methoxy-2-(3-oxo-3,4-dihydro-2H-benzo[l,4]oxazin-6-)d)-acetamide. Light yellow solid. 47.2 (RS)-N-(4-Cyano-benz)d)-2-methoxy-2-(3-oxo-3,4-dihydro-2H-benzo[l,4]oxazin-6-jd)-acetamide was converted to (IlS)-N-(4-carbaniimidoyl-benzyl)-2-methoxy-2-(3-oxo-3,4-dihydro-2H-benzo[l,4]oxa2in-6-yI)-acetamide hydrochloride according to general procedure D. Off-white sohd. MS 369.2 ([M+H] *) Example 48 48.1 4-(l-Pyrrolidino)benzaldehyde was reacted according to general procedure A using methanol I ioxane as a solvent. The product of this reaction was subsequently coupled with 4-aminomethyl benzonitrile according to general procedure B to give (RS)-N-(4-cyano-benz)d)-2-methoxy-2-(4-pyrroUdin-l-yl-phenyl)-acetaiinde, Off-white solid. MS 350.4 ([M+H]^) 48.2 (RS)-N-(4-Cyano-benzyl)-2-methoxy-2-(4-pyrrolidin-l-yi-phenyl)-acetamide was converted to (RS)-N-(4-caTbaniimidoyl-benzyl)-2-methoxy-2-(4-pyrroKdm-l-)d-phenyl)-acetamide hydrochloride according to general procedure D. Light red foam. MS 367.2 (EM+Hin Example 49 49.1 2-Chloroben2aldehyde was converted to (RS)-(2-chloro-phenyI)-methoxy-acetic acid according to general procedure A. Li^t yellow oil. MS 198.9 ([M-H]") 49.2 (RS)-(2-Chloro-phenyl)-methoxy-acetic acid was coupled with 4-aininomethyl benzonitrile according to general procedure B to give (RS)-2-(2-chIoro-phenyl)-N-(4-c7ano-beii27l)-2-methoxy--acetamide. Light yellow oil. MS 315.1 ([M+H]"^} 49.3 (RS)-2'(2'Chloro-phenyl)-N-(4-cyano-ben2yl)-2-methoxy-acetaniide was converted to i {RS)-N-C4-carbamimidoyi-benz;>d)-2-(2-cliIoro-phenyl)-2-methoxy-acetaimde hydrochloride according to general procedure D. Off-white, amorphous solid. MS 332.2 ([M+H]"') Example 50 50.1 4-Acetainidbenzaldehyde was converted to (RS)-(4-acetyian]ino-phen)d)-methoxy-acetic acid according to general procedure A. Yellow, amorphous solid. MS 222.0 {[M-H]') 50.2 (RS)-(4-Acetylamino-phen)^)-methoxy-acetic add was coupled with 4-aminomethyl benzonitrile according to general procedure B to give (RS)-2-(4-acetyianiino-phenyl}-N-(4-cyano-benzyI)-2-methoxy-acetamide. Off-white, amorphous solid. MS 338.3([M+H]"*') 50.3 (RS)-2-(4-Acetylamino-phenyl)-N-(4-cyano-ben2yl)-2-methoKy-acetaniide was converted to (RS}-2-(4-acetylanuno-phenyl)-N-(4-carbamimidoyl-benzyl)-2-methoxy-acetamide hydrochloride according to general procedure D. Orange amorphous soKd. MS 355.2 {[M+H]^) Example 51 51.1 4-(Trifluoromethoxy)benzaldehyde was converted to (RS)-methoxy-{4-trifiuoromethoxy- phenyl)-acetic add according to general procedure A. Light yellow oil. MS 249.3 ([M-H]") 51.2 {RS)-Methoxy-(4-tri£luoromethoxy-phenyl)-acetic add was coupled with 4-aminomethyl benzonitrile according to general procedure B to give (RS)-N-(4-cyano-ben2yl)-2- methoxy-2-{4-trifluoromethoxy-phenyI)-acetaniide. Light blue semisolid. MS 365.2 ([M+H]^) 51.3 CRS)-N-(4-Cyano-benz)^)-2-methoxy-2-(4-trifluoroniethoxy-phenyl)-acetamide was converted to (RS)-N-(4-carbaminiidoyl-ben2yi)-2-methoxy-2-(4-trifluoromethoxy- phenyl)-acetamide hydrochloride according to general procedure D. Off-white amorphous sohd. MS 3S2.3 ([M+HD Example 52 52.1 l-{4-Fonnylphenyi)-lH-imidazole was reacted according to general procedure A using methanol / dioxane as a solvent. The product of this reaction was subsequently coupled with 4-aininomethjd benzonitrile according to general procedure B to give {RS)-N-(4-cyano-ben2:jd)-2-(4-imidazol-l-yl-phenyl}-2-methoxy-acetamide. Colorless foam. MS 347.2 ([M+H]^) 52.2 (RS)-N-{4-Cyano-benzyl)-2-(4-imidazol-l-yl-phenyl)-2-methoxy-acetaniide was converted to (RS)-N-(4-carbamimidoyl-ben2yl)-2-(4-imidazol-l-yl-ph,enyl)-2-methoxy- acetamide hydrochloride according to general procedure D. Light yeJlow solid. MS 364.3 ([M+H]*) Example 53 53.1 6-Methoxy-2-naphtaldehyde was converted to {RS)-methoxy-(6-methoxy-naphthalen-2- yl)-acetic add according to general procedure A. light yellow solid. MS 245.2 ([M-H]") 53.2 {RS)-Methoxy-(6-methoxy-naphthalen-2-)d)-acetic acid was coupled with 4-aminometh)d benzonitrile according to general procedure C to give (RS)-N-(4-cyano-benzyl)-2-methoxy-2-(6-methoxy-naphthalen-2-yl)-acetamide. Off-white foam. MS 361.2 ([M+H]*) 53.3 {RS)-N-{4-Cyano-benZ)d)-2-methoxy-2-(6-methoxy-naphthalen-2-)d)-acetamide was converted to (RS)-N-(4-carbamiinidoyI-ben2yi)-2-methoxy-2-(6-methoxy-naphthalen-2- )d)-acetamide hydrochloride according to general procedure D. Off-white soUd. MS 378.3 ([M+H]^) Example 54 54.1 4-Morpholinobenzaldehyde was reacted according to general procedure A using methanol / dioxane as a solvent The product of this reaction was subsequently coupled with 4-aminomethyl benzonitrile according to general procedure B to give (RS)-N-(4-cyano- benzyl)-2-methox)'-2-(4-inorpliolm-4-yl-phenyl)-acetamide. Orange oil. MS 366.2 ([M+H]^) 54.2 (RS)-N-(4-Cyano-ben2)d)-2-methoxy-2-(4-morplioUn-4-yl-phenyi)-acetamide was converted to (RS}-N-{4-carbaininiidoyl-benzyI)-2-methoxy-2-(4-morpho]iii-4-yl-phenyl)-acetamide hydrochloride according to general procedure D. Orange foam. MS 383.3 {[M+H]*) Example 55 55.1 2-MorphoIinoben2aIdehyde was reacted according to general procedure A using methanol / dioxane as a solYent. The product of this reaction was subsequently conj^ed with 4-aminomethjd benzonitrile according to general procedure B to give (RS)-N-(4-cyano- benzyl)-2-methoxy-2-(2-morpholin-4-yl-phenyl)-acetamide. Orange oil. 55.2 (RS)-N-(4-Cyano-benz)d)-2-methoxy-2-(2-morpholin-4-yl-phenyI)-acetamide was converted to (RS)-N-(4-carbamirnidoyl-benzyl)-2-methoxy-2-(2-morpholin-4-yl-phenyI)-acetamide hydrochloride according to general procedure D. Light brown foam. MS 383.3 ([M+H]*) Example 56 56.1 4-[3-(Dimethylamino)propoxy] benzaldehyde was reacted according to general procedure A using methanol / dioxane as a solvent The product of this reaction was subsequently coupled with 4-aniinomethyl benzonitrile according to general procedure B to give (RS)-N-(4-cyano-benzyl)-2- [4-(3-dimethylarnino-propoxy)-phenyI] -2-methoxy-acetamJde. Colorless solid. MS 382.3 ([M+H]"") 56.2 (RS)-N-(4-Cyano-benzyI)-2-[4-(3-dimeth)4amino-propoxy)-phenyI]-2-methoxy-acetamide was converted to (RS)-N-(4-carbamiraidoyl-benzyi)-2-[4-(3-dimethyiamino-propoxy)-phenyl]-2-methoxy-acetamide hydrochloride according to general procedure D. Colorless soUd. MS 399.2 ([M+H]"") Example 57 57.1 To a stirred solution of (RS)-2-(4-bromo-2-fluoro-phenyl)-N-(4-cyano-benzyl)-2-methoxy-acetamide (example 41.2, 173 mg) in 1,2-diniethoxyethane (8 ml) were added PdQiCdppf) (34 mg), an aqueous 10% solution of Na2C03 (2 ml) and 4-dimethylaminophenylboronic acid (378 mg). The mixtuie was then stirred at 85 "C under an argon atmosphere for 1.5 h. After cooling to r.t. the mixture was diluted witii ethyl acetate (15 ml) and washed with water (10 ml). The aqueous layer was extracted with ethyl acetate and the combined organics were washed with water and brine, dried (MgS04), filtered and concentrated. The product was purified by chromatography (silica gel, gradient cyclohexane => cyclohexane / ethyl acetate 2:3) to give (RS)-N-(4-cyano-benz)i)-2-(4'-dimethylamino-3-fluoro-biphen)d-4-yl)-2-methoxy-acetamide (167 mg) as a Hght yellow solid. 57.2 (RS) -N- (4-Cyano-benzyl)-2- (4'-dimethyiamino-3-fiuoro-biphenyl-4-yl)-2-methoxy-acetamide was converted to (RS)-N-(4-carbamimidoyl-benzyl)-2-(4'-dimeth)danuno-3-fiuoro-biphenyl-4-)4)-2-methoxy-acetamide hydrochloride according to general procedure D. Off-white solid. MS 435.4 ([M+H]"") Example 58 58.1 In analogy to example 57.1, (RS)-2-(4-bromo-2-fiuoro-phenyI)-N-(4-cyano-benz>i)-2- methoxy-acetamide (example 41.2) was reacted with 4-methoxyphen>^oronic add to give (RS)-N-(4-cyano-benzyi)-2-(3-fluoro-4'-methoxy-biphenyl-4-)d)-2-methoxy-acetamide. Off-white solid. 58.3 (RS)-N-(4-Cyano-ben2;)d)-2-(3-fluoro-4'-methoxy-biphenyl-4-yl)-2-methoxy-acetamide was converted to (RS)-N-(4-carbamirmdoyi-benzyl)-2-(3-fluoro-4'-niethoxy-biphenyl-4- }^)-2-medioxy-acetamide hydrochloride according to general procedure D. White solid. MS 422.3 ([M+H]"") Example 59 59.1 In analogy to example 57.1, (RS)-2-(4-bromo-2-fluoro-phenyl)-N-(4'Cyano-ben2yl)-2- medioxj^-acetamide (example 41.2) was reacted with 2-methoxyphenylboromc add to give (RS)-N-(4-cyano-benzyI}-2-(3-£Iuoro-2'-methoxy-biphenyl-4-yI}-2-methoxy-acetamide. Light yellow gum. 59.2 CRS)-N-(4-Cyano-ben2yl)-2-(3-fluoro-2'-methoxy-biphenyl-4-yl)-2-methoxy-acetamide was converted to (RS)-N-(4-carbaiminidoyi-ben2yI)-2-(3-fluoro-2'-methoxy-biphenyI-4-yl)-2-methoxy-acetainide hydrochloride according to general procedure D. Off-white solid. MS 422.3 ([M+H]*) Example 60 60.1 In analogy to example 57.1, ,(RS)-2-(4-bromo-2-fiuoro-phenyl)-N-(4-cyano-benzyl)-2-methoxy-acetamide (example 41.2) was reacted with phenyiboronic acid to give (RS}-N-{4-cyano-benzyl)-2-(3-fluoro-biphenyl-4-yi)-2-methoxy-acetaniide. Light yellow gum. 60.2 (RS)-N-(4-Cyano-benzyI}-2-(3-fluoro-biphenyl-4-yi)-2-methoxy-acetamide was converted to (RS)-N-(4-carbamimidoyl-benzyl)-2-(3-fluoro-biphenyl-4-yl)-2-methoxy-acetamide hydrochloride according to general procedure D. White solid. MS 392.3 {[M+H]"*") Example 61 61.1 In analogy to example 57.1, ,(KS)-2-{4-bromo~2-fluoro-phen)d)-N-(4-cyano-ben27l)-2- methoxy-acetamide (example 41.2) was reacted with 3-methoxyphen)dboroDic add to give (RS)-N-(4-c)^no-ben2)d)-2-(3-fluoro-3'-methoxy-biphen)i-4-yl)-2-methoxy-acetamide. Light yellow gum. 6U (RS)-N-(4-Cyano-benzyi)-2-(3-fluoro-3'-methoxy-biphenyl-4-yi)-2-methoxy-acetamide was converted to (RS)-N-(4-carbaminiido)4-benz)d}-2-(3-fluoro-3'-methoxy-biphen)d-4-yl)-2-methoxy-acetamide hydrocbloride according to general procedure D. White soHd MS 422.3 ([M+H]"-) Example 62 62.1 2,2-Dimethylchromane-6-carbaldehyde was converted to (RS)-{2,2-dimethyl-chroman-6-5d)-methoxy-acetic add according to general procedure A. Light yellow oil. MS 249.1 ([M- 62.2 (RS)-(2,2-Diineth7l-chroman-6-yl)-methoxy--acetic acid was coupled with 4-aiiunometh7l benzonitrile according to general procedure C to give (RS)-N-(4-cyano-beii2yI)-2-(2,2-diinethyl-chroman-6-yl)-2-methDxy-acetamide. Off-white semi-solid. MS 365.2 ([M+H]"") 62.3 (RS)-N-(4-Cyano-benzy]}-2-{2,2-dimethyI-chroman-6-yl)-2-methoxy--acetamide was converted to (RS)-N-(4-carbamimidoyl-benzyl)-2-{2,2-dimethyi-chroman-6--54)-2-methoxy-acetamide hydrochloride according to general procedure D. Light yellow solid. MS3S2.4([M+H]^) Example 63 63.1 2-FIuoro-4-methoxyben2aldehyde was converted to (RS)-ethoxy-(2-fluoro-4-methoxy-phen)^)-acetic add according to general procedure A using ethanol / dioxane as a solvent Yellow oil. MS 227.2 ([M-H]") 63.2 (RS)-EthoKy-(2-fluoro-4-niethoxy-phenyl)-acetic acid was coupled with 4-aminoinethyl benzonitrile according to general procedure B to give (RS)-N-(4-cyano-benZ)^)-2-ethoxy-2-(2-fluoro-4-medioxy-phenyl)-acetamide. Yellow oil. MS 343.2 ([M+H]*) 63.3 (RS)-N-(4-Cyano-benzyi)-2-edioxy-2-(2-fluoro-4-inethoxy-phen)d)-acetamide was converted to (RS)-N-{4-carbanuniidoyl-ben2yI)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide hydrochloride according to general procedure D. Colorless foam. MS 360.3 {[M+H]^) 63.4 In analogy to example 15.5, give (RS)-N-(4-cyano-benzyi)-2-ethoxy-2-{2-fluoTO-4-methoxy-phenyl)-acetamide (example 63.2) was converted to (RS)-2-ethoxy-2-(2-£Iuoro-4-methoxy-phen}d)-N-[4-(N-hydroxycarbamimidoyl)-benz)4]-acetainide. Colorless foam. MS 376.3 ([M-^H]^) Example 64 64.1 3-(Cydopentyloxy)-4-methoxy-benzaldehyde was converted to (RS)-{3-cyclopentyloxy-4- methoxy-phenyl)-methoxy-acetic acid according to general procedure A. Yellow oil. MS 279.2 ([M-H]-) 64.2 (RS)-(3-Cydopentyloxy-4-methoxy-phenyl)-methoxy-acetic add was coupled with 4-aminomethyl benzonitrile according to general procedure B to give (RS)-N-(4-cyano-ben2yl)-2-(3-c7dopentjdoxy-4-methoxy-pheiiyi)-2-methoxy-acetainide. Colorless solid. 64.3 (RS)-N-(4-Cyano-benzyl)-2-(3-cydopentyloxy-4-metboxy-plienyI)-2-methoxy-acetainide was converted to (RS)-4-[3-{3-cyclopentyloxy-4-metIioxy-phen-)d)-3-methoxy-2-oxo-puQpylaminoj-benzamidine hydrochloride according to general procedure D. Off-white foam. MS 412.4 ([M+H]"") Example 65 65.1 2-Cfaloro-4-methoxybenzaldehyde (CAS No: 54439-75-7) was converted to CRS}-(2-chloro-4-methoxy-phenyl)-inethosy-acetic add according to general procedure A. Yellow oil. MS 228.9 ([M-H]") 65.2 {RS)-(2-Chloro-4-inethoxy-phenyl)-methoxy-acetic add was coupled with 4-aminomethyI benzonitrile according to general procedure B to give (RS)-2-(2-chloro-4-methoxy-phenyl)-N-(4-cyano-benzyl)-2-methoxy-acetainide. Light yellow oiL MS 345.2 ([M+H]"*) 65.3 (RS)-2-(2-Chloro-4-methoxy-phenyi)-N-{4-cyano-benzyl)-2-methoxy-acetamide was converted to (RS)-N-(4-caTbaiminidoyl-beiizyl)-2-(2-diloro-4-niethoxy-phenyl)-2-methoxy-acetamide hydrochloride according to general procedure D. Colorless foam. MS 362.2 ([M+H]-') Example 66 66.1 2,6-DifluDrQ-4-methoxybenzaldehyde (CAS No: 256417-10-4) was converted to (RS)-(2,6-difluoro-4-methoxy"phenyl)-methoxy-acetic add according to general procedure A. YeUow oil. MS 230.9 ([M-H]') 66.2 (RS)-(2,6-Difluoro-4-methoxy-phen}d)-methoxy-acetic add was coupled with 4-aminometbjd benzonitrile according to general procedure B to give (RS)-N-(4'cyano-benzyl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-methoxy-acetaniide. Light yellow amorphous soUd. MS 347.1 ([M+H]*) 66.3 (RS)-N-(4-Cyaiio-benz)4)-2-(2,6-diiluoro-4-methoxy-phen7i)-2-methoxy-acetaimde was converted to {RS)--N-(4-carbamimidoyl-benzyi)-2-C2,6-difiuoro-4-metboxy-phen)d)-2-methoxy-acetaroide hydrochloride according to general procedure D. Colorless foam. MS 364.2 {[M+Hf) Example 67 67.1 2-Fluoro-4-inethoxybenzaldehyde was reacted according to general procedure A using n-propanol / dioxane as a solvent The product of this reaction was subsequently coupled ■with 4-aminomethyl benzonitiile according to general procedure B to give (RS)-N-(4-cyano-benzyl)-2-{2-fiuoro-4-niethoxy-phenyl)-2-propoxy-acetamide. Light yellow oil. MS 357.2 ([M+H]"") 67.2 (RS)-N-(4-Cyano-benz>d)-2-{2-fluoro-4-methoxy-phenyl)-2-propoxy-acetaniide was converted to (RS)-N-(4-carbamiinidoyl-beiiz)d)-2-(2-fluoro-4-metiioxy-phenyl)-2-propoxy-acetamide hydrochloride according to general procedure D. Colorless foam. MS 374.2 ([M+H]"} Example 68 68.1 2-Methoxy-2-{l-naphtyl)propionic acid was coupled with 4-aminomethj4 benzonitrile according to general procedure B to give (RS}-N-(4-cyano-benzyl)-2-methoxy-2-naphthalen-l-yl-propionamide. Colorless foam. MS 345.2 ([M+H]*) 68^ (RS)-N-(4-Cyano-ben2yi)-2-methoxy-2-naphthalen-l-yl-propicnamide was converted to (IlS)-N-(4-carbamimidoyl-beiizyl)-2-methoxy-2-naphthalen-l-^-propionamide hydrochloride according to general procedure D. Colorless foam. MS 362.2 ([M+H] ) Example 69 69.1 A solution of l-bromo-3,5-difluorobenzene (16.8 g) in THE (180 ml) was cooled to -75 °C under an argon atmosphere. A 2 M solution of Uthiumdiisopropyiamide in THE / heptane / ethylbenzene (43.1 ml) was slowly added at below -70 "C The mixture was stirred at -78 "C for 1 h. Dimethylformamide (12.6 ml) was added and the mixture was stirred for 2 h. The cooling bath was removed and the mixture was slovrfy wanned to r.t. The mixture was diluted with diethyl ether and washed with 0.5 M HCI. The aqueous phase was extracted with diethyl ether. The combined organic phase was dried (MgS04), filtered and the solvent was removed to give the crude 4-bromo-2,6-difluorobeiizaldehyde (12.4 g). The crude aldehyde was reacted according to general procedure A using methanol / dioxane as a solvent. The product of this reaction was subsequently coupled with 4-aminomethjd benzonitrile according to general procedure B to give CRS)-2-(4-bromo-2,6-difluoro-phenyl)-N-(4-cyano-benzyl)-2-methoxy-acetamide. Yellow oil. MS 395.0 {[M+H]^) 69.2 (RS)-2-(4-Bromo-2,6-difluoro-phenyl)-N-(4-cyano-t>enzyl)-2-methoxy-acetamide was converted to (RS)-2-{4-bromo-2,6-difluoro-phenyl)-N-(4-carbaininiidoyl-benz)4)-2-methoxy-acetamide hydrochloride according to general procedure D. Off-white solid. MS 412.2 ([M+H]^) Example 70 70.1 In analogy to example 16.4, 2-fluDro-4-hydroxy-beiizaldehyde (CAS-No: 348-27-6) was alkylated with benzylbromide / potassium carbonate in DMF to give 4-benzyloxy-2-fluoro-benzaldehyde. OfF-white solid. MS 230.1 ([M+H]+) 70.2 4-Ben2yloxy-2-fluoro-benzaldehyde was converted to (RS)-(4-benz)doxy-2-fluoro- phenyO-methoxy-acetic acid according to general procedure A. White solid. MS 289.1 ([M-H]-) 70.3 (RS)-(4-Beiizyloxy-2-fluoro-phenyi)-methoxy-acetic add was hydrogenated at r.t. and normal pressure using 10% Pd/C as a catalyst and EtOH as a solvent to give (RS)-(2-fluoTO-4-hydroxy-phenyI)-methoxy-acetic acid as a hght yellow oil. MS 199.2 {[M-H]") 70.4 (RS)-(2-Fluoro-4-hydroxy-phenyl)-methoxy-acetic acid was coupled with 4-aininomethyl benzonitrile according to general procedure C to give {RS)-N-(4-cyano-benzyl)-2-(2-fluoro-4-hydroxy-phenyI)-2-inethoxy-acetamide. White solid. MS 315.1 ([M+H]'") 70.5 In analogy to example 16.4, (RS}-N-(4-cyano-benzyl)-2-(2-fiuoro-4-hydroxy-phenyl)-2- methoxy-acetamide was alkylated with 2-iodopropaiie and cesium carbonate in DMF to give (RS)-N-(4-cyano-benzyl)-2-f2-fluoro-4-isopropoxy-phenyl)-2-medioxy-acetaimde. Light yellow oil. MS 357.2 ([M+H]"") 70.6 (RS)-N-{4-Cyano-benz}d)-2-{2-fluoro-4-isopropoxy-phenyl)-2-inethoxy-acetainide was converted to (R.S)-N-(4-carbaiminidoyl-beiizyl)-2-{2-fluoro-4-isopropoxy-phenyl)-2-methoxy-acetamide hydrochloride according to general procedure D. Off-white solid. MS 374.2 ([M+H]') Example 71 71.1 In analogy to example 16.4, (RS)-N-(4-cyano-ben2yi)-2-(2-fluoro-4-hydroxy-phenyI}-2-methoxy-acetamide (example 70.4) was alkylated with l-iDdo-2-methylpropane and cesium carbonate in DMF to give (RS)-N-C4-cyano-benzyI}-2-(2-fluoro-4-isobutoxy-phenyl)-2-methoxy-acetamide. Off-white, amorphous solid. MS 371.3 ([M+H]"^) 71.2 (RS)-N-(4-Cyano-ben2y[)-2-{2-fluoro-4-isobutoxy-phenyi)-2-methosy-acetaiiiide was converted to (RS)-N-{4-carbamimido)^-benzyi)-2-(2-fluoro-4-isobutoxy-phen)d)-2-methoxy-acetamide hydrochloride according to general procedure D. Off-white solid. MS 388.3 ([M+H]^) Example 72 72.1 Li analogy to example 22.1, (RS)-N-(4-cyano-benzyl)-2-(2-fiuoro-4-hydroxy-pbenyI)-2-methoxy-acetamide (eisample 70.4) was reacted with 4-fl.uorophenethyl alcohoU diethyl azodicarboxylate and triphenyl-phosphine in THF to give (RS)-N-{4-cyano-benzyI)-2-{2-fluoro-4'[2-(4-fiuoro-phenyl)-ethoxy]-phenjd}-2-methoxy-acetamide. Colorless oil. MS 437.3 ([M+H]-") 72.2 (RS)-N-{4-Cyano-beiizyl)-2-{2-fiuoro-4-l2-(4-fluoro-phenyl)-ethoxy}-phenyl}-2-methoxy-acetamide wa^ converted to (RS)-N-(4-carbamitnidQyl-ben2yl)-2-{2-fluoro-4-[2-{4-fluoro-phenyl)-etfaoxy]-phenyl}-2-methoxy-acetarnide hydrochloride accordiR2 to general procedure D. Off-white, amorphous solid. MS 454.5 {[M+H]"*") Example 73 73.1 To a stirred solution of {RS)-2-(4-bromo-2-fiuoro-phenyl)-N-{4-cyano-benzyl)-2-methoxy-acetamide (example 41.2, 1,16 g) at r.L in dioxane were added bis(pinacolato)diboron (1.17 g) and potassium acetate (0.91 g). The mixture was purged with argon and bis(triphenylphospiune)palladium(II) chloride (0.13 g) was added. The mixture was then stirred at 80°C under an argon atmosphere for 18 L The solids were filtered off and washed with EtOAc. The filtrate was concentrated to leave the crude product as a dark brown oil. The product was isolated by chromatography (silica gel, gradient cyclohexane => cydohexane/EtOAc 3:2) to give (RS)-N-(4-cj^no-ben2yl)'2-[2-fluoro-4-(4,4,5,5-tetramethyl-[l,3)2]dioxaborolan-2-}4)-phenyI]-2-methoxy-acetamide as brown oil (0.64 g). Brown oil. MS 425.4 ([M+H]"") 73^ In analogy to example 57.1 (RS)-N-(4-cyano-benzyl)-2-[2-fluoro-4-(4,4.5,5-tetramethyl-[l,3,2]dioxaboroIan-2-yl)-pheDyl]-2-methoxy-acetamide was reacted with 3-bromopyridine to give (RS)-N-(4-cyano-benzyl)-2-(2-fiuoro-4-pyridin-3-yl-phenyI)-2-methoxy-acetamide. Light brown amorphous soHA MS 376.3 ([M+H]"*") 73.3 (RS)-N-(4-Cyano-ben2yl)-2-(2-fluoro-4-pyridin-3-yl-phenyl)-2-methoxy-acetamide was converted to (RS)-N-(4-carbamiraido)d-benzyl)-2-(2-fluoro-4-pyridin-3-yl-phenyl)-2-methoxy-acetamide; hydrochloride according to general procedure D. Off-white solid. MS 393.2 ([M+H]-") Example 74 74.1 In analogy to example 57.1 (RS)-N-(4-cyano-ben2yl)-2-[2-fluoro-4-(4,4,5,5-tetramethyl- [i,3,2]dioxaborolan'2-)d)-phenyl]-2'raethoxy-acetaniide (example 73.1) was reacted with 4-bromopyridine, hydrochloride to give (RS)-N-(4-cyano-benzyl)-2-(2-fluoro-4-pyridin-4-yl-phenyl)-2-methoxy-acetamide. Li^t brown amorphous solid. MS 376.3 ([M+H] ) 74.2 (RS)-N-(4-cyano-benzyl)-2-(2-fluoro-4-pyridin-4-yl-phenyl)-2-methoxy-acetamide was converted to (RS)-N-(4-carbamimidoyl-benzyl)-2-(2-fluoro-4-pyridin-4-yl-phenyl)-2-methoxy-acetamide; hydrochloride according to general procedure D. Off-white soHd. MS 393.2 {[M+H]^) Example 75 75.1 5-Bromo-2-fluorobenzaIdehyde was converted to (RS)-{5-bromo-2-fluoro-phenyl)-methoxy-acetic acid according to general procedure A using methanol/dioxane as solvent LightyeUowliquid. MS 262.0 ([M-H]") 75^ (RS)-(5-Bromo-2-fluoro-phenyl)-methoxy-acetic add was reacted with 4-aminomethyl benzonitrile according to general procedure C to give (RS)-2-(5-bromo-2-fiuoro-phenyl)-N-{4-cyano-benzyI)-2-methoxy-acetamide. Colorless solid. MS 377.2 ([M+H]"") 75.3 (RS)-2-(5-Bromo-2-fiuoro-pbenyl)-N-(4-cyano-benzyl)-2-methoxy-acetamidewas converted to (RS}-2-(5-bromo-2-fluoro-phenyl)-N-(4-carbanmnidoyI-benzyI)-2-methoxy-acebimide; hydrochloride according to general procedure D. Colorless soKd. MS 394.0 ([M+H]"*") Example 76 76.1 In analogy to example 57.1 give {RS)-2-(5-bromo-2-fluoro-phen)d)-N-(4-cyano-benzyl)-2-methoxy-acetannde (example 75.2) was reacted with phenylboronic acid to give (R£)-N-(4-cyano-benzyl)-2-(4-fiuoro-bipheayl-3-yi)-2-methoxy-acetamide. Off-white solid. MS I 374.1 (M). 76.2 (RS)-N-(4-Cyano-benzyI)-2-(4-fluoro-bipben)4-3-yl)-2-methoxy-acetamide was converted to (RS}-N-(4-carbamimidoyl-benzyl)-2-(4-fluoro-biphen)i-3-)d)-2-methoxy-acetamide; hydrocfaloride according to general procedure D. Colorless solid. MS 392.2 ([M+H]"^) Example 77 77.1 2-Fluoro-5-methyiben2aldehyde was converted to (RS)-{2-fluoro-5-meth)d-phen)d)-methoxy-acetic acid according to general procedure A using methanol/dioxane as solvent. Off-white liquid. MS 197.1 ([M-H]') 77.2 (RS)-(2-Fluoro-5-methyl-phenyi)-methoxy-acetic acid was reacted with 4-aminDmethyl benzonitrile according to general procedure C to give (RS)-N-(4-cyano-benzyl)-2-(2- fluoro-5-methyl-phenyI)-2-inethoxy-acetamide. Colorless amorphous solid MS 313.2 ([M+H]^) 773 (RS)-N-(4-Cyano-benz)d)-2-(2-fluoro-5-methyl-phenyI)-2-methoxy-acetamidewas converted to (RS)-N-(4-carbainmiidoyl-benzyl)-2-(2-fluoro-5-inethyl-phenyl)-2-methoxy-acetamide; hydrochloride accordmg to general procedure D. Colorless soUd. MS 330.2 ([M+H]"") Example 78 78.1 5-{Trifluoromethyl)-2-fiuorobenzaldehyde was converted to (RS)-(2-fluoro-5-trifluoromethyl-phenyl)-methoxy-acetic add according to general procedm-e A using methanol/dioxane as solvent. Colorless amourphous solid. MS 251.1 {[M-H]') 78.2 (RS)-(2-Fluoro-5-trifluoromethyl-phenyl)-methoxy-acetic add was reacted with 4-aminomethyl benzonitrile according to general procedure C to (RS}-N-(4-cyano-benzyl)-2-{2-fluoro-5-trifluoromethyl-phenyl)-2-methoxy-acetamide. Colorless amorphous solid. MS 367.1 {[M+H]"'} 78.3 {RS) -N-(4-Cyano-benzyi)-2- (2-fluoro-5-trifluoromethjd-phenyl)-2-methoxy-acetamide was converted to (RS)-N-C4-carbamiinidoyI-benzyi)-2-(2-fluoro-5-triflaoromethyl-phen5d)-2-methoxy-acetamide; hydrochloride according to general procedure D. Example 79 79.1 2-Fluoro-6-methoxybenzaldehyde was converted to (RS)-(2-fluoro-6-methoxy-phenyl)-methoxy-acetic acid according to general procedure A using methanol/dioxane as solvent. Off-white Hquid. MS 213.1 ([M-H]-) 79.2 (RS)-{2-Fluoro-6-methoxy-phenyl)-methoxy-acetic add vfas reacted with 4-aminomethyl benzonitrile according to general procedure C to {RS)-N-(4-cyano-benzy!)-2-(2-fIuoro-6-methoxy-phenyI)-2-methoxy-acetamide. Colorless soUd. MS 329.2 ([M+H]"^) 79.3 (■RS)-N-(4-Cyano-ben2yl)-2-(2-fl.uoio-6-methoxy-phen-^)-2-meth.oxy-acetainidewas converted to (RS)-N-(4-carbamimidoyl-benzyl)-2-(2-fluoro-6-inethoxy-phenyl)-2-methoxy-acetamide; hydrochloride according to general procedure D. Example 80 80.1 A solution of O-benzyl-3-fluorobenzene (4.66 g) in THF (50 ml) was cooled to -65°C. n-Buthyllithium in hexane (1.5 M, 15.8 ml) was added within 15 minutes. The reaction mixture was stirred at -eS'C for 30 minutes. Then DMF (1.95 ml) was added dropwise. The reaction mixture was wanned to r.t. overnight, then poured onto ice and extracted with ethji acetate. The oi^anic layers were washed with brine, dried over MgS04 and concentrated to give (RS)-2-benz>doxy-6-f!uoro-benzaldehyde (4.66 g). Yellow Uquid. MS 230.1 ([M]). 80.2 (RS)-2-Benzyloxy-6-fluoro-benzaIdehyde was converted to (RS)-(2-benzyloxy-6-fluoro-phenyl)-methoxy-acetic add according to general procedure A using methanol/dioxane as solvent YeUowHquid. MS 289.1 ([M-H]") 80.3 Inanalogyto example 16.2 (RS)-(2-benzyioxy-6-fluoro-phenyl)-methoxy-aceticaddwas converted to (RS)-(2-fluoro-6-hydroxy-phenyl)-methoxy-acetic add Colorless amorphous solid. MS 199.1 ([M-H]") 80.4 (RS)-(2-FIuoro-6-hydroxy-phenyl)-methoxy-acetic add was reacted with 4-aminometh)1 benzonitrile according to general procedure C to give (RS)-N-(4-cyano-benzyl)-2-(2-fluoro-6-hydroxy-phenyl)-2-methoxy-acetamide. Colorless solid. MS 315.1 ([M+H]"^) 80.5 (RS)-N-(4-Cyano-ben2yi)-2-(2-fiuoro-6-hydroxy-phenyl)-2-methoxy-acetamide was converted to (RS)-N-(4-carbaniimidoyl-benzyI)-2-(2-fluoro-6-hydroxy-phenyl)-2-methoxy-acetamide; hydrochloride according to general procedure D. Example 81 8L1 a-Bromophenylacetic add was reacted with 4-aminomethyl benzonitrile according to general procedure C to give (RS)-2-bromo-N-(4-cyano-benzyl)-2-phenyl-acetamide. White solid. MS 329.1 ([M+H]^) 81.2 To a stirred solution of {RS)-2-bromo-N-(4-cyano-ben2yl)-2-phenyI-acetainide (200 mg) in THF (10 ml) at r.t under an Ar atmosphere were added dimethylamine, hydrochloride (149 mg), trieth}iamine (0.42 ml) and tetrabutylammonium iodide (34 mg). The reaction mixture was stirred for 19 hrs, then treated with additional dimethjiamine, hydrochloride (149 mg) and triethylamine (0.42 ml). After another 8 hrs stirring at r.t., the soUds were filtered off and washed with EtOAc. The filtrate was washed with water and brine, dried over MgS04 and concentrated. The product was isolated by chromatography (siHca gel, gradient dichloromethane => dichlofomethane/MeOH 9:1) to give (RS}-N-(4-cyano-benzyI)-2-dimethylamino-2-phenyl-3cetamide (165 mg). Orange solid. MS 294.3 ([M+H]^) 81.3 (RS)-N-(4-Cyano-benzyl)-2-dimethylamino-2-phenyl-acetamide was converted to (RS)-N-(4-carbamimidoyI-benzyl)-2-dimethylamino-2-phenyl-acetamide; hydrochloride according to general procedm-e D. Off-white solid. MS 311.2 ([M+H]"^) Example 82 82.1 In analogy to example 81.2 of (RS)-2-bromo-N-(4-cyano-ben2yl)-2-phenjd-acetaniide (example 81.1) was reacted with methylamine, hydrochloride to (RS)-N-(4-cyano-benzyl)-2-methylamino-2-phenyl-acetamide. Off-white amorphous solid. MS 280.1 ([M+H]"^) 82.2 (RS)-N-(4-Cyano-ben2yl)-2-methylajnino-2-phen)i-acetamide was converted to (RS)-N-(4-carbamimidoyl-benzyl)-2-mediylamino-2-phenyl-acetamide; hydrochloride according to general procedure D. Off-white solid. MS 297.3 ([M+H]"*) Example 83 83.1 To a stirred solution of sodium methanethiolate (0.43 g) at r.t. in methanol (15 ml) were added the (RS)-2-bromo-N-(4-cyano-benzyl)-2-phenyl-acetamide (0.5 g, example 81.1) and a catalytic amount of tetrabutyl ammonium iodide. The mixture was then stirred at r.L for 1 hr. The mixture was concentrated. The residue was taken up in EtOAc, washed with 1.0 N and brine, dried over MgS04, filtered and concentrated. The product was isolated by chromatography (silica gel, cydohexane/EtOAc 2:1) to give (RS)-N-(4-cyano-benzyl)-2-methyIsuIfanyl-2-phenyl-acetamide (0.36 g). Colorless solid. MS 297.2 ([M+H]^) 83.2 (RS)-N-(4-Cyano-ben2yl)-2-methyIsulfanyl-2-phenyl-acetainide was converted to (RS)-N-(4-carbainiraidoyl-benz)d}-2-methylsulfenyl-2-phenyi-acetainide; hydrochloride according to general procedure D. Colorless solid. MS 314.2 ([M+H]"*") Example 84 84.1 In analogy to example 83.1 (RS)-2-bromo-N-{4-cyano-benz^)-2-phenyl-acetamide (example 81.1) was reacted with sodium ethanethiolate to give (RS)-N-{4-cyano-ben2yl)-2-eth)dsulfenyl-2-phenyl-acetamide. Off-white solid. MS 311.2 {[M+H]"^) 84.2 (RS)-N-{4-Cyano-benzyl)-2-ethylsulfanyl-2-phenyl-acetaniide was converted to (RS)-N-(4-carbaiiiiniidoyl-benzyI)-2-ethylsulfen>d-2-phenyl-acetaraide; hydrochloride accordiR2 to general procedure D. Colorless solid. MS 328.2 ([M+H]"^) Example 85 85.1 A solution of CRS)-N-(4-cyano-benzyl)-2-methylsu]fanyl-2-phen)d-acetaniide (0.11 g, example 83.1) in dichloromethane (10 ml) was cooled to -ICC and treated with mCPBA (0.27 g). The reaction mixture was stirred at 0°C, then diluted with dichloromethane and washed with aqueous sodium hydrogen sulfite solution. The organic layer was further washed with satinrated KHC03 solution and brine, dried over MgS04, filtered and concentrated. The product was isolated by chromatography (silica gd, gradient cyclohexane => EtOAc) to give (RS)-N-(4-cyaiio-benzyI)-2-methanesulfon)d-2-phen54-acetamide (0.084 g). White soUd. MS 329.2 ([M+H]"^) 85.2 (RS)-N-(4-Cyano-benzyl)-2-methanesulfon)i-2-phenyl-acetamide Vfas converted to (RS)-N-(4-carbamimido)d-benzyi)-2-metlianesulfonyl-2-phenyl-acetamide; hydrochloride according to general procedure D. Colorless sohd. MS 346.1 ([M+H]"^) Example 86 86.1 Boc-DL-phenyiglycine was reacted with 4-aniinomethyl benzonitrile according to general procedure C to give (RS)-[(4-cyano-benzylcarbamoyl)-phen)d-methyl]-carbamic acid tert-butyl ester. Off-white sohd. MS 366.2 ([M-hH]"") 86.2 (RS}-[(4-Cyano-benz7lcarbainoyl)-phenyI-methyl]-carbamic add tert-butyl ester was converted to (RS)-2-amino-N-(4-carbamimidoyl-ben2yl)-2-phenyl-acetamide; hydrochloride according to general procedure C. Off-white solid. MS 283^2 ([M+H]"^) Example 87 87.1 A solution of give (RS)-[(4-cyano-benzylcarbamoyl)-phenyl-methyi]-carbamic add tert-butyl ester (0.77 g, example 86.1) in dichloromethane (20 ml) was cooled to O^C and treated with trifiuoro acetic add (5 ml). The reaction mixture was stirred at r.t. for 5 hrs, then diluted with dichloromethane, cooled to CC and brought to pH 9 by dropwise addition of saturated aqueous Na2C03. The organic layer was washed with brine, dried over MgS04, filtered and concentrated to give (RS)-2-amino-N-(4-cyano-benzyl)-2-phenyl-acetamide (0.56 g). Ofif-white amorphous solid. MS 266.2 ([M+H]"^) 87.2 A solution of (RS)-2-aniino-N-(4-cyano-ben2yl)-2-phen)i-acetaniide (0.1 g) in dichloromethane (5 ml) was cooled to 0°C and treated with triethylamine (58 |il) and acetyl chloride (28 (4l). The reaction mixture was stirred at r.t for 1 hr, then diluted with dichloromethane, washed with IN HCl and brine. The organic layer was dried over MgS04, filtered and concentrated The product was isolated by chromatography (silica gel, gradient dichloromethane => dicMoromethane/MeOH 9:1) to give (RS)-2-acet)daraino-N-(4-cyano-benzyl)-2-phenyl-acetaniide (98 mg). Off-whitesoUd. MS 308.2 ([M+H]"^) 87.3 (RS)-2-Acetylamino-N-(4-cyano-benzyI)-2-phenyl-acetamide was converted to (RS)-2-acetylamino-N-(4-carbanuinidoyl-ben2yl)-2-phenyi-acetamide; hydrochloride according to general procedure D. Example 88 88.1 In analogy to example 22.1, (RS)-N-(4-cyano-benzyl)-2-(2-fluoro-4-hydroxy-phenyi}-2- methoxy-acetamide (example 70.4) was reacted with 2-phenoxyethanol, diethyl azodicarboxylate and triphenyl-phosphine in THF to give (KS)-N-(4-cyano-ben2:)d)-2-[2- fluoro-4-(2-phenoxy-ethoxy)-phenyl]-2-methoxy-acetamide. Colorless oil. MS 435.3 ([M+H]^) 88.2 {RS)-N-(4-Cyano-benzyl)-2-[2-fluoro-4-(2-phenoxy-ethoxy)-phenyl]-2-inethoxy-acetamide was converted to (RS)-N-(4-carbamiinido)d-beiizyl)-2-[2-fluoro-4-(2-phenox}'-ethox7)-piienyI]-2-inethoxy-acetamide hydrochloride according to general procedure D. White solid. MS 452.2 ([M+H]"") Example 89 89.1 2-Pyridinecarboxaldehyde was converted to (RS)-niethoxy-pyridin-2-}d-acetic add according to general procedure A using methanol/dioxane as solvent Brown oil. MS 166.1 ([M-H]-} 89.2 (RS)-Methoxy-pyridin-2-yl-acetic acid was reacted with 4-arainomethyi benzonitrile according to general procedure B to give (RS)-N-{4-cyano-ben2yI)-2-methoxy-2-pyridin-2-yl-acet3inide. Brown oil. MS 282.2 ([M+H] ■") 89.3 (RS)-N-(4-Cyano-benzyl)-2-methoxy-2-pyridin-2-yl-acetamide was converted to (RS)-N-(4-carbaiiiinudoyi-benzyl)-2-methoxy-2-pyridin-2-yl-acetamide hydrochloride according to general procedure D. Off-white, amorphous soHd. MS 299.2 ([M+H]"^) Example 90 90.1 Acetophenone was converted to (RS)-2-methoxy-2-phen>i-propiomc add according to general procedure A using methanol/dioxane as solvent Brown oil. MS 179.1 ([M-H]") 90.2 (RS)-2-Methoxy-2-phenyl-propionic add was reacted with 4-aminomethyl benzonitrile according to general procedure B to give (RS)-N-(4-cpno-ben2yi)-2-methoxy-2-phenyl-propionainide. Off-white, waxy solid. MS 295.0 ([M+H]"^) 90.3 (RS)-N-(4-Cyano-benzyl)-2-methoxy-2-phenyl-propionamide was converted to (RS)-N-(4-carbamimido)i-benzyl)-2-methoxy-2-phenyl-propionamide hydrochloride according to general procedure D. Off-white, amorphous solid. MS 312.2 ([M+H]"^) Example 91 91.1 The crude 4-bromo-2,6-difluorobenzaldehyde described in example 69.1 was reacted according to general procedure A using ethanol / dioxane as a solvent. The product of this reaction was subsequently coupled with 4-aminomethyl benzonitrile according to general procedure B. The product of this reaction could not be obtained pure and was directly converted to [RS)-2-(4-bromo-2,6-difluoro-phenyi)-N-(4-carbamimidoyl-benz)4)-2-ethoxy-acetamide hydrochloride according to general procedure D. Off-white soHd. MS 426.2{[M+H]"') Example 92 92.1 In analogy to example 16.4 (RS)-N-(4-cyano-benZ)d)-2-(2-fiuoro-6-hydroxy-phenyl)-2-methoxy-acetamide (example 80.4) was reacted with 2-bromoethanol in the presence of cesium carbonat in DMF to give N-{4-cyano-benzyl)-2-[2-fluoro-6-(2-hydroxy-ethoxy)-phenyl3-2-methoxy-acetamide. White solid. MS 359.2 ([M+H]"^) 92.1 N-(4-Cyano-benzyl) -2- [2-fluoro-6-(2-hydroxy-ethoxy)-phenyi] -2-methoxy-acetamide was converted to N-(4-carbainunidoyl-benzyl)-2-[2-fluoro-6-(2-hydroxy-ethoxy)-phenyl]-2-methoxy-acetamide; hydrochloride according to general procedure D. White solid. MS 376.3 ([M+H]"") Example 93 93.1 In analogy to example 16.4 (RS)-N-(4-cyano-benzyi)-2-(2-fluoro-6-hydroxy-phen)^)-2-methoxy-acetamide (example 80.4) was reacted with iodo acetamide in the presence of potassium carbonate in DMF to give 2-(2-carbamoylmethoxy-6-fluoro-phen)d)-N-(4-cyano-benzji)-2-methoxy-acetamide. Solid. MS 372.2 ([M+H]"^) 93.2 2-(2-Carbamoyhnethoxy-6-fluoro-phenyi)-N-(4-cyano-benzyl)-2-methoxy-acetamidewas converted to N-(4-carbamimidoy!-benzyl)-2-(2-carbamoyimethoxy-6-fluoro-phenyI)-2-methoxy-acetamide; hydrochlorideaccording to general procedure D. White soHd. MS 389.2 ([M+H]^) Example 94 94.1 To a solution of 2-biphenyI-4-yI-2-hydroxy-propionic add (CAS 6244-54-8,943 mg) in THF (10 ml), stirred at 0 "C was added NaH (60 % in mineral oil, 342 mg). After 50 min, ethyl iodide (0.69 ml) was added and the mixture was stirred at r.t. for 14 li. DMF (10 ml) was added. After 2 days, 47 mg NaH and 0.16 ml ethyl iodide were added subsequently. In the course of three weeks, a total of 653 mg NaH and 1.32 ml ethyl iodide were added. Water was added and the mixture was extracted with EtOAc (2x). The org. phase was washed with water, dried, filtered and evaporated. The crude product was purified by flash chromatography (EtOAc/ cydohexane 5:95 => 1:4) to give (RS)-2-biphenyl-4-yl-2-ethoxy-propionic acid ethjd ester (276 mg) as a light yellow oil. MS 298.1 ([M]"^) 94.2 (RS)-2-Biphenyl-4-yl-2-ethoxy-propionic add ethyl ester was hydrolyzed to (RS)-2-biphenyl-4-)d-2-ethoxy-propionic acid in analogy to example 20.1. Colorless waxy soHd. MS 269.1 ([M-H]') 943 (RS)-2-Biphenyl-4-)d-2-ethoxy-propionic acid was coupled with 4-aminomethyl benzonitrile to give (RS)-2-biphenyl-4-yl-N-{4-cyano-benzyl)-2-ethoxy-propionaniide according to general procedure C. Colorless solid. MS 385.1 ([M+H]^) 94.4 (RS)-2-BiphenyI-4-yl-N-(4-cyano-benzyl)-2-ethoxy-propionamide was converted to (RS)- 2-biphenyi-4-)d-N-(4-carbamimidoyl-benz)d)-2-ethoxy-propionamide hydrochloride according to general procedure D. Colorless solid. MS 402.3 ([M+H]"^) Example 95 95.1 4-(5-Ethoxy-2-fluoro-3-formyl-phenoxy)-piperidine-l-carboxylic add tert-but)d ester was converted to (RS)-4-[3-(carboxy-methoxy-metbyi)-5-ethoxy-2-fluoro-phenosy]-piperidine-1-carboxylic add tert-butjd ester according to general procedure A. Off-white solid. MS 445.3 {[M+NH4]0 95.2 (RS)-4-[3-(Carboxy-methoxy-methyl)-5-ethoxy-2-fiuoro-phenoxy]-piperidine-l-carboxyUc add tert-butyi ester was coupled with 4-aminomethyl benzonitrile to give (RS)-4-{3-[(4-cyano-ben2ylcarbamoyl)-methoxy-methyi]-5-ethoxy-2-fluoro-phenoxy}- piperidine-1-carboxyiic add tert-butjd ester according to general procedure B. Yellow oil. MS 564.4 ([M+Na]^) 95.3 The BOC-protecting group of (RS)-4-{3-[(4-cyano-benzylcarbainoyi)-methoxy-methyl]-5-ethox}'-2-fluoro-phenox7}-piperidine-l-carbox}dic add tert-butyl ester was removed according to standard procedures (TFA in CH2CI2) to give (RS)-N-(4-cyano-benzyl)-2-[5-ethoxy-2-£luoro-3-(piperidin-4-yloxy)-phenyl]-2-methoxy-acetainide. Off-white solid. MS 442.3 ([M+H]') 95.4 To a solution of (RS)-N-(4-cyano-benzyl)-2-[5-ethoxy-2-fluoro-3-Cpiperidin-4-ylox)')-phenyl]-2-methoKy-acetaimde (300 mg) in THF (3 ml) were added benzenesulfonyl chloride (127 mg) and trieth)damine {138 mg). The mixture was stirred over the weekend. Ice-water and EtOAc were added and the pH of the aq. Phase was adjusted to 2. The mixture was extracted with EtOAc. The org. Phase was washed with sat. NaHCOj soln. and water, dried, filtered and evaporated to give {RS)-2-[3-(l-beiizenesulfonyl-piperidin-4-)4oxy)-5-ethoxy-2-fiuoro-pheDyll-N-(4-cyano-benzyl)-2-methoxy-acetamide {396 mg) as an off-white solid. MS 582.2 ([M+H]^). 95.5 (RS)-2-[3-(l-Benzenesulfonyl-piperidin-4-}4oxy)-5-ethoxy-2-fluoro-phenyl]-N-(4-<:: was converted to hydrodiloride according general procedure d. colorless soud. ms> Using similar conditions to the ones described in examples 95.4 and 95.5, (RS)-N-(4-cyano-benzyI)-2-[5-ethoxy-2-fluoro-3-(piperidin-4-yloxy)-phenyl]-2-methoxy-acetainide was converted to the foJIowiug compounds: Example 96: {RS)-N-(4-Carbaniiniidoyl-benzyi)-2-[5-ethoxy-2-fluoro-3-(l-methanesulfonyl-piperidin-4-yloxy)-phenyl]-2-methoxy-acetaimde hydrochloride, MS 537.3 ([M+H]-") Example 97: (RS)-2-[3-{l-AcetyI-piperidin-4-yloxy)-5-ethoxy-2-fluoro-phenyl]-N-(4-carbaraainidoyi-benzyI)-2-methoxy-acetamide hydrochloride, MS 501.3 {[M+H]"^) Example 98: {RS)-2-[3-{l-Benzoyl-piperidin-4-yioxy)-5-ethoKy-2-fluoro-phenjd]-N-(4-carbaininiidoyl-benzyI)-2-methoxy-acetamide hydrochloride, MS 563.5 ([M+H]"^) Example 99 99.1 (RS)-(2-Fluoro-4-methox7-phenyl)-inethoxy-aceticacid, described in example 15.1 was coupled with 4-ammomethyl-3-chloroben2onitrile (CAS 202521-97-9) according to general procedure B to give (RS)-N-(2-cbloro-4-cyano-benzyl)-2-(2-fluoro-4-methoxy-phenyl)-2-niethoxy-acetainide. Light green soUd. MS 361.1 ([M-H]") 99.2 (RS)-N-(2-Chloro-4-cyano-benzyl)-2-(2-fiuoro-4-methoxy-phenyi)-2-metiioxy-acetaniide was converted to (RS)-N-(4-carbamimidoyl-2-cfaloro-ben2)d}-2-{2-fluoro-4-methox)'-phenyl)-2-methosy-acetainide hydrochloride according to general procedure D. Off-white soUd. MS 378.1 ((M-HD Ejmmple 100 100.1 (RS)-Ethoxy-(2-fluoro-4-methoxy-phenyl)-acetic acid, described in example 63.1 was coupled with 4-aniinometiiyl-3-chlorobenzomtrile (CAS 202521-97-9) according to general procedure C to give (RS)-N-(2-chloro-4-cyano-benz^)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide. Yellow oil. MS 377.2 ([M+H]"^) 100^ (RS)-N-(2-chloro-4-cyano-benzyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide was converted to (RS)-N-(4-carbaminudo)d-2-chloTO-benz}d)-2-ethoxy-2-{2-fluoro-4-methoxy-phenyl)-acetamide hydrochloride according to general procedure D. Colorless foam. MS 394.1 ([M+HD Example 101 101.1 To a solution of 3,5-difluoroaiiisole (20 g) in THE (200 ml) was added pentamethyldiethylenetriamine (24.05 g). The mixture was cooled to -75 "C. n-butyilithium (85 ml, 1.6 M in hexane) was added in such a way that the temperature did not exceed -67 "C. The mixture was stirred for 2 h. Ethylglyoxalate ( 55.5 g, 50 % in toluene) was added and the mixture was stirred for a further 2 h. Afterwards, the mixture was allowed to warm up to r.t. Water was added and the mixture vras made acidic (pH 3) with 25 % HCl. The mixture was ejctracted with EtOAc. The org. phase was washed with 0.5 N HCI, dried, filtered and concentrated. The product was purified by flash chromatography (Si02, cyclohexane / EtOAc 7:1} to give (RS)-(2,6-difluoro-4-methoxy-phenyI)-hydroxy-2cetii: add ethyJ ester (13.09 g). Colorless oil. MS 246.1 ([M]"^) 101.2 To a suspension of (RS)-(2,6-difluoro-4-methoxy-phenyl}-hydroxy-acetic acid ethyl ester (13.06 g) and Ag20 (24.58 g) in toluene (100 ml) was added ethyl iodide (24.81 g). The mixture was heated to reflux for 2.5 h. Ethyl iodide (24.81 g) and AgiO (12.29 g) were added and the mixture was refluxed for a fiirther 7 h. The soHd was filtered off and the filtate was concentrated to give (RS)-(2,6~difiuoro-4-methoxy-phenyl)-ethoxy-acetic acid ethyl ester (14.6 g). Light yellow oil. MS 274.1 ([MD 101.3 (RS)-(2,6-Difluoro-4-methcxy-phen)d)-ethoxy-acetic add ethyl ester was hydrolyzed to (RS)-(2,6-difluoro-4-methoxy-phen)4)-ethoxy-acetic add in analogy to example 20.1. MS Light yellow oil 245.2 C[M-H]") 101.4 (RS)- (2,6-DifIuoro-4-methoxy-phenyi)-ethoxy-acetic add was coupled with 4-anunomethyl-3-chlorobenzonitrile (CAS 202521-97-9) according to general procedure C to give (RS)-N-(2-chloro-4-cyano-benzyl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide. Colorless oil. MS 395.0 {[M+H]"*") 101.5 (RS}-N-(2-Ch]oro-4-cyano-benzyi}-2-(2,6-difiuoro-4-methoxy-phenyl)-2-ethoxy-acetamide was converted to (RS)-N-(4-carbaniimidoyl-2-chloro-benzyl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetaniide hydrochloride according to general procedure D. Coloriess foam. MS 412.3 ([M+H]"*"} Example 102 102.1 (RS)-(2,6-Difluoro-4-methoxy-phenyl)-methoxy-acetic add, described in example 66.1 was coupled with 4-aminometh)i-3-chlorobenzonitrile (CAS 202521-97-9) according to general procedure C to give (RS)-N-(2-chloro-4-cyano-benzyl)-2-(2,6-difluoro-4- methoxy-phenyl)-2-methoxy-acetamide. Light yellow oil. MS 379.2 ([M-H]') 102.2 (RS) -N-(2-Chloro-4-cyano-benzyl) -2- (2,6-difluoro-4-methoay-phenyl)-2-methoxy- acetamide was converted to (RS)-N-(4-carbamimidoyl-2-ch]oro-benzyl)-2-(2,6-difluoro- 4-methox)'"-plieny])-2-methoiy-acetamide h}^drochloride according to general procedure D. Colorless foam. MS 398.2 ([M+H]^) Example 103 103.1 (RS)-Ethoxy-(2-fluorD-4-methoxy-phenyI)-acetic acid, described in example 63.1 was coupled with 4~aminomethyl-2-chlorobenzoiiitrile (CAS 202522-15-4) according to general procediire C to give {RS)-N-(3-chloro-4-cyano-ben2yl)-2-ethoxy-2-(2-fiuoro-4-methoxy-phenyO-acetamide. Yellow oil. MS 377.2 ([M+H]"^) 103.2 (RS )-N-{3-Chloro-4-cyano-benzyl) -2-ethoxy-2- (2-fluoro-4-niethoxy-plienyi) -acetamide was converted to (RS)-N-[3-chloro-4-(N-hydTOxycarbamiinidoyi)-benzyl] -2-ethoxy-2-{2-fluoro-4-methoxy-pben)d)-acetanude according to general procedure D. Colorless solid. MS410.0 {[M+H]^) 103.3 In analogy to example 37.5, (RS)-N-[3-chloro-4-(N-hydroxycarbamimidoyl)-benzyl|-2- ethoxy-2-(2-fluoro-4-methoxy-phenyI)-acetainide was reduced to give (RS)-N-(4- carbamimido}^-3-chloro-ben2yl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide acetate. Colorless solid. MS 394.2 ([M-i-H]') Example 104 The crude 4-brorao-2,6-difluorobenzaldehyde described in example 69.1 was reacted according to general procedure A using ethanol / dioxane as a solvent The product of this reaction was subsequently coupled with 4-arainometh)d-3-methoxy-benzomtrile (CAS 182159-14-4) according to general procedure B. The product of this reaction could not be obtained pure and was directly converted to (RS)-2-(4-bromo-2,6-difluoro-phenjd)-N-(4-carbamimidoyl-2-methoxy-ben2yl)-2-ethoxy-acetamide hydrochloride according to general procedure D. Off-white solid. MS 456.1 ([M-l-H]'^) Example 105 105.1 (RS)-Ethoxy-(2-fluoro-4-methoxy-phenyi)-acetic acid, described in example 63.1 was coupled with 4-aminomethyl-3-methoxy-ben2onitrile (CAS 182159-14-4) according to general procedure B to give (RS)-N-(4-cyano-2-methoxy-benzyl)-2-ethoxy-2-(2-fiuoro-4-methoxy-phenyl)-acetamJde. Yellow oil. MS 373.2 ([M+H]"^) 105.2 (RS) -N-{4-Cyano-2-methox)'-ben2yl) -2-etitoxy-2- (2-fluoro-4-methoxy-phenyl)-acetamide was converted to (RS)-N-(4-carbamiinidoyl-2-met±ioxy-benzyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetainide hydrochloride according to general procedure D. Colorless solid. MS 390.3 ([M+H]') Example 106 106.1 A suspension of 3-fluoro-4-formyl-benzonitrile (CAS 105942-10-7,3 g), phenol (2.14 g) and potassium carbonate {3.14 g) in DMF (20 ml) was stirred at 120 "C for 90 min. After cooling down to r.t, water was added and the mixture was extracted with diethyl ether. The org. phase was washed with 0.1M NaOH and brine, dried, filtered and evaporated. The crude 4-formyl-3-phenoxy-benzonitrile (brown oil, 3.75 g) was used in the next step without finrtiier purification. 106.2 To a solution of 4-formyi-3-phenoxy-ben20nitrile (2.21 g) in dry ethanol (45 ml) was added sodium acetate (0.894 g) and hydroxylamine hydrochloride (0.757 g). The mixture was stirred at r.t. for 4.5 h. The solvent was evaporated and the product was purified by flash chromatography (cydohexane/EtOAc 8:2 => 3:7) to give 4-(hydroxyimino-meth>d)-3-pheno3^-benzonitrile (1.42 g). Light yellow solid. MS 238.1 ([M]"^) 106.3 A solution of 4-(hydroxyimino-methyl)-3-phenoxy-benzonitrile (200 mg) in acetic acid (1.2 ml) was stirred at 65 °C. Zinc powder (500 mg) was added portionwise during 30 min. After stirring for a further 1 h, the reaction mixture was filtered and the filtrate was concentrated to near dryness. Water was added and the mixture was washed with diethyl ether. The org. Phase was extracted (Ix) with diluted acetic add. The pH of the combined aq. phases was adjusted to 11 using 2 N NaOH. The mixture was extracted with EtOAc. The org Phase was dried, filtered and concentrated to give 4-aminomethyi-3-phenoxy-benzonitrile (165 mg) as a l^ht yellow oiL 106A (RS)-Ethoxy-(2-fluoro-4-methoxy-phen)d)-acetic add, described in example 63.1 was coupled with 4-aminomethyl-3-phenoxy-benzonitrile according to general procedtire B to give (RS)->f-(4-cyano-2-phenoxy-benzyI)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyi)- acetamide. Colorless oil. MS 435.2 ([M+H]"") 106.5 (RS)-N-(4-Cyano-2-phenoxy-beiiz)d)-2-ethoxy-2-{2-fluoro-4-methoxy-phenyl)-acetamide was converted to (RS)-N~(4-carbainimidoyI-2-phenoxy-ben2)'i)-2-ethosy-2-(2-fluoro-4-niethoxy-phen)d)-acetamide hydrochloride according to general procedure D. Colorless solid. MS 452.4 ([M+HJ""} Using similar procedures to the ones described in example 106, 3-fIuoro-4-formyl-benzonitrile (CAS 105942-10-7) was converted to the following compounds: Example 107: (RS)-N-(4-Carbaniiimdoyl-2-o-tolyloxy-benzyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide hydrochloride, MS 466.5 ([M+H]"^) Example 108: (IlS)-N-[4-Carbainimidoyi-2-(4-fluoro-phenoxy)-beiizyl]-2-ethoxy-2-(2-fluojo-4-inethoxy-phen]d)-acetamide hydrochloride, MS 470.3 ([M+H]'*} Example 109: (RS)-N-[4-Carbamimido)d-2-(pyridin-3-yIoxy)-benzyl]-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide acetic add, MS 453.5 ([M+H]"^) Example 110 110.1 To a solution of 4-fonnyl-3-hydroxy-benzomtrile (CAS 84102-89-^) (6.90 g) in dry ethanol (165 ml) was added sodium acetate (4.23 g) and hydroxylamine hydrochloride (3.58 g). The mixture was stirred at r.t. for 1 h. The solvent was evaporated and the product was purified by flash chromatography (cyclohexane/EtOAc 8:2 => 1:1) to give 3-hydroxy-4-(hydroxyimino-methyI)-benzonitrile (4.70 g). Light yellow soHd. MS 162.0 ([M]"*") 110.2 A solution of 3-hydroxy-4-(hydroxyimino-methyl)-benzonitrile (1.79 g) in acetic add (16.6 ml) was stirred at 65 "C. Zinc powder (6.59 g) was added portionwise during 30 min. After stirring for a further 1.5 h, the reaction mixture was filtered and the filtrate was concentrated to dryness. 1 N HCl (55.3 ml) was added and the solvent was evaporated. The same procedure was repeated with with water (2x), EtOH (2x) and toluene (2x}. The resulting colorless soHd was dissolved in diethyl ether, filtered and the filtrate was concentrated to give 4-aminomethyl-3-hydroxy-benzonitrile hydrochloride (colorless soKd, 2.5 g) which was used in the next step without further purification. MS 149.2 ([M+H]^) 110.3 (RS}-Ethoxy-(2-fluoro-4-methoxy-phenyl)-acetic acid, described in example 63.1 was coupled with 4-aminomethyl-3-hydroxy-ben2onitrile hydrochloride according to general procedure B to give (RS)-N-{4-cyano-2-hydrosy-beiizyi)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide. Colorless solid. MS 457.1 ([M-H]") 110.4 To a solution of (RS)-N-(4-cyano-2-faydroxy-benZ7l}-2'ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide (310 mg) and 2-cliloro-5-nitropyridine (205 mg) in DMSO (2 ml) was added cesium carbonate (423 mg). The mixture was stirred at 50 "C for 5 h. The solvent was evaporated, the residue was dissolved in EtOAc and washed with water (2x} and brine (Ix). The org. Phase was dried, filtered and concentrated. The product was purified by flash chromatography (cycIohexane/EtOAc 9:1 => 4:6) to give (RS)-N-[4-cyano-2-(5-mtro-pyridin-2-yioxy)-benzyl]-2-ethoxy-2-(2-f!uoro-4-methoxy-phenyi)-acetainide. Light yellow foam. MS 481.4 ([M+H]^) 110.5 (RS)-N-[4-Cyano-2-(5-nitro-pyridin-2-yloxy)-benzyi]-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetaTnide was converted to (RS)-N-[4-carbamimidoyI-2-(5-iiitro-pyridin-2-yloxy)-benzyl]-2-etho::9'-2-(2-fluoro-4-methoxy-phenyl)-acetamide hydrochloride according to general procedure D. Off-white solid. MS 498.3 ([M+H]*) Example 111 (RS)-N-[4-Carbamimidoyl-2-(5-nitro-pyridin-2-)doxy)-ben2yi]-2-ethoxy-2-(2-fluoro-4-methoxy-phenyi)-acetamide hydrochloride was hydrogenated at r.t and normal pressure in EtOH/THF using Vd (10 % on charcoal) as a catalyst to give (RS)-N-[2-(5-amino-pyridin-2-yloxy)-4-carbamimidoyl-benz>d]-2-ethoxy-2-(2-fiuoro-4-methoxy-phenyl)-acetamide hydrochloride. Light yellow solid. MS 468.1 ([M+H]"^) Example 112 112.1 A solution of (RS)-N-(4-cyano-2-hydroxy-benzyl)-2-etiioxy-2-(2-fiuoro-4-methoxy-phenyl)-acetaimde (example 17.3, 626 mg), 4-dimeliiyiajnino pyridine (22 mg) and triethyiamine (407 mg) in dichloromethane (14 ml) was stirred at -20 °C. Trifluoromethanesulfonic add anhydride (604 n^) was added dropwise. The cooling bath was removed and the mixture was stirred at r.t. overnight The mixture was dQuted with dichloromethane and washed with 0.1 N HCl and with water. The org. Phase was dried, filtered and concentrated. The product was purified by flash chromatography (CH2C12 => CH2C12:MeOH 9:1) to give 766 mg of the triflate as a light brovra oil. The trifiate (358 mg) was dissolved in l,2-diinethox7ethane (7.4 ml) and isopropanol (0.9 inl).Phenylboronicacid (184mg)andNa2C03 (10% as a solution in water, 1.6 ml) were added and the mixture was stirred for 30 inin under an argon atmosphere. Tetralds-(triphenylphosphine)-palladium (42 mg) was added and the mixture was heated to reflux for 4 h and stirred at r.t. ovem^ht. The mixture was filtered and the filtrate was diluted with EtOAc and washed with 1 N NaOH (2x) and with water (2x). The org. Phase was dried, filtered and concentrated. The product was purified by flash chromatography (EtOAc/cydohexane 3:7 => 6:4) to give (RS)-N-(5-cyano-biphenyl-2-yhnethyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide (157 mg). Colorless foam. MS 419.3 ([M+H]"^) 112^ (RS)-N-( 5-C7ano-biphenyi-2-ylmethyi) -2-ethoxy-2- (2-fluoro-4-methoxy-phenyl)-acetamide was converted to (RS)-N-(5-carbamimido)d-biphenyl-2-ylmethyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide hydrochloride according to general procedure D. White soHd. MS 436.2 ([M+H]"") Example 113 113.1 In analogy to example 16.4, (RS)-N-(4-cyano-2-hydroxy-benzyl)-2-ethoxy-2-{2-fluoro-4-raethoxy-phenyl)-acetamide (example 110.3) was alkylated with eth^ bromoacetate / cesium carbonate in DMF to give (RS)-(5-cyano-2-{[2-ethoxy-2-(2-fluoro-4-njethoxy-phenyI)-acetylajnino]-methyl}-phenoxy)-acetic add ediyl ester as a colorless soHd. MS 443.4 ([M-H]') 113^ (RS)-(5-C)^no-2-{[2-etiioxy-2-(2-fluoro-4-methoxy-phenyl)-acetylaniino]-methyi}-phenoxy)-acetic add eth'j^ ester was converted to (RS)-(5-carbamimido^-2-l [2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetylamino]-methyl}-phenoxy)-acetic add ethyl ester hydrochloride according to general procedure D. Colorless foam. MS 462.2 ([M+H]"") Using similar procedures to the ones described in example 113, (RS)-N-(4-cyano-2-hydroxy-ben2yl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyi)-acetarnade (example 110.3) was converted to the following compounds: Example 114: (RS)-N-(4-Carbamimidoyi-2-carbamoylmethoxy-benzyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phen}4)-acetamide hydrochloride, MS 433.3 ([M+H]"^) Example 115: (RS)-N-(4-Carbaraimidoyi-2-isopropoxy-beiizyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetarnide hydrochloride, MS 418.3 ([M+H]"^) E^ampJe 116: (RS)-N-[4-Carbamimidoyl-2-(2~hydroxy-ethoxy}-benzyl]-2-ethoxy-2-{2-fluoro-4-methoxy-pheii)^)-acetamide hydrochloride, MS 420.2 ([M+H]"^) Example 317:2-(5-Carbamirnidoy]-2-{[2-etho3cy-2-{2-fluoro-4-methoxy-phenyl)-acetylainino]-methyl}-phenoxy)-N-isopropy!-2-phenyl-acetamide hydrochloride, MS 551.2 ([M+H]"") The starting material for the preparation of 2-(5-carbaimmidoyl-2-{[2-ethoxy-2-(2-fiuoro-4-methoxy-phenyl)-acet)damino]-methyl)-phenoxy)-N-isopropyl-2-phen)^-acetamide hydrochloride, 2-chloro-N-isopropyl-2-phenyl-acetainide, was prepared from alpha-chlorophenylacetyl chloride with isopropyl amine in CH2Cl2/aq. NaOH. Example 118 In analogy to example 20.1, (RS)-(5-carbaininiidoyi-2-{[2-ethoxy-2-(2-fIuoro-4-methox)'-phenyl)-acetylamino]-methyl}-phenoxy)-acetic add ethyl ester hydrochloride (example 113.2) was hydrolysed to give (RS)-(5-carbanimudoyl-2-{[2-ethoxy-2-(2-fl.uoro-4-methoxy-phen)d)-acetylamino]-methyl}-phenoxy)-acetic add Colorless solid. MS 434.2 ([M+H]^) Example 119 In analogy to example 22.1, (RS)-N-(4-cyano-2-liydroxy-benzyl)-2-ethoxy-2-(2-fluoro-4-metiioxy-phenyi)-ace^nnde (example 110.3) was reacted in a Mitsunobu reaction with methyl-(R)-(+)-lactate. The product of this reaction was converted to (RS)-(S)-2-(5-carbamimidoyl-2-| [2-ethoxy-2-C2-fluoro-4-methoxy-phenyl)-acetylatnino] -mediyl}-phenoxy)-propioiuc add ethyl ester hydrochloride according to general procedure D. Colorless foam. MS 476.3 ([M+Hf) Example 120 As a side product of the synthesis of (RS)-(S)-2-(5-carbamimidoyi-2-{[2-ethoxy-2-(2-9uoro-4-methoxy-pheny!)-acetyIamino]-methyl]-phenoxy)-propiomc add ethyl ester hydrochloride (example 119), there was obtained ((RS)-S)-2-(5-caibamiinidoyl-2-U2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetylamino]-meth^}-phenoxy)-propionanQide hydrochloride as a colorless foam. MS 447.3 ([M+H]'') Using similar procedures to the ones described in examples 119 and 120, (RS)-N-(4-q^no-2-hydroxy-benzyl)-2-ethoxy-2-(2-fluoTo-4-methox)'-phenyl)-acetamide (example 110.3) was converted to the following compounds: Example 121: (RS)-(R)-2-(5-Carbamiinidoyl-2-{[2-ethoxy-2-(2-fluoro-4-metfaoxy-phenyl)-acetyiamino]-methyl}-phenoxy)-propionic add ethyl ester hydrochloride, MS 476.1 ([M+H]*) Example 122: (RS)-(R)-2-(5-Carbaniimidoyi-2-I[2-ethosy-2-C2-fluoro-4-methox7-phenyl)-acetylamino]-medi)d}-phenoxy)-propionamide hydrochloride, MS 447.3 ([M+H]^) Example 123 123.1 To a solution of 4-aminomethyl-3-hydroxy-benzonitrile hydrochloride (example 110.2,2.0 g) and triethyiamine (2.19 g) in dichloromethane (20 ml) was added di-tert-butyldicarbonate (2,41 g). The mixture was stirred at r.t for 3.5 h. The mixture was washed with water (3x), dried, filtered and concentrated. The crude product was dissolved in DMF (15.5 ml). Cesium carbonate (4.00 g) and iodoacetamide (2.27 g) were added and the mixture was stirred at r.t. for 3 days. Water was added and the mixtxire was extracted with EtOAc. The org. phase was washed with water, dried, filtered and concentrated. The crude product was dissolved in MeOH and then concentrated to obtain a thick suspension. The solid was filtered off and washed with a small amount of MeOH. This procedure was repeated with the mother liquor to give (2-carbamoyimet}ioxy-4-c}'ano-ben2yI)-carbamic acid tert-butyl ester (a total of 1.88 g) as a colorless solid. MS 304.2 ([M-H]") 123.2 The BOC protecting group of (2-carbamoylmethoxy-4-cyano-benzyl)-carbamic add tert-butyl ester was removed using HCl in dioxane to give 2-(2-aminometh)d-5-cyano-phenoxy)-acetamide hydrochloride as an ofif-white powder. MS 206.1 ([M+H]"^) 123.3 (RS)-(2-Fluoro-4-methoxy-phenyl)-methoxy-acetic add (example 15.1) was coupled with 2-(2-aminoraethyl-5-cyano-phenoKy)-acetamide hydrochloride according to general procedure C. The product of this reaction was converted to (RS}-N-(4-carbaminndoyI-2- carbamoylmethoxy-ben2yI)-2-(2-fluoro-4-methoxy-phen)d)-2-inethoxy-acetamide hydrochloride according to general procedure D. Colorless foam. MS 419.3 ([M+H]"*") Example 124 124.1 {RS}- (2,6-Difluoro-4-methox}^-pheiiyl}-ethoxf-acetic acid (example 101.3) was coupled with 4-aininomethyl-3-phenoxy-ben2omiiile {example 106.3) according to general procedure C to give (RS)-N-(4-cyano-2-phenoxy-benzyl)-2-(2,6-di£luoro-4-methoxy-phenyl)-2-ethoxy-acetamide. Colorless foam. MS 453.1 ([M+H]"^) 124.2 (RS) -N-(4-Cyano-2-phenoxy-beiiz)d) -2 -(2,6-difIuoro-4-methoxy-pheiiyl)-2-ethoxy-acetamide was converted to (RS)-N-{4-carbainiinidoyi-2-phenoxy-benz)d)-2-{2,6-difluoro-4-methoxy-phenyI)-2-ethoxy-acetamide hydrochloride according to general procedure D. Colorless foam. MS 470.2 ([M+H]"^) Example 125 125.1 (RS)- (2,6-I>ifluoro-4-methoxy-phenyl)-ethoxy-acetic add (example 101.3) was coupled with 4-aminomethyi-3-methoxy-benzonitrile (CAS 182159-14-4) according to general procedure B to give (RS)-4-[3-(2,6-difluoro-4-inethoxy-phen7l)-3-ethoxy-2-oxo-propylamino]-3-methoxy-benzonitrile. Colorless oil. MS 391.1 ([M+H]'^) 125.2 (RS)-4-[3-(2,6-Difluoro-4-raethoxy-phenyl)-3-ethoxy-2-oxo-prop)damino]-3-methoxy-benzonitrile was converted to (RS)-N-(4-carbamimidoyl-2-methoxy-benzyl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetainide hydrochloride according to general procedure D. Colorless foam. MS 408.2 ([M+H]"") Example 126 126.1 (RS)- (2,6-Difluoro-4-methoxy-pheny])-ethoxy-acetic add (example 101.3) was coupled with 4-aminomethyl-3-hydroxy-benzonitrile hydrochloride (example 110.2) according to general procedure B to give (RS)-N-(4-cyano-2-hydroxy-benzyl)-2-(2,6-diftuoro-4-methoxy-phenyl)-2-ethoxy-acetamide. Colorless foanx MS 375.4 ([M-H]') 126.2 In analogy to example 16.4, (RS)-N-(4-cyano-2-hydroxy-ben2yl)-2-(2,6-difluoro-4- niethoxy-phenyl)-2-ethoxy-acetamide was alkjdated with iodoacetamide / cesium carbonate in DMF to give (RS)-N-{2-caxbamoyimetiiox)'-4-cyano-beiizyl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetainide as a colorless solid. MS 434.3 ([M+H]"*") 126.3 (RS)-N-{2-Carbamoylmethoxy-4-cyano-benzyi)-2-(2,6-difliioro-4-methoxy-phenyl)-2-ethoxy-acetamide was converted to {RS)-N-(4-carbanuimdoyI-2-carbainoylinethoxy-benz)d)-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetaimdehydrocbloride according to general procedure D. Colorless foam. MS 451.3 ([M+H]"*") Using similar procedures to the ones described in example 126, (RS)-H-(4-cyano-2-hydroxy-ben2yl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetaraide (example 126.1) was converted to the following compounds: Example 127: (RS)-N-[4-Carbamimidoyl-2-{2-fluoro-benzyioxy)-benzyl]-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethox7-acetamide hydrochloride, MS 502.3 ([M+H]"^) Example 128: (RS)-N-[4-Carbamimidoyl-2-(5-chlora-2-fluoro-benzyloxy)-benzyi]-2-{2,6-difIuoro-4-methoxy-phenyl)-2-ethoxy-acetainide hydrochloride , MS 536.3 ([M+H] '*) Example 129: (RS}-N-{4-Carbamimidoy]-2-[(2-methoxy-ethylcarbamoyi)-inethQxy]-benzyi}-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide hydrochloride, MS 509.5 ([M+H]^) The starting material for the preparation of (RS)-N-14-carbamimidoyi-2-[(2-methoxy-ethylcarbamoyi)-inethoxy]-benzyl}-2-(2,6-difluoro-4-methoxy-pheny])'2-ethoxy-acetamide hydrochloride, 2-chloro-N-(2-methoxy-ethyl)-acetamide, was prepared from chloroacetyl chloride with 2-methoxyethyl amine and trieth)damine in CH2C12- Example 130: (RS)-N-{4-Carbamimidoyl-2-[(2-mOTpholin-4-yl-ethylcarbamoyl)-methoxy]-benz>i}-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide hydrochloride, MS 564.3 ([M+H]"") The starting material for the preparation of (RS)-N-{4-carbamimidoyl-2- [(2-morpholin-4-)d-ethTdcarbamoyl)-methoxy]-benzyl}-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide hydrochloride, 2-chloro-N-(2-morpholin-4-yl-eth)d)-acetamide hydrochloride, Was prepared from chloroacet>i chloride with morpholine in CH2CI2. Example 131: {RS)-N-{4-Carbamimidoyl-2-[(2-diethylaiiiino-ethylcarbamoyl)-methoxy]-benzyl}-2-(2,6-difluoro-4-methoxy-phenyl)-2-etho]cy-acetainide hydrocUoride, MS 550.3 ([M+H]^) The starting material for the preparation of (RS)-N-{4-carbamimidoyl-2-[(2-diethylamino-ethylcarbamo}d)-methoxy]-ben2yl}-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide hydrochloride, 2-chloro-N-{2-diethylaimno-ethyl)-acetamide hydrochloride, was prepared from chloroacetyl chloride with diethyiamine in CH2CI2. Examples 132 and 133 In analogy to example 16.4, (RS)-N-(4-cyano-2-hydroxy-benzyl)-2-(2,6-difiuoro-4-methoxy-phenyl)-2-ethoxy-acetaraide {example 126.1) was alkylated with 3-{chlorometh}d)-l,2,4-oxadiazole / cesium carbonate in DMF to give a mixture of N-[4-cyano-2-{[l,2,4]oxadiazol-3-)dmethoxy)-ben2yl]-2-(2,6-difluoro-4-methoxy-phenyI)-2-ethoxy-acetamide and N-(4-cyano-2-cyanomethoxy-benzyl)-2-(2,6-difiuoro-4-methoxy-phenyl)-2-ethoxy-acetamide. These compounds were converted according to general procedure D to give Example 132: (RS)- N-[4-Carbaminiidoyl-2-([l,2,4]oxadiazol-3-yimethoxy)-ben2yl]-2-(2,6-difluoro-4-methoxy-phenyI)-2-ethoxy-acetamide hydrochloride, MS 476.1 ([M+H]"*^) Example 133: (RS)- N-{4-Carbamiinidoyl-2-carbamimido)dmethoxy-ben2yi)-2-(2,6-difiuoro-4-methoxy-phenyl)-2-ethoxy-acetamide hydrochloride ,MS 450.1 {[M+H]"*^) Example 134 In analogy to example 22.1, (RS)-N-(4-cyano-2-hydroxy-benZ)4)-2-(2,6-difluoro-4-methoxy-phenyi)-2-ethoxy-acetamide (example 126.1) was reacted in a Mitsunobu reaction with lH-benzimidazole-2-methanol. The product of this reaction could not be obtained pure and was directly converted to (RS}-N-[2-(lH-benzoimidazol-2-yimethoxy)-4-carbaniimidoyI-benz)4]-2-(2,6-difluoro-4-methoxy-phen}d)-2-ethoxy-acetamide hydrochloride according to general procedure D. Off-\^te foam. MS 524.4 ([M+H]"^) Example 135 135.1 In analogy to example 22.1, {RS)-N-(4-cyano-2-hydroxy-benzyl)-2-(2,6-difiuoro-4-methoxy-phenyl)-2-ethoxy-acetamide (example 126.1) was reacted in a Mitsunobu reaction with [3aS,5R,6aR]-2,2-dimethyl-tetrahydro-cyclopenta[l,3]dioxol-5-ol (CAS 25494-07-9) to give (RS)-N-[4-cyano-2-{(3aS,5S,6aR)-2,2-dimethyl-tetrahydro- c>'clopenta[l,3]dioxol-5-yloxy)-benzyl]-2-(2,6-difluoro-4-methoxy-phenyi)'2-elhoxy-acetamide . Colorless oil. MS 517.3 ([M+H]"") 135.2 (RS)-N-[4-Cyano-2-((3aS,5S,6aR)-2,2-dimethyl-tetrahydro-cydopenta[l,3]dioxol-5-yloxy)-benzyl]-2-(2,6-difiuoro-4-methoxy-phenyl)-2-ethoxy-acetamide was converted to (RS)-N-[4-carbamimido)4-2-({1 S,3R,4S)-3,4-dihydroxy-cydopentyloxy)-beiizyl]-2-(2,6-difluoro-4-methoxy-phen)^)-2-ethoxy-acetamide hydrochloride according to general procedure D. Off-white soUd. MS 494.4 {[M+H]'} Example 136 136.1 To a solution of (RS)-N-(4-cyano-2-hydroxy-benzyl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide (example 126.1, 200 mg) and cyclopentene oxide (894 mg) in ethanol (2 ml) was added potassium carbonate (18 mg). The mixture was stirred at 105 "C for 17 h. The mixture was concentrated and the crude product was purified by flash chromatography (cydohexane => cydohexane/EtOAc 1:1) to give a mixture of (RS) and (SR)-N-[4-cyano-2-((lR,2R)-2-hydroxy-cydopentyloxy)-benzyl]-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide (148 mg). Lightydlowoil. MS 461 ([M+H]"^) 136.2 A mixture of (RS) and (SR)-N-[4-Cyano-2-((lR2R)-2-hydroxy-cydopent)doxy)-benzylj- 2-(2,6-difIuoro-4-methoxy-phenyl)-2-ethoxy-acetamide was converted to a mixture of (RS)and(SR)-N-[4-Carbaraimidojd-2-((lRS,2RS)-2-hydroxy-cydopentyloxy)-benz)i]-2- (2,6-difluoro-4-methoxy-phen)d)-2-ethoxy-acetamide hydrochloride according to general procedure D. Colorless solid. MS 478.1 ([M+H] ^) Example 137 (RS)-(2,6-Difluoro-4-methoxy-phenyI)-methoxy-aceticadd (example 66.1) was coupled with2-(2-aminomethyI-5-cyano-phenoxy)-acetamide hydrochloride (example 123.2) according to general procedure C. The product of this reaction was converted to (RS)-N-(4-carbamimidoyl-2-carbamoylmetfaoxy-benzyl)-2-(2,6-dtfluoro-4-methoxy-phenyI)-2-methoxy-acetamide hydrochloride according to general procedure D. Colorless foam. MS 437.4 ([M+HD Example 138 138.1 (RS)-(2,6-Difluoro-4-methoxy-plien)d)-meliioxy-acetic add (example 66.1) was coupled with 4-aminoinethyl-3-hydroxy-benzomtri]e hydrochloride (example 110.2) according to ■ general procedure C to give (RS)-N-(4-cyano-2-hydroxy-ben27l)-2-(2,6-difluoro-4-methoxy-phenyI)-2-methoxy-acetamide . Colorless foam. MS 361.1 ([M-H]") 13S.2 In analogy to example 16.4, (RS)-N-(4-cyano-2-hydroxy-benzyl)-2-(2,6-difluoTO-4-methoxy-phenyl)-2-methoxy-acetamide was alkylated with 2-cfaloro-N-methylacetamide / cesium carbonate in DMF to give (RS)- N-{4-cyano-2-methyicarbamo)dmethoxy-benZ)d)-2-(2,6-difluoro-4-methoxy-phen)d)-2-methoxy-acet2mide as a colorless foam. MS 434.2 ([M+H]"") 138.3 (RS)-N-(4-Cyano-2-metiiylcarbamoylmethoxy-benzyl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-methoxy-acetamide was converted to {RS)-N-(4-carbamimidoyl-2-methyicarbamo)dmelhoxy-benzyl}-2-(2,6-difluoro-4'methoxy-phenyl)-2-methoxy-acetamide hydrochloride according to general procedure D. Colorless soHd. MS 451.2 ([M+H]^) Using similar procedures to the ones described in example 138.2 and 138.3, (RS)-N-{4-cyano-2-hydroxy-ben2yI) -2-{ 2,6-difIuoro-4-methoxy-phenyI) -2-methoxy-acetamide (example 138.1) was converted to the foDowing compounds: Example 139: (RS)-N-[4-Carbamimido)i-2-(isopropyIcarbamo>d-methoxy)-benz)d]-2-(2,6-difluoro-4-methoxy-phen)d)-2-methoxy-acetaniide hydrochloride, MS 479.3 ([M+H]") Example 140: (RS)-N-l4-Carbamimidoyl-2-[(4-fluoro-phenylcarbamoyl)-methoxy]-benz)d}-2-(2,6-di3uoro-4-methoxy-phenyl)-2-methoxy-acetamide hydrochloride, MS 531.2 ([M+H]"*") Example 141 In analogy to example 22.1, (RS)-N-(4-cyano-2-hydroxy-benzyl)-2-C2,6-difluoro-4-methoxy-phenyl)-2-raethoxy-acetamide (example 138.1) was reacted in a Mitsunobu reaction with 2-hydroxymethyI pyridine. The product of this reaction could not be obtained pure and was directly converted to (RS)- N-[4-carbamiinidoyi-2-(pyridin-2- ylmethoxy)-benzyi]-2-(2,6-difluoro-4-niethoxy-phenyI)-2-inethoxy-acetainide hydrochloride according to general procedure D. Colorless foam, MS 471,2 ([M+H]"^) Example 142 142.1 A solution of 3-fiuoro-4~forrayl-benzomtrile (CAS 1O5942-10-7, 1 g) in THF (25 ml) was cooled to 0°C under argon. Trifluoroethanol (3.36 g) and potassium tert-butylate (0.83 g) were added subsequently. The mixture was stirred for 2 h. The mixture was diluted with EtOAc and washed with water. The org. phase was dried, filtered and concentrated. The product was purified by flash chromatography (SiOa, cyclohexane / EtOAc 1:1) to give 4-formyl-3-(2^2,2-trifluoro-ethoxy)-benzomtrile. Yellow solid. 142.2 In analogy to example 106.2, 4-formyl-3-(2,2,2-trifluoro-ethoxy)-benzonitrile was reacted with hydroxylamine hydrochloride and sodium acetate in ethanol to give 4-(hydroxyimino-methyl)-3-(2^,2-trifluoro-ethoxy)-benzonitrile as a yellow solid. 142.3 In analogy to example 106.3, 4-(hydroxyimino-nieth)d)-3-(2,2,2-trifluoro-ethoxy)- benzonitrile was reduced to 4-aminomethyl-3-(2^,2-trifluoro-ethoxy)-benzQnitrile using zinc in acetic acid. 142.4 (RS)-(2,6-Difluoro-4-methoxy-phenyl)-methoxy-acetic add (example 66.1) was coupled with 4-aminomethyl-3-(2,2,2-trifluoro-ethoxy)-benzomtrile according to general procedure B to give (RS)-N-[4-cyano-2-(2,2,2-trifluoro-ethoxy)-benz)4]-2-(2,6-difiuoro-4-methoxy-phenyl)-2-methoxy-acetamide. Colorless solid. MS 445.0 ([M+H]"^) 142.5 (RS)-N-[4-Cyano-2-(2,2,2-trifluoro-ethoxy)-benz>d]-2-(2,6-difluoro-4-methoxy-phenyl)-2-methoxy-acetamide was converted to (RS)- N- [4-carbamimidoyl-2-(2,2,2-trifluoro-ethoxy)-benzj^]-2-(2,6-difiuoro-4-methoX7-phen}d)-2-methoxy-acetamide hydrochloride according to general procedure D. Colorless soKd. MS 462.1 ([M+H]"") Examples 143 and 144 Using similar procedures to the ones described in example 138.2 and 138.3, (RS)-N-(4-cyano-2 -hydroxy-benzyl) - 2 - (2,6-difluoro-4 - roethoxy-phenyl) - 2- methoxy-acetamide (example 138.1) was converted to the following compounds: Example 143: (RS)-N-[4-Carbamimidoyl-2-(pyridin-3-yhnethox>')-benzyI]-2-(2,6- difluoro-4-methoxy-phenyl)-2-melhoxy-acetamide hydrochloride, MS 471.2 ([M+H]"") Example 144: (RS)-N-[4-CarbamimidoyI-2-(pyridin-4-ylmethoxy)-benzyI]-2-C2,6-difluoro-4-methoxy-phenyl)-2-methoxy-acetamide hydrochloride, MS 471.1 ([M+H]"") Referential Example 145 To a weil stirred ice cooled solution of 3,5-difluorophenol (30.0 g) in CH2CI2 (500 ml) under N2 were added tert-butyldiphenylchlorosilane (63.4 g) and imidazole (17.3 g). The reaction mixture was stirred 15 min before removing the cooling bath. After 3.5 h the reaction was stopped by washing 1 N HCl sol. (2 x 300 ml and 1 x 200 ml), sat. aq. NazCOs sol. (200 ml) and brine (200 ml). The aqueous layers were extracted with more CHiClj (200 ml). After drying (MgSO^) the solvent was evaporated to obtain 84.8 g (100 %) of tert-butyl-(3,5-difIuoro-phenoxy)-diphenyl-silane. Colorless oil. MS 368.1 (M^). Referential Example 146 A well stirred solution under N2 of tert-butyl-(3,5-difluoro-phenoxy)-diphenyl-silane (20.0 g) and N,N,N',N'-pentamethyldiethylenetriamine {9.9 g) in dry THE (600 ml) was cooled to -75 "C. A 1.6 M sol. of BuLi in Hex (35.6 ml) was added via syringe. The reaction mixture was stirred 1 h under cooling (-78 "C). A white precipitate was formed. Glyoxalic acid ethyl ester (50 % in Tol, 22.2 g) was added and it was stirred 2 h at -78 "C. The cooling bath was removed and the clear solution was left to warm to -10 °C (1 h). After dilution with TBME (500 ml) the mixture was washed with 1 N HCl (2 x 500 ml) and brine (250 ml), dried over MgS04 and the solvent was evaporated. The crude product was purified by CC (Hept. then Hept/CHzCb 1:4). 27.9 g (60 %) of (RS)-[4-(lert-butyl-diphenyl-silanyloxy)-2,6-difluoro-phenyl]-hydroxy-acetic acid ethyl ester were obtained next to 7.3 g (36 %) of recovered starting material. Colorless viscous oil. MS 488.4 ([M-t-NH4]'^). Referential Example 147 To a well stirred solution under N2 of (RS)-[4-(tert-butyl-diphenyl-silanyloxy)-2,6-difluoro-phenyl]-hydroxy-acetic acid ethyl ester (14.9 g) in Tol (100 ml) was added Ag20 (14.7 g). The mixture was heated in an oil bath at 115-120 °C and iodoethane( 12.8 ml) in Tol (50 ml) was slowly added from a dropping funnel. After a total of 2 h and 4 h more iodoethane (7.7 ml each) was added. After a total of 5.5 h heating was stopped and the mixture was left to stir over night at RT. The solids were filtered away over 1 cm of dicalite and were washed with AcOEt. The solvent was evaporated to obtain 16.3 g of crude product as a yellow oU. CC (Hepi;CH:Cl2 9:1 to pure CH2CI2) afforded 10.5 (66 %) of (RS)-[4-(tert-butyl-diphenyl-silanyloxy)-2,6-difluoro-phenyl]'ethoxy-acetic acid ethyl ester next to 2.6 g (17 %) of recovered starting material. Colorless oil. MS 453.2 (4, [M-OEty), 441.1 (24, [M--rBu]^)425.2 (100. [M-COOEt]'"). Referential Example 148 To a solution of (RS)-[4-(tert-buryl-diphenyl-si]anyIoxy)-2,6-difluoro-phenyl]-ethoxy-acetic acid ethyl ester (10.4 g) in a THE (50 ml), MeOH (50 ml) and H2O (20 ml) mixture was added LiOH.HaO {1.75 g) and it was stirred 2 h at 60 "C. After cooling water (240 ml) was added and the solution was washed with TBME (240 ml). The aqueous layer was collected, TBME was added (240 ml) and the mixture was acidified with 1 N HCl soL The aqueous layer was extracted with one more portion of TBME. The combined organic layers were dried (MgS04) and the solvent was evaporated to obtained an oil. Solid {RS)-(2,6-difluoro-4-hydroxy-phenyl)-ethoxy-acetic acid (4.6 g, 95 %) was obtained after addition of AcOEt, evaporation of it and drying on the high vacuum over night. Off-white solid. MS 231.1 ([M-H]"). Referential Example 149 (RS}-(2,6-Difluoco-4-hydro)cy-phenyl)-ethoxy-acetic acid (2,3 g) was dissolved in DMF (75 ml) and [(4-aminomethyl-phenyI)-iniino-methyl]-carbamic acid benzyl ester dihydrochloride [Prepared according to Ch. Lila, Ph. Gloanec, L. Cadet, Y. Herve, J. Fournier, F, Leborgne, T. J. Verbeuren, G. De Nanteuil, Synthetic Communications 1998, 28, 23, 4419-4429] (3.18 g) and HOBt (2.15 g) were successively added. The slurry was cooled in an ice bath and N-(3-dimethyl3minopropyl)-N'-ethylcarbodiimide hydrochloride (3.05 g) was added. EtjN (8.0 ml) was slowly added. The resulting mixture was left to stir over night warming up to rt. After removing the solvent precipitation from CH2C!2/MeOH 19:1 yielded the product. Drying over night on the high vacuum afforded 3.0 g (60 g) of pure (RS)'[(4-([2-(2,6-difluoro-4-hydroxy-phenyl)-2-ethoxy-acetylamino]-methyl}-phenyl)-imino-methyI]-carbamic acid benzyl ester. White solid. MS 498.3 (IM+H]"). Referential Example 150 (IlS)-[4-(tert-Butyl-diphenyl-silanylosy)-2,6-difluoro-phenyi]-ethoxy-acetic acid ethyl ester (6.85 g) was dissolved in THF (135 ml) and a 1 M TBAF sol. in THF (15.1 ml) was added. After 3 h the reaction mixture was poured on AcOEt (300 ml) and H20 (300 ml). The aqueous layer was detracted with two more portions of AcOEt (100 ml). The combined organic layers were washed with brine and dried (MgS04) and the solvent was evaporated. Crystallization from ice cold CH:Cl2 afforded 3.08 g (86 %) of (RS)-(2,6-difIuoro-4-hydroxy-phenyl)-ethoxy-acetic add ethyl ester. White crystals. MS 258.9 ([M-H]"). Example 151 (RS)-[(4-{[2-{2,6-difluoro-4-hydroxy-phenyl)-2-ethoxy-acetyiamino]-meth)i}-phea)d)-imino-metiiyI]-cartiamic add benzyl ester (100 mg) was dissolved in EtOH (2 ml). 1-25 M UCl in EtOH (0.1 ml) was added and the mixture was hydrogenated 1.5 h at 1 atm H2 in the presence of a catalytic amount of 10 % Pd/C. After filtration of the catalyst the solvent was removed to obtain 71 mg (88 %) of (RS)-N-(4-carbaiiiiinidoyl-benzyl)-2-(2,6-difluoro-4-hydroxy-phenyi)-2-ethoxy-acetainide hydrochloride. White powder. MS 364.3 ([M+H]^). Example 152 152.1 To a mixture of (RS)-[(4-i[2-(2,6-difluoro-4-hydroxy-phenyl)-2-ethoxy-acetylaiiiino]-methyl)-phenyl)-imino-methyl]-carbamic acid benzyl ester (100 mg), N-(2-hydroxyeth)d)morpholine (29 mg) and polymer bound triphenyiphosphine (-3 mmol/g, 167 mg) in CH2CI2 (2 ml) was added di-tert-butyl azodicarboxylate (93 mg) before shaking 22 h at rt. After filtration of the polymer the solvent was evaporated and the residue was purifiedbyHPLCtoobtain28mgof(23%)(RS)-{[4-({2-[2,6-difluoro-4-(2-morpholin-4-yI-ethoxy)-phenyl]-2-ethoxy-acetylainino}-methyl)-phenyl]-iinino-methyl}-carbamic add benzyl ester. 152.2 (RS)-{[4-({2-i2,6-Difluoro-4-(2-morpholin-4-yl-ethoxy)-phenyl]-2-ethoxy-acetylamino}-methyi)-phenyI]-irnino-methyi}-carbamic add benzyl ester (25 mg) was dissolved in EtOH (2 ml) and hydrogenated 2 h at rt and 1 atm H2 in presence of a catalytic amount of 10 % Pd/C. The catalyst was filtered off, the solvent was evaporated and (RS)-N-(4-carbamimidoyl-benzyi)-2-[2,6-difiuoro-4-(2-morpholin-4-yl-ethoxy)-phenyl]-2-ethoxy-acetamide dihydrochloride was obtained in quantitative yield by predpitation from AcOEt with a 4.6 N HCl sol. in AcOEt. White solid. MS 477.2 ([M+H]*). Examples 153,154 Examples 153 and 154 were obtained in analogy to example 152. 153 (RS)-N-(4-Carbanmmdoyi-benzyl)-2-(2,6-difluoro-4-phenethyioxy-phenyi)-2-ethoxy-acetamide hydrochloride from phenethyl alcohol. White solid. MS 468.2 ([M+H]"^). 154 (RS)-N-(4-Carbamimidoyl-ben2yl)-2-{4-cyclopropylmethoxy-2,6-difluoro-phenyi)-2-ethoxy-acetamide hydrochloride from hydroxymethylcyclopropane. White solid. MS 418.3 ([M+H]^}. Example 155 To a mixture of (RS)-[(4-{[2-{2,6-difluoro-4-hydroxy-phenyl)-2-ethoxy-acetylamino]-methylJ-phenyl)-imino-meth)d]-carbaniic add benzyl ester (300 mg), ethanol (61 mg) and polymer bound triphenylphosphine (~3 nunol/g, 501 mg) in CH2CI2 (6 ml) and DMF (1.5 ml) was added di-tert-butyl azodicarboxyiate (555 mg) before shaking 60 h at rt. After filtration of the polymer the solvent was evaporated and the residue was purified by HPLC. The resulting material was dissolved in MeOH (10 ml) and the solution was acidified with 2 mi of 125 M HCl in MeOH and hydrogenated 2 h at rt and 1 atm H2 in the presence of a catalytic amount of 10 % PdC. After filtration, evaporation of the solvent, HPLC purification and hydrochloride formation 27 mg (10 %) of (RS)-N-(4-carbamimidoyl-benz)d)-2-ethoxy-2-(4-ethoxy-2,6-difluoro-phen)d)-acetamide hydrochloride are obtained. Light yellow soUd. MS 392.1 ([M+H]+). Example 156 156.1 (R5)-(2,6-Di£luoro-4-hydroxy-phenyl)-ethoxy-acetic acid ethyl ester (500 mg) was dissolved in CH2CI2 (20 ml). Cu(0Ac)2 (349 mg), 4-methoxyphenylboronic add (876 mg) and MS4A were added followed by pyridine (760 mg). The mixture was stirred over night before filtration and evaporation of the solvent CC (Kept/ CH2CI2 1:4) afforded 455 mg (65 %) of (RS)-[2,6-difluoro-4-(4-methoxy-phenoxy)-phenyl]-ethoxy-acetic add ethyl ester. Yellow oil. 156.2 (RS)-[2,6-DifIuoro-4-(4-methoxy-phenoxy)-phenyl]-ethoxy-acetic acid ethyl ester (455 mg) was dissolved in THE (2.4 ml), MeOH (2.4 ml) and H2O (1.0 ml) and LiORHaO (104 mg) was added. The reaction mixture was stirred 1 h at 60 °C- The solution was diluted with cold H2O (15 ml) and TBME (15 ml) and acidified with 1 N HQ. The aqueous layer was extracted with two more portions of TBME (15 ml). The combined organic layers were dried (MgS04) and the solvent was evaporated to obtain 398 mg (95 %) of (RS)-[2,6-difluoro-4-(4-roethoxy-phenosy)-phenyl]-ethoxy-acetic add. White waxy solid. MS 336.9 {[M-H]-). 156.3 (RS)-[2,6-Difluoro-4-(4-methoxy-phenoxy)-phen^]-ethoxy-acetic add (398 mg) was dissolved in DMF (15 ml). [(4-aminomethyl-phenyi)-imino-methyi]-carbamic add benzyl ester dihydrochloride [Prepared according to Ch. Lila, Ph. Gloanec, L. Cadet, Y. Herve, J. Fournier, F. Leborgne, T. J. Verbem-en, G. De Nanteuil, Synthetic Communications 1998, 28, 23, 4419-4429] (367 mg) and 1-hydroxybenzotriazole (254 mg) were added and the mixture was cooled to 0 "C. N-(3-Dimethylaminopropyl)-N'-ethylcarbodiimide hydrochloride (254 mg) and triethylamine (1,38 ml) were added and it was stirred 1 h at 0 °C and 5.5 h at rL The solvent was evaporated and the residue was taken up in H2O (40 ml) and CH2CI2 (30 ml). The organic layer was separated, washed with brine and dried (MgS04). The aqueous layers were extracted with two more portions CH2CI2. After evaporation of the solvent CC (CH2CI2 to CH2Clz/MeOH 98:2) afforded 228 mg (32 %) of (RS)-{[4-({2-[2,6-difluoro-4-(4-methoxy-phenoxy)-phenyl]-2-ethoxy-acetylaniino}-roethyl)-phenyl]-imino-methylj-carbamic acid benz)^ ester. White foam. MS 602.0 ([M-H]-). 156.4 (RS)-{[4-({2-[2,6-Difluoro-4-(4-methoxy-phenoxy)-phenyl]-2-ethoxy-acetylamino}-meth)i)-phenyl]-imino-methyl}-carbainic add benzyl ester (181 mg) was hydrogenated 3 h in MeOH (3 ml) at rt and 1 atm H2 in the presence of 10 % Pd/C (6 mg) and 2 M NHs sol- in MeOH (75 |JL). The free benzamidine was isolated by filtration and evaporation of the solvent, dissolved in AcOEt (3 ml) and treated with 1 N HQ to obtain 109 mg (72 %) of (RS)-N-(4-carbamimidoyl-benz)d)-2-[2,6-difluoro-4-(4-methoxy-phenoxy)-phen)d]-2-ethoxy-acetamide. White solid. MS 470.1 ([M+H]"^). Examples 157-161 Examples 157-161 were prepared in analogy to example 156. 157.1 (RS)-[4-(3,4-Dimethoxy-phenoxy)-2,6-difIuoro-phenyl]-ethoxy-acetic add ethyl ester. Yellow oil. 157.2 (RS)-[4-(3,4-Dimethoxy-phenoxy)-2,6-di£luoro-phenyl]-ethox7-acetic acid. Yellow oil. MS 366.9 ([M-H]-). 157.3 (RS)-{[4-(|2-[4-(3,4-Dimethox7-phenoxy)-2,6-di£luoro-piien)'I]-2-ethoxy-acet)damino}-methyl)-phenyl]-iniino-methyl}-carbainic acid benzyl ester. White foam. MS 632.2 ([M-H]-). 157.4 (RS)-N-(4-Carbaiiuinidoyl-benzyl)-2-[4-(3,4-dimethoxy-phenoxy)-2,6-difluoro-phenyl]-2-etiioxy-acetamide hydrochloride. White soUd. MS 500.5 ([M+H]*). 158.1 (RS)-[2,6-Difluoro-4-(3-methoxy-phenoxy)-phenyl]-ethoxy-acetic acid eth)4 ester. Colorless oil. MS 384.4 ([M+NHi]"^). I5S.2 (RS)-[2,6-Difluoro-4-(3-methoxy-phenoxy)-phenyl]-ethoxy-acetic add. Off-white semisolid. MS 356.4 ([M+NHtD. 158.3 (RS)-{[4-({2-[2,6-Difluoro-4-(3-methoxy-phenoxy)-phenyi]-2-ethoxj'-acet)daininD}-methyI)-phenyl]-imino-methyl}-carbamic acid benzyl ester. Yellow foam. MS 604.3 ([M+HD. 158.4 (RS)-N-(4-Carbaminiidoyl-beii2yl)-2-[2,6-difluoro-4-(3-metho3(y-pheaoxy)-phenyl]-2- ethoxy-acetamide hydrochloride. White powder. MS 470.4 ([M+H]"*). 159.1 (RS)-[4-(3-AcetyIamino-phenoxy)-2,6-difluoro-phen)d]-ethoxy-acetic add ethyl ester. Colorless oil. MS 392.1 ([M-H]')- 159.2 (RS)-[4-{3-Acety]amino-phenoxy)-2,6-difluoro-phenyl]-ethoxy-acetic acid. Light yellow foam. MS 364.1 ([M-H]-). 1593 (RS)-{[4-({2-[4-{3-Acet)damino-phenox}')-2,6-difluoro-phenyl]-2-ethoxy-acet)daniino}- metiiyl)-phenyl]-iniino-methyI}-carbamic add benzyl ester. Colorless oil, MS 631.2 ([M+H]^). 159.4 (RS)-2-[4-{3-Acetylaimno-plienoxy)-2,6-difluoro~phenyl]-N-(4-carbamiinidoyl-benzyi)-2-ethoxy-acetamide hydrochloride. Off-white solid. MS 495.4 {[M-H]"). 160.1 (RS)-[4-(4-Cyano-phenoxy)-2,6-difluoro-phenyI]-ethoxy-acetic acid ethyl ester. White solid. 160.2 (RS)-[4-(4-Cyano-phenoxy)-2,6-difluoro-phenyl]-ethoxy-acetic acid. Yellowish gum. MS 332.4 ([M-H]"). 160.3 (RS)-{[4-({2-[4-(4-Cyano-phenoxy)-2,6-difluoro-phenyi]-2-ethoxy-acet)damino}-methyi)-phenyl]-iniino-inethyl}-carbamic acid benzji ester. Orange powder. MS 599.5 au+nr). 160.4 (RS)-N-(4-Carbamimidoyl-benzyl)-2-[4-(4-cyano-phenoxy)-2,6-di£luoro-phenj^]-2-ethoxy-acetamide hydrochloride. Yellowish foam. MS 465.5 ([M+H]*^). 361.1 (RS-)[2,6-Difluoro-4-(3-trifluoromethoxy-phenoxy)-phenyl]-ethoxy-acetic add ethyl ester. Colorless oil. MS 438.3 ([M+NH4]"'). 161.2 (RS)-[2,6-Difluoro-4-(3-trifluoromethoxy-phenoxy)-phenyl]-etiioxy-acetic add. Yellowish oil. MS 391.3 ([M-H]"). 161.3 (RS)-{[4-({2-[2,6-Difiuoro-4-(3-trifluoromethoxy-phenoxy)-phenyl]-2-ethoxy-acetyIamino}-meth)d)-phenyl]-imino-methyi}-carbaniic add benzyl ester. Off-white powder. MS 658.3 ([M+H]*). 161.4 (RS)-N-(4-Carbamimidoyl-benzyl)-2-[2,6-difluoro-4-(3-trifIuoromethoxy-phenoxy)-phenyl]-2-ethoxy-acetamide hydrochloride. White foam. MS 524.5 ([M-t-H]"^). Referential Example 162 A solution of (RS)-(2,6-difluoro-4-hydroxy-phenyl)-ethoxy-acetic acid ethyl ester (500 mg) in pyridine (5 ml) was placed under Ni and cooled to 0 °C. T^jO (813 mg) was added and the resulting solution was left to stir in the ice bath. After 18 h the reaction mixture was poured on a mixture of 50 ml 1 N HCl and ice. The product was extracted with AcOEt. The organic layer was washed with more 1 N HCl (50 ml), water (50 ml) and brine (30 ml). The aqueous layers were extracted with more AcOEt. After drying (MgS04) the solvent was evaporated to obtain 738 mg (98 %) of (RS)-(2,6-difluoro-4-trifluoromethanesulfonyloxy-phenyI)-ethoxy-acetic acid ethyl ester. Yellow oil. MS 393.4 ([M+H]"*"). Referential Example 163 To a solution of (RS)-(2,6-difluoro-4-trifluoromethanesulfonyloxy-phenyl)-ethoxy-acetic acid ethyl ester (200 mg) and 2-(trimethylsilyl)ethanol (603 mg) in DMSO (2.5 ml) was added triethylamine (1.8 ml) followed by Pd(OAc)2 (6 mg) and 1,3-bis(diphenylphosphino)propane (II mg). The flask was put under carbon monoxide and the reaction mixture was stirred 2 h at 70 °C. AcOEt (30 ml) was added and it was washed with 1 N HCl (2x 40 ml), water (2x 40 ml) and brine (30 ml). After drying (MgS04) the solvent was evaporated. CC (Hept/ AcOEt 98:2) afforded 151 mg (76 %) of (RS)-4-(ethoxy-ethoxycarbonyl-methyl)-3,5-difluoro-benzoic acid 2-trimethyisilanyl-ethyl ester. Colorless oil. MS 406.6 ([M+NH4]^). Referential Example 164 (RS-4-(Ethoxy-ethoxycarbonyl-methyI)-3,5-difluoro-benzoic acid 2-trimethyIsilanyl-ethyl ester (414 mg) was dissolved in DMF (1 ml) and a 1 M TBAF sol. in THE (1.12 ml) was added. After 3.5 h more TBAF sol. (0.5 ml) was added. AcOEt (15 ml) was added and the solution was washed with 1 N HCl (15 ml), water (15 ml) and brine (15 ml). After drying (Na2S04) the solvent was evaporated to yield 32 mg (100 %) of (RS)-4-(ethoxy-ethoxycarbonyl-methyl)-3,5-difluoro-benzoic acid. Colorless oil. MS 287.0 ([M-H] ). Example 165 165.1 l,r-Carbonyldiimidazole (88 mg) was dissolved in THF (1 ml) and a solution of (RS)-4-{ethaxy-ethoxycarbonyl-methyl)-3,5-difluoro-benzoic acid (156 mg) in THF (1 ml) was added. After 30 min stirring at rt isobutylamine (41 mg) was added and the mixture was stirred 3 h. AcOEt (20 ml) was added and the solution was washed with 1 N HCl (20 ml). The aqueous layer was extracted with two more portions AcOEt (20 ml), the the combined organic layers were dried (Na2S04) and the solvent was evaporated. CC (Hept/AcOET 3:1) afforded 125 mg (67 %) of (RS)-(2,6-difluoro-4-isobutylcarbamo)d-phen^)-ethoxy-acetic acid ethyl ester. White solid. 165.2 To a solution of (RS)-(2,6-difluoro-4-isobutylcarbamoyl-phenyl)-ethoxy-acetic acid ethyl ester (125 mg) in a mixture of THF (1 ml), MeOH (1 ml) and H2O (0.5 ml) was added LiOH.H20 (31 mg). After stirring 1.5 h at 60 "C AcOEt was added (10 ml) and the product was extracted with H2O (10 ml). The aqueous layer was collected, acidified with 1 N HQ and extracted with AcOEt (2 x 15 ml).The combined organic layers were dried (Na2S04) and the solvent is evaporated to obtain 76 mg (66 %) of (RS)-(2,6-difluoro-4-isobutylcarbamoyl-phenyl)-ethoxy-acetic acid. Off-white solid. MS 333.4 ([M+H]"*). 165.3 (RS)-(2,6-DifIuoro-4-isobutylcarbamoyi-phenyl)-ethoxy-acetic acid (71 mg) was dissolved in DMF (3.5 ml) and [(4-aminomethyl-phenyl)-imino-methyI]-carbamic acid benzyl ester dihydrochloride [Prepared according to Ch. Lila, Ph. Gloanec, L. Cadet, Y. Herv6, J. Foumier, F. Leborgne, T. J. Verbeuren, G. De NanteuH, Synthetic Communications 1998, 28, 23, 4419-4429] (88 mg), disopropylamine (114 mg) and 2-(lH-benzotriazole-l-yl)l,l,3,3-tetramethyIuronium tetrafluoroborate (TBTU) (80 mg) were subsequently added. After 30 min stirring at rt AcOEt (10 ml) was added and the organic layer was washed with 1 N HCl (2 x 10 ml), H^O (10 ml) and brine. The aqua^us layers were extracted with more AcOEt (10 ml). After drying (MgS04) the solvent was evaporated and the crude product was purified by HPLC to obtain 30 mg (23 %) of (RS)-[(4-{[2-(2,6-difluoro-4-isobutyIcarbamoyi-phenyl)-2-ethoxy-acetylamino]-methyI}-phenyl)-iniino-methyl]-carbamic acid benzyl ester. White soHd, MS 581.4 ([M+H]"^). 165.4 To a solution of [(4-{[2-(2,6-difluoro-4-isobutylcarbamo)d-phenyl)-2-ethoxy-acetylamino]-methyi}-phenyl)-imino-methyl]-carbaniic acid benzjd ester (27 mg) in MeOH (1 ml) and 2 M NH3 m MeOH (0.3 ml) was added a spatula tip of 10 % Pd/C. The mixture was placed under 1 atm H2 and stirred 4 h at rt. Filtration and evaporation of the solvent afforded 14 mg (64 %) of 4-(RS)-[(4-carbamimidoyl-benzjicarbamoyl)-ethoxy-methyi]-3,5-difluoro-N-isobutyI-benzainide hydrochloride. White solid. MS 447.5 ([M+H]-^). Examples 166-170 Examples 166-170 were prepared in analogy to example 165. Instead of using CD! for the first coupling step, the products were prepared by following the TBTU mediated coupling procedure described in example 165.3. 166 ; {RS)-4-[(4-CarbamimidoyI-benzykarbamoyl)-ethoxy-methyl]-N-ethyl-3,5-difluoro-benzamide hydrochloride. Yellowish solid. MS 419.4 ([M+H]"^). 167 (RS)-4-[(4-Carbamimidoyi-benzylcacbamoy!)-ethoKy-methyll-3,5-difluoio-H-(2-methoxy-ethyl)-benzamide hydrochloride. Yellow foam. MS 449.5 ([M+H]"^). 168 (RS)-4-[{4-Carbamimidoyl-benzylcarbamoyl)-ethoxy-methyl]-N-cyclopentyl-3,5-difluoro-benzamide hydrochloride. Yellow powder. MS 459.6 ([M+H]*), 169 (RS)-4-[(4-Carbamimidoyl-benzyicarbamoyI)-ethoxy-methyI]-3,5-difluoro-N-{2,2,2-trifluoro-ethylj-benzamidehydrochloride. Yellowish powder. MS 473.3 ([M+H]"*"). 170 (RS)-4-[{4-Carbamimidoyl-benzylcarbamoyl)-ethoxy-methyl]-N-cyclopropylmethyl-3,5-difluoro-benzamide hydrochloride. MS 445.5 ([M+H]"^). Referential Example 171 tert-Butydiphenylchlorosiiane (76.8 g) was added over 30 min to a cooled (0 °C) solution of 2,4-difluorophenol (34.6 g) and imidazole (19.9 G) in CHzCU (400 ml). The cooling bath was removed and the reaction mixture was stirred 2 h at rt before washing it with H2O (400 ml), 5 % aq. NaHCOs (300 ml) and brine. The aqueous layers were extracted with two more portions of CH2CI2 (150 ml). The combined organic layers were dried (Na2S04) and the solvent was evaporated to obtain 102 g (99 %) of tert-butyI-(2,4-difluoro-phenoxy)-diphenyl-silane. Colorless liquid. Referential Example 172 A solution under Ar of terl-butyl-(2,4-difluocQ-phenoxy)-diphenyl-siiane (102 g) and 1,1,4,7,7-pentamethyldiethylenetriamine (50.6 g) in DME (800 ml) was cooled to -70 °C before addition of 1.6 N n-BuLi in hexane (182 ml) over a period of 1 h. The yellow solution was stirred 1 h at -70 °C. 50 % glyoxalic acid ethylester in toluene (113 g) was added over a period of 1 h. The reaction mixture was stirred 2 h more at -70 °C before heating up over 1 "h to 0 °C. Sat. NH4 sol. (300 ml) was added and the pH was lowered to pH = 6 with 2 N HCl. The product was extracted with AcOEt (2 x 400 ml). The organic layers were washed widi brine (500 ml) and dried (NaiSO^) and the solvent was evaporated. CC (Hept to Hept/AcOEt 9:1) afforded 70.8 g (54 %) of (RS)-[3-(tert-butyl-diphenyl-silanyIoxy)-2,6-difluoro-phen)d]-hydroxy-acetic acid ethyl ester. Yellowish oQ. MS 488.5 ([M+H]""). Referential Example 173 A mixture of (RS)- [3-(tert-butyl-diphenyl-silanyloxy)-2,6-difluoro-phenyl] -hydroxy-acetic acid ethyl ester (70.8 g), Ag^O (69.7 g) and iodoethane (117 g) in Tol (700 ml) was stirred 68 h at 90 "C. After filtration and evaporation of the solvent the product was separated from the remaining starting material by MPLC (Hept to Hept/AcOEt 1:9). The procedure was repeated vrith the recovered starting material. 62.5 g (83 %) of (RS)-[3-(tert-butyI-diphenyl-siIanyloxy)-2,6-difluoro-phenyi]-ethoxy-acetic acid ethyl ester were obtained. Light yellow oil. MS 498.3 (1, M^); 441.1 (73. [M-fBu]'); 425.2 (33, [M-COOEt]*). Referential Example 174 To a solution of (RS)-[3-(tert-butyl-diphenyl-silanyloxy)-2,6-difluoro-phenyl]-ethoxy-acetic acid ethyl ester (62.5 g) in THF (250 ml) and MeOH (250 ml) was added H2O (200 ml) and LiOH.H20 (10.5 g) and it was stirred 2 h at 65 °C. MeOH and THF were evaporated and the aqueous residue was washed with Hept/Et20 9:1 ( 2 x 150 ml). The organic layers were extracted with two portions of H2O (200 ml). The combined aqueous layers were cooled in an ice bath and acidified with 35 ml 25 % aq. HCl. Extraction with AcOEt (3 X 200 ml) followed by washing with brine, drying (NajSOi) and evaporation of the solvent afforded 28.7 g (99 %) of (RS)-(2,6-difluoro-3-hydroxy-phenyl)-ethoxy-acetic acid. Yellow viscous oil. MS 231.2 ([M-H]'). Referential Example 174a A solution of (RS)-(2,6-difluoro-3-hydroxy-phenyl)-ethoxy-acetic acid (14.8 g) in EtOH (200 ml) and 1.25 N HCl in EtOH (60 ml) was stirred over night at rt. The solvent was evaporated and the residue was purified by CC (AcOEt/Hept 1:1) to obtain 15.5 g (93 %) of (RS)-(2,6-difluoro-3-hydroxy-phenyl)-ethoxy-acetic acid ethyl ester. Off-white sohd. MS 258.9 ([M-H]-). Referential Example 175 To a solution of (RS)-(2,6-difluoro-3-hydroxy-phenyl)-ethoxy-aceticacid (12.0 g) in DMF (600 ml) was added [(4-aminomethyl-phenyl)-imino-methyl]-carbamic acid benzyl ester dihydrochloride [Prepared according to Ch. Lila, Ph. Gloanec, L. Cadet, Y. Herve, J. Foumier, F. Leborgne, T. J. Verbeuren, G. De Nanteml, Synthetic Communications 199S, 28,23,4419-4429] (18.2 g) and l-hydroxybenzotriazole. The mixture was cooled to 0-5 X and EDC (15.8 g) and trietylamine (62 ml) were added. The mixture was stirred 1 h at 0-5 °C and over night at rt The solvent was evaporated and the residue was dissolved in CH2CI2 and washed with H2O (600 ml), and brine (300 ml). The aqueous layers were extracted with more CH2CI2 (2 x 300 ml). The combined organic layers were dried (Na2S04) and the solvent was evaporated. CO (CH2CI2/2 N NH3 in MeOH 97:3 to 19:1) afforded 10.2 g (40 %) of CRS)-[(4-{[2-(2,6-difIuoro-3-hydroxy-phen5d)-2-ethoxy-acetylamino]-methyl}-phenyi)-imino-methyl]-carbamic add benzyl ester. White foam. MS 498.2 ([M-HH]""). Example 176 (RS)-[(4-{[2-(2,6-Difluoro-3-hydroxy-phenyi)-2-ethoxy-acetyIamino]-methyl5-phenyi)-imino-meth)i]-carbamic acid benzjd ester (250 mg) was dissolved in EtOH (20 ml) and 0.9 N HQ in EtOH (5 ml) was added. After 10 min stirring 10 % Pd/C (II mg) was added and the mixture was hydrogenated 2 h at rt under 1 atm Hj. Filtration, evaporation of the solvent and trituration with MeCN (4 ml) afforded the solid product that was washed with two portions of Et20 (5 ml). After drying on the vacuum at 50 °C 175 mg (87 %) of (RS)-N-(4-carbamimidoyi-benzyl)-2-(2,6-difluoro-3-hydroxy-phenyi)-2-ethoxy-acetamide hydrochloride were obtained. White solid. MS 364.0 ([M+H]"*"). Examples 177-207,207a, 2D7b Examples 177-207b were prepared in two steps (E1/E2 and F1/F2) from (RS)-[(4-{ [2-(2,6-difiuoro-3-hydroxy-phenyi)-2-ethoxy-acetylamino]-methyl}-phenyl)-iniiQO-niethyl]-carbamic add benzyl ester and an appropriate alcohol by the following procedures: Procedure El: A mixture of 1.0 equivalent of (RS)-[(4-{[2-(2,6-di£luoro-3-hydTOxy-phenyI)-2-etioxy-acet)^amino]-methyl}-phenyl)-imino-methyI]-carbamic add benzyl ester, 1.1 equivalents of alcohol, ca. 2 equivalents of polymer bound triphenylphosphine (~3 mM/g) and 2.0 equivalents ofdi-tert-butylazodicarboxylate are shaken 2 days atrLThe reaction mixture is absorbed on a 20 g siEca gel samplet and the product is purified by chromatography (CH2CI2/2 N NHa in MeOH system) Procedure E2: As El but with 1.25 equivalents alcohol and stirriR2 40 h. Procedure Fl: The products from procedure E were hydrogenated at rt and 1 atm H2 in EtOH/1.25 N HCl in EtOH 5:1 in the presence of a catalytic amount of 10 % Pd/C. Filtration and evaporation of the solvent afforded the final compounds. Procedure F2: As Fl but in MeOH instead of EtOH. Were necessary the final compounds were purified by HPLC. No. Name Alcohol Proc. Appearance MS [M+H]^ 177 (RS)-N-(4-Carbamimidoyl- Diethylene El/Fl Brownish 480.1 benzyl}-2-ethoxy-2-{3-[2-(2- ^ycol foam ethoxy-ethoxy)-ethoxy]-2,6- monoethyl difluoro-phenyll-acetamide ether hydrochloride 178 (RS)-N-(4-Carbamimidoyl- 3-Dimethyl- El/Fl Yellowish 449.1 benzyl)-2-[3-(3- amino-1- foam dimethyiamino-propoxy)-2,6- propanol difluoro-phenyl]-2-ethoxy- acetamide dihydrochloride 179 {RS)-N-{4-Carbamimidoyl- Triethylene El/Fl Brownish 510.3 benzyl)-2-(2,6-difluoro-3-{2- glycol foam [2-(2-methoxy-ethoxy)- monomethyl ethoxyj-ethoxyj-phenyl)-2- ether ethox/-acetamide hydrochloride 180 (RS)-N-(4-Carbamknidoyl- 4-Pyridine- El/Fl Brownish 483.1 benzyl)-2-[2,6-dxfluoro-3-(3- propanol foam pyridin-4-yI-propoxy)- phenyl]-2-ethoxy-acetaroide dihydrochloride 181 (RS)-N-(4-CarbamimidoyI- l-(2-Hydroxy- El/Fl Brownish 461.0 benzyl)-2-[2,6-difluoro-3-(2- ethyl)- foam pyrroKdin-1-yl-ethoxy)- pyrrolidine phenyl]-2-ethoxy-acetamide dihydrochloride 182 (RS)-N-(4-Carbaiiuinidoyl- l-Methyl- El/Fl White solid 432.0 benzyl)-2-[2,6-difluoro-3-{l- cyclopropan- methyl-cyclopropylmethoxy)- emethanol phenyl j-2-ethoxy-acetaimde hydrochloride 183 {RS)-N-{4-Carbamimidoyl- l(2-Hydroxy- E2/F2 Yellow foam 475.8 benzyl)-2-[2,6-difluoro-3-(2- ethyl)- piperidin-1-yl-ethoxy)- piperidine phenyl] -2-ethoxy-acetainide dihydrochloride 184 (RS,RS)-N-{4- 3-Methyl-3- E2/F1 Off-white 484.2 Carbamimidoyl-benzyl)-2- [3- oxetane- foam (3-ch]oro-2-h)'droxymeth7l-3- methanol methyl-prop oxy)-2,6-difluoro- phenyl]-2-ethoxy-acetamide hydrochloride 185 {RS)-N-(4-Carbamimidoyl- 2-Ethoxy- E2/F2 Brownish 436.2 benzyI)-2-ethoxy-2-[3-(2- ethanol foam ethoxy-ethoxy)-2,6-difluoro- phenyl] -acetamide hydrochloride 186 (RS)-N-(4-Carbamimidoyl- 2-Methoxy- E2/F2 Brownish 422.1 benzyl)-2-[2,6-difluoro-3-(2- ethanol foam methoxy-ethoxy)-phenyl]-2- ethoxy-acetamide hydrochloride 187 (RS)-N-(4-Carbamimidoyl- 3-Dimethyl- E2/F2 WHtefoam 477.1 ben2yl)-2-[3-{3- amino-2,2- dimethylamino-2,2-dimethyl- dimethyl-1 - propoxy)-2,6-dLfluoro- propanol phenyl] -2-ethoxy-acetamide dihydrochloride 188 CRS)-N-(4-Carbaroimidoyl- 2-(2-Thieny!)- E2/F2 Brownish 474.1 benzyl)-2-[2,6-difluoro-3-(2- ethanol foam thiophen- 2-yl- ethoxy) - phenyl] -2-ethoxy-acetamide hydrochloride 189 (RS,RS)-N-(4- Tetrahydro- E2/F2 Brownish 448.1 CarbamimidoyI-benzyl}-2- furfuryl alcohol foam [2,6-difluoro-3-(tetrahydro- fLiran-2-ylmethoxy) -phenyl] -2-ethoxy-acetamide . hydrochloride 190 {RS)-N-(4-CarbamimidoyI- 2-Methyl E2/F2 White solid 420.1 benzyl)-2-(2,6-difluoro-3- propanol isobutoxy-phenyl) -2 -ethoxy-acetamide hydrochloride 191 CRS,RS,RS)-N-(4- 2-Methyl- E2/F2 Brownish 432.0 Carbamimidoyl-benzyl)-2- cyclopropane- foam [2,6-difluoro-3-{2-methyl- methanol cydopropylmethoxy)-phen)d] - 2-ethoxy-acetainide hydrochloride 192 (RS)-N-(4-Carbaniimidoyl- 2-Cydopropyl- E2/F2 White foam 432.2 benzyl)-2-[3-(2-cyclopropyl- ethanol ethoxy)-2,6-difluoro-phenyl]- 2-ethoxy-acetamide hydrochloride 193 (RS)-N-(4-Carbamimidoyl- Ethanol E2/F2 YeUowish 391.9 benzyl)-2-ethoxy-2-C3-ethoxy- foam 2,6-difluoro-phenyi)- acetamide hydrochloride 194 (RS)-N-(4-Carbaniimidoyi- 1-PropanoI E2/F2 Brownish 406.0 benz7l)-2-(2,6-difluoro-3- foam propoxy-phenyl)-2-ethoxy- acetamide hydrochloride 195 CRS)-N-(4-earbamimidoyl- Hydroxy- E2/F2 Brownish 417.9 benzyl)-2-(3- methyl- foam cyclopropylmethoxy-2,6- cyclopropane difluoro-phenyl)-2-ethoxy-acetamide hydrochloride 196 (RS}-N-(4-Carbamimidoyl- 2-Dimethyl- E2/F2 Brownish 434.9 benzyl)-2-[3-(2- aminoetianol foam dimethylamino-ethoxy)-2,6- difluoro-phenyl]-2-ethoxy-acetamide dihydrochloride 197 (RS)-N-{4-Carbamimidoyl- Cyclobutane- E2/F2 Brownish 432.0 ben2yl)-2-(3- methanol foam cyclobutylmethoxy-2,6- difluoro-phenyl)-2-ethoxy-acetamide hydrochloride 198 (RS)-lSl-(4-Carbamimidoyl- N-(2-Hydroxy- E2/F2 Brownish 475.0 benzyl)-2-{2,6-difluoro-3-[2- ethyl)-2- foam (2-oxo-pyrrolidin-l-yI)- pyrrolidone ethoxy] -phenyU - 2-ethQxy-acetamide hydrochloride 199 (RS)-N-(4-Carbaminiidoyl- 3,3,3- E2/F2 Brownish 460.1 benzyl)-2-[2,6-difluoro-3- Trifluoro-l- foam (3,3>3-trifluoro-propoxy)- propanol phenyI]-2-ethoxy-acetamide hydrochloride 200 (RS}-N-(4-Carbamimidoyl- 3-(2-Hydrox)'- E2/F2 Yellow foam 469.9 benzyl}-2-[2,6-difIuoro-3-(2- ethyl)pyridine pyridin-3-yl-ethoxy)-phenyI]- 2-ethoxy-acetainide dihydrochloride 201 (RS)-N-(4-Carbamiinidoyl- N,N-Diethyl-2- E2/F2 Brownish 477.1 benzyl)-2-(3- hydroxy- foam diethylcarbamoyimethoxy-2,6- acetamide difluoro -phenyl) -2-ethoxy-acetamide hydrochloride 202 (RS)-N-(4-Carbamimidoyl- N-(2-Hydroxy- E2/F2 Brownish 477.0 ben2yl)-2-[2,6-difluoro-3-{2- ethyl)- foam morpholLn-4-)4-ethoxy)- morpholine phenyI]-2-ethoxy-acetaniide dihydrochloride 203 (RSJlS)-N-(4- l-Methyl-3- E2/F2 Brownish 475.0 Carbamimidoyl-benzyl)-2- piperidine- foam [2,6-di£luoro-3-{ 1-methyl- methanol piperidin-3-yImethoxy) - phenyl]-2-ethoxy-acetaniide dihydrochloride 204 {RS,RS)-N-(4- l-Methyl-2- E2/F2 Brownish 475.2 Carbamimidoyl-benzyl)-2- piperidine- oil [2,6-difluoro-3-(l-methyl- methanol piperidin-2-ylmethoxy) -phenyl] -2-ethoxy-acetamide dihydrochloride 205 (RS)-N-(4-Carbamimidoyl- 2-{2-Hydroxy- E2/F2 Yellow foam 469.0 benzyl)-2-[2,6-difluoro-3-(2- ethyl)pyridine pyridin-2-yl-ethoxy)-phenyl]- 2-ethoxy-acetamide dihydrochloride 206 (RS,RS)-N-(4- 2-Piperidm- E2/F2 Brownish 475.0 Carbamimidoyl-benzyl)-2- eethanol foam [2,6-difluoro-3-(2-piperidin-2- yl-ethoxy)-plienyl]-2-ethoxy-acetamide dihydrochloride 207 (RS)-N-(4-Carbamimidoyl- Methanol(3 E2/F2 Off-white 378.5 benzyl)-2-(2,6-difluoro-3- equivalents) foam methoxy-phenyl)-2-ethoxy- acetamide hydrochloride 207a {RS)-N-(4-Carbamimidoyl- Cyclohexanol E2/F2 Off-white 446.0 benzyl)-2-(3-cydohex}doxy- sohd 2,6-difluoro-phenyl}-2-ethoxy-acetamide hydrochloride 207b (RS)-N-(4-Carbamimidoyl- 1-tert-Butoxy- E2/F2 Off-white 447.5 benzyl)-2- [2,6-difluoro-3- carbonyl-4- foam {piperidin-4-yloxy)-phenyl]-2- hydroxy- ethoxy-acetamide piperdine dihydrochloride Example 208 208.1: To a solution under Ar of (RS)-(2,6-difluoro-3-hydroxy-phenyl)-ethoxy-acetic acid ethyl ester (320 mg) in CH2C12 (10 ml) was added copper(II)acetate (230 mg), 4-fluorobenzeneboronic acid 516 mg) and powdered MS4A (2 g). After addition of triethlyamine (622 mg) the mixture was stirred 40 h at rt. The solids were filtered away and the solvent was evaporated. CC (AcOEt:Hept 1:9 to 1:1) afforded 154 mg of (RS)-[2,6-difluoro-3-(4-fiuoro-phenox7)-phenyll-ethoxy-acetic acid ethyl ester as a brownish oil. 208.2; (R,S)-[2,6-Difluoro-3-(4-fluoro-phenoxy)-phenyl]-ethoxy-acetic acid ethyl ester (145 mg) was dissolvedin MeOH/THF 1:1 (2 ml) and H2O (0.5 ml) and LiOH.H20 (36 mg) were added. The solution was stirred 2 h at 60 °C. THF and MeOH were evaporated and the residue was diluted with H2O (10 ml) and acidified with 1 N HCl (pH = 2). The product was extracted with AcOEt (2 x 30 ml). The organic layers were washed with brine (20 ml). Drying {Na2S04) and evaporation of the solvent afforded 140 mg of (RS)-[2,6-difluoro-3-(4-fluoro-phenoxy)-phenyl]-etho3cy-acetic acid as a yellowish oil. 208,3: To a solution of (RS)-[2,6-difIuoro-3-(4-fluoro-phenoxy)-phen)d]-ethoxy-acetic acid (140 mg) in DMF (5 ml) was added [(4-aminomethyI-phenyl)-iinino-inethyI]-carbamic acid benzyl ester dihydrochloride (149 mg) and l-hydroxybenzotriazole (92 mg). The mixture was cooled to 0-5 °C and EDC (130 mg) and triethylamine (0.5 mi) were added. After stirring 2 h at 0-5 °C the solvent was evaporated and the residue was partitioned between KjO (25 ml) and AcOEt (25 ml). The aqueous layer was extracted with more AcOEt (25 ml). The organic layers were washed with brine (25 ml) and dried (Na2S04) and the solvent was evaporated. CC (AcOEt/Hept 1:3 to 4:1) afforded 120 mg of (R,S)-N-[4-(amino-benzyloxycarbonimidoyIiniino-methyl)-benzyI]-2-[2,6-difluoro-3-(4-fluoro-phenoxy)phenyl)-2-ethoxy-acetamide as white crystals. 208.4: (R,S)-N-[4-(Aniino-benzyloxycarbonimidoylimino-methyl)-benzyl]-2-[2,6- difluoro-3-(4-fluoro-phenoxy)phenyl)-2-ethoxy-acetamide (120 mg) was dissolved in MeOH (10 ml) and 1.25 N HCl in MeOH (2 ml) was added. The mixture was hydrogenated 1 h at 1 atm H; and rt in presence of 10 % Pd/C (12 mg). After filtration and evaporation of the solvent (R,S)-N-(4-carbaminiidoyl-benzyl)-2-[2,6-difluorO'3-(4-fluoro-phenoxy)-phenyl]-2-ethoxy-acetamide hydrochloride was obtained by crystallization from MeCN/EtjO. White solid. MS 458.5 ([M+H]^). Examples 209-212 Examples 209-212 were prepared in analogy to example 208: No. Name Appearance MS [M-HH]^ 209 (RS)-N-(4-Carbamimidoyl-benzyl)-2-[2,6- Off-white 441.5 difiuoro-3-(pyridin-3-yloxy)~phenyl]-2-ethoxy- foam acetamide dihydrochloride 210 (RS)-N-(4-Carbamimidoyl-benzyl)-2-[2,6- White 508.1 difluoro-3-(3-trifluoromethyI-phenoxy)- crystals phenyl] -2-ethoxy-acetamide hydrochloride 211 (RS)-N-(4-Carbamimidoyl-benzyI)-2-(2,6- White 454.1 difluoro-3-m-tolyloxy-phenyl)-2-ethoxy- crystals acetamide hydrochloride 212 (RS)-N-(4-Carbaniunidoyl-benzyl)-2-ethoxy-2- White 484.1 [3-(3-ethoxy-phenoxy)-2,6-difluoro-phenyl]- crystals acetamide hydrochloride Example 213 To an ice cooled mixture under Ar of (RS}-(2,6-difIuoro-3-hydroxy-phenyl)-ethoj:y-acetic ad-d, 4-aminomethyl-benzordtrile hydrochloride (10.6 g) and 1-hydroxybenzotriazole {9.8 g) in DMF (140 ml) was added EDC (13.9 g) and triethylamine (55 ml). The mixture was stirred 2.5 h at 0 °C and 2 d at rt The solvent was evaporated and H2O (250 ml) was added. The product was extracted with AcOEt (2 x 200 ml). The organic layers were washed with 5 % NaHCOs aq. sol. (100 ml), brine 100 ml). After drying (Na2S04) the solvent was evaporated. CC (AcOEt/Hept 2:3) afforded 7.66 g (49 %) of (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-3-hydroxy-phenyl)-2-ethoxy-acetamide. White solid. MS 364.1 ([M+NH4]'^). General procedure G for the preparation of the N-hydroxy-benzamldines: 1.0 equivalent of the benzonitrile was dissolved in EtOH and 5.0 equivalents of hydroxylamine hydrochloride and triethylamine were added. The solution was stirred over night before addition of 5.0 equivalents more of hydrox)damine hydrochloride and triethylamine. After stirring again over night the products were isolated by evaporation of the solvent and CC. General procedure H for the reduction of the N-hydroxy-benzamidines: The n-hydroxy-benzamidines were hydrogenated in EtOH over night at rt and 1 atm H2 in presence of a catalytic amount of 10 % Pd/C and 10 equivalents of AcOH. The products were isolated by filtration and evaporation of the solvent. Where necessary a crystallization or CC were carried out. Example 214 To a solution under Ar of (RS)-N-(4-cyano-ben2yl)-2-(2,6-difluoro-3-hydroxy-phenyl)-2-ethoxy-acetamide (200 mg) in DMF (10 ml) was added CSCO3 (226 mg) and 3-bromopentane (105 mg). The solution was stirred over night at 80 °C. The solvent was evaporated and the residue was taken up in H2O (50 ml). The product was extracted with AcOEt (2 X 100 ml). The organic layers were washed with H2O (2 x 50 ml) and dried (NaaS04) and the solvent was evaporated. CC (AcOEt/Hept 2:3 to AcOEt) afforded 190 mg (79 %) of (RS)-N-(4-cyano-benzyl)-2-ethoxy-2-[3-(l-ethyl--propoxy)-2,6-difluoro- 1 phenyl]-acetamide. This material was converted to (RS)-N-(4-carbarnimidoyl-benzyl)-2- ;thoxy-2-[3-(I-ethyl-propoxy)-2,6-difluoro-phenyl]-acetamide acetate by the sequence of procedures G and H. Off-white soHd. MS 434.4 ([M+H]^). Examples 215-216 Example 215 was prepared in analogy to example 214. Example 216 was prepared from (RS)-N-(4-cyano-ben2yl)-2-(2,6-difluor 0-3-hydroxy-phenyl)-2-ethoxy-acetamide by a sequence of procedures E2, G and H. No. Name Appearance MS [M+H]* 215 (RS)-N-(4-Carbamimidoyl-benzy!)-2-(3- Brown solid 432.5 cyciopentyIoxy-2,6-difluoro-phenyI)-2-ethoxy- acetamide acetate 216 (RS)-N-(4-CarbamimidoyI-benzyl)-2-[2,6- White solid 448.2 difluoro-3-(tetrahydro-pyran-4-yioxy)-phenyl]-2- ethoxy-acetamide acetate Referential Example 217 A solution under Ar of (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-3-hydroxy-phenyl)-2-ethoxy-acetamide (5.0 g) in pyridine (50 ml) was cooled to -10 "C and Irifluoromethanesulfonic acid anhydride (4.5 g) was added over a period of 10 min. The reaction mixture was stirred 2 h at 0 °C. More Irifluoromethanesulfonic acid anhydride was added {4.5 g) over 30 min and it was stirred 30 min more at 0 "C. Pyridine was evaporated, H2O (200 ml) was added and the product was extracted with AcOEt (2 x 100 ml). The organic layers were washed with brine, combined and dried (Na2S04) before evaporation of the solvent. CC (AcOEfHept to AcOEt) afforded 6.2 g (89 %) of (R,S)-trif!uoro-methanesulfonic acid 3-[(4-cyano-benzylcarbamoyl)-ethoxy-methyl]-2,4-difluoro-phenyl ester. YeUowoil. MS 479.1 ([M+H]*). General procedure I for the reduction of the N-hydroxy-benzamidines: To a 0.015 M solution of the N-hydroxy-benzamidine in EtOH was added AcOH (10 equivalents) and Raney-Ni (2.5 equivalents, Degussa 313 Z type). The reaction mixture was stirred over night at rt. The catalyst was filtered away, the solvent was evaporated, H2O (3/5 of the initial EtOH volume) was added and the mixture was treated with 25 % aq. NH4OH (1/5 of the initial EtOH volume). The solvent was evaporated and the residue was purified by CC (CH2Cl2/MeOH/25 % aq. NH4OH). The products were isolated as the hydrochlorides after treatment of a niethanoHc solution with 1.25 N HCl/MeOH. Example 218 218.1 To a solution of (RS)-trifluoro-methanesulfonic add 3-[(4-cyano-benzylcarbamoyl)-ethoxy-methyl]-2,4-difluoro-phenyl ester (570 mg) in dioxane (20 ml) was added bis(pinacolato)diboron (454 mg), dry KOAc (351 mg) and [PdCl2(PPh3)2] (25 mg). The reaction mixture was stirred 24 h at 100 °C. After cooling to rt 5-bromopyridine (377 mg), 2 N aq. NasCOa sol. (6 ml) and [PdCl2(PPh3)2] (25 mg) were added. The resulting mixture was stirred 1 h at 90 "C. The sohds were filtered away and washed with H2O (100 ml) and AcOEt (80 ml). The aqueous layer was isolated and extracted with more AcOEt (100 ml). The organic layers were washed with brine (2 X 80 ml), combined and dried over Na2S04. The solvent was evaporated and the crude product was purified by CC (AcOEt/Hept 3:7 to 3:1) to obtain 315 mg (65 %) of (RS)-N-{4-cyano-benzyl)-2-(2,6-difluoro-3-pyridin-2-yl-phenyl)-2-ethoxy-acetamide. Colorless oil. MS 408.3 ([M+H]^). 218.2 (RS)-N-(4-Cpno-benzyl)-2-(2,6-difluoro-3-pyridin-2-yl-phenyl)-2-ethoxy-acetamide (310 mg) was converted into (RS)-2-(2,6-difluoro-3-pyridin-2-yl-phenyl)-2-ethoxy-N-[4-(N-hydroxycarbamimidoyI)-benzyl]-acetamide (320 mg, 95 %) following procedure G. Colorless oil. MS 441.3 ([M+H]^). 218.3 (RS)-2-(2,6-Difluoro-3-pyridin-2-yl-phenyl)-2-ethoxy-N-[4-(N-hydroxycarbamimidoyI)-benzyll-acetamide (315 mg) was converted into (RS)-N-(4-carbamimidoyl-benzyl)-2-(2,6-difluoro-3-pyridin-2-yl-phenyl)-2-ethoxy-acetamide dihydrochloride (225 mg, 63 %) following procedure I Off-white foam. MS 425.3 ([M+H]"*"). Examples 219-222 Examples 219-222 were prepared in analogy to example 218: No. Name Aryl-X Appearance MS [M-i-Hl^ 219 (RS)-N-(4-Carbamimidoyl- 5-Bromo-2- Off-white 455.5 benzyl)-2- [2,6-difluoro-3-(6- methoxy-pyridine foam methoxy-pyridin-3-yl)-plienyi]- 2-ethoxy-acetamide dihydrochioride 220 {RS)-N-(4-Carbamimidoyl- 3-Bromopyridine Off-white 425.4 benzyl)-2-(2,6-difluoro-3- foam pyridin-3-yl-phenyl)-2-ethoxy- acetamide dihydrochioride 221 (RS)-N-(4-Carbamimidoyl- 5-Bromo- White foam 426.4 benzyI)-2-{2,6-difluoro-3- pyrimidine pyrimidin-5-yl-phenyl)-2- ethoxy-acetamide dihydrochioride 222 (RS)-N-{4-Carbamimidoy!- 4-Iodopyridine Yellowish 425.3 benzyl)-2-(2,6-difiuoro-3- foam pyridin-4-yl-phenyl)-2-ethoxy- acetamide dihydrochioride Referential Example 223 (RS)-[3-(tert-Butyl-diphenyl-siIanyloxy)-2,6-difiuoro-phenyl]-methoxy-acetic acid ethyl ester was prepared in analogy to example 173 from (RS)-[3-(tert-butyl-diphenyl-siIanyIoxy)-2,6-difluoro-phenyi]-hydroxy-acetic acid ethyl ester and iodomethane. Yellowish oU. MS 484.2 (4, [M'^]^); 427.1 (29, [M-tBu']""); 411.2 (14, [M-COOEt]^). Referential Example 224 I A 1.0 M solution of TBAF in THF (100 ml) was added under stirring to a solution of (RS)-(2,6-difluoro-3-hydroxy-phenyl)-methoxy-acetic acid ethyl ester (38.5 g) in THF (500 mi). The reaction mixture was stirred over night at rt before evaporation of the solvent. The residue was partitioned between 600 ml AcOEt/HjO 1:1 and extracted with more AcOEt (200 ml). The organic layers were washed with brine 200 ml, combined and dried over NajSO*. After evaporation of the solvent CC {CH2CI2, then CH2CI2/2 N NH3 in MeOH 97:3) yielded 18.3 g {94 %) of (RS)-(2,6-difluoro-3-hydroxy-phenyl)-methoxy-acetic acid ethyl ester. YeUowish solid. MS 24S.3 ([M-H]"). Referential Example 225 A solution of (RS)-(2,6-difluoro-3-hydroxy-phenyl)-methoxy-acetic add ethyl ester (11.6 g) and LiOH.HiO in THF (40 ml), MeOH (40 ml) and H2O was stirred 2 h at 65 "C. The organic solvents were evaporated, H2O was added (50 ml) and the pH was lowered with 2 N HCl to pH — 2. The product was extracted with AcOEt (3 x 50 ml). The organic layers were washed with brine (100 ml), combined and dried (Na2S04). Evaporation of the solvent afforded 9.6 g (94 %) of (RS)-(2,6-difluoro-3-hydroxy-phenyl)-methoxy-acetic add. White solid. MS 217.1 ([M-H]")- Referential Example 226 (RS)-N-(4-Cyano-benzyl)-2-(2,6-difluoro-3-hydroxy-phenyl)-2-methoxy-acetamide was prepared from (RS)-(2,6-difluoro-3-hydroxy-phenyl)-methoxy-acetic add in analogy to (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-3-hydroxy-phenyl)-2-ethoxy-acetamide (example 213). White foam. MS 330.8 ([M-H]"). Referential Example 227 (RS)-Trifluoro-methanesulfonic acid 3-[(4-cyano-benzyicarbamoyl)-methoxy-methyl]-2,4-difluoro-phenyl ester was prepared from (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-3-hydroxy-phenyl)-2-methoxy-acetamide in analogy to (RS)-trifluoro-methanesiilfonic add 3-[(4-cyano-benzylcarbamoyl)-ethoxy-methyl]-2,4-difluoro-phenyl ester (example 217). YeUowoil. MS 482.3 ([M-i-NH^]"^). General procedure K for the Suzuki coupling reaction: To a 0.1 M solution in Tol of (RS)-triSuoro-metlianesuIfonic add 3"[(4-cyano-benzyicarbamoyl)-methoxy-methyI]-2,4-difluoro-phenyl ester (1.0 equivalent) was added KzCOj (1.5 equivalents) and the boronic acid (2.0 equivalents). The solution was degassed by bubbling 10 min Ar through it before adding [Pd(PPh)4] (0.03 equivalents). The reaction mixture was stirred over night at 100 "C before isolation of the product by CC (AcOEtHept). Examples 228-233 Examples 228-233 were prepared from (RS)-trifluoro-methanesulfonic acid 3-[(4-cyano-beii2ylcarbamoyl)-methoxy-methyl]-2,4-difluoro-phenyl ester by subsequently carrying out procedures K, G and H. Procedure H was modified by replacing HCl with 10 equivalents of AcOH. No. Name RBCOH); Appearance MS [M+H]^ 228 (RS)-N-(4-CarbamimidoyI-benzyl)-2- m-Tolyl- White 424.0 (2,4-difluoro-3'-methyl-biphenyl-3-y!)- boronic acid crystals 2-methoxy-acetamide 229 (RS)-N-(4-CarbaminiidoyI-benzyI)-2- 4-Methyl- Orange 424.4 (2,4-difluoro-4'-methyl-biphenyl-3-yl)- benzene foam 2-raethoxy-acetamide hydrochloride boronic acid 230 (RS)-N-(4-Carbaminiidoyl-benzyI)-2- 4-Fluoro- White solid 428.5 methoxy-2-(2,4,4'-trifluoro-biphenyl-3- benzene yl)-acetamide acetate boronic acid 231 {RS)-N-(4-CarbamimidoyI-benzyl)-2- 4-(Methy]thio)- Whitesolid 456.4 {2,4-difluoro-4'-methylsulfanyl- phenyl-boronic biphenyl-3-yl)-2-methoxy-acetamide acid hydrochloride 232 (RS)-N-(4-Carbarainiidoyl-benzyl)-2- 3-(Trifluoro- Whitesolid 478.3 (2,4-difluoro-3'-trifiuoromethyl- niethyl)phenyl biphenyl-3-yl)-2-methoxy-acetamide boronic acid acetate 233 (RS)-N-(4-Carbamimidoyi-benzyl)-2- 4-Methoxy- Whitesolid 440.5 (2,4-difluoro-4'-methoxy-biphenyl-3- phenylboronic yl)-2-methoxy-acetamide add hydrochloride Referential Example 234 To a solution in DMSO (40 ml) of (RS)-trifluoro-methanesiilfonic acid 3-[(4-cyano-benzyicarbamoyl)-methoxy-methyi]-2,4-difluoro-phen}4 ester (5.0 g) was added MeOH (21.8 ml), EtsN (4.5 ml), [Pd(0Ac)2] (73 mg) and l,3-bis-(diphenylphosphino)propane. The solution was saturated with carbon monoxide. The dark reaction mixture was stirred 2 h at 70 "C and 1 atm carbon monoxide. The mixture was poured on ice cold H2O (400 ml) and 2 N aq. HCl sol. (30 ml). The product was extracted with AcOEt (2 x 200 ml). The organic layers were washed with brine (2 x 200 ml), combined and dried over Na2S04. The solvent was evaporated and the residue was fractionated by CC (AcOEt/Hept 1:9 to 4:1) to obtain 2.45 g (61 %) of (RS)-3-[(4-cyano-benzylcarbamoyl)-methoxy-methyl]-2,4-difiuoro-benzoic acid methyl ester. Yellowish solid. Referential Example 235 A solution of (RS)-3-[(4-cyano-benzyIcarbamoyl)-methoxy-methyl]-2,4-di£luoro-benzoic acid methyl ester (2.05 g) and LiOH.HjO (241 mg) in THF/MeOH/HiO 1:1:0.5 (75 mi) was stirred 1 h at rt. The organic solvents were evaporated, ice cold H2O (50 ml) was added and the pH was lowered (pH = 2) by addition of 2 N aq. HCl sol. The product was extracted with AcOEt (2 x 120 ml). The organic layers were washed with brine (100 ml), combined and dried over Na2S04. Evaporation of the solvent yielded 1.80 g of (RS)-3-[(4-cyano-benzylcarbamoyI)-methoxy-methyl]-2,4-difluoro-benzoic acid. White solid. MS 359.4 ([M-H]'). Example 236 236.1 To a solution under Ar of (RS)-3-[(4-cyano-benzylcarbamoyl)-methoxy-methyl]-2,4-difluoro-benzoic acid (150 mg) in DMF (2 ml) was added l.l'-carbonyldiimidazole (74 mg). The reaction mixture was stirred 15 min at rt before addition of morpholine. After stirring 2 h at rt hydroxylamine hydrochloride (289 mg) and EtsN (0.3 ml) were added. The reaction mixture was stirred 20 h at rt, then it was poured on H2O (20 ml) and extracted with AcOEt (2 x 20 ml). The organic layers were washed with brine and dried (NaiSO^) and the solvent was evaporated. CC (AcOEt/MeOH 99:1 to 9:1) yielded 111 mg (58 %) of (RS)-2-[2,6-difluoro-3-(morpholine-4-carbonyl)-phenyl]-N-[4-(N-hydroxycarbaminiidoyl)-benzyl]-2-methoxy-acetamide. White solid. MS 463.5 ([M+H]"^). 236.2 A solution of (RS)-2-[2,6-difluoro-3-(morpholine-4-carbonyl)-phenyl]-N-[4-(N-hydroxycarbamimidoyl)-benzyl]-2-methoxy-acetamide (125 mg) was hydrogenated 2 days atrtand 1 atm H2 in presence of 10 % Pd/C {13 mg)andAcOH (143 mg). The catalyst was filtered away and the solvent was evaporated to obtain 115 mg of (RS)-N-(4-carbaniiniidoyI-benzyl)-2-[2,6-difluoro-3-(morpholine-4-carbonyI)-phenyI]-2-methoxy-acetamide acetate. Off-white solid, MS 447.1 ([M+H]^). Examples 237-241 Examples 237-241 were prepared in analogy to example 236: No. Name Amine Appearance MS 237 (RS)-3-[(4-Carbamimidoyl- Ethylamine Off-white 405.3 benzylcarbamoyl)-methoxy-methyI]- hydrochloride solid N-ethyl-2,4-difluoro-benzamide acetate 238 {RS)-3-[(4-Carhamimidoyl- 2-Methoxy- Off-white 435.3 benzylcarbamoyl)-methoxy-methyl]- ethylamine solid 2,4-difluoro-N-(2-methoxy-ethyl)- benzamide acetate 239 (RS)-3-[(4-Carbamimidoyi- Diethylamine Off-white 433.4 benzylcarbamoyO-methoxy-methyl]- foam N,N-diethyI-2,4-difluoro-benzamide acetate 240 (RS)-3-[(4-CarbamimidoyI- 2,2,2- Off-white 459.1 benzylcarbamoyl)-methoxy-methyl]- Trifluoro- solid 2,4-difluoro-N-(2,2,2-trif[uoro-ethyl)- ethylamine benzamide acetate 241 (RS)-3-[(4-Carbamimidoyl- Aminomethylc Off-white 431.4 benzylcarbamoyl)-methoxy-methyl]- yclopropane solid N-cyclopropyImethyl-2,4-difluoro- benzamide acetate Examples 242-244 Example 242-244 were prepared from (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-3-hydroxy-plienyl)-2-methoxy-acetaniide by a sequence consisting of a Mitsiinobii reaction (procedure E2), the formation of the N-hydroxy-benzamidines (procedure G) and the reduction to the benzamidines (procedure I). No. Name ROH Appearan MS ce [M+H]^ 242 (RS)-N-(4-Carbamimidoyi-benzy!)- 2-(Hydroxy- White 441.5 2-[2,6-difluoro-3-(pyridin-2- methyl)pyridine) foam ylmethoxy)-phenyl]-2-methoxy- acetamide dihydrochloride 243 {RS)-N-(4-Carbamimidoyl-benzyl)- 3-CHydroxy- Off-white 441.3 2-[2,6-difluoro-3-(pyridin-3- ineth}d)pyridine foam yhnethoxy) -phenyl J -2-methoxy- acetamide dihydrochloride 244 (RS}-N-(4-Carbamimidoyl-benzyl)- 4-(Hydroxy- Greenish 441.4 2-[2,6-difluoro-3-(pyridin-4- methyl)pyridine foam ylmethoxy)-phenyI]-2-methoxy- acetamide dihydrochloride Example 245 (RS)-N-(4-Carbaraimidoyl-benzyl)-2-[2,6-difluoro-3-(4-fluoro-phenoxy)-phenyI]-2-methoxy-acetamide acetate 245.1 To a solution of (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-3-hydroxy-phenyl)-2-methoxy-acetamide (370 mg) in 1,2-dichloroethane (10 ml) was added copper(II)acetate (222 mg), 4-fiuorobenzoic acid (467 mg) and powdered MS4A (2 g). EtsN (563 mg) was added and the mixture was stirred 2 days at rt. The mixture was passed over silica ge! eluting with AcOEt. CC (AcOEt/Hept 1:3 to 3:1) yielded 203 mg (61 %) of (RS)-N-(4-cyano-benzyl)-2-[2,6-difluoro-3-(4-fluoro-phenoxy)-phenyl]-2-methoxy-acetainide. Yellow oil. MS 427.0 ([M-HH]"). 245.2 {RS)-N-(4-Cyano-benzyi)-2-[2,6-di£luoro-3-{4-fluoro-phenoxy)-phenyl]-2-methox7-acetamide (200 mg) was transformed in (RS}-2-[2,6-difluoro-3-(4-fluoro-phenoxy}-phenyl]-N-[4-(N-hydroxycarbainiinidoyl)-benzyl]-2-methoxy-acetamide (174 mg, 81 %) by procedure G. 245 Reduction of (RS)-2-[2,6-difluoro-3-(4-fluoro-phenoxy)-phenyl]-N-[4-(N- hydroxycarbamimidoyi)-ben2yl]-2-methoxy-acetamide (173 mg) by procedxire H afforded 176 mg (93 %) of (RS}-N-(4-carbamiinidoyl-beiizyl)-2-[2,6-difluoro-3-(4-fluoro-phenoxy)-phenyl]-2-methoxy-acetaniide acetate. White crystals. MS 444.1 ([M+H]"*"). Example 246 (RS)-N-(4-Carbamimido)d-benzyl)-2-[2,6-difluoro-3-(pyridin-3-yloxy)-phenyl]-2-methoxy-acetamide acetate was prepared in analogy to example 245. Off-white crystals. MS 427.1 ([M+H]^). Example 247 247.1 To a solution of (RS)-2-(4-bromo-2,6-difluoro-phenyl)-N-(4-cyano-beiizyl)-2-methoxy-acetamide (example 69.1, 247 mg) in 1,2-dimethoxyethane (5 ml) was added tetralds(triphenyiphosphine) palladium (0) (73 mg). A solution of phen)dboromc acid (118 mg) in EtOH (2.1 ml) and a solution of sodium carbonate (563 mg) in water (3 ml) were added. The mixture was stirred for 1.5 h at 85 "C. The solids were filtered off and the filtrate was evaporated. The product was purified by flash chromatography (cyclohexane/EtOAc 2:1 => EtOAc) to give (RS)-N-(4-cyano-benzyi)-2-(3,5-difluoro-biphenyl-4-yI)-2-methoxy-acetamide (172 mg). Off-white solid. MS 393.1 ([M+H]"^) 247.2 (RS)-N-(4-Cyano-benzyl)-2-(3,5-difiuoro-biphenyl-4-yl)-2-methoxy-acetaniide was converted to (RS)-N-(4-carbamimidoyi-benz)d)-2-(3,5-difluoro-biphenyl-4-)d)-2-methoxy-acetamide hydrochloride according to general procedure D. Off-white solid, MS 410.2 ([M+H]"") Example 248 248.1 The crude 4-bromo-2,6-difluorobenzaldehyde described in example 69.1 was reacted according to general procedure A using ethanol / dioxane as a solvent The product of this reaction was subsequently coupled with 4-aininomethyi benzonitrile according to general procedure B to give (RS)-2-(4-bromo-2,6-difluoro-phenyl)-N-{4-cyano-benzyl)-2-ethoxy-acetamide. Yellow oil. 248.2 In analogy to example 247.1, (RS)-2-(4-bromo-2,6-difluoro-phenyl)-N-(4-cyano-benzyl)-2-ethoxy-acetamide was reacted with phenylboronic acid to give (RS)-N-(4-cyano-benz)d)-2-(3,5-difluoro-biphenyl-4-yl)-2-ethoxy-acetamide. Yellow solid. MS 407.3 ([M+H]"^) 248.3 (RS)-N-(4-Cyano-benzyl)-2-(3,5-difIuoro-biphenyl-4-yl)-2-ethoxy-acetamide was converted to {RS)-N-(4-carbamiinidoyl-benzyi)-2-(3,5-difluoro-biphenyl-4-5d)-2-ethoxy-acetamide hydrochloride according to general procedure D. Ofif-white solid. MS 424.4 C[M+H1") Example 249 Using similar procedures to the ones described in example 248.2 and 248.3, (RS)-2-{4-bromo-2,6-difluoro-phenyl)-N-(4-cyano-benzyl)-2-ethoxy-acetamide was converted to (RS)-N-(4-carbamimidoyl-benzyI)-2-[2,6-difiuoro-4-(lH-indol-5-yl)-phenyI]-2-ethoxy-acetamide acetic acid. Colorless solid. MS 463.0 ([M+H]"*") Example 250 250.1 In analogy to example 247.1, (RS)-2-(4-bromo-2,6-difluoro-phenyl)-N-(4-cyano-benzyl)-2-ethoxy-acetamide (example 248.1) was reacted with 2-fiiranboromc acid to give (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-4-furan-2-yl-phenyl)-2-ethoxy-acetamide. Off-white soUd. MS 397.0 {[M+H]"^) 250.2 In analogy to example 15.5, (RS)-N-(4-cyano-ben2yl)-2-(2,6-difluoro-4-ftiran-2-yl- phenyl)-2-ethoxy-acetamide was reacted with hydroxylamine hydrochloride to give (RS)- 2-(2,6-difluoro-4-furan-2-yI-phen)d)-2-ethoxy-N-[4-(N-hydroxycarbamiinidoyl)-benzyl]- acetaraide. Colorless solid. MS 430.0 ([M+H]"^) 250.3 In analogy to example 37.5, (RS)-2-{2,6-difluoro-4-fiiran-2-yl-phenyl)-2-ethoxy-N-[4-(N-hydroxycarbaminiidoyl)-benzyI]-acetamide was reduced to give (RS)-N-(4-carbamimidoyl-ben2yi)-2-(2,6-difluoro-4-ftiran-2-yl-phenyl)-2-ethoxy-acetainide acetate. Colorless soHd. MS 414.0 ([M+H]"") Example 251 As a side product of example 250.3, there was obtained N-{4-carbamimidoyI-benzyl)-2-[2,6-difluoro-4-(tetrahydro-furan-2-yl)-phenyl]-2-etlioxy-acetamide acetic acid . Off-white soUd. MS 418.0 ([M+H]"") Example 252 252.1 In analogy to example 247.1, (RS)-2-(4-bromo-2,6-difluoro-phenyl)-N-(4-cyano-ben2yl)-2-ethoxy-acetamide (example 248.1) was reacted with 3-hydroxyphenylboronic add. The product of this reaction was alkylated with ethylbromoacetate and cesiumcarbonate in DMF (analogous to example 16.4) to give (RS)-{4'-[(4-cyano-ben2:ylcarbamoyl)-ethoxy-methyl]-3',5'-difluoro-biphenyl-3-yloxy}-acetic add ethyl ester. Colorless oil. MS 509.1 ([M+H]") 252.2 (RS)-{4'-[(4-Cyano-benzyIcarbamoyl)-ethoxy-methyI]-3',5'-difluoro-biphenyl-3-yIoxy)-acetic acid ethyl ester was converted to (RS)-l4'-[(4-carbamimidoyi-benZ}dcarbamoyl)-ethoxy-meth)4]-3',5'-difluoro-biphenyl-3-yloxy}-acetic add ethyl ester hydrochloride according to general procedure D. Colorless foam. MS 526.2 ([M+H]"^) 252,3 In analogy to example 20.1, (E5)-{4'-[(4-carbamimidoyl-benzyicarbamoyl)-ethoxy-methyl]-3',5'-difluoro-biphenyl-3-yloxy}-acetic add ethyl ester hydrochloride was hydrolyzed to (RS}-{4'-[(4-carbamimidoyl-benzylcarbamo)d)-ethoxy-methyl]-3',5'-difluoro-biphen5d-3-yloxy}-acetic add. Colorless solid. MS 498.3 ([M+H]^) Using similar procedures to the ones described in example 252.1 and 252.2, (RS)-2-(4-bromo-2,6-difluoro-phenyl)-N-(4~q^ano-benzyl)-2-ethoxy-acetamide (example 248.1) was converted to the following compounds: Example 253: (RS)-N-(4-Carbamimidoyl-benzyl)-2-(3'-carbamoylmethoxy-3,5-difluoro-biphenyl-4~yl)-2-ethoxy-acetamide hydrochloride,MS 497.2 ([M+H]"*) Example 254: (RS)-N-(4-Carbamimidoyl-ben2yl)-2-[3,5-difluoro-3'-(2-hydroxy-ethoxy)-biphen)d-4~yl]-2-ethoxy-acetamide hydrochloride, MS 484.3 ([M+H]"^) Example 255: (RS)-N-(4-Carbamiinidoyl-benzyl)-2-[3'-(3-dimethyIaniino-propoxy)-3,5-difluoro-biphenyl-4-yl]-2-ethoxy-acetamidehydrochloride, MS 525.3 ([M+H]"^) Example 256 256.1 In analogy to example 247.1, (RS)-2-(4-bromo-2,6-difluoro-phenyi)-N-(4-cyano-benzyI}- 2-ethox)'-acetamide (example 248.1) was reacted with 2-hydroxyphenyIboronic add to give {RS)-N-(4-cyano-benzyl)-2-(3,5-difiuoro-2'-hydroxy-biphenyl-4-yl)-2-etlioxy-acetamide. Off-white solid. MS 423.0 ([M+H]"") 256.2 In analogy to example 22.1, {RS)-N-(4-cyano-benzyI)-2-(3,5-difluoro-2'-hydrox}'-biphenyI-4-yl)-2-ethoxy-acetamide was reacted in a Mitsunobu reaction with 2-benzyloxy-ethanol, diethyl azodicarboxylate and triphenyl phosphine in THF to give (RS)-2-[2'-(2-benzyIoxy-ethoxy)-3»5-difluoro-biphenyl-4-yl]-N-(4-cyano-benzyl)-2-ethoxy-acetamide. YeUow oil. MS 557.2 ([M+H]"") 256.3 {RS)-2-[2'-(2-Ben2yloxy-ethoxy)-3,5-difIuoro-biphenyl-4-yl]-N-(4-cyano-benzyl)-2-ethoxy-acetamide was converted to (RS)-2-[2'-(2-benzyioxy-ethoxy)-3,5-difluoro-bipheny!-4-yl]-N-(4-carbamimidoyI-benzyI)-2-ethoxy-acetamide hydrochloride according to general procedure D. Colorless solid. MS 574.3 {[M+H]"^) Example 257 257.1 In analogy to example 16.4, (RS)-N-{4-cyano-ben2;)^)-2-{3,5-difluoro-2'-hydroxy- biphen)d-4-yl)-2-ethoxy-acetamide (e:rample 256.1) was alkylated with l-chloro-2- dimethylaminoethane hydrochloride and cesimncarbonate in DMF to give (RS)-N-(4- cyano-benzyl)-2-[2'-(2-dimetbylamino-ethoxy)-3,5-difluoro-biphenyl-4-yl]-2-ethoxy- acetamide. Colorless solid. MS 494.1 ([M+H]"^) 257.2 (RS)-N-{4-Cyano-benzyl)-2-[2'-(2'dimethylamino-ethoxy)-3,5-difluoro-biphenyl-4-)i]-2-ethoxy-acetamide was converted to {RS)-N-(4-carbamiinidoyI-benzyl)-2-[2'-(2-dimethylamino-ethoxy)-3,5-dtfluoro-biphenyl-4-yl]-2-etho::q'-acetaniide hydrochloride according to general procedure D. Colorless sohd. MS 511.1 ([M+H]"*") Using similar procedures to the ones described in example 257.1 and 257.2, (RS)-N-(4-cyano-benzyl)-2-(3,5-di£luoro-2'-hydroxy-biphenyI-4-yl)-2-ethoxy-acetainide {example 256.1) was converted to the following compounds: f Example 258: {RS)-N-(4-CarbaininiidoyI-benzyl)-2-[3,5-difluoro-2'-(2-hydro3y-ethosy)-biphenyl-4-yl]-2-ethoxy-acetamide hydrochloride, MS 484.1 {[M+H]'^) Example 259: (RS)-{4'-[(4-Carbamimidoyl-benzylcarbariioyl)-ethoxy-rQethyl]-3',5'-difluoro-biphenyl-2-yloxy}-acetic acid ethyl ester hydrochloride, MS 526.2 {[M+H]"^) Example 260 In analogy to example 20.1, (RS)-{4'-[(4-carbamiiiudoyl-benzjdcarbamoyl)-ethoxy-methyi]-3',5'-difluoro-biphenyl-2-yloxy}-acetic acid ethyl ester hydrochloride was hydrolyzed to (RS)-{4'-[(4-carbamimidoyI-ben2ylcarbamoyI)-ethoxy-methyl]-3',5'-difluoro-biphenyI-2-yloxy}-acetic add. Coloriess solid. MS 496.4 ([M-H]") Example 261 261.1 In analogy to example 16.4, (RS)-N-(4-cyano-benzyl)-2-(3,5-difluoro-2'-hydroxy- biphenyI-4-yl)-2-ethoxy-acetamide (example 256.1) was alkylated wilii iodoacetamide and cesiumcarbonate in DMF. The product of this reaction was reacted with hydroxylamine hydrochloride in analogy to example 15.5 to give (RS)-2-(2'-carbamoy(inethoxy-3,5- di£luoro-bipheny]-4-yl)-2-ethoxy-N-[4-(N-hydroxyc3rbamimidoyl)-benzyl]-acetamide. Colorless solid. MS 513.1 CIM+H]"") 261^ In analogy to example 37.5, (RS)-2-(2'-carbamoyimethoxy-3,5-difluoro-biphenyl-4-y!)-2- ethoxy-N-[4-(N-hydroxycarbamimidoyI)-benzyl]-acetaniide was reduced to give (RS)-N- {4-carbamimidoyl-benzyl)-2-(2'-carbamoylmethoxy-3,5-difluoro-biphen54-4-)d)-2- ethoxy-acetamide acetate. Colorless soUd. MS 497.2 ([M+H]"^) Example 262 262.1 To a solution of (RS)-2-(4-bromo-2,6-difluoro-phen)^)-N-(4-cyano-benz;^)-2-ethoxy- acetamide (example 248.1, 800 mg) in DMSO (9 ml) were added bis(pinacolato)diboron (546 mg), potassium acetate (581 mg) and dichloro(l,r- bis(diphenylphosphino)ferrocene)paUadium(II) (44 mg).The mixture was stirred at 85°C for 5 h and at 50 "C ovemighL Dicfaloro(l,l'- bis(diphenyiphosphino)ferrocene)palladium(n) (44 mg) was added and the mixture was stirred at 85°C for 8 h and at 50 °C ovemighL After cooling to r.t., ice water was added. The mixture was filtered and the filtrate "was extracted with EtOAc. The org. phase was dried, filtered and concentrated. The product was purified by chromatography (Si02, cyclohexane /EtOAc 4:1 ^> EtOAc) to give CRS)-N-(4-cy^no-benz)d)-2-[2,6-difluoro-4-(4,4,5,5-tetramethyl-[l,3,2]dioxaborolan-2-yI)-phenyI]-2-ethoxy-acetamide (625 mg). Off-white soHd. MS 457.3 ([M+H]"") 262.2 To a stirred solution of (RS)-N-(4-q'ano-benzyl)-2-[2,6-difiuoro-4-(4,4,5,5-tetrainethyl- [l,3,2]dioxaborolan-2-yl)~phen)d]~2-ethoxy-acetamide (300 mg) in l^-dimethoxyethane (8 ml) was added 4-bromopyridine hydrochloride (387 mg). A solution of sodium carbonate (210 mg) in water (2.1 ml) and dichloro(l,r- bis(diphenylphosphino)ferrocene)palladium (11) (48 mg) were added. The mixture was I stirred at 85'C for 4 h and at r.L overnight. After cooling to i.t, ice water was added. The mixture was filtered and the filtrate was extracted with EtOAc. The org. phase was washed with brine, dried, filtered and concentrated. The product was purified by chromatography ■ (Si02, cyclohexane /EtOAc 2:1 => EtOAc) to give (RS)-N-(4-cyano-benz)^)-2-(2,6-difiuoro-4-pyridin~4-yI-phen)^)-2-ethoxy-acetamide (189 mg). Ofif-white solid. MS 408.2 ([M+H]") 262.3 (RS)-N-(4-Cyano-benzyl)-2-(2,6-difluoro-4-pyridin-4-yl-phen}d)-2-etlioxy-acetamide was converted to (RS)-N-(4-carbaniimidoyl-benzyi}-2-(2,6-difiuoro-4-pyridin-4-yl-phen>d)-2-ethoxy-acetamide hydrochloride according to general procedure D. Colorless solid. MS 425.2 ([M+H]-") Using similar procedures to the ones described in example 262.2 and 262.3, (RS)-N-(4-cyano-benzyl)-2-l2,6-difluoro-4-(4,4,5,5-tetramethyi-[l,3,2]dioxaborolan-2-yi)-phen)4]-2-ethoxy-acetamide (example 262.1) was converted to the following compounds: Example 263: (RS)-N-(4-Carbamimidoyl-benz)4)-2-(2,6-difluoro-4-pyrimidin-5-)d-phen)d)-2-ethoxy-acetamide hydrochloride, MS 426.2 ([M+H]"^) Example 264: (RS)-N-{4-Carbamimidoyl-benz)4)-2-(2,6-difluoro-4-pyrimidin-2-yl-phenyl)-2-ethoxy-acetamide hydrochloride, MS 426.1 ([M+H]*) Example 265: (RS)-N-(4-Carbamiimdoyl-benz)4)-2-(2,6-difluoro-4-pyridin-2-yI-phenyl)-2-ethoxy-acetamide hydrochloride, MS 425.1 ([M+H]"^) Example 266: (RS}-2-[4-(2-Amino-pyriDiidin-5-yl}-2,6-difluoro-phenyi]-N-(4-carbamimido}d-benzyl)-2-ethoxy-acetamide hydrochloride, MS 441.0 ([M+H]"*") E:rample267:(RS)-N-(4-Carbamimidoyl-benzyl)-2-(2,6-difluoro-4-pyridin-3-yl-phenyl)-2-ethoxy-acetamidehydrochloride , MS 424.6 ([M]"*") Example 268: (RS)-2-[4-(6-Ainino-pyridin-2-yl)-2,6-difluoro-phen7l|-N-(4-carbainimidoyl-benz7l)-2-ethox7-acetamidehy-drochloride , MS 440.1 {[M+H]"^) Example 269: (RS)-2-[4-{5-Amino-pyridm-2-yl)-2,6-difluoro-phenyl]-N-(4-carbaniimidoyl-beiizyl)-2-ethoxy-acetamide hydrochloride, MS 440.0 ([M+H]'*') Example 270: (RS)-4'-[(4-CaTbamimidoyl-benzylcarbainoyl)-ethoxy-iiiethyi]-3',5'-difluoro-biphenyl-3-carboxyIic acid methyl ester hydrochloride, MS 482.1 {[M+H]"^) Example 271: (RS)-(2-[4-(6-Amino-pyridin-3-yl)-2,6-difiuoro-phenyl]-N-{4-carbamimidoy]-beiizyl)-2-ethoxy-acetamide hydrochloride, MS 440.3 ([M+H]'^) Example 272 In analogy to example 20.1, (RS)-4'-[(4-carbamimidoyi-benzylcarbamoyl)-ethoxy-methyl]-3',5'-difluoro-biphenyl-3-carboxyiic acid methyl ester hydrochloride (example 270) was hydrolyzedto (RS)-4'-[(4-carbamimido)d-benzylcarbamo54)-ethoxy-methyl]-3',5'-difluoro-biphen)d-3-carboxyUc acid. Off-white solid. MS 468.1 ([M+H]^) Example 273 In analogy to example 15.4, (RS)-{2-[4-(6-amino-pyridin-3-yI)-2,6-difluoro-phenyl]-N-(4-carbamimidoyl-benzyl)-2-ethoxy-acetamide hydrochloride (example 271) was reacted with ethylchloroformate and triethylamine in DMF to give (RS)-{amino-[4-({2-[4-C6-araino-pyridin-3-yl)-2,6-difluoro-phenyl] -2-edioxy-acetyIamino} -methyi)-phenyl] -methylene)-carbamic add eth}^ ester. Off-white solid. MS 512.1 ([M+H]"^) Example 274 To a a solution of (RS)-(2-[4-(6-amino-pyridin-3-yl)-2,6-difluoro-phen}d]-N-(4- carbamimidoyl-benzyl)-2-ethoxy-acetamide hydrochloride (example 271,60 mg) in DMF (1 ml) were added hydroxylamine hydrochloride (27 mg) and triethylamine (38mg).The mixture was stirred at 50 °C for 2.5 h. After cooling to r.t, the mixture was partitioned between EtOAc and ice water and extracted with EtOAc. The oR2. phase was washed with water, dried, filtered and concentrated to give (RS}2-[4-(6-aniino-pyridin-3-yi)-2,6-difluoro-phenyl]-2-ethoxy-N-[4-(N-hydroxycarbaniimidoyl)-benzyi]-acetamide{57mg). Colorless solid. MS 456.0 ([M+H]^) Example 275 275.1 In analogy to example 262.2, {RS)-N-(4-cyano-ben2yl)-2-[2,6-difluoro-4-(4,4,5,5- tetraineth.yl-[l,3,2]dioxaborolan-2-yl)-ph.enyl]-2-ethoxy-acet:amide (example 262.1) was reacted with 2-bromobenzaldehyde to give (RS)-N-(4-cyaiio-benZ)d)-2-(3,5-di£luoro-2'-formyl-biphenyl-4-yI)-2-ethoxy-acetamide. Off-white solid. MS 435.0 ([M+H]"^) 275.2 To a suspension of (RS)-N-(4-cyano-benzyI)-2-(3,5-difiuoro~2'-formyl-biphenyl-4-yl)-2-ethoxy-acetamide (500 mg) in EtOH (1.2 nJ) at 0 "C was added sodium borohydride (91 mg). After 5 min the ice bath was removed. Ice water was added and the mixture was extracted with EtOAc. The org. phase was dried, filtered and concentrated. The product was purified by chromatography (Si02, cyclohexane /EtOAc 1:2 => EtOAc) to give (RS)-N-(4-cyano-benzyl)-2-(3,5-difluoro-2'-hydroxymethyl-biphenyl-4-yl)-2-ethoxy-acetamide {413 mg). Colorless solid. MS 437.0 ([M+H]*) 275.3 (RS) -N-{4-Cyano-benzjd) -2-( 3,5-difluoro-2'-hydroxymethyl-biphenyl-4-yl)-2-ethoxy-acetamide was converted to (RS)-N-(4-carbaiiiimidoyl-benzyl)-2-(3,5-difluoro-2'-hydroxyinethyl-biphenyl-4-yi)-2-ethoxy-acetamide hydrochloride according to general procedure D. Colorless solid. MS 454.0 ([M+H]*) Example 276 As a side product of example 275.3, there was obtained (RS)-N-(4-carbanumidoyl-benzyl)-2-(2'-chloromethyi-3,5-difluoro-biphenyl-4-^)-2-ethoxy-acetamide. Colorless solid. MS 472.0 ([M+H]"") Example 277 277.1 In analogy to example 15.5, (RS)-N-(4-cyano-benz}d}-2-(3,5-difluoro-2'-formyl-biphen)4-4-yl)-2-ethoxy-acetainide (example 275.1) was reacted with hydroxjdamine hydrochloride to give (RS)-2-[3,5-difluoro-2'-(hydroxyimino-methyl)-biphenyi-4-yI]-2-ethoxy-N-[4-(N-hydroxycarbamimidoyI)-ben2:)d]-acetamide. Colorless solid. MS 483.1 ([M+H]"^) 277.2 In analogy to example 37.5, (RS)-2-[3,5-difiuoro-2'-(hydroxyimino-meth)4)-biphen}4-4- yl]-2-ethox}'-N-[4-(N-hydroxycarbanumido5d)-benzyl]-acetamide was reduced to give (RS)-2-(2'-aminomethyl-3,5-difluoro-biphenyl-4-yl}-N-(4-carbamimidoyi-benzyl)-2- ethoxy-acetamide acetate. Light green soHd. MS 453.4 ([M+H]"^) Example 278 27S.1 2-Fluoro-3-hydroxy-4-methox}'-benzaldehyde (CAS 79418-73-8) was benzylated to give 3-beiizylo]Q'-2-fluoro-4-methox7-ben2aldehyde in analogy to example 15.4. Light yellow oil. MS 260.1 ([M]"^) 278.2 3-Beiizyloxy-2-fluoro-4-methoxy-benzaldehyde was converted to (RS)-(3-benzyloxy-2-fluoro-4-methoxy-phenyl)-methoxy-acetic add according to general procedure A. Colorless gum. MS 319.1 ([M-H]") 278.3 (RS)-(3-Benzyloxy-2-fluoro-4-methoxy-phenyl)-methoxy-acetic acid was debenzylated by hydrogenation in analogy to example 16.2 and then coupled with 4-aminobenzonitrile according to general procedure C to give (RS)-N-(4-cyano-benzyl)-2-(2-fluoro-3-hydroxy-4-methoxy-phenyl)-2-methoxy-acetamide. Off-white foam. MS 345.1 ([M+H]"^) 278.4 A mixture of (RS)-N-(4-cyano-bemyl)-2-(2-fluoro-3-hydroxy-4-methoxy-phen)d)-2-methoxy-acetamide (150 mg), phenyl boronic add (58 iR2), copper (11) acetate (79 mg), pyridine (0.18 ml) and activated molecular sieves (4 A) at r.t in CH2CI2 under an argon atmosphere was stirred for 24 h. More copper (II) acetate (40 mg), phen)4 boronic add (29 mg) and pyridine (0.9 ml) were added to the mixture and stirring was continued for 16 h. The mixture was filtered and the cake washed with 15 ml CH2C12, The filtrate was washed with 1.0 N Ha (25 ml), 1.0 N NaOH (25 ml) and brine (25 ml), dried (MgS04). filtered and concentrated (rotavapor) to leave the crude product as a brown gum. The crude produd was purified by flash chromatography (cyclohexane => cydohexane/EtOAc 2:3) to give (RS)-N-(4-Cyano-benzyl)-2-(2-fluoro-4-methoxy-3-phenoxy-phen)d)-2-methoxy-acetamide (107 mg) as an off-white foam. MS 421.2 ([M+H]"^) 278.5 (RS) -N-(4-Cyano-ben2yl) -2~(2-fluoro-4-methoxy-3-phenoxy-phen7[)-2-methoxy-acetamide was converted to (RS)-N-(4-carbamimidoyl-benzyi)-2-(2-fluoro-4-methoxy-3-phenoxy-phenyI)-2-methoxy-acetamide hydrochloride according to general procedure D. Colorless soHd. MS 438.3 ([M+H]"") Example 279 279.1 To a solution of (RS)-N-(4-c7ano-benzyl)-2-(2-fluoro-6-hydroxy-phenyi)-2-metiioxy-acetamide {1 g, example 80.4) in dichloromethane (25 ml) were triethylamine (1.02 ml) and DMAP (39 mg). WhUe maintaining temperature at 0'C by cooling with an ice bath, trifluormethane sxilfonic anhydride (0.63 ml) was added slowly. The ice bath was removed after 15 min. Stirring was continued for 5 hrs at r.t. The reaction mixture was diluted with dichloromethane, and washed with water, KHCO3 solution (10%) and again water. The organich layer was dried over MgS04, filtered and concentrated. The crude product was purified by flash chromatography (cydohexane => cyclohexane/EtOAc 1:1) to give (RS)-trifluoro-methanesulfonic add 2-[(4-cyano-benzyicarbamoyl)-methoxy-methyi]-3-fluQro-phenyl ester (1.16 g) as light yeUow soHd. MS 447.2 ([M+H]"") 279.2 A solution of (RS}-trifluoro-methanesulfonic acid 2-[(4-cyano-benz)^carbamoyl)-methoxy-methyi]-3-fluoro-phenyl ester (600 mg) and PPhs (42 mg) in TEA (10 ml) was deoxygenated by passing a stream of argon through the reaction mixture. Ethynyltrimethylsilane (0.28 ml) and palladium(II)acetate (9 mg) were added- The mixture was stirred for 5 hrs at 50°C. After cooling to r.L, the reaction mixture was diluted with water and extracted with EtOAc. The organic layers were combined, dried over MgSO^, filtrated and concentrated. The crude product was purified by flash chromatography (cydohexane => cydohexane/EtOAc 7:3) to give (RS)-N-(4-cyano-ben2yl)-2-(2-fluoro-6-trimethyisilany]ethynyl-phenyl)-2-methoxy-acetainide (278 mg) as ofif-white soUd. MS 395.2 ([M+H]*) 279.3 A solution of (RS)-N-(4-cyano-benz;)d)-2-(2-fluoro-6-trimethylsilan-)dethynyl-phen}d)-2-methoxy-acetamide (214 mg) inEtOH (10 ml) was treated with KzCOs (82 mg). The reaction mixture was stirred over night at r.t, then concentrated. The residue was taken up in water and extracted with EtOAc The organic layers were combined, dried over MgS04 and concentrated to give (RS)-N-(4-cyano-ben2y])-2-(2-fluoro-6-triniethyisilan5dethynyI-phenyl)-2-methoxy-acetaniide (150 rag) as off-white solid. MS 323.2 ([M+H]*) 279.4 (RS)-N-(4-Cyano-ben2)d)-2-(2-fluoro-6-trimethylsilanyIethynyl-phenyl)-2-methoxy-acetamide was converted to (RS)-N-(4-carbaraimido>d-benzyi)-2-(2-ethynyl-6~fluoro-phenyl)-2-methoxy-acetamide hydrochloride according to general procedure D. Light ydlow soUd. MS 340.1 ([M+H]*) Example 280 (RS) -N- (4-carbaminiidoyl-benzyl)-2 - {2-ethynyl-6-fluoro-phenyl) -2-inethoxy-acetamide hydrochloride according was hydrogenated in analogy to example 16.2 to give (RS)-N-(4-carban]imidoyl-benzyl}-2-(2-ethyl-6-fluoro-phenyI)-2-methoxy-acetamide hydrochloride. Off-white solid. MS 344.2 ([M+H]"") Example 281 281.1 A suspension of (RS)-tri£luoro-methanesuIfonic acid 2-[{4-cyano-ben2yicarbamoyl)-methoxy-methyl]-3-fluoro-phenyl ester (520 mg, example 279.1) in DMF (10 ml) was heated to 100°C and treated with TEA (0.49 ml), tetrahydro-2-(2-propyn>doxy)-2H-pyTane (0.33 ml) and Cu(I)I (18 mg). The reaction mixture was degassed by passing a stream of Argon through the reaction mixture. Then bis(triphenylphosphine)paUadium(II)chloride (32 mg) was added. The reaction was heated for 6 hrs at IOO°C. After cooling to r.t., the mixture was concentrated. The residue was taken up in EtOAc and H20. After filtration through a glass microfibre filter, phases were separated. The organic layer was washed with brine, dried over MgS04, filtered and concentrated. The crude product was purified by flash chromatography (cyclohexane => cyclohexane/EtOAc 3:2) to give (RS)-N-(4-c)^no-benzyl)-2-j2-fluoro-6-[3-(tetrahydro-pyran-2-)doxy)-prop-l-ynyi]-phenyi}-2-methoxy-acetamide as off-white solid. MS 454.3 ([M-i-NH4]^) 28U (RS)-N~(4-Cyano-b«i2yl}-2-{2-fluoro-6-[3-(tetrahydro-pyran-2-yJoxy)-prop-l-ynyl]-phenyI}-2-methoxy-acetaniide was converted to (RS)-N-(4-carbamiimdoyl-benz)d)-2-[2-fluoro-6-(3-hydroxy-prop-l-ynyl)-phenyl]-2-methoxy-acetamide hydrochloride according to procedure D. Light yellow soUd. MS 370.2 ([M+H]"*) Example 282 (RS)-N-(4-carbamimidoyl-benzyl)-2-[2-fluoro-6-(3-hydroxy-prop-l-ynyl)-phenyi]-2-methoxy-acetamide hydrochloride was hydrogenated in analogy to example 16.2 to give (RS)-N-(4-carbamimido5d-benz:)d)-2-[2-fluoro-6-(3-hydroxy-propyl)-phenyl]-2-methoxy-acetamide hydrochloride. White solid. MS 374.2 ([M-t-H]"^) Example 283 283.1 Using a similar procedure as described in example 57.1 (RS)-trifluoro-methanesulfonic acid 2- [(4-cyano-benz)dcarbamoyl)-methoxy-methyl] -3-fluoro-phenyl ester (example 279.1) was reacted with phenyl boronic add to give {RS)-N-{4-cyano-benzyl)-2-(3-fluoro-biphenyl-2-yI)-2-methox)'-acetainide. Solid. MS 375.3 ([M+H]"^) 283.2 {RS}-N-(4-Cyano-benzyl)-2-(3-fliioro-biphenyl-2-yl)-2-methoxy-acetaimde was converted to (RS)-N-(4-carbaminiidoyl-benzyl)-2-(3-fluoro-biphenyl-2-yl)-2-methoxy-acetaimde hydrochloride according to general procedure D. OfF-white solid. MS 392.3 ([M+H]"^) Using a similar procedure as described in example 283 (RS)-trifiuoro-methanesuifomc add 2-[(4-cyano-benzylcarbamoyI)-methoxy-methyl]-3-fluoro-phenyl este (example 279.1) was converted to Example 284: (RS)-2-(3'-Aniino-3-fluoro-biphenyi-2-yl)-N-(4-carbamimidoyl-benzyl)-2-methoxy-acetamide hydrochloride. White soHd, MS 407.4 {[M+H]*) Example 285: (RS)-N-(4-Carbaminiido)d-benzyi)-2-(3-fluoro-3'-nitro-biphenyl-2-yl)-2-methoxj'-acetamide hydrochloride. Off-white solid. MS 437.2 {[M+H]"^) Example 286: (RS)-2-[2-(6-Amino-pyridin-2-yl)-6-fluoro-phen)d]-N-(4-carbamimidoyl-ben2yl)-2-methoxy-acetaniide acetate. Off-white solid. MS 408.3 ([M+H]"^) Example 287 287.1 In analogy to example 16.4 {RS)-N-(4-cyano-ben2yl)-2-(2-fiuoro-6-hydroxy-phen5d)-2-methoxy-acetamide (example 80.4) was reacted with ethyl bromoacetate to give (RS)-{2-[(4-cyano-benz)icarbamo}^)-methoxy-methyl]-3-fluoro-phenoxy}-acetic acid methyl ester. YeUowoil. MS 3872 ([M+HD 287.2 (RS)-{2-[(4-Cyano-benzylcarbamoyl)-methoxy-methyl]-3-Suoro-phenoxy}-acetic acid meth)4 ester was converted to (RS)-{2-[(4-carbamin3idoyl-ben27icarbamoyl)-methoxy-methyi]-3-fluoro-phenoxy]-acetic add methyl ester acetate according to general procedure D. White soUd. MS 404.3 ([M+H]*) Example 288 In analogy to example 20.1 (RS)-{2-[{4-carbainimidoji-benz)4carbamoyl}-methoxy-methyI]-3-fIuoro-phenoxy}-acetic acid methyl ester acetate was converted to (RS)-N-(4-Carbamimidoyl-benzyl) -2- (2-fluoro-6-phenoxy-phenyl)-2-methoxy-acetainide hydrochloride. White soHd. MS 390.2 ([M+H]"") Example 289 Using a similar procedure as describe in example 287 (RS)-N-(4-q'ano-benzyi)-2-(2-fluoro-6-hydroxy-phenyl)-2-methoxy-acetamide (example 80.4) was converted to (RS)-N-{4-carbamimidoyl-benzyl)-2-[2-(3-dimethylamino-propoxy)-6-fluoro-phenyi]-2-methoxy-acetamide hydrochloride. White solid. MS 417.2 ([M+H]^) Example 290 Using a similar procedure as describe in example 278.4 and example 278.5 (RS)-N-(4-cyano-ben2yl)-2-(2-fluoro-6-hydroxy-plienyl)-2-methoxy-acetamide (example 80.4} was converted to (4-carbamimidoyl-beiiZ)d}-2-(2-fluoro-6-plienoxy-phen)d)-2-methoxy-acetamide hydrochloiide. White solid. MS 408.2 {{M+H]"^) Example 291 291.1 (RS)-(2,6-Difluoro-4-methoxy-phenyi)-ethoxy-acetic add (example 101.3) was coupled with 4-amino benzonitrile according to general procsduie B to give (RS)-N-(4-cyano-benzyi)-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide. Colorless oil. 291.2 (RS)-N-(4-Cyano-benz)^)-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide was converted to (RS)-N-(4-carbamimidoyl-beiiz;}d)-2-(2,6-difiuoro-4-methoxy-phen)d)-2-ethoxy-acetamide hydrochloride according to general procedure D. White solid. MS 378.3 ([M+H]^) Example 292 292.1 Using analogous procedures as described in 101.1, 101.2 and 101.3 l-benzyloxy-3,5- difluoro-benzene {CAS 176175-97-6) was converted to (RS)-(4-benzyloxy-2,6-difluoro- phenyl)-ethoxy-acetic acid. Light yellow oil. MS 321.1 ([M-H]") 292.2 (RS)-(4-benz3doxy-2,6-difluoro-phen)^)-ethoxy-acetic acid was converted to (RS)-2-(4-benzyloxy-2,6-difluoro-phenyl)-N-(4-cyano-benzyl)-2-ethoxy-acetainide according to general procedure B. Colorless oil. MS 437.2 ([M+H]^) 292.3 (RS)-2-(4-Beiiz}doxy-2,6-difluoro-phen}4)-N-(4-cyano-benzyl)-2-ethoxy-acetaniide was converted to {RS)-2-(4-beii2ylox)'-2,6-difluoro--phenyl)-N-(4-carbaminiidoyi-benzyl}-2-ethoxy-acetamide hydrochloride according to general procedure D. Colorless solid. MS 454.3 {IM+H]+) Example 293 293.1 In analogy to example 16.2 (RS)-(4-benzyloxy-2,6-difluorO'pheiiyi)-ethoxy~acetic acid (example 292.1) was debenzylated to give {RS)-(2,6-difiuoro-4-hydroxy-phenyl)-ethoxy-acetic add. Light yellow solid. MS 255.1 ([M+Na]"") 293.2 According to general procedure B {RS)-(2,6-difluoro-4-hydroxy-phenyl)-ethoxy-acetic acid was reacted with 4-amino benzonitrile to give (RS}-N'-(4-cyano-benzj^)-2-(2,6-difluoro-4-hydroxy-phen}d)-2-ethoxy-acetamide. Colorless solid. MS 345.0 ([M-H]') 293.3 In analogy to example 16.4 (RS)-N-{4-cyano-beiizyl)-2-(2,6-difluoro-4-hydroxy-phenyl)-2-ethoxy-acetamide was reacted with isopropyl iodide to give (RS}-N-(4-cyano-benzyI}-2-(2,6-difluoro-4-isopropoxy-phenyl)-2-ethoxy-acetamide. Colorless oil. MS 387.1 ([M-H]") 293.4 (RS)-N-(4-Cyano-benzyi)-2-(2,6-difluoro-4-isopropoxy-phen)i)-2-ethoxy-acetamide was converted to (RS)-N-(4-carbamimidoy]-benzyl)-2-(2,6-difluoro-4-isopropoxy-phenyi)-2-ethoxy-acetamide hydrochloride according to general procedure D. Colorless foam. MS 406.2 ([M+H]^) Example 294 294.1 In analogy to example 22.1 (RS)-N-(4-cyano-benzyi)-2-(2,6-difluoro-4-hydroxy-phenyl)- 2-ethoxy-acetamide (example 293.2) was reacted with 2-(hydroKymethyl)-pyridine to give (RS)-(4-cyano-benzyl)-2-[2,6-difluoro-4-(pyridin-2-yimethoxy)-phenyl]-2-ethoxy-acetamide. Colorless oil. 294.2 According to general procedure D (RS)-(4-cyano-benzyl)-2-[2,6-difluoro-4-(pyridin-2-)dniethoxy)-phenyl]-2-ethoxy-acetamide was converted to (RS)-N-(4-carbainimidoyl-benzyl)-2-[2,6-difiuoro-4-(pyridin-2-ylmethoxy)-phenyl]-2-ethoxy-acetamide hydrochloride. Colorless solid. MS 455.2 ([M+H]"^) Example 295 In analogy to example 15.5 {RS)-(4-q^o-benzyl)-2-[2,6-difluoro-4-(pyridin-2-yiniethoxy)-phenyI]-2-etlioxy-acetainide {example 294.1) was converted to (RS)-2-[2,6-difluoro-4-(pyridin-2-ylinethoxy)-plienyl]-2-ethoxy-N-[4-(N-faydroxycarbaHiimidoyl)-benzylj-acetamide. Colorless foam.MS471.2 ([M+H]"^) Example 296 In analogy to example 15.4 (RS)-{4-cyano-ben2;)d)-2-[2,6-difluoro-4-(pyridin-2-ylmethoxy)-phenyl]-2-ethoxy-acetamide (example 294.1} was reacted ethyl chlorofonnate to give (RS)-{ammo-[4-({2-[2,6-difluoro-4-(pyridm-2-ylmethoxy)-phenyl]-2-ethoxy-acetylaniino}-methyl)-phenyi]-methylene}-cafbaroic add ethyl ester. Colorless foam. MS 527.2 ([M+H]^) Using analogous procedures as described in example 294.1 and 294.2 (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-4-hydroxy-phen)i)-2-ethoxy-acetamide (example 293.2) was converted to Example 297: (RS)-N-(4-carbamimidoyl-benzyl)-2-[2,6-difluoro-4-(pyridin-3- )dmethoxy)-phenyl]-2-ethoxy-acetamide hydrochloride. Colorless foam. MS 455.2 {[M+H]^) Example 298: (RS)-N-(4-carbamimido)d-benzyl)-2-[2,6-difluoro-4-(pyridin-4- ylmetboxy)-phenyl]-2-ethoxy-acetamide hydrochloride. Light yeDow foam. MS 455.2 ([M+H]") Example 299 299.1 In analogy to example 278.4 (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-4-hydroxy-phenyI)-2-ethoxy-acetamide {example 293.2) was reacted with phenyl boronic acid to give (RS)-N-(4-cyano-ben2yl)-2-C2,6-difluoro-4-phenoxy-phen)d)-2-ethoxy-acetamide. Light yellow soUd. MS 423.1 ([M+H]^* 299.2 (RS)-N-(4-Cyano-ben2yl)-2-(2,6-difluoro-4-phenoxy-phenyl)-2-ethoxy-acetamide was converted to (RS}-N-(4-carbamimidoyl-benz)d)-2-(2,6-difluoro-4-phenoxy-phen)d)-2-ethoxy-acetamide hydrochloride according to general procedure D. White solid. MS 440.2 {[M+H]") Example 300 Using analogous procedures as described in example 22 (RS)-N-(4-cyano-ben2yl)-2-(2,6-difluoro-4-h7droxy-phenyl)-2-ethox)'-acetainide (example 293.2) was converted to RS)-N- (4-carbainiinidoyl-ben27l)-2-[2,6-difluoro-4-(pyridin-3-yloxy-)-phenyl]-2-etlioxy-acetamide hydrochloride. Colorless foam. MS 441.2 ([M+H]"*") Using analogous procedures as described in example 293.3 and 293.4 {RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-3-hydroxy-phenyl)-2-ethoxy-acetamide (example 213) was converted to Example 301: (RS)-N-(4-Carbamimidoyl-benzyI)-2-(2,6-difluoro-3-isopropoxy-phenyl)-2-ethoxy-acetaniide hydrochloride. Colorless foam. MS 406.3 ([M+H]"*") Example 302: (RS)-N-(4-Carbamimidoyl-benzyl)-2-(3-carbamoylmethoxy-2,6-difluoro-phenyl)-2-ethoxy-acetamide hydrochloride. Colorless foam. MS 421.1 ([M+H]"*") Using analogous procedures as described in example 294 (RS)-N-(4-cyano-ben2yl)-2-(2,6-diSuoro-3-hydroxy-phenyl)-2-ethoxy-acetamide (example 213) was converted to Example 303; (RS)-2-[3-(2-Benzyioxy-ethoxy)-2,6-difluoro-phen^]-N-{4-carbamimidoyl-benzyl)-2-ethoxy-acetamide hydrochloride. Colorless foam. MS 498.3 ([M+H]^) Example 304 was isolated as a side product in the preparation of example 26. (RS)-N-(4-carbamiinidoyl-benzyl)-2-[2,6-difluoro-3-(2-hydroxy-ethoxy)-phenyl]-2-ethoxy-acetamide hydrochloride. Colorless foam. MS 408.3 ([M+H]"^) Example 305 Using analogous procedm-es to example 299 (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-3-hydroxy-phenyl)-2-ethoxy-acetamide (example 213) was converted to (RS)-N-(4-carbamimidojd-benzyl)-2-(2,6-difluoro-3-phenoxy-phenyI)-2-ethoxy-acetamide acetate. SoUd. MS 408.3 ([M+H]') Example 306 Using analogous procedures to example 283 (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-3-hydroxy-phenjd)-2-ethoxy-acetamide (example 213) was converted to (RS)-N-(4-carbamimidoyI-benzyI)-2-(2,4-difluoro-biphenyl-3-yI)-2-ethoxy-acetamide hydrochloride. Colorless soUd. MS 424.2 ([M+H]*) Example 307 307.1 A stirred solution of 2,4-difiuorbenzoic add (20.8 g) and N-ethyldiisopropylamine (26.8 ml) in dioxane (80 ml) was treated with diphenyi phosphory- azide (37.9 ml; very exothermicl) and tert-butanoJ (80 ml) at r.t. and under an argon atmosphere. The mixture was then heated to 90°C and stirring was continued for 16 h. The mixture (brown solution) was cooled to r.t., diluted with EtOAc, washed with water and brine, dried over MgSO^ and treated at the same time with decolorizing charcoal, and finally filtered over a celite pad. The yellow filtrate was concentrated to leave the crude product as an orange oil. The crude product was purified by flash chromatography (cydohexane/EtOAc 85:15). The product-containing fi-actions were combined and concentrated. The residue (yellow oil containing white soUd) was taken up in 50 ml heptane. The solid (symmetric urea which was formed as by-product during the Curtius reaction) was filtered off. The filtrate was concentrated. The residue was destilled in a Kugehohr oven (0.73 mbar, 120'C) to give (2,4-difluoro-phenyl)-carbainic acid tert-butyl ester {24.9 g) as Hght yellow oil. 307.2 To a stirred, cooled (-78°C) solution of (2,4-difluoro-phenyl)-carbamic add tert-butji ester (5 g) in THF (50 ml) under an argon atmosphere was added dropvidse a 1.6 M solution of BuLi in hexanes (28.6 ml) for 20 min (temperature below -68°C during the addition). When addition was complete, the mixture (turning to orange, then to light red) was stirred at -78°C for 1 h 30. DMF (7.55 ml) was then added for 10 min (temperature below -70°C) and stirring at -78°C was continued for 15 min. As the mixture had turned to a compact mas (no more stirring), it was allowed to warm to room temperature. Water (50 ml) was added and the pH was set to 3 by the dropwise addition of 3 N HCl. EtOAc (50 ml) was added. The organic phase was washed with water and brine dried over MgS04, filtered and concentrated. The crude product was purified by flash chromatography (cyclohesane => cydohexane/EtOAc 85:15) to give (2,4-difluoro-3-formyl-phenyl)-carbamic add tert-butyl ester (1.75 g) as an off-white solid. 307.3 According to general procedure A (2,4-difluoro-3-formyi-phen)d)-carbamic add tert-butyl ester was converted to (RS)-(3-tert-butoxycarbonylamino-2,6-difluoro-phenyl)-methoxy-acetic acid. Orange gum. MS 316.1 ([M-H]-) 307.4 According to general procedure C (RS)-(3-tert-butoxycarbonylamino-2,6-difluoro-phenyl)-methoxy-acetic add was reacted with 4-amino benzonitrile to give (RS)-{3-[(4- cyano-benzylcarbamo)'l)-inethoxy-methyl]-2,4-difIuoro-phenyl}-carbainic acid tert-but)d ester. Solid. MS 430.3 {[M-H]0 307.5 To a stirred solution of (RS)-l3-[(4-cyano-benzyicarbamoyl)-inethosy-methyl]-2,4-difluoro-phenyll-carbamic add tert-butyi ester (514 mg) at r.L in dioxane {10 ml) under an argon atmosphere was added 4 M HCI solution in dioxane {6 ml). Stirring at r.t. was then continued for 3 h. The light yellow solution was concentrated. The solid residue was suspended in EtOAc and washed with 1 N NaOH. The organic layer was dried over MgS04, filtered and concentrated. The crude product was purified by flash chromatography (cyclohexane -> cyclohexane/EtOAc 2:3) to give (RS)-2-(3-amino-2,6-difluoro-phenyl)-N-(4-cyano-benzyl)-2-methoxy-acetamide (215 mg) as an off-white sohd MS 332.3 ([M+H]^) 307.6 To a stirred solution of (RS)-2-(3-amino-2,6-difiuoro-phen}d)-N-{4-cyano-benzyl)-2- methoxy-acetamide (130 mg) at r.t. in dichloromethane were added sucessively dry 4A molecular sieves (50 mg), phenyl boronic acid (96 mg), triethylamine (0.11 ml), copper (U) acetate (71 mg) and TEMPO (67 mg). A "CaCl2 trap" was placed over the flask and stirring at r.t. was continued over the week-end. Then the soUds were filtered off and washed with EtOAc. The dark brown filtrate was concentrated to leave a dark brown residue. The crude product was purified by flash chromatography (cyclohexane => cyclohexane/EtOAc 3:2) to give (RS)-N-(4-cyano-benzyI)-2-(2,6-difluoro-3-phenylainino-phenyl)-2-methoxy- acetamide (123 mg) as Ught grey gum. MS 408.3 ([M+H]"^) 307.7 In analogy to example 15.5 (RS)-N-(4-cyano-benzyi)-2-(2,6-difluoro-3-phen^^amino-phenyI)-2-methoxy-acetaraide was converted to (RS)-2-(2,6-difluoro-3-phenylamino-phen)d)-N-[4-(N-hydroxycarbamimidoyl)-benz)d]-2-methoxy-acetamide. Off-white soHd. MS 441.6 ([M+H]"") 307.8 To a stirred solution of (RS)-2-(2,6-dfluoro-3-phenylarmno-phenyl)-N-[4-(N-hydroxycarbaminudoyl)-benzyl]-2-methoxy-acetamide (106 mg) at r.t. in ethanol (5 ml) under an argon atmosphere were added 5 drops of acetic acid and and a catalytic amount of Raney-Nickel. The mixture was then stirred at r.t. under a hydrogen atmosphere for 23 h. The catalyst was filtered off and the filtrate was concentrated. The crude product was purified using flash chromatography (EtOAc/acetone/HjO/HOAc 6:2:1:1) to give (RS)-N- (4--carbamimidoyl-benzyl) -2- (2,6-difIuoro-3-phenyl2inino-pheny]) -2-methoxy-acetarnide acetate (92 mg) as on off-white solid. MS 425.5 ([M+H]"") Example 308 30S.1 To a stirred solution of (RS}-2-(3-amino-2,6-difluoro-phenyl)-N-(4-cyano-benzyl)-2-methoxy-acetamide (example 307.5) 81 mg) at r.t in THF (5 ml) under an argon atmosphere were added N-eth)ddiisopropylamine (0.017 ml) and 2-iodopropane (0.01ml). The mixture was heated to reflux and stirring was continued for 17 h. More 2-iodopropane (0.1 ml) and N-ethyldiisopropylamine (0.17 ml) were added and stirring at reflux was continued for 7 h. DMF (5 ml) was added and the mixture was stirred at HO^C for 21 h. The mixture had turned to light brown. More DMF (5 ml), N-ethyldiisopropjdamine (0.35 ml,) and 2-iodQpropane (0.2 ml) were added and stirring at 90°C was continued for 17 h. The mixture was cooled to r.t., diluted with 20 ml water and extracted widi EtOAc. The combined organics were washed with water and brine , dried (MgS04), filtered and concentrated. The crude product was purified by column chromatography (cyclohexane => cyclohexane/EtOAc 1:1) to give H-(4-cyano-benzyl)-2- (2,6-difluoro-3-isopropyianiJno-phenyi)-2-methoxy-acetamide (28 mg) as light brown gum. 30S.2 In analogy to example 307.7 and 307.8 H-(4-cj^no-benzyi)-2-(2,6-difluoro-3- isopropyiainino-phenyl)-2-methoxy-acetamide was converted to (RS)-N-(4- carbamimido)d-ben2yl)-2-(2,6-difluoro-3-isopropylamino-phen)d)-2-methoxy-acetamide acetate. Light green crystals. MS 391.3 ([M+H]"^) Example 309 309.1 In analogy to example 87.2 (RS)-2-(3-amino-2,6-difluoro-phenyl)-N-(4-cyano-benzyi)-2- methoxy-acetamide (example 30.5) was reacted with acetyl chloride to give (RS)-2-(3- acet7lam!no-2,6-difiuoro-phenyl)-N-(4-cyano-ben2yl)-2-methoxy-acetamideas white foam. 309.2 Using general procedure D (RS)-2-(3-acetylamino-2,6-difluoro-phenyl)-N-(4-cyano-benzyl)-2-methoxy-acetamidewas converted to (RS)-2-(3-acetylamino-2,6-difluoro-phenyl)-N-(4-carbamimidoyI-ben2yl)-2-methoxy-acetamide hydrochloride. OS-white solid. MS 391.3 ([M+H]^) Example 310 In analogy to example 309 (RS)-2-(3-ammo-2,6-di£!ucro-piienyl)-N-(4-c)'ano-faenzyl)-2-methoxy-acetamide (example 30.5) was converted to (RS)-(4-carbamimidoyl-benzyl)-2-{2,6-difluoro-3-plien)dacetylamino-phenyi)-2-methoxy-acetaimde hydrochloride. Off-i white sohd. MS 467.4 {[M+H] ^) Example 311 311.1 A stirred solution of 2,4-difluorobenzaldehyde (15.4 ml) in toluene (200 ml) was treated with eth}iene ^ycol (23.2 ml) and p-toluene sulfonic add (0.53 g). The ruction mixture was heated to reflux during 5 hrs (Dean-Stark trap), then it was cooled to r.t and poured onto ice. The organic layer was separated off, washed with 10% KHCOs-solution and brine, dried over MgS04, filtered and concentrated to give 2-(2,4-difluoro-phenyl)-[l,3]dioxolane (26.8 g) as a light yellow oU. MS 186.1 ([M]"") 311.2 In analogy to procedures 101.1, 101.2 and 101.3 2-(2,4-difluoro-phenyl)-[l,3]dioxolane was converted to (RS)-(3-[l,3]dioxolan-2-yi-2,6-difluoro-phen)d)-ethoxy-acetic add. During the addic work-up after the final ester hydrolysis, the acetal protecting group was pardy lost It was completdy deaved off by treating the mixture of protected and unprotected compoimd with 3N aqueous HCI/THF/H2O 1:10:1 overnight at r.t.. Upon complete deprotection, the THE was distilled off and the product was isolated by extraction with EtOAc No further purification. (RS)-(2,6-Difluoro-3-form)d-phenyl)-ethoxy-acetic add. Ydlow oil. MS 262.0 ([M+NH*]') 311.3 According to general procedure B (RS)-(2,6-difluoro-3-formyl-phenyl)-ethoxy-acetic add was reacted with 4-aminomethyl benzonitrile to give (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-3-formyl-phenyl)-2-ethoxy-acetamide. Amorphous ofif-white solid. MS 359.2 ([M+H]-^) 311.4 A suspension of (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-3-formyI-phenyl)-2-ethoxy-acetamide (300 mg) in EtOH (1 ml) was treated with NaBH4 (66 mg) at 0°. The reaction mixture was stirred for 4 hrs at r.L, then poured onto ice and extracted with EtOAc. The organic layers were combined, dried over MgS04, filtrated and concentrated. The cmde product was isolated by flash chromatography (CH2CHI2 => CH2Cl2/MeOH 4:1) to give {RS)-N-{4-c7^o-berizyl)-2-(2,6-difluoro-3-hydroxymethyl-phenyl)-2-ethoxy--acetamide (174 mg) as amourphous white solid. MS 361.3 ([M+H]"^) 311.5 (RS)-N-{4-Cyano-benz)'l)-2-{2,6-difiuoro-3-hydroxyinethyl-phenyl)-2-ethoxy-acetainide was converted according to general procedure D to give (RS)-N-(4-carbamiinidoyl-benzyI)-2-(2,6-difluoro-3-hydroxymethyi-phenyl)-2-ethoxy-acetamide hydrochloride as amorphous white soiid. MS 378.3 ([M+H]^) Example 312 312.1 In analogy to example 106.2 (RS)-N-(4-cyano-benz)d)-2-(2,6-difluoro-3-form>i-phenyl)-2-ethoxy-acetamide (example 311.3) was converted to (RS)-N-(4-cyano-benzyl)-2-[2,6-difluoro-3-(hydroxyiinino-methjd)-phen)d] -2-ethoxy-acetamide. Off-white amorphous soUd. MS 374.3 ([M+H]*) 312.2 In analogy to example 106.3 (RS)-N-(4-cyano-benz)d)-2-[2,6-difiuoro-3-(hydroxyimino- meth5d)-pben)d]-2-ethoxy-acetainide was converted to (RS)-2-(3-aminomethyl-2,6- difluoro-phenyl)-N-(4-cyano-benzyI)-2-ethoxy-acetamide acetic acid. Yellow oil. MS 360.3 ([M+H]") 312.3 In analogy to example 87.2 (RS)-2-(3-aminomethyl-2,6-difiuoro-phen)i)-N-(4-cyano- benzyl)-2-ethoKy-acetamide acetic acid was reacted with acetyl chloride to give (RS)-2-[3- (acet)^amino-methyl)-2,6-difluoro-phenyI]-N-(4-cyano-benzyi)-2-ethoK7-acetamide. White foam. MS 402.5 ([M+H]"") 312.4 According to general procedure D (RS)-2-[3-{acetylamino-methyI)-2,6-difluoro-phenyl]- N-(4-cyano-benzyl)-2-ethoxy-acetamide was converted to (RS)-2-[3-(acet)^amino- methyl)-2,6-difluoro-phenyl]-N-(4-carbamimidoyl-benzyi)-2-ethoxy-acetamide hydrochloride. White soHd. MS 419.2 ([M+H]"*") Example 313 313.1 In analogy to example 15.5 (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-3-formyI-phenyI)-2-ethoxy-acetamide (example 311.3) was converted to (RS)-2-[2,6-difluoro-3- (hydroxyiinino-meth)d)-phenyl]-2-ethoxy-N-[4-(N-hydroxycarbaimmidoyl)-beiizyl]-acetamide. Amorphous off-white solid. MS 407.2 ([M+H]"^' 313.2 In analogy to example 307.8 (RS)-2-[2,6-difluoro-3-(hydroxyiinino-methyI)-phenyl]-2- ethoxy-N-[4-CN-hydroxycarfaamimidoyI)-ben2yl]-acetamide was hydrogenated to give (RS)-2-{3-aminometh'^-2,6-difluoTO-phenyl)-N-(4-caTbanuinidoyl-benzyi)-2-eiiioxy- acetamide acetic acid 1:4. White soUd. MS 377.3 ([M+H]"^) E3tample 314 314.1 To a solution of (RS)-N-(4-cyano-ben2yi)-2-(2,6-difluoro-3-formyl-phenyl)-2-ethoxy-acetamide (250 mg, example 311.3) in EtOH (5 ml) was added aniline (64 mg). The suspension was stirred over night, then cooled to 0°C and treated with NaBH4 (38 mg). The reaction mixture was stirred 1 fa at 0° and 1 h at r.L, then poured onto ice and extracted with EtOAc. The organic layer was dried over MgS04, filtrated and concentrated. The crude product was purified by flash chromatography (cyclohexane/EtOAc 1:4 => BtOAc) togive(RS)-N-(4-cyano-benz)d)-2-(2,6-difiuoro-3-phenyIaminomethyl-phenyl)-2-ethoxy-acetamide (230 mg) as off-white amourphous solid. MS 436.3 ([M+H]^) 314.2 According to general procedure D (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-3-' phenyiaminomethyi-phen)d)-2-ethoxy-acetaraide was converted to (RS)-(4-carbamiraidoyl-benzyl)-2-(2,6-difluoro-3-phen)daminomethyi-phen)i)-2-ethoxy-acetamide hydrochloride. Amorphous white sohd. MS 453.5 ([M+H]"*") Using analogous procedures as described in example 37 (RS)-N-(4-cyano-benzyi)-2-(2,6-difluoro-3-formyl-phen)i)-2-ethoxj'-acetamide (example 311.3) was converted to Example 315; (RS)-(4-Carbamimidoyi-benzyl)-2-(2,6-difluoro-3-morpholin-4-ylmeth)^-phenyl)-2-ethoxy-acetamide hydrochloride. White solid. MS 447.2 ([M+H] '^) Example 316: (RS)-(4-Carbamimidoyi-benz)d)-2-(2,6-difluoro-3-piperidin-l-ylmethyl-phenyi)-2-ethoxy-acetaniide hydrochloride. Amorphous off-white sohd. MS 445.2 ([M+H]^) Example 317 In analogy to example 307.8 (RS)-2-(3-diethoxymethyi-2,6-difluoro-phenyl)-2-ethoxy-N-[4-(N-hydroxycarbamimidoyl)-beii2yl]-acetamide (obtained side product in the synthesis of example 312.1) was converted to (RS)-(4-carbamimidoyl-benzyl)-2-(2,6-difIuoro-3-formyI-phenyl)-2-ethoxy-acetamide acetic add (1:4). White solid. MS 376.3 ([M+H]"^) Example 318 318.1 In analogy to procedures 106.2 and 106.3 3,5-difluoro-4-formyl-benzonitrile (CAS 467442-15-5) was converted to 4-aniinomethyi-3,5-difluoro-benzomtrile hydrochloride. Off-white soUd. MS 169.2 ([M+H]"") 318.2 According to general procedure C 4-aminomethyl-3,5-difluoro-benzonitrile hydrochloride was reacted with {RS)-(2,6-difluoro-4-methoxy-phenyI)-ethoxy-acetic acid (example 101.3) give to (RS)-N-(4-cyano-2,6-difIuoro-benzyl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetaniide. Off-white soUd. MS 397.1 ([M-i-H]^) 318.3 According to general procedure D (RS)-N-(4-cyano-2,6-difluoro-benzyl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide was converted to (RS)-N-(4-carbamiimdoyl-2,6-difiuoro-benzyl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide hydrochloride. White solid. MS 414.2 ([M+H]^) Using similar procedures &s described in example 318 4-aminomethyl-3,5-difluoro-benzonitrile hydrochloride (example 318.1) was coupled with the appropriate adds and converted to the following arnidine products: Example 319: (RS)-N-(4-Carbamimidoyl-2,6-difluoro-benzyi)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyi)-acetamide acetate (coupling with add (RS)-ethoxy-(2-fluoro-4-methoxy-phenyO-acetic add, example 63.1). Off-white powder. MS 396.1 ([M+H] ) Example 320; (RS)-N-(4-Carbaniimido5d-2,6-difiuoro-ben2yI)-2-(2,6-di£luoro-4- methoxy-phenyI)-2-methoxy-acetamid acetate (coupling with add (RS)-(2,6-difluoro-4-methoxy-phenyl)-methoxy-acetic add, example 66.1). Off-white soUd. MS 400.5 ([M+HD Example 321: (RS)-N-(4-Carbamimidoyl-2,6-difluoro-benz)d)-2-(2-fluoro-4-methoxy-phenyl)-2-methoxy-acetamide acetate (coupling with acid (RS)-(2-fluoro-4-methoxy-phenyD-methoxy-acetic acid, example 15.1). Off-white solid. MS 382.3 ([M-l-H]"^) nxampie m 322.1 To a mechanically stirred solution of 4-bromomethyl-3-nitro-benzomtrile (21.7 g, CAS 223 512-70-7) in chlorofonn (250 ml) under argon atmosphere was added hexamethylenetetramine (7.1 g). A white precipitate appeared a few minutes after the addition. After 3 hrs heating to reflux (oil bath SO^C) he mixture was cooled to r.L. The solid was collected by filtration, washed with chloroform and dried under high vacuum) to give l-(4-cyano-2-nitro-benzyl)-3,5,7-triaza-l-azoma-tricyclodecane hydrobromide (13.8 g). Off-white powder. MS 322.2 To a mechanically stirred suspension of l-(4-cyano-2-mtro-beiizyl)-3,5,7-triaza-l-azonia-tricyclodecane hydrobromide (13.8 g) in ethanol (150 ml) mider argon atmosphere, was added concentrated aqueous HCl (20 ml). After 6 hours stirring at reflux the mixture was concentrated, diluted with NaOH IN until pH>12. The product was extracted with EtOAc. The combined organic phases were washed twice with water and with brine. Then the solution was dried over MgS04), filtered and concentrated to give 4-aminometh)i-3-mtro-benzonitrile (5.8 g) as yellow soUd. MS 322.3 Accordk^ to general procedure B 4-aminomethyl-3-nitro-benzonitrile was reacted with (RS)-ethoxy-(2-fluoro-4-methoxy-phenyi}-acetic acid (example 63.1) to give (RS}-(4-cyano-2-nitro-benzyl)-2-ethoxy-2-(2-fIuoro-4-methoxy-phenyl)-acetamide. Yellow foam. MS 388.1 ([M-hH]^) 322.4 To a stirred solution of (RS)-(4-cyano-2-nitro-benzyl)-2-ethoxy-2-(2-fluoro-4-metfaoxy-phenyl)-acetamide in THF (5 ml) and ethanol (15 ml) was added palladium/C (250 mg). After 24 hrs stirring at r.L under hydrogen atmosphere the mixture was filtered, and the filtrate was concentrated to leave a light yellow foam. The crude product was purified by flash chromatography (cyclohexane => cyclohexane/EtOAc 1:1) to give (RS)-(2-amino-4-cyano-benzjd)~2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide (4.45 g) as light yellow foam. MS 358.7 ([M-hH]*) 322.5 To a stirred solution of (RS)-(2-ainino-4-cyano-benzyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide (470 mg) in DMF (8 ml) were added iodoacetamide (376 mg) and N-ethyldiisoprop>damine (0.34 ml). After 50 hrs stirring at 110°C under argon atmosphere. The mixture was diluted with EtOAc and water. The organic phase was separated and washed with water and brine, dried ovef MgS04, filtered and concentrated. The crude product was purified by flash chromatography CCH2a2 => CHjClj/MeOH 4:1) to give (RS)-[2-(carbamoylmeth]i-ainino)-4-cyano-benzyl]-2-ethoxy-2-(2-fluoro-4-rnethoxy-phenyl)-acetamide (133 mg) as an off-white soUd. MS 415.1{[M+H]'*') 322.6 According to general procedure D CRS)-[2-(carbamoylniethyl-ainino}-4-cyano-beii2yI]-2-ethoxy-2-(2-fluoro-4-methoxy-phenyI)-acetamide was converted to (RS)-[4-carbamimidoyi-2-{carbamoylmethyi-amino)-benzyl]-2-ethoxy-2-(2-fluoro-4-methoxy-phenyi)-acetamide hydrochloride. Off-white soHd. MS 432 ([M+HD Using similar procedures as described in example 322.4 and 322.6 (RS)-(2-amino-4-cyano- benzyl)-2-ethoxy-2-(2-fl.uoro-4-methoxy-phenyl)-acetamide (ecample 322.4) was converted to Example 323: (RS)-N-(2-Benzylamino-4-carbamimidoyl-benzyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phen}d)-acetamide acetate. Off-white soUd. MS 465 ([M+H]"^) Example 324: (RS)-[4-Carbaminiidoyl-2-(2-fluoro-benzylamino)-benz)d]-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide hydrochloride. Off-white soUd. MS 483.3 ([M+H]"^) Example 325; (RS)-{4-CarbamimidoyI-2-[(pyridin-2-yImethyl)-aniino]-ben2yi}-2-ethoxy-2-(2-fluoro-4-methoxy-phenyi)-acetamide hydrochloride. Off-white sohd. MS 466.4 ([M+H]-^) ■ Example 326: (RS)-[4-Carbamimidoyl-2-(4-chloro-2-fluoro-benz)danuno)-benzj4]-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide hydrochloride. Off-white solid. MS 517.3 ([M+H]') Example 327: (RS)-(4-Carbamunidoyl-2-phenethyianiino-benzj4}-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamidehydrochloride. Off-white foam. MS 479.5 {[M-i-H]"^) Example 328: (RS)-(5-Carbamimidoyl-2-{[2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acet)damino]-raeth)d}-phenylamino)-acetic add ethyl ester hydrochloride. Off-white solid. MS461.1([M+H]-') Example 329 In analogy to example 20.1 (RS)-(5-carbamimidoyl-2-{[2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acer}'lamino]-methylt-phenylainino)-acetic add ethyl ester hydrochloride (example 328) was hydrolysedto give (RS)-(5-carbamimidoyl-2-{[2-ethoKy-2-(2-fluoro-4- methoxy--phenyl)-acetyiamino]-methyl}-phenyiarnino)-acetic acid acetate. Off-white solid. MS 433.4 {[M+H]^} Example 330 330.1 ; In analogy to example 95.4 (RS)-C2-amino-4-cyano-ben2)d)-2-ethoxy-2-{2-£luoro-4- methoxy-phenyl)-acetamide {example 322.4) was reacted with benzyl sulfonylchloride to give (RS)-(4-cyano-2-phenylmethanesulfonylamino-ben2yl)-2-ethoxy-2-(2-fiuoro-4- methoxy-phenyl)-acetainide. Off-white foam. MS 512.3 ([M+H]"^) 330.2 According to general procedure D (RS)-{4-cyano-2-phenylmethanesulfon}damino-benzyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetaniide was converted to (RS)-{4-carbamimidoyl-2-phenylmetfaanesuIfonylamino-ben2yl)-2-ethoxy-2-{2-fluoro-4-methoxy-phenyl)-acetamide hydrochloride. Off-white soUd. MS 529.2 ([M+H]** Example 331 Using similar procedures as described in example 330 (RS)-(2-amino-4-cyano-benzyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetainide (example 322.4) was reacted with benzylisocyanate and subsequently converted into the corresponding amidine to give (RS)-[2-C3-benzyl-ureido)-4-carbamimidoyl-ben2yl]-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide acetate as a white solid. MS 508.4 ([M+H]"^) Example 332 Using similar procedures as described in example 53 (RS)-(2-amino-4-cyano-ben2yl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyi)-acetamide {example 322.4) was reacted with benzyl chloroformate and subsequently converted into the corresponding amidine to give (RS)-{5-carbamimidoyl-2-{[2-ethoxy-2-{2-fluoro-4-methoxy-phenyl)-acetj4amino]-methyll-phenyl)-carbamic acid benzyl ester hydrochloride. White solid. MS 509.4 ([M+H]^) Example 333 333.1 In analogy to example 30.6 {RS)-{2-amino-4-cyano-benzyl)-2-ethoxy-2-(2-fluoro-4- methoxy-phenyl)-acetaraide (example 322.4) was reacted with phenyl boronic acid to give (RS)-(4-cyano-2-phenylamino-benzyl)-2-ethoxy-2-(2-fluoro-4-inethoxy-phen^)- acetamide. Off-white foam. MS 434.1 ([M+H]"^* 333.2 According to general procedure D (RS)-(4-cyano-2-phenylamino-benzyi)-2-ethoxy-2-(2-fiuoro-4-methoxy-phenyl)-acetamide was converted to (RS)-(4-carbaniiinidoyl-2-phenylamino-benz}'l)-2-ethoxy-2-{2-fluoro-4-metlioxy-phenyl)-acetamide hydrochloride, i light green soUd. MS 451.1 ([M+H]"*") Example 334 334.1 A solution of (RS)-(2,6-difluoro-4-trifluoromethanesulfQnylory-phen^)-ethoxy-acetic add ethyl ester {3.5 g, example 162) in dioxane (115 ml) was treated with bis(pinacolato)diboron (3.43 g) and K2CO3 (2.65 g). The solution vfas deoxj^enated by passing a stream of argon through it Then bis(triphenylphosphine)paIladiuni(II) chloride (0.62 g) was added. The reaction mixuter was heated to 100° for 16 hrs, then cooled to r.t and filtrated. The solids were washed with diosane/EtOAc. The filtrate was concentrated. The crude product was isolated by flash chromatography (cyclohexane/EtOAc 1:1 => EtOAc) to give (RS)-[2,6-difluoro-4-(4,4,5,5-tetramethyl-[l,3,2]dioxaborolan-2-yl)-phenyI]-ethoxy-acetic acid ethyl ester (3.51 g) as yellow oil. MS 388.0 ([M+NH4]'^) 334.2 A solution of (RS)-[2,6-difluoro-4-(4,4,5,5-tetramethyl-[13,2]dioxaborolan-2-yl)-phenyl]-ethoxy-acetic acid ethyl ester in li2-dimetiioxyethane was treated with 2-amino-5-bromopyridine and CsF. The reaction mixture was deoxygenated by passing a stream of argon throi^ it Tetrakis(triphenylphosphine)palladium(0) was added. The reaction mixture was heated to 80° for 2 days, then cooled to r.t and concentrated. The crude product was isolated by flash chromatography (cyclohexane/EtOAc 2:1 => EtOAc) to give (RS)-[4-(6-amino-pyridin-3-yl)-2,6-difluoro-phenyl]-ethosy-acetic acid ethyl ester as amorphous brown solid. This material which was contaminated with triphenyl phosphinoxid was dissolved in THF and treated with 4.5 ml IN NaOH and stirred for 18 hrs at r.t.. The solution was neutralized with IN HCl, then concentrated. The residue was taken up in Et20. The solid was filtered off and washed with ether to give (RS)-[4-(6-amino-pyridin-3-)d)-2,6-difluoro-phenylj-ethoxy-acetic acid (1.36 g, contains 2 equivalent of NaCl). According to general method B this material (350 mg) which was contaminated with triphenyl phosphinoxid was reacted with 2-(2-aniinometh)4-5-cyano-phenoxy)-acetaraide hydrochloride (example 123.2) to give (RS}-2-[4-(6-amino-pyridin-3-yl)-2,6-difluoro-phen)d]-N-(2-carbamoylmethoxy-4-cyano-benzyl)-2-ethoxy-acetamide (186 mg) as off-vfinte soUd. MS 496.3 ([M+H]"") 334.3 According to general procedure D (RS)-2-[4-(6-amino-pyridin-3-yl)-2,6-difluoro-pfaenyl]-N-(2-carbamoylmethoxy-4-cyano-benzyl)-2-ethoxy-acetainide was converted to (RS)-2-[4-{ 6-ainmo-pyridin-3-yI)-2,6-difluoro-phenyl]-N-(4-carbamimidoyl-2-carbamoyl^lethosy-benzyl)-2-ethoxy-acetamide hydrochloride acetic add (1:1:2). Off-white soUd. MS 513.3 ([M+H]"^) Example 335 335.1 In analogy to example 22.1 (RS)-{2,6-difluoro-4-hydroxy-phenyl)-etboxy-acetic acid ethyl ester (example L6) was reacted with 2-(hydroxymethyl)pyridine to give (RS)-[2,6-difluoro-4-(pyTidin-2-ylmethoxy)-phenyl]-ethoxy-acetic acid ethyl ester as a yellow semisolid. This material was hydrolysed in analogy to example 101.3 to give (RS)-[2,6-difluoro-4-(pyridin-2-yhnethoxy)-phenyl]-ethoxy-acetic acid. White soUd. MS 324.1 ([M+H]*) 335.2 According to general procedure C (RS)-[2,6-difluoro-4-(pyridin-2-ylmethoxy)-phenyl]-ethoxy-acetic acid was reacted with 2-(2-aminomethyi-5-cyano-phenoxy)-acetamide hydrochloride (example 123.2) to give (RS)-(2-carbamo)imethoxy-4-cyano-benzyl)-2- [2,6-difluoro-4-(pyridin-2-}dmethoxy}-phenyl]-2-ethoxy-acetamide. Amorpbous off-white soUd. MS 511.3 ([M+H]^) 335.3 According to general procedure D (RS)-(2-carbamo)dmethoxy-4-cyano-benzyl)-2-[2,6- difluoro-4-(pyridin-2-ylmethoxy)-phen)d]-2-ethoxy-acetamide was converted to (RS)-(4- carbamiimdo)4-2-carbamoylmethoxy-ben2yl)-2-[2,6-diSuoro-4-(pyridin-2-3dmethoxy}- phenyl]-2-ethoxy-acetamide hydrochloride. Off-white solid. MS 528.2 ([M+H]"^) Example 336 336.1 According to general procedure C (RS)-[4-(6-amino-pyridin-3-yl)-2,6-difluoro-phenyl]-ethoxy-acetic add (intermediate from example 334.4, contains 2 eqmvalent of NaCl) was reacted with 4-aminomethyl-3,5-difiuoro-ben2omtrile hydrochloride (example 318.1) to give (E.S)-2-[4-(6-aniino-pyridin-3-)d)-2,6-difluoio-phenyl]-N-(4-cyano-2,6-difluoro-benzyl)-2-ethoxy-acetamide as off-white solid. MS 459.6 ([M+H]"^) 336.2 In analogy to example 307.7 and 307.8 (RS)-2-[4-(6-amino-pyridin-3-yl)-2,6-difluoro- phenyl]-N-(4-cyano-2,6-di£luoro-benzyl)-2-ethoxy-acetarmde was converted to (RS)-2-[4-(6-aiiiino-pyTidin-3-yi)-2,6-difluoro-phenyi]-N-{4-carbainiiiiidoyl-2,6-difluoro-ben2yI)-2-ethoxy-acetaniide acetate. White powder. MS 476.5 ([M+H]"^) Example 337 337.1 A suspension of (RS)-N-(4-carbamimido)^-benzyl)-2-(2,6-difluoro-4-inethoxy-phenyl}-2-methoxy-acetamide hydrochloride (600 mg, example 66.3) in CH2CI2 (15 ml), H2O (7.5 ml) and saturated NajCOs-solution (7.5 ml) was treated with B0C2O (333 mg) and stirred for 6 hrs at r.t. The mixture was poured onto ice and extracted with CH2CI2. The organic layers were dried over MgSOi, filtrated and concentrated. The crude product was purified by flash chromatography (cyclohexane/EtOAc 4:1 => EtOAc) to give (RS)-[(4-{[2-(2,6-difluoro-4-methoxy-phenyl)-2-methoxy-acetylamino]-metfayI}-phenyl)-imino-methyl]-carbamic acid tert-butyl ester (630 mg). Amorphous off-white soUd. 337.2 The racemic (I^)-[(4-l[2-(2,6-difiuorQ-4-meJiioxy-phenyl)-2-methoxy-acetylamino]-methyl}-phenyl)-iinino-methyi]-carbamic acid tert-butyl ester (620 mg) was separated by HPLC on ChiralPak AD (15% EtOH in heptane) to give (S)-[(4-{[2-(2,6-difluoro-4-methoxy-phenyI)-2-methoxy-acetylamino]-methyl}-phenyl)-inmio-methyl]-carbamic add tert-butyl ester (193 mg) as a white foam and (R)-[(4-{[2-(2,6-difluoro-4-methoxy-phenyl)-2-methoxy-acetyianiino]-meth)d}-phenyI)-imino-methyl]-carbamic acid tert-butyl ester (223 mg) as a white foam. 337.3 A suspension of (S)-[(4-{[2-(2,6-difluoro-4-methoxy-ph.enyl)-2-methoxy-acetylaimno]- methyi}-phenyl)-iniino-meth>i]-carbamic add tert-butyl ester in water was treated with formic add. The solution was stirred for 8 hrs at r.t, then concentrated, redissolved twice in water, concentrated and dried to give (S)-N-(4-carbaniiinidoyl-benzyl)-2-(2,6-di£luoro- 4-methoxy-phenyl)-2-methoxy-acetainide formiate (78 mg) as white foam. MS 364.1 ([M+H]^) 337.4 In analogy to example 341-3 (R)-[(4-{[2-(2,6-difluoro-4-methoxy-phenyl)-2-methoxy- acetylaniinol-methyl}-phenyl)-imino-methyll-carbainic add tert-butyl ester was converted to (R)-N-(4-carbamimidoyl-benzyl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-methoxy- acetamide formiate. White foam. MS 364.1 ([M+H]"^) 338.1 A solution of (RS)-ethoxy-(2-fiuoro-4-methoxy-phenyl)-acetic add {7.26 g, example 63.1), ethanol (16.7 ml) and DMAP (1.57 g) in dichlororaethane (120 ml) was cooled to 0* and treated with EDCI (6.59 g). The reaction stirred was stirred at r.t for 18 hrs, then washed with 0.5 N HQ, H2O, saturated NaHCOs and brine. The organic layer was dried over MgSO^, filtrated and concentrated. The crude product was purified by flash chromatography (cyclohexane => cyclohexane/EtOAc 85:15) to give (RS)-ethoxy-(2-fiuoro-4-methoxy-phen}i)-acetic add ethyl ester (4.42 g) as yellow oil. MS 256.2 ([M]"^) 338.2 An emulsion of (RS)-ethoxy-{2-fluoro-4-methoxy-phenyI)-acetic add ethyi ester (1.11 g) in O.IM NaQ, 3 mM Natriumphosphat buffer pH 7.0 (260 ml) was cooled to 4-5°C and treated with lipase from Rhizomucor miehei. The reaction mixture was stirred for 4 days at 4-5° while maintaining the pH at 7 by gradual addition of O.lN NaOH (totally 25.5 ml), then extracted with CH2CI2 and then EtOAc. The organic layers were dried over Na2S04, then concentrated to give (R)-ethoxy-(2-fluoro-4-methoxy-phenyl)-acetic acid ethyl ester (330 mg, 98.9% ee). An emulsion of (R)~ethoxy-(2-fluoro-4-methoxy-phenyi)-acetic add ethyl ester (416 mg) in O.lM NaCl, 3 mM Natriumphosphat buffer pH 7.0 (75 ml) was cooled to 4-5'=C was treated with hog hver esterase suspension (0.175 ml). The reaction mixture was stirred for 4 days while maintaining the pH at 7 by gradual addition of O.lN NaOH (totally 12.8 ml). The reaction mixture was washed with CH2CI2, then brought to pH 2 by the addition of 2N HCl and extracted with EtOAc. The EtOAc layer was dried over Na2S04, filtrated and concentrated to give (R)-ethoxy-(2-fluoro-4-methoxy-phenyI)-acetic add (304 mg, 97.1% ee) as yellow semisoUd. 338.3 According to general procedure B (R)-ethoxy-(2-fluoro-4-methoxy-phenyl)-acetic add was reacted with [aniino-(4-aminomethyl-phenyi)-mediylene]-carbamic add berizyl ester hydrochloride 1:2 (prepared according to Ch. Lila, Ph. Gloanec, L. Cadet, Y. Herve, J. Foumier, F. Leborgne, T. J. Verbeuren, G. De Nanteuil, Synthetic Commimications 1998, 28, 23, 4419-4429) to give [l-amino-l-(4-{[(R)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyi)-acetylamino]-me^yi}-phenyl)-meth-(E)-ylidene]-carbamic add benzyl ester (96.5% ee). Off-white solid. 338.4 A solution of [l-amino-l-(4-{[(R)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)- acelylamino]-methyl}-phen)d)-meth-(E)-ylidene]-carbamic acid benzyl ester (1.95 mg) in EtOH (20 ml) was treated with HOAc (0.05 ml) and Pd/C 10% (20 mg) and hydrogenated over night at normal pressure. The catalyst was filtered off, the filtrate was concentrated to give (R)-N-(4-carbamimidoyl-benzyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)- acetamide acetate (151 mg, 96.3% ee) as white sohd. Example 339 Using general procedure C (RS)-ethoxy-(2-fluoro-4-methoxy-phenyl)-acetic acid (example 63.1) was reacted with [amino-(4-aminocnethyl-phenyl)-methylene]-carbamic acid benzyl ester hydrochloride 1:2 (prepared according to Ch. Lila, Ph. Gloanec, L. Cadet, Y. Herv^, J. Fournier, F. Leborgne, T. J. Verbeuren, G. De Nanteuil, Synthetic Communications 1998, 28, 23, 4419-4429) to give (RS)-[amino-(4-{[2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetylamino]-methyl}-phenyl)-methylenel-carbamic acid benzyl ester. White solid. MS 494.3 ([M+H]^) Referential Example 340 (RS)-[(4-{[2-(2,6-Difiuoro-4-methoxy-phenyl)-2-methoxy-acetyiamino]-methyi]-phenyl)-imino-methyl]-carbamic acid benzyl ester was prepared using a similar procedure as described in example 339. MS 498.4 ([M-t-H]"") Example 341 341.1 Using analogous procedures as described in examples LI - L4 3,5-difluoro-phenol was converted to (RS)-(2,6-difluoro-4-hydroxy-phenyl)-methoxy-acetic acid ethyl ester. White solid. MS 245.2 ([M-H]") 341.2 Using analoguous procedures as describen in examples 279.1 and 334.3 (RS)-(2,6-difluoro-4-hydroxy-phenyl)-methoxy-acetic acid ethyl ester was converted to (RS)-[2,6-difluoro-4-(4,4,5,5-tetramethyl-[ 1,3,2jdioxaborolan-2-yl)-phenyl]-methoxy-acetic add ethyl ester. YeUowoU. MS 356.2 ([M]"^) 341.3 Using a similar procedure as describe in example 57.1 (RS)-[2,6-difluoro-4-(4,4,5,5-tetramethyl-| 1,3,2] dioxaborolan-2-yl)-phenyl]-methoxy-acetic acid ethyl ester was converted to (RS)-(2,6-difluoro-4-pyridin-4-yl-phenyl)-methoxy-acetic acid ethyl ester. Waxy off-white solid. 341.4 A solution of (RS)-{2,6-difluoro-4-pyridm-4-)d-phenyl)-methox7-acetic acid ethyl ester (1.83 g) in CH2CI2 (25 ml) was treated with mCPBA (1.61 g). After stirring overnight at r.t. additional mCPBA (0.6 g) was added and stirring continued for 24 hrs. The reaction mixture was poured onto ice and saturated Na2C03-solution, then extraaed with dichloromethane. The organic layer was washed mit saturated NaiCOs-solution and brine, dried over MgS04, filtered and concentrated. The crude product was isolated by flash chromatography (cydohexane/EtOAc 1:4 => EtOAc; then CUtCh/MeOH 9:1 => 4:1) to give (RS)-[2,6-difluoro-4-(l-oxy-pyTidin-4-yl)-phenyl]-metho3Cy-acetic acid ethyl ester (474 mg) as yeUow oil. MS 324.2 ([M+H]^) 343.5 A solution of (RS)-[2,6-dfluoro-4-(l-oxy-pyridin-4-yl)-phenyl]-methoxy-acetic add ethyl ester (509 mg) in THF was treated with IN NaOH (3.15 ml) and stirred for 5 hrs at r.L. Then, the reaction mixture was neutralized with IN HQ (1.57 ml) and concentrated. The residue was taken up in diethyl ether. The soKd was filtered off, washed with diethyl ether and dried to give (RS)-[2,6-difluoro-4-(l-oxy-pyridin-4-)d)-phenyl]~methoxy-acetic add (599 mg, contains 1 equivalent of NaCl) as off-white sohd. MS 296.2 ([M+H]"") 341.6 (RS)-[2,6-Difluoro-4-(l-oxy-pyridin-4-yl)-phenyl]-methoxy-acetic add vras coupled with 4-aminomethyl-benzamidine hydrochloride (CAS 217313-79-6) according to general procedure C to give (RS)-(4-carbamimidoyl-ben2yl)-2-[2,6-difiuoro-4-(l-oxy-pyridin-4- yl)-phenyl]-2-methoxy-acetamide hydrochloride as amorphous white solid. MS 427.4 ([M+H]^) Example 342 342.1 To a stirred solution of (RS}-N-(4-Cyano-benzyl)-2-[2,6-difiuoro-4-(4,4,5,5-tetrameth)4-[l,3,2]dioxaborolan-2-yI)-phenyi]-2-ethoxy-acetamide (350 mg, example 262.1) at i.t. in dioxane (3 ml) under an argon atmosphere were added trifluoro-methanesulfonic add 3,6-dihydro-2H-pyran-4-yl ester (196 mg, CAS 188975-30-6, solution in 2 ml dioxane), KOH (86 mg), PdCMdppf) (31 mg) and l,l'-bis(diphen5dphosphino)ferrocene (21 mg). The mixtuie was then heated to SO^C for 6 hrs. The mixture was concentrated to leave a dark brown solid. The crude product was isolated by column chromatography (cydohexane => cyclohexane/EtOAc 55:45) to give (RS)-(4-cyano-benzyl)-2-[4-(3,6-dihydro-2H-pyran-4-yl)-2,6-difluoro-phenyl]-2-ethoxy-acetamide {107 mg) as Ught yellow gum. MS 413.1 ([M+HD 342.2 In analog)' to example 307.7 and 307.8 (RS)-(4-cyano-benzyl)-2-[4-(3,6-dihydro-2H- pyran-4-yl)-2,6-difIuoro-phenyll-2-ethoxy-acetainide was converted to (RS)-(4- carbamimidoyl-benzyl)-2-[2,6-difluoro-4-(tetrahydjo-pyran-4-yl)-phenyl]-2-ethox}'- acetamide acetate. Off-white powder. MS 432.4 ([M+H] +) Example 343 Using similar procedures as described in example 342 (RS)-N-(4-cyano-benz)4)-2-[2,6-difiuoro-4-(4,4,5,5-tetramethyl-[l,3)2]dioxaborolan-2-yl)-phenyl]-2-ethoxy-acetamide (example 262.1) was converted to (RS)-(4-carbaEQimidoyl-ben2yl)-2-(4-cycloliexyl-2,6-difluoro-phenyl)-2-ethoxy-acetamide acetate. Off-white powder. MS 430.4 ([M+H]"^) Example A Film coated tablets containing the following ingredients can be manufactured in a conventional manner: Ingredients Per tablet Kernel: Compound of formula (I) 10.0 mg 200.0 mg Microcrystalline cellulose 23.5 mg 43.5 mg Lactose hydrous 60.0 mg 70.0 mg Povidone K30 12.5 mg 15.0 mg Sodium starch glycolate 12.5 mg 17.0 mg Magnesium stearate 1.5 mg 4.5 mg (Kernel Weight) 120.0 mg 350.0 mg Film Coat Hydroxypropyi methyl cellulose 3.5 mg 7.0 mg Polyethylene glycol 6000 0.8 mg 1.6 mg Talc 1.3 mg 2.6 mg Iron oxyde (yellow) 0.8 mg 1.6 mg Titan dioxide 0.8 mg 1.6 mg The active ingredient is sieved and mixed with microcristalline cellulose and the mixture is granulated with a solution of polyvinylpyrrolidon in water. The granulate is mixed with sodium starch glycolate and magesiumstearate and compressed to yield kernels of 120 or 350 mg respectively. The kernels are lacquered with an aqueous solution / suspension of the above mentioned film coat Example B Capsules containing the following ingredients can be manufactured in a conventional manner: Ingredients Per capsule Compound of formula (I) 25.0 mg Lactose 150.0 mg Maize starch 20.0 mg Talc 5.0 mg The components are sieved and mixed and filled into capsules of size 2. Example C Injection solutions can have the following composition: Compound of formula (I) 3.0 mg Polyethylene Glycol 400 150.0 mg Acetic Acid q.s. ad pH 5.0 Water for injection solutions ad 1.0 ml The active ingredient is dissolved in a mixture of Polyethylene Glycol 400 and water for injection (part). The pH is adjusted to 5.0 by Acetic Acid. The volume is adjusted to 1.0 ml by addition of the residual amount of water. The solution is filtered, filled into vials using an appropriate overage and sterilized. Example D Soft gelatin capsules containing the following ingredients can be manufactured in a conventional manner: Capsule contents Compound of formula (I) 5.0 mg Yellow wax 8,0 mg Hydrogenated Soya bean oil 8.0 mg Partially hydrogenated plant oils 34.0 mg Soya bean oil 110.0 mg Weight of capsule contents 165.0 mg Gelatin capsule Gelatin 75.0 mg Glycerol 85 % 32.0 mg Karion 83 8.0 mg (dry matter) Titan dioxide 0.4 mg Iron oxide yellow 1-1 mg The active ingredient is dissolved in a warm melting of the other ingredients and the mixtm-e is filled into soft gelatin capsules of appropriate size. The filled soft gelatin capsules are treated according to the usual procedures. Example E Sachets containing the following ingredients can be manufectured in a conventional manner: Compound of formula (1) 50.0 mg Lactose, fine powder 1015-0 mg MicrocristalHne cellulose (AVICEL PH 102) 1400.0 mg Sodium carboxymethyl cellulose 14.0 mg Polyvin)ipyrrolidon K 30 10.0 mg Magnesiumstearate 10.0 mg Flavoring additives 1,0 mg The active ingredient is mixed with lactose, microcristalline cellulose and sodium carboxymethyl cellulose and granulated with a mixture of polyvinylpyrrolidon in water. The granulate is mixed with magnesiumstearate and the flavouring additives and filled into sachets. WE CLAIM : wherein R1 is hydrogen. OH, NHj, C1,7 aUcoxy-carbonyl, aryI-C[.7 alkoxy-carbonyl, aryloxy-carbonyi, C1.7 alkyl-carbonyl, aryl-carbonyl, or C1.7 alkoxy-carfaonyl which is substituted with halogen; R2, R3 and R4 independently from each other are selected from the group consisting of hydrogen, halogen, hydroxy, carboxy-C1.7 alkyl-NH, carbamoyl-C 1.7 alkyl-NH, C1.7 alkoxy-carbon)d-C1.7 alkyl-NH, hydroxy- Cj-iocycloalkyl-oxy, dihydroxy-C3.10 cyc!oallcyl-oxy, aryl, aryloxy, aryl-NH, aryl-C1,? alkyl-NH, aryl-C1.? alkyl-SO2-NH, aryl-C1.7 alkoxy-carbonyl-NH, aryl-C1.7 alkyl-NH-carbonyl-NH, heteroaryloxy, heteroaryl-Cj.? alkyl-NH, and C1-7 alkoxy, whichQ.? alkox/can optionally be substituted with hydroxy, carboxy, carbamoyl, carbamimidoylt CF3, aryl, heteroaryl, C1.7 alkyl-carbamoyi, C1.7 aikoxy-carbonjd, aryl-carbamoyl, C1.7 alkoxy-C1.7 alkyl-carbamoyl, heterocycl)d-C|.7 alkyi-carbamoyl, or N(C!.7 aIkyl)2-C1.7 alkyl-carbamoyl; R1 isC1.7alkyi orCj-iocycloalkyl, or, ifXis O or NR12R5 can also be hydrogen; R1 is hydrogen, C1-7 alkyl, or fluoro- C1.7 alkyl; Y isNorC-R11; R7, R9, R9, R10 and R" independently from each other are selected from the group consisting of hydrogenj hydroxy, halogen, amino, C^.j alkyl-amino, di- C1.7 alkyl-amino, C1-7 alkyl-carbonyl-amino, NO2, fluoro- C1-7 alkyt, C1.7 alkoxy, hydroxy- C1.7 alkoxy. fluoro- C1.7 alkoxy, C2-7 alkinyl, hydroxy- C2.7 alkinyl. aryl, aryi- Q.? alkoxy, aryloxy, aryloxy- C|.7alkoxy, heterocyclyl, heterocydylo3cy. Ct.7 alkoxy-carbonyl- C1.7 alkoxy. carbamoyl- C1.7 alkoxy, carboxy- C;.? alkoxy, C3.10 cycloalkyloxy, heteroaryl, amino- C1-7 alkoxy. d .7 alkyl-amino-C1.jalkoxy, and di-C1-7alkyl-amino-C1.7alkoxy, C1./alkyl-carbonyI-amino-C1.7alkyl, H0'1>}=CH, HCO, fluoro-C1.j alkyi-SOi-O, {C1.7 alkoxy)2^. CH(C1-7 alkoxy)], hydroxy-CH2oro-C1.7alkoxy, atyl-C1-7alkoxy-Q.? alkoxy, aryl-NH, aryl-NH-C1.7 alkyi, aryl-C1-; aikyl-carbonyi-NH, heterocyclyl-C1.7alkyl, heterocyclyl-carbonyl,heterocydyl-C1.7 alkoxy, C1.7alkyl-carbamoyI, fluoro-C1.7alkyI-carbamoyI, Cj-iQi^C1oaikyi-carbamoyi, C3_iocyC1oalkyi-C1.7 alkyl-carbamoyl, di-C1-^alkyl-carbamoyl, Cj,7alkDxy-C1-7alkyl-carbamoyl, di-Ct.7 alkyl-carbamoyl-C1^? alkoxy, heteroaryloxy, heteroaryl-C1-7 alkoxy, amino-C|.7allc)d, C1.7alk^, hydroxy-C1.7alkyl, Cj-iocydoalkyl.and Cj.iocycloalkyl- Q. 7 alkoxy which is optionally substituted with C1-7 alkyl; or R* and R9 or R7 and R9 are bound to each other to form a ring together with the carbon atoms to which they are attached and R and R together or R and R together are -0-CHj-O-. -O-CH2-CO-NH-, -O-CHj-CHrCH2-. or -CH=CH-CH=CH-, which can optionally be substituted with C1.7 alkyl or C(_7 alkoxy, and R"', R" andR1 or R9 respectively are as definde above; X isO R1^ is hydrogen, C1.7 alkyl, or C1.7 alkyl-carbonyl; and pharmaceutically acceptable salts thereof wherein the term "aryl" means a phenyl or naphthyl group, which can optionally be substituted by 1 to 5 substituents independently selected from the group consisting of C2.7 alkenyl, C2.7 alkinyl, dioxo-C1.7alk)dene, halogen, hydroxy, CN, CF3, NHi, N(H, C1.7 alkyl). N{C1-7 alkyDz, aminocarbonyl. carboxy, NO2, C1-7 alkoxy, thio- C1-7alkoxy, C1.7 alkylcarbonyl, C).? aUcylcarbon)dOxy, C1.7 alkoxycarbonyl, C1.7 alkyl-carbonyi-NH, fluoro-C1.7 alkyl, fluoro-C1.7 alkoxy, C|.7 allcoxy-carbonyl- C1.7alkoxy, carboxy-C|-7alkoxy, carfaamoyl-C1.? alkoxy, hydroxy-C1.7 alkoxy, NHrC1.7 alkoxy, N(H, Q.? alk)4)-C1.7 aUcoxy, NCC1.7 alkyl)3-C,.7 alkoxy, benz>^oxy-C,-7 alkoxy, HO-N=:CH-, and C1.? alkyl which can optionaUy be substituted with haJogen, hydroxy, NH2, N(H, C1.7 aikyl) or N(C1.7a]kyl)2: the term "heteroaryl" means an aromatic 5 to 6 membered monocyclic ring or 9 to 10 membered bicyclic ring which can comprise 1, 2 or 3 atoms selected from nitrogen, oxygen and/or sulphur, and the heteroaryl group may have a substituent described in connection with the term "aryl"; the term "heterocyclyi" means non-aromatic monocyclic heterocycles with 5 or 6 ring members, which comprise 1, 2 or 3 hetero atoms selected from nitrogen, oxygen and sulfur, and the heterocyclyi group may have a substituent described in connection with the term "aryl". 2. The compounds according to claim 1, wherein R1 is hydrogen, OH, NH2, C1.7alkoxy-carbonyl, aryl-Cj.? alkoxy-carbonyl, aryloxy- carbony!, C1-7 alkyl-carbonyi, aryl-carbonyl, or C].? alfcoxy-carbonyl which is substituted with halogen; R7, R7 and R* independently from each other are selected from the group consisting of hydrogen, halogen, hydroxy, and C1.7 alkoxy, which C1.7 alkoxy can optionaUy be substituted with hydroxy, carboxy or carbamoyl; R1 ■ isC1.7alkyIorC3.iocycloalkyi, or, ifXisOorNR1^, R7can also behydrogen; R* is hydrogen, C1.7 alkyl, or 9uoro-C|.7 alkyi; Y isNorC-R7; R1, R", R9, R10 and R9 ' independently from each other are selected, from the group consisting of hydrogen, hydroxy, halogen, amino, C(.7alkyl-amino, di-Cj.? alkyl-amino, C1.7alkyl-carbonyl-amino, NOz, fluoro-C1.7alkyl, C1_7alkoxy, hydroxy-C1-7 alkoxy, fluoro-C)-7alkoxy, C1.j alkin>i, hydroxy-C2.7 alkinyt, aryl, aryl-Cj.7 alkoxy, aryloxy, aryloxy-C1.7alkoxy, heterocyclyi, heterocydyloxy, C1.7 alkoxy-carbonyl-C1.7 alkoxy, carbamoyl-C1.7 alkoxy, carboxy-C|.7 alkoxy, Cs-io cycJoalkyJoxy, heteroaryl, amino-C1-?alkoxy, Cj-7 alkyl-amino-C1.? alkoxy, and di-C1.7 alkyl-amino-C1.7 alkoxy. or R* and R9 or R* and R9' are bound to each other to form a ring together with the carbon atoms to which they are attached and R* and R9 together or R* and R7 together are -0-CH2-0-, -O-CH3-CO-NH-, -O-CH2-CH2-CH2-, or -CH=CH-CH=CH-, which can optionally be substituted with C1 .7 alkyl or C1.7 alkoxy, and R10, R9 ' and R7 or R* respectively are as definde above; X isO R1^ is hydrogen, C1.7 alkyl, or C1.7 alkyl-carbonyl; and pharmaceutically acceptable salts thereof. 3. The compounds according to any of claims 1-2, wherein R is hydrogen, OH, NH2, or Cj.jalkoxy-carbonyl. 4 The compounds according lo any of claims 1-3, v^erein R9is hydrogen, OH, or C1.,alkoxy-carDonyi. 5, The compounds according 10 any of claims 1 - 4, wherein R is hydrogen, OH, or ethoxycarbonyl. 6. The compounds according to any of claims I -5, wherein R is hydrogen. y_ The compounds according lo any of claims 1-6, wherein R7, R9and R* independently from each other are hydrogen or halogen. 8. The compounds according to any of claims I - 7, wherein R , R and R are hydrogen. 9. The compounds according to any of claims 1 - 6, wherein R andR are hydrogen. IQ The compounds according to claim I, wherein R7 is hydrogen, halogen, hydroxy, caiboxy-C1-yalkyl-NH, carbamoyl-C1-yaM-NH, C1.7alkoxy-carbonyl- C1.7a!kyl-NH,hydroxy-C3.iocycloalkyl-oxy, dihydroxy-C3.iocydoalkyl-oxy,aryl, aryloxy, aryl-NH, aryl-C1.7 alkyl-NH, aryI-C1.7 alkyl-S02-NH, aryl-C,.? alkoxy-carbonyl-NH, aryi- C,.? alkyl-NH-carbonyl-NH, heteroaryloxy, heteroar)d-C1.7 alkyl-NH, or C1-7 alkoxy, which C1.7 alkojcy can optionally be substituted with hydroxy, carboxy, carbamoyl, carbamimidoyl, CFs, ary], heteroaryl. C1.7alk>^-carbamo)4, C1.7 alkoxy-carbonyl, aryl-carbamoyl, C1.7 alkoxy-C1.yalkyl-carbamoyl, heteroq'dyl-C|.7alkyl-carbamoyLorN{C|.7alkyl)2-C|.7aIk)'l-caibamoyl. U. The compounds according to claim I, wherein R7 is hydrogen, halogen, carboKy-C1.7aIfc)4-NH, aryUC1-? alkyl-NH, heteroaryt-C1.jalkyl-NH, or Q.y alkoxy, which C1-Talkoxycan optionally be substituted with carbamoyl, heteroar)d, or C1-Talkoxy-C1.y alkyl-carbamoyl. 12, The compounds according to claim J, wherein R7 i* hydrogen, fluorine, carbamoyimelhoxy, (2-methoxy-ethylcarbainoyI}-methoxy, pyridin-2-y!-methoxy, benzylamino, carboxymethl-amino, or pyridin-2-yImethyl-amino. 13. The compounds accordingto any of claims 1 - 12, wherein R7 is C1-7alkyl. 14. The compounds according to any of claims 1-13, wherein R7 is methyl or ethyl. 15. The compounds according to any of claims 1 - 14, wherein R* is hydrogen, methyl, or CFs. 16. Thecompounds according to any of claims I - r5, wherein R* is hydrogen. 17. The compounds according to any of claims 1 -16. wherein Y is C-R" and R9 R*, R9, R9° and R9 ' independently from each other are selected from the group consisting of hydrogen, hydroxy, halogen, di-C1-yallcyl-amino, C1.7aikyl-carbonyl-amino, NO3, fluoro-C1-7 alkyl, C1.7 alkoxy, hydroxy- C1.7 aUtoxy, fluoro- C1-7 aDcojfy, aryl, aryl-C1.7alkoxy, aryloxy, aryloxy-C1-? alkoxy, heterocyclyl, hcterocydyloxy, Cj-7 alkoxy-carbonyl-C1.? alkoxy, carbamoyl-C1-7 alkoxy, carboKy-C1.7 alkoxy, C3.10 cycloalkyloxy, heteroaryl, and di-C1-? atkyl-amino-C1.7 alkoxy. 18. The compounds according to any of claims I -17, wherein Y is C-R" and R7 R*, R9, R10 and R" independently from each other are selected from the group consisting of hydrogen, halogen, C1.7 alkoxy, and pyridyL 19. The compounds according to any of claims 1-18, wherein Y is C-R" and R"", R7, R9, R10 and R" independently from each other are selected from the group consisting of hydrogen, fluoro, bromo, methoxy, and pyridyl. 20. The compounds according to claim 1, wherein Y is C-R1\ R7 andR7or R9and R9 are bound to each other to form a ring together with the carbon atoms to which they are attached and R7 and R7 together or R* and R7 together are -O-CH2-O-, -O-CH2-CO-NH-. -O-CH2-CH2-CH2-, or -CH=CH-CH=CH-. which can optionally be substituted with C1.7 alley] or C1.7 aJkoxy, and R10, R7 and R7 or R7 respectiveiy are hydrogen. 21. The compounds according to any of claims I -16, wherein Y is C-R" and R9 R8, R9, R10 and R7 independently from each other are selected from the group consisting of hydrogen, halogen, Cj.? alkcoxy and heteroaryl. 22. The compounds according to any of claims 1 - 16, wherein Y is C-R" R7 is halogen, R* is hydrogen, R9 is C1.7 alkoxy, heteroaryl or heteroaryl-Cj.? alkoxy, R10is hydrogen and R" is hydrogen or halogen. 23. The compounds according to any of claims 1 - 16, wherein Y is C-R", R9 is fluorine, R7 is hydrogen, R9 is methoxy, pyridin-3-yI, 5-amino-pyridin-2-yI, 6-amJno-pyridin-3-yl, pyTidin-2-ylmethoKy, or 2-amino-pyTimidin-5-yl, R9° is hydrogen and R" is hydrogen or fluorine. 24. The compounds according to claim 1, selected from the group consisting of (S)-N-(4-Carbamimidoyl-benzyl)-2-methoxy-2-phenyi-acetamide hydrochloride, (RS)-N-(4-Carbamimidoyl-ben2yI)-2-(2-fluoro-4-methoxy-phenyl)-2-methoxy-acetamide hydrochloride, (RS)-lAniino-(4-l[2-{2-fluoro-4-methoxy-phenyi)-2-methoxy-acetylamino]-methyl}-phenyl)-methylene]-carbamic aC1d ethyl ester, (RS)-2-C2-Fluoro-4-methoJcy-phenyl)-N-[4-(N-hydroxycarbamimidoyl)-beiizyl]-2-methoxy-acetamide, (RS)-N-(4-Carbamimidoyl-ben2yI)-2-(3-fluoro-3'-methoxy-biphenyl-4-yl)-2-methoxy-acetamide hydrochloride, (RS)-N-(4-Carbamimidoyl-benzyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyI)-acetamide hydrochloride, {RS)-N-(4-Carbamimidoyl-benzyl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-methoxy-acetamide hydrochloride, (RS)-N-(4-Carbamimido)1-benzyI)-2-(2-fluoro-4-pyridin-3-yl-phenyi)-2-methoxy-acetamide hydrochloride, and (RS)-2-{4-Bronio-2,6-difluoro-phenyl )-N-(4-carbamimidoyl-benzyi)-2-ethoxy-acetamide hydrochloride, and pharmaceuticaily acceptable salts thereof. 25. The compounds according to claim I, selected from the group consisting of (RS)-N-(4-Carbamimidoyl-2-carbaraoylmethoxy-benzyl)-2-(2,6-difluoro-4-methoxy-phenyI)-2-ethoxy-acetainide hydrochloride, (RS)-N-{4-Carbaminiidoyl-2-[{2-rnethOxy-eth7lcarbamoy!)-melhoxy]-benzyl}-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide hydrochloride, (RS)-N-l4-Carbamim!doyl-2-(pyridin-2-y!inetho);y)-benzyl]-2-{2,6-difluoro-4-niethoxy-phcny3)-2-jiietbQxy-acetaniidehydroc]3]oride, (RS)-2-[4-(2-Ainino-pyrimidin-5-yl)-2,6-difluaro-phen)d]-N-(4-caibamimidoyl-benzyl)-2-ethDxy-acetamidc hydrochloride, (RS)-N-(4-Carbaminiidoyl-benzyl)-2-{2,6-difluoro-4"pyTidin-3-yl-phenyt)-2-ethoxy-acetamide hydrochloride, (RS)-2-[4-{5-Amino-pyridin-2-yl)-2,6-diQuoro-phenyll-N-(4-carbamimidoyI-benzyl)-2-ethoxy-acetamide hydrochloride, (RS)-(2-[4-(6-Amino-pyridin-3-yl)-2,6-difluoro-phenyI]-N-(4-carbamimidoyl-benzyl)-2-ethoxy-acetamide hydrochloride, (RS)-N-C4-Carbamimidoyl-benzyl)-2-l2,6-difluoro-4-(pyridin-2-ylmethoxy)-phenyl]-2-ethoxy-acetamide hydrochloride, (RS)-N-(2-Benzylamino-4-carbaniiinidoy!-benzyl}-2-ethoxy-2-(2-fluoro-4'inethoxy-phenyO-acetamide acetate, (RS)-(5-CarbamimidoyI-2-{[2-ethoxy-2-{2-fluoro-4-methoxy-phenyl)-acety!araino)-methyil-phenytainino)-acetic aC1d acetate, (RS)-(4-Carbaniimidoyl-2-carbamo)dmelhoxy-benzyl)-2-[2,6-difluoro-4~(pyTidin-2-yImethoxy)-phenyI]-2-ethoxy-acetamide hydrochloride, (RS)-2-[4-(6-Amino-pyridin-3-yl)-2,6-difluoro-phenyll-N-(4-carbamimidoyl-2,6-difluoro^benzy])-2-ethoxj'-acetamide acetate, and (RS)-i4-Carbamimido>d-2-[(pyridiii-2-yiinethyl)-aminol-benzyl}-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide hydrochloride, and pharmaceylicajly acceptable salts thereof. 26. A process for the manufacture of compounds of formula {I) as defined in any of claims I -25 which process comprises converting the nitrile group in a compound of formula (11) wherein R2 R3 R4 R5 R6 R7, R8, R9, R10, X and Y have the significances given in any of claims 1-25 into a carbamimidoyl group, or into a N-hydroxy-carbamimidoyl group, or into a N-amino-carbamimidoyl group, and, if desired, converting an obtained compound of formula (I) into a pharmaceutically acceptable "salt. 27. The Compounds according to any of claims 1 - 26, when manufectured by a process according to claim 26. 28. Compounds of formula (II) wherein R7 R7 R*, R7 R*, R9, R*, R9, R9*". X and Y have the significances given in claim 1. 29, Pharmaceutical compositions comprising a compound according to any of claims 1-25, and a pharmaceutically acceptable carrier and/or adjuvant Mandelic acid derivatives The invention is concerned with novel mandelic acid derivatives of the formula (I) wherein R1 is hydrogen, OH, NH2, lower-alkoxy-carbonyl, aryi-lower-alkoxy-carbonyi, aryloxy-carbonyl, lower-alkyl-carbonyl, aryi-carbonyi, or lower-alkoxy-carbonyl which is substituted with halogen; R2, R2 and R8 independently from each other are selected from the group consisting of hydrogen, halogen, hydroxy, carboxy-lower-allqd-NH, carbamoyl-lower-alk)4-NH, lower-alkoxy-carbonyl-lower-alkyl-NH, hydroxy-cycloalkyl-oxy, dihydroxy-cydoaBcyi-oxy, aryl, aryioxy, aryl-NH, aryl-lower-alkyl-NH, aryl-lower-alkyi-S02-NH, aryl-lower-alkoxy-carbonyl-NH, aryl-lower-alkyl-NH-carbonyl-NH, heteroaryloxy, heteroaryl-lower-alkyl-NH, and lower-alkoxy, which lower-alkoxy can optionally be substituted with hydroxy, carboxy, carbamo)d, carbamimidoyl, CF3, arji, heteroaryl, lower-alkyl-carbamoyl, lower-alkoxy-carbonyl, aryl-carbamoyi, lower-alkoxy-lower-alkyl-carbanioyl, heterocyclyl-lower-alkji-carbamoyl, or N(lower-alk)d)2-Iower-aIkyi-carbamoyl; R2 is lower-aDcyl or cycloalkyl, or, if X is O or NR , R2 can also be hydrogen; R6 is hydrogen, lower-alkyl, or fluoro-lower-alkyl; CS / 02.10^003 y isNorC-R6; R , R , R1, R and R independently from each other are selected from the group consisting of hydrogen, hydroxy, halogen, amino, lower-alkyl-amino, di-lower-alkyl-amino, lower-alkyl-carbonyl-amino, NO2, fluoro-lower-alkyi, lower-alkoxy, hydroxy-Iower-alkoxy, fluoro-lower-alkoxy, lower-alkinyl, hydroxy-lower-alkinyl, aryi, aryl-Iower-alkoxy, aiyloxy, aryloxy-lower-alkoxy, heterocyclyl, heterocyclyloxy, lower-alkoxy-carbonyi-lower-alkoxy, carbamoyl-lower-allcoxy, carboxy-lower-alkoxy, cycloalkyloxy, heteroaryl, amino-lower-alkosy, lower-alkyl-amino-loweR1alkoxy, and di-lower-alkyl-amino-lower-aJkoxy, lower-alk)d-carbonyl-amino-lower-altyl, HO-N=CH, HCO, fluoro-lower-aIkyl-S02-0, (lower-alkoxy):^) CH(lower-aIkoxy)2, hydroxy-chloro-lower-alkoxy, aryl-lower-alkoxy-lower-alkoxy, aryl-NH, aryi-NH-lower-alkyl, aryl-lower-alkyl-carbonyl-NH, heterocycl^-lower-alkyi, heterocyclyj-carbonyl, heterocyclyl-lower-alkoxy, lower-alkyl-carbamoyl, fluoro-lower-alkji-carbamojd, cycloalkyl-carbamoyl, cycioalkyi-lower-aBcjd-carbamoyl, di-lower-alk)i-carbamoyl, lower-alkoxy-Iower-alkyl-carbamoyi, di-lower-aUcyl-carbamo^d-lower-alkoxy, heteroaryloxy, heteroaryl-lower-alkoxy, amino-lower-alkyl, lower-alkyl, hydroxy-lower-allcjd, cycloalkyl, and cycloalkyi-lower-alkoxy which is optionally substituted with lower-alkyl; or R2 and R2 or R2 and R2 are bound to each other to form a ring together with the carbon atoms to which they are attached and R2 and R1 together or R2 and R2 together are -O-CH2-O-, -O-CHa-CXD-NH-, -O-CH2-CH2-CH2-. or -CH=CH-CH=CH-, which can optionally be substituted with lower-allcyd or lowei-alkoxy, and R2°, R6 and R2 oi R1 respectively are as defiiide above; X is O, S, NR112 or SO2; R2^ is hydrogen, lower-alkyl, or lower-alkjd-carbonyl; and pharraaceutically acceptable salts diereof. Further, the invention is concerned with a process for the manufecture of the above compounds, pharmaceutical preparations which contain such compounds as well as the use of these compounds for the production of pharmaceutical preparations. The compounds of formula (I) are active compounds and inhibit the formation of coagulation &ctors Xa, IXa and thrombin induced by fector Vila and tissue fector or are derivatives which are converted under physiological conditions to such active compounds. These compounds consequently influence both platelet aggregation which is induced by these factors and plasmatic blood coagulation. They therefore inhibit the formation of thrombi and can be used for the treatment and/or prevention of diseases, such as arterial and venous thrombosis, deep vein thrombosis, pulmonary embolism, unstable angina pectoris, cardiac infarction, stroke due to atrial fibrillation, inflammation and arteriosclerosis. Furthermore, these compounds have an effect on tumour cells and prevent metastases. They can therefore also be used as antitumour agents. Inhibitorsof factor Vlla had previously been suggested for the inhibition of the formation of thrombi and for the treatment of related diseases (WO 00/35858). However, there is still a need for novel factor Vlla inhibitors which exhibit improved pharmacological properties. The present invention provides the novel compounds of formula (I) which are factor Vila inhibitors. The compounds of the present invention exhibit improved pharmacological properties compared to the known compounds. Unless otherwise indi In this specification the term "loweR6 is used to mean a group consisting of one to seven, preferably of one to four carbon atom{s). The term "halogen" refers to fluorine, chlorine, bromine and iodine, with fluorine, chlorine and bromine being preferred. The term "alkyl", alone or in combination with other groups, refers to a branched or straight-chain monovalent saturated aliphatic hydrocarbon radical of one to twenty carbon atoms, preferably one to sixteen carbon atoms, more preferably one to ten carbon atoms. Lower-alkyl groups as described below also are preferred alkyl groups. The term "lower-alkyl", alone or in combination with other groups, refers to a branched or straight-chain monovalent alkyl radical of one to seven carbon atoms, preferably one to four carbon atoms. This term is further exemplified by such radicals as methyl, ethyl, n-propyl, isopropyl, n-butyl, s-butyl, t-butyl and the like. The term "fluoro-lower-alkyl" refers to lower-alkyl groups which are mono- or multiply substituted with fluorine. Examples of fluoro-lower-alkyi groups are e.g. CFH2, CF2H, CF3, CF3CH2, CF3(CH2)2, (CFjjiCH and CF2H-CF2 The term "cycloalkyl" refers to a monovalent carbocydic radical of 3 to 10 carbon atoms, preferably 3 to 6 carbon atoms, such as cyclopropyl, cyclobutyi, cyclopentyl, or cydohexyl. The term "cycloalkyloxy" refers to the group cydoaIky!-0-. The term "alkoxy" refers to the group R1-O-, wherein R1 is an alkyl. The term "lower-alkoxy" refers to the group R1-O-, wherein R1 is a lower-alkyl. The term "thio-alkoxy" refers to the group R1-S-, wherein R1 is an alkyl. The term "thio-lower-alkoxy" refers to the group R1-S-, wherein R1 is a lower-alkyl. The term "fluoro-lower-alkoxy" refers to the group R6-0-, wherein R6 is fluoro-lower-alkyl. Examples of fluoro-lower-alkoxy groups are e.g. CFH2-O, CF2H-O, CF3-O, CF3CH2-O, CF3(CH2)2-0. (CF3)2CH-0, and CF2H-CF2-O, The term "alkenyl", alone or in combination with other groups, stands for a straight-chain or branched hydrocarbon residue comprising an olefinic bond and 2 to 20, preferably2 to 16 carbon atoms, more preferrabiy2 to 10 carbon atoms. Lower-alkenyl groups as described below also are preferred alkenyl groups. The term "lower-alkenyl" refers to a straight-chain or branched hydrocarbon residue comprising an olefinic bond and 2 to 7, preferably 2 to 4 carbon atoms, such as e.g. 2-propenyl. The term "alkinyl", alone or in combination with other groups, stands for a straight-chain or branched hydrocarbon residue comprising a tripple bond and up to 20, preferably up to 16 carbon atoms. The term "lower-alkinyl" refers to a straight-chain or branched hydrocarbon residue comprising a tripple bond and 2 to 7, preferably 2 to 4 carbon atoms, such as e.g. 2-propinyl. Lower-alkinyl groups can be substituted, e.g. by hydroxy. The term "alkylene" refers to a straight chain or branched divalent saturated aliphatic hydrocarbon group of 1 to 20 carbon atoms, preferably 1 to 16 carbon atoms, more preferably up to 10 carbon atoms. Lower-alkylene groups as described below also are preferred alkylene groups. The term "lower-alkylene" refers to a straight chain or branched divalent saturated aliphatic hydrocarbon group of 1 to 7, preferably 1 to 6 or 3 to 6 carbon atoms. Straight chain alkyiene or lower-alkylene groups are preferred. The term "aryl" relates to the phenyl or naphthyl group, preferably the phenyl group, which can optionally be substituted by 1 to 5 , preferably 1 to 3, substituents independently selected from the group consisting of lower-alkenjd, lower-alldnyl, dioxo-lower-alkylene {forming e.g. a benzodioxyl group), halogen, hydroxy, CN, CFa, NH;, N(H, lower-allcyl), N(lower-alk)'l)2, aminocarbonyl, carboxy, NO2, lower-alkoxy, tbio-lower-alkoxyi lower-alkylcarbonyl, lower-alkyicarbonyloKy, lower-alkoxycarbonyl, lower-alkyl-carbonyl-NH, fluoro-lower-alkyl, fluoro-lower-alkoxy, lower-alkoxy-carbonyi-lower-alkoxy, carboxy-lower-altoxy, carbamoyl-lower-alkoxy, hydroxy-lower-alkoxy, NH2-lower-alkoxy, N(H, lower-allcyl)-lower-alkoxy, N(Iower-alkyl)2-lower-alkoxy, benzyloxy-lower-alkoxy, HO-N=CH-, and lower atkyl which can optionaEy be substituted with halogen, hydroxy, NH2, N(H, lower-allcyl) or N(lower-alkyl)2. Preferred substituents are halogen, lower-alkoxy, lower-alkyl-carbamoyl-NH, CN, fluoro-lower-aHcoxy, fluoro-lower-alkyl, lower-allcyl, thio-Iower-allcoxy, lower-alkoxy-carbonyl-lower-alkoxy, carboxy-lowei-allcoxy, carbamoyl-lower-aBcoxy, hydroxy-lower-alkoxy, N(lower-alkyl)2-lower-alkoxy, benzyloxy-lower-alkoxy, lower-alkoxy-carbonyl, carboxy, hydroxy-lower-alkyl, chloro-lower-alkyl, HO-N=CH-, amino-lower-allcyl, amino, and NO;- The term "aryloxy" refers to the group aryl-0-. The term "heterocycl)^' as used herein denotes non-aromatic monocydic heterocydes with 5 or 6 ring members, which comprise 1,2 or 3 hetero atoms selected from nitrogen, oxygen and sulfiir. Examples of suitable heterocydes are pyrrolidine^, oxopyrrolidinyl, pyrrolinyl, imidazoUdinyl, imidazolinyl, pyraioUdinyl, pyrazoUnyl, piperidyl, piperazinyl, morphohn^d, pyranyl, tetrahydropyran-jd, 4,5-dihydro-oxa2olyl, 4,5-dihydro-thiazolyi. Preferred heterocydes are piperidinyl, morpholinyl, pyrrolidinyl, oxopyrroHdinyl, tefrahydrofiiranyl and tetrahydropyranyl. A heterocyd)^ group may have a substitution pattern as described earher in coimection with the term "aryl". Preferred substituents are lower-alfcjd, lower-alkj^-sulfonjd, benzenesulfonyi, lower-alkyl-carbonyl and benzoyl. The term "heterocydyloxy" refers to the group heterocydyl-O-. The term "heteroaryl" refers to an aromatic 5 to 6 membered monocycUc ring or 9 to 10 membered bicycUc ring which can comprise 1,2 or 3 atoms selected from nitrogen, oxygen and/or sulphur, such as furyl, pyridyl, oxo-pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, thienyl, isoxazolyl, oxazol^, oxadiazolyl, imidazolyl, pyrtolyl, tetiazolyl, benzoimidazolyl, indolyl. Preferred heteroaryl groups are pyridinyi, oxo-pyridinyl, thienyl, furyl, oxadiazolyi, pyiimidinyl, benzoimidazolyl, indolyl. A heteroaryl group may have a substitution pattern as described earlier in connection with the term "aryl". Preferred substituents are NO2, NH2, lower-alkoxy. The term "heteroaryloxy" refers to the group heteroaryl-O-. Compounds of fonnula (I) can form pharmaceutically acceptable add addition salts. Examples of such phannaceaticaHy acceptable salts are salts of compounds of formula (I) with physiologically compatible mineral adds, such as hydrochloric add, sulphuric add, sulphurous acid or phosphoric addi 01 with organic adds, such as methanesulphonic add, p-toluenesulphonic add, acetic add, lactic add, trifiuoroacetic add, citric add, fumaric acid, maleic add, tartaric add, sucdnic add or salicylic add. The term "pharmaceutically acceptable salts" refers to such salts. Compounds of formula (I) in which a COOH group is present can further form salts with bases. Examples of such salts are alkaline, earth-alkaline and ammonium salts such as e.g. Na-, K-, Ca- and Trimeth)^ammoniumsalt The term "pharmaceutically acceptable salts" also refers to such salts. Add addition salts as described above are preferred. In detail, the present invention relates to compounds of formula (I) wherein R2 is hydrogen, OH, NH2, lower-alkoxy-carbonyl, aryl-lower-alkoxy-carbonyl, aryloxy-carbon)d, lower-aIk)d-carbonyi, ar)d-carbon)d, or lower-aikoxy-carbonyl which is substituted with halogen; R2, R2 and R8 independently from each other are selected from the group consisting of hydrogen, halogen, hydroxy, carboxy-lower-alkyi-NH, carbamoyl-Iower-alkyl-NH, lower-alkoxy-carbonyl-lower-alkji-NH, hydrory-cycloalkyl-oxy, dihydroxy-cycloalkj^-oxy, aryl, aryloxy, aryi-NH, aryHower-alkyl-NH, aryi-lower-alkyl-SOz-NH, ar)^-lower-alkoxy-carbonyi-NH, aryl-lower-alkyl-NH-carbonyl-NH, heteroaryloKy, heteroaryl-lowet-alfcyl-NH, andlower-alkoxy, which lower-alkoxy can optionally be substituted with hydroxy, carboxy, carbamo)4, carbamimidoyi, CF3, aryl, heteroaryl, lower-aUqd-carbamoyl, lower-alkoxy-carbonyl, aryl-carbamoyl, lower-alkoxy-lower-alkyl-carbamoyi, heterocyclyl-lower-alkyl-carbamoyl, or N(lower-alkyl)2-lower-aIkyl-carbamoyl; R2 is lower-alkyl or cycioalkyl, or, if X is O 01NR12, R2 can also be hydrogen; R8 is hydrogen, lower-alkyi, or fluoro-lower-alkyi; Y isNorC-R2^ R6", R2, R1, R2*' and R6 independently from each other are selected from the group consisting of hydrogen, hydroxy, halogen, amino, lower-alkyl-amino, di-lower- alkyl-amino, lower-alkyl-carbonjd-anmio, NO2, fluoro-lower-allcyi, lower-alkoxy, hydroxy-lower-alkoxy, fluoro-lower-alkoxy, lower-aBdnyl, hydroxy-lower-aDdnyl, aryl, ar)i-lower-alkoxy, aryloxy, aryioxy-Iower-alkoxy, heterocyclyl, heterocyclyioxy, lower-aDcoxy-carbonyl-lower-alkosy, carbamoyl-lower-alkoxy, carboxy-lower-alkoxy, cycloalfcyloxy, heteroarjd, amino-lower-alkoxy, lower-alkjd-amino-lower-alkoxy, and di-lower-alkyl-amino-Iower-alkoxy, lower-alkyl-carbonyI-amino-lower-alkyl,HO-N=CH, HCO, fluoro-lower-aIkyl-S02-0, (lower-alkox7)2^, CH(lower-a]koxy)2, hydroxy-chloro-lower-alkoxy, aryl-lower-alkoxy-lower-alkoxy, aryl-NH, ar)d-NH-lower-aIkyl, ar)d-iower-alkyi-carbonyl-NH, heterocyd^-lower-alkyl, heterocydyl-carbonyl, heterocyclyl-lower-alkoxy, lower-alkyl-carbamo^, fluoro-lower-alkyl-carbamoyi, cycloalk)i-carbainoyl, cydoalkyl-lower-alkyl-carbamoyi, di-lower-alkyi-carbamoyl, lower-alkoxy-lower-alkyi-carbamoyl, di-lower-alkyl-carbamoyl-lower-alkoxy, heteroaryloxy, heteroarjd-lower-alkoxy, amino-lower-alkyl, lower-alkyl, hydroxy-lower-alkyl, q'doalkyl, and cydoalkyl-lower-alkoxy whidi is optionally substituted with lower-alkyi; or R2andR2orR2andR2 are bound to each other to form a ring together with the carbon atoms to which they are attached and R2 and R togeflier or R and R together are -O-CH2-O-, -O-CH2-CO-NH-, -O-CH2-CH2-CH2-, or -CH=CH-CH=CH-, which can optionally be substituted with lower-alkyl or lower-alkoxy, and R2°, R6 and R2 or R1 respectively are as definde above; X is O, S, NR12 or SO2; R2^ is hydrogen, lower-alkyl, or lower-allcyl-carbonyl; and pharmaceutically acceptable salts thereof. One preferred embodiment of the present invention rdates to compounds of formula (I) as defined above, wherein R2 is hydrogen, OH, NH2, lower-alkoxy-carbon)4, arjd-lower-alkoxy-carbonyl, aryloxy-carbonyl, lower-alkyl-carbonyl, aryl-carbonyl, or lower-alkoxy-carbonyi which is substituted with halogen; R2, R2 and R2 independently from each other are sdected from the group consisting of hydrogen, halogen, hydroxy, and lower-alkoxy, which lower-alkoxy can optionally be substituted witii hydroxy, carboxy or carbamoyl; R2 is iower-alkyl or cycloalkyl, or, if X is O or NR12, R2 can also be hydrogen; R is hydrogen, lower-alkyl, or fluoro-lower-altji; Y isNorC-R11; VJ, R2, R2, R10 and R6 independently from each other are selected &om the group consisting of hydrogen, hydroxy, halogen, amino, lower-alkyl-amino, di-Iower-alkyi-amino, lower-alkjd-carbonyl-amino, NO2) fluoro-lower-alkyl, lower-alkoxy, hydroxy-lower-alkoxy, fluoro-lower-alkoxy, lower-alkinyl, hydroxy-lower-alldnyi, aryl, ar}^-Iower-alkoxy, aryloxy, arjdoxy-lower-alkoxy, heterocyclyl, heteiocyclyloxy, iower-alkoxy-carbonyl-Iowar-alkoxy, carbamoyl-lower-alkoxy, carboxy-lower-aUtoxy, cycloalkyloxy, heteroaryl, amino-lower-alkoxy, lower-alkyi-amino-Iower-alkoxy, and di-Iower-alkyl-amino-lower-alkoxy, or R2 and R2 or R8 and R6" are bound to each other to form a ring together with the carbon atoms to which they are attached and R8 and R1 together or R2 and R2 together are -O-CH2-O-, -O-CH2-CO-NH-, -O-CH2-CH3-CH2-, or -CH=CH-CH=CH-, which can optionally be substituted with lower-alkyl or lower-alkoxy, and R2'*, R6 and R2 or R2 respectively are as definde above; X is O, S, NR12 or SO2; R1^ is hydrogen, lower-alkyl, or lower-alkyl-carbon^; and pharmaceutically acceptable salts thereof. The compounds of formula (I) have at least one asymmetric C atom and can therefore exist as an enantiomeric mixture, diastereomeric mixture or as optically pure compounds. Compounds of formula (I) can exist in tautomeric forms and the invention encompasses all such tautomeric forms. In particular, the substituent R can be exchanged with a hydrogen atom bound to the other nitrogen atom of the amidino (carbaniimido)d) group. Compounds of formula {I) are individually preferred and physiologically acceptable salts thereof are individually preferred, with the compounds of formula (I) being particularly preferred. Preferred compounds of formula (I) are those, wherein R1 is hydrogen, OH, NHi, or lower-alkoxy-carbon^, preferably liiose. "wherdn R1 is hydrogen, OH, or lower-alkoxy-carbonyl, more preferably those wherein R2 is hydrogen, OH, or ethoxycarbonyl, and most preferably those wherein R1 is hydrogen. Another preferred embodiment of the present invention relates to compounds as described above, wherein R2, R2 and R8 independently from each other are hydrogen or halogen, with those compounds wherein R6, R2 and R2 are hydrogen being most preferred. In another preferred embodiment of the present invention, R2 and R8 are hydrogen. Compotinds as defined above, wherein R is hydrogen, halogen, hydroxy, carboxy-lower-alkyl-NH, carbamoyl-lower-alkyl-NH, iQwer-alkoxy-caibonyl-Iower-alkyl-NH, hydroxy-cycioaliyl-oxy, dihydroxy-cycloalkyi-oxy, aryl, arjdoxy, aryl-NH, aryl-lower-alkyl-NH, aryl-lower-alkyl-S02-NH, aryl-lower-allcoxy-carbonyl-NH, aryl-Iower-alk)d-NH-carbonyl-NH, beteroaiylosy, heteroaryl-Iowei-alkyi-NH, or lower-alkoxy, vriiich lower-alkosy can optionally be substituted with hydroxy, carboxy, carbamo}d, carbamimidoyi, CFs, aR2d, heteroaryl, lower-alkyd-carbamoyl, lower-alkoxy-carbonyl, aryi-carbamoyl, lower-alkoxy-lower-alkyl-caxbamoyl, heterocydyi-lower-alkyl-carbamoyl, or N(lower-alkyl)2-lowex-alkyl-carbamoyl, are also preferred. More preferably, R2 is hydrogen, halogen, carboxy-lower-alkyl-NH, aryl-lower-alkyl-NH, heteroaryi-lower-alkyl-NH, or iower-alkoxy, which lower-alkoxy can optionally be substituted with carbamoyl, heteroaR2d, or lower-alkoxy-lower-aHcyl-carbamoyl. Even more preferably, R2 is hydrogen, fluorine, carbamoylmethoxy, (2-methoxy-ethyicarbamoyl)-methoxy, pyridin-2-yi-methoxy, benzylamino, carboxymethl-amino, or pyridin-2-ylmetiiyl-amino. In a further preferred embodiment the invention rdates to compounds as described above in which X is O. Compounds in which R2 is lower-alkyl, or, if X is O or NR12, R2 can also be hydrogen, are preferred. Compounds in which R2 is lower-alkyi are also preferred, with those compounds wherein R2 is methyl or ethyl being particularly preferred. The invention embraces especially compounds in accordance with the above definitions in which R1^ is hydrogen, methyl or CFa, preferably hydrogen. In one preferred embodiment, R2 and R2 or R2 and R1 are not bound to each other to form a ring together with the carbon atoms to which they are attached. Moreover, the invention relates especially to compounds as defined above wherein Y is C-R and R , R , R2, V}° and R2' independently from each other are selected from the group consisting of hydrogen, hydroxy, halogen, di-lowei-aUcyl-amino, lower-alkjd-carbonyl-amino, NO2, fluoro-lower-atkyl, Iower-alkoxy, hydroxy-lower-alkoxy, fiuoro-Iower-alkoxy, aryl, axyi-lower-alkoxy, aryloxy, aryioxy-lower-alkoxy, heterocyclyl, heterocyclyloxy, Iower-alkoxy- carbonyl-lower-alkoxy, carbamoyl-lower-alkoxy, carboxy-lower-allcoxy, qfcloaIk)doxy, heteroaryl, and di-lower-alkyi-amino-Iower-alkoxy. More preferably, Y is C-R2' and iC, R2 R , R and R independently from each other are selected from the group consisting of hydrogen, halogen, lower-alkoxy, and pyridji. Even more preferably, Y is C-R2^ and R2, R2 R , R and R independentiy from each other are selected from the group consisting of hydrogen, fluoro, bromo, methoxy, and pyridyl. In another preferred embodiment of the present invention, Y is C-R6, R8 and R1 or R and R2 are bound to each other to form a ring together with the carbon atoms to which they are attached and R2 and R1 together or R2 and R2 together are -O-CHz-O-, -O-CH2-CO-NH-, -O-CH2-CH2-CH2-, or -CH=CH-CH=CH-, which can optionaUy be substituted with lower-allqd or lower-alkoxy, and R2", R6 and R2 or R2 respectivdy are hydrogen. Compounds as defined above, wherein Y is C-R2^ and R2 R2, R2, R2" and R6 independently from each other are selected from the group consisting of hydrogen, halogen, lower-alkoxy and heteroaryl, are also preferred. Even more preferred are compounds as defined above, wherein Y is C-R2\ R2 is halogen, R2 is hydrogen, R1 is lower-alkoxy, heteroaryl or heteroarjd-lower-alkoxy, R2° is hydrogen and R2' is hydrogen or halogen. Most preferred are those compounds as defined above, wherein Y is C-R , R is fluorine, R8 is hydrogen, R is methoxy, pyridin-3-yI, 5-amino-pyridin-2-yi, 6-amino-pyridin-3-yl, pyTidin-2-ylmethoxy, or 2-amino-pyrimidin-5-yI, R1° is hydrogen and R is hydrogen or fluorine. In particular, preferred compounds are the compounds of formula (I) described in the examples as individual compounds as well as pharmaceutically acceptable salts thereof. Preferred compounds of formula (I) are those selected from the group consisting of (S)-N-(4-Carbaroiniidoyl-benzyl)-2-methoxy-2-phenyl-acetamide hydrochloride, {R)-N-(4-Carbamimidoyl-benzj^)-2-methoxy-2-phenyI-acetamide hydrochloride, (RS)-2- (4-Ben2yloxy-phenyi)-N-(4-carbamimido)4-benzyl)-2-methoxy- acetamide hydrochloride, (RS) -N-{4-Carbamimido)d-benzyl) -2-methoxy-2-(4-phenoxy-phenyl) -acetamide hydrochloride, {RS) -N- (4-Carbamimidoyl-benzyI)-2-methoxy-2-(3-phenoxy-phenyl)-acetaniide hydrochloride, (RS)-N-(4-Carbamimidoyl-benzyl)-2-ethoxy-2-phenyl-acetamide hydrochloride, (RS) -N- {4-Carbanumido)^-ben2yi) -2-(2-fluoro-phenyI)-2-methoxy- acetamide hydrochloride. (RS)-2-(S-Benzyloxy-phenyi)-N-(4-carbammiidoyI-benzyl}-2-inethoxy-acetar[iide hydrochloride, (RS) -N- (4-Carbamimido)d-benzj'l) -2- (S-hydroxy-phen)^) -2-methoxy-acetaiiiide hydrochloride, (RS) -N- (4-Carbamimido)4-benzyl) -2-methoxy-2-(3-mtxo-phen}d)-acetamide hydrochloride, (RS)-2-Biphenyi-4-yi-N-(4-carbamimidoyl-benzjd)-2-inethoxy-acetainide hydrochloride, (RS)-2-Benzo[l,3]dioxoI-5-yl-N-(4-carbaniiniidoyl-ben2yl)-2-methoxy-acetainide hydrochloride, (RS)-2-Benzo[13]dioxol-5-yl-N-{4-carbairiimidoyi-beiizyi)-2-ethoxy-acetarnide hydrochloride, (RS)-N-{4-Carbainiinido)4-ben2yl) -2 - [5-ethoxy-2-fluoro-3- (1 -methyi-piperidin-4-yioxy)- phenyl]-2-methosy-acetainide hydrochloride, (RS)-N-(4-CarbamirnidoyI-benzyI)-2-{2-fluorO'4-methoxy-pheii)d)-2-methoxy-acetaimde hydrochloride, (RS)-[Amino-(4-{[2-{2-fluoro-4-methoxy-phenyi}-2-methoxy-acet)dammo]-methyl}- phenyl)-methylenej-carbarDic acid ethyl ester, {RS)-2-(2-Huoro-4-methoxy-phenyl)-N-[4-(N-hydroxycarbainimidoyi)-benzyl]-2- methoxy-acetamide, RS)-2-(2-nuoro-4-metboxy-phenyl)-N- [4^(N-aminocarbamimidoyl)-benzyll -2-inethoxy- acetamide, (RS)-{5-[(4-Carbarniniidoyl-faeiiz}icarbarnoyl)-methory-inethyll-2-methoxy-pheiioxy}- acetic acid methyl ester hydrochloride, (RS)-N-(4-Carbamiinidoyi-benzyl)-2-{3-carbamoylmethoxy-4-roethoxy-phen)d)-2- methoxy-acetamide hydrochloride, (RS)-{5-[(4-Carbamiinidoyl-benzylcarbamoyl)-ethoxy-meth)d]-2-methoxy-phenoxy}- acetic add c\hyl ester hydrochloride, (RS)-N- (4-Carbaniimidoyl-benzyl) -2-{ 3-carbainoyimethoxy-4-methoxy-phenyl) -2- elhoxy-acetamide hydrochloride, (RS)-{5-[(4-Carbanii[mdoyI-benzy]carbamoyl)-ethoxy-methyl]-2-methoxy-phenoxy}- acetic acid, (RS)-N-(4-CarbainimidoyI'benzyi)-2-etho3cy-2-{4-ethoxy-phenyi)-acetaniid hydrochloride, (RS)-N-(4-Carbamimidoyl-benZ)d)-2-methoxy-2-[4-(l-methyl-piperidin-4-yIoxy)- phenylj-acetamide hydrochloride, (RS)-N-(4-Carbaraiinidoyl-benzjd)-3,3,3-trifluoro-2-metboxy-2-phenyi-propionainide hydrochloride, (RS)-N-(4-Carbaminiidoyl-benzyl)-2-{2-fluoro-4,5-dimethoxy-phenyi)-2-methoxy- acetamide hydrochloride, (RS)-N- (4-Carbaniiiiiidoyl-benz)'l) -2-{3-isopropox7-phenyl)-2 -methoxy-acetamide hydrochloride, (RS)-N- (4-Carbainimidoyi-benzyl) -2- (4-cyclopentyloxy-pheny3)-2-methoxy- acetamide hydrochloride, (RS)-N-(4-Caibamiinidoyl-benzyl) -2-(4-isopropoxy-phenj^) -2 -methoxy-acetamide hydrochloride, (RS)-i4-[(4-Carbainiinidoyi-ben2yicarbainoyl)-methoxy-niethyl]-phenoxy}-aceticadd meth)^ ester hydrochloride, (RS)-{4-E(4-Carbamimidoyl-beii2ylcarbamoyl)-metiioxy-inetiiyl]-phenoxy}-aceticacid, (RS)-N-(4-Carbaiiiimidoyl-benzyl)-2-methoxy-2-[3-(tetrahydro-pyran-4->doxy)-phenyl]- acetamide hydrochloride, (RS) -N- (4-Carbainiimdoyl-benzyl}-2- (3,5-diethoxy-2-fluoro-phenyl)-2-niethoxy- acetamide hydiocbioride, {RS)-N-(4-Carbaniiinidoyi-ben2yl)-2-[5-ethoxy-2-fluoro-4-(2-hydroxy-ethoxy)-phenyl]- 2-methoxy-acetamide hydrochloride, (RS}-N- (4-Carbainimidoyl-benzyl) -2- (3,4-diethoxy-2-fluoro-phenyl) -2-methoxy- acetamide hydrochloride, (RS) -N- (4-Cari)ainiimdoyl-2-fluoro-benzyl)-2- (2-fluoro-4-methoxy-phenyl)-2-methoxy- acetamide hydrochloride, (RS)-N-{4-Carbamiinido)d-3-fiuoro-benz)d)-2-{2-fluoro-4-methoxy-phenyi)-2-methoxy- acetamide hydrochloride, (RS)-2-(2,4-Bis-trifluoromethyl-phenyl)-N'(4-carbamiiuidoyI-benzjd)-2-methoxy- aceUmide hydrochloride, (RS)-N-[4-(N-Hydroxycarbainimido)d)-ben2yl]-2-(2-hydroxy-4-inethoxy-phenyl)-2- methoxy-acetamide, (RS)-N- (4-Carbaiiiiimdoyl-ben2yl) -2- (2-hydroxy-4-metJioxy-phen)i)-2-medioxy- acetamide actetate, (RS)-N-{4-Carbamimidoyl-ben2yl) -2- (2-fiuoro-5-niethoxy-phenyl) -2-methoxy-acetamide hydrochloride, (R.S)-N-(4-Carbaminiido)d-benzyl)-2-(2,3-difluoro-phenyl)-2-methoxy-acetamide hydrochloride, (RS)-N-(4-Carbaimniidoyl-benzyl)-2-(2,6-difiuoro-phenyl)-2-methoxy-acetaniide hydrochloride, (RS) -2- (4-Bromo-2-fluoro-phenyl) -N-(4-carbamiinidoyi-benzyl) -2-methoxy-acetamide hydrochloride, (RS)-2-(4-Bromo-2-fluoro-phenyl)-N-(4-carbarminidoj4-benz)d)-2-ethoxy-acetamide hydrochloride. (RS)-2- (4-Bromo-2-fluoro-phenyl) -N- (4-carbamiimdoyi-benzyI)~2-propoxy-acetaniide hydrochloride, (RS)-N- {4-CarbarDimidoyl-benzyI)-2- (2-fluoro-4-trifluoromethyl-phenyi) -2-methoxy-acetamide hydrochloride, (IlS)-]SI-(4'Carbamiinidoyl-benz)d)-2-[4-{2-hydroxy-ethoxy)-phenyI]-2-methoxy-acetamide hydrochloride, (RS )-N-{4-Carbamimidoyl-benzyl) -2 - (4-diinethyIainino-phenyl)-2-methoxy-acetainLde hxdrochloride, (RS) -N- (4-Carbamiimdoyl-benzyI) -2-methoxy'2- (3 -oxo-3,4-dihydro-2H- benzo[l,4]oxa2in-6-yI)-acetamide hydrochloride, (RS)-N- (4-Carbamimidoyl-benzyi)-2 -methoxy-2- (4-pyiTolidin-1 -yl-phenyl)-acetainide hydrochloride, (RS) -N-(4-Carbainiinidoyl-benzyl)-2- (2-chIoro-phenyl)-2-methoxy-acetaniide hydrochloride, (RS)-2--(4-Acetylamino-phenyl)-N-(4-carbamimidoyI-benzyI}-2-rnethoxy-acetainide hydrochloride, (RS )-N' (4-Carbaniiinidoyl-benzj^)-2-mefhoxy-2-(4-trifluoromethoiy-pheiiyl)-acetainide hydrochloride, (RS)-N-(4-Carbamimidoyl-benz)^)-2-(4-imidazol-1 -yl-phenyl)-2-methoxy-acetainide hydrochloride, (RS)-N-(4-Carbamiinidoyi-benzyI)-2-methoxy-2-(6--methoxy-naphthalen-2-yl)-acetaniide hydrochloride, (RS)-N-(4-Carbamiinidoyl-benzyi)-2-methoxy-2-(4-morphoiin-4-yl-phenyl)-acetamide hydrochloride, (RS) -N-(4-Carbamiinidoyl-benzyl)-2-methoxy-2-(2-morpholiii-4-yl-phenyI)-acetamide hydrochloride, (RS)-N-(4-Carbainimidoyl-benzyI)-2-[4-(3-dimethylaniiBo-propoxy)-phenyl]-2- methoxy-acetamide hydrochloride, {R5)-N-(4-Carbainiinidoyl-beii2yl)-2-(4'-dinieth)^amiiio--3--fluoro-biphenyi-4-yi)-2- methoxy-acetamide hydrochloride, (RS)-N-(4-CarbamiimdoyI-beii2yl)-2-(3-£Iuoro-4'-methoxy-biphenyl-4-yi)-2-methoxy- acetamide hydrochloride, (RS) -N-(4-Carbamimidoyl-benzyl)-2 - (3-fluoro-2'-metho3cy-biphenyI-4-yi)-2-methoxy- acetamide hydrochloride, (RS)-N-(4-Carbammiidoyl-benz)4) -2-(3-fluoro-biphen}d-4-^) -2-methoxy-acetamide hydrochloride, (RS) -N-{4-CarbainimidoyI-beiizyl}-2- (3-fluoro-3 '-methoxy-biphenyl-4-yI) -2-raethoxy- acetamide hydrochloride, I (RS )-N-(4-CarbamimidoyI-ben2yi)-2-(2,2-diinethyI-ciiromaii-6-yl)-2-methoxy-acetamide hydrochloride, (RS)-N-{4-CarbamiinidoyI-beiizyl)-2-ethoxy-2-(2-fiuoro-4-methoxy-pheii)^)-acetamide hydrochloride, {RS)-2-Ethoxy-2-(2-fluoro-4-methoxy-plienyl)-N-[4-(N--hydroxycarbamimidoyl)-benzyl] -acetamide, (RS)-4-[3-(3-Cyclopent>doxy-4-inethoxy-phenyl)-3-methoxy-2-oxo-prop^ainino]-benzamidine hydrochloride, {RS)-N-(4-CarbaiiiiimdoyI-benzyI}-2-C2-chloro-4-methoxy-phenyl)-2-methoxy-acetainide hydrochloride, (RS) -N- (4-Carbainimido)d-benzyl)-2-(2,6-difluoro-4-met±ioxy-phenyl)-2-methoxy- acetamide hydrochloride, (RS) -N- (4-CarbainimidoyI-benzyI )-2- (2'fluoro-4-methoxy-phen)^) -2-propoxy-acetamide hydrochloride, (RS)-N-(4-Carbaniimidoyl-benzy!)-2-methoxy-2-naphthaleii-l-yl-propionamide hydrochloride, (RS) -2- (4-Bromo- 2,6-difluoro-phen.yl) -N- (4-carbamimidoyl-ben2yl)-2-iuethQxy- acetamide hydrochloride, (RS)-N[-(4-Carbamiinido^-benzyl)-2-(2-fluoro-4-isopropoxy-phenyl)-2-metho}!y- acetamide hydrochloride, (RS)-N-(4^Carbamimidoyl-ben2yl) - 2-(2-fiuoro-4-isobu.toxy-pbenyl)-2-methoxy- acetamide hydrochloride, (RS)-N-(4-Carbainiimdoyl-beiizyl)-2-{2-fluoio-4-[2-(4-fluoro-phenyl)-ethoxy]-phenyl}- 2-methoxy-acetaniide hydrochloride, (RS) -N-(4-CaTbamimidoyl-ben2yl)-2- (2-fluDTD-4-pyridiii-3-^-phenyl)-2-mellioxy- acetamide hydrochloride, (RS) 'N-(4-Carbamiinido)^-benz)^) -2-(2-fluoro-4-pyridin-4-yl-piienyl)-2-metlioxy- acetamide hydrochloride, (RS)-2-(5-Bromo-2-fluoro-phenyl)-N-(4-carbamimido)d-ben2yl)--2-ineihoxy-acetamide hydrochloride, (RS)-N-(4-Carbamiinidoyi'ben2yl)-2-(4-fluoro-biphenyl-3-yi)-2-methoxy-3cetainide hydrochloride, (RS)-N-(4-Carbainiinidoyi'benzyl)-2-(2-fluoro-5-methyl-phenyi)-2-methoxy'acetaimde hydrochloride, (RS)-N- (4-Carbanumidoyi'ben2yl) -2 -(2-fluoro-5-trifiuoromethyl-phenyl)-2-metiioxy- acetamide hydrochloride, (RS)-N-(4-Carbamimidojd-benzyl)-2 - (2-fluoro-6-methoxy-phenyi) -2-methoxy-acetamide hydrochloride. CRS}-N-(4-Carbaminiidoyl-benzyi)-2 - (2-fluoro-6-liydroxy-phenyl)-2 -methoxy-acetamide hydrochloride, {RS)-N-(4-Carbaimmidoyl-benzyI)-2-diinethylainino-2-phenyI-acetamide hydrochloride, (RS)-N-(4-Carbaniimidoyl-beiizyi)-2-methyiamino-2-phenyl-acetamide hydrochloride, (RS)-N-(4-Carbamiimdo}d-ben2fl)-2-methylsulfanyl~2-phenyl-acetamide hydrochloride, (RS)-N-(4-Carbarnimidoyl-beiizyi)-2-ethyIsulfenyl-2-phenyl-acetainide hydrochloride, [RS)-N-(4-Carbamiinido)d-benzyl)-2-melhanesiilfonyl-2-phenyl-acetainide hydrochloride, (RS)-2-Amino-N-(4-carbaiminidoyl-benzyl)-2-phenyl-acetaniidehydiochIoride, (RS}-2-Acet7lamino-N-(4-carbainiinidoyl-ben27l)-2-phenyl-acetamide hydrochloride, (RS)-N-(4-Carbamiimdoyl-benzyl)-2-[2-fluoro-4-(2-phenoxy-ethoxy)-phenyll-2- methoxy-acetamide hydrochloride, (RS)-N-(4-Carbamimido>^-benz)d)-2-methoxy-2-pyridiii-2-jd-acetamide hydrochloride, (RS)-N-(4-Carbaminiidoyl-benzyl)-2-niethoxy-2-phenyl-propionaiiiide hydrochloride, (RS)-2-(4-Broiiio-2,6-difluoro-phenyl)-N-(4-carbaimniidoyi-benzyl)-2-ethoxy-acetamide hydrochloride, N-(4-CarbainiinidoyI-benzyl)-2-[2-fluoro-6-(2-hydroxy-ethoxy}-phenyl]-2-methoxy- acetamide hydrodiloride, and N-(4-Carbanuimdoyl-benzyi)-2-(2-carbamoylmethoxy-6-fluoro-pheDyl)-2-methoxy- acetamide hydrochloride, and pharmaceutically acceptable salts thereof. Other preferred compounds of formula (I) are those selected from the group consisting of (RS)-2-Biphenyi-4-)d-N-(4-carbamimidoyl-benzyl)-2-ethoxy-propionanude hydrochloride, (RS)-2-[3-(l-Benzenesulfonyl-piperidm-4-yloxy)-5-ethoxy-2-fluoTO-pfaenyl]-N-(4- carbamimidoyl-benzyl)-2-methoxy-acetainide hydrochloride, (RS)-N-(4-Garbamimidoyl-ben2yl)-2- [ 5-ethosy'2-fluoro-3-(l-metfaanesulfonyl-piperidin-4-)^oiy)-phenyl] -2-methoxy-acetamide hydrochloride, (RS)-2-[3-Cl-Acetyl-piperidin-4-)^oxy)-5-ethoxy-2-fluoro-phenyl]-N-(4-carbamimidoyi- benz)d)-2-methoxy-acetamide hydrochloride, (RS)-2-[3-(l-Benzoyi-piperidin-4-yloxy)-5-ethoxy-2-fluoro-phenyl]-N-(4- carbaminiidoyl-benzyl)-2-methoxy-acetamide hydrochloride, (RS)-N-(4-Carbamimidoyl-2-chloro-ben2yl)-2-{2-fluoro-4-methoxy-phenyi)-2-inethoxy' acetamide hydrochloride, (RS) -N-(4-CarbaminiidoyI-2-chIoro-ben2yl)-2 -ethoxy-2- (2-fluoro-4-methoxy-phen)i)- acetamide hydrochloride. (RS)'N-(4-CarbamiinidoyI-2-chloro-benzyl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-etiaoxy-acetamide hydrodiloride, {RS )-N- (4-CarbamimidoyI-2-chloro-benzyI) -2 -{2,6-diguoro-4-methoxy-phenyl) -2-methoxy-acetamide hydrochloride, (RS)-N-[3-Chloro-4-(N-hydroxycaibamimidoyl)-benzyl]-2-ethoxy-2-(2-fiuoro-4-methoxy-phenyl) -acetamide, (RS)-N-(4-Carbamiinidoyl-3-chloro-berizyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl) -acetamide acetate, (RS)-2 - (4-Bromo-2,6-difluoro-phenyl)-N- C4-carbamiinidoyl-2-methoxy-benzyi)-2- ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbaniimidoyl-2-methoxy-beiizyl)-2-e&oxy-2-(2-fluoro-4-methoxy-phenyi}- acetamide hydrochloride, (RS )-N- (4-CarbamirmdoyI-2-phenoxy-benzyI) -2-ethoxy-2-(2-fluoro-4-methoxy-phen)d) - acetamide hydrochloride, (RS)-N-(4-Carbamunidoy]-2-o-tolyIoxy-benzyl)-2-ethoxy-2-(2-fluoro-4-methoxy- phenji)-acetamide hydrochloride, {RS)-N-[4-Carbainiinidoyl-2-{4-fiuoro-phenoxy)-beiizyi]-2-ethoxy-2-{2-fluoro-4- methoxy-phenyl)-acetamide hydrochloride, (RS )-N- [4-Carbamimido}d-2-{pyridin-3-)doxy) -benzyl] -2-ethoxy-2- (2-fIuoro-4-methoxy- phenyl)-acetamide acetic add, (RS)-N-[4-Carbamimidoyl-2-(5-nitro-pyridin-2-yioxy)-benzyI]-2-ethoxy-2-(2-fluoro-4- methoxy-phenjd)-acetamide hydrochloride, (RS)-N-[2-(5-Amino-pyridin-2-yloxy)-4-carbamimidoyi-beii2)d]-2-ethoxy-2-(2-fluoro-4- methoxy-phenyI)-acetamide hydrochloride, (RS) -N-(5-Carbamimidoyl-biphenyl-2-ylmeth)d)-2-€thoxy-2- (2-fiuoro-4-methoxy- phen)4)-acetamide hydrochloride, (RS)-(5-Carbamimidoyl-2-{[2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetylamino]- methyl}-phenoxy)-acetic acid ethyl ester hydrochloride 1:1, (RS) -N- (4-Carbamimidoyl-2-carbamoyhnethoxy-ben2yl)-2-ethoxy-2-(2-fluoro-4- methoxy-phenyl)-acetamide hydrochloride 1:1, (RS}-N- (4-Carbamimidoyi-2-isopropoxy-benzyl) -2-ethoxy-2-(2-fluoro-4-methoxy- phenyl)-acetamide hydrochloride, (RS)-N-[4-Carbamimidoyl-2-(2-hydroxy-ethoxy)-beiizyl]-2-ethoxy-2-(2-fluoro-4- methoxy-phenyI)-acetainide hydrochloride, 2-{5-Carbamimidoyl-2-{[2-ethoxy-2-(2-fluoro-4-methoxy-phen)d)-acet>damino]-methyl}-phenoxy)-N-isopropyi-2-phenyl-acetamide hydrochloride, (RS)-(5-Carbamii]iido)d-2-{[2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetylamino]-methyl}-phenoKy)-acetic add. (IlS)-(S)-2-(5-Carbainiiiudoyi'2-{[2-ethoxy-2-(2-fluoro-4-meTiioxy-phenyl)-acetyiamino]-methyl }-phenoxy)-propionic acid ethyl ester hydrochloride, ((RS)-S)-2-C5-CarbaminiidoyI-2-{[2-ethoxy-2-(2-fluoro-4-methoxy-phenyI)-acet)'lamiiio]-methyi}-phenoxy)-propionaiiude hydrochloride, (RS)-{R)-2-(5-Carbamiinidoyl-2-[[2-ethoxy-2-(2-fluoTO-4-methoxy-phenyl)-acetylamino]-methyl}-phenoxy)-propiomc add ethyl ester hydrochloride, (RS)-(R)-2-(5-Carbamimidoyl-2-{[2-ethoxy-2-(2-fluoro-4-methoxj'-phenyl)-acetylamino] -methyl}-phenoxy)-propionamide hydrochloride, (RS)-N- (4-Carbainimidoyi-2-carbamoylmethoxy-benzyl)-2- (2-fluoro-4-Inethox)^-phenyI)-2-methoxy-acetaraidehyd^ochIoride, (RS)-N-(4-Carbainiinidoyl-2-phenoxy-beiizyi)-2- (2,6-difluoro-4-methoxy'pheii}^) -2-ethoxy-acetamide hydrochloride, (RS) -N- (4-Carbainiinidoyl-2-methoxy-ben2yl) -2- (2,6-difluoro-4-methoxy-phenyi) -2-ethoxy-acetamide hydrochloride, {RS)-N-{4-Carbamimidoyl-2-carbamoylmethoxy-benzyl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide hydrodiloride, (RS)-N-[4-Carbainiinidoyi-2-(2-fluoro-beiizyloxy)-benzyl]-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide hydrochloride, (RS)-N-[4-Carbamiiiiido)d-2-(5-chloro-2-fluoro-benz)4oxy)-benzyl]-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide hydrochloride, (RS}-N-{4-CarbamiimdoyI-2-[(2-methoxy-ethyicarbamoyl)-methoxy]-benzyi}-2-{2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetainide hydrochloride, (RS)-N-{ 4-Carbainimidoyl-2- [ (2-morpholin-4-yl-ethylcaibainoyl)-nietho3cy] -benzy!} -2-(2,6-difluoro-4-methoxy-pbenyI)-2-ethoxy-acetamide hydrochloride, (RS)-N-{4-Carbamimidoyl-2-[{2-diethyIainmo-ethylcarbainoyl)-metboxy]-ben2}i}-2-(2,6-difluoro-4-niethoxy-phenyi)-2-ethoxy-acetamide hydrochloride, (RS}-N-[4-Carbarmmidoyl-2-C[l,2,4]oxadiazol-3-ybnethoxy)-benzyl]-2-(2,6-difluoro-4- methoxy-phenyl}-2-ethoxy-acetarmde hydrochloride, (RS)-N-C4-Carbaniiinidoyl-2-carbamimido)dinethoxy-benzyl)-2-(2,6-difiuoro-4-methcixy-phenyl)-2-ethoxy-acetainidehydiochloride, (RS)-N-[2-{lH-Benzoiniida2ol-2-yhnethoxy)-4-carbamiimdoyl-benz)d]-2-(2,6-difluoro-4-niethoxy-phenyl}-2-ethoxy-acetamide hydrochloride, (RS)-N-[4-Carbamiimdoyl-2-((lS,3R,4S)-3,4-dihydroxy-cydopentyioxy)-beiizyl]-2-(2,6-difluoro-4-methosy-phenyl)-2-ethoxy-acetamide hydrochloride, amiitureof (RS) and (SR)-N-[4-Carbamimidoyl-2-((lRS,2RS)-2-hydroxy' cyclopentyloxy) -benzyl] -2- (2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetainide hydrochloride, (RS)-N-(4-Carbainiinidoyi-2-carbamoylmethoxy-benzyi)-2-(2,6-difiuoro-4-methoxy- pheiiyI)-2-methosy-acetamide hydrochloride, (RS)-N-(4-Carbaniimidoyl-2-methylcarbamoyImethoxy-beiizjd)-2-(2,6-difluoro-4- methosy-phenyl)-2-methoxy-acetainide hydrochloride, (RS)-N-[4-Carbamiinidoyl-2-(isopropylcarbanioyl-methoxy)-ben2yl]-2-(2,6-difluoro-4- methoxy-phenyI)-2-methoxy-acetainide hydrochloride, (RS)-N-{4-Carbaniimidoyl-2-[(4-fluoro-phenylcarbanioyI)-methoxy]-ben2yl}-2-(2,6- difluoro-4-methoxy-phenyl)-2-methoxy-acetaniide hydrochloride, (RS)-N-[4-Carbamimido)d-2-(pyridm-2-ylmethoxy)-beii2)d]-2-(2,6-difluoro-4-methoxy- phenyl)-2-rQethoxy-acetaimde hydrochloride, (RS)-N-[4-Carbaiminidoyl-2-(2,2J-trifluoro-ethoxy)-benz)i]-2-(2,6-(Muoro-4- methoxy-phenyi)-2-inethoxy-acetamide hydrochloride, (RS)-N- [4- Carbamiimdo)d-2 - (pyridin-3 -^methoxy)-benzyl] -2- (2,6-difluoro-4-methoxy- phenyl)-2-metiiojty-acetainide hydrochloride, (RS)-N-[4-Carbamin2idoyl-2-{pyridin-4-ylmethoxy)-benzyl]-2-(2,6-difluoro-4-methoxy- phenyl}-2-methoxy-acetamide hydrochloride, (RS) -N- (4-Carbamimidoyi-benz)d) -2-(2,6-difluoro-4-hydroxy-phenyl) -2-ethoxy- acetainide hydrochloride, (RS)-N-(4-Carbamimidoyi-benz)d)-2-[2,6-difluoro-4-C2-morpholm-4-yl-ethoxy)-phenyi]- 2-ethoxy-acetarmde dihydrochloride, (RS)-{[4-({2-[2,6-Difluoro-4-(2-morphoIin-4-)d-etiioxy)--phenyl]-2-ethoxy-acetylaimno}- metiiyl)-phenyl]-imino-methyl}-carbainic add benzyl ester> (RS)-N-{4-Carbainimidoyi-benz)d)-2- C2,6-difluoro-4-phenethyloxy-phenyi) -2-ethoxy- acetamide hydrochJoride, (RS)-N-(4-Carbainiiiiidoyi-benz)4)-2-(4-cydopTOp)dmethoxy-2,6-difluoro-pbenyl)-2- ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbaniiinidoyi-benzyl)-2-ethoxy-2-(4-ethoxy-2,6-difluoro-phenyl)-acetamide hydrochloride, (RS)-N-C4-Carbainimidoyl-ben2:>i)-2-[2,6-difluoro-4-(4-methoxy-phenoxy)-phenyl]-2- ethoxy-acetamide, (RS)-N-{4-CarbamiinidoyI-benzyl)-2-[4-(3,4-dimethoxy-phenoxy)-2,6-difluoro-pbenyl]- 2-ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbaminiidoyl-benz)i)-2-[2,6-difIuoro-4-{3-inethoxy-phenoxy)-phenyl]-2- ethory-acetamide hydrochloride, (RS)-2- [4-(3 -Acetylamino-phenoxy) -2,6-difluoro-phenyl] -N-(4-carbainimido)d-benzyl) - 2-etlioxy-acetamide hydrochloride, (RS)-N-{ 4-CarbainimidoyI-beiiz}d)-2 - [4-(4-cyano-phenoxy)-2,6-difluDro-phen)d]-2- ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbamiinido)d-beii2}d)-2- [2,6-difiuoro-4-( 3-trifliaoTomethoxy-plienoxy)- phenyl]-2-ethoxy-acetainideh7drochJoride, (RS)-(2,6-DifIuoro-4-trifluoromethanesulfonyloxy-phenyl)-ethosy-acetic acid ethyl ester, (RS)-4-(Ethoxy-ethQKycarbonyl-inethyl)-3,5-di£luoro-benzoicacid2-tiimeth.ylsUaiiyl-ethyl ester, (RS)-4-[(4-Carbamiinidoyi-benzylcarbamoyl)-ethoxy-metiiyl]-3,5-difluoTO-N-isobntyl- benzamide hydrochloride, (RS)-4-[(4-Carbamimido)^-benzylcarbaino)d)-ethoxy-me&yl]-N-ethyl-3,5-difluoro- benzamide hydrochloride, (RS)-4-[(4-Carbamimidoyl-benzylcarbamoyl)-ethoxy-methyl]-3,5-difluoro-N-(2- methoxy-ethyI)-beiizaiiude hydrochloride, (RS)-4- [ C4-Carbamiinidoyl-benzylcarbainoyl)-ethoxy-meth)d] -N-cyclopentyl-3,5- difluoro-benzamide hydrochloride, (RS)-4-[(4-CarbamiinidoyI-ben2ylcarbamoyl)-ethoxy-methyl]-3,5-difiuoro-N-(2,2,2- trifluoro-ethyl)-benzamide hydrochloride, (RS)-4-[(4-Carbainiimdoyl-benzylcarbamoyI)-ethoxy-methyl]-N-cyclopropylmethyi-3,5- difluoro-benzamide hydrochloride, (RS)-[(4-{[2-(2,6-Difluoro-3-hydrox)'-phenyl)-2-ethoxy-acetylainino]-meth}d}-phenyl)- imino-methyl]-carbamic acid benzyl ester, (RS)-N-(4-Carbaiiiiinido)d-benzyl)-2-(2,6-difluoro-3-hydroxy-phenyi)-2-ethoxy- aceUmide hydrochloride, (RS)-N-(4-CarbamiimdoyI-benzyl)-2-ethoxy-2-{3-[2-(2-ethoxy-ethoxy)-ethoxy]-2,6- difluoio-phenyl}-acetainide hydrochloride, (RS)-N-{4-Carbainiinidoyl-benzyi)-2-[3-(3-dimeth)darnino-propoxy)-2,6-dif[uoro- phenyl]-2-ethoxy-acetaniide dihydrochloride, (RS)-N-(4-Carb3niiniido)d-ben2yl)-2-(2,6-difluoro-3-{2-[2-(2-methoxy-ethoxy)-ethoxy]- ethoxy}-phenyl)-2-ethoxy-acet3mide hydrochloride, (RS)-N-(4-Carbaiiiimido)d-benzyl)-2-[2,6-difluoro-3-C3-pyridin-4-yI-propoxy)-phen>d]- 2-ethoxy-acetaniide dihydrochloride, (RS)-N-C4-Carbamiinido}4-benzyI)-2-[2,6-difluoro-3-(2-pyrroIidiii-1-yl-ethoxy)-phenyl]- 2-ethoxy-acetamide dihydrochloride, {RS)-N-(4-Carbaininiidoyl-benzyl)-2-[2,6-difluoro-3-(l-inethyI-cyclopropylmethoxy)- phen>d]~2-ethoxy-acetaniide hydrochloride, (RS)-N-{4-CarbamimidoyI-benzyl)-2-[2,6-dif[uoro-3-(2-piperidin'l-yl-ethoxy)-phenyl]- 2-ethoxy-acetaiiude dihydrochloride, (RS,RS)-N-C4-Carbamiinidoyl-ben2yl)-2-[3-(3-chloro-2-hydroxyinethyl-2-methyl- propoxy)-2,6-difiuoro-phenyi]-2-ethoxy-acetainide hydrochloride, (RS) -N-(4-Carbainirmdoyl-benzyl)-2-ethQxy-2-13- (2-ethoxy-ethoxy)-2,6-difluoro - phenyl]-acetamide hydrochloride. (RS)-N-(4-Carbamimidoyl-benzyl)-2-[2,6-di3uoro-3-(2-methoxf-ethoxy)-phenyl]-2- ethoxy-acetamide hydrochloride, (RS)-N-(4-Carfaaniiinidoyl-benzyi)-2-[3-(3-dimethylamino-2^-diinethyl-propoxy)-2,6- difIuoro-phenyl]-2-ethoxy-acetaroidedihydrochloride, (RS)-N-(4-Carbaniiniidoyl-ben2yl)-2-[2,6-difluoro-3-(2-thiophen-2-yl-ethoxy)-phenyi]- 2-eihoxy-acetamide hydrochloride, (IIS,RS)-N- (4-Carbamiinidoyl-benzyl) -2- [2,6- di&uoro-3- (tetrahydro-ftiran-2-ylinetiioxy) - phenyl]-2-ethosy-acetainide hydrochloride, (RS)-N- (4-CaTbamimidoyl-benzyi)-2- (2,6-difluoro-3-isobutoxy-phenyl)-2-etlioxy- acetamide hydrochloride, (RS,RS,RS)-N-{4-Carbainimidoyl-benzyl)-2-[2,6-difiuoro-3-(2-inethyl- cyclopropyhnethoxy)-phenyl] -2-ethoxy-acetainide hydrochloride, (RS)-N-{4-Carbamimidoyi-ben2yl)-2-[3-(2-cydopropyl-ethoxy)-2,6-difluoro-phenyl]-2- ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbainiinidoyl-ben2yl)-2-etiioxy-2-(3-ethoxy-2,6-difluoro-phen5d)-acetanude hydrochloride, (RS)-N-(4-Carbaminiidoyi-benzyl)-2-(2,6-difluoro-3-propoxy-phenyl)-2-ethoxy- acetamide hydrochloride, (RS)-N-(4-Carbamimidoyl-benz34}-2-(3-cycloprop)dmethoxy-2,6-difiuoro-phenyl)-2- ethoxy-acetamide hydrochloride, (RS) -N- (4-Carbainimido)d-ben2yl)-2- [ 3- (2-diniethyiamino-ethoxy)-2,6-difluoro-phenyl] - 2-ethoxy-acetarDide dihydrochloride, (RS)-N-(4-Carbainiinidoyl-benzyl)-2-{3-cydobut)dinethoxy-2,6-difluoro-phen)d)'2- ethoxy-acetamide hydrochloride, (RS)-N-(4-CarbamirQidoyl-ben2)d)-2-{2,6-difluoro-3-[2-(2-oxo-pyrrolidin-l-yl)-ethoxy]- phenyi}-2-ethoxy-acetainide hydrochloride, (RS)-N-(4-Carbamimido)^-benzyi}-2-[2,6-difluoro-3-(3,3,3-Qifiuoro-propoxy}-phenyl]- 2-ethoxy-acetainide hydrochloride, (RS)-N-(4-Caibamiimdo)d-benzyi)-2-[2,6-difluoro-3-(2-pyridm-3-yi-ethoxy)-phenyl]-2- ethoxy-acetamide dihydrochloride, (RS)-N-(4-CarbamimidoyI-benzyi)-2-(3-diethylcarbanioylmethoxy-2,6-difluoro-phenyl)- 2-ethoxy-acetainide hydrochloride, [RS)-N-(4-Carbamiimdoyl-benzyl)-2-[2,6-difluoro-3-(2-morpholJn-4-yl-ethoxy)-phenjd]- 2-edioxy-acetamide dihydrochloride, (RS,RS)-N-(4-Carbamiinidoyl-benzyl)-2-[2,6-difluoro-3-(l-methyl-piperidiji-3- ylmethoxy)-phenyl]-2-ethoxy-acetamide dihydrochloride, (RS JlS}-N-(4-CarbamimidoyI-benz)d)-2-[2,6-difluoro-3-{ 1-niethyl-piperidin-2- )dinethoxy)-phenyl]-2-ethoxy-acetainide dihydrochloride. CRS)-N-C4-Carbainimidoyi-benzyi)-2-[2,6-dJfluoro-3-(2-pyridin-2-yl-ethoxy')-phenyl]-2- ethoxf-acetamide dihydrochloride, {RSJlS)-N-C4-Carbaiminido)^-benzyI)-2-[2,6-difIuoro-3-(2-piperiain-2'yl-ethoxy)- phenyl]-2-ethoxy-acet3mide dihydrochloride, (RS)-N-(4-Carbaniiimdoyl-beiizyl)-2-(2,6-difluoro-3-methoxy-phenyl)-2-ethoxy- acetainide hydrochloride, (RS) -N- (4-Carbamimidoyl-ben2^)-2-(3-cydohexyloxy-Z,6-difluoro-phenyl) -2-etfaoxy- acetamide hydrochloride, (RS)-N-{4-Carbainimidoyl-benzyi)-2-[2,6-difluoro-3-(piperidin-4-yloxy)-phenyl]-2- ethoxy-acetamide dihydrochloride, (R,S) -N-(4-Carbaniiimdoyl-benzyl)-2 - [2,6-difiuoro-3-(4-fliioro-phenoxy)-phenyl] -2- ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbamiimdoyl-beii2yl)-2-[2,6-difluoro-3-(pyridin-3-')4oxy)-phenyll-2-ethoxy- acetamide dihydrochloride, (RS)-N-{4-Carbainimidoyl-benzyl)-2-[2,6-difluoro-3-{3-trifluoromethyl-phenoxy)- phenyl] -2-ethoxy-acetaniide hydrochloride, (RS) -N-(4-Carbamiinidoyl-beiiz)i) -2-(2,6-difluoro-3-m-tolyioxy-phenyl) -2-ethoxy- acetamide hydrochloride, (RS)-N-(4-Carbamiimdoyl-ben2yi)-2-ethQxy-2-[3-(3-ethoxy-phenoxy)-2,6-difluoro- phen)1]-acetamide hydrochloride, (RS)-N-(4-Carbainimidoyl-benzyl)-2-ethoxy-2-[3-{ l-ethyl-propoxy)-2,6-difluoro- phenyl]-acetamide acetate, (RS)-N-(4-Carbamimido^-benzyl)-2-(3-cydopentyloxy-2,6-dif[uoro-phen}^)-2-ethoxy- acetamide acetate, {RS)-N-(4-Carbainimidoyl-benzyi)-2-[2,6-difluoro-3-(tetrahydro-pyran-4-yioxy)- pIienyl]-2-ethoxy-acetamide acetate, (RS)-N-(4-Carbamimidoyl-beiiz)d)-2-(2,6-difiuoro-3-pyridin-2-)^-phen)d)-2-ethoKy' acetamide dihydrochloride, (RS)-N-(4-Carbamimido)i-beiiz^)-2-[2,6-difl.uoro-3-(6-methoxy-pyridin-3-yl)-pheti^]- 2-ethoxy-acetamide dihydrochloride, (RS)-N- (4-Carbamimidoyl-benzyI) -2- (2,6-difIuoro-5-pyridin-3-yl-phenyi)-2-ethoxy- aceUmide dihydrochloride, CRS)-N- (4-Carbamimidoyl-benzyi) -2 -{2,6-difluoro-3-pyrimidin-5-yl-phenyl)-2'ethoxy- acetamide dihydrochloride, (RS)-N-(4-Carbamiinidoyl-ben!yl)-2- (2,6-difiuoro- 3-pyridin-4-yI-phenyl)-2-ethoxy- acetamide dihydrochloride, (RS) -N-(4-Carbamimidoyl-benzyl) -2 -(2,4-difluoro-3'-methyl-biphenyl-3 -yl)-2-methox7- acetamide. (RS) -N- (4-Carbainimido}d-ben2yl)-2-( 2,4-difluoro-4'-methyi-biphenyl-3-)^}-2-methoxy- acetamide hydrochloride, (RS)-N-(4-Carbaininiido7l-beii2yl)-2-methoxy-2-(2,4,4'-trifluoro-bipiienyI-3-}d)- acetamide acetate, (RS) -N-(4-CaTbamiimdDyl-beiizyl) -2-(2,4-difluoro-4' -methylsulfanyi-biphenyl-3-yi) -2- methoxy-acetamide hydrochloride, CRS)-N-{4-Carbamiinidoyl-benzyl)-2-(2,4-difIuoro-3'-trifluoromethyl-biphenyI-3-yl)-2- methoxy-acetamide acetate, (RS) -N- (4-CarbamimidoyI-beiizyI) -2- (2,4-difluoro-4'-methoxy-biphen)d-3-yl) -2- methoxy-acetamide hydrochloride, (RS)-N-(4-Carbamiiiiidoyl-benzyi)-2-[2,6-difluoro-3-(morphohne-4-carbon)i)-phenjd]- 2-methoxy-acetamide acetate, (RS)-2-[2,6-difluoro-3-(morpholine-4-caibonyl)-phenyl j-N-[4-(N- hydrQxycarbamiinidQ^)-ben2yl] -2-methoxy-acetanude, CRS)-3- [ (4-Carb3niimidoyl-ben2ylcarbamoyl)-methoxy-methyl] -N-eth)4-2,4-difIuoro- benzamide acetate, (RS)-3-[(4-Carbamimido)i-beiizylcarbaino)^)-methoxy-methyl]-2,4-dif[uoro-N-(2- inethoxy-ethyI)-ben2aniide acetate, (RS)-3-[{4-Carbainiinidoyl-benzj^carbamoyi)-methoxy-meth)d]-N,N-diethyi-2,4- difluoro-benzajnide acetate, (RS)-3-[(4-CaTbainiinidoyl-benz^caibamoyl)-metiioxy-methyi]-2,4-difiuoTO~N-(2,2,2- trifluoro-ethyI)-benzamide acetate, (RS)-3-[(4-Carbamimido7i-ben2yicarbaino}d)-methoxy-methyl]-N-cyclopropyimethyl- 2,4-difluoro-benzainide acetate, (RS)-N- (4-Carbamimidojd-benz)^)-2- [2,6-difiuoro-3-(pyridin-2-yimethoxy) -phenyl] - 2- methoxy-acetamide dihydrochloride, (RS)-N-(4-Carbamimidoyl-benzyl)-2-[2,6-difluoro-3-(pyridm-3-)dmethoxy)-phen)d]-2- tnedioxy-acetamide dihydrochloride, (RS)-N-(4-Carbamiinidoyl-ben2yl)-2-[2,6-difluoro-3-(pyridin-4-ylmethoxy)-phenyi]-2- methoxy-acetamide dihydrochloride, (RS) -N- (4-Carbainimidoyl-benzyl) -2- [2,6-difluoro-3- (4-fluoro-phenoxy)-phenyi] -2- methoxy-acetamide acetate, (RS)-2-[2,6-difluoro-3-(4-fluoro-phenoxy)-phenyi]-N-[4-(N-hydroxycarbainiraidoyl)- beiiz)d] -2-methoxy-acetanude, (RS)-N-(4-Carbamimidoyi-benzyl)-2-[2,6-difluoro-3-(pyridin-3-yloxy)-plienyl]-2- methoxy-acetamide acetate, (RS}-N- (4-Carbaniimidoyl-beii2yl)-2- (3 ^-difluoro-biphen^-4-yl)-2-methoxy-acetamide hydrochloride. (RS) -N- (4-Carbamimidoyl-ben2yl)--2- (3,5-difluoro-biphenyi-4-yl)-2-ethox)'-acetamide hydrochloride, (RS)-N-(4-Carbamimidoyl-benzyl)-2-[2,6-difluoro-4-(lH-indol-5-yi)-phen)d]-2-ethoxy-acetamide acetic acid, (RS}-2~(2,6-Difluoro-4-furan-2-yl-phenyl)-2-ethoxy-N-[4-(N-hydroxycarbainimidoyl)-benzyl] -acetamide, (RS)-N-(4-Carbamimidoyi-benzyl)-2 - (2,6-difluoro-4-furan-2-yi-phenyl)-2-ethoxy-acetamide acetate, N-(4-Carbamimidoyl-benzyl)-2-[2,6-difluoro-4-(tetrahydro-furan-2-yI)-phen)d]-2-ethoxy-acetamide acetic acid, (RS)-J4'-[(4-Carbamimidoyl-ben2ylcarbamoyl)-ethoxy-methyl]-3',5'-difluoro-biphenyl-3-yloxy}-acetic add ethyl ester hydrochloride, (RS )-{4'- [ (4-Carbamimidoyl-benzylcarbamo}d) -etboxy-methyl] -3',5 '-difluoro-biphenyl-3-yloxf}-acetic add, (RS)-N-(4-Carb amiimdoyI-benz)4)-2-(3'-carbamoylmethoxy-3,5-difluoro-biphenyl-4-)i)-2-ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbainiinidoyl-benzyI)-2-[3,5-difluoro-3'-(2-hydroxy-ethoxy)-bipheiiyl~4-yl]-2-ethoxy-acetainide hydrochloride, (RS)-N-(4-Carbamiinido)d-ben2)d)-2-[3'-(3-dimethylaiiiino-propoxy)-3,5-difluoro-biphenyl-4-yl] -2-ethoxy-acetamide hydrochloride, (RS)-2-[2'-(2-Benzyloxy-ethoxy)-3,5-difluoro-biphenyl-4-)^l-N-(4-carbamimidoyl-benZ)^)-2-ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbamimidoyl-benz)d)-2-[2'-(2-dimethylamino-ethoxy)-3,5-difluoro-biphenyl-4-ylJ-2-ethoxy-acetamide hydrochloride, {RS )-N- (4-Carbainiinidoyi-ben2yI) -2- [3,5-difluoro-2'-(2-hydroxy-ethoxy)-biphenyl-4-yl] -2-ethoxy-acetamide hydrochloride, (RS)-{4'-[(4-Carbamimidoyl-benzyIcarbamoyl)-ethoxy-methyi]-3',5'-difluoro-bipheByl-2-)ioxy}-acetic add ethyi ester hydrochloride, (RS)-{4'-[(4-Carbamimidoyl-benzylcarbamoyl)-ethoxy-meth)d]-3',5'-difluoro-biphenyi-2-yloxy}-acetic add, (RS)-2-(2'-Carbamoylmethoxy-3,5-difiuoro-biphenyl-4-^)-2-ethoxy-N-[4-(N-hydroxycarbamiinido>d)-benzyl] -acetamide, (RS)-N-(4-CarbamimidoyI-benz>i)-2-(2'-carbamoylmethoxy-3,5-difluoro-biphen)d-4-yi)-2-ethoxy-acetamide acetate, (RS) -N-(4-Carbamimidoyl-benzyl)-2- (2,6-difluoro-4-pyridin-4-yl-phenyl) -2-ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbamimidoyl-benz)i) -2- (2,6-difluoro-4-pyrimidin-5-yl-phenyl) -2-ethoxy-acetamide hydrochloride. (RS)-N-(4-Carbamiimdoyi-benzy']J-2-(2,6-difluoro-4-pyriimdin-2-yl-plienyl}-2-ethoxy- acetamide hydrochloride, (RS)-N-(4-Carbamiinidoyl-benzyl)-2-(2,6-difluoro-4-pyridin-2-yl-phenyI)-2-ethoxy- acetamide hydrochloride, (liS}-2-[4-(2-Ammo-pjTimidin-5-yl}-2,6-difluoro-phenyl]-N-(4-carbamimidoyl-benzyI}- 2-ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbamiimdo>^-benzyl)-2-(2,6-difluoro-4-pyridin-3-yl-phenyi)-2-ethoxy- acetamide hydrochloride, iRS)-2- [4-(6-Amino-pyridm-2-yI)-2,6-dMuoro-phenf]] -N-(4-carbamimidoy]-beiizyI)-2- ethoxy-acetamide hydrochloride, (RS)-2-[4-(5-Amino-pyridin-2-yl)-2,6-difluoro-phenyl]-N-(4-carbamiinidoyl-benzyl)-2- ethoxy-acetamide hydrochloride, (RS) -4' -[ {4-CarbainiinidoyI-benzylcarbainoyl) -ethoxy-mefeyJ] -3 ',5' -difluoro-bipheiiyi-3- carboxyHc add methyl ester hydrochloride, (RS)-(2-[4-(6-Ammo-pyridin-3-yl)-2,6-difluoro-phen)i]-N-(4-carbainiinidoyl-benzyl)-2- ethoxy-acetamide hydrochloride, {RS)-4'-[(4-Carbarnimido)d-benzykarbanioyl)-ethoxy-iDethylJ-3'^'-difluoro-biphenyi-3- caiboxyUc add, (RS){Aimno-[4-({2-[4-(6-ainmo-pyridin-3-yl)-2,6-difluoro-phenyl]-2-ethoxy- acetylaiiuno}-meUiyl)-phenyl]-niethylenei-carbamic add ethyl ester, (RS)2-[4-(6-Amino-pyridin-3-yI)-2,6-difluoro-phenyl]-2-ethoxy-N-l4-(N- hydroxycarbaminiidoyl)-beiizyl] -acetamide, (RS)-N- (4-Carbamiiiiidoyl-benzyl)-2-(3,5-difluoro-2' -hydroxyinethyI-biphenyl-4-yl)-2- ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbainimido)d-benz)d)-2-(2'-chloromethyl-3,5-difluoro-biphenyl-4-yl)-2- ethoxy-acetamide, (RS)-2-[3,5-Difluoro-2'-(hydroxyiinino-inethyl)-biphenyl-4-yl]-2-ethoxy-N-[4-(N- hydroxycarbamiinido}4)-benzy[]-acetamide, (RS)-2-(2'-Aminomethyl-3,5-difluoro-biphenyl-4-yl)-N-{4-carbamiinidoyi-benzyl)-2- ethoxy-acetamide acetate, (RS)-N-(4-Carbamimido)4-benzyl)-2-(2-fluoro-4-methoxy-3-phenoxy-phenyl)-2- methoxy-acetamide hydrochloride, (RS) -N- (4-carbainiinidoyl-benzyi) -2- (2-ethynyl-6-fluoro-phenyl)-2-methoxy-acetamide hydrochiorideaccording, (RS) -N- (4-Carbainimidoyl-beiizyl) -2-(2-ethyl- 6-fluoro-phen)d)-2-methoxy-acetaraide hydrochloride, (RS)-N-(4-CarbaiiiiinidoyI-beii2yl}-2-[2-fluoro-6-(3-hydroxy-prop-l-ynyi)-phenyl]-2- methoxy-acetamide hydrochloride. (RS)-N-{4-Carbaminiidoyl-benzyl)-2-[2-f[uoro-6-(3-hydroxy-propyl)-pheO)^]-2-methoxy-acetamide hydrochloride, (RS) -N- (4-Carbamiinido)i-beBzyl) -2- (3-fluoro-biphenyI-2-yl)-2-methoxy-acetamide hydrochloride, i (RS)-2-(3'-Ainino-3-fIuoro-biphenyi-2-yI}-N-C4-carbainirmdoyl-benzyl)-2-methoxy-acetamide hydrochloride, (RS) - N-(4-CarbaininiidoyI-beii2yl) -2-{3- 9uoro-3 '-mtro-biphenyl-2-yl) -2-niethoxy-acetamide hydrochloride, (RS)-2-[2-{6-Ainino-pyridin-2-yl)-6-f[uorD-phen)d]-N-(4-caTbamiinidoyi-benzyi)-2-methoxy-acetamide acetate, (RS)-{2-[(4^Carbainimido}d-beiizylcarbamoyl)-methoxy-methyl]-3-fluoro-phenoxy}-acetic add meth)^ ester acetate, (RS)-{2-[(4-CarbamimidoyI-benzyIcarbamoyl}-methoxy-methyl]-3-fluoro-pbenoxy}-acetic add, (RS)-N-C4-Carbamimidoyi-benzyl)-2-[2-(3-dimediylainino-propoxy)-6-fluoro-phenyI]-2-methoxy-acetamide hydrochloride, {RS)-N- (4-Carbainiimdoyl-benzyl) -2- (2-fluoro-6-phenoxy-phenyl) -2-methoxy-acetainide hydrochloride, (RS)-N- (4-Carbaimiradoyl-beiizyl)-2-(2,6-difluoro-4-methoxy-phenyl) -2-ethoxy-acetamide hydrochloride, (RS)-2-{4-Beiizyloxy-2,6-difiuoro-phenyl)-N-(4-carbamiimdoyl-beiizyI)-2-ethoxy-acetamide hydrochloride 1:1, (RS)-N-C4-Carbainiiiiidoyl-benz)d)-2- (2,6-difluoro-4-isopropoxy-phen)d) -2-ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbainiimdoyl-ben2)d)-2-[2,6-difluoro-4-(pyridin-2-)iinethoxy)-phen)4]-2-ethoxy-acetamide hydrochloride, (RS)-2-[2,6-Difluoro-4-{pyridin-2-ylmethoxy)-phenyi]-2-ethoxy-N-[4-(N-hydroxycarbamimido^) -benzyl] -acetamide, (RS)-|Ainino-[4-({2-[2,6-difiuoro-4-(pyridin-2-yiinethoxy)-phen'jd]-2-etho3cy-acetylainino}-methyl)-phenyi]-methyleDe}-carbaimc add ethyl ester, (RS)-N-(4-CarbaininudoyI-benzyl)-2-[2,6-difluoro-4-(pyridin-3-ylmethoxy)-phenyl]-2-ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbanixinidoyl-benzyi)-2-[2,6-difluoro-4-(pyridin-4-ylmethoxy)-phenyl]-2-ethoxy-acetamide hydrochloride, (RS) -N- (4'CarbainimidoyI-benzyl)-2-(2,6-di£[uoro-4-phenoxy-phen)4)-2-ethoxy-acetamide hydrochloride, (RS)-N-(4'CarbaniiimdoyI-benzyl)-2-[2,6-difluoro-4-(pyridin-3-)doxy)-phenyl]-2-ethoxy-acetamide hydrochloride. (RS)-N-(4-Carbamimidoyl-beiizyl)-2-(2,6-difluoro-3-isopropoxy--phenyl)-2-ethoxy"- acetaraide hydrochloride, (RS)-N-(4-CarbainiinidoyI-ben2yl)-2-(3-carbamoyhnethoxy-2,6-difluoro-phenyl)-2- ethoxy-acetamide hydrochloride, (RS)-2-[3-(2-Benzyloxy-ethoxy)-2,6-difluoro-phenyl]-N-(4-carbamiinidoyl-benzy!)-2- ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbainiimdoyl-benzyl)-2-[2,6-difluoro-3-(2-hydroKy-ethoxy)-phenyl]-2- ethoxy-acetamide hydrochloride, (RS)-N-(4-Carbamiinidoyi-benzyl)-2-(2,6-difluoro-3-phenoxy-phen)i)-2-etiioxy- acetamide acetate, (RS)-N-(4-Carbarminidoyl-benzyl)-2-(2,4-difiuoro-biphenyl-3-yl)-2-ethoxy-acetaniide hydrochloride, (RS)-2-(2,6-Difluoro-3-phenyIaimno-phenyl)-N-[4-(N-hydroxycarbainiimdoyl)-benzyl]- 2-methoxy-acetainide, (RS) -N- (4-Carbainimidoyl-benzyl) -2-(2,6-difluoro-3-phenyIaniino-phenyl)-2-methoxy- acetamide acetate, (RS)-N-(4-Carbaniimidoyl-beii27l)-2-(2,6-difluoro-3-isopropylamino-phenyI)-2- methoxy-acetamide acetate, (RS)-2-(3-AcetylamiTio-2,6-difluoro-phenyl)-N-(4-carbainiinido)4-beiizjd)-2-inethoxy- acetamide hydrochloride, (RS)-(4-Carbammiido)4-benzyl) -2-(2,6-difluoro-3-phenylacetylainino-pheiiyI) -2- methoxy-acetamide hydrochloride, (RS )-N- (4-Carbarminidoyl-beiizyl) -2- (2,6- difluoro-3-hydroxymethyl-phenyl}-2-ethox)'- acetamide hydrochloride, (RS)-2-[3-(Acet)dammo-methyl)-2,6-difluoro-phenyl]-N--(4~carbamiinidoyl-benzyl)-2- ethoxy-acetamide hydrochloride, (RS )-2- (3-Ammomethyl-2,6-difluoro-phenyl)-N- (4-carbaimimdoyI-benzyi) -2-ethoxy- acetamide acetic acid 1:4, (RS)-(4-Carbamiinidoyl-benzyl)-2-(2,6-difluoro-3-phenylairdnomethyl-pheii)d)-2-ethoxy- acetamide hydrochloride, (RS)-(4-Carbaimniidoyl-benz)i)-2-(2,6-difluoro-3-inorpholin-4-)dinethyl-phenyI)-2- ethoxy-acetamide hydrochloride, (RS)-(4-Carbamimidoyl-benz}d)-2-(2,6-difluoro-3-piperidin-1-ybiiethyl-phen)d)-2- ethoxy-acetamide hydrochloride, (RS) -2 -{3-Diethoxymethyl-2,6-dif[uoro-phenyl) -2-ethoxy-N- [4- (N- hydroxycarbaraimidojd)-benz)d] -acetamide, (RS)- (4-Caxbarmmidoyl-ben2yl) -2-(2,6-difluoro-3-formyl-phenyi)-2-ethoxy-acetamide acetic add (1:4), (RS)-N-(4-Carbamiinidoyl-2,6-difluoro-benzyl)-2-(2,6-difiuoro-4-methoxy-phen^)-2-ethoxy-acetamide; hydrochloride, (R.S)-N-(4-Carbamimidoyl-2,6-difluoro-beiizyI)-2-ethoxy-2-(2-fluoro-4-inethoxy-phenyl)-acetaimde acetate, (RS }-N- (4-Carbammudo)d-2,6-difiuoro-b enzyl)-2- (2,6- difluoro-4-methoxy-phenyl) -2-methoxy-acetamide acetate, (RS)-N-(4-Carbainimidoyl-2,6-difluoro-benzyl)-2-(2-fluoro-4-niethoxy-phen)d)-2-methoxy-acetamide acetate, (RS)-[4-Carbammiidoyl-2-(carbanioylmethyl-ainiiio)-benzyl]-2-ethoxy-2-( 2-fluoro-4-methoxy-phenyl) -acetamide hydrochloride, (RS) -N- (2-Benzylamino-4.carbainimidoyl-beiizyl}-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl}-acetamide acetate, (RS)-[4-Carbamiinido5d-2-(2-fluoro-benzylamino)-benzyl]-2-ethoxy-2-(2-fluoro-4-methoxy-phenyI}-acetainide hydrochloride, (RS)- {4-CarbamirnidoyI-2- [ (pyridin-2-yhnethyl) -amino] -benzyl}-2 -ethoxy-2- (2-fluoro-4-methoxy-phenyl)-acetamide hydrochloride, (RS)-[4-Carbamimidojd-2-(4-chloro-2-fluoro-benzylamino)-ben2)d]-2-ethoxy-2-(2-fiuoro-4-inethoxy-phenj4)-acetaimde hydrochloride, (RS)- (4-Carbamimidoyl-2-plienethylamino-beiiz:>d)-2-ethoxy-2-{ 2-fluoro-4-methoxy-phenyl)-acetamide hydrochloride, (RS)-(5-Carbamimidoyl-2-{[2-ethoxy-2-(2-fiuoro-4-methoxy-phen)d)-acet)damino]-methyl}-phenylamino)-acetic add eth}d ester hydrochloride, (RS)-(5-Carbamimidoyl-2-{[2-ethoxy-2-(2-fluoro-4-methoxy-phen)d)-acetylainino]-methyll-phenylamino)-acetic add acetate, (RS)-(4-Carbaminiidoyl-2-phenylmethanesulfonylainino-benzyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide hydrochloride, (RS)-[2-(3-Beiizyl-urddo)-4-carbaminiidoyl-benzyi]-2-ethoxy-2-(2-fluoro-4-methoxy-phenyi)-acetamide acetate, (RS)-(5-Carbamimidoyl-2-{[2-ethoxy-2-(2-fluoro-4-methoxy-phenyi)-acetylamino]-methyl}-phenyl)-carbamic add benzyl ester hydrochloride, (RS) -(4-Carbamimidoyl-2-phenylainino-benzyi) -2-ethoxy-2-(2-fiuoro-4-methoxy-pheny]}-acetamide hydrochloride, (RS)-2- [4- (6-Amino-pyridin-3-)d)-2,6-difluoro-phenyl] -N-(4-carbamimidoyl-2-carbamo)dmethoxy-benz:>d)-2-ethoxy-acetamidehydrochloride acetic add (1:1:2), (RS) - (4-Carbamimidoyl-2-carbamoyhnethoxy-benzyl) -2- [2,6-difluoro-4-(pyridin-2-yhnethoxy)-phenylj-2-ethoxy-acetamide hydrochloride, (RS)-2-[4-(6-Ainino-pyridin-3-yl)-2,6-difluoro-phenyi]-N-(4-carbarmrmdoyl-2,6-diiluoro-benzyi)-2-ethoxy-acetamide acetate. (RS)-[(4-{[2-{2,6-Difluoro-4-methoxy-phenyl)-2-methoxy-acetylamino]-methyl}-phenyl)-imino-methyi]-carbainic acid tert-butyl ester, (S)-[(4-{[2-(2,6-Difluoro-4'medioxy-phenyl)-2-niethoxy-acetylaiiimo]-methyl}-phenyl)-imino-methylj-carbamic add tert-butyl ester, (R)-[(4-{[2-(2,6-Difluoro-4-methoxy-phenyl}-2-methoxy-acetylaminoj-methyl}-phenyI)-imino-methyij-carbamic add tert-butyl ester, (S)-N- (4-Carbaiminidoyl-benzyl)-2 -(2,6-difluoro-4-methoxy-phenyi)-2-methoxy-acetaInide fortniate^ (R)-N-(4-CarbaniiinidoyI-beiizyi)-2-(2,6-difluoro-4-metboxy-phenyI)-2-raetiioxy-acetamide formiate, [l-Ainmo-l-(4-{[(R)-2-edioxy-2-(2-fiuoro-4-methoxy-phenyl)-acetylamino]-niethyl}-phenyI)-meth-(E)-)didene]-carbamic add benzyl ester, {R)-N-(4-CarbaiTiimidoyl-benzyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phen^)-acetamide acetate, (RS)-[Ammo-(4-{[2-ethoxy-2-(2-fluoro-4-methoxy-phen)d)-acetylamino]-methyl}-phenji)-methylene]-carbamic acid bemyl ester, (RS)-[(4-{[2-(2,6-Difluoro-4-inethoKy-phenyl)-2-methoxy-acetylammo]-methyl}-phenyl)-immo-methyl]-carbaniic add benzyl ester, (RS)-N-(4-Carbamimido^'benzyl)-2-[2,6-difluoro-4-(I-oxy-pyridm-4-yl)-pheny]]-2-methoxy-acetamide hydrochloride, (RS)-(4-Carbainiiiiidoyl-benz)d)-2-[2,6-di£luoro-4-(tetrafaydro-pyran-4-yl)-phenyl]-2-ethoxy-acetamide acetate, and (RS) - (4-Carbainimidoyl-benzyi) -2-(4-cydohex^-2,6-difluoro-phenyl)-2-ethoxy-acetamide acetate, and pharraaceutically acceptable salts thereof. Particularly preferred compounds of formula (I) are those selected from the group consisting of (S)-N-{4-CarbaiiiiinidoyI-ben2yl)-2-methoxy-2-phenyl-acetamide hydrochloride, {RS)-N-(4-Carbainiinidoyl-benzyl)-2-(2-fIuoro-4-methoxy-phen5d}-2-methosy-acetamide hydrochloride, (RS)-[Amino-(4-{[2-(2-fluoro-4-methoxy-phenyl)-2-methoxy-acetyiamino]-methyll-phenj^)-methylene]-carbamJc add ethyl ester, (RS)-2-(2-Fluoro-4-methoxy-phenyl)-N-[4-(N-hydroxycarbamimido)d)-benzyl]-2-methoxy-acetamide, (RS) -N-(4-Carbamimidoyi-benzyl)-2- (3-fIuoro-3 '-methoxy-biphenyl-4-}d)-2-methoxy-acetamide hydrochloride, (RS) -N- (4-Carbamimidoyl-benzyl) -2-ethoxy-2- (2-fluoro-4-methoxy-phenyI)-acetamide hydrochloride, (RS) -N-(4-Carbaininiidoyl-benzyl)-2 -(2,6-difl^^oTO-4-methc^X)'-pheIlyl)-2-^lethox7-acetaImde hydrochloride, (RS)-N- (4-CaTbarQiimdoyl-benzyl) -2-( 2-fluDro-4-pyridm-3-yl-phenyl)-2-methoxy-acetamide hydrochloride, and (RS)-2-(4-Bromo-2,6-difluoro-phenyl)-N-(4-carbainiimdoyl-benzyl)-2-ethox7'acetainide hydrochloride, and pharmaceutically acceptable salts thereof. Other particularly preferred compounds are those selected from the group consisting of (RS)-N-(4-Carbamimidoyl-2-carbamoylmethoxy-benzyl)-2-(2,6-difluoro-4-methoxy-phen^)-2-ethoxy-acetamide hydrochloride, (RS)-N-{4-Carbamimidoyl-2-[(2-methoxy-eth)dcarbamo)i)-methoxy]-benzyl}-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide hydrochloride, (RS)-N-[4-Carbainimidoyl-2-(pyridin-2-ylmethoxy)-benzyl]-2-(2,6-difluoro-4-methoxy-phen)4)-2-methox)'-acetainide hydrochloride, (RS)-2-[4-(2-Amino-pyriniidin-5-)d)-2,6-difluoro-phenyl]-N-(4-carbamimidoyl-benzyl}-2-ethoxy-acetaniide hydrochloride, (RS)-N- (4-Carbamimido)i-benzyl) -2-(2,6'difluoro-4-pyridm-3-)d-phen5d) -2-ethoxy-acetamide hydrochloride, (RS)-2-[4-(5-Amino-pyridin-2-yl)-2,6-difluoro-phen)d]-N-(4-carbamimidoyl-benzyl)-2-ethoxy-acetamide hydrochloride, (RS)-(2-[4-{6-Amino-pyridin-3-yl)-2,6-difiuoro-phenyl]-N-(4-carbamimidoyl-benzyl)-2-ethoxy-acetamide hydrochloride, (RS)-N-{4-Carbaininiidoyl-beiizyl}-2-[2,6-difluoro-4-(pyridin-2-yhnetho]cy)-phenyI]-2-ethoxy-acetamide hydrochloride, (RS)-N-(2-Beiizylanuno-4-carbamimidoyl-benzyl)-2-ethoxy-2-(2-fluDro-4-methoxy-phenyl)-acetamide acetate, (RS)-(5-Carbamimidoyl-2-{[2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetylamino]-meth)^}-phenjdamino)-acetic acid acetate, (RS)-(4-Carbaminiidoyi-2-carbamoylmethoxy-ben2yi)-2-[2,6-difluoro-4-(pyridiii-2-)dmethoxy)-phenyI]-2-ethoxy-aceta]aiide hydrochloride, (RS)-2-[4-C6-Amino-pyridin-3-yI)-2,6-difluoro-phenyl]-N-(4-carbaminudoyI-2,6-difluoro-ben2yi)-2-ethoxy-acetamide acetate, and (RS)-{4-Carbamimidoyl-2-[{pyridin-2-ylmethyI)-amino]-benzyl}-2-ethoxy-2-(2-fluoro-4-methox)'-phenyi)-acetamide hydrochloride, and pharmaceutically acceptable salts thereof. It will be appreciated that the compounds of general formula (I) in this invention maybe derivatised at ftmctional groups to provide derivatives virhich are capable of conversion back to the parent compound in vivo. The invention further relates to a process for the manufacture of conipounds of formula (I) as defined above, which process comprises converting the nitrile group in a compound of formula (H) wherein R2 R2 R2 R2 R2 R2 R2 R1, R2", X and Y have the significances given above, into a carbamimidoyl group, or into a N-hydroxy-caibamimidoyl group, or into a N-amino-carbamimidoyl group, and, if desired, converting an obtained compound of formula (I) into a phannaceutically acceptable salt. A preferred process as described above comprises the conversion of the nitrile group into a carbamamidoyl group, or into a N-hydroxy-carbamimidojd group, or into a N-amino-carbannmidoyl group. The conversion of the nitrile group in a compound of formula II into a carbamimidoyl group -C{NH)NH2 or into a N-hydroxy-carbamimidoyl group -C(NOH)NH2 or into a N-amino-carbamimidouyi group -C(N-NH2)NH2 can be carried out according to methods known per se. For example, the conversion into a N-hydroxy-carbamimidoyl group can be performed by dissolving a compound of formula n in a solvent, such as DMF, ethanol or methanol, treating the solution with hydroxylamine or a salt of hydroxylamine with an inorganic acid, such as hydroxylamine hydrochloride, and thereafter with a base, such as diisopropylethylamine or triethylamine, sodium hydride or sodium methanolate, conveniently at a temperature up to 80°C. The conversion of the nitrile group into a carbamimidoyl group can be carried out e.g. by treating a compound of formula II in a solvent, such as ethanol or methanol, or a solvent mixture, such as chloroform and methanol or chloroform and ethanol, with a dry stream of hydrogen chloride, conveniently at a temperature below 10 °C. The solution containing the iminoether can be evaporated and the residue can be treated with gaseous ammonia or an ammonium salt in methanol or ethanol. In an analogous manner, the iminoether can be converted into a N-hydroxy-carbamimidoyl compound of formula I with hydroxyiamine or a salt thereof in the presence of a base or into a N-amino-caibamimidoyl compound of formula I with hydrazine or a salt thereof in the presence of a base. In so doing, other reactive groups present in the compound of formula I and reactive towards the treatment wih hydrogen chloride or gaseous ammonia or ammonium chloride or hydroxyiamine or hydrazine can be modified. For example, in the case of treatment with hydrogen chloride a benzjdoxy group R6, R2, R2, R1, R2, R1, R1° or R6 can be converted into the hydroxy group. In the case of treatment with gaseous ammonia in methanol or ethanol a lower-alkoxy-carbonyl-lower-alkoxy group R2 R1, R6*, R2 R2 R2, R2° or R6 can be converted into a carbamo)d-lower-alkoxy group. If a carbamimidoyl compound of formula (I) is obtained from a nitrile of formula (U) by treatment with hydrogen chloride and subsequent reaction with gaseous ammonia or ammonium chloride, the carbamimidoyl product is obtained as hydrochloride salt. This salt can be converted into any other pharmaceutically acceptable salt by thromatography over an adequately charged basic ion exchange resin. Alternatively the hydrochloride salt of a carbamimidoyl compound of formula (I) can be converted into the corresponding free base by treatment with sodium ethanolate in ethanol and subsequently treated with an excess of an appropriate acid to generate any pharmaceutically acceptable salt. Any pharmaceutically acceptable salt of a carbamimidoyl compound of formula (I) can ftirthermore be obtained when a N-hydroxy-carbamimidoyl compound of formula (I) is hydrogenated in a solvent like ethanol, methanol, dioxan or THF, with hydrogen and a catalyst such as palladium, platinum or nickel in the presence of an appropriate acid. Functional groups in compounds of formula (I) can be modified. As modifications of functional groups in a compound of formula I there come into consideration especially the conversion of a N-hydroxy-carbamimidojd group into a carbamimidoyl group, the esterification of a carboxy group, the saponification of an ester group and the cleavage of an ether group, such as an arylalkyl ether group, e.g. the benzjd ether group. All of these reactions can be carried out according to methods known per se. A compound of formula (I) in which R1 represents a hydroxy group can be converted into a compound of formula (I) in which R2 represents hydrogen by hydrogenation in a solvent, such as ethanol, methanol, dioxane, THF or ^cial acetic add, or a solvent mixture, such as ethanol and glacial acetic add, with hydrogen and a catalyst, such as palladium, platinum or nickel. In so doing, other reactive groups present in the compound of formula I and reactive towards the reducing agent can be modified. A compound of formula (I) in which R2 represents benzyloxy-carbonyl can be converted into a compound of formula (I) in which R represents hydrogen by hydrogenation in a solvent, such as ethanol, methanol, dioxane, THF oi glacial acetic acid, or a solvent mixture, such as ethanol and glacial acetic acid, with hydrogen and a catalyst, such as palladiimi. The reaction can be optionally performed in the presence of an acid such as HCl in a solvent such as EtOH or MeOH. In so doing, other reactive groups present in the compound of formula I and reactive towards the reducing agent can be modified. A compound of formula (I) in which R2 represents lower-alkoxy-carbonyl or aryl-lower-alkoxy-caibonyl is obtdned by reacting a compound of formula (I) in which R2 represents hydrogen with a chlorofonnic add lower alkyl ester or a chloroformic acid aryl-lower-alkyl ester in a solvent, such as dichloromethane, dioxane or DMF, or a solvent mbcture, such as dichloromethane and water or ethyl acetate and water, in the presence of an organic base, such as pyridine or triethylamine, or an inorganic base, such as sodiimi hydroxide, sodium carbonate or potassium bicarbonate. A compound of formula (1) in which R2 represents benzyloxy-carbonyl and R6^.^ and R2 have the significance of hydrogen can be prepared according to general methods known per se, e,g. by coupling of an add of formula (III) and [{4-aminomethyI-phenyl)-imino-methyI]-carbaraic add. benzyl ester in the presence of coupling reagents as BOP or EDCI/HOBt and a organic base such as triethylamine or diisoprop)d ethyl amine in a solvent such as THF. A compound of formula (1) in which R1^ represents lower-alkyi-carbonyl or aryl-carbonyl is obtained by reacting a compound of formula (I) in which R1 represents hydrogen with a acyl chloride in a solvent, such as dichloromethane, dioxane or DMF, or a solvent mixture, such as dichloromethane and water or ethyl acete.te and water, in the presence of an organic base, such as pyridine or triethylamine, or an inorganic base, such as sodium hydroxide, sodium carbonate or potassium bicarbonate. A compound of formula (11) in which R2 R\ R8, R1, R2 R2 V}'^ or R2^ has the significance of a hydroxy group, or a compound of formula (I) in which R2 has the significance of benz>doxy-carbon)d and R2 R2Jl^, R2 R6, R1, R2" or R6 has the significance of a hydroxy group can be reacted: - with an alkylating agent such as an appropriately substituted alkyl bromide, alkyl iodide or alkyl mesylate in tib.e presence of a base such as potassium carbonate or caesium carbonate in a solvent such as DMF or acetone, or - with an alkene oxide in a solvent like EtOH, or - by a Mitsunobu reaction witli an appropriately substituted alcohol in the presence of DEAD, DIAD, or di-tert.-butyl-azodicarboxylate, and triphenjdphosphine or triphenylphosphine on sohd suppert in a solvent such as THF, dichloromethane or dioxane, or by an oxidative coupling with an ar>d boronic add or a heteroarylboronic add in the presence of a copper salt like Cu(0Ac)2, a base like pyridine or triethylamine and a solvent like dichloromethane or 1,2-dichloroethane, or with trifluorosulfonic add anhydride and an organic base Uke triettylamine or pyridine in a solvent such as THF or dichloromethane. A compound of formula (II) in which R2, R2Jl*, R2, R2 R2, R2° or R2^ has the significance of an aniline group or a compotmd of formula (I) in which R1 has the significance of benzyioxy-carbonyl and R6^, R2.R1*, R2, R2 R1, R1" or R6 has the significance of an aniline group can be reacted: - with an alkylating agent such as an appropriately substituted alkyl bromide, aUcyl iodide or alkyl mesylate in the presence of an organic base such as trieth^ amine or diisopropyl ethyi amine in a solvent such as DMF, or with an acyi or a sulfonyl chloride or a chloroformic add ester in the presence of an organic base such as triethyl amine OT diisopropyl ethyl amine in a solvent such as DMF, THF or acetonitrile, or - by reaction with isocyanate in a solvent such as dichloromethane or 1,2-dichloroethane, or - by oxidative coupling with an arylboronic add or a heteroaryi boronic add with a copper salt like Cu(0Ac)2, an organic base such as triethylamine or pyridine and an oxidant like TEMPO in a solvent like dichloromethane or 1,2-dichloroethane. A compound of formula (H) in which R2 R2 R8, R1, R2 R1, R2° or R6 has the significance of a bromide or of CF3-SO2-O-, or a compound of formula (I) in which R1 has the significance of benzyloxy-carbonjd and R2 R2,R8, R2, R2, R2, R2" or R6 has the significance of of a bromide or of CF3-SO2-O- can be reacted - with a aryl boronic add or a heteroaryi boronic add in the presence of a base such as sohd or aqueous potassium carbonate or sodium carbonate and a palladiimi catalyst such as tetrakis(triphen)4phosphin)palladium{0) or l,r-bis(diphenyi-phosphin) ferrocene-palladium dichloride in a solvent such as toluene or THF, or - with bis(pmacolato)diboron in the presence of a base sudi as potassium acetate and a palladium catalyst like bis(triphenylpliosphine)palladium(n) chloride and a solvent such as dioxane. The boronic acid ester thus obtained is fiirther converted by reaction with an arylhalogenide or a heteroaryl halogenide and a base such as sohd or aqueous potassium carbonate or sodium carbonate and a palladium catalyst such as bis(diphenylphosphin)ferrocene-paUadiuni dichloride in a solvent such as 1^-dimethoxyethane, or with carbon monoxide in the presence of a catalyst such as Pd(0Ac)2, a Ugand such as l,3-his-{diphenylphosphino)propane, an alcohol such as MeOH or 2-trimethylsilyl ethanol and a soiventsuch as DMSO, or ' with an appropriately substituted alkine in the presence of an organic base such as triethylamine and copper(I)iodide in a solvent such as DMF and a palladium catalyst such as tetrakis(triphen)4phosphin)palladiimi(0). A compound of formula {II) in which R2 R1,R8, R1, R2 R2, R1° or R6 has the s^ficance of a COOH group or a compound of formula (I) in which R has the significance of benzyloxy-carbonyl and R1, R2R2 R2 R2 R2 R2° or R6 has the significance of a COOH group can be reacted: in the presence of coupling reagents such as BOP or EDCI/HOBt and an organic base such as trieth)damine or diisopropyl ethyl amine in a solvent such as THF, DMF or dichloromethane. A compound of formula (11) in which R2, R2Jl^, R2 R8, R2, R2° or R2^ has the significance of a CHO group, or a compound of ftinnula (I) in which R2 has the significance of benzyloxy-carbonyl and R-, R2^\ R2 R2 R1, R2° or R2^ has the significance of a CHO group can be reacted: - by reduction with NaBH4 in EtOH, or by reductive amination with an amine in the presence of a reducing agent sudi as NaBH4 or NaBHsCN and a solvent such as EtOH, or - by reaction with hydroxylamine, hydrochloride in the presence of a base such as NaOAc and a solvent such as EtOH, and subsequent reduction of the intermediate oxime by Zn in HOAc. The aminomethyl derivative thus obtained can be reacted with an acyl chloride or a sulfonyl chloride in the presence of an organic base and a solvent such as THF, dichloromethane or DMF. The compounds of formula (II) in which X has the significance of an oxygen are prepared according to general methods known per se, e.g.by coupling of an acid of formula (III) and an appropriately substituted 4-aniinomethyl benzonitrile of formula (VI) in the presence of coupling reagents such as BOP or EDCI/HOBt and an organic base such as triethylamine or diisopropyl ethyl amine in a solvent such as THF. Compounds of formula (III) in which X has the significance of oxygen are known per se or can be prepared according to general methods known per se, e.g. as described hereinafter and/or as described in the Examples or in analogy to these methods. For example, a compound of formula (EI) in which X has the significance of oxygen and R2 has the significance of hydrogen can be prepared - by reaction of an aldehyde of formula (IV) with bromoform or chloroform in a mixture of solvents like dioxane/methanol or dioxane/ethanol in the presence of an inoi^anic base like sodiimi hydroxide or potassium hydroxide, or - by reaction of an aldehyde of formula (IV) with trimethylsilyl cyanide in the presence of Znl2 in a solvent such as dichloromethane. The trimetiiylsilyi cyanohydrine thus obtained is subsequently hydrolysed in concentrated hydrochloric acid to the corresponding a-hydroxy carboxylic add which is then alkylated to give a compound of formula (III) using an appropiately substituted alkyl halide in the presence of silver oxide in a solvent such as toluene. Compounds of formula (IV) are known per se or can be prepared according to general methods known per se, e.g. as described hereinafter and/or as ciescribed in the Examples or in analogy to these methods. Compounds of formula (III) can be prepared from compounds of fonnula (V) in which R2 and/or R6 have the significance of substituents which have an ortho-directing effect in a metallation reaction by reaction with a strong base like n-butyl lithium, IDA or lithium 2,2,6,6-tetramethyi piperidide, with ediyl glyoxalate as electrophile, witii N,N,N',N',N"-pentamethyldieth}dentriamine or N,N,N',N'-tetramethyiethylendiamine as additive and THF as solvent. The a-hydroxy phenyl acetic add ester thus obtained is reacted with an alkylatii^ agent such as eth)4 iodide or methyl iodide in the presence of silver oxide in toluene as solvent The G-aikoxy phenyl acetic acid ester is then hydrolysed by a base such as aqueous NaOH or LiOH in a solvent such as THF or EtOH- A compound of formula (III) in which X has the significance of oxygen and R has the significance of methyl can be prepared by reaction of an appropriately substituted acetophenone with bromoform or chloroform in a mixture of solvents like dioxane/methanol or dioxane/ethanol in the presence of an inorganic base like sodium hydroxide or potassium hydroxide. Compounds of formula (VI) can be prepared according to general methods known per se, e.g as described hereinafter and/or as described in the Examples or in analogy to these. For example, a substituted 4-aminomethyl benzonitrile of formula (VI) can be prepared from the correspondingly substituted 4^cyano-benzaldehyde by reaction with hydroxylamine hydrochloride in the presence of a base such as NaOAc in a solvent such as EtOH. Subsequently, the oxime thus obtained can be reduced by zinc in acetic acid. Alternatively, a substituted 4-aniinomethyi benzonitrile of formula (VI) can be prepared from the correspondingly substituted 4-bromoinethyl benzonitrile by reaction with hexamethylene tetramine (HMTA) in chloroform and subsequent hydrolysis of the HMTA adduct by concentrated aqueous hydrochloric add in EtOH. The compounds of formxila (II) in which X has the significance of an NR1^ and R1^ has the significance of lower-alfcyl are prepared according to general methods known per se> e.g. as described hereinafter and/or as described in the Examples or in analogy to these methods. For example, a compound of formula (VII) can be reacted with a lower-alkyl amine or a di-lower-alkjd amine or the corresponding anunonium hydrochlorides in the presence of an organic base such as triethylamine and a catalyst such as tetrabutylammonium iodide in a solvent such as THF. Compounds of formula (II) in w^ch X has the significance of NR12 and R1 has the significance of lower-alkjd-carbonyl can be obtained by coupling an appropriately substituted N-Boc-phenylglycine and an appropriately substituted 4-aminomethyl benzonitrile in the presence of coupling reagents such as BOP or EDCI/HOBt and an organic base such as triethyiamine or diisopropy] ethyl amine in a solvent such as THF. The Boc group can be cleaved by reaction with trifluoroacetic add in a solvent like dichloromethane. The amino group thus Kberated can then be reacted with an appropriately substituted acyl chloride or acyl anhydride in the presence of an organic amine like triethyiamine in a solvent lilce THF or dichloromethane. The compounds of formula (II) in which X has the significance of sulfin are prepared according to general methods known per se, e.g. as described hereinafter and/or as described in the Examples or in analogy to these methods. For example, a compound of formula (VII) can be reacted with the sodium salt of a lower-aUcyl mercaptane in the presence of a catalyst such as tetrabutylammoniimi iodide in a solvent such as methanol. Compounds of formula (11) in which X has the significance of SO2 can be obtained from compounds of formula (H) in which X has the significance of sulfiir by reaction with an oxidant such as m-chloro perbenzoic acid in a solvent like dichloromethane. Compounds of formula (VH) can be obtained by coupling an appropriately substituted a-bromo-phen)iacetic acid and an appropriately substituted 4~aniinomethyI benzonitrile in the presence of coupling reagents such as BOP or EDCI/HOBt and an organic base as triethyiamine or diisopropyl ethyl amine in a solvent such as THF. Insofer as their preparation is not described in the examples, the compounds of formulae (I), (II), (III), (IV), (V), (VI) and (VII) can be prepared according to analogous methods or according to die methods set forth above. Furthermore, the invention relates to compounds of formula (I) as defined above, when manufectured by a process as described above. In another embodiment, the invention relates to the intermediates, the compounds of formula (II) As described above, the compounds of formula (I) are active compounds and inhibit the formation of coagulation factors Xa, IXa and thrombin induced by fector Vila and tissue factor or are derivatives which are converted under physiological conditions to such active compounds. These compounds consequently influence both platelet aggregation which is induced by these factors and plasmatic blood coagulation. They therefore inhibit the formation of thrombi and can be used for the treatment and/or prevention of diseases, such as arterial and venous thrombosis, deep vein thrombosis, pulmonary embolism, unstable angina pectoris, cardiac inferction, stroke due to atrial fibrillation, inflammation and arteriosclerosis. Furthermore, these compounds have an effect on tumour cells and prevent metastases. They can therefore also be used as antitumour agents. Prevention and/or treatment thrombosis, particularly arterial or deep vein thrombosis, is tiie preferred indication. The invention therefore also relates to pharmaceutical compositions comprising a compound as defined above and a pharmaceutically acceptable carrier and/or adjuvant. The invention likewise embraces compounds as described above for use as therapeutically active substances, espedaliy as therapeutically active substances for the treatment and/or proph)daxis of diseases which are associated with the formation of clotting fectors Xa, IXa and thrombin induced by fector Vila and tissue fector, particularly as therapeutically active substances for the treatment and/or prophylaxis of arterial and venous thrombosis, deep vein thrombosis, pulmonary embolism, unstable angina pectoris, cardiac inferction, stroke due to atrial fibrillation, inflammation, arteriosclerosis and/or tumour. In another preferred embodiment, the invention relates to a method for the therapeutic and/or prophylactic treatment of diseases which are asscodated with the formation of dotting fectors Xa, IXa and thrombin induced by fector Vila and tissue fector, particularly for the therapeutic and/or prophylactic treatment of arterial and venous thrombosis, deep vein thrombosis, pulmonary embolism, unstable angina pectoris, cardiac inferction, stroke due to atrial fibrillation, inflammation, arteriosclerosis and/or tumour, which method comprises administering a compound as defined above to a human being or animal. The invention also embraces the use of compounds as defined above for tiie therapeutic and/or prophylactic treatment of diseases which are asscodated with the formation of clotting fectors Xa, IXa and thrombin induced by fector Vila and tissue fector, particularly for the therapeutic and/or prophylactic treatment of arterial and venous thrombosis, deep vein thrombosis, pulmonary embolism, unstable angina pectoris, cardiac inferction, stroke due to atrial fibrillation, inflammation, arteriosclerosis and/or tumour. The invention also relates to the use of compounds as described above for the preparation of medicaments for the therapeutic and/or proph)dactic treatment of diseases which are asscodated mdi the formation of dotting factors Xa, IXa and thrombin induced by factor Vila and tissue factor, particularly for the therapeutic and/or prophylactic treatment of arterial and venous thrombosis, deep vein thrombosis, pulmonary embolism, unstable angina pectoris, cardiac infarction, stroke due to atrial fibrillation, inflammation, arteriosclerosis and/or tmnour. Such medicaments comprise a compound as described above. Tlie inhibition of tie amidolytic acdvity of factor Vila/tissue fector complex by the compounds in accordance with the invention can be demonstrated with the aid of a chromogenic peptide substrate as described hereinafter. The measurements were carried out by an automated robotic assay on microtitre plates at room temperature. To this end, 100 pi. of a solution of 26 nM of tissue fector, 9 nM of soluble ^ctor Vila and 8 mhi of caldum chloride were added to 25 jil of a solution of the inhibitor in a buffer [pH 7.5, lOO mM, comprising O.UM NaCl, O.IM N-(2-hydroxyethyl)piperazine-N'-(2-elhanesulphomc acid) (HEPES), 0.5 mg/1 of fatty-acid-free BSA (bovine serum albumin} and 0.05% NaNj] in each well of the plate. After an incubation time of 15 minutes the reaction was started by the addition of 50 jU of chromogenic substrate Chromozym-tPA {3,5 mM, MeSOj-D-Phe-GIy-Ai^-paranitroaniHde) and the hydrolysis of the substrate was followed spectrophotometrically on a kinetic microtitre plate reader over 10 minutes. Using the plot of the inhibition curves, the Ki values were determined according to the method described in Biochem. J. 55, 1953, 170-171. The activity of the low molecular weight substances can, moreover, be characterized in the "prothrombin time" (FT) clotting test. The substances are prepared as a 10 mM solution in DMSO or DMSO/O.IM HQ (DHCl) and thereafter made up to the desbed dilution in the same solvent Thereafter, 0.25 ml of human plasma (obtained from whole blood anticoa^ulated with 1/10 volume of 108 mM Na dtrate) was placed in the instrument-specific sample container. In each case 5 ^ of each dilution of the substance-dilution series was then mixed with the plasma provided. This plasma/inhibitor mixture was incubated at 37°C for 2 minutes. Thereafter, there were pipetted to the semi-automatic device (ACL, Automated Coagulation Laboratory (Instrument Laboratory)) 50 ^il of plasma/ inhibitor mixture in the measurement container. The dotting reaction was initiated by the addition of 0.1 ml of Innovin® (recombinant human tissue factor combined with caldum buffer and synthetic phosphoHpids( Dade Behring®, Inc.). The time up to the fibrin cross-linking was determined photoopticaUy from the ACL. The inhibitor concentration, which brought about a doubling of the PT dotting time, was determined by means of a graph. The Ki value of the active compounds of the present invention preferably amounts to about O.OOI to 50 jiM.espedally about O.OOI Co I fxM. The PT values preferably amount to about 1 to 100 |iM, espedaliy to about 1 to 10 (AM. The compounds of formxJa I and/or their pharmaceutically acceptable salts can be used as medicaments, e.g. in the form of pharmaceutical preparations for enteral, parenteral or topical administration. They can be administered, for example, perorally, e.g. in the form of tablets, coated tablets, dragees, hard and soft gelatine capsules, solutions, emulsions or suspensions, rectaUy, e.g. in the form of suppositories, parenterally, e.g. in the form of injection solutions or suspensions or infusion solutions, or topically, e,g. in the form of ointments, creams or oils. Oral administration is preferred. The production of the pharmaceutical preparations can be effected in a manner which will be ^miliar to any person skilled in the art by bringing the described compounds of formula I and/or their pharmaceutically acceptable salts, optionally in combination with other therapeutically valuable substances, into a galenical administration form together with suitable, non-toxic, inert, therapeutically compatible solid or liquid carrier materials and, if desired, usual pharmaceutical adjuvants. Suitable carrier materials are not only inorganic carrier materials, but also organic carrier materials. Thus, for example, lactose, com starch or derivatives thereof, talc, stearic acid or its salts can be used as carrier materials for tablets, coated tablets, dragees and hard gelatine capsules. Suitable carrier materials for soft gelatine capsules are, for example, vegetable oils, waxes, fets and semi-solid and liquid polyols (depending on the nature of the active ingredient no carriers might, however, be required in the case of soft gelatine capsules). Suitable carrier materials for the production of solutions and syrups are, for example, water, polyols, sucrose, invert sugar and the like. Suitable carrier materials for injection solutions are, for example, water, alcohols, polyols, glycerol and vegetable oUs. Suitable carrier materials for suppositories are, for example, natural or hardened oils, waxes, fats and semi-liquid or liquid polyols. Suitable carrier materials for topical preparations are glycerides, semi-synthetic and synthetic glycerides, hydrogenated oils, hquid waxes, Hquid paraffins, liquid fatty alcohols, sterols, polyethylene glycols and cellulose derivatives. Usual stabilizers, preservatives, wetting and emulsifying agents, consistency-improving agents, flavour-improving agents, salts for varying the osmotic pressm-e, buffer substances, solubilizers, colorants and masking agents and antioxidants come into consideration as pharmaceutical adjuvants. The dosage of the compounds of formula I can vary within wide limits depending on die disease to be controlled, the age and the individual condition of the patient and the mode of administration, and will, of course, be fitted to the individual requirements in each particular case. For adult patients a daily dosage of about 1 to 1000 iR2, especially about 1 to 100 mg, comes into consideration. Dependii^ on severity of the disease and the precise pharmacokinetic profile the compound could be administered with one or several daily dosage units, eg. in J to 3 dosage units. The pharmaceutical preparations conveniently contain about 1-500 mg, preferably 1-100 mg, of a compound of formula I. The following Examples serve to illustrate the present invention in more detail. They are, however, not intended to limit its scope in any manner. Examples Abbreviations BOP = (benzotriazol-l-yloxy)-tris-(diinethylamino)-phosphomiiin-hexaflnorophosphat, CAS = Chemical Abstract Services, DEAD = diethyl azodicarboxylate, DMF = dimethyl formamide, EDCI = l-[3-(dimethylamiiio)propyl]-3-ethyicarbodiiinide hydrochloride, EtOH = ethanol, HOST = l-hydroxybenzotriazole, MS = mass spectroscopy, MeOH = methanol, r.L = room temperature, THF = tetrahydrofiiran General Procedures General Procedure A: Conversion of an aromatic aldehyde into an aryl-a-alkosyacetic acid. To a stirred solution of the aldehyde (1 eq) andbromoform (1.27 eq) in the appropriate alkohol (MeOH or EtOH, 1 ml/mmol aldehyde) and dioxane (1 ml/mmol aldehyde) is added dropwise a solution of potassium hydroxyde (5 eq) in the appropriate alkohol (MeOH or EtOH, I ml/mmol aldehyde) for 15 min. For larger amounts a slight cooling is appUed. Stirring at r.L under an argon atmosphere is then continued for 18 - 48 h. The sohd is filtered off and washed with the appropriate alkohol. The filtrate is concentrated (rotavapor). The residue is taken up in water. The resiilting solution is washed with Et20 and acidified to pH 1 by dropwise addition of 3.0 N HCl. This is extracted with BtiO, dried (MgS04), filtered and concentrated (rotavapor). The crude product can be purified by chromatography (silicagel) or by crystallization. General Procedure 6: Coupling of an aryl-a-alkoxyacetic acid widi a primary amine using EDCI as a coupling reagent To a stirred solution of the amine (1 eq) in THF is added the acid (1.2 eq), triethylamine (1.2 eq) and EDCI (1.2 eq). HOST (1.2 eq) can also be added. The mixture is then stirred at r.t. under an argon atmosphere for 16 - 24 h. The mixture is diluted with EtOAc, washed with sat KHSO4 solution / water (1:1) and water; dried (MgS04), filtered and concentrated. The crude product can be purified by chromatography (silicagel) or by crystallization. General Procedure C: Coupling of an aryl-a-alkoxyacetic acid with a primary amine using BOP as a coupiing recent To a stirred solution of die amine (1 eq) in THF is added the add (1.5 eq), N-diisopropylamine (1.5 eq) and BOP-reagent (1.5 eq). The mixture is then stiirred at r.t under an argon atmosphere for 16 - 24 h. The mixture is diluted with EtOAc, washed with water, 1.0 N NaOH and brine; dried (MgS04), filtered and concentrated. The crude produrt can be purified by chromatography (silicagel) or by crystallization. Cjenerai Procedure D: Conversion of an aromatic nitrile into an amidine (Pinner reaction). Dry HCl gas is passed over a cooled (-10°C), stirred solution of the starting material in CHCls / EtOH (or MeOH) 5:1 for 15 min. The flask is stoppered and left at 4 "C overnight If conversion is not complete, the reaction mixture is allowed to warm to r.t. The mixture is concentrated (rotavapor and high vacutmi) at r.L The residue is dissolved in EtOH and treated with a 2.0 M NH3 solution in EtOH. The resulting mixture is stirred at r.t (sensitive compounds) or 60°C for 2 -18 h. The mixture is then concentrated (rotavapor) and purified by chromatography (silicagel). Example 1 1.1 (S)-(+)-Methoxyphenyiacetic add was coupled with 4-aminoraethyi benzonitrile (CAS No: 10406-25-4) according to general procedure C to give (S)-N-(4-cyano-benzyl)-2-methoxy-2-phenyl-acetamide as an off-white soUd. MS 281.2 ([M+H]"^) 1.2 (S)-N-(4-Cyano-ben2yl)-2-methoxy-2-phenyl-acetamide was converted to (S)-N-(4-carbamimido)^-benzyi)-2-methoxy-2-phen)d-acetamide hydrochloride according to general procedure D. Colorless solid. MS 298 ([M+H]'^) Example 2 2.1 (R)-(+)-Methoxyphenylacetic acid was coupled with 4-aminomethyl benzonitrile {CAS No: 10406-25-4} according to general procedure C to give (R)-N-(4-cyano-benzyI}-2-methoiy-2-phenyl-acetamideas an off-white solid. MS 281.1 ([M+H]"*") 2.2 {R)-N-(4-Cyano-benzyl)-2-metho3cy-2-phenyl-acetamide was converted to (R)-N-(4-carbamimidoyl-benzyi)-2-methoxy-2-phenyI-acetamide hydrochloride accordic^ to general procedure D. Colorless solid. MS 298.2 ([M+H]*) Example 3 3.1 4-Benzyloxybeti2aldehyde was converted to (RS)-(4-benzyioxy-phenyl)-methoxy-acetic add according to general procedure A. Off-white solid. MS 271.1 ([M-H]') 3.2 (RS)-{4-Ben2:)ioxy-phenyl)-inetliox7-acetic acid was coupled with 4-aminomethyl benzonitrile to give {RS)-2-(4-benzyloxy-phenyI)-N-(4-cyano-benzyi)-2-methoxy-acetamide according to general procedure B. Colorless solid. MS 387.3 ([M+H]'') 3.3 (RS)-2-{4-Benzyloxy-phenyi)-N-(4-cyano-benzyl)-2-methoxy-acetamide was converted to (RS)-2- (4-benzyloxy-phenyi) -N- (4-carbaniimido)d-benzjd)-2-methoxy-acetaimde hydrochloride according to general procedure D. Colorless foam. MS 404.5 ([M+H]"^) Example 4 4.1 4-PhenoxybenzaIdehyde was converted to (RS)-methoxy-(4-phenoxy-phenyl)-acetic add according to general procedure A. Yellow oil. MS 257.0 ([M-H]') 4.2 (RS)-Methoxy-(4-phenoxy-phenyl)-acetic add was coupled with 4-aminomethyl benzonitrile according to general procedure B to give (RS)-N-(4-cyano-benzyi)-2-methoxy-2-{4-phenoxy-phenyl)-acetamide. Colorless solid. MS 373.3 ([M+H]"^) 4.3 (RS)-N-(4-Cyano-benzyi)-2-methox7-2-(4-phenoxy-phen)^)-acetamide was converted to (RS )-N- (4-carbamimidoyi-benzyl) -2 -methoxy-2-(4-phenoxy-phen)4)-acetairude hydrochloride according to general procedure D. Colorless foam. MS 390.3 ([M-f-H]"^) Example 5 5.1 3-Phenoxybenzaldehyde was converted to (RS)-methoxy-(3-phenoxy-phenyI)-acetic add according to general procedure A. Light yellow liquid. 5.2 {RS)-Methoxy-(3-phenoxy-phenyl)-acetic add was coupled with 4-arQinomethyi benzonitxile accordmg to general procedure B to give (RS)-N-(4-cyano-benz7l)-2-methoxy-2-(3-phenoxy-phenyl)-acetainide. Light yellow oil. MS 373.3 {[M+H]"^) 5.3 (RS)-N-(4-Cyano-benzyl)-2-methoxy-2-(3-phenox)'-phenyl)-acetamide was converted to (RS)-N- (4-carbamimido)i-benzyl)-2 -methoxy-2- (3-phenoxy-phenyl)-acetaimde hydrochloride according to general procedure D. Colorless amorphous soHd. MS 390.3 ([M+H]^) Example 6 6.1 Benzaldehyde was converted to (RS)-ethoxy-phenyl-acetic add according to general procedure A. Light yellow liquid. 6.2 (RS)-Ethoxy-phenyl-acetic acid was coupled with 4-aminometh5d benzonitrile according to general procedure B to give (RS)-N-(4-cyano-benzyl}-2-ethoxy-2-phenyi-acetamide. Light yellow semisolid. MS 295.3 ([M+H]"') 6.3 (RS)-N-(4-Cyano-benz)d)-2-ethoxy-2-phenyl-acetainide was converted to (RS)-N-(4-carbaniimxdoyl-benzyl}-2-ethoxy-2-phenyi-aeetamide hydrodiloride according to general procedure D. Colorless amorphous solid. MS 312.2 ([M+H]"*^) Example? 7.1 2-Fluorobenzaldehyde was converted to CRS)-(2-fluoro-phenyl)-methoxy-acetic acid according to general procedure A. Off-white amorphous solid. MS 1S2.9 ([M-H]") 7.2 (RS)-(2-Fluoro-phenyI)-methoxy-acetic add was coupled with 4-aniinometh)^ benzonitrile according to general procedure B to give {ES)-N-(4-cyano-benzjd)-2-(2-fluoro-phenyl)-2-methoxy-acetamide. Colorless oil. MS 299.2 ([M+H]"^) 73' (RS)-N-(4-Cyano-ben2yl)-2-(2-fIuoro-phenyl)-2-methoxy-acetamide was converted to (RS)-N-(4-carbami[nidoyI-benz)d)-2-(2-fluoro-phenyl)-2-methQxy-acetaniide hydrochloride according to general procedure D. Colorless foam. MS 316.2 ([M+H]"*") Examples 8.1 3-Benzyloxybeiizaldehyde was converted to (RS)-(3-ben2yloxy-phen)i)-methoxy-acetic add according to genera! procedure A. Colorless solid. 8.2 {RS)-(3-Benzyloxy-phen)d)-methoxy-acetic acid was coupled with 4-aminomethyl benzonitrile according to general procedure B to give (RS)-2-(3-ben2yloxy-phenyl)-N-(4-cyano-benzyl)-2-methoxy-acetaniide. Light yellow oil. 8.3 (RS)-2-(3-Ben2:)doxy-phenyl)-N-(4-cyano-benzyi)-2-niethoxy-acetainide was converted to (RS) -2' (3-benzyloxy-phenyi)-N- (4-carbaminiidoyl-ben2)d)-2-niethoxy-acetamide hydrochloride according to general procedure D. Colorless amorphous soUd. MS 404.5 ([M+H]") Example 9 9.1 As a side product of the synthesis of (RS)-2-(3-benzyloxy-phen)i)-N-(4-carbaininiido)^- benzyl)-2-methoxy-acetainide hydrochloride (example 8.3) there was obtained (RS)-N-(4- carbaminiidoyl-ben2;)d)-2-(3-hydroxy-phenyl)-2-methoxy-acetamide hydrochloride. Colorless amorphous solid. MS 314.2 ([M+H]^) Example 10 10.1 To a stirred solution of 3-mtrobenza!dehyde (4.043 g) at r.t. in 190 ml CH2C12 Was added Znl: (0.427 g). The mixture was purged with N2 and cooled to 0°C. Trimethylsilyl cyanide (2.92 g as a solution in 10 ml CH2CI2) was then added dropwise to the mixture for 15 min. The mixture was then allowed to warm to room temperature and stirrii^ was continued for 16 h. Water (250 ml) was then added to the mixture. The layers were separated and the aqueous phase was ractracted with CH2CI2 (125 ml). The combined organics were washed with water (125 ml) and brine (125 ml), dried (MgS04), filtered and concentrated (rotavapor) to leave the crude (RS)-(3-nitro-phenyl)-trimeth^silanyloxy-acetonitrile (6.56 g) as an orange oil which was used in the next step without further purification. 10.2 (RS)-(3-Nitro-phenyl)-trimeth)4silanyloxy-acetoiutrile (6.30 g) was dissolved in concentrated HQ with stirring. The mixture was then refluxed for 3 h. After cooling to room temperature, the yellow solution was poured into 200 g of crushed ice. This was extracted with Et20 (150 ml + 150 ml + 150 ml). The combined organics were washed with water (200 ml) and brine (200 ml), dried (MgS04), filtered and concentrated (rotavapor) to leave a yellow solid. This solid was triturated m a mixture of n-hexane (20 ml) and Et20 (2 ml), collected by filtration and washed with n-hexane to give (RS)-hydroxy-(3-nitro-phenyl)-acetic acid as a light yellow soUd (4.56 g). 103 A mixture of (RS)-hydroxy-(3-nitro-phenyl)-acetic acid (1.054 g), A&O (2.478 g) and Mel (2.304 g) was heated to reflux in toluene (10 ml). Stirring was then continued for 3 h. After cooling to r.t., the soUd was filtered off and washed with EtOAc. The filtrate was concentrated (rotavapor) to leave the crude (RS)-methoxy-(3-mtro-phen}d)-acetic acid methyl ester (1.161 g) as a light yellow oil. 10.4 A mixture of (RS)-methoxy-(3-nitro-phenyl)-acetic acid methyl ester (1.039 g) and NaOH (0.239 g) in water (0.75 ml) and methanol (10 ml) was stirred at 0°C for 4.5 h. The reaction mianjre was then concentrated (rotavapor, high vac.) and the residue (light yellow soHd) was taken in water (25 ml). The resulting solution was acidified to pH ~ 1 by dropwise addition of 3.0 N HCl. This was extracted with EtOAc (50 ml + 25 ml). The combined organics were dried (MgS04), filtered and concentrated (rotavapor) to leave the crude (RS)-methoxy-(3-nitro-phenyl)-acetic acid (0.944 g) as a Hghtyellow sohd. 10.5 (RS)-Methoxy-(3-mtro-phenyl)-acetic acid was coupled with 4-aminomethyi benzonitrile according to general procedure C to give (RS)-N-(4-cyano-benzyl)-2-methoxy-2-(3-nitro-phenyl)-acetamide. Light yellow gum. 10.6 (RS)-N-(4-Cyano-benz)d)-2-melhoxy-2-(3-mtro-phenyl)-acetaiiiide was converted to (RS )-N-(4-carbaimmidoyl-benzyl)-2-methoxy-2-(3-nitro-phen5d) -acetamide hydrochloride according to general procedure D. Off-white solid. MS 343.2 ([M+H] '^) Example 11 11.1 4-Biphenylaldehyde was converted to (RS)-biphenyl-4-yI-methoxy-acetic acid according to general procedure A. Light brown solid. 11.2 (RS)-Biphenyl-4-yl-methoxy-acetic acid was coupled with 4-aiiunometh)i benzonitrile according to general procedure C to give (RS)-2-biphenyl-4-yl-N-(4-cyano-ben2yI)-2-methoxy-acetamide. Light yellow soUd. U.3 {RS)-2-Biphen)d-4-yl-N-(4-cyano-benzyl)-2-methoxy-acetamide was converted to (RS)-2- biphenyI-4-yl-N-(4-carbaininiidoyl-benzyl)-2-raethoxy-acetanude hydrochloride according to general procedure D. Off-white soUd. MS 374.4 ([M+H]*) Example 12 12.1 Piperonal was converted to (RS)-ben2o[l,3]dioxcl-5-yl-methoxy-acetic acid according to general procedure A. Orange oil. 12.2 (RS)-Benzo[l,3]dioxol-5-yl-methoxy-acetic add was coupled with 4-aniinometh)i ben20nitrile according to general procedure C to give (RS}-2-benzo[l,3]dioxo}-5-y]-N-(4-cyano-benzyl)-2-methoxy-acetanude. Light yellow solid. 12.3 (RS)-2-Benzo[l,3]dioxoi-5-yi-N-{4-cj^no-benzyi}-2-methoxy-acetomde vras converted to (RS)-2-benzo[l,3]dioxol-5-)d-N-(4-carbainimidoyl-benz)4)-2-niethoxy-acetaimde hydrochloride according to general procedure D (Pinner reaction in EtOH/CHQg as a solvent). OfF-white soHd. MS 342.2 ([M+H]"") Example 13 13.1 As a side product of the synthesis of {RS)-2-ben2o[l,3]dioxoI-5-)d-N-(4-carbaniiinidoyl-ben2yI)-2-methoxy-acetaimde hydrochloride (example 12.3) there was obtained (RS)-2-benzo[l,3]dioxol-5-yI-N-(4-carbamiinidoyl-benz)^)-2-ethoxy-acetaniide hydrochloride. Light brown solid. MS 356.3 ([M+H]"^) Example 14 14.1 5-Ethoxy-2-fluoro-3-(l-methyl-piperidin-4-)doxy)-benzaldehyde was converted to (RS)- [5-ethoxy-2-fluoro-3-(I-methyl-piperidin-4-yloxy)-phenyl]-methoxy-acetic acid according to general procedure A. Off-white solid. MS 342.2 ([M+H]^) U.2 (RS)-[5-Ethoxy-2-fluoro-3-(l-methyl-piperidm-4-yloxy)-phenyi]-methoxy-aceticadd was coupled with 4-aminomethyt benzonitrile according to general procedure B to give (RS)-N-(4-cyano-benzyl)-2-[5-ethoxy-2-fiuoro-3-(l-inethyl-piperidin-4-yloxy)-phenyi]-2-methoxy-acetamide. Colorless foam. MS 456.5 ([M+H]'*') 14.3 (RS}-N-(4-Cyano-benz)i)-2-[5-ethoxy-2-£luoro-3-(i-methyI-piperidin-4-yloxy)-phen)d]- 2-methoxy-acet2inide was converted to (RS)-N-(4-carbamiinidoyl-benzyl)-2-[5-ethoxy-2- fluoro-3-{l-methyI-piperidin-4-yIoxy)-pfaenyi]-2-methoxy-acetamide hydTochloride according to general procedure D. Colorless foam. MS 473.5 {[M+H]"*") Example 15 15.1 2-Fluoro-4-methoxybenzaldehyde was converted to {RS)-(2-fluoro-4-methoxy-phenyl)- methoxy-aceticaddaccordingtogeneralprocedure A, Light yellow oil. MS 213.4 ([M-H]") 15.2 (RS)-(2-Fluoro-4-methoxy-phenyl)-methoxy-acetic add was coupled with 4-anunomethyl benzonitrile according to general procedure B to give (RS)-N-(4rCyano-benzyl)-2-(2-£luoro-4-methoxy-phen)4)-2-inethosy-acetamide. Colorless oil. MS 329.2 {[M+H]"^) 15.3 {RS)-N-(4-Cyano-benzyl)-2-(2-fluoro-4-methoxy-phenyl)-2-methoxy-acetanude was converted to (RS)-N-C4-carbamimidoyl-benzyi)-2-(2-fluoro-4-methoxy-phenyl)-2-methoxy-acetamide hydrochloride according to general procedure D. Colorless foam. MS 346.4 ([M+H]"") 15.4 (RS)-N- (4-CarbaniiinidoyI-benzyI) -2- (2-fluoro-4-methoxy-phenyl)-2-niethoxy-acetainide hydrochloride (example 15.3,200 mg) was dissolved in DMF (2.2 ml). The flask was placed in an ice bath. Ethyl chloroformate (58 mg) and triethylamine (160 mg) were added dropwise. The reaction mixture was stirred for 1.5 h at 0 "C. Ethyl acetate (30 ml) and ice water (40 ml) were added and the mixture was extracted with eth-jd acetate. The organic phase vtfas washed with water, dried, filtered and evaporated. The product was purified by chromatography (silic^el, ethylacetate) to give (RS)-[amino-(4-i[2-(2-fluoro-4-methoxy-phenyl)-2-niethoxy-acet)iamino]-methjd}-phenyl)-methyIene]-carbainic add ethyl ester (218 mg) as a colorless amorphous solid. MS 418.3 ([M+H]*) 15.5 (RS)-N-(4-Cyano-benzyi)-2-(2-fluoro-4-rnethoxy-phenyl)-2-inethoxy-acetamide (example 15.2, 251 mg) was dissolved in methanol (7 ml).Hydroxylaimne hydrochloride (212 mg) and triethyiamine (618 mg) were added. The mixture was stirred for 19 h at r.L The solvent was evaporated. The residue was dissolved in methylene chloride, washed with water, dried and filtered. The solvent was evaporated to give (RS)-2-(2-fluoro-4-methox7-phenyl)-N-[4-(N-hydroxycarbainimidoyl)-benzyl]-2-methoxy-acetamide (269 mg) as an off-white foam. MS 362.2 ([M+H]*) 15.6 (RS)-N-(4-Cyano-benzyl)-2-(2-fluoro-4-methoxy-phen)4)-2-methoxy-acetamide (example 15.2, 285 mg) was dissolved in methanol (0.7 ml) and chloroform (3.3 ml). The mixture was placed in an ice-NaCl bath. Dry HCl gas was passed over the reaction mixture for 15 min. The flask was stoppered and left overnight at 4 °C. The mixture was concentrated (rotavapor and high vacuum) at r.t The residue was dissolved in methanol (i.9 ml). Hydrazine hydrochloride (66 mg) and triethyiamine (264 mg) were added. The mixture was stirred ovemighL The solvent was evaporated and the product was purified by chromatography (silica gel, CH2CI2 => CH2Cl2/MeOH 4:1) to give RS)-2-(2-fluoro-4-methoxy-phenyl)-N-[4-(N-aniinocarbaniimidoyl)-benzyi]-2-methoxy-acetamide (205 mg) as an off-white foam. MS 361.2 ([M+H]^) Example 16 16.1 3-Ben2yloxy-4-methoxy-benzaldehyde was converted to (RS)-(3-benzyloxy-4-methoxy- phenyl)-raethoxy-acetic add according to general procedure A. Orange solid. 16.2 To a stirred solution of (RS)-(3-benzyloxy-4-methoxy-pheni4)-methoxy-acetic add (0.923 g) at T,t. in ethanol was added 10% Pd/C. The mixture was then stirred at i.t. under a hydrogen atmosphere for 17 h. The catalyst was filtered off and washed with dichloromethane. The filtrate was concentrated (rotavapor) to give (RS)-(3-hydroxy-4-methoxy-phen)d)-methoxy-acetJc add (0.642 g) as an orange gum. 16.3 (RS}-(3-Hydroxy-4-methoxy-phenyl)-methoxy-acetic add was coupled with 4-aminomethyl benzonitrile according to general procedure C to give (RS)-N-(4-cyano-benzyl}-2-(3-hydroxy-4-methoxy-phenyl)-2-methoxy-acetamide. White foam. 16.4 To a stirred solution of (RS)-N-(4-cyano-benzyl)-2-(3-hydroxy-4-methoxy-phenyl)-2-methoxy-acetamide (0.303 g) at r.t. in DMF {3 ml) were added KsCOs (0.14 g) and ethyl bromoacetate (0.169 g). The reaction mixture was then stirred at r.L under an argon atmosphere for 5 h 45. The mixture was diluted with EtOAc (25 ml), washed with water (25 ml) and brine (25 ml), dried (MgS04), filtered and concentrated (rotavapor) to leave the crude product as a light yellow gum. The product was purifiied by chromatography (Siiicagel (20 g) using a gradient profile: cyclohexane to cyclohexane / EtOAc 35:65) to give (RS)-(5-[(4-cyano-ben2)4carbamoyl)-methoxy-methyl]-2-methoxy-phenoxy}-acetic add ethyl ester (0.342 g) as a white solid. 16.5 (RS)-{5-[(4-Cyano-benz>dcarbarnoyI)-metboxy-methyl]-2-metiioxy-phenoxy}-acetic add ethyl ester was converted to (RS)-{5-[(4-carbamiinidoyl-ben2ylcarbamoyi)-methoxy-methyl]-2-methoxy-phenoxy}-acetic add methyl ester hydrochloride according to general procedure D. OfF-white soUd. MS 416.3 ([M+H]^) Example 17 17.1 As a side product of the synthesis of {RS)-{5-[(4-carbamimidoyi-benzy/carbamoyi)- methoxy-methyl]-2-methoxy-phenoxy}-acetic add methyl ester hydrochloride (example 16.5) there was obtained (RS)-N-(4-carbamimidoyi-ben2yl)-2-(3-carbamoj4methoxy-4- methoxy-phenyl)-2-methoxy-acetamide hydrodiloride. Off-white solid. MS 401.5 ([M+H]^) Example 18 I8.I 3-Benzyloxy-4-methoxy-ben2aldehyde was converted to (RS)-(3-benz)4oxy-4-methoxy- phenyl)-etiio]9^-acetic add according to general procedure A. Light yellow soHd. 18.2 To a stirred solution of (RS)-(3-benzyloxy-4-m^oxy-phenyl}-ethoxy-acetic acid (0.801 g) at r.t in ethanol was added 10% Pd/C (0.1 g). The mixture was then stirred at r.t. under a hydrogen atmosphere for 17 h. The catalyst was filtered off and washed with dichlorometiiane. The filtrate was concentrated (rotavapor). The residue was purified by chromatography to give (RS)-ethoxy-(3-hydroxy-4-methoxy-phenyl)-acetic acid (0.250 g) as a light yellow gum. 18.3 (RS)-Ethoxy-(3-hydroxy-4-metlioxy-plienyl)-acetic add was coupled with 4-aminomethyl benzonitrile according to genera] procedure C to give CRS)-N-(4-cyano-benzyi)-2-ethoxy-2-(3-hydroxy-4-methoxy-phenyl)-acetamide. Light yellow gum. 18.4 To a stirred solution of (RS)-N-{4-cyano-beiizyl)-2-ethoxy-2-(3-hydroxy-4-methoxy-phenyD-acetamide (0.158 g) at r.L in DMF (1.5 ml) were added K2CO3 (0.067 g) and ethyl bromoacetate (0.081 g). The reaction mixture was then stirred at r.t under an argon atmosphere for 24 h. The mixture was diluted with EtOAc (10 ml), washed with water (10 ml+10 ml) and brine (10 ml), dried (MgSO^), filtered and concentrated (rotavapor). The product was purified by chromatography (Sihcagel (20 g) using a gradient profile: cydohexane to cyclohexane / EtOAc 45:55) to give (RS)-{5-[(4-cyano-benz)dcarbamoyl)-ethoxy-methyl]-2-methoxy-phenoxy}-acetic acid eth)d ester (0.160 g) as a colorless gum. 18.5 (RS)-{5-[(4-Cyano-benzylcarbamoyl)-ethoxy-methyi]-2-methoxy-phenoxy}-acetic add ethyl ester was converted to (RS)-{5-[(4-carbaniimido)d-benzylcarbamoyl)-ethoxy-methyl]-2-methoxy-phenoxy^}-acetic add ethyl ester hydrochloride according to general procedure D. OfF-white solid. MS 444.4 ([M+Hf) Example 19 19.1 As a side product of the synthesis of (RS)-{5-[(4-carbamimidoyI-benzyIcarbamoyi}-ethoxy-methyl]-2-methoxy-phenoxy}-acetic add ethyl ester hydrochloride (example 18.5) there was obtained (RS)-N-(4-carbamimidoyl-ben2yi)-2-(3-carbamo)dmethoxy-4-methoxy-phenyi)-2-ethoxy-acetamidehydrochloride. Off-white solid. MS 415.4 ([M+H]"^) Example 20 20.1 To a stirred suspension of (RS)-{5-[(4-carbamimidoyl-benz)4carbamoyl)-ethoxy-methyl]-2-methoxy-phenoxy}-acetic add ethyl ester hydrochloride (example 18.5, 0.045 g) at r.L in THE (1 ml) and water (0.5 ml) was added 1.0 N NaOH (0.2 ml). The mixture was then stirred at r.L under an argon atmosphere for 3 h. The mixture waa addified to pH 5-6 by addition of 1.0 N HCl. The THF was removed (rotavapor) and the product predpitated out from the remaining water. It was collected by filtration, washed with water and cydohexane and dried overnight under high vacuum to give (RS)-{5-[{4-carbaniiniidoyI- benzylcarbaiaoyl)-ethoxy-methyI]-2-methosy-plienoxy}-acetic add (0.027 g) as a white powder. MS 416.3 {[M+H]"") Example 21 21.1 (RS}-(4-Benzyloxy-phenyl)-inethoxy-acetic add (example 3.1) was hydrogenated at r.t. and normal pressure using 10% Pd/C as a catalyst and EtOH as a solvent to give (RS)-(4-hydroxy-plienyl)-methoxy-acetic add as a light grey solid. MS 181.4 ([M-H]') 21.2 (RS)-(4-Hydroxy-phenyi)-methoxy-acetic add was coupled with 4-aniinometh.yl benzonitrile according to general procedure B to give (RS)-N-(4-cyano-benzy]}-2-(4-hydroxy-phenyl)-2-metlioxy-acetamide. Colorless foam. MS 295.2 ([M-H]") 21.3 In analogy to example 16.4, (RS)-N-(4-cyano-ben2yi)-2-(4-hydroxy-phenyl)-2-methoxy-acetamide was alkylated with ethyl iodide / cesium carbonate in DMF to give (RS)-N-(4-cyano-benz)^)-2-(4-ethoxy-phenyl)-2-methoxy-acetainide as a colorless soHd. MS 325.3 ([M+H]^) 21.4 (RS)-N-(4-Cyano-ben2)^)-2-(4-ethoxy-phenyl)-2-methoxy-acetamide was converted to (RS)-N-(4-carbaminiido)d-benzyl)-2-ethoxy-2-(4-ethoxy-phenyl)-acetamid hydrochloride according to general procedure D using EtOH/CHCls as a solvent. OfF-white amorphous soUd. MS 365.3 ([M+H]"^) Example 22 22.1 (RS)-N-(4-Cyano-ben2yI)-2-(4-hydroxy-phenyl)-2-methoxy-acetamide (example 21.2, 0.406 g) was dissolved in THF (12 ml). Triphenylphosphine (0.539 g) and 4-hydroxy-N-methylpiperidine (0.237 g) were added. The reaction mixture was cooled to 0 *C. Slowly, DEAD (0.384 g) was added. The reaction mixture was stirred at 0 °C for 30 min and at r.L for 5 days. The solvent was evaporated and the product vras purified by chromatography (siHcagel, mobile phase: gradient from CH2CI2 to CH2a2/MeOH 4:1) to give (RS)-N-(4-cyano-benz}d)-2-methoxy-2-[4-(l-meth)^-piperidin-4-yloxy)-phen-)4]-acetamide as a colorless foam (0.241 g). MS 394.4 (fM+H]"") 22^ (RS)-N-(4-Cyano-beDzy])-2-inethoxy-2-[4-(l-meth)d-piperidin-4-yloxj')-phenyl]- acetamide was converted to {RS)-N-(4-carbamiimdoyi-benzyl)-2-methoxy-2-[4-(l-metfayI-piperidin-4-yloxy)-phenyl]-acetarmde hydrochloride according to general procedure D. Colorless foam. MS 411.4 ([M+HJ^ Example 23 23.1 (+/-}-a-Methoxy-alpha-trifluoromethyl phenylacetic add was coupled with 4-aminometh)^ benzonitrile according to general procedure C to give (RS)-N-(4-cyano-benzyl)-3,3,3-trifluoro-2-methoxy-2-phenyl-propionamide. Off-white solid. 23.2 (RS)-N-(4-Cyano-benzyi)-3,3,3-trifluoro-2-methoxy-2-phenyi-propionainide was converted to (RS)-N-(4-carbamimidoyl-benzyl)-3,3,3-tri0.uoro-2-methoxy-2-phenyl- propionamide hydrochloride according to general procedure D. White solid. MS 366.2 ([M+H]^) Example 24 24.1 6-Fiuorveratraidehyde was converted to (RS)-(2-fIuoro-4,5-diinethoxy-phenyl)-methox)'- acetic add according to general procedure A. Light yellow oil. MS 243.1 ([M-H]"} 24.2 (RS)-(2-Fluoro-4,5-dimethoxy-phenyl)-methoxy-acetic add was coupled with 4- aminometbyl benzonitrile according to general procedure B to give (RS}-N-{4-cyano- benzyl)-2-(2-fluoro-4,5-dimethoxy-phenyl)-2-methoxy-acetamide. Red foam. MS 359.2 ([M+H]^) 24.3 (RS)-N-(4-Cyano-benzyl)-2-(2-fluoro-4,5-dimethoxy-phenyi)-2-niethoxy-acetamide was converted to (RS)-N-{4-carbamimidoyl-benz5d)-2-{2-fluoro-4,5-dimethoxy-phen)d)-2-methoxy-acetamide hydrochloride according to general procedure D. Orange solid. MS 376.4 ([M+H]"") Example 25 25.1 (RS)-(3-Beuzyloxy-phen)^)-methoxy-acetic add (example 8.1) was hydrogenated at r.t. and normal pressure using 10% Pd/C as a catalyst and EtOH as a solvent to give (RS)-(3-hydroxy-phen)d}-methoxy-acetic add as a colorless foam. 25.2 (RS)-( 3-Hydroxy-phenyl)-medioxy-acetic add was coupled -with 4-anunomethyl benzonitrile according to general procedure B to give (RS)-N-(4-cyano-benzyl)-2-(3-hydroxy-phenyl)-2-methoxy-acetamide. Colorless oil. 25.3 In analogy to example 16.4, (RS)-N-(4-c)'ano-benzyi)-2-(3-hydroxy-phenyi)-2-methpxj'-acetamide was alkylated with 2-iodopropane / cesium carbonate in DMF to give (RS)-N-(4-cyano-benzyl)-2~(3-isopropoxy-phenyl)-2-methox7-acetainide as a colorless oil. MS 339.2 {[M+H]'*') 25.4 (RS)-N-{4-Cyano-ben2yi)-2-(3-isopropoK7-phen)d)-2-methoxy-acetarmde was converted to (RSJ-N-(4-carbainimidoyl-benzyl}-2-(3-isopropoxy-p£ienyI}-2-methoxy-acetaimde hydrochloride according to general procedure D. Colorless amorphous solid. MS 356.3 ([M+H]^) Example 26 26.1 In analogy to example 22.1, (RS)-N-{4-cyano-benz)d)-2-{4-hydrQxy-phenyl)-2-methoxy-acetamide (example 21.2) was reacted with cyclopentanol, triphen)dphosphine and DEAD in THF. Further conversion according to general procedure D gave (RS)-N-(4-carbamimidoyl-benzyl)-2-(4-cyclopentyioxy-phenyI)-2-methoxy-acetamide hydrochloride as a Hght yellow sohd. MS 282.3 ([M+H]^) Example 27 27.1 In analogy to example 16.4, (RS)-N-(4-cyano-benzyI)-2-{4-hydroxy-phen)d)-2-methoxy-acetamide (example 21.2) was alkylated with 2-iodopropane / cesium carbonate in DMF to give (RS)-N-(4-cyano-benzyl)-2-(4-isopropoxy-phen>^)-2-methoxy-acetamide as a colorless solid. MS 339.2 ([M-KH]*) 27.2 (RS)-N-(4-Cyano-benzyi)-2-(4-isopropoxy-phenyi)-2-metfaoxy-acetamide was converted to (RS)-N-(4-carbamiinidoyl-benzyl)-2-(4-isopropoxy-phenyI)-2-methox7-acetamide hydrochloride according to general procedure D. Colorless foam. MS 356.3 ([M+H]"*") Example 28 28.] In analogy to example I6.4, (RS)-N-{4-cyano-benzyl)-2-(4-liydroxy-phenyl)-2-methoxy-acetamide (example 21.2) was alkylated with ethylbromoacetate / cesium carbonate in DMF to give (RS)-{4-[(4-cyano-benzylcarbamoyl)-methoxy-methyl]-phenoxy}-acetic add ethyl ester as a colorless solid. MS 383.3 {[M+H]'^) 28.2 (RS)-{4-[(4-Cyano-ben2)4carbaino)d)-metlioxy-methyI]-phenoxy}-acetic acid ethyl ester was converted to CIlS)-{4-[(4-carbamiinidoyl-benzylcarbanioyl)-methoxy-methyl]-phenoxyj-acetic acid methyl ester hydrochloride according to general procedure D using MeOH/CHCl3 as a solvent Colorless foam. MS 386.3 ([M+H]^) Example 29 29.1 In analogy to example 20.1, (RS)-|4-[(4-carbaminiidoyi-ben2ylcarbamoyI)-methoxy-methyi]-phenoxy}-acetic acid methyl ester hydrochloride (example 28.2) was hydrolyzed to (RS}-{4-[(4-carbamimidoyl-benzylcarbamoyi)-methoxy-methyl]-phenoxyl-acetic add. Colorless soUd. MS 370.2([M-H]') Example 30 30.1 In analogy to example 22.1, (RS)-N-(4-cyano-benzylJ-2-(3-hydroxy-phenyi)-2-methoxy-acetamide (example 25.2) was reacted with tetrahydro-2H-pyran-4-ol, DEAD and triphen^dphosphine in THE and subsequently converted into (RS)-N-(4-carbamimidoyl-benzyi)-2-methoxy-2-[3-(tetrahydro-pyran-4-yloxy)-phenyl]-acetamide hydrochloride according to general procedure D. Colorless amorphous solid. MS 398.4 ([M+H]"^) Example 31 31.1 3,5-Diethoxy-2-fluoro-ben2aldehyde (CAS 277324-21-7) was converted to (RS)-(3,5- diethoxy-2-fluoro-pbenyi)-methoxy-acetic add according to general procedure A Yellow oil MS 271.1 ([M-H]") 31.2 (RS)-(3,5-Diethoxy-2-fluoro-phenyi)-methoxy-acetic acid was coupled with 4- aminomethyl benzonitrile according to general procedure B to give (RS)-N-(4-cyano- benzyl)-2-{3,5-diethoxy-2-fluoro-phen)d)-2-methoxy-acetaimde. Light yellow oil. MS 387.3 ([M+H]^) 31.3 (RS}-N-(4-Cyano-benz7l)-2-(3,5-diethoxy-2-fluoro-phen^)-2-methoxy-acetamide was converted to (RS)-N~{4-carbamimidoyi-beiizyl)-2-(3,5-diethoxy-2-fluoro-phenyl)-2-methoxy-acetamide hydrocHoride according to general procedure D. Light brown foam. MS 404.5 ([M+H]"*") Example 32 32.1 5-Ethoxy-2-fiuoro-4-(2-hydroxy-ethoxy)-benzaIdehyde (CAS 376600-66-7) was converted to {RS)-[5-ethoxy-2-fiuoro-4-(2-hydroxy-ethoxy)-phenyI]-tuethoxy-acetic add according to general procedure A. Yellow oil. MS 287.0 ([M-H]") 32.2 {RS)-[5-Ethoxy-2-fluoro~4-(2-hydrojq'-ethoj^)-phenyl]-metho39'-acetic add was coupled with 4-aminoinethyl benzonitrile according to general procedure B to give (RS)-N-(4-cyano-ben2yl) -2- [ 5-ethoxy-2-fluoro-4- (2-hydroxy-ethoxy)-phenyl] -2-medioxy-acetaniide. Light yeCow oil. MS 403.4 ([M+H]"*") 32.3 (RS)-N-(4-Cyano-benzyi)~2-[5-ethoxy-2-fluoro-4-(2-hydroxy-ethoxy)-phenTd]-2-methoxy-acetamide was converted to (RS)-N-(4-carbamiinido)d-ben27l)-2-[5-ethoxy-2-fluoro-4-(2-hydroxy-ethoxy)-phenyl]-2-methoxy-acetamide hydrochloride according to general procedure D. Off-white foam. MS 420.3 ([M+H]'*') Example 33 33.1 3,4-Diethoxy-2-fluoro-ben2aldehyde was converted to (RS)-(3,4-diethoxy-2-fluoro- phenyI)-methoxy-acetic add according to general procedure A, Yellow oil. MS 27L1 {[M- H]-) 33.2 (RS)-(3,4-Diethoxy-2-fluoro-phenyl)-methoxy-acetic acid was coupled with 4- aminomethjd benzonitrile according to general procedure B to give (RS)-N-(4-cyano- ben2yl)-2-C3,4-diethoxy-2-fiuoro-phen)d)-2-methoxy-acetamide. Colorless solid. MS 387.3 ([M+H]") 33.3 (RS)-N-(4-Cyano-benzyl)-2-(3,4-diethoxy-2-fluoro-phenyl)-2-methoxy-acetainide was converted to (RS)-N-(4-carbamimidoyl-beiizyl)-2-(3,4-diethoxy-2-fIuoro-plienyi)-2-metboxy-acetamide hydrochloride according to general procedure D. Colorless foam. MS 404.5 ([M+H]-") Example 34 34.1 4-(Bromomethyl)-3-fluoroben2omtrile (CAS 105942-09-4, 21 g) was dissolved in DMF (90 ml). Phthalimide potassium salt (19.64 g) was added and the mixture was stirred for 9 h at 130 °C. After cooling to r.t., the naixture was poured on ice. The solid was filtered off. Ethyl acetate and water were added and extracted with ethyl acetate. The organic phase was washed with water, dried, filtered and evaporated to give a light brown solid (14.1 g, 42 % pure as judged by NMR). This sohd was suspended in ethanol (50 ml), A solution of hydrazine in water (24%, 15 ml) was added and the mixture was refluxed for a total of 14 h. The mixture was filtered and the solvent was evaporated. Tlie product was purified by chromatography (silica gel, CH2CI2 => CH2Cl2/MeOH 4:1) to give 4-aminomethyl-3-fluoro-benzonitrile (0.63 g) as a brown oil. 34.2 CRS)-(2-Fluoro-4-methoxy-phen)d)-methoxy-acetic acid (aample 15.1) was coupled with 4-aminomethyl-3-fluoro-benzonitrile according to general procedure B to give (RS)-N-(4-cyano-2-fluoro-benzyi)-2-(2-fiuoro-4-methoxy-phenyl)-2-metiioxy-acetamide. Yellow oil. MS 347.3 ([M+H]') 34.3 (RS) -N- (4-Cyano-2-fluoro-benz}4}-2 - (2-fluoro-4-methoxy-phen)1) -2-methoxy-acetamide was converted to (RS)-N-(4-carbanumidoyl-2-fluoro-benzyl)-2-(2-fluQro-4-methoxy-phen7])-2-inethoxy-acetajiiide hydrochloride according to general procedure D. Off-white amorphous soHd. MS 364.2 ([M+H]"") Example 35 35.1 (RS)-(2-FIuoro-4-inethoxy-phen)^)-methoxy-acetic add (example 15.1) was coupled with 4-aminomethyl-2-fluorobenzonitrile (CAS 368426-73-7) according to general procedure B to give (RS)-N-(4-cyano-3-fluoro-benzyl)-2-(2-£luoro-4-methoxy-phenyl)-2-methoxy-acetamide. Light yellow solid. MS 347.3 ( [M+HD 35.2 (RS )-N-(4- Cyano-3 -fluoro-beiizyl)-2- {2-fluoro-4-inethoxy-phenyl)-2-methoxy-acetamide was converted to (RS)-N-(4-carbaimmido-;^-3-fluoro-ben2yl)-2-(2-fluoro-4-methoxy-phenyl)-2-methoxy-acetaimde hydrochloride according to general procedure D. Off-white amorphous solid. MS 364.2 ([M+H]^) Example 36 36.1 2,4-Bis-(trifluoromelhyl)benza]dehyde was converted to (RS)-(2,4-bis-trifluoromethyl-phenyi)-methoxy-acetic acid according to general procedure A. White solid. 36.2 {RS)-(2,4-Bis-trifluoromeihyi-phenyl)-methoxy-acetic acid was coupled with 4-aminomethyl benzonitrile according to general procedure C to give (RS)-2-(2,4-bis-trifluoromethyl-phenyl)-N-{4-cyano-benzyl)-2-methoxy-acetamide. Colorless gum. 36.3 (RS)-2-(2,4-Bis-trifluoromethyI-phenyl)-N-(4-cyano-benz>i)-2-methoxy-acetaniide was converted to (RS)-2-(2,4-bis-trifluorometh)4-phenyi)-N-(4-carbainiinidoyl-benzyl)-2-methoxy-acetamide hydrochloride according to general procedure D. Off-white solid. MS 434.4 ([M+H]^) Example 37 37.1 2-BenzyIoxy-4-methoxy-benzaldehyde (CAS 32884-23-4) was converted to (RS)-(2-benzyioxy-4-metlioxy-phenyI)-methoxy-acetic add according to general procedure A. Light yeUow oil. MS 301.1 ([M-H]') 37.2 In analogy to example 16.2, (RS)-(2-ben2yloxy-4-methoxy-phenyi}-methoxy-acetic acid was hydrogenated to give (RS)-(2-hydroxy-4-inethoxy-phen^)-methoxy-acetic acid. Purple soUd. MS 211.0 ([M-H]') 37.3 (RS)-(2-Hydroxy-4-methoxy-phenyl)-metiiory-acetic acid was coupled with 4-aminomethyl benzonitrile according to general procedure B to give (RS)-N-(4-cyano-ben2yl)-2-(2-hydroxy-4^methoxy-phenyl)-2-methoxy-acetamide. Orange amorphous 5oJid. MS 327.3 ([M+H]"") 37.4 In analogy to example 15.5, (RS)-N-(4-cyano-lienzy])-2-{2-hydroxy-4-methox7-phenyl)-2-methoxy-acetamide was converted to (RS)-N-[4-CN-liydroxycarbarnimidoyl)-benzyi]-2-C2-hydrox)'-4-methoxy-phenyl)-2-methoxy-acetamide. White solid. MS 358.1 ([M-H]") 37.5 A suspension of (RS)-N-[4-(N-hydroiycarbamimidoyl)-benzyl] -2-(2-hydroxy-4-inethoxy-ph.enyl)-2-niethoxy-acetamide {240 mg) in ethanol (9 ml) and acetic acid (0.38 ml) was hydrogenated for 7.5 h using 10% Pd/C as a catalyst. The reaction mixture was filtered and the solvent was evaporated. The product was purified by chromatography (sifica gel, CH2CI2 => CH2Cl2/MeOH 4:1) to give (RS)-N-{4-carbamimidoyl-benzyl)-2-(2-hydroxy-4-methoxy-phenyI)-2-methoxy-acetanude actetate (12 mg) as an off-white, amorphous soUd. MS 344.2 ([M+H]') Example 38 38.1 2-FIuoro-3-methoxybenzaidefayde was converted to (RS)-(2-fluoro-5-methoxy-phenyi}- methoxy-acetic add according to general procedure A. Light yellow oil. 38^ (RS)-(2-Fluoro-5-methoxy-phenyl)-methoxy-acetic acid was coupled with 4-aminomethyl benzonitrile according to general procedure C to give (RS)-N-(4-cyano-benz)d)-2-(2-fluoro-5-niethoxy-phenyi)-2-methoxy-acetamide. Colorless gum. 38.3 (RS)-N-(4-Cyano-benzyl)-2-(2-fluoro-5-methoxy-phenyl)-2-methoxy-acetamide was converted to (RS)-N-(4-carbaniimido^-benz)i)-2-(2-fluoro-5-methoxy-phenyI)-2-methoxy-acetamide; hydrochloride according to general procedure D. "White solid. MS 346.2 ([M-t-H]') Example 39 39.1 2,3-Difluorobenzaldehyde was converted to (RS)-(2,3-difiuoro-phenyl)-methoxy-acetic add according to general procedure A. Off-white soUd, 39.2 (RS)-(2,3-Difluoro-phenyi)-methoxy-acetic add was coupled with 4-aminomethyl benzonitrile according to general procedure C to give (RS)-N-{4-cyano-benzyi)-2-(2^-difluoro-phenyl)-2-methoxy-acetamide. Off-white soHd. 39.3 (RS)-N-(4-C7ano-benz}'l)-2-(2,3-diiluoro-phenyl)-2-inetboxy-acetaii!ide was converted to (RS) -N- (4-carbamimidoyl-benzyl) -2-(2,3-difluoro-piienyl}-2-methoxy-acetainide; hydrochloride according to genera! procedure D. White solid. MS 334.3 ([M+H]"^) Example 40 40.1 2,6-Difluorobenzaldehyde was converted to (RS)-(2,6-difluoro-phenyl)-methoxy-acetic acid according to general procedure A. Light yellow soHd. 40.2 (RS)-(2,6-E>ifluoro-phenyl)-methoj:y-acetic add was coupled with 4-aininQmethyl benzonitrile according to general procedure C to give (RS)-N-(4-cyano-benzyi)-2-(2,6-difluoro-phenyl)-2-methoxy-acetaniide. Off-white solid. 40.3 (RS)-N-(4-Cyano-benzylJ-2-{2,6-difluoro-phenyi)-2-methoxy-acetanude was converted to (RS)-N-(4-carbaiminidoyl-benz)d)-2-{2,6-difluoro-phenyl)-2-methoxy-acetamide; hydrochloride according to general procedure D. White solid. MS 334.2 ([M+IJ]"^) Example 41 41.1 4-Bromo-2-fluorobenzaIdehyde was converted to (RS)-{4-bromo-2-fluoro-phen)d)-methoxy-acetic acid according to general procedure A using methanol / dioxane as a solvent Light yellow oil. 41.2 (RS)-(4-Bromo-2-fluoro-phenyI)-methoxy-acetic add was coupled with 4-aniinomethy! benzonitrile according to general procedure C to give (RS)-2-(4-bromo-2-fluoro-phenjd)-N-(4-c)^no-benzyl)-2-methoxy-acetamide. Light yellow gum. 41.3 (RS)-2-(4-Bromo-2-fluoro-phenyl)-N-(4-cyano-benzyi)-2-methoxy-acetamide was converted to (RS)-2-(4-bromo-2-fluoro-phenyl)-N-(4-carbamimidoyl-benzyl)-2-methoxy-acetamide hydrochloride according to general procedure D. Off-white solid. MS 394.1 ([M+H]-") Example 42 42.1 4-Bromo-2-Quorobeii2aldehyde was reacted according to general procedure A using ethanol / dioxane as a solvent. The product of this reaction was subsequentJy coupled with 4-aminomethyl benzonitrile according to general procedure B to give (RS)-2-(4-bromo-2-fluoro-phenyl)-N-(4-cyano-benzyl)-2-ethoxy-acetaimde. Light yeUow oil, MS 39U ([M+H]^) 42.2 (RS)-2-(4-Bromo-2-fluoro-phenyl)-N-(4-cyano-ben2yl)-2-ethoxy-acetamide was converted to (RS}-2-(4-bromo-2-fluoro-phenyl}-N-(4-carbainiimdoj^-benzyl)-2-erfioxy-acetamide hydrochloride according to general procedure D. Off-white foam. MS 408.2 Example 43 43.1 4-Bromo-2-fluorobenzaldehyde was converted to (RS)-(4-bromo-2-fluoro-phen)4)-propoxy-acetic acid according to general procedure A using n-propanol / dioxane as a solvent- Colorless semisolid. 43.2 (RS)-(4-Bromo-2-fluoro-phenyl)-propoxy-acetic acid was coupled with 4-aniinomethyl benzonitrile according to general procedure C to give (RS)-2-(4-bromo~2-fluoro-phenyl)-N-(4-cyano-benz)^)-2-propcixy-acetaniide. Colorless oil. MS 405.3 ([M+H]"^) 43.3 (RS)-2-C4-Bromo-2-fluoro-phen^)-N-(4-cyano-benzyl)-2-propoxy-acetarnide was converted to (RS)-2-(4-bromo-2-fluoro-pheDyl)-N-(4-carbainimidoyl-beiizyl)-2-propoxy- acetamide hydrochloride according to general procedure D. Colorless solid. MS 423.3 ([M+H]^) Example 44 44.1 2-Fluoro-4-(trifluoromeUiyI)benzaldehyde was converted to (RS)-(2-fluoro-4-trifluoromethyl-phenyl)-methoxy-acetic add according to general procedure A. Light yellow gum. 44.2 (RS)-(2-Fluoro-4-triiluorometh)i-phenyI)-methoxy-acetic acid was coupled with 4-aminomethyl benzonitrile according to general procedure C to give CRS)-N-(4-cyano-benzyl)-2-{2-fluoro-4-trifIuoroinethyI-phen>d)-2-inethox7-acetaniide. Light yellow gum. 44.3 (RS) -N- (4-Cyano-benzyI)-2 - (2-fluoro-4-trifluoromethyl-phenyI)-2-methoxy-acetamide was converted to (RS)-N-{4-carbaniii[iidoyl-benzyl)-2-(2-fluoro-4-trifluoromethyl-phenyl)-2-inethoxy-acetainide hydrochloride according to general procedure D. Off-white soUd. MS 384.2 C[M+H]*) Example 45 45.1 In analogy to example 16.4, (RS)-N-(4-cyano-benzyl)-2-(4-hydroxy-phenyl)-2-methoxy-acetamide (example 21.2) was alkylated with bromoethanol/cesium carbonate in DMF to give (RS)-N-(4-cyano-benzyl)-2-[4-{2-hydroxy-ethoxy)-phenjd]-2-methoxy-acetamide as a colorless oil. MS 363.1 ([M+Na]"") 45.2 (RS)'N-(4-Cyano-benz}d)-2-[4-(2-hydroxy-ethoxy)-phen}^]-2-methoxy-acetaniide was converted to {RS)-N-(4-carbaniimidoyl-benzyl)-2-[4-(2-hydroxy-ethoxy)-phenyl]-2-methoxy-acetamide hydrochloride according to general procedure D. Colorless foam. MS 358.2 {[M-FH]"") Example 46 46.1 4-DimethyIaniinobenzaIdehyde was converted to (RS)-(4-dimefh}damino-phen)d)- methoxy-acetic add according to general procedure A. Light brown foam. MS 208.2 ([M- 46.2 (RS)-(4-0imeth)damLno-phenyI)-methoxy-acetic add was coupled with 4-aminomethyl benzonitrile according to general procedure B to give (RS)-N-(4-cyano-benz)d)-2-(4-dimethylamino-phenyl)-2-methoxy-acetaniide. Off-white solid. MS 324.2 ([M+H]"*") 46.3 (RS)-N-(4-Cyano-benzyi)-2-{4-dimethylamino-phenyl)-2-methoxy-acetamide . was converted to (RS)-N-(4-carbamimidoyl-benzyi)-2-(4-diniethylamino-phenyl)-2-methoxy- acetamide hxdrochloride according to general procedure D. Colorless solid. MS 341.2 ([M+H]") Example 47 47.1 3-Oxo-3,4-dihydro-2H-ben2o[l,4]oxaziiie-6-carba]dehyde (CAS 200195-15-9) was reacted according to general procedure A using methanol / dioxane as a solvent. The product of this reaction was subsequendy coupled with 4-aminomethyl benzonitrile according to general procedure C to give (RS)-N-(4-cpno-beiizyl)-2-methoxy-2-(3-oxo-3,4-dihydro-2H-benzo[l,4]oxazin-6-)d)-acetamide. Light yellow solid. 47.2 (RS)-N-(4-Cyano-benz)d)-2-methoxy-2-(3-oxo-3,4-dihydro-2H-benzo[l,4]oxazin-6-jd)-acetamide was converted to (IlS)-N-(4-carbaniimidoyl-benzyl)-2-methoxy-2-(3-oxo-3,4-dihydro-2H-benzo[l,4]oxa2in-6-yI)-acetamide hydrochloride according to general procedure D. Off-white sohd. MS 369.2 ([M+H] *) Example 48 48.1 4-(l-Pyrrolidino)benzaldehyde was reacted according to general procedure A using methanol I ioxane as a solvent. The product of this reaction was subsequently coupled with 4-aminomethyl benzonitrile according to general procedure B to give (RS)-N-(4-cyano-benz)d)-2-methoxy-2-(4-pyrroUdin-l-yl-phenyl)-acetaiinde, Off-white solid. MS 350.4 ([M+H]^) 48.2 (RS)-N-(4-Cyano-benzyl)-2-methoxy-2-(4-pyrrolidin-l-yi-phenyl)-acetamide was converted to (RS)-N-(4-caTbaniimidoyl-benzyl)-2-methoxy-2-(4-pyrroKdm-l-)d-phenyl)-acetamide hydrochloride according to general procedure D. Light red foam. MS 367.2 (EM+Hin Example 49 49.1 2-Chloroben2aldehyde was converted to (RS)-(2-chloro-phenyI)-methoxy-acetic acid according to general procedure A. Li^t yellow oil. MS 198.9 ([M-H]") 49.2 (RS)-(2-Chloro-phenyl)-methoxy-acetic acid was coupled with 4-aininomethyl benzonitrile according to general procedure B to give (RS)-2-(2-chIoro-phenyl)-N-(4-c7ano-beii27l)-2-methoxy--acetamide. Light yellow oil. MS 315.1 ([M+H]"^} 49.3 (RS)-2'(2'Chloro-phenyl)-N-(4-cyano-ben2yl)-2-methoxy-acetaniide was converted to i {RS)-N-C4-carbamimidoyi-benz;>d)-2-(2-cliIoro-phenyl)-2-methoxy-acetaimde hydrochloride according to general procedure D. Off-white, amorphous solid. MS 332.2 ([M+H]"') Example 50 50.1 4-Acetainidbenzaldehyde was converted to (RS)-(4-acetyian]ino-phen)d)-methoxy-acetic acid according to general procedure A. Yellow, amorphous solid. MS 222.0 {[M-H]') 50.2 (RS)-(4-Acetylamino-phen)^)-methoxy-acetic add was coupled with 4-aminomethyl benzonitrile according to general procedure B to give (RS)-2-(4-acetyianiino-phenyl}-N-(4-cyano-benzyI)-2-methoxy-acetamide. Off-white, amorphous solid. MS 338.3([M+H]"*') 50.3 (RS)-2-(4-Acetylamino-phenyl)-N-(4-cyano-ben2yl)-2-methoKy-acetaniide was converted to (RS}-2-(4-acetylanuno-phenyl)-N-(4-carbamimidoyl-benzyl)-2-methoxy-acetamide hydrochloride according to general procedure D. Orange amorphous soKd. MS 355.2 {[M+H]^) Example 51 51.1 4-(Trifluoromethoxy)benzaldehyde was converted to (RS)-methoxy-{4-trifiuoromethoxy- phenyl)-acetic add according to general procedure A. Light yellow oil. MS 249.3 ([M-H]") 51.2 {RS)-Methoxy-(4-tri£luoromethoxy-phenyl)-acetic add was coupled with 4-aminomethyl benzonitrile according to general procedure B to give (RS)-N-(4-cyano-ben2yl)-2- methoxy-2-{4-trifluoromethoxy-phenyI)-acetaniide. Light blue semisolid. MS 365.2 ([M+H]^) 51.3 CRS)-N-(4-Cyano-benz)^)-2-methoxy-2-(4-trifluoroniethoxy-phenyl)-acetamide was converted to (RS)-N-(4-carbaminiidoyl-ben2yi)-2-methoxy-2-(4-trifluoromethoxy- phenyl)-acetamide hydrochloride according to general procedure D. Off-white amorphous sohd. MS 3S2.3 ([M+HD Example 52 52.1 l-{4-Fonnylphenyi)-lH-imidazole was reacted according to general procedure A using methanol / dioxane as a solvent. The product of this reaction was subsequently coupled with 4-aininomethjd benzonitrile according to general procedure B to give {RS)-N-(4-cyano-ben2:jd)-2-(4-imidazol-l-yl-phenyl}-2-methoxy-acetamide. Colorless foam. MS 347.2 ([M+H]^) 52.2 (RS)-N-{4-Cyano-benzyl)-2-(4-imidazol-l-yl-phenyl)-2-methoxy-acetaniide was converted to (RS)-N-(4-carbamimidoyl-ben2yl)-2-(4-imidazol-l-yl-ph,enyl)-2-methoxy- acetamide hydrochloride according to general procedure D. Light yeJlow solid. MS 364.3 ([M+H]*) Example 53 53.1 6-Methoxy-2-naphtaldehyde was converted to {RS)-methoxy-(6-methoxy-naphthalen-2- yl)-acetic add according to general procedure A. light yellow solid. MS 245.2 ([M-H]") 53.2 {RS)-Methoxy-(6-methoxy-naphthalen-2-)d)-acetic acid was coupled with 4-aminometh)d benzonitrile according to general procedure C to give (RS)-N-(4-cyano-benzyl)-2-methoxy-2-(6-methoxy-naphthalen-2-yl)-acetamide. Off-white foam. MS 361.2 ([M+H]*) 53.3 {RS)-N-{4-Cyano-benZ)d)-2-methoxy-2-(6-methoxy-naphthalen-2-)d)-acetamide was converted to (RS)-N-(4-carbamiinidoyI-ben2yi)-2-methoxy-2-(6-methoxy-naphthalen-2- )d)-acetamide hydrochloride according to general procedure D. Off-white soUd. MS 378.3 ([M+H]^) Example 54 54.1 4-Morpholinobenzaldehyde was reacted according to general procedure A using methanol / dioxane as a solvent The product of this reaction was subsequently coupled with 4-aminomethyl benzonitrile according to general procedure B to give (RS)-N-(4-cyano- benzyl)-2-methox)'-2-(4-inorpliolm-4-yl-phenyl)-acetamide. Orange oil. MS 366.2 ([M+H]^) 54.2 (RS)-N-(4-Cyano-ben2)d)-2-methoxy-2-(4-morplioUn-4-yl-phenyi)-acetamide was converted to (RS}-N-{4-carbaininiidoyl-benzyI)-2-methoxy-2-(4-morpho]iii-4-yl-phenyl)-acetamide hydrochloride according to general procedure D. Orange foam. MS 383.3 {[M+H]*) Example 55 55.1 2-MorphoIinoben2aIdehyde was reacted according to general procedure A using methanol / dioxane as a solYent. The product of this reaction was subsequently conj^ed with 4-aminomethjd benzonitrile according to general procedure B to give (RS)-N-(4-cyano- benzyl)-2-methoxy-2-(2-morpholin-4-yl-phenyl)-acetamide. Orange oil. 55.2 (RS)-N-(4-Cyano-benz)d)-2-methoxy-2-(2-morpholin-4-yl-phenyI)-acetamide was converted to (RS)-N-(4-carbamirnidoyl-benzyl)-2-methoxy-2-(2-morpholin-4-yl-phenyI)-acetamide hydrochloride according to general procedure D. Light brown foam. MS 383.3 ([M+H]*) Example 56 56.1 4-[3-(Dimethylamino)propoxy] benzaldehyde was reacted according to general procedure A using methanol / dioxane as a solvent The product of this reaction was subsequently coupled with 4-aniinomethyl benzonitrile according to general procedure B to give (RS)-N-(4-cyano-benzyl)-2- [4-(3-dimethylarnino-propoxy)-phenyI] -2-methoxy-acetamJde. Colorless solid. MS 382.3 ([M+H]"") 56.2 (RS)-N-(4-Cyano-benzyI)-2-[4-(3-dimeth)4amino-propoxy)-phenyI]-2-methoxy-acetamide was converted to (RS)-N-(4-carbamiraidoyl-benzyi)-2-[4-(3-dimethyiamino-propoxy)-phenyl]-2-methoxy-acetamide hydrochloride according to general procedure D. Colorless soUd. MS 399.2 ([M+H]"") Example 57 57.1 To a stirred solution of (RS)-2-(4-bromo-2-fluoro-phenyl)-N-(4-cyano-benzyl)-2-methoxy-acetamide (example 41.2, 173 mg) in 1,2-diniethoxyethane (8 ml) were added PdQiCdppf) (34 mg), an aqueous 10% solution of Na2C03 (2 ml) and 4-dimethylaminophenylboronic acid (378 mg). The mixtuie was then stirred at 85 "C under an argon atmosphere for 1.5 h. After cooling to r.t. the mixture was diluted witii ethyl acetate (15 ml) and washed with water (10 ml). The aqueous layer was extracted with ethyl acetate and the combined organics were washed with water and brine, dried (MgS04), filtered and concentrated. The product was purified by chromatography (silica gel, gradient cyclohexane => cyclohexane / ethyl acetate 2:3) to give (RS)-N-(4-cyano-benz)i)-2-(4'-dimethylamino-3-fluoro-biphen)d-4-yl)-2-methoxy-acetamide (167 mg) as a Hght yellow solid. 57.2 (RS) -N- (4-Cyano-benzyl)-2- (4'-dimethyiamino-3-fiuoro-biphenyl-4-yl)-2-methoxy-acetamide was converted to (RS)-N-(4-carbamimidoyl-benzyl)-2-(4'-dimeth)danuno-3-fiuoro-biphenyl-4-)4)-2-methoxy-acetamide hydrochloride according to general procedure D. Off-white solid. MS 435.4 ([M+H]"") Example 58 58.1 In analogy to example 57.1, (RS)-2-(4-bromo-2-fiuoro-phenyI)-N-(4-cyano-benz>i)-2- methoxy-acetamide (example 41.2) was reacted with 4-methoxyphen>^oronic add to give (RS)-N-(4-cyano-benzyi)-2-(3-fluoro-4'-methoxy-biphenyl-4-)d)-2-methoxy-acetamide. Off-white solid. 58.3 (RS)-N-(4-Cyano-ben2;)d)-2-(3-fluoro-4'-methoxy-biphenyl-4-yl)-2-methoxy-acetamide was converted to (RS)-N-(4-carbamirmdoyi-benzyl)-2-(3-fluoro-4'-niethoxy-biphenyl-4- }^)-2-medioxy-acetamide hydrochloride according to general procedure D. White solid. MS 422.3 ([M+H]"") Example 59 59.1 In analogy to example 57.1, (RS)-2-(4-bromo-2-fluoro-phenyl)-N-(4'Cyano-ben2yl)-2- medioxj^-acetamide (example 41.2) was reacted with 2-methoxyphenylboromc add to give (RS)-N-(4-cyano-benzyI}-2-(3-£Iuoro-2'-methoxy-biphenyl-4-yI}-2-methoxy-acetamide. Light yellow gum. 59.2 CRS)-N-(4-Cyano-ben2yl)-2-(3-fluoro-2'-methoxy-biphenyl-4-yl)-2-methoxy-acetamide was converted to (RS)-N-(4-carbaiminidoyi-ben2yI)-2-(3-fluoro-2'-methoxy-biphenyI-4-yl)-2-methoxy-acetainide hydrochloride according to general procedure D. Off-white solid. MS 422.3 ([M+H]*) Example 60 60.1 In analogy to example 57.1, ,(RS)-2-(4-bromo-2-fiuoro-phenyl)-N-(4-cyano-benzyl)-2-methoxy-acetamide (example 41.2) was reacted with phenyiboronic acid to give (RS}-N-{4-cyano-benzyl)-2-(3-fluoro-biphenyl-4-yi)-2-methoxy-acetaniide. Light yellow gum. 60.2 (RS)-N-(4-Cyano-benzyI}-2-(3-fluoro-biphenyl-4-yi)-2-methoxy-acetamide was converted to (RS)-N-(4-carbamimidoyl-benzyl)-2-(3-fluoro-biphenyl-4-yl)-2-methoxy-acetamide hydrochloride according to general procedure D. White solid. MS 392.3 {[M+H]"*") Example 61 61.1 In analogy to example 57.1, ,(KS)-2-{4-bromo~2-fluoro-phen)d)-N-(4-cyano-ben27l)-2- methoxy-acetamide (example 41.2) was reacted with 3-methoxyphen)dboroDic add to give (RS)-N-(4-c)^no-ben2)d)-2-(3-fluoro-3'-methoxy-biphen)i-4-yl)-2-methoxy-acetamide. Light yellow gum. 6U (RS)-N-(4-Cyano-benzyi)-2-(3-fluoro-3'-methoxy-biphenyl-4-yi)-2-methoxy-acetamide was converted to (RS)-N-(4-carbaminiido)4-benz)d}-2-(3-fluoro-3'-methoxy-biphen)d-4-yl)-2-methoxy-acetamide hydrocbloride according to general procedure D. White soHd MS 422.3 ([M+H]"-) Example 62 62.1 2,2-Dimethylchromane-6-carbaldehyde was converted to (RS)-{2,2-dimethyl-chroman-6-5d)-methoxy-acetic add according to general procedure A. Light yellow oil. MS 249.1 ([M- 62.2 (RS)-(2,2-Diineth7l-chroman-6-yl)-methoxy--acetic acid was coupled with 4-aiiunometh7l benzonitrile according to general procedure C to give (RS)-N-(4-cyano-beii2yI)-2-(2,2-diinethyl-chroman-6-yl)-2-methDxy-acetamide. Off-white semi-solid. MS 365.2 ([M+H]"") 62.3 (RS)-N-(4-Cyano-benzy]}-2-{2,2-dimethyI-chroman-6-yl)-2-methoxy--acetamide was converted to (RS)-N-(4-carbamimidoyl-benzyl)-2-{2,2-dimethyi-chroman-6--54)-2-methoxy-acetamide hydrochloride according to general procedure D. Light yellow solid. MS3S2.4([M+H]^) Example 63 63.1 2-FIuoro-4-methoxyben2aldehyde was converted to (RS)-ethoxy-(2-fluoro-4-methoxy-phen)^)-acetic add according to general procedure A using ethanol / dioxane as a solvent Yellow oil. MS 227.2 ([M-H]") 63.2 (RS)-EthoKy-(2-fluoro-4-niethoxy-phenyl)-acetic acid was coupled with 4-aminoinethyl benzonitrile according to general procedure B to give (RS)-N-(4-cyano-benZ)^)-2-ethoxy-2-(2-fluoro-4-medioxy-phenyl)-acetamide. Yellow oil. MS 343.2 ([M+H]*) 63.3 (RS)-N-(4-Cyano-benzyi)-2-edioxy-2-(2-fluoro-4-inethoxy-phen)d)-acetamide was converted to (RS)-N-{4-carbanuniidoyl-ben2yI)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide hydrochloride according to general procedure D. Colorless foam. MS 360.3 {[M+H]^) 63.4 In analogy to example 15.5, give (RS)-N-(4-cyano-benzyi)-2-ethoxy-2-{2-fluoTO-4-methoxy-phenyl)-acetamide (example 63.2) was converted to (RS)-2-ethoxy-2-(2-£Iuoro-4-methoxy-phen}d)-N-[4-(N-hydroxycarbamimidoyl)-benz)4]-acetainide. Colorless foam. MS 376.3 ([M-^H]^) Example 64 64.1 3-(Cydopentyloxy)-4-methoxy-benzaldehyde was converted to (RS)-{3-cyclopentyloxy-4- methoxy-phenyl)-methoxy-acetic acid according to general procedure A. Yellow oil. MS 279.2 ([M-H]-) 64.2 (RS)-(3-Cydopentyloxy-4-methoxy-phenyl)-methoxy-acetic add was coupled with 4-aminomethyl benzonitrile according to general procedure B to give (RS)-N-(4-cyano-ben2yl)-2-(3-c7dopentjdoxy-4-methoxy-pheiiyi)-2-methoxy-acetainide. Colorless solid. 64.3 (RS)-N-(4-Cyano-benzyl)-2-(3-cydopentyloxy-4-metboxy-plienyI)-2-methoxy-acetainide was converted to (RS)-4-[3-{3-cyclopentyloxy-4-metIioxy-phen-)d)-3-methoxy-2-oxo-puQpylaminoj-benzamidine hydrochloride according to general procedure D. Off-white foam. MS 412.4 ([M+H]"") Example 65 65.1 2-Cfaloro-4-methoxybenzaldehyde (CAS No: 54439-75-7) was converted to CRS}-(2-chloro-4-methoxy-phenyl)-inethosy-acetic add according to general procedure A. Yellow oil. MS 228.9 ([M-H]") 65.2 {RS)-(2-Chloro-4-inethoxy-phenyl)-methoxy-acetic add was coupled with 4-aminomethyI benzonitrile according to general procedure B to give (RS)-2-(2-chloro-4-methoxy-phenyl)-N-(4-cyano-benzyl)-2-methoxy-acetainide. Light yellow oiL MS 345.2 ([M+H]"*) 65.3 (RS)-2-(2-Chloro-4-methoxy-phenyi)-N-{4-cyano-benzyl)-2-methoxy-acetamide was converted to (RS)-N-(4-caTbaiminidoyl-beiizyl)-2-(2-diloro-4-niethoxy-phenyl)-2-methoxy-acetamide hydrochloride according to general procedure D. Colorless foam. MS 362.2 ([M+H]-') Example 66 66.1 2,6-DifluDrQ-4-methoxybenzaldehyde (CAS No: 256417-10-4) was converted to (RS)-(2,6-difluoro-4-methoxy"phenyl)-methoxy-acetic add according to general procedure A. YeUow oil. MS 230.9 ([M-H]') 66.2 (RS)-(2,6-Difluoro-4-methoxy-phen}d)-methoxy-acetic add was coupled with 4-aminometbjd benzonitrile according to general procedure B to give (RS)-N-(4'cyano-benzyl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-methoxy-acetaniide. Light yellow amorphous soUd. MS 347.1 ([M+H]*) 66.3 (RS)-N-(4-Cyaiio-benz)4)-2-(2,6-diiluoro-4-methoxy-phen7i)-2-methoxy-acetaimde was converted to {RS)--N-(4-carbamimidoyl-benzyi)-2-C2,6-difiuoro-4-metboxy-phen)d)-2-methoxy-acetaroide hydrochloride according to general procedure D. Colorless foam. MS 364.2 {[M+Hf) Example 67 67.1 2-Fluoro-4-inethoxybenzaldehyde was reacted according to general procedure A using n-propanol / dioxane as a solvent The product of this reaction was subsequently coupled ■with 4-aminomethyl benzonitiile according to general procedure B to give (RS)-N-(4-cyano-benzyl)-2-{2-fiuoro-4-niethoxy-phenyl)-2-propoxy-acetamide. Light yellow oil. MS 357.2 ([M+H]"") 67.2 (RS)-N-(4-Cyano-benz>d)-2-{2-fluoro-4-methoxy-phenyl)-2-propoxy-acetaniide was converted to (RS)-N-(4-carbamiinidoyl-beiiz)d)-2-(2-fluoro-4-metiioxy-phenyl)-2-propoxy-acetamide hydrochloride according to general procedure D. Colorless foam. MS 374.2 ([M+H]"} Example 68 68.1 2-Methoxy-2-{l-naphtyl)propionic acid was coupled with 4-aminomethj4 benzonitrile according to general procedure B to give (RS}-N-(4-cyano-benzyl)-2-methoxy-2-naphthalen-l-yl-propionamide. Colorless foam. MS 345.2 ([M+H]*) 68^ (RS)-N-(4-Cyano-ben2yi)-2-methoxy-2-naphthalen-l-yl-propicnamide was converted to (IlS)-N-(4-carbamimidoyl-beiizyl)-2-methoxy-2-naphthalen-l-^-propionamide hydrochloride according to general procedure D. Colorless foam. MS 362.2 ([M+H] ) Example 69 69.1 A solution of l-bromo-3,5-difluorobenzene (16.8 g) in THE (180 ml) was cooled to -75 °C under an argon atmosphere. A 2 M solution of Uthiumdiisopropyiamide in THE / heptane / ethylbenzene (43.1 ml) was slowly added at below -70 "C The mixture was stirred at -78 "C for 1 h. Dimethylformamide (12.6 ml) was added and the mixture was stirred for 2 h. The cooling bath was removed and the mixture was slovrfy wanned to r.t. The mixture was diluted with diethyl ether and washed with 0.5 M HCI. The aqueous phase was extracted with diethyl ether. The combined organic phase was dried (MgS04), filtered and the solvent was removed to give the crude 4-bromo-2,6-difluorobeiizaldehyde (12.4 g). The crude aldehyde was reacted according to general procedure A using methanol / dioxane as a solvent. The product of this reaction was subsequently coupled with 4-aminomethjd benzonitrile according to general procedure B to give CRS)-2-(4-bromo-2,6-difluoro-phenyl)-N-(4-cyano-benzyl)-2-methoxy-acetamide. Yellow oil. MS 395.0 {[M+H]^) 69.2 (RS)-2-(4-Bromo-2,6-difluoro-phenyl)-N-(4-cyano-t>enzyl)-2-methoxy-acetamide was converted to (RS)-2-{4-bromo-2,6-difluoro-phenyl)-N-(4-carbaininiidoyl-benz)4)-2-methoxy-acetamide hydrochloride according to general procedure D. Off-white solid. MS 412.2 ([M+H]^) Example 70 70.1 In analogy to example 16.4, 2-fluDro-4-hydroxy-beiizaldehyde (CAS-No: 348-27-6) was alkylated with benzylbromide / potassium carbonate in DMF to give 4-benzyloxy-2-fluoro-benzaldehyde. OfF-white solid. MS 230.1 ([M+H]+) 70.2 4-Ben2yloxy-2-fluoro-benzaldehyde was converted to (RS)-(4-benz)doxy-2-fluoro- phenyO-methoxy-acetic acid according to general procedure A. White solid. MS 289.1 ([M-H]-) 70.3 (RS)-(4-Beiizyloxy-2-fluoro-phenyi)-methoxy-acetic add was hydrogenated at r.t. and normal pressure using 10% Pd/C as a catalyst and EtOH as a solvent to give (RS)-(2-fluoTO-4-hydroxy-phenyI)-methoxy-acetic acid as a hght yellow oil. MS 199.2 {[M-H]") 70.4 (RS)-(2-Fluoro-4-hydroxy-phenyl)-methoxy-acetic acid was coupled with 4-aininomethyl benzonitrile according to general procedure C to give {RS)-N-(4-cyano-benzyl)-2-(2-fluoro-4-hydroxy-phenyI)-2-inethoxy-acetamide. White solid. MS 315.1 ([M+H]'") 70.5 In analogy to example 16.4, (RS}-N-(4-cyano-benzyl)-2-(2-fiuoro-4-hydroxy-phenyl)-2- methoxy-acetamide was alkylated with 2-iodopropaiie and cesium carbonate in DMF to give (RS)-N-(4-cyano-benzyl)-2-f2-fluoro-4-isopropoxy-phenyl)-2-medioxy-acetaimde. Light yellow oil. MS 357.2 ([M+H]"") 70.6 (RS)-N-{4-Cyano-benz}d)-2-{2-fluoro-4-isopropoxy-phenyl)-2-inethoxy-acetainide was converted to (R.S)-N-(4-carbaiminidoyl-beiizyl)-2-{2-fluoro-4-isopropoxy-phenyl)-2-methoxy-acetamide hydrochloride according to general procedure D. Off-white solid. MS 374.2 ([M+H]') Example 71 71.1 In analogy to example 16.4, (RS)-N-(4-cyano-ben2yi)-2-(2-fluoro-4-hydroxy-phenyI}-2-methoxy-acetamide (example 70.4) was alkylated with l-iDdo-2-methylpropane and cesium carbonate in DMF to give (RS)-N-C4-cyano-benzyI}-2-(2-fluoro-4-isobutoxy-phenyl)-2-methoxy-acetamide. Off-white, amorphous solid. MS 371.3 ([M+H]"^) 71.2 (RS)-N-(4-Cyano-ben2y[)-2-{2-fluoro-4-isobutoxy-phenyi)-2-methosy-acetaiiiide was converted to (RS)-N-{4-carbamimido)^-benzyi)-2-(2-fluoro-4-isobutoxy-phen)d)-2-methoxy-acetamide hydrochloride according to general procedure D. Off-white solid. MS 388.3 ([M+H]^) Example 72 72.1 Li analogy to example 22.1, (RS)-N-(4-cyano-benzyl)-2-(2-fiuoro-4-hydroxy-pbenyI)-2-methoxy-acetamide (eisample 70.4) was reacted with 4-fl.uorophenethyl alcohoU diethyl azodicarboxylate and triphenyl-phosphine in THF to give (RS)-N-{4-cyano-benzyI)-2-{2-fluoro-4'[2-(4-fiuoro-phenyl)-ethoxy]-phenjd}-2-methoxy-acetamide. Colorless oil. MS 437.3 ([M+H]-") 72.2 (RS)-N-{4-Cyano-beiizyl)-2-{2-fiuoro-4-l2-(4-fluoro-phenyl)-ethoxy}-phenyl}-2-methoxy-acetamide wa^ converted to (RS)-N-(4-carbamitnidQyl-ben2yl)-2-{2-fluoro-4-[2-{4-fluoro-phenyl)-etfaoxy]-phenyl}-2-methoxy-acetarnide hydrochloride accordiR2 to general procedure D. Off-white, amorphous solid. MS 454.5 {[M+H]"*") Example 73 73.1 To a stirred solution of {RS)-2-(4-bromo-2-fiuoro-phenyl)-N-{4-cyano-benzyl)-2-methoxy-acetamide (example 41.2, 1,16 g) at r.L in dioxane were added bis(pinacolato)diboron (1.17 g) and potassium acetate (0.91 g). The mixture was purged with argon and bis(triphenylphospiune)palladium(II) chloride (0.13 g) was added. The mixture was then stirred at 80°C under an argon atmosphere for 18 L The solids were filtered off and washed with EtOAc. The filtrate was concentrated to leave the crude product as a dark brown oil. The product was isolated by chromatography (silica gel, gradient cyclohexane => cydohexane/EtOAc 3:2) to give (RS)-N-(4-cj^no-ben2yl)'2-[2-fluoro-4-(4,4,5,5-tetramethyl-[l,3)2]dioxaborolan-2-}4)-phenyI]-2-methoxy-acetamide as brown oil (0.64 g). Brown oil. MS 425.4 ([M+H]"") 73^ In analogy to example 57.1 (RS)-N-(4-cyano-benzyl)-2-[2-fluoro-4-(4,4.5,5-tetramethyl-[l,3,2]dioxaboroIan-2-yl)-pheDyl]-2-methoxy-acetamide was reacted with 3-bromopyridine to give (RS)-N-(4-cyano-benzyl)-2-(2-fiuoro-4-pyridin-3-yl-phenyI)-2-methoxy-acetamide. Light brown amorphous soHA MS 376.3 ([M+H]"*") 73.3 (RS)-N-(4-Cyano-ben2yl)-2-(2-fluoro-4-pyridin-3-yl-phenyl)-2-methoxy-acetamide was converted to (RS)-N-(4-carbamiraido)d-benzyl)-2-(2-fluoro-4-pyridin-3-yl-phenyl)-2-methoxy-acetamide; hydrochloride according to general procedure D. Off-white solid. MS 393.2 ([M+H]-") Example 74 74.1 In analogy to example 57.1 (RS)-N-(4-cyano-ben2yl)-2-[2-fluoro-4-(4,4,5,5-tetramethyl- [i,3,2]dioxaborolan'2-)d)-phenyl]-2'raethoxy-acetaniide (example 73.1) was reacted with 4-bromopyridine, hydrochloride to give (RS)-N-(4-cyano-benzyl)-2-(2-fluoro-4-pyridin-4-yl-phenyl)-2-methoxy-acetamide. Li^t brown amorphous solid. MS 376.3 ([M+H] ) 74.2 (RS)-N-(4-cyano-benzyl)-2-(2-fluoro-4-pyridin-4-yl-phenyl)-2-methoxy-acetamide was converted to (RS)-N-(4-carbamimidoyl-benzyl)-2-(2-fluoro-4-pyridin-4-yl-phenyl)-2-methoxy-acetamide; hydrochloride according to general procedure D. Off-white soHd. MS 393.2 {[M+H]^) Example 75 75.1 5-Bromo-2-fluorobenzaIdehyde was converted to (RS)-{5-bromo-2-fluoro-phenyl)-methoxy-acetic acid according to general procedure A using methanol/dioxane as solvent LightyeUowliquid. MS 262.0 ([M-H]") 75^ (RS)-(5-Bromo-2-fluoro-phenyl)-methoxy-acetic add was reacted with 4-aminomethyl benzonitrile according to general procedure C to give (RS)-2-(5-bromo-2-fiuoro-phenyl)-N-{4-cyano-benzyI)-2-methoxy-acetamide. Colorless solid. MS 377.2 ([M+H]"") 75.3 (RS)-2-(5-Bromo-2-fiuoro-pbenyl)-N-(4-cyano-benzyl)-2-methoxy-acetamidewas converted to (RS}-2-(5-bromo-2-fluoro-phenyl)-N-(4-carbanmnidoyI-benzyI)-2-methoxy-acebimide; hydrochloride according to general procedure D. Colorless soKd. MS 394.0 ([M+H]"*") Example 76 76.1 In analogy to example 57.1 give {RS)-2-(5-bromo-2-fluoro-phen)d)-N-(4-cyano-benzyl)-2-methoxy-acetannde (example 75.2) was reacted with phenylboronic acid to give (R£)-N-(4-cyano-benzyl)-2-(4-fiuoro-bipheayl-3-yi)-2-methoxy-acetamide. Off-white solid. MS I 374.1 (M). 76.2 (RS)-N-(4-Cyano-benzyI)-2-(4-fluoro-bipben)4-3-yl)-2-methoxy-acetamide was converted to (RS}-N-(4-carbamimidoyl-benzyl)-2-(4-fluoro-biphen)i-3-)d)-2-methoxy-acetamide; hydrocfaloride according to general procedure D. Colorless solid. MS 392.2 ([M+H]"^) Example 77 77.1 2-Fluoro-5-methyiben2aldehyde was converted to (RS)-{2-fluoro-5-meth)d-phen)d)-methoxy-acetic acid according to general procedure A using methanol/dioxane as solvent. Off-white liquid. MS 197.1 ([M-H]') 77.2 (RS)-(2-Fluoro-5-methyl-phenyi)-methoxy-acetic acid was reacted with 4-aminDmethyl benzonitrile according to general procedure C to give (RS)-N-(4-cyano-benzyl)-2-(2- fluoro-5-methyl-phenyI)-2-inethoxy-acetamide. Colorless amorphous solid MS 313.2 ([M+H]^) 773 (RS)-N-(4-Cyano-benz)d)-2-(2-fluoro-5-methyl-phenyI)-2-methoxy-acetamidewas converted to (RS)-N-(4-carbainmiidoyl-benzyl)-2-(2-fluoro-5-inethyl-phenyl)-2-methoxy-acetamide; hydrochloride accordmg to general procedure D. Colorless soUd. MS 330.2 ([M+H]"") Example 78 78.1 5-{Trifluoromethyl)-2-fiuorobenzaldehyde was converted to (RS)-(2-fluoro-5-trifluoromethyl-phenyl)-methoxy-acetic add according to general procedm-e A using methanol/dioxane as solvent. Colorless amourphous solid. MS 251.1 {[M-H]') 78.2 (RS)-(2-Fluoro-5-trifluoromethyl-phenyl)-methoxy-acetic add was reacted with 4-aminomethyl benzonitrile according to general procedure C to (RS}-N-(4-cyano-benzyl)-2-{2-fluoro-5-trifluoromethyl-phenyl)-2-methoxy-acetamide. Colorless amorphous solid. MS 367.1 {[M+H]"'} 78.3 {RS) -N-(4-Cyano-benzyi)-2- (2-fluoro-5-trifluoromethjd-phenyl)-2-methoxy-acetamide was converted to (RS)-N-C4-carbamiinidoyI-benzyi)-2-(2-fluoro-5-triflaoromethyl-phen5d)-2-methoxy-acetamide; hydrochloride according to general procedure D. Example 79 79.1 2-Fluoro-6-methoxybenzaldehyde was converted to (RS)-(2-fluoro-6-methoxy-phenyl)-methoxy-acetic acid according to general procedure A using methanol/dioxane as solvent. Off-white Hquid. MS 213.1 ([M-H]-) 79.2 (RS)-{2-Fluoro-6-methoxy-phenyl)-methoxy-acetic add vfas reacted with 4-aminomethyl benzonitrile according to general procedure C to {RS)-N-(4-cyano-benzy!)-2-(2-fIuoro-6-methoxy-phenyI)-2-methoxy-acetamide. Colorless soUd. MS 329.2 ([M+H]"^) 79.3 (■RS)-N-(4-Cyano-ben2yl)-2-(2-fl.uoio-6-methoxy-phen-^)-2-meth.oxy-acetainidewas converted to (RS)-N-(4-carbamimidoyl-benzyl)-2-(2-fluoro-6-inethoxy-phenyl)-2-methoxy-acetamide; hydrochloride according to general procedure D. Example 80 80.1 A solution of O-benzyl-3-fluorobenzene (4.66 g) in THF (50 ml) was cooled to -65°C. n-Buthyllithium in hexane (1.5 M, 15.8 ml) was added within 15 minutes. The reaction mixture was stirred at -eS'C for 30 minutes. Then DMF (1.95 ml) was added dropwise. The reaction mixture was wanned to r.t. overnight, then poured onto ice and extracted with ethji acetate. The oi^anic layers were washed with brine, dried over MgS04 and concentrated to give (RS)-2-benz>doxy-6-f!uoro-benzaldehyde (4.66 g). Yellow Uquid. MS 230.1 ([M]). 80.2 (RS)-2-Benzyloxy-6-fluoro-benzaIdehyde was converted to (RS)-(2-benzyloxy-6-fluoro-phenyl)-methoxy-acetic add according to general procedure A using methanol/dioxane as solvent YeUowHquid. MS 289.1 ([M-H]") 80.3 Inanalogyto example 16.2 (RS)-(2-benzyioxy-6-fluoro-phenyl)-methoxy-aceticaddwas converted to (RS)-(2-fluoro-6-hydroxy-phenyl)-methoxy-acetic add Colorless amorphous solid. MS 199.1 ([M-H]") 80.4 (RS)-(2-FIuoro-6-hydroxy-phenyl)-methoxy-acetic add was reacted with 4-aminometh)1 benzonitrile according to general procedure C to give (RS)-N-(4-cyano-benzyl)-2-(2-fluoro-6-hydroxy-phenyl)-2-methoxy-acetamide. Colorless solid. MS 315.1 ([M+H]"^) 80.5 (RS)-N-(4-Cyano-ben2yi)-2-(2-fiuoro-6-hydroxy-phenyl)-2-methoxy-acetamide was converted to (RS)-N-(4-carbaniimidoyl-benzyI)-2-(2-fluoro-6-hydroxy-phenyl)-2-methoxy-acetamide; hydrochloride according to general procedure D. Example 81 8L1 a-Bromophenylacetic add was reacted with 4-aminomethyl benzonitrile according to general procedure C to give (RS)-2-bromo-N-(4-cyano-benzyl)-2-phenyl-acetamide. White solid. MS 329.1 ([M+H]^) 81.2 To a stirred solution of {RS)-2-bromo-N-(4-cyano-ben2yl)-2-phenyI-acetainide (200 mg) in THF (10 ml) at r.t under an Ar atmosphere were added dimethylamine, hydrochloride (149 mg), trieth}iamine (0.42 ml) and tetrabutylammonium iodide (34 mg). The reaction mixture was stirred for 19 hrs, then treated with additional dimethjiamine, hydrochloride (149 mg) and triethylamine (0.42 ml). After another 8 hrs stirring at r.t., the soUds were filtered off and washed with EtOAc. The filtrate was washed with water and brine, dried over MgS04 and concentrated. The product was isolated by chromatography (siHca gel, gradient dichloromethane => dichlofomethane/MeOH 9:1) to give (RS}-N-(4-cyano-benzyI)-2-dimethylamino-2-phenyl-3cetamide (165 mg). Orange solid. MS 294.3 ([M+H]^) 81.3 (RS)-N-(4-Cyano-benzyl)-2-dimethylamino-2-phenyl-acetamide was converted to (RS)-N-(4-carbamimidoyI-benzyl)-2-dimethylamino-2-phenyl-acetamide; hydrochloride according to general procedm-e D. Off-white solid. MS 311.2 ([M+H]"^) Example 82 82.1 In analogy to example 81.2 of (RS)-2-bromo-N-(4-cyano-ben2yl)-2-phenjd-acetaniide (example 81.1) was reacted with methylamine, hydrochloride to (RS)-N-(4-cyano-benzyl)-2-methylamino-2-phenyl-acetamide. Off-white amorphous solid. MS 280.1 ([M+H]"^) 82.2 (RS)-N-(4-Cyano-ben2yl)-2-methylajnino-2-phen)i-acetamide was converted to (RS)-N-(4-carbamimidoyl-benzyl)-2-mediylamino-2-phenyl-acetamide; hydrochloride according to general procedure D. Off-white solid. MS 297.3 ([M+H]"*) Example 83 83.1 To a stirred solution of sodium methanethiolate (0.43 g) at r.t. in methanol (15 ml) were added the (RS)-2-bromo-N-(4-cyano-benzyl)-2-phenyl-acetamide (0.5 g, example 81.1) and a catalytic amount of tetrabutyl ammonium iodide. The mixture was then stirred at r.L for 1 hr. The mixture was concentrated. The residue was taken up in EtOAc, washed with 1.0 N and brine, dried over MgS04, filtered and concentrated. The product was isolated by chromatography (silica gel, cydohexane/EtOAc 2:1) to give (RS)-N-(4-cyano-benzyl)-2-methyIsuIfanyl-2-phenyl-acetamide (0.36 g). Colorless solid. MS 297.2 ([M+H]^) 83.2 (RS)-N-(4-Cyano-ben2yl)-2-methyIsulfanyl-2-phenyl-acetainide was converted to (RS)-N-(4-carbainiraidoyl-benz)d}-2-methylsulfenyl-2-phenyi-acetainide; hydrochloride according to general procedure D. Colorless solid. MS 314.2 ([M+H]"*") Example 84 84.1 In analogy to example 83.1 (RS)-2-bromo-N-{4-cyano-benz^)-2-phenyl-acetamide (example 81.1) was reacted with sodium ethanethiolate to give (RS)-N-{4-cyano-ben2yl)-2-eth)dsulfenyl-2-phenyl-acetamide. Off-white solid. MS 311.2 {[M+H]"^) 84.2 (RS)-N-{4-Cyano-benzyl)-2-ethylsulfanyl-2-phenyl-acetaniide was converted to (RS)-N-(4-carbaiiiiniidoyl-benzyI)-2-ethylsulfen>d-2-phenyl-acetaraide; hydrochloride accordiR2 to general procedure D. Colorless solid. MS 328.2 ([M+H]"^) Example 85 85.1 A solution of CRS)-N-(4-cyano-benzyl)-2-methylsu]fanyl-2-phen)d-acetaniide (0.11 g, example 83.1) in dichloromethane (10 ml) was cooled to -ICC and treated with mCPBA (0.27 g). The reaction mixture was stirred at 0°C, then diluted with dichloromethane and washed with aqueous sodium hydrogen sulfite solution. The organic layer was further washed with satinrated KHC03 solution and brine, dried over MgS04, filtered and concentrated. The product was isolated by chromatography (silica gd, gradient cyclohexane => EtOAc) to give (RS)-N-(4-cyaiio-benzyI)-2-methanesulfon)d-2-phen54-acetamide (0.084 g). White soUd. MS 329.2 ([M+H]"^) 85.2 (RS)-N-(4-Cyano-benzyl)-2-methanesulfon)i-2-phenyl-acetamide Vfas converted to (RS)-N-(4-carbamimido)d-benzyi)-2-metlianesulfonyl-2-phenyl-acetamide; hydrochloride according to general procedure D. Colorless sohd. MS 346.1 ([M+H]"^) Example 86 86.1 Boc-DL-phenyiglycine was reacted with 4-aniinomethyl benzonitrile according to general procedure C to give (RS)-[(4-cyano-benzylcarbamoyl)-phen)d-methyl]-carbamic acid tert-butyl ester. Off-white sohd. MS 366.2 ([M-hH]"") 86.2 (RS}-[(4-Cyano-benz7lcarbainoyl)-phenyI-methyl]-carbamic add tert-butyl ester was converted to (RS)-2-amino-N-(4-carbamimidoyl-ben2yl)-2-phenyl-acetamide; hydrochloride according to general procedure C. Off-white solid. MS 283^2 ([M+H]"^) Example 87 87.1 A solution of give (RS)-[(4-cyano-benzylcarbamoyl)-phenyl-methyi]-carbamic add tert-butyl ester (0.77 g, example 86.1) in dichloromethane (20 ml) was cooled to O^C and treated with trifiuoro acetic add (5 ml). The reaction mixture was stirred at r.t. for 5 hrs, then diluted with dichloromethane, cooled to CC and brought to pH 9 by dropwise addition of saturated aqueous Na2C03. The organic layer was washed with brine, dried over MgS04, filtered and concentrated to give (RS)-2-amino-N-(4-cyano-benzyl)-2-phenyl-acetamide (0.56 g). Ofif-white amorphous solid. MS 266.2 ([M+H]"^) 87.2 A solution of (RS)-2-aniino-N-(4-cyano-ben2yl)-2-phen)i-acetaniide (0.1 g) in dichloromethane (5 ml) was cooled to 0°C and treated with triethylamine (58 |il) and acetyl chloride (28 (4l). The reaction mixture was stirred at r.t for 1 hr, then diluted with dichloromethane, washed with IN HCl and brine. The organic layer was dried over MgS04, filtered and concentrated The product was isolated by chromatography (silica gel, gradient dichloromethane => dicMoromethane/MeOH 9:1) to give (RS)-2-acet)daraino-N-(4-cyano-benzyl)-2-phenyl-acetaniide (98 mg). Off-whitesoUd. MS 308.2 ([M+H]"^) 87.3 (RS)-2-Acetylamino-N-(4-cyano-benzyI)-2-phenyl-acetamide was converted to (RS)-2-acetylamino-N-(4-carbanuinidoyl-ben2yl)-2-phenyi-acetamide; hydrochloride according to general procedure D. Example 88 88.1 In analogy to example 22.1, (RS)-N-(4-cyano-benzyl)-2-(2-fluoro-4-hydroxy-phenyi}-2- methoxy-acetamide (example 70.4) was reacted with 2-phenoxyethanol, diethyl azodicarboxylate and triphenyl-phosphine in THF to give (KS)-N-(4-cyano-ben2:)d)-2-[2- fluoro-4-(2-phenoxy-ethoxy)-phenyl]-2-methoxy-acetamide. Colorless oil. MS 435.3 ([M+H]^) 88.2 {RS)-N-(4-Cyano-benzyl)-2-[2-fluoro-4-(2-phenoxy-ethoxy)-phenyl]-2-inethoxy-acetamide was converted to (RS)-N-(4-carbamiinido)d-beiizyl)-2-[2-fluoro-4-(2-phenox}'-ethox7)-piienyI]-2-inethoxy-acetamide hydrochloride according to general procedure D. White solid. MS 452.2 ([M+H]"") Example 89 89.1 2-Pyridinecarboxaldehyde was converted to (RS)-niethoxy-pyridin-2-}d-acetic add according to general procedure A using methanol/dioxane as solvent Brown oil. MS 166.1 ([M-H]-} 89.2 (RS)-Methoxy-pyridin-2-yl-acetic acid was reacted with 4-arainomethyi benzonitrile according to general procedure B to give (RS)-N-{4-cyano-ben2yI)-2-methoxy-2-pyridin-2-yl-acet3inide. Brown oil. MS 282.2 ([M+H] ■") 89.3 (RS)-N-(4-Cyano-benzyl)-2-methoxy-2-pyridin-2-yl-acetamide was converted to (RS)-N-(4-carbaiiiinudoyi-benzyl)-2-methoxy-2-pyridin-2-yl-acetamide hydrochloride according to general procedure D. Off-white, amorphous soHd. MS 299.2 ([M+H]"^) Example 90 90.1 Acetophenone was converted to (RS)-2-methoxy-2-phen>i-propiomc add according to general procedure A using methanol/dioxane as solvent Brown oil. MS 179.1 ([M-H]") 90.2 (RS)-2-Methoxy-2-phenyl-propionic add was reacted with 4-aminomethyl benzonitrile according to general procedure B to give (RS)-N-(4-cpno-ben2yi)-2-methoxy-2-phenyl-propionainide. Off-white, waxy solid. MS 295.0 ([M+H]"^) 90.3 (RS)-N-(4-Cyano-benzyl)-2-methoxy-2-phenyl-propionamide was converted to (RS)-N-(4-carbamimido)i-benzyl)-2-methoxy-2-phenyl-propionamide hydrochloride according to general procedure D. Off-white, amorphous solid. MS 312.2 ([M+H]"^) Example 91 91.1 The crude 4-bromo-2,6-difluorobenzaldehyde described in example 69.1 was reacted according to general procedure A using ethanol / dioxane as a solvent. The product of this reaction was subsequently coupled with 4-aminomethyl benzonitrile according to general procedure B. The product of this reaction could not be obtained pure and was directly converted to [RS)-2-(4-bromo-2,6-difluoro-phenyi)-N-(4-carbamimidoyl-benz)4)-2-ethoxy-acetamide hydrochloride according to general procedure D. Off-white soHd. MS 426.2{[M+H]"') Example 92 92.1 In analogy to example 16.4 (RS)-N-(4-cyano-benZ)d)-2-(2-fiuoro-6-hydroxy-phenyl)-2-methoxy-acetamide (example 80.4) was reacted with 2-bromoethanol in the presence of cesium carbonat in DMF to give N-{4-cyano-benzyl)-2-[2-fluoro-6-(2-hydroxy-ethoxy)-phenyl3-2-methoxy-acetamide. White solid. MS 359.2 ([M+H]"^) 92.1 N-(4-Cyano-benzyl) -2- [2-fluoro-6-(2-hydroxy-ethoxy)-phenyi] -2-methoxy-acetamide was converted to N-(4-carbainunidoyl-benzyl)-2-[2-fluoro-6-(2-hydroxy-ethoxy)-phenyl]-2-methoxy-acetamide; hydrochloride according to general procedure D. White solid. MS 376.3 ([M+H]"") Example 93 93.1 In analogy to example 16.4 (RS)-N-(4-cyano-benzyi)-2-(2-fluoro-6-hydroxy-phen)^)-2-methoxy-acetamide (example 80.4) was reacted with iodo acetamide in the presence of potassium carbonate in DMF to give 2-(2-carbamoylmethoxy-6-fluoro-phen)d)-N-(4-cyano-benzji)-2-methoxy-acetamide. Solid. MS 372.2 ([M+H]"^) 93.2 2-(2-Carbamoyhnethoxy-6-fluoro-phenyi)-N-(4-cyano-benzyl)-2-methoxy-acetamidewas converted to N-(4-carbamimidoy!-benzyl)-2-(2-carbamoyimethoxy-6-fluoro-phenyI)-2-methoxy-acetamide; hydrochlorideaccording to general procedure D. White soHd. MS 389.2 ([M+H]^) Example 94 94.1 To a solution of 2-biphenyI-4-yI-2-hydroxy-propionic add (CAS 6244-54-8,943 mg) in THF (10 ml), stirred at 0 "C was added NaH (60 % in mineral oil, 342 mg). After 50 min, ethyl iodide (0.69 ml) was added and the mixture was stirred at r.t. for 14 li. DMF (10 ml) was added. After 2 days, 47 mg NaH and 0.16 ml ethyl iodide were added subsequently. In the course of three weeks, a total of 653 mg NaH and 1.32 ml ethyl iodide were added. Water was added and the mixture was extracted with EtOAc (2x). The org. phase was washed with water, dried, filtered and evaporated. The crude product was purified by flash chromatography (EtOAc/ cydohexane 5:95 => 1:4) to give (RS)-2-biphenyl-4-yl-2-ethoxy-propionic acid ethjd ester (276 mg) as a light yellow oil. MS 298.1 ([M]"^) 94.2 (RS)-2-Biphenyl-4-yl-2-ethoxy-propionic add ethyl ester was hydrolyzed to (RS)-2-biphenyl-4-)d-2-ethoxy-propionic acid in analogy to example 20.1. Colorless waxy soHd. MS 269.1 ([M-H]') 943 (RS)-2-Biphenyl-4-)d-2-ethoxy-propionic acid was coupled with 4-aminomethyl benzonitrile to give (RS)-2-biphenyl-4-yl-N-{4-cyano-benzyl)-2-ethoxy-propionaniide according to general procedure C. Colorless solid. MS 385.1 ([M+H]^) 94.4 (RS)-2-BiphenyI-4-yl-N-(4-cyano-benzyl)-2-ethoxy-propionamide was converted to (RS)- 2-biphenyi-4-)d-N-(4-carbamimidoyl-benz)d)-2-ethoxy-propionamide hydrochloride according to general procedure D. Colorless solid. MS 402.3 ([M+H]"^) Example 95 95.1 4-(5-Ethoxy-2-fluoro-3-formyl-phenoxy)-piperidine-l-carboxylic add tert-but)d ester was converted to (RS)-4-[3-(carboxy-methoxy-metbyi)-5-ethoxy-2-fluoro-phenosy]-piperidine-1-carboxylic add tert-butjd ester according to general procedure A. Off-white solid. MS 445.3 {[M+NH4]0 95.2 (RS)-4-[3-(Carboxy-methoxy-methyl)-5-ethoxy-2-fiuoro-phenoxy]-piperidine-l-carboxyUc add tert-butyi ester was coupled with 4-aminomethyl benzonitrile to give (RS)-4-{3-[(4-cyano-ben2ylcarbamoyl)-methoxy-methyi]-5-ethoxy-2-fluoro-phenoxy}- piperidine-1-carboxyiic add tert-butjd ester according to general procedure B. Yellow oil. MS 564.4 ([M+Na]^) 95.3 The BOC-protecting group of (RS)-4-{3-[(4-cyano-benzylcarbainoyi)-methoxy-methyl]-5-ethox}'-2-fluoro-phenox7}-piperidine-l-carbox}dic add tert-butyl ester was removed according to standard procedures (TFA in CH2CI2) to give (RS)-N-(4-cyano-benzyl)-2-[5-ethoxy-2-£luoro-3-(piperidin-4-yloxy)-phenyl]-2-methoxy-acetainide. Off-white solid. MS 442.3 ([M+H]') 95.4 To a solution of (RS)-N-(4-cyano-benzyl)-2-[5-ethoxy-2-fluoro-3-Cpiperidin-4-ylox)')-phenyl]-2-methoKy-acetaimde (300 mg) in THF (3 ml) were added benzenesulfonyl chloride (127 mg) and trieth)damine {138 mg). The mixture was stirred over the weekend. Ice-water and EtOAc were added and the pH of the aq. Phase was adjusted to 2. The mixture was extracted with EtOAc. The org. Phase was washed with sat. NaHCOj soln. and water, dried, filtered and evaporated to give {RS)-2-[3-(l-beiizenesulfonyl-piperidin-4-)4oxy)-5-ethoxy-2-fiuoro-pheDyll-N-(4-cyano-benzyl)-2-methoxy-acetamide {396 mg) as an off-white solid. MS 582.2 ([M+H]^). 95.5 (RS)-2-[3-(l-Benzenesulfonyl-piperidin-4-}4oxy)-5-ethoxy-2-fluoro-phenyl]-N-(4-<:: was converted to hydrodiloride according general procedure d. colorless soud. ms> Using similar conditions to the ones described in examples 95.4 and 95.5, (RS)-N-(4-cyano-benzyI)-2-[5-ethoxy-2-fluoro-3-(piperidin-4-yloxy)-phenyl]-2-methoxy-acetainide was converted to the foJIowiug compounds: Example 96: {RS)-N-(4-Carbaniiniidoyl-benzyi)-2-[5-ethoxy-2-fluoro-3-(l-methanesulfonyl-piperidin-4-yloxy)-phenyl]-2-methoxy-acetaimde hydrochloride, MS 537.3 ([M+H]-") Example 97: (RS)-2-[3-{l-AcetyI-piperidin-4-yloxy)-5-ethoxy-2-fluoro-phenyl]-N-(4-carbaraainidoyi-benzyI)-2-methoxy-acetamide hydrochloride, MS 501.3 {[M+H]"^) Example 98: {RS)-2-[3-{l-Benzoyl-piperidin-4-yioxy)-5-ethoKy-2-fluoro-phenjd]-N-(4-carbaininiidoyl-benzyI)-2-methoxy-acetamide hydrochloride, MS 563.5 ([M+H]"^) Example 99 99.1 (RS)-(2-Fluoro-4-methox7-phenyl)-inethoxy-aceticacid, described in example 15.1 was coupled with 4-ammomethyl-3-chloroben2onitrile (CAS 202521-97-9) according to general procedure B to give (RS)-N-(2-cbloro-4-cyano-benzyl)-2-(2-fluoro-4-methoxy-phenyl)-2-niethoxy-acetainide. Light green soUd. MS 361.1 ([M-H]") 99.2 (RS)-N-(2-Chloro-4-cyano-benzyl)-2-(2-fiuoro-4-methoxy-phenyi)-2-metiioxy-acetaniide was converted to (RS)-N-(4-carbamimidoyl-2-cfaloro-ben2)d}-2-{2-fluoro-4-methox)'-phenyl)-2-methosy-acetainide hydrochloride according to general procedure D. Off-white soUd. MS 378.1 ((M-HD Ejmmple 100 100.1 (RS)-Ethoxy-(2-fluoro-4-methoxy-phenyl)-acetic acid, described in example 63.1 was coupled with 4-aniinometiiyl-3-chlorobenzomtrile (CAS 202521-97-9) according to general procedure C to give (RS)-N-(2-chloro-4-cyano-benz^)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide. Yellow oil. MS 377.2 ([M+H]"^) 100^ (RS)-N-(2-chloro-4-cyano-benzyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide was converted to (RS)-N-(4-carbaminudo)d-2-chloTO-benz}d)-2-ethoxy-2-{2-fluoro-4-methoxy-phenyl)-acetamide hydrochloride according to general procedure D. Colorless foam. MS 394.1 ([M+HD Example 101 101.1 To a solution of 3,5-difluoroaiiisole (20 g) in THE (200 ml) was added pentamethyldiethylenetriamine (24.05 g). The mixture was cooled to -75 "C. n-butyilithium (85 ml, 1.6 M in hexane) was added in such a way that the temperature did not exceed -67 "C. The mixture was stirred for 2 h. Ethylglyoxalate ( 55.5 g, 50 % in toluene) was added and the mixture was stirred for a further 2 h. Afterwards, the mixture was allowed to warm up to r.t. Water was added and the mixture vras made acidic (pH 3) with 25 % HCl. The mixture was ejctracted with EtOAc. The org. phase was washed with 0.5 N HCI, dried, filtered and concentrated. The product was purified by flash chromatography (Si02, cyclohexane / EtOAc 7:1} to give (RS)-(2,6-difluoro-4-methoxy-phenyI)-hydroxy-2cetii: add ethyJ ester (13.09 g). Colorless oil. MS 246.1 ([M]"^) 101.2 To a suspension of (RS)-(2,6-difluoro-4-methoxy-phenyl}-hydroxy-acetic acid ethyl ester (13.06 g) and Ag20 (24.58 g) in toluene (100 ml) was added ethyl iodide (24.81 g). The mixture was heated to reflux for 2.5 h. Ethyl iodide (24.81 g) and AgiO (12.29 g) were added and the mixture was refluxed for a fiirther 7 h. The soHd was filtered off and the filtate was concentrated to give (RS)-(2,6~difiuoro-4-methoxy-phenyl)-ethoxy-acetic acid ethyl ester (14.6 g). Light yellow oil. MS 274.1 ([MD 101.3 (RS)-(2,6-Difluoro-4-methcxy-phen)d)-ethoxy-acetic add ethyl ester was hydrolyzed to (RS)-(2,6-difluoro-4-methoxy-phen)4)-ethoxy-acetic add in analogy to example 20.1. MS Light yellow oil 245.2 C[M-H]") 101.4 (RS)- (2,6-DifIuoro-4-methoxy-phenyi)-ethoxy-acetic add was coupled with 4-anunomethyl-3-chlorobenzonitrile (CAS 202521-97-9) according to general procedure C to give (RS)-N-(2-chloro-4-cyano-benzyl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide. Colorless oil. MS 395.0 {[M+H]"*") 101.5 (RS}-N-(2-Ch]oro-4-cyano-benzyi}-2-(2,6-difiuoro-4-methoxy-phenyl)-2-ethoxy-acetamide was converted to (RS)-N-(4-carbaniimidoyl-2-chloro-benzyl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetaniide hydrochloride according to general procedure D. Coloriess foam. MS 412.3 ([M+H]"*"} Example 102 102.1 (RS)-(2,6-Difluoro-4-methoxy-phenyl)-methoxy-acetic add, described in example 66.1 was coupled with 4-aminometh)i-3-chlorobenzonitrile (CAS 202521-97-9) according to general procedure C to give (RS)-N-(2-chloro-4-cyano-benzyl)-2-(2,6-difluoro-4- methoxy-phenyl)-2-methoxy-acetamide. Light yellow oil. MS 379.2 ([M-H]') 102.2 (RS) -N-(2-Chloro-4-cyano-benzyl) -2- (2,6-difluoro-4-methoay-phenyl)-2-methoxy- acetamide was converted to (RS)-N-(4-carbamimidoyl-2-ch]oro-benzyl)-2-(2,6-difluoro- 4-methox)'"-plieny])-2-methoiy-acetamide h}^drochloride according to general procedure D. Colorless foam. MS 398.2 ([M+H]^) Example 103 103.1 (RS)-Ethoxy-(2-fluorD-4-methoxy-phenyI)-acetic acid, described in example 63.1 was coupled with 4~aminomethyl-2-chlorobenzoiiitrile (CAS 202522-15-4) according to general procediire C to give {RS)-N-(3-chloro-4-cyano-ben2yl)-2-ethoxy-2-(2-fiuoro-4-methoxy-phenyO-acetamide. Yellow oil. MS 377.2 ([M+H]"^) 103.2 (RS )-N-{3-Chloro-4-cyano-benzyl) -2-ethoxy-2- (2-fluoro-4-niethoxy-plienyi) -acetamide was converted to (RS)-N-[3-chloro-4-(N-hydTOxycarbamiinidoyi)-benzyl] -2-ethoxy-2-{2-fluoro-4-methoxy-pben)d)-acetanude according to general procedure D. Colorless solid. MS410.0 {[M+H]^) 103.3 In analogy to example 37.5, (RS)-N-[3-chloro-4-(N-hydroxycarbamimidoyl)-benzyl|-2- ethoxy-2-(2-fluoro-4-methoxy-phenyI)-acetainide was reduced to give (RS)-N-(4- carbamimido}^-3-chloro-ben2yl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide acetate. Colorless solid. MS 394.2 ([M-i-H]') Example 104 The crude 4-brorao-2,6-difluorobenzaldehyde described in example 69.1 was reacted according to general procedure A using ethanol / dioxane as a solvent The product of this reaction was subsequently coupled with 4-arainometh)d-3-methoxy-benzomtrile (CAS 182159-14-4) according to general procedure B. The product of this reaction could not be obtained pure and was directly converted to (RS)-2-(4-bromo-2,6-difluoro-phenjd)-N-(4-carbamimidoyl-2-methoxy-ben2yl)-2-ethoxy-acetamide hydrochloride according to general procedure D. Off-white solid. MS 456.1 ([M-l-H]'^) Example 105 105.1 (RS)-Ethoxy-(2-fluoro-4-methoxy-phenyi)-acetic acid, described in example 63.1 was coupled with 4-aminomethyl-3-methoxy-ben2onitrile (CAS 182159-14-4) according to general procedure B to give (RS)-N-(4-cyano-2-methoxy-benzyl)-2-ethoxy-2-(2-fiuoro-4-methoxy-phenyl)-acetamJde. Yellow oil. MS 373.2 ([M+H]"^) 105.2 (RS) -N-{4-Cyano-2-methox)'-ben2yl) -2-etitoxy-2- (2-fluoro-4-methoxy-phenyl)-acetamide was converted to (RS)-N-(4-carbamiinidoyl-2-met±ioxy-benzyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetainide hydrochloride according to general procedure D. Colorless solid. MS 390.3 ([M+H]') Example 106 106.1 A suspension of 3-fluoro-4-formyl-benzonitrile (CAS 105942-10-7,3 g), phenol (2.14 g) and potassium carbonate {3.14 g) in DMF (20 ml) was stirred at 120 "C for 90 min. After cooling down to r.t, water was added and the mixture was extracted with diethyl ether. The org. phase was washed with 0.1M NaOH and brine, dried, filtered and evaporated. The crude 4-formyl-3-phenoxy-benzonitrile (brown oil, 3.75 g) was used in the next step without finrtiier purification. 106.2 To a solution of 4-formyi-3-phenoxy-ben20nitrile (2.21 g) in dry ethanol (45 ml) was added sodium acetate (0.894 g) and hydroxylamine hydrochloride (0.757 g). The mixture was stirred at r.t. for 4.5 h. The solvent was evaporated and the product was purified by flash chromatography (cydohexane/EtOAc 8:2 => 3:7) to give 4-(hydroxyimino-meth>d)-3-pheno3^-benzonitrile (1.42 g). Light yellow solid. MS 238.1 ([M]"^) 106.3 A solution of 4-(hydroxyimino-methyl)-3-phenoxy-benzonitrile (200 mg) in acetic acid (1.2 ml) was stirred at 65 °C. Zinc powder (500 mg) was added portionwise during 30 min. After stirring for a further 1 h, the reaction mixture was filtered and the filtrate was concentrated to near dryness. Water was added and the mixture was washed with diethyl ether. The org. Phase was extracted (Ix) with diluted acetic add. The pH of the combined aq. phases was adjusted to 11 using 2 N NaOH. The mixture was extracted with EtOAc. The org Phase was dried, filtered and concentrated to give 4-aminomethyi-3-phenoxy-benzonitrile (165 mg) as a l^ht yellow oiL 106A (RS)-Ethoxy-(2-fluoro-4-methoxy-phen)d)-acetic add, described in example 63.1 was coupled with 4-aminomethyl-3-phenoxy-benzonitrile according to general procedtire B to give (RS)->f-(4-cyano-2-phenoxy-benzyI)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyi)- acetamide. Colorless oil. MS 435.2 ([M+H]"") 106.5 (RS)-N-(4-Cyano-2-phenoxy-beiiz)d)-2-ethoxy-2-{2-fluoro-4-methoxy-phenyl)-acetamide was converted to (RS)-N~(4-carbainimidoyI-2-phenoxy-ben2)'i)-2-ethosy-2-(2-fluoro-4-niethoxy-phen)d)-acetamide hydrochloride according to general procedure D. Colorless solid. MS 452.4 ([M+HJ""} Using similar procedures to the ones described in example 106, 3-fIuoro-4-formyl-benzonitrile (CAS 105942-10-7) was converted to the following compounds: Example 107: (RS)-N-(4-Carbaniiimdoyl-2-o-tolyloxy-benzyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide hydrochloride, MS 466.5 ([M+H]"^) Example 108: (IlS)-N-[4-Carbainimidoyi-2-(4-fluoro-phenoxy)-beiizyl]-2-ethoxy-2-(2-fluojo-4-inethoxy-phen]d)-acetamide hydrochloride, MS 470.3 ([M+H]'*} Example 109: (RS)-N-[4-Carbamimido)d-2-(pyridin-3-yIoxy)-benzyl]-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide acetic add, MS 453.5 ([M+H]"^) Example 110 110.1 To a solution of 4-fonnyl-3-hydroxy-benzomtrile (CAS 84102-89-^) (6.90 g) in dry ethanol (165 ml) was added sodium acetate (4.23 g) and hydroxylamine hydrochloride (3.58 g). The mixture was stirred at r.t. for 1 h. The solvent was evaporated and the product was purified by flash chromatography (cyclohexane/EtOAc 8:2 => 1:1) to give 3-hydroxy-4-(hydroxyimino-methyI)-benzonitrile (4.70 g). Light yellow soHd. MS 162.0 ([M]"*") 110.2 A solution of 3-hydroxy-4-(hydroxyimino-methyl)-benzonitrile (1.79 g) in acetic add (16.6 ml) was stirred at 65 "C. Zinc powder (6.59 g) was added portionwise during 30 min. After stirring for a further 1.5 h, the reaction mixture was filtered and the filtrate was concentrated to dryness. 1 N HCl (55.3 ml) was added and the solvent was evaporated. The same procedure was repeated with with water (2x), EtOH (2x) and toluene (2x}. The resulting colorless soHd was dissolved in diethyl ether, filtered and the filtrate was concentrated to give 4-aminomethyl-3-hydroxy-benzonitrile hydrochloride (colorless soKd, 2.5 g) which was used in the next step without further purification. MS 149.2 ([M+H]^) 110.3 (RS}-Ethoxy-(2-fluoro-4-methoxy-phenyl)-acetic acid, described in example 63.1 was coupled with 4-aminomethyl-3-hydroxy-ben2onitrile hydrochloride according to general procedure B to give (RS)-N-{4-cyano-2-hydrosy-beiizyi)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide. Colorless solid. MS 457.1 ([M-H]") 110.4 To a solution of (RS)-N-(4-cyano-2-faydroxy-benZ7l}-2'ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide (310 mg) and 2-cliloro-5-nitropyridine (205 mg) in DMSO (2 ml) was added cesium carbonate (423 mg). The mixture was stirred at 50 "C for 5 h. The solvent was evaporated, the residue was dissolved in EtOAc and washed with water (2x} and brine (Ix). The org. Phase was dried, filtered and concentrated. The product was purified by flash chromatography (cycIohexane/EtOAc 9:1 => 4:6) to give (RS)-N-[4-cyano-2-(5-mtro-pyridin-2-yioxy)-benzyl]-2-ethoxy-2-(2-f!uoro-4-methoxy-phenyi)-acetainide. Light yellow foam. MS 481.4 ([M+H]^) 110.5 (RS)-N-[4-Cyano-2-(5-nitro-pyridin-2-yloxy)-benzyi]-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetaTnide was converted to (RS)-N-[4-carbamimidoyI-2-(5-iiitro-pyridin-2-yloxy)-benzyl]-2-etho::9'-2-(2-fluoro-4-methoxy-phenyl)-acetamide hydrochloride according to general procedure D. Off-white solid. MS 498.3 ([M+H]*) Example 111 (RS)-N-[4-Carbamimidoyl-2-(5-nitro-pyridin-2-)doxy)-ben2yi]-2-ethoxy-2-(2-fluoro-4-methoxy-phenyi)-acetamide hydrochloride was hydrogenated at r.t and normal pressure in EtOH/THF using Vd (10 % on charcoal) as a catalyst to give (RS)-N-[2-(5-amino-pyridin-2-yloxy)-4-carbamimidoyl-benz>d]-2-ethoxy-2-(2-fiuoro-4-methoxy-phenyl)-acetamide hydrochloride. Light yellow solid. MS 468.1 ([M+H]"^) Example 112 112.1 A solution of (RS)-N-(4-cyano-2-hydroxy-benzyl)-2-etiioxy-2-(2-fiuoro-4-methoxy-phenyl)-acetaimde (example 17.3, 626 mg), 4-dimeliiyiajnino pyridine (22 mg) and triethyiamine (407 mg) in dichloromethane (14 ml) was stirred at -20 °C. Trifluoromethanesulfonic add anhydride (604 n^) was added dropwise. The cooling bath was removed and the mixture was stirred at r.t. overnight The mixture was dQuted with dichloromethane and washed with 0.1 N HCl and with water. The org. Phase was dried, filtered and concentrated. The product was purified by flash chromatography (CH2C12 => CH2C12:MeOH 9:1) to give 766 mg of the triflate as a light brovra oil. The trifiate (358 mg) was dissolved in l,2-diinethox7ethane (7.4 ml) and isopropanol (0.9 inl).Phenylboronicacid (184mg)andNa2C03 (10% as a solution in water, 1.6 ml) were added and the mixture was stirred for 30 inin under an argon atmosphere. Tetralds-(triphenylphosphine)-palladium (42 mg) was added and the mixture was heated to reflux for 4 h and stirred at r.t. ovem^ht. The mixture was filtered and the filtrate was diluted with EtOAc and washed with 1 N NaOH (2x) and with water (2x). The org. Phase was dried, filtered and concentrated. The product was purified by flash chromatography (EtOAc/cydohexane 3:7 => 6:4) to give (RS)-N-(5-cyano-biphenyl-2-yhnethyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide (157 mg). Colorless foam. MS 419.3 ([M+H]"^) 112^ (RS)-N-( 5-C7ano-biphenyi-2-ylmethyi) -2-ethoxy-2- (2-fluoro-4-methoxy-phenyl)-acetamide was converted to (RS)-N-(5-carbamimido)d-biphenyl-2-ylmethyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide hydrochloride according to general procedure D. White soHd. MS 436.2 ([M+H]"") Example 113 113.1 In analogy to example 16.4, (RS)-N-(4-cyano-2-hydroxy-benzyl)-2-ethoxy-2-{2-fluoro-4-raethoxy-phenyl)-acetamide (example 110.3) was alkylated with eth^ bromoacetate / cesium carbonate in DMF to give (RS)-(5-cyano-2-{[2-ethoxy-2-(2-fluoro-4-njethoxy-phenyI)-acetylajnino]-methyl}-phenoxy)-acetic add ediyl ester as a colorless soHd. MS 443.4 ([M-H]') 113^ (RS)-(5-C)^no-2-{[2-etiioxy-2-(2-fluoro-4-methoxy-phenyl)-acetylaniino]-methyi}-phenoxy)-acetic add eth'j^ ester was converted to (RS)-(5-carbamimido^-2-l [2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetylamino]-methyl}-phenoxy)-acetic add ethyl ester hydrochloride according to general procedure D. Colorless foam. MS 462.2 ([M+H]"") Using similar procedures to the ones described in example 113, (RS)-N-(4-cyano-2-hydroxy-ben2yl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyi)-acetarnade (example 110.3) was converted to the following compounds: Example 114: (RS)-N-(4-Carbamimidoyi-2-carbamoylmethoxy-benzyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phen}4)-acetamide hydrochloride, MS 433.3 ([M+H]"^) Example 115: (RS)-N-(4-Carbaraimidoyi-2-isopropoxy-beiizyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetarnide hydrochloride, MS 418.3 ([M+H]"^) E^ampJe 116: (RS)-N-[4-Carbamimidoyl-2-(2~hydroxy-ethoxy}-benzyl]-2-ethoxy-2-{2-fluoro-4-methoxy-pheii)^)-acetamide hydrochloride, MS 420.2 ([M+H]"^) Example 317:2-(5-Carbamirnidoy]-2-{[2-etho3cy-2-{2-fluoro-4-methoxy-phenyl)-acetylainino]-methyl}-phenoxy)-N-isopropy!-2-phenyl-acetamide hydrochloride, MS 551.2 ([M+H]"") The starting material for the preparation of 2-(5-carbaimmidoyl-2-{[2-ethoxy-2-(2-fiuoro-4-methoxy-phenyl)-acet)damino]-methyl)-phenoxy)-N-isopropyl-2-phen)^-acetamide hydrochloride, 2-chloro-N-isopropyl-2-phenyl-acetainide, was prepared from alpha-chlorophenylacetyl chloride with isopropyl amine in CH2Cl2/aq. NaOH. Example 118 In analogy to example 20.1, (RS)-(5-carbaininiidoyi-2-{[2-ethoxy-2-(2-fIuoro-4-methox)'-phenyl)-acetylamino]-methyl}-phenoxy)-acetic add ethyl ester hydrochloride (example 113.2) was hydrolysed to give (RS)-(5-carbanimudoyl-2-{[2-ethoxy-2-(2-fl.uoro-4-methoxy-phen)d)-acetylamino]-methyl}-phenoxy)-acetic add Colorless solid. MS 434.2 ([M+H]^) Example 119 In analogy to example 22.1, (RS)-N-(4-cyano-2-liydroxy-benzyl)-2-ethoxy-2-(2-fluoro-4-metiioxy-phenyi)-ace^nnde (example 110.3) was reacted in a Mitsunobu reaction with methyl-(R)-(+)-lactate. The product of this reaction was converted to (RS)-(S)-2-(5-carbamimidoyl-2-| [2-ethoxy-2-C2-fluoro-4-methoxy-phenyl)-acetylatnino] -mediyl}-phenoxy)-propioiuc add ethyl ester hydrochloride according to general procedure D. Colorless foam. MS 476.3 ([M+Hf) Example 120 As a side product of the synthesis of (RS)-(S)-2-(5-carbamimidoyi-2-{[2-ethoxy-2-(2-9uoro-4-methoxy-pheny!)-acetyIamino]-methyl]-phenoxy)-propiomc add ethyl ester hydrochloride (example 119), there was obtained ((RS)-S)-2-(5-caibamiinidoyl-2-U2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetylamino]-meth^}-phenoxy)-propionanQide hydrochloride as a colorless foam. MS 447.3 ([M+H]'') Using similar procedures to the ones described in examples 119 and 120, (RS)-N-(4-q^no-2-hydroxy-benzyl)-2-ethoxy-2-(2-fluoTo-4-methox)'-phenyl)-acetamide (example 110.3) was converted to the following compounds: Example 121: (RS)-(R)-2-(5-Carbamiinidoyl-2-{[2-ethoxy-2-(2-fluoro-4-metfaoxy-phenyl)-acetyiamino]-methyl}-phenoxy)-propionic add ethyl ester hydrochloride, MS 476.1 ([M+H]*) Example 122: (RS)-(R)-2-(5-Carbaniimidoyi-2-I[2-ethosy-2-C2-fluoro-4-methox7-phenyl)-acetylamino]-medi)d}-phenoxy)-propionamide hydrochloride, MS 447.3 ([M+H]^) Example 123 123.1 To a solution of 4-aminomethyl-3-hydroxy-benzonitrile hydrochloride (example 110.2,2.0 g) and triethyiamine (2.19 g) in dichloromethane (20 ml) was added di-tert-butyldicarbonate (2,41 g). The mixture was stirred at r.t for 3.5 h. The mixture was washed with water (3x), dried, filtered and concentrated. The crude product was dissolved in DMF (15.5 ml). Cesium carbonate (4.00 g) and iodoacetamide (2.27 g) were added and the mixture was stirred at r.t. for 3 days. Water was added and the mixtxire was extracted with EtOAc. The org. phase was washed with water, dried, filtered and concentrated. The crude product was dissolved in MeOH and then concentrated to obtain a thick suspension. The solid was filtered off and washed with a small amount of MeOH. This procedure was repeated with the mother liquor to give (2-carbamoyimet}ioxy-4-c}'ano-ben2yI)-carbamic acid tert-butyl ester (a total of 1.88 g) as a colorless solid. MS 304.2 ([M-H]") 123.2 The BOC protecting group of (2-carbamoylmethoxy-4-cyano-benzyl)-carbamic add tert-butyl ester was removed using HCl in dioxane to give 2-(2-aminometh)d-5-cyano-phenoxy)-acetamide hydrochloride as an ofif-white powder. MS 206.1 ([M+H]"^) 123.3 (RS)-(2-Fluoro-4-methoxy-phenyl)-methoxy-acetic add (example 15.1) was coupled with 2-(2-aminoraethyl-5-cyano-phenoKy)-acetamide hydrochloride according to general procedure C. The product of this reaction was converted to (RS}-N-(4-carbaminndoyI-2- carbamoylmethoxy-ben2yI)-2-(2-fluoro-4-methoxy-phen)d)-2-inethoxy-acetamide hydrochloride according to general procedure D. Colorless foam. MS 419.3 ([M+H]"*") Example 124 124.1 {RS}- (2,6-Difluoro-4-methox}^-pheiiyl}-ethoxf-acetic acid (example 101.3) was coupled with 4-aininomethyl-3-phenoxy-ben2omiiile {example 106.3) according to general procedure C to give (RS)-N-(4-cyano-2-phenoxy-benzyl)-2-(2,6-di£luoro-4-methoxy-phenyl)-2-ethoxy-acetamide. Colorless foam. MS 453.1 ([M+H]"^) 124.2 (RS) -N-(4-Cyano-2-phenoxy-beiiz)d) -2 -(2,6-difIuoro-4-methoxy-pheiiyl)-2-ethoxy-acetamide was converted to (RS)-N-{4-carbainiinidoyi-2-phenoxy-benz)d)-2-{2,6-difluoro-4-methoxy-phenyI)-2-ethoxy-acetamide hydrochloride according to general procedure D. Colorless foam. MS 470.2 ([M+H]"^) Example 125 125.1 (RS)- (2,6-I>ifluoro-4-methoxy-phenyl)-ethoxy-acetic add (example 101.3) was coupled with 4-aminomethyi-3-methoxy-benzonitrile (CAS 182159-14-4) according to general procedure B to give (RS)-4-[3-(2,6-difluoro-4-inethoxy-phen7l)-3-ethoxy-2-oxo-propylamino]-3-methoxy-benzonitrile. Colorless oil. MS 391.1 ([M+H]'^) 125.2 (RS)-4-[3-(2,6-Difluoro-4-raethoxy-phenyl)-3-ethoxy-2-oxo-prop)damino]-3-methoxy-benzonitrile was converted to (RS)-N-(4-carbamimidoyl-2-methoxy-benzyl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetainide hydrochloride according to general procedure D. Colorless foam. MS 408.2 ([M+H]"") Example 126 126.1 (RS)- (2,6-Difluoro-4-methoxy-pheny])-ethoxy-acetic add (example 101.3) was coupled with 4-aminomethyl-3-hydroxy-benzonitrile hydrochloride (example 110.2) according to general procedure B to give (RS)-N-(4-cyano-2-hydroxy-benzyl)-2-(2,6-diftuoro-4-methoxy-phenyl)-2-ethoxy-acetamide. Colorless foanx MS 375.4 ([M-H]') 126.2 In analogy to example 16.4, (RS)-N-(4-cyano-2-hydroxy-ben2yl)-2-(2,6-difluoro-4- niethoxy-phenyl)-2-ethoxy-acetamide was alkjdated with iodoacetamide / cesium carbonate in DMF to give (RS)-N-{2-caxbamoyimetiiox)'-4-cyano-beiizyl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetainide as a colorless solid. MS 434.3 ([M+H]"*") 126.3 (RS)-N-{2-Carbamoylmethoxy-4-cyano-benzyi)-2-(2,6-difliioro-4-methoxy-phenyl)-2-ethoxy-acetamide was converted to {RS)-N-(4-carbanuimdoyI-2-carbainoylinethoxy-benz)d)-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetaimdehydrocbloride according to general procedure D. Colorless foam. MS 451.3 ([M+H]"*") Using similar procedures to the ones described in example 126, (RS)-H-(4-cyano-2-hydroxy-ben2yl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetaraide (example 126.1) was converted to the following compounds: Example 127: (RS)-N-[4-Carbamimidoyl-2-{2-fluoro-benzyioxy)-benzyl]-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethox7-acetamide hydrochloride, MS 502.3 ([M+H]"^) Example 128: (RS)-N-[4-Carbamimidoyl-2-(5-chlora-2-fluoro-benzyloxy)-benzyi]-2-{2,6-difIuoro-4-methoxy-phenyl)-2-ethoxy-acetainide hydrochloride , MS 536.3 ([M+H] '*) Example 129: (RS}-N-{4-Carbamimidoy]-2-[(2-methoxy-ethylcarbamoyi)-inethQxy]-benzyi}-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide hydrochloride, MS 509.5 ([M+H]^) The starting material for the preparation of (RS)-N-14-carbamimidoyi-2-[(2-methoxy-ethylcarbamoyi)-inethoxy]-benzyl}-2-(2,6-difluoro-4-methoxy-pheny])'2-ethoxy-acetamide hydrochloride, 2-chloro-N-(2-methoxy-ethyl)-acetamide, was prepared from chloroacetyl chloride with 2-methoxyethyl amine and trieth)damine in CH2C12- Example 130: (RS)-N-{4-Carbamimidoyl-2-[(2-mOTpholin-4-yl-ethylcarbamoyl)-methoxy]-benz>i}-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide hydrochloride, MS 564.3 ([M+H]"") The starting material for the preparation of (RS)-N-{4-carbamimidoyl-2- [(2-morpholin-4-)d-ethTdcarbamoyl)-methoxy]-benzyl}-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide hydrochloride, 2-chloro-N-(2-morpholin-4-yl-eth)d)-acetamide hydrochloride, Was prepared from chloroacet>i chloride with morpholine in CH2CI2. Example 131: {RS)-N-{4-Carbamimidoyl-2-[(2-diethylaiiiino-ethylcarbamoyl)-methoxy]-benzyl}-2-(2,6-difluoro-4-methoxy-phenyl)-2-etho]cy-acetainide hydrocUoride, MS 550.3 ([M+H]^) The starting material for the preparation of (RS)-N-{4-carbamimidoyl-2-[(2-diethylamino-ethylcarbamo}d)-methoxy]-ben2yl}-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide hydrochloride, 2-chloro-N-{2-diethylaimno-ethyl)-acetamide hydrochloride, was prepared from chloroacetyl chloride with diethyiamine in CH2CI2. Examples 132 and 133 In analogy to example 16.4, (RS)-N-(4-cyano-2-hydroxy-benzyl)-2-(2,6-difiuoro-4-methoxy-phenyl)-2-ethoxy-acetaraide {example 126.1) was alkylated with 3-{chlorometh}d)-l,2,4-oxadiazole / cesium carbonate in DMF to give a mixture of N-[4-cyano-2-{[l,2,4]oxadiazol-3-)dmethoxy)-ben2yl]-2-(2,6-difluoro-4-methoxy-phenyI)-2-ethoxy-acetamide and N-(4-cyano-2-cyanomethoxy-benzyl)-2-(2,6-difiuoro-4-methoxy-phenyl)-2-ethoxy-acetamide. These compounds were converted according to general procedure D to give Example 132: (RS)- N-[4-Carbaminiidoyl-2-([l,2,4]oxadiazol-3-yimethoxy)-ben2yl]-2-(2,6-difluoro-4-methoxy-phenyI)-2-ethoxy-acetamide hydrochloride, MS 476.1 ([M+H]"*^) Example 133: (RS)- N-{4-Carbamiinidoyl-2-carbamimido)dmethoxy-ben2yi)-2-(2,6-difiuoro-4-methoxy-phenyl)-2-ethoxy-acetamide hydrochloride ,MS 450.1 {[M+H]"*^) Example 134 In analogy to example 22.1, (RS)-N-(4-cyano-2-hydroxy-benZ)4)-2-(2,6-difluoro-4-methoxy-phenyi)-2-ethoxy-acetamide (example 126.1) was reacted in a Mitsunobu reaction with lH-benzimidazole-2-methanol. The product of this reaction could not be obtained pure and was directly converted to (RS}-N-[2-(lH-benzoimidazol-2-yimethoxy)-4-carbaniimidoyI-benz)4]-2-(2,6-difluoro-4-methoxy-phen}d)-2-ethoxy-acetamide hydrochloride according to general procedure D. Off-\^te foam. MS 524.4 ([M+H]"^) Example 135 135.1 In analogy to example 22.1, {RS)-N-(4-cyano-2-hydroxy-benzyl)-2-(2,6-difiuoro-4-methoxy-phenyl)-2-ethoxy-acetamide (example 126.1) was reacted in a Mitsunobu reaction with [3aS,5R,6aR]-2,2-dimethyl-tetrahydro-cyclopenta[l,3]dioxol-5-ol (CAS 25494-07-9) to give (RS)-N-[4-cyano-2-{(3aS,5S,6aR)-2,2-dimethyl-tetrahydro- c>'clopenta[l,3]dioxol-5-yloxy)-benzyl]-2-(2,6-difluoro-4-methoxy-phenyi)'2-elhoxy-acetamide . Colorless oil. MS 517.3 ([M+H]"") 135.2 (RS)-N-[4-Cyano-2-((3aS,5S,6aR)-2,2-dimethyl-tetrahydro-cydopenta[l,3]dioxol-5-yloxy)-benzyl]-2-(2,6-difiuoro-4-methoxy-phenyl)-2-ethoxy-acetamide was converted to (RS)-N-[4-carbamimido)4-2-({1 S,3R,4S)-3,4-dihydroxy-cydopentyloxy)-beiizyl]-2-(2,6-difluoro-4-methoxy-phen)^)-2-ethoxy-acetamide hydrochloride according to general procedure D. Off-white soUd. MS 494.4 {[M+H]'} Example 136 136.1 To a solution of (RS)-N-(4-cyano-2-hydroxy-benzyl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide (example 126.1, 200 mg) and cyclopentene oxide (894 mg) in ethanol (2 ml) was added potassium carbonate (18 mg). The mixture was stirred at 105 "C for 17 h. The mixture was concentrated and the crude product was purified by flash chromatography (cydohexane => cydohexane/EtOAc 1:1) to give a mixture of (RS) and (SR)-N-[4-cyano-2-((lR,2R)-2-hydroxy-cydopentyloxy)-benzyl]-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide (148 mg). Lightydlowoil. MS 461 ([M+H]"^) 136.2 A mixture of (RS) and (SR)-N-[4-Cyano-2-((lR2R)-2-hydroxy-cydopent)doxy)-benzylj- 2-(2,6-difIuoro-4-methoxy-phenyl)-2-ethoxy-acetamide was converted to a mixture of (RS)and(SR)-N-[4-Carbaraimidojd-2-((lRS,2RS)-2-hydroxy-cydopentyloxy)-benz)i]-2- (2,6-difluoro-4-methoxy-phen)d)-2-ethoxy-acetamide hydrochloride according to general procedure D. Colorless solid. MS 478.1 ([M+H] ^) Example 137 (RS)-(2,6-Difluoro-4-methoxy-phenyI)-methoxy-aceticadd (example 66.1) was coupled with2-(2-aminomethyI-5-cyano-phenoxy)-acetamide hydrochloride (example 123.2) according to general procedure C. The product of this reaction was converted to (RS)-N-(4-carbamimidoyl-2-carbamoylmetfaoxy-benzyl)-2-(2,6-dtfluoro-4-methoxy-phenyI)-2-methoxy-acetamide hydrochloride according to general procedure D. Colorless foam. MS 437.4 ([M+HD Example 138 138.1 (RS)-(2,6-Difluoro-4-methoxy-plien)d)-meliioxy-acetic add (example 66.1) was coupled with 4-aminoinethyl-3-hydroxy-benzomtri]e hydrochloride (example 110.2) according to ■ general procedure C to give (RS)-N-(4-cyano-2-hydroxy-ben27l)-2-(2,6-difluoro-4-methoxy-phenyI)-2-methoxy-acetamide . Colorless foam. MS 361.1 ([M-H]") 13S.2 In analogy to example 16.4, (RS)-N-(4-cyano-2-hydroxy-benzyl)-2-(2,6-difluoTO-4-methoxy-phenyl)-2-methoxy-acetamide was alkylated with 2-cfaloro-N-methylacetamide / cesium carbonate in DMF to give (RS)- N-{4-cyano-2-methyicarbamo)dmethoxy-benZ)d)-2-(2,6-difluoro-4-methoxy-phen)d)-2-methoxy-acet2mide as a colorless foam. MS 434.2 ([M+H]"") 138.3 (RS)-N-(4-Cyano-2-metiiylcarbamoylmethoxy-benzyl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-methoxy-acetamide was converted to {RS)-N-(4-carbamimidoyl-2-methyicarbamo)dmelhoxy-benzyl}-2-(2,6-difluoro-4'methoxy-phenyl)-2-methoxy-acetamide hydrochloride according to general procedure D. Colorless soHd. MS 451.2 ([M+H]^) Using similar procedures to the ones described in example 138.2 and 138.3, (RS)-N-{4-cyano-2-hydroxy-ben2yI) -2-{ 2,6-difIuoro-4-methoxy-phenyI) -2-methoxy-acetamide (example 138.1) was converted to the foDowing compounds: Example 139: (RS)-N-[4-Carbamimido)i-2-(isopropyIcarbamo>d-methoxy)-benz)d]-2-(2,6-difluoro-4-methoxy-phen)d)-2-methoxy-acetaniide hydrochloride, MS 479.3 ([M+H]") Example 140: (RS)-N-l4-Carbamimidoyl-2-[(4-fluoro-phenylcarbamoyl)-methoxy]-benz)d}-2-(2,6-di3uoro-4-methoxy-phenyl)-2-methoxy-acetamide hydrochloride, MS 531.2 ([M+H]"*") Example 141 In analogy to example 22.1, (RS)-N-(4-cyano-2-hydroxy-benzyl)-2-C2,6-difluoro-4-methoxy-phenyl)-2-raethoxy-acetamide (example 138.1) was reacted in a Mitsunobu reaction with 2-hydroxymethyI pyridine. The product of this reaction could not be obtained pure and was directly converted to (RS)- N-[4-carbamiinidoyi-2-(pyridin-2- ylmethoxy)-benzyi]-2-(2,6-difluoro-4-niethoxy-phenyI)-2-inethoxy-acetainide hydrochloride according to general procedure D. Colorless foam, MS 471,2 ([M+H]"^) Example 142 142.1 A solution of 3-fiuoro-4~forrayl-benzomtrile (CAS 1O5942-10-7, 1 g) in THF (25 ml) was cooled to 0°C under argon. Trifluoroethanol (3.36 g) and potassium tert-butylate (0.83 g) were added subsequently. The mixture was stirred for 2 h. The mixture was diluted with EtOAc and washed with water. The org. phase was dried, filtered and concentrated. The product was purified by flash chromatography (SiOa, cyclohexane / EtOAc 1:1) to give 4-formyl-3-(2^2,2-trifluoro-ethoxy)-benzomtrile. Yellow solid. 142.2 In analogy to example 106.2, 4-formyl-3-(2,2,2-trifluoro-ethoxy)-benzonitrile was reacted with hydroxylamine hydrochloride and sodium acetate in ethanol to give 4-(hydroxyimino-methyl)-3-(2^,2-trifluoro-ethoxy)-benzonitrile as a yellow solid. 142.3 In analogy to example 106.3, 4-(hydroxyimino-nieth)d)-3-(2,2,2-trifluoro-ethoxy)- benzonitrile was reduced to 4-aminomethyl-3-(2^,2-trifluoro-ethoxy)-benzQnitrile using zinc in acetic acid. 142.4 (RS)-(2,6-Difluoro-4-methoxy-phenyl)-methoxy-acetic add (example 66.1) was coupled with 4-aminomethyl-3-(2,2,2-trifluoro-ethoxy)-benzomtrile according to general procedure B to give (RS)-N-[4-cyano-2-(2,2,2-trifluoro-ethoxy)-benz)4]-2-(2,6-difiuoro-4-methoxy-phenyl)-2-methoxy-acetamide. Colorless solid. MS 445.0 ([M+H]"^) 142.5 (RS)-N-[4-Cyano-2-(2,2,2-trifluoro-ethoxy)-benz>d]-2-(2,6-difluoro-4-methoxy-phenyl)-2-methoxy-acetamide was converted to (RS)- N- [4-carbamimidoyl-2-(2,2,2-trifluoro-ethoxy)-benzj^]-2-(2,6-difiuoro-4-methoX7-phen}d)-2-methoxy-acetamide hydrochloride according to general procedure D. Colorless soKd. MS 462.1 ([M+H]"") Examples 143 and 144 Using similar procedures to the ones described in example 138.2 and 138.3, (RS)-N-(4-cyano-2 -hydroxy-benzyl) - 2 - (2,6-difluoro-4 - roethoxy-phenyl) - 2- methoxy-acetamide (example 138.1) was converted to the following compounds: Example 143: (RS)-N-[4-Carbamimidoyl-2-(pyridin-3-yhnethox>')-benzyI]-2-(2,6- difluoro-4-methoxy-phenyl)-2-melhoxy-acetamide hydrochloride, MS 471.2 ([M+H]"") Example 144: (RS)-N-[4-CarbamimidoyI-2-(pyridin-4-ylmethoxy)-benzyI]-2-C2,6-difluoro-4-methoxy-phenyl)-2-methoxy-acetamide hydrochloride, MS 471.1 ([M+H]"") Referential Example 145 To a weil stirred ice cooled solution of 3,5-difluorophenol (30.0 g) in CH2CI2 (500 ml) under N2 were added tert-butyldiphenylchlorosilane (63.4 g) and imidazole (17.3 g). The reaction mixture was stirred 15 min before removing the cooling bath. After 3.5 h the reaction was stopped by washing 1 N HCl sol. (2 x 300 ml and 1 x 200 ml), sat. aq. NazCOs sol. (200 ml) and brine (200 ml). The aqueous layers were extracted with more CHiClj (200 ml). After drying (MgSO^) the solvent was evaporated to obtain 84.8 g (100 %) of tert-butyl-(3,5-difIuoro-phenoxy)-diphenyl-silane. Colorless oil. MS 368.1 (M^). Referential Example 146 A well stirred solution under N2 of tert-butyl-(3,5-difluoro-phenoxy)-diphenyl-silane (20.0 g) and N,N,N',N'-pentamethyldiethylenetriamine {9.9 g) in dry THE (600 ml) was cooled to -75 "C. A 1.6 M sol. of BuLi in Hex (35.6 ml) was added via syringe. The reaction mixture was stirred 1 h under cooling (-78 "C). A white precipitate was formed. Glyoxalic acid ethyl ester (50 % in Tol, 22.2 g) was added and it was stirred 2 h at -78 "C. The cooling bath was removed and the clear solution was left to warm to -10 °C (1 h). After dilution with TBME (500 ml) the mixture was washed with 1 N HCl (2 x 500 ml) and brine (250 ml), dried over MgS04 and the solvent was evaporated. The crude product was purified by CC (Hept. then Hept/CHzCb 1:4). 27.9 g (60 %) of (RS)-[4-(lert-butyl-diphenyl-silanyloxy)-2,6-difluoro-phenyl]-hydroxy-acetic acid ethyl ester were obtained next to 7.3 g (36 %) of recovered starting material. Colorless viscous oil. MS 488.4 ([M-t-NH4]'^). Referential Example 147 To a well stirred solution under N2 of (RS)-[4-(tert-butyl-diphenyl-silanyloxy)-2,6-difluoro-phenyl]-hydroxy-acetic acid ethyl ester (14.9 g) in Tol (100 ml) was added Ag20 (14.7 g). The mixture was heated in an oil bath at 115-120 °C and iodoethane( 12.8 ml) in Tol (50 ml) was slowly added from a dropping funnel. After a total of 2 h and 4 h more iodoethane (7.7 ml each) was added. After a total of 5.5 h heating was stopped and the mixture was left to stir over night at RT. The solids were filtered away over 1 cm of dicalite and were washed with AcOEt. The solvent was evaporated to obtain 16.3 g of crude product as a yellow oU. CC (Hepi;CH:Cl2 9:1 to pure CH2CI2) afforded 10.5 (66 %) of (RS)-[4-(tert-butyl-diphenyl-silanyloxy)-2,6-difluoro-phenyl]'ethoxy-acetic acid ethyl ester next to 2.6 g (17 %) of recovered starting material. Colorless oil. MS 453.2 (4, [M-OEty), 441.1 (24, [M--rBu]^)425.2 (100. [M-COOEt]'"). Referential Example 148 To a solution of (RS)-[4-(tert-buryl-diphenyl-si]anyIoxy)-2,6-difluoro-phenyl]-ethoxy-acetic acid ethyl ester (10.4 g) in a THE (50 ml), MeOH (50 ml) and H2O (20 ml) mixture was added LiOH.HaO {1.75 g) and it was stirred 2 h at 60 "C. After cooling water (240 ml) was added and the solution was washed with TBME (240 ml). The aqueous layer was collected, TBME was added (240 ml) and the mixture was acidified with 1 N HCl soL The aqueous layer was extracted with one more portion of TBME. The combined organic layers were dried (MgS04) and the solvent was evaporated to obtained an oil. Solid {RS)-(2,6-difluoro-4-hydroxy-phenyl)-ethoxy-acetic acid (4.6 g, 95 %) was obtained after addition of AcOEt, evaporation of it and drying on the high vacuum over night. Off-white solid. MS 231.1 ([M-H]"). Referential Example 149 (RS}-(2,6-Difluoco-4-hydro)cy-phenyl)-ethoxy-acetic acid (2,3 g) was dissolved in DMF (75 ml) and [(4-aminomethyl-phenyI)-iniino-methyl]-carbamic acid benzyl ester dihydrochloride [Prepared according to Ch. Lila, Ph. Gloanec, L. Cadet, Y. Herve, J. Fournier, F, Leborgne, T. J. Verbeuren, G. De Nanteuil, Synthetic Communications 1998, 28, 23, 4419-4429] (3.18 g) and HOBt (2.15 g) were successively added. The slurry was cooled in an ice bath and N-(3-dimethyl3minopropyl)-N'-ethylcarbodiimide hydrochloride (3.05 g) was added. EtjN (8.0 ml) was slowly added. The resulting mixture was left to stir over night warming up to rt. After removing the solvent precipitation from CH2C!2/MeOH 19:1 yielded the product. Drying over night on the high vacuum afforded 3.0 g (60 g) of pure (RS)'[(4-([2-(2,6-difluoro-4-hydroxy-phenyl)-2-ethoxy-acetylamino]-methyl}-phenyl)-imino-methyI]-carbamic acid benzyl ester. White solid. MS 498.3 (IM+H]"). Referential Example 150 (IlS)-[4-(tert-Butyl-diphenyl-silanylosy)-2,6-difluoro-phenyi]-ethoxy-acetic acid ethyl ester (6.85 g) was dissolved in THF (135 ml) and a 1 M TBAF sol. in THF (15.1 ml) was added. After 3 h the reaction mixture was poured on AcOEt (300 ml) and H20 (300 ml). The aqueous layer was detracted with two more portions of AcOEt (100 ml). The combined organic layers were washed with brine and dried (MgS04) and the solvent was evaporated. Crystallization from ice cold CH:Cl2 afforded 3.08 g (86 %) of (RS)-(2,6-difIuoro-4-hydroxy-phenyl)-ethoxy-acetic add ethyl ester. White crystals. MS 258.9 ([M-H]"). Example 151 (RS)-[(4-{[2-{2,6-difluoro-4-hydroxy-phenyl)-2-ethoxy-acetyiamino]-meth)i}-phea)d)-imino-metiiyI]-cartiamic add benzyl ester (100 mg) was dissolved in EtOH (2 ml). 1-25 M UCl in EtOH (0.1 ml) was added and the mixture was hydrogenated 1.5 h at 1 atm H2 in the presence of a catalytic amount of 10 % Pd/C. After filtration of the catalyst the solvent was removed to obtain 71 mg (88 %) of (RS)-N-(4-carbaiiiiinidoyl-benzyl)-2-(2,6-difluoro-4-hydroxy-phenyi)-2-ethoxy-acetainide hydrochloride. White powder. MS 364.3 ([M+H]^). Example 152 152.1 To a mixture of (RS)-[(4-i[2-(2,6-difluoro-4-hydroxy-phenyl)-2-ethoxy-acetylaiiiino]-methyl)-phenyl)-imino-methyl]-carbamic acid benzyl ester (100 mg), N-(2-hydroxyeth)d)morpholine (29 mg) and polymer bound triphenyiphosphine (-3 mmol/g, 167 mg) in CH2CI2 (2 ml) was added di-tert-butyl azodicarboxylate (93 mg) before shaking 22 h at rt. After filtration of the polymer the solvent was evaporated and the residue was purifiedbyHPLCtoobtain28mgof(23%)(RS)-{[4-({2-[2,6-difluoro-4-(2-morpholin-4-yI-ethoxy)-phenyl]-2-ethoxy-acetylainino}-methyl)-phenyl]-iinino-methyl}-carbamic add benzyl ester. 152.2 (RS)-{[4-({2-i2,6-Difluoro-4-(2-morpholin-4-yl-ethoxy)-phenyl]-2-ethoxy-acetylamino}-methyi)-phenyI]-irnino-methyi}-carbamic add benzyl ester (25 mg) was dissolved in EtOH (2 ml) and hydrogenated 2 h at rt and 1 atm H2 in presence of a catalytic amount of 10 % Pd/C. The catalyst was filtered off, the solvent was evaporated and (RS)-N-(4-carbamimidoyl-benzyi)-2-[2,6-difiuoro-4-(2-morpholin-4-yl-ethoxy)-phenyl]-2-ethoxy-acetamide dihydrochloride was obtained in quantitative yield by predpitation from AcOEt with a 4.6 N HCl sol. in AcOEt. White solid. MS 477.2 ([M+H]*). Examples 153,154 Examples 153 and 154 were obtained in analogy to example 152. 153 (RS)-N-(4-Carbanmmdoyi-benzyl)-2-(2,6-difluoro-4-phenethyioxy-phenyi)-2-ethoxy-acetamide hydrochloride from phenethyl alcohol. White solid. MS 468.2 ([M+H]"^). 154 (RS)-N-(4-Carbamimidoyl-ben2yl)-2-{4-cyclopropylmethoxy-2,6-difluoro-phenyi)-2-ethoxy-acetamide hydrochloride from hydroxymethylcyclopropane. White solid. MS 418.3 ([M+H]^}. Example 155 To a mixture of (RS)-[(4-{[2-{2,6-difluoro-4-hydroxy-phenyl)-2-ethoxy-acetylamino]-methylJ-phenyl)-imino-meth)d]-carbaniic add benzyl ester (300 mg), ethanol (61 mg) and polymer bound triphenylphosphine (~3 nunol/g, 501 mg) in CH2CI2 (6 ml) and DMF (1.5 ml) was added di-tert-butyl azodicarboxyiate (555 mg) before shaking 60 h at rt. After filtration of the polymer the solvent was evaporated and the residue was purified by HPLC. The resulting material was dissolved in MeOH (10 ml) and the solution was acidified with 2 mi of 125 M HCl in MeOH and hydrogenated 2 h at rt and 1 atm H2 in the presence of a catalytic amount of 10 % PdC. After filtration, evaporation of the solvent, HPLC purification and hydrochloride formation 27 mg (10 %) of (RS)-N-(4-carbamimidoyl-benz)d)-2-ethoxy-2-(4-ethoxy-2,6-difluoro-phen)d)-acetamide hydrochloride are obtained. Light yellow soUd. MS 392.1 ([M+H]+). Example 156 156.1 (R5)-(2,6-Di£luoro-4-hydroxy-phenyl)-ethoxy-acetic acid ethyl ester (500 mg) was dissolved in CH2CI2 (20 ml). Cu(0Ac)2 (349 mg), 4-methoxyphenylboronic add (876 mg) and MS4A were added followed by pyridine (760 mg). The mixture was stirred over night before filtration and evaporation of the solvent CC (Kept/ CH2CI2 1:4) afforded 455 mg (65 %) of (RS)-[2,6-difluoro-4-(4-methoxy-phenoxy)-phenyl]-ethoxy-acetic add ethyl ester. Yellow oil. 156.2 (RS)-[2,6-DifIuoro-4-(4-methoxy-phenoxy)-phenyl]-ethoxy-acetic acid ethyl ester (455 mg) was dissolved in THE (2.4 ml), MeOH (2.4 ml) and H2O (1.0 ml) and LiORHaO (104 mg) was added. The reaction mixture was stirred 1 h at 60 °C- The solution was diluted with cold H2O (15 ml) and TBME (15 ml) and acidified with 1 N HQ. The aqueous layer was extracted with two more portions of TBME (15 ml). The combined organic layers were dried (MgS04) and the solvent was evaporated to obtain 398 mg (95 %) of (RS)-[2,6-difluoro-4-(4-roethoxy-phenosy)-phenyl]-ethoxy-acetic add. White waxy solid. MS 336.9 {[M-H]-). 156.3 (RS)-[2,6-Difluoro-4-(4-methoxy-phenoxy)-phen^]-ethoxy-acetic add (398 mg) was dissolved in DMF (15 ml). [(4-aminomethyl-phenyi)-imino-methyi]-carbamic add benzyl ester dihydrochloride [Prepared according to Ch. Lila, Ph. Gloanec, L. Cadet, Y. Herve, J. Fournier, F. Leborgne, T. J. Verbem-en, G. De Nanteuil, Synthetic Communications 1998, 28, 23, 4419-4429] (367 mg) and 1-hydroxybenzotriazole (254 mg) were added and the mixture was cooled to 0 "C. N-(3-Dimethylaminopropyl)-N'-ethylcarbodiimide hydrochloride (254 mg) and triethylamine (1,38 ml) were added and it was stirred 1 h at 0 °C and 5.5 h at rL The solvent was evaporated and the residue was taken up in H2O (40 ml) and CH2CI2 (30 ml). The organic layer was separated, washed with brine and dried (MgS04). The aqueous layers were extracted with two more portions CH2CI2. After evaporation of the solvent CC (CH2CI2 to CH2Clz/MeOH 98:2) afforded 228 mg (32 %) of (RS)-{[4-({2-[2,6-difluoro-4-(4-methoxy-phenoxy)-phenyl]-2-ethoxy-acetylaniino}-roethyl)-phenyl]-imino-methylj-carbamic acid benz)^ ester. White foam. MS 602.0 ([M-H]-). 156.4 (RS)-{[4-({2-[2,6-Difluoro-4-(4-methoxy-phenoxy)-phenyl]-2-ethoxy-acetylamino}-meth)i)-phenyl]-imino-methyl}-carbainic add benzyl ester (181 mg) was hydrogenated 3 h in MeOH (3 ml) at rt and 1 atm H2 in the presence of 10 % Pd/C (6 mg) and 2 M NHs sol- in MeOH (75 |JL). The free benzamidine was isolated by filtration and evaporation of the solvent, dissolved in AcOEt (3 ml) and treated with 1 N HQ to obtain 109 mg (72 %) of (RS)-N-(4-carbamimidoyl-benz)d)-2-[2,6-difluoro-4-(4-methoxy-phenoxy)-phen)d]-2-ethoxy-acetamide. White solid. MS 470.1 ([M+H]"^). Examples 157-161 Examples 157-161 were prepared in analogy to example 156. 157.1 (RS)-[4-(3,4-Dimethoxy-phenoxy)-2,6-difIuoro-phenyl]-ethoxy-acetic add ethyl ester. Yellow oil. 157.2 (RS)-[4-(3,4-Dimethoxy-phenoxy)-2,6-di£luoro-phenyl]-ethox7-acetic acid. Yellow oil. MS 366.9 ([M-H]-). 157.3 (RS)-{[4-(|2-[4-(3,4-Dimethox7-phenoxy)-2,6-di£luoro-piien)'I]-2-ethoxy-acet)damino}-methyl)-phenyl]-iniino-methyl}-carbainic acid benzyl ester. White foam. MS 632.2 ([M-H]-). 157.4 (RS)-N-(4-Carbaiiuinidoyl-benzyl)-2-[4-(3,4-dimethoxy-phenoxy)-2,6-difluoro-phenyl]-2-etiioxy-acetamide hydrochloride. White soUd. MS 500.5 ([M+H]*). 158.1 (RS)-[2,6-Difluoro-4-(3-methoxy-phenoxy)-phenyl]-ethoxy-acetic acid eth)4 ester. Colorless oil. MS 384.4 ([M+NHi]"^). I5S.2 (RS)-[2,6-Difluoro-4-(3-methoxy-phenoxy)-phenyl]-ethoxy-acetic add. Off-white semisolid. MS 356.4 ([M+NHtD. 158.3 (RS)-{[4-({2-[2,6-Difluoro-4-(3-methoxy-phenoxy)-phenyi]-2-ethoxj'-acet)daininD}-methyI)-phenyl]-imino-methyl}-carbamic acid benzyl ester. Yellow foam. MS 604.3 ([M+HD. 158.4 (RS)-N-(4-Carbaminiidoyl-beii2yl)-2-[2,6-difluoro-4-(3-metho3(y-pheaoxy)-phenyl]-2- ethoxy-acetamide hydrochloride. White powder. MS 470.4 ([M+H]"*). 159.1 (RS)-[4-(3-AcetyIamino-phenoxy)-2,6-difluoro-phen)d]-ethoxy-acetic add ethyl ester. Colorless oil. MS 392.1 ([M-H]')- 159.2 (RS)-[4-{3-Acety]amino-phenoxy)-2,6-difluoro-phenyl]-ethoxy-acetic acid. Light yellow foam. MS 364.1 ([M-H]-). 1593 (RS)-{[4-({2-[4-{3-Acet)damino-phenox}')-2,6-difluoro-phenyl]-2-ethoxy-acet)daniino}- metiiyl)-phenyl]-iniino-methyI}-carbamic add benzyl ester. Colorless oil, MS 631.2 ([M+H]^). 159.4 (RS)-2-[4-{3-Acetylaimno-plienoxy)-2,6-difluoro~phenyl]-N-(4-carbamiinidoyl-benzyi)-2-ethoxy-acetamide hydrochloride. Off-white solid. MS 495.4 {[M-H]"). 160.1 (RS)-[4-(4-Cyano-phenoxy)-2,6-difluoro-phenyI]-ethoxy-acetic acid ethyl ester. White solid. 160.2 (RS)-[4-(4-Cyano-phenoxy)-2,6-difluoro-phenyl]-ethoxy-acetic acid. Yellowish gum. MS 332.4 ([M-H]"). 160.3 (RS)-{[4-({2-[4-(4-Cyano-phenoxy)-2,6-difluoro-phenyi]-2-ethoxy-acet)damino}-methyi)-phenyl]-iniino-inethyl}-carbamic acid benzji ester. Orange powder. MS 599.5 au+nr). 160.4 (RS)-N-(4-Carbamimidoyl-benzyl)-2-[4-(4-cyano-phenoxy)-2,6-di£luoro-phenj^]-2-ethoxy-acetamide hydrochloride. Yellowish foam. MS 465.5 ([M+H]*^). 361.1 (RS-)[2,6-Difluoro-4-(3-trifluoromethoxy-phenoxy)-phenyl]-ethoxy-acetic add ethyl ester. Colorless oil. MS 438.3 ([M+NH4]"'). 161.2 (RS)-[2,6-Difluoro-4-(3-trifluoromethoxy-phenoxy)-phenyl]-etiioxy-acetic add. Yellowish oil. MS 391.3 ([M-H]"). 161.3 (RS)-{[4-({2-[2,6-Difiuoro-4-(3-trifluoromethoxy-phenoxy)-phenyl]-2-ethoxy-acetyIamino}-meth)d)-phenyl]-imino-methyi}-carbaniic add benzyl ester. Off-white powder. MS 658.3 ([M+H]*). 161.4 (RS)-N-(4-Carbamimidoyl-benzyl)-2-[2,6-difluoro-4-(3-trifIuoromethoxy-phenoxy)-phenyl]-2-ethoxy-acetamide hydrochloride. White foam. MS 524.5 ([M-t-H]"^). Referential Example 162 A solution of (RS)-(2,6-difluoro-4-hydroxy-phenyl)-ethoxy-acetic acid ethyl ester (500 mg) in pyridine (5 ml) was placed under Ni and cooled to 0 °C. T^jO (813 mg) was added and the resulting solution was left to stir in the ice bath. After 18 h the reaction mixture was poured on a mixture of 50 ml 1 N HCl and ice. The product was extracted with AcOEt. The organic layer was washed with more 1 N HCl (50 ml), water (50 ml) and brine (30 ml). The aqueous layers were extracted with more AcOEt. After drying (MgS04) the solvent was evaporated to obtain 738 mg (98 %) of (RS)-(2,6-difluoro-4-trifluoromethanesulfonyloxy-phenyI)-ethoxy-acetic acid ethyl ester. Yellow oil. MS 393.4 ([M+H]"*"). Referential Example 163 To a solution of (RS)-(2,6-difluoro-4-trifluoromethanesulfonyloxy-phenyl)-ethoxy-acetic acid ethyl ester (200 mg) and 2-(trimethylsilyl)ethanol (603 mg) in DMSO (2.5 ml) was added triethylamine (1.8 ml) followed by Pd(OAc)2 (6 mg) and 1,3-bis(diphenylphosphino)propane (II mg). The flask was put under carbon monoxide and the reaction mixture was stirred 2 h at 70 °C. AcOEt (30 ml) was added and it was washed with 1 N HCl (2x 40 ml), water (2x 40 ml) and brine (30 ml). After drying (MgS04) the solvent was evaporated. CC (Hept/ AcOEt 98:2) afforded 151 mg (76 %) of (RS)-4-(ethoxy-ethoxycarbonyl-methyl)-3,5-difluoro-benzoic acid 2-trimethyisilanyl-ethyl ester. Colorless oil. MS 406.6 ([M+NH4]^). Referential Example 164 (RS-4-(Ethoxy-ethoxycarbonyl-methyI)-3,5-difluoro-benzoic acid 2-trimethyIsilanyl-ethyl ester (414 mg) was dissolved in DMF (1 ml) and a 1 M TBAF sol. in THE (1.12 ml) was added. After 3.5 h more TBAF sol. (0.5 ml) was added. AcOEt (15 ml) was added and the solution was washed with 1 N HCl (15 ml), water (15 ml) and brine (15 ml). After drying (Na2S04) the solvent was evaporated to yield 32 mg (100 %) of (RS)-4-(ethoxy-ethoxycarbonyl-methyl)-3,5-difluoro-benzoic acid. Colorless oil. MS 287.0 ([M-H] ). Example 165 165.1 l,r-Carbonyldiimidazole (88 mg) was dissolved in THF (1 ml) and a solution of (RS)-4-{ethaxy-ethoxycarbonyl-methyl)-3,5-difluoro-benzoic acid (156 mg) in THF (1 ml) was added. After 30 min stirring at rt isobutylamine (41 mg) was added and the mixture was stirred 3 h. AcOEt (20 ml) was added and the solution was washed with 1 N HCl (20 ml). The aqueous layer was extracted with two more portions AcOEt (20 ml), the the combined organic layers were dried (Na2S04) and the solvent was evaporated. CC (Hept/AcOET 3:1) afforded 125 mg (67 %) of (RS)-(2,6-difluoro-4-isobutylcarbamo)d-phen^)-ethoxy-acetic acid ethyl ester. White solid. 165.2 To a solution of (RS)-(2,6-difluoro-4-isobutylcarbamoyl-phenyl)-ethoxy-acetic acid ethyl ester (125 mg) in a mixture of THF (1 ml), MeOH (1 ml) and H2O (0.5 ml) was added LiOH.H20 (31 mg). After stirring 1.5 h at 60 "C AcOEt was added (10 ml) and the product was extracted with H2O (10 ml). The aqueous layer was collected, acidified with 1 N HQ and extracted with AcOEt (2 x 15 ml).The combined organic layers were dried (Na2S04) and the solvent is evaporated to obtain 76 mg (66 %) of (RS)-(2,6-difluoro-4-isobutylcarbamoyl-phenyl)-ethoxy-acetic acid. Off-white solid. MS 333.4 ([M+H]"*). 165.3 (RS)-(2,6-DifIuoro-4-isobutylcarbamoyi-phenyl)-ethoxy-acetic acid (71 mg) was dissolved in DMF (3.5 ml) and [(4-aminomethyl-phenyl)-imino-methyI]-carbamic acid benzyl ester dihydrochloride [Prepared according to Ch. Lila, Ph. Gloanec, L. Cadet, Y. Herv6, J. Foumier, F. Leborgne, T. J. Verbeuren, G. De NanteuH, Synthetic Communications 1998, 28, 23, 4419-4429] (88 mg), disopropylamine (114 mg) and 2-(lH-benzotriazole-l-yl)l,l,3,3-tetramethyIuronium tetrafluoroborate (TBTU) (80 mg) were subsequently added. After 30 min stirring at rt AcOEt (10 ml) was added and the organic layer was washed with 1 N HCl (2 x 10 ml), H^O (10 ml) and brine. The aqua^us layers were extracted with more AcOEt (10 ml). After drying (MgS04) the solvent was evaporated and the crude product was purified by HPLC to obtain 30 mg (23 %) of (RS)-[(4-{[2-(2,6-difluoro-4-isobutyIcarbamoyi-phenyl)-2-ethoxy-acetylamino]-methyI}-phenyl)-iniino-methyl]-carbamic acid benzyl ester. White soHd, MS 581.4 ([M+H]"^). 165.4 To a solution of [(4-{[2-(2,6-difluoro-4-isobutylcarbamo)d-phenyl)-2-ethoxy-acetylamino]-methyi}-phenyl)-imino-methyl]-carbaniic acid benzjd ester (27 mg) in MeOH (1 ml) and 2 M NH3 m MeOH (0.3 ml) was added a spatula tip of 10 % Pd/C. The mixture was placed under 1 atm H2 and stirred 4 h at rt. Filtration and evaporation of the solvent afforded 14 mg (64 %) of 4-(RS)-[(4-carbamimidoyl-benzjicarbamoyl)-ethoxy-methyi]-3,5-difluoro-N-isobutyI-benzainide hydrochloride. White solid. MS 447.5 ([M+H]-^). Examples 166-170 Examples 166-170 were prepared in analogy to example 165. Instead of using CD! for the first coupling step, the products were prepared by following the TBTU mediated coupling procedure described in example 165.3. 166 ; {RS)-4-[(4-CarbamimidoyI-benzykarbamoyl)-ethoxy-methyl]-N-ethyl-3,5-difluoro-benzamide hydrochloride. Yellowish solid. MS 419.4 ([M+H]"^). 167 (RS)-4-[(4-Carbamimidoyi-benzylcacbamoy!)-ethoKy-methyll-3,5-difluoio-H-(2-methoxy-ethyl)-benzamide hydrochloride. Yellow foam. MS 449.5 ([M+H]"^). 168 (RS)-4-[{4-Carbamimidoyl-benzylcarbamoyl)-ethoxy-methyl]-N-cyclopentyl-3,5-difluoro-benzamide hydrochloride. Yellow powder. MS 459.6 ([M+H]*), 169 (RS)-4-[(4-Carbamimidoyl-benzyicarbamoyI)-ethoxy-methyI]-3,5-difluoro-N-{2,2,2-trifluoro-ethylj-benzamidehydrochloride. Yellowish powder. MS 473.3 ([M+H]"*"). 170 (RS)-4-[{4-Carbamimidoyl-benzylcarbamoyl)-ethoxy-methyl]-N-cyclopropylmethyl-3,5-difluoro-benzamide hydrochloride. MS 445.5 ([M+H]"^). Referential Example 171 tert-Butydiphenylchlorosiiane (76.8 g) was added over 30 min to a cooled (0 °C) solution of 2,4-difluorophenol (34.6 g) and imidazole (19.9 G) in CHzCU (400 ml). The cooling bath was removed and the reaction mixture was stirred 2 h at rt before washing it with H2O (400 ml), 5 % aq. NaHCOs (300 ml) and brine. The aqueous layers were extracted with two more portions of CH2CI2 (150 ml). The combined organic layers were dried (Na2S04) and the solvent was evaporated to obtain 102 g (99 %) of tert-butyI-(2,4-difluoro-phenoxy)-diphenyl-silane. Colorless liquid. Referential Example 172 A solution under Ar of terl-butyl-(2,4-difluocQ-phenoxy)-diphenyl-siiane (102 g) and 1,1,4,7,7-pentamethyldiethylenetriamine (50.6 g) in DME (800 ml) was cooled to -70 °C before addition of 1.6 N n-BuLi in hexane (182 ml) over a period of 1 h. The yellow solution was stirred 1 h at -70 °C. 50 % glyoxalic acid ethylester in toluene (113 g) was added over a period of 1 h. The reaction mixture was stirred 2 h more at -70 °C before heating up over 1 "h to 0 °C. Sat. NH4 sol. (300 ml) was added and the pH was lowered to pH = 6 with 2 N HCl. The product was extracted with AcOEt (2 x 400 ml). The organic layers were washed widi brine (500 ml) and dried (NaiSO^) and the solvent was evaporated. CC (Hept to Hept/AcOEt 9:1) afforded 70.8 g (54 %) of (RS)-[3-(tert-butyl-diphenyl-silanyIoxy)-2,6-difluoro-phen)d]-hydroxy-acetic acid ethyl ester. Yellowish oQ. MS 488.5 ([M+H]""). Referential Example 173 A mixture of (RS)- [3-(tert-butyl-diphenyl-silanyloxy)-2,6-difluoro-phenyl] -hydroxy-acetic acid ethyl ester (70.8 g), Ag^O (69.7 g) and iodoethane (117 g) in Tol (700 ml) was stirred 68 h at 90 "C. After filtration and evaporation of the solvent the product was separated from the remaining starting material by MPLC (Hept to Hept/AcOEt 1:9). The procedure was repeated vrith the recovered starting material. 62.5 g (83 %) of (RS)-[3-(tert-butyI-diphenyl-siIanyloxy)-2,6-difluoro-phenyi]-ethoxy-acetic acid ethyl ester were obtained. Light yellow oil. MS 498.3 (1, M^); 441.1 (73. [M-fBu]'); 425.2 (33, [M-COOEt]*). Referential Example 174 To a solution of (RS)-[3-(tert-butyl-diphenyl-silanyloxy)-2,6-difluoro-phenyl]-ethoxy-acetic acid ethyl ester (62.5 g) in THF (250 ml) and MeOH (250 ml) was added H2O (200 ml) and LiOH.H20 (10.5 g) and it was stirred 2 h at 65 °C. MeOH and THF were evaporated and the aqueous residue was washed with Hept/Et20 9:1 ( 2 x 150 ml). The organic layers were extracted with two portions of H2O (200 ml). The combined aqueous layers were cooled in an ice bath and acidified with 35 ml 25 % aq. HCl. Extraction with AcOEt (3 X 200 ml) followed by washing with brine, drying (NajSOi) and evaporation of the solvent afforded 28.7 g (99 %) of (RS)-(2,6-difluoro-3-hydroxy-phenyl)-ethoxy-acetic acid. Yellow viscous oil. MS 231.2 ([M-H]'). Referential Example 174a A solution of (RS)-(2,6-difluoro-3-hydroxy-phenyl)-ethoxy-acetic acid (14.8 g) in EtOH (200 ml) and 1.25 N HCl in EtOH (60 ml) was stirred over night at rt. The solvent was evaporated and the residue was purified by CC (AcOEt/Hept 1:1) to obtain 15.5 g (93 %) of (RS)-(2,6-difluoro-3-hydroxy-phenyl)-ethoxy-acetic acid ethyl ester. Off-white sohd. MS 258.9 ([M-H]-). Referential Example 175 To a solution of (RS)-(2,6-difluoro-3-hydroxy-phenyl)-ethoxy-aceticacid (12.0 g) in DMF (600 ml) was added [(4-aminomethyl-phenyl)-imino-methyl]-carbamic acid benzyl ester dihydrochloride [Prepared according to Ch. Lila, Ph. Gloanec, L. Cadet, Y. Herve, J. Foumier, F. Leborgne, T. J. Verbeuren, G. De Nanteml, Synthetic Communications 199S, 28,23,4419-4429] (18.2 g) and l-hydroxybenzotriazole. The mixture was cooled to 0-5 X and EDC (15.8 g) and trietylamine (62 ml) were added. The mixture was stirred 1 h at 0-5 °C and over night at rt The solvent was evaporated and the residue was dissolved in CH2CI2 and washed with H2O (600 ml), and brine (300 ml). The aqueous layers were extracted with more CH2CI2 (2 x 300 ml). The combined organic layers were dried (Na2S04) and the solvent was evaporated. CO (CH2CI2/2 N NH3 in MeOH 97:3 to 19:1) afforded 10.2 g (40 %) of CRS)-[(4-{[2-(2,6-difIuoro-3-hydroxy-phen5d)-2-ethoxy-acetylamino]-methyl}-phenyi)-imino-methyl]-carbamic add benzyl ester. White foam. MS 498.2 ([M-HH]""). Example 176 (RS)-[(4-{[2-(2,6-Difluoro-3-hydroxy-phenyi)-2-ethoxy-acetyIamino]-methyl5-phenyi)-imino-meth)i]-carbamic acid benzjd ester (250 mg) was dissolved in EtOH (20 ml) and 0.9 N HQ in EtOH (5 ml) was added. After 10 min stirring 10 % Pd/C (II mg) was added and the mixture was hydrogenated 2 h at rt under 1 atm Hj. Filtration, evaporation of the solvent and trituration with MeCN (4 ml) afforded the solid product that was washed with two portions of Et20 (5 ml). After drying on the vacuum at 50 °C 175 mg (87 %) of (RS)-N-(4-carbamimidoyi-benzyl)-2-(2,6-difluoro-3-hydroxy-phenyi)-2-ethoxy-acetamide hydrochloride were obtained. White solid. MS 364.0 ([M+H]"*"). Examples 177-207,207a, 2D7b Examples 177-207b were prepared in two steps (E1/E2 and F1/F2) from (RS)-[(4-{ [2-(2,6-difiuoro-3-hydroxy-phenyi)-2-ethoxy-acetylamino]-methyl}-phenyl)-iniiQO-niethyl]-carbamic add benzyl ester and an appropriate alcohol by the following procedures: Procedure El: A mixture of 1.0 equivalent of (RS)-[(4-{[2-(2,6-di£luoro-3-hydTOxy-phenyI)-2-etioxy-acet)^amino]-methyl}-phenyl)-imino-methyI]-carbamic add benzyl ester, 1.1 equivalents of alcohol, ca. 2 equivalents of polymer bound triphenylphosphine (~3 mM/g) and 2.0 equivalents ofdi-tert-butylazodicarboxylate are shaken 2 days atrLThe reaction mixture is absorbed on a 20 g siEca gel samplet and the product is purified by chromatography (CH2CI2/2 N NHa in MeOH system) Procedure E2: As El but with 1.25 equivalents alcohol and stirriR2 40 h. Procedure Fl: The products from procedure E were hydrogenated at rt and 1 atm H2 in EtOH/1.25 N HCl in EtOH 5:1 in the presence of a catalytic amount of 10 % Pd/C. Filtration and evaporation of the solvent afforded the final compounds. Procedure F2: As Fl but in MeOH instead of EtOH. Were necessary the final compounds were purified by HPLC. No. Name Alcohol Proc. Appearance MS [M+H]^ 177 (RS)-N-(4-Carbamimidoyl- Diethylene El/Fl Brownish 480.1 benzyl}-2-ethoxy-2-{3-[2-(2- ^ycol foam ethoxy-ethoxy)-ethoxy]-2,6- monoethyl difluoro-phenyll-acetamide ether hydrochloride 178 (RS)-N-(4-Carbamimidoyl- 3-Dimethyl- El/Fl Yellowish 449.1 benzyl)-2-[3-(3- amino-1- foam dimethyiamino-propoxy)-2,6- propanol difluoro-phenyl]-2-ethoxy- acetamide dihydrochloride 179 {RS)-N-{4-Carbamimidoyl- Triethylene El/Fl Brownish 510.3 benzyl)-2-(2,6-difluoro-3-{2- glycol foam [2-(2-methoxy-ethoxy)- monomethyl ethoxyj-ethoxyj-phenyl)-2- ether ethox/-acetamide hydrochloride 180 (RS)-N-(4-Carbamknidoyl- 4-Pyridine- El/Fl Brownish 483.1 benzyl)-2-[2,6-dxfluoro-3-(3- propanol foam pyridin-4-yI-propoxy)- phenyl]-2-ethoxy-acetaroide dihydrochloride 181 (RS)-N-(4-CarbamimidoyI- l-(2-Hydroxy- El/Fl Brownish 461.0 benzyl)-2-[2,6-difluoro-3-(2- ethyl)- foam pyrroKdin-1-yl-ethoxy)- pyrrolidine phenyl]-2-ethoxy-acetamide dihydrochloride 182 (RS)-N-(4-Carbaiiuinidoyl- l-Methyl- El/Fl White solid 432.0 benzyl)-2-[2,6-difluoro-3-{l- cyclopropan- methyl-cyclopropylmethoxy)- emethanol phenyl j-2-ethoxy-acetaimde hydrochloride 183 {RS)-N-{4-Carbamimidoyl- l(2-Hydroxy- E2/F2 Yellow foam 475.8 benzyl)-2-[2,6-difluoro-3-(2- ethyl)- piperidin-1-yl-ethoxy)- piperidine phenyl] -2-ethoxy-acetainide dihydrochloride 184 (RS,RS)-N-{4- 3-Methyl-3- E2/F1 Off-white 484.2 Carbamimidoyl-benzyl)-2- [3- oxetane- foam (3-ch]oro-2-h)'droxymeth7l-3- methanol methyl-prop oxy)-2,6-difluoro- phenyl]-2-ethoxy-acetamide hydrochloride 185 {RS)-N-(4-Carbamimidoyl- 2-Ethoxy- E2/F2 Brownish 436.2 benzyI)-2-ethoxy-2-[3-(2- ethanol foam ethoxy-ethoxy)-2,6-difluoro- phenyl] -acetamide hydrochloride 186 (RS)-N-(4-Carbamimidoyl- 2-Methoxy- E2/F2 Brownish 422.1 benzyl)-2-[2,6-difluoro-3-(2- ethanol foam methoxy-ethoxy)-phenyl]-2- ethoxy-acetamide hydrochloride 187 (RS)-N-(4-Carbamimidoyl- 3-Dimethyl- E2/F2 WHtefoam 477.1 ben2yl)-2-[3-{3- amino-2,2- dimethylamino-2,2-dimethyl- dimethyl-1 - propoxy)-2,6-dLfluoro- propanol phenyl] -2-ethoxy-acetamide dihydrochloride 188 CRS)-N-(4-Carbaroimidoyl- 2-(2-Thieny!)- E2/F2 Brownish 474.1 benzyl)-2-[2,6-difluoro-3-(2- ethanol foam thiophen- 2-yl- ethoxy) - phenyl] -2-ethoxy-acetamide hydrochloride 189 (RS,RS)-N-(4- Tetrahydro- E2/F2 Brownish 448.1 CarbamimidoyI-benzyl}-2- furfuryl alcohol foam [2,6-difluoro-3-(tetrahydro- fLiran-2-ylmethoxy) -phenyl] -2-ethoxy-acetamide . hydrochloride 190 {RS)-N-(4-CarbamimidoyI- 2-Methyl E2/F2 White solid 420.1 benzyl)-2-(2,6-difluoro-3- propanol isobutoxy-phenyl) -2 -ethoxy-acetamide hydrochloride 191 CRS,RS,RS)-N-(4- 2-Methyl- E2/F2 Brownish 432.0 Carbamimidoyl-benzyl)-2- cyclopropane- foam [2,6-difluoro-3-{2-methyl- methanol cydopropylmethoxy)-phen)d] - 2-ethoxy-acetainide hydrochloride 192 (RS)-N-(4-Carbaniimidoyl- 2-Cydopropyl- E2/F2 White foam 432.2 benzyl)-2-[3-(2-cyclopropyl- ethanol ethoxy)-2,6-difluoro-phenyl]- 2-ethoxy-acetamide hydrochloride 193 (RS)-N-(4-Carbamimidoyl- Ethanol E2/F2 YeUowish 391.9 benzyl)-2-ethoxy-2-C3-ethoxy- foam 2,6-difluoro-phenyi)- acetamide hydrochloride 194 (RS)-N-(4-Carbaniimidoyi- 1-PropanoI E2/F2 Brownish 406.0 benz7l)-2-(2,6-difluoro-3- foam propoxy-phenyl)-2-ethoxy- acetamide hydrochloride 195 CRS)-N-(4-earbamimidoyl- Hydroxy- E2/F2 Brownish 417.9 benzyl)-2-(3- methyl- foam cyclopropylmethoxy-2,6- cyclopropane difluoro-phenyl)-2-ethoxy-acetamide hydrochloride 196 (RS}-N-(4-Carbamimidoyl- 2-Dimethyl- E2/F2 Brownish 434.9 benzyl)-2-[3-(2- aminoetianol foam dimethylamino-ethoxy)-2,6- difluoro-phenyl]-2-ethoxy-acetamide dihydrochloride 197 (RS)-N-{4-Carbamimidoyl- Cyclobutane- E2/F2 Brownish 432.0 ben2yl)-2-(3- methanol foam cyclobutylmethoxy-2,6- difluoro-phenyl)-2-ethoxy-acetamide hydrochloride 198 (RS)-lSl-(4-Carbamimidoyl- N-(2-Hydroxy- E2/F2 Brownish 475.0 benzyl)-2-{2,6-difluoro-3-[2- ethyl)-2- foam (2-oxo-pyrrolidin-l-yI)- pyrrolidone ethoxy] -phenyU - 2-ethQxy-acetamide hydrochloride 199 (RS)-N-(4-Carbaminiidoyl- 3,3,3- E2/F2 Brownish 460.1 benzyl)-2-[2,6-difluoro-3- Trifluoro-l- foam (3,3>3-trifluoro-propoxy)- propanol phenyI]-2-ethoxy-acetamide hydrochloride 200 (RS}-N-(4-Carbamimidoyl- 3-(2-Hydrox)'- E2/F2 Yellow foam 469.9 benzyl}-2-[2,6-difIuoro-3-(2- ethyl)pyridine pyridin-3-yl-ethoxy)-phenyI]- 2-ethoxy-acetainide dihydrochloride 201 (RS)-N-(4-Carbamiinidoyl- N,N-Diethyl-2- E2/F2 Brownish 477.1 benzyl)-2-(3- hydroxy- foam diethylcarbamoyimethoxy-2,6- acetamide difluoro -phenyl) -2-ethoxy-acetamide hydrochloride 202 (RS)-N-(4-Carbamimidoyl- N-(2-Hydroxy- E2/F2 Brownish 477.0 ben2yl)-2-[2,6-difluoro-3-{2- ethyl)- foam morpholLn-4-)4-ethoxy)- morpholine phenyI]-2-ethoxy-acetaniide dihydrochloride 203 (RSJlS)-N-(4- l-Methyl-3- E2/F2 Brownish 475.0 Carbamimidoyl-benzyl)-2- piperidine- foam [2,6-di£luoro-3-{ 1-methyl- methanol piperidin-3-yImethoxy) - phenyl]-2-ethoxy-acetaniide dihydrochloride 204 {RS,RS)-N-(4- l-Methyl-2- E2/F2 Brownish 475.2 Carbamimidoyl-benzyl)-2- piperidine- oil [2,6-difluoro-3-(l-methyl- methanol piperidin-2-ylmethoxy) -phenyl] -2-ethoxy-acetamide dihydrochloride 205 (RS)-N-(4-Carbamimidoyl- 2-{2-Hydroxy- E2/F2 Yellow foam 469.0 benzyl)-2-[2,6-difluoro-3-(2- ethyl)pyridine pyridin-2-yl-ethoxy)-phenyl]- 2-ethoxy-acetamide dihydrochloride 206 (RS,RS)-N-(4- 2-Piperidm- E2/F2 Brownish 475.0 Carbamimidoyl-benzyl)-2- eethanol foam [2,6-difluoro-3-(2-piperidin-2- yl-ethoxy)-plienyl]-2-ethoxy-acetamide dihydrochloride 207 (RS)-N-(4-Carbamimidoyl- Methanol(3 E2/F2 Off-white 378.5 benzyl)-2-(2,6-difluoro-3- equivalents) foam methoxy-phenyl)-2-ethoxy- acetamide hydrochloride 207a {RS)-N-(4-Carbamimidoyl- Cyclohexanol E2/F2 Off-white 446.0 benzyl)-2-(3-cydohex}doxy- sohd 2,6-difluoro-phenyl}-2-ethoxy-acetamide hydrochloride 207b (RS)-N-(4-Carbamimidoyl- 1-tert-Butoxy- E2/F2 Off-white 447.5 benzyl)-2- [2,6-difluoro-3- carbonyl-4- foam {piperidin-4-yloxy)-phenyl]-2- hydroxy- ethoxy-acetamide piperdine dihydrochloride Example 208 208.1: To a solution under Ar of (RS)-(2,6-difluoro-3-hydroxy-phenyl)-ethoxy-acetic acid ethyl ester (320 mg) in CH2C12 (10 ml) was added copper(II)acetate (230 mg), 4-fluorobenzeneboronic acid 516 mg) and powdered MS4A (2 g). After addition of triethlyamine (622 mg) the mixture was stirred 40 h at rt. The solids were filtered away and the solvent was evaporated. CC (AcOEt:Hept 1:9 to 1:1) afforded 154 mg of (RS)-[2,6-difluoro-3-(4-fiuoro-phenox7)-phenyll-ethoxy-acetic acid ethyl ester as a brownish oil. 208.2; (R,S)-[2,6-Difluoro-3-(4-fluoro-phenoxy)-phenyl]-ethoxy-acetic acid ethyl ester (145 mg) was dissolvedin MeOH/THF 1:1 (2 ml) and H2O (0.5 ml) and LiOH.H20 (36 mg) were added. The solution was stirred 2 h at 60 °C. THF and MeOH were evaporated and the residue was diluted with H2O (10 ml) and acidified with 1 N HCl (pH = 2). The product was extracted with AcOEt (2 x 30 ml). The organic layers were washed with brine (20 ml). Drying {Na2S04) and evaporation of the solvent afforded 140 mg of (RS)-[2,6-difluoro-3-(4-fluoro-phenoxy)-phenyl]-etho3cy-acetic acid as a yellowish oil. 208,3: To a solution of (RS)-[2,6-difIuoro-3-(4-fluoro-phenoxy)-phen)d]-ethoxy-acetic acid (140 mg) in DMF (5 ml) was added [(4-aminomethyI-phenyl)-iinino-inethyI]-carbamic acid benzyl ester dihydrochloride (149 mg) and l-hydroxybenzotriazole (92 mg). The mixture was cooled to 0-5 °C and EDC (130 mg) and triethylamine (0.5 mi) were added. After stirring 2 h at 0-5 °C the solvent was evaporated and the residue was partitioned between KjO (25 ml) and AcOEt (25 ml). The aqueous layer was extracted with more AcOEt (25 ml). The organic layers were washed with brine (25 ml) and dried (Na2S04) and the solvent was evaporated. CC (AcOEt/Hept 1:3 to 4:1) afforded 120 mg of (R,S)-N-[4-(amino-benzyloxycarbonimidoyIiniino-methyl)-benzyI]-2-[2,6-difluoro-3-(4-fluoro-phenoxy)phenyl)-2-ethoxy-acetamide as white crystals. 208.4: (R,S)-N-[4-(Aniino-benzyloxycarbonimidoylimino-methyl)-benzyl]-2-[2,6- difluoro-3-(4-fluoro-phenoxy)phenyl)-2-ethoxy-acetamide (120 mg) was dissolved in MeOH (10 ml) and 1.25 N HCl in MeOH (2 ml) was added. The mixture was hydrogenated 1 h at 1 atm H; and rt in presence of 10 % Pd/C (12 mg). After filtration and evaporation of the solvent (R,S)-N-(4-carbaminiidoyl-benzyl)-2-[2,6-difluorO'3-(4-fluoro-phenoxy)-phenyl]-2-ethoxy-acetamide hydrochloride was obtained by crystallization from MeCN/EtjO. White solid. MS 458.5 ([M+H]^). Examples 209-212 Examples 209-212 were prepared in analogy to example 208: No. Name Appearance MS [M-HH]^ 209 (RS)-N-(4-Carbamimidoyl-benzyl)-2-[2,6- Off-white 441.5 difiuoro-3-(pyridin-3-yloxy)~phenyl]-2-ethoxy- foam acetamide dihydrochloride 210 (RS)-N-(4-Carbamimidoyl-benzyl)-2-[2,6- White 508.1 difluoro-3-(3-trifluoromethyI-phenoxy)- crystals phenyl] -2-ethoxy-acetamide hydrochloride 211 (RS)-N-(4-Carbamimidoyl-benzyI)-2-(2,6- White 454.1 difluoro-3-m-tolyloxy-phenyl)-2-ethoxy- crystals acetamide hydrochloride 212 (RS)-N-(4-Carbaniunidoyl-benzyl)-2-ethoxy-2- White 484.1 [3-(3-ethoxy-phenoxy)-2,6-difluoro-phenyl]- crystals acetamide hydrochloride Example 213 To an ice cooled mixture under Ar of (RS}-(2,6-difIuoro-3-hydroxy-phenyl)-ethoj:y-acetic ad-d, 4-aminomethyl-benzordtrile hydrochloride (10.6 g) and 1-hydroxybenzotriazole {9.8 g) in DMF (140 ml) was added EDC (13.9 g) and triethylamine (55 ml). The mixture was stirred 2.5 h at 0 °C and 2 d at rt The solvent was evaporated and H2O (250 ml) was added. The product was extracted with AcOEt (2 x 200 ml). The organic layers were washed with 5 % NaHCOs aq. sol. (100 ml), brine 100 ml). After drying (Na2S04) the solvent was evaporated. CC (AcOEt/Hept 2:3) afforded 7.66 g (49 %) of (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-3-hydroxy-phenyl)-2-ethoxy-acetamide. White solid. MS 364.1 ([M+NH4]'^). General procedure G for the preparation of the N-hydroxy-benzamldines: 1.0 equivalent of the benzonitrile was dissolved in EtOH and 5.0 equivalents of hydroxylamine hydrochloride and triethylamine were added. The solution was stirred over night before addition of 5.0 equivalents more of hydrox)damine hydrochloride and triethylamine. After stirring again over night the products were isolated by evaporation of the solvent and CC. General procedure H for the reduction of the N-hydroxy-benzamidines: The n-hydroxy-benzamidines were hydrogenated in EtOH over night at rt and 1 atm H2 in presence of a catalytic amount of 10 % Pd/C and 10 equivalents of AcOH. The products were isolated by filtration and evaporation of the solvent. Where necessary a crystallization or CC were carried out. Example 214 To a solution under Ar of (RS)-N-(4-cyano-ben2yl)-2-(2,6-difluoro-3-hydroxy-phenyl)-2-ethoxy-acetamide (200 mg) in DMF (10 ml) was added CSCO3 (226 mg) and 3-bromopentane (105 mg). The solution was stirred over night at 80 °C. The solvent was evaporated and the residue was taken up in H2O (50 ml). The product was extracted with AcOEt (2 X 100 ml). The organic layers were washed with H2O (2 x 50 ml) and dried (NaaS04) and the solvent was evaporated. CC (AcOEt/Hept 2:3 to AcOEt) afforded 190 mg (79 %) of (RS)-N-(4-cyano-benzyl)-2-ethoxy-2-[3-(l-ethyl--propoxy)-2,6-difluoro- 1 phenyl]-acetamide. This material was converted to (RS)-N-(4-carbarnimidoyl-benzyl)-2- ;thoxy-2-[3-(I-ethyl-propoxy)-2,6-difluoro-phenyl]-acetamide acetate by the sequence of procedures G and H. Off-white soHd. MS 434.4 ([M+H]^). Examples 215-216 Example 215 was prepared in analogy to example 214. Example 216 was prepared from (RS)-N-(4-cyano-ben2yl)-2-(2,6-difluor 0-3-hydroxy-phenyl)-2-ethoxy-acetamide by a sequence of procedures E2, G and H. No. Name Appearance MS [M+H]* 215 (RS)-N-(4-Carbamimidoyl-benzy!)-2-(3- Brown solid 432.5 cyciopentyIoxy-2,6-difluoro-phenyI)-2-ethoxy- acetamide acetate 216 (RS)-N-(4-CarbamimidoyI-benzyl)-2-[2,6- White solid 448.2 difluoro-3-(tetrahydro-pyran-4-yioxy)-phenyl]-2- ethoxy-acetamide acetate Referential Example 217 A solution under Ar of (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-3-hydroxy-phenyl)-2-ethoxy-acetamide (5.0 g) in pyridine (50 ml) was cooled to -10 "C and Irifluoromethanesulfonic acid anhydride (4.5 g) was added over a period of 10 min. The reaction mixture was stirred 2 h at 0 °C. More Irifluoromethanesulfonic acid anhydride was added {4.5 g) over 30 min and it was stirred 30 min more at 0 "C. Pyridine was evaporated, H2O (200 ml) was added and the product was extracted with AcOEt (2 x 100 ml). The organic layers were washed with brine, combined and dried (Na2S04) before evaporation of the solvent. CC (AcOEfHept to AcOEt) afforded 6.2 g (89 %) of (R,S)-trif!uoro-methanesulfonic acid 3-[(4-cyano-benzylcarbamoyl)-ethoxy-methyl]-2,4-difluoro-phenyl ester. YeUowoil. MS 479.1 ([M+H]*). General procedure I for the reduction of the N-hydroxy-benzamidines: To a 0.015 M solution of the N-hydroxy-benzamidine in EtOH was added AcOH (10 equivalents) and Raney-Ni (2.5 equivalents, Degussa 313 Z type). The reaction mixture was stirred over night at rt. The catalyst was filtered away, the solvent was evaporated, H2O (3/5 of the initial EtOH volume) was added and the mixture was treated with 25 % aq. NH4OH (1/5 of the initial EtOH volume). The solvent was evaporated and the residue was purified by CC (CH2Cl2/MeOH/25 % aq. NH4OH). The products were isolated as the hydrochlorides after treatment of a niethanoHc solution with 1.25 N HCl/MeOH. Example 218 218.1 To a solution of (RS)-trifluoro-methanesulfonic add 3-[(4-cyano-benzylcarbamoyl)-ethoxy-methyl]-2,4-difluoro-phenyl ester (570 mg) in dioxane (20 ml) was added bis(pinacolato)diboron (454 mg), dry KOAc (351 mg) and [PdCl2(PPh3)2] (25 mg). The reaction mixture was stirred 24 h at 100 °C. After cooling to rt 5-bromopyridine (377 mg), 2 N aq. NasCOa sol. (6 ml) and [PdCl2(PPh3)2] (25 mg) were added. The resulting mixture was stirred 1 h at 90 "C. The sohds were filtered away and washed with H2O (100 ml) and AcOEt (80 ml). The aqueous layer was isolated and extracted with more AcOEt (100 ml). The organic layers were washed with brine (2 X 80 ml), combined and dried over Na2S04. The solvent was evaporated and the crude product was purified by CC (AcOEt/Hept 3:7 to 3:1) to obtain 315 mg (65 %) of (RS)-N-{4-cyano-benzyl)-2-(2,6-difluoro-3-pyridin-2-yl-phenyl)-2-ethoxy-acetamide. Colorless oil. MS 408.3 ([M+H]^). 218.2 (RS)-N-(4-Cpno-benzyl)-2-(2,6-difluoro-3-pyridin-2-yl-phenyl)-2-ethoxy-acetamide (310 mg) was converted into (RS)-2-(2,6-difluoro-3-pyridin-2-yl-phenyl)-2-ethoxy-N-[4-(N-hydroxycarbamimidoyI)-benzyl]-acetamide (320 mg, 95 %) following procedure G. Colorless oil. MS 441.3 ([M+H]^). 218.3 (RS)-2-(2,6-Difluoro-3-pyridin-2-yl-phenyl)-2-ethoxy-N-[4-(N-hydroxycarbamimidoyI)-benzyll-acetamide (315 mg) was converted into (RS)-N-(4-carbamimidoyl-benzyl)-2-(2,6-difluoro-3-pyridin-2-yl-phenyl)-2-ethoxy-acetamide dihydrochloride (225 mg, 63 %) following procedure I Off-white foam. MS 425.3 ([M+H]"*"). Examples 219-222 Examples 219-222 were prepared in analogy to example 218: No. Name Aryl-X Appearance MS [M-i-Hl^ 219 (RS)-N-(4-Carbamimidoyl- 5-Bromo-2- Off-white 455.5 benzyl)-2- [2,6-difluoro-3-(6- methoxy-pyridine foam methoxy-pyridin-3-yl)-plienyi]- 2-ethoxy-acetamide dihydrochioride 220 {RS)-N-(4-Carbamimidoyl- 3-Bromopyridine Off-white 425.4 benzyl)-2-(2,6-difluoro-3- foam pyridin-3-yl-phenyl)-2-ethoxy- acetamide dihydrochioride 221 (RS)-N-(4-Carbamimidoyl- 5-Bromo- White foam 426.4 benzyI)-2-{2,6-difluoro-3- pyrimidine pyrimidin-5-yl-phenyl)-2- ethoxy-acetamide dihydrochioride 222 (RS)-N-{4-Carbamimidoy!- 4-Iodopyridine Yellowish 425.3 benzyl)-2-(2,6-difiuoro-3- foam pyridin-4-yl-phenyl)-2-ethoxy- acetamide dihydrochioride Referential Example 223 (RS)-[3-(tert-Butyl-diphenyl-siIanyloxy)-2,6-difiuoro-phenyl]-methoxy-acetic acid ethyl ester was prepared in analogy to example 173 from (RS)-[3-(tert-butyl-diphenyl-siIanyIoxy)-2,6-difluoro-phenyi]-hydroxy-acetic acid ethyl ester and iodomethane. Yellowish oU. MS 484.2 (4, [M'^]^); 427.1 (29, [M-tBu']""); 411.2 (14, [M-COOEt]^). Referential Example 224 I A 1.0 M solution of TBAF in THF (100 ml) was added under stirring to a solution of (RS)-(2,6-difluoro-3-hydroxy-phenyl)-methoxy-acetic acid ethyl ester (38.5 g) in THF (500 mi). The reaction mixture was stirred over night at rt before evaporation of the solvent. The residue was partitioned between 600 ml AcOEt/HjO 1:1 and extracted with more AcOEt (200 ml). The organic layers were washed with brine 200 ml, combined and dried over NajSO*. After evaporation of the solvent CC {CH2CI2, then CH2CI2/2 N NH3 in MeOH 97:3) yielded 18.3 g {94 %) of (RS)-(2,6-difluoro-3-hydroxy-phenyl)-methoxy-acetic acid ethyl ester. YeUowish solid. MS 24S.3 ([M-H]"). Referential Example 225 A solution of (RS)-(2,6-difluoro-3-hydroxy-phenyl)-methoxy-acetic add ethyl ester (11.6 g) and LiOH.HiO in THF (40 ml), MeOH (40 ml) and H2O was stirred 2 h at 65 "C. The organic solvents were evaporated, H2O was added (50 ml) and the pH was lowered with 2 N HCl to pH — 2. The product was extracted with AcOEt (3 x 50 ml). The organic layers were washed with brine (100 ml), combined and dried (Na2S04). Evaporation of the solvent afforded 9.6 g (94 %) of (RS)-(2,6-difluoro-3-hydroxy-phenyl)-methoxy-acetic add. White solid. MS 217.1 ([M-H]")- Referential Example 226 (RS)-N-(4-Cyano-benzyl)-2-(2,6-difluoro-3-hydroxy-phenyl)-2-methoxy-acetamide was prepared from (RS)-(2,6-difluoro-3-hydroxy-phenyl)-methoxy-acetic add in analogy to (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-3-hydroxy-phenyl)-2-ethoxy-acetamide (example 213). White foam. MS 330.8 ([M-H]"). Referential Example 227 (RS)-Trifluoro-methanesulfonic acid 3-[(4-cyano-benzyicarbamoyl)-methoxy-methyl]-2,4-difluoro-phenyl ester was prepared from (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-3-hydroxy-phenyl)-2-methoxy-acetamide in analogy to (RS)-trifluoro-methanesiilfonic add 3-[(4-cyano-benzylcarbamoyl)-ethoxy-methyl]-2,4-difluoro-phenyl ester (example 217). YeUowoil. MS 482.3 ([M-i-NH^]"^). General procedure K for the Suzuki coupling reaction: To a 0.1 M solution in Tol of (RS)-triSuoro-metlianesuIfonic add 3"[(4-cyano-benzyicarbamoyl)-methoxy-methyI]-2,4-difluoro-phenyl ester (1.0 equivalent) was added KzCOj (1.5 equivalents) and the boronic acid (2.0 equivalents). The solution was degassed by bubbling 10 min Ar through it before adding [Pd(PPh)4] (0.03 equivalents). The reaction mixture was stirred over night at 100 "C before isolation of the product by CC (AcOEtHept). Examples 228-233 Examples 228-233 were prepared from (RS)-trifluoro-methanesulfonic acid 3-[(4-cyano-beii2ylcarbamoyl)-methoxy-methyl]-2,4-difluoro-phenyl ester by subsequently carrying out procedures K, G and H. Procedure H was modified by replacing HCl with 10 equivalents of AcOH. No. Name RBCOH); Appearance MS [M+H]^ 228 (RS)-N-(4-CarbamimidoyI-benzyl)-2- m-Tolyl- White 424.0 (2,4-difluoro-3'-methyl-biphenyl-3-y!)- boronic acid crystals 2-methoxy-acetamide 229 (RS)-N-(4-CarbaminiidoyI-benzyI)-2- 4-Methyl- Orange 424.4 (2,4-difluoro-4'-methyl-biphenyl-3-yl)- benzene foam 2-raethoxy-acetamide hydrochloride boronic acid 230 (RS)-N-(4-Carbaminiidoyl-benzyI)-2- 4-Fluoro- White solid 428.5 methoxy-2-(2,4,4'-trifluoro-biphenyl-3- benzene yl)-acetamide acetate boronic acid 231 {RS)-N-(4-CarbamimidoyI-benzyl)-2- 4-(Methy]thio)- Whitesolid 456.4 {2,4-difluoro-4'-methylsulfanyl- phenyl-boronic biphenyl-3-yl)-2-methoxy-acetamide acid hydrochloride 232 (RS)-N-(4-Carbarainiidoyl-benzyl)-2- 3-(Trifluoro- Whitesolid 478.3 (2,4-difluoro-3'-trifiuoromethyl- niethyl)phenyl biphenyl-3-yl)-2-methoxy-acetamide boronic acid acetate 233 (RS)-N-(4-Carbamimidoyi-benzyl)-2- 4-Methoxy- Whitesolid 440.5 (2,4-difluoro-4'-methoxy-biphenyl-3- phenylboronic yl)-2-methoxy-acetamide add hydrochloride Referential Example 234 To a solution in DMSO (40 ml) of (RS)-trifluoro-methanesiilfonic acid 3-[(4-cyano-benzyicarbamoyl)-methoxy-methyi]-2,4-difluoro-phen}4 ester (5.0 g) was added MeOH (21.8 ml), EtsN (4.5 ml), [Pd(0Ac)2] (73 mg) and l,3-bis-(diphenylphosphino)propane. The solution was saturated with carbon monoxide. The dark reaction mixture was stirred 2 h at 70 "C and 1 atm carbon monoxide. The mixture was poured on ice cold H2O (400 ml) and 2 N aq. HCl sol. (30 ml). The product was extracted with AcOEt (2 x 200 ml). The organic layers were washed with brine (2 x 200 ml), combined and dried over Na2S04. The solvent was evaporated and the residue was fractionated by CC (AcOEt/Hept 1:9 to 4:1) to obtain 2.45 g (61 %) of (RS)-3-[(4-cyano-benzylcarbamoyl)-methoxy-methyl]-2,4-difiuoro-benzoic acid methyl ester. Yellowish solid. Referential Example 235 A solution of (RS)-3-[(4-cyano-benzyIcarbamoyl)-methoxy-methyl]-2,4-di£luoro-benzoic acid methyl ester (2.05 g) and LiOH.HjO (241 mg) in THF/MeOH/HiO 1:1:0.5 (75 mi) was stirred 1 h at rt. The organic solvents were evaporated, ice cold H2O (50 ml) was added and the pH was lowered (pH = 2) by addition of 2 N aq. HCl sol. The product was extracted with AcOEt (2 x 120 ml). The organic layers were washed with brine (100 ml), combined and dried over Na2S04. Evaporation of the solvent yielded 1.80 g of (RS)-3-[(4-cyano-benzylcarbamoyI)-methoxy-methyl]-2,4-difluoro-benzoic acid. White solid. MS 359.4 ([M-H]'). Example 236 236.1 To a solution under Ar of (RS)-3-[(4-cyano-benzylcarbamoyl)-methoxy-methyl]-2,4-difluoro-benzoic acid (150 mg) in DMF (2 ml) was added l.l'-carbonyldiimidazole (74 mg). The reaction mixture was stirred 15 min at rt before addition of morpholine. After stirring 2 h at rt hydroxylamine hydrochloride (289 mg) and EtsN (0.3 ml) were added. The reaction mixture was stirred 20 h at rt, then it was poured on H2O (20 ml) and extracted with AcOEt (2 x 20 ml). The organic layers were washed with brine and dried (NaiSO^) and the solvent was evaporated. CC (AcOEt/MeOH 99:1 to 9:1) yielded 111 mg (58 %) of (RS)-2-[2,6-difluoro-3-(morpholine-4-carbonyl)-phenyl]-N-[4-(N-hydroxycarbaminiidoyl)-benzyl]-2-methoxy-acetamide. White solid. MS 463.5 ([M+H]"^). 236.2 A solution of (RS)-2-[2,6-difluoro-3-(morpholine-4-carbonyl)-phenyl]-N-[4-(N-hydroxycarbamimidoyl)-benzyl]-2-methoxy-acetamide (125 mg) was hydrogenated 2 days atrtand 1 atm H2 in presence of 10 % Pd/C {13 mg)andAcOH (143 mg). The catalyst was filtered away and the solvent was evaporated to obtain 115 mg of (RS)-N-(4-carbaniiniidoyI-benzyl)-2-[2,6-difluoro-3-(morpholine-4-carbonyI)-phenyI]-2-methoxy-acetamide acetate. Off-white solid, MS 447.1 ([M+H]^). Examples 237-241 Examples 237-241 were prepared in analogy to example 236: No. Name Amine Appearance MS 237 (RS)-3-[(4-Carbamimidoyl- Ethylamine Off-white 405.3 benzylcarbamoyl)-methoxy-methyI]- hydrochloride solid N-ethyl-2,4-difluoro-benzamide acetate 238 {RS)-3-[(4-Carhamimidoyl- 2-Methoxy- Off-white 435.3 benzylcarbamoyl)-methoxy-methyl]- ethylamine solid 2,4-difluoro-N-(2-methoxy-ethyl)- benzamide acetate 239 (RS)-3-[(4-Carbamimidoyi- Diethylamine Off-white 433.4 benzylcarbamoyO-methoxy-methyl]- foam N,N-diethyI-2,4-difluoro-benzamide acetate 240 (RS)-3-[(4-CarbamimidoyI- 2,2,2- Off-white 459.1 benzylcarbamoyl)-methoxy-methyl]- Trifluoro- solid 2,4-difluoro-N-(2,2,2-trif[uoro-ethyl)- ethylamine benzamide acetate 241 (RS)-3-[(4-Carbamimidoyl- Aminomethylc Off-white 431.4 benzylcarbamoyl)-methoxy-methyl]- yclopropane solid N-cyclopropyImethyl-2,4-difluoro- benzamide acetate Examples 242-244 Example 242-244 were prepared from (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-3-hydroxy-plienyl)-2-methoxy-acetaniide by a sequence consisting of a Mitsiinobii reaction (procedure E2), the formation of the N-hydroxy-benzamidines (procedure G) and the reduction to the benzamidines (procedure I). No. Name ROH Appearan MS ce [M+H]^ 242 (RS)-N-(4-Carbamimidoyi-benzy!)- 2-(Hydroxy- White 441.5 2-[2,6-difluoro-3-(pyridin-2- methyl)pyridine) foam ylmethoxy)-phenyl]-2-methoxy- acetamide dihydrochloride 243 {RS)-N-(4-Carbamimidoyl-benzyl)- 3-CHydroxy- Off-white 441.3 2-[2,6-difluoro-3-(pyridin-3- ineth}d)pyridine foam yhnethoxy) -phenyl J -2-methoxy- acetamide dihydrochloride 244 (RS}-N-(4-Carbamimidoyl-benzyl)- 4-(Hydroxy- Greenish 441.4 2-[2,6-difluoro-3-(pyridin-4- methyl)pyridine foam ylmethoxy)-phenyI]-2-methoxy- acetamide dihydrochloride Example 245 (RS)-N-(4-Carbaraimidoyl-benzyl)-2-[2,6-difluoro-3-(4-fluoro-phenoxy)-phenyI]-2-methoxy-acetamide acetate 245.1 To a solution of (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-3-hydroxy-phenyl)-2-methoxy-acetamide (370 mg) in 1,2-dichloroethane (10 ml) was added copper(II)acetate (222 mg), 4-fiuorobenzoic acid (467 mg) and powdered MS4A (2 g). EtsN (563 mg) was added and the mixture was stirred 2 days at rt. The mixture was passed over silica ge! eluting with AcOEt. CC (AcOEt/Hept 1:3 to 3:1) yielded 203 mg (61 %) of (RS)-N-(4-cyano-benzyl)-2-[2,6-difluoro-3-(4-fluoro-phenoxy)-phenyl]-2-methoxy-acetainide. Yellow oil. MS 427.0 ([M-HH]"). 245.2 {RS)-N-(4-Cyano-benzyi)-2-[2,6-di£luoro-3-{4-fluoro-phenoxy)-phenyl]-2-methox7-acetamide (200 mg) was transformed in (RS}-2-[2,6-difluoro-3-(4-fluoro-phenoxy}-phenyl]-N-[4-(N-hydroxycarbainiinidoyl)-benzyl]-2-methoxy-acetamide (174 mg, 81 %) by procedure G. 245 Reduction of (RS)-2-[2,6-difluoro-3-(4-fluoro-phenoxy)-phenyl]-N-[4-(N- hydroxycarbamimidoyi)-ben2yl]-2-methoxy-acetamide (173 mg) by procedxire H afforded 176 mg (93 %) of (RS}-N-(4-carbamiinidoyl-beiizyl)-2-[2,6-difluoro-3-(4-fluoro-phenoxy)-phenyl]-2-methoxy-acetaniide acetate. White crystals. MS 444.1 ([M+H]"*"). Example 246 (RS)-N-(4-Carbamimido)d-benzyl)-2-[2,6-difluoro-3-(pyridin-3-yloxy)-phenyl]-2-methoxy-acetamide acetate was prepared in analogy to example 245. Off-white crystals. MS 427.1 ([M+H]^). Example 247 247.1 To a solution of (RS)-2-(4-bromo-2,6-difluoro-phenyl)-N-(4-cyano-beiizyl)-2-methoxy-acetamide (example 69.1, 247 mg) in 1,2-dimethoxyethane (5 ml) was added tetralds(triphenyiphosphine) palladium (0) (73 mg). A solution of phen)dboromc acid (118 mg) in EtOH (2.1 ml) and a solution of sodium carbonate (563 mg) in water (3 ml) were added. The mixture was stirred for 1.5 h at 85 "C. The solids were filtered off and the filtrate was evaporated. The product was purified by flash chromatography (cyclohexane/EtOAc 2:1 => EtOAc) to give (RS)-N-(4-cyano-benzyi)-2-(3,5-difluoro-biphenyl-4-yI)-2-methoxy-acetamide (172 mg). Off-white solid. MS 393.1 ([M+H]"^) 247.2 (RS)-N-(4-Cyano-benzyl)-2-(3,5-difiuoro-biphenyl-4-yl)-2-methoxy-acetaniide was converted to (RS)-N-(4-carbamimidoyi-benz)d)-2-(3,5-difluoro-biphenyl-4-)d)-2-methoxy-acetamide hydrochloride according to general procedure D. Off-white solid, MS 410.2 ([M+H]"") Example 248 248.1 The crude 4-bromo-2,6-difluorobenzaldehyde described in example 69.1 was reacted according to general procedure A using ethanol / dioxane as a solvent The product of this reaction was subsequently coupled with 4-aininomethyi benzonitrile according to general procedure B to give (RS)-2-(4-bromo-2,6-difluoro-phenyl)-N-{4-cyano-benzyl)-2-ethoxy-acetamide. Yellow oil. 248.2 In analogy to example 247.1, (RS)-2-(4-bromo-2,6-difluoro-phenyl)-N-(4-cyano-benzyl)-2-ethoxy-acetamide was reacted with phenylboronic acid to give (RS)-N-(4-cyano-benz)d)-2-(3,5-difluoro-biphenyl-4-yl)-2-ethoxy-acetamide. Yellow solid. MS 407.3 ([M+H]"^) 248.3 (RS)-N-(4-Cyano-benzyl)-2-(3,5-difIuoro-biphenyl-4-yl)-2-ethoxy-acetamide was converted to {RS)-N-(4-carbamiinidoyl-benzyi)-2-(3,5-difluoro-biphenyl-4-5d)-2-ethoxy-acetamide hydrochloride according to general procedure D. Ofif-white solid. MS 424.4 C[M+H1") Example 249 Using similar procedures to the ones described in example 248.2 and 248.3, (RS)-2-{4-bromo-2,6-difluoro-phenyl)-N-(4-cyano-benzyl)-2-ethoxy-acetamide was converted to (RS)-N-(4-carbamimidoyl-benzyI)-2-[2,6-difiuoro-4-(lH-indol-5-yl)-phenyI]-2-ethoxy-acetamide acetic acid. Colorless solid. MS 463.0 ([M+H]"*") Example 250 250.1 In analogy to example 247.1, (RS)-2-(4-bromo-2,6-difluoro-phenyl)-N-(4-cyano-benzyl)-2-ethoxy-acetamide (example 248.1) was reacted with 2-fiiranboromc acid to give (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-4-furan-2-yl-phenyl)-2-ethoxy-acetamide. Off-white soUd. MS 397.0 {[M+H]"^) 250.2 In analogy to example 15.5, (RS)-N-(4-cyano-ben2yl)-2-(2,6-difluoro-4-ftiran-2-yl- phenyl)-2-ethoxy-acetamide was reacted with hydroxylamine hydrochloride to give (RS)- 2-(2,6-difluoro-4-furan-2-yI-phen)d)-2-ethoxy-N-[4-(N-hydroxycarbamiinidoyl)-benzyl]- acetaraide. Colorless solid. MS 430.0 ([M+H]"^) 250.3 In analogy to example 37.5, (RS)-2-{2,6-difluoro-4-fiiran-2-yl-phenyl)-2-ethoxy-N-[4-(N-hydroxycarbaminiidoyl)-benzyI]-acetamide was reduced to give (RS)-N-(4-carbamimidoyl-ben2yi)-2-(2,6-difluoro-4-ftiran-2-yl-phenyl)-2-ethoxy-acetainide acetate. Colorless soHd. MS 414.0 ([M+H]"") Example 251 As a side product of example 250.3, there was obtained N-{4-carbamimidoyI-benzyl)-2-[2,6-difluoro-4-(tetrahydro-furan-2-yl)-phenyl]-2-etlioxy-acetamide acetic acid . Off-white soUd. MS 418.0 ([M+H]"") Example 252 252.1 In analogy to example 247.1, (RS)-2-(4-bromo-2,6-difluoro-phenyl)-N-(4-cyano-ben2yl)-2-ethoxy-acetamide (example 248.1) was reacted with 3-hydroxyphenylboronic add. The product of this reaction was alkylated with ethylbromoacetate and cesiumcarbonate in DMF (analogous to example 16.4) to give (RS)-{4'-[(4-cyano-ben2:ylcarbamoyl)-ethoxy-methyl]-3',5'-difluoro-biphenyl-3-yloxy}-acetic add ethyl ester. Colorless oil. MS 509.1 ([M+H]") 252.2 (RS)-{4'-[(4-Cyano-benzyIcarbamoyl)-ethoxy-methyI]-3',5'-difluoro-biphenyl-3-yIoxy)-acetic acid ethyl ester was converted to (RS)-l4'-[(4-carbamimidoyi-benZ}dcarbamoyl)-ethoxy-meth)4]-3',5'-difluoro-biphenyl-3-yloxy}-acetic add ethyl ester hydrochloride according to general procedure D. Colorless foam. MS 526.2 ([M+H]"^) 252,3 In analogy to example 20.1, (E5)-{4'-[(4-carbamimidoyl-benzyicarbamoyl)-ethoxy-methyl]-3',5'-difluoro-biphenyl-3-yloxy}-acetic add ethyl ester hydrochloride was hydrolyzed to (RS}-{4'-[(4-carbamimidoyl-benzylcarbamo)d)-ethoxy-methyl]-3',5'-difluoro-biphen5d-3-yloxy}-acetic add. Colorless solid. MS 498.3 ([M+H]^) Using similar procedures to the ones described in example 252.1 and 252.2, (RS)-2-(4-bromo-2,6-difluoro-phenyl)-N-(4~q^ano-benzyl)-2-ethoxy-acetamide (example 248.1) was converted to the following compounds: Example 253: (RS)-N-(4-Carbamimidoyl-benzyl)-2-(3'-carbamoylmethoxy-3,5-difluoro-biphenyl-4~yl)-2-ethoxy-acetamide hydrochloride,MS 497.2 ([M+H]"*) Example 254: (RS)-N-(4-Carbamimidoyl-ben2yl)-2-[3,5-difluoro-3'-(2-hydroxy-ethoxy)-biphen)d-4~yl]-2-ethoxy-acetamide hydrochloride, MS 484.3 ([M+H]"^) Example 255: (RS)-N-(4-Carbamiinidoyl-benzyl)-2-[3'-(3-dimethyIaniino-propoxy)-3,5-difluoro-biphenyl-4-yl]-2-ethoxy-acetamidehydrochloride, MS 525.3 ([M+H]"^) Example 256 256.1 In analogy to example 247.1, (RS)-2-(4-bromo-2,6-difluoro-phenyi)-N-(4-cyano-benzyI}- 2-ethox)'-acetamide (example 248.1) was reacted with 2-hydroxyphenyIboronic add to give {RS)-N-(4-cyano-benzyl)-2-(3,5-difiuoro-2'-hydroxy-biphenyl-4-yl)-2-etlioxy-acetamide. Off-white solid. MS 423.0 ([M+H]"") 256.2 In analogy to example 22.1, {RS)-N-(4-cyano-benzyI)-2-(3,5-difluoro-2'-hydrox}'-biphenyI-4-yl)-2-ethoxy-acetamide was reacted in a Mitsunobu reaction with 2-benzyloxy-ethanol, diethyl azodicarboxylate and triphenyl phosphine in THF to give (RS)-2-[2'-(2-benzyIoxy-ethoxy)-3»5-difluoro-biphenyl-4-yl]-N-(4-cyano-benzyl)-2-ethoxy-acetamide. YeUow oil. MS 557.2 ([M+H]"") 256.3 {RS)-2-[2'-(2-Ben2yloxy-ethoxy)-3,5-difIuoro-biphenyl-4-yl]-N-(4-cyano-benzyl)-2-ethoxy-acetamide was converted to (RS)-2-[2'-(2-benzyioxy-ethoxy)-3,5-difluoro-bipheny!-4-yl]-N-(4-carbamimidoyI-benzyI)-2-ethoxy-acetamide hydrochloride according to general procedure D. Colorless solid. MS 574.3 {[M+H]"^) Example 257 257.1 In analogy to example 16.4, (RS)-N-{4-cyano-ben2;)^)-2-{3,5-difluoro-2'-hydroxy- biphen)d-4-yl)-2-ethoxy-acetamide (e:rample 256.1) was alkylated with l-chloro-2- dimethylaminoethane hydrochloride and cesimncarbonate in DMF to give (RS)-N-(4- cyano-benzyl)-2-[2'-(2-dimetbylamino-ethoxy)-3,5-difluoro-biphenyl-4-yl]-2-ethoxy- acetamide. Colorless solid. MS 494.1 ([M+H]"^) 257.2 (RS)-N-{4-Cyano-benzyl)-2-[2'-(2'dimethylamino-ethoxy)-3,5-difluoro-biphenyl-4-)i]-2-ethoxy-acetamide was converted to {RS)-N-(4-carbamiinidoyI-benzyl)-2-[2'-(2-dimethylamino-ethoxy)-3,5-dtfluoro-biphenyl-4-yl]-2-etho::q'-acetaniide hydrochloride according to general procedure D. Colorless sohd. MS 511.1 ([M+H]"*") Using similar procedures to the ones described in example 257.1 and 257.2, (RS)-N-(4-cyano-benzyl)-2-(3,5-di£luoro-2'-hydroxy-biphenyI-4-yl)-2-ethoxy-acetainide {example 256.1) was converted to the following compounds: f Example 258: {RS)-N-(4-CarbaininiidoyI-benzyl)-2-[3,5-difluoro-2'-(2-hydro3y-ethosy)-biphenyl-4-yl]-2-ethoxy-acetamide hydrochloride, MS 484.1 {[M+H]'^) Example 259: (RS)-{4'-[(4-Carbamimidoyl-benzylcarbariioyl)-ethoxy-rQethyl]-3',5'-difluoro-biphenyl-2-yloxy}-acetic acid ethyl ester hydrochloride, MS 526.2 {[M+H]"^) Example 260 In analogy to example 20.1, (RS)-{4'-[(4-carbamiiiudoyl-benzjdcarbamoyl)-ethoxy-methyi]-3',5'-difluoro-biphenyl-2-yloxy}-acetic acid ethyl ester hydrochloride was hydrolyzed to (RS)-{4'-[(4-carbamimidoyI-ben2ylcarbamoyI)-ethoxy-methyl]-3',5'-difluoro-biphenyI-2-yloxy}-acetic add. Coloriess solid. MS 496.4 ([M-H]") Example 261 261.1 In analogy to example 16.4, (RS)-N-(4-cyano-benzyl)-2-(3,5-difluoro-2'-hydroxy- biphenyI-4-yl)-2-ethoxy-acetamide (example 256.1) was alkylated wilii iodoacetamide and cesiumcarbonate in DMF. The product of this reaction was reacted with hydroxylamine hydrochloride in analogy to example 15.5 to give (RS)-2-(2'-carbamoy(inethoxy-3,5- di£luoro-bipheny]-4-yl)-2-ethoxy-N-[4-(N-hydroxyc3rbamimidoyl)-benzyl]-acetamide. Colorless solid. MS 513.1 CIM+H]"") 261^ In analogy to example 37.5, (RS)-2-(2'-carbamoyimethoxy-3,5-difluoro-biphenyl-4-y!)-2- ethoxy-N-[4-(N-hydroxycarbamimidoyI)-benzyl]-acetaniide was reduced to give (RS)-N- {4-carbamimidoyl-benzyl)-2-(2'-carbamoylmethoxy-3,5-difluoro-biphen54-4-)d)-2- ethoxy-acetamide acetate. Colorless soUd. MS 497.2 ([M+H]"^) Example 262 262.1 To a solution of (RS)-2-(4-bromo-2,6-difluoro-phen)^)-N-(4-cyano-benz;^)-2-ethoxy- acetamide (example 248.1, 800 mg) in DMSO (9 ml) were added bis(pinacolato)diboron (546 mg), potassium acetate (581 mg) and dichloro(l,r- bis(diphenylphosphino)ferrocene)paUadium(II) (44 mg).The mixture was stirred at 85°C for 5 h and at 50 "C ovemighL Dicfaloro(l,l'- bis(diphenyiphosphino)ferrocene)palladium(n) (44 mg) was added and the mixture was stirred at 85°C for 8 h and at 50 °C ovemighL After cooling to r.t., ice water was added. The mixture was filtered and the filtrate "was extracted with EtOAc. The org. phase was dried, filtered and concentrated. The product was purified by chromatography (Si02, cyclohexane /EtOAc 4:1 ^> EtOAc) to give CRS)-N-(4-cy^no-benz)d)-2-[2,6-difluoro-4-(4,4,5,5-tetramethyl-[l,3,2]dioxaborolan-2-yI)-phenyI]-2-ethoxy-acetamide (625 mg). Off-white soHd. MS 457.3 ([M+H]"") 262.2 To a stirred solution of (RS)-N-(4-q'ano-benzyl)-2-[2,6-difiuoro-4-(4,4,5,5-tetrainethyl- [l,3,2]dioxaborolan-2-yl)~phen)d]~2-ethoxy-acetamide (300 mg) in l^-dimethoxyethane (8 ml) was added 4-bromopyridine hydrochloride (387 mg). A solution of sodium carbonate (210 mg) in water (2.1 ml) and dichloro(l,r- bis(diphenylphosphino)ferrocene)palladium (11) (48 mg) were added. The mixture was I stirred at 85'C for 4 h and at r.L overnight. After cooling to i.t, ice water was added. The mixture was filtered and the filtrate was extracted with EtOAc. The org. phase was washed with brine, dried, filtered and concentrated. The product was purified by chromatography ■ (Si02, cyclohexane /EtOAc 2:1 => EtOAc) to give (RS)-N-(4-cyano-benz)^)-2-(2,6-difiuoro-4-pyridin~4-yI-phen)^)-2-ethoxy-acetamide (189 mg). Ofif-white solid. MS 408.2 ([M+H]") 262.3 (RS)-N-(4-Cyano-benzyl)-2-(2,6-difluoro-4-pyridin-4-yl-phen}d)-2-etlioxy-acetamide was converted to (RS)-N-(4-carbaniimidoyl-benzyi}-2-(2,6-difiuoro-4-pyridin-4-yl-phen>d)-2-ethoxy-acetamide hydrochloride according to general procedure D. Colorless solid. MS 425.2 ([M+H]-") Using similar procedures to the ones described in example 262.2 and 262.3, (RS)-N-(4-cyano-benzyl)-2-l2,6-difluoro-4-(4,4,5,5-tetramethyi-[l,3,2]dioxaborolan-2-yi)-phen)4]-2-ethoxy-acetamide (example 262.1) was converted to the following compounds: Example 263: (RS)-N-(4-Carbamimidoyl-benz)4)-2-(2,6-difluoro-4-pyrimidin-5-)d-phen)d)-2-ethoxy-acetamide hydrochloride, MS 426.2 ([M+H]"^) Example 264: (RS)-N-{4-Carbamimidoyl-benz)4)-2-(2,6-difluoro-4-pyrimidin-2-yl-phenyl)-2-ethoxy-acetamide hydrochloride, MS 426.1 ([M+H]*) Example 265: (RS)-N-(4-Carbamiimdoyl-benz)4)-2-(2,6-difluoro-4-pyridin-2-yI-phenyl)-2-ethoxy-acetamide hydrochloride, MS 425.1 ([M+H]"^) Example 266: (RS}-2-[4-(2-Amino-pyriDiidin-5-yl}-2,6-difluoro-phenyi]-N-(4-carbamimido}d-benzyl)-2-ethoxy-acetamide hydrochloride, MS 441.0 ([M+H]"*") E:rample267:(RS)-N-(4-Carbamimidoyl-benzyl)-2-(2,6-difluoro-4-pyridin-3-yl-phenyl)-2-ethoxy-acetamidehydrochloride , MS 424.6 ([M]"*") Example 268: (RS)-2-[4-(6-Ainino-pyridin-2-yl)-2,6-difluoro-phen7l|-N-(4-carbainimidoyl-benz7l)-2-ethox7-acetamidehy-drochloride , MS 440.1 {[M+H]"^) Example 269: (RS)-2-[4-{5-Amino-pyridm-2-yl)-2,6-difluoro-phenyl]-N-(4-carbaniimidoyl-beiizyl)-2-ethoxy-acetamide hydrochloride, MS 440.0 ([M+H]'*') Example 270: (RS)-4'-[(4-CaTbamimidoyl-benzylcarbainoyl)-ethoxy-iiiethyi]-3',5'-difluoro-biphenyl-3-carboxyIic acid methyl ester hydrochloride, MS 482.1 {[M+H]"^) Example 271: (RS)-(2-[4-(6-Amino-pyridin-3-yl)-2,6-difiuoro-phenyl]-N-{4-carbamimidoy]-beiizyl)-2-ethoxy-acetamide hydrochloride, MS 440.3 ([M+H]'^) Example 272 In analogy to example 20.1, (RS)-4'-[(4-carbamimidoyi-benzylcarbamoyl)-ethoxy-methyl]-3',5'-difluoro-biphenyl-3-carboxyiic acid methyl ester hydrochloride (example 270) was hydrolyzedto (RS)-4'-[(4-carbamimido)d-benzylcarbamo54)-ethoxy-methyl]-3',5'-difluoro-biphen)d-3-carboxyUc acid. Off-white solid. MS 468.1 ([M+H]^) Example 273 In analogy to example 15.4, (RS)-{2-[4-(6-amino-pyridin-3-yI)-2,6-difluoro-phenyl]-N-(4-carbamimidoyl-benzyl)-2-ethoxy-acetamide hydrochloride (example 271) was reacted with ethylchloroformate and triethylamine in DMF to give (RS)-{amino-[4-({2-[4-C6-araino-pyridin-3-yl)-2,6-difluoro-phenyl] -2-edioxy-acetyIamino} -methyi)-phenyl] -methylene)-carbamic add eth}^ ester. Off-white solid. MS 512.1 ([M+H]"^) Example 274 To a a solution of (RS)-(2-[4-(6-amino-pyridin-3-yl)-2,6-difluoro-phen}d]-N-(4- carbamimidoyl-benzyl)-2-ethoxy-acetamide hydrochloride (example 271,60 mg) in DMF (1 ml) were added hydroxylamine hydrochloride (27 mg) and triethylamine (38mg).The mixture was stirred at 50 °C for 2.5 h. After cooling to r.t, the mixture was partitioned between EtOAc and ice water and extracted with EtOAc. The oR2. phase was washed with water, dried, filtered and concentrated to give (RS}2-[4-(6-aniino-pyridin-3-yi)-2,6-difluoro-phenyl]-2-ethoxy-N-[4-(N-hydroxycarbaniimidoyl)-benzyi]-acetamide{57mg). Colorless solid. MS 456.0 ([M+H]^) Example 275 275.1 In analogy to example 262.2, {RS)-N-(4-cyano-ben2yl)-2-[2,6-difluoro-4-(4,4,5,5- tetraineth.yl-[l,3,2]dioxaborolan-2-yl)-ph.enyl]-2-ethoxy-acet:amide (example 262.1) was reacted with 2-bromobenzaldehyde to give (RS)-N-(4-cyaiio-benZ)d)-2-(3,5-di£luoro-2'-formyl-biphenyl-4-yI)-2-ethoxy-acetamide. Off-white solid. MS 435.0 ([M+H]"^) 275.2 To a suspension of (RS)-N-(4-cyano-benzyI)-2-(3,5-difiuoro~2'-formyl-biphenyl-4-yl)-2-ethoxy-acetamide (500 mg) in EtOH (1.2 nJ) at 0 "C was added sodium borohydride (91 mg). After 5 min the ice bath was removed. Ice water was added and the mixture was extracted with EtOAc. The org. phase was dried, filtered and concentrated. The product was purified by chromatography (Si02, cyclohexane /EtOAc 1:2 => EtOAc) to give (RS)-N-(4-cyano-benzyl)-2-(3,5-difluoro-2'-hydroxymethyl-biphenyl-4-yl)-2-ethoxy-acetamide {413 mg). Colorless solid. MS 437.0 ([M+H]*) 275.3 (RS) -N-{4-Cyano-benzjd) -2-( 3,5-difluoro-2'-hydroxymethyl-biphenyl-4-yl)-2-ethoxy-acetamide was converted to (RS)-N-(4-carbaiiiimidoyl-benzyl)-2-(3,5-difluoro-2'-hydroxyinethyl-biphenyl-4-yi)-2-ethoxy-acetamide hydrochloride according to general procedure D. Colorless solid. MS 454.0 ([M+H]*) Example 276 As a side product of example 275.3, there was obtained (RS)-N-(4-carbanumidoyl-benzyl)-2-(2'-chloromethyi-3,5-difluoro-biphenyl-4-^)-2-ethoxy-acetamide. Colorless solid. MS 472.0 ([M+H]"") Example 277 277.1 In analogy to example 15.5, (RS)-N-(4-cyano-benz}d}-2-(3,5-difluoro-2'-formyl-biphen)4-4-yl)-2-ethoxy-acetainide (example 275.1) was reacted with hydroxjdamine hydrochloride to give (RS)-2-[3,5-difluoro-2'-(hydroxyimino-methyl)-biphenyi-4-yI]-2-ethoxy-N-[4-(N-hydroxycarbamimidoyI)-ben2:)d]-acetamide. Colorless solid. MS 483.1 ([M+H]"^) 277.2 In analogy to example 37.5, (RS)-2-[3,5-difiuoro-2'-(hydroxyimino-meth)4)-biphen}4-4- yl]-2-ethox}'-N-[4-(N-hydroxycarbanumido5d)-benzyl]-acetamide was reduced to give (RS)-2-(2'-aminomethyl-3,5-difluoro-biphenyl-4-yl}-N-(4-carbamimidoyi-benzyl)-2- ethoxy-acetamide acetate. Light green soHd. MS 453.4 ([M+H]"^) Example 278 27S.1 2-Fluoro-3-hydroxy-4-methox}'-benzaldehyde (CAS 79418-73-8) was benzylated to give 3-beiizylo]Q'-2-fluoro-4-methox7-ben2aldehyde in analogy to example 15.4. Light yellow oil. MS 260.1 ([M]"^) 278.2 3-Beiizyloxy-2-fluoro-4-methoxy-benzaldehyde was converted to (RS)-(3-benzyloxy-2-fluoro-4-methoxy-phenyl)-methoxy-acetic add according to general procedure A. Colorless gum. MS 319.1 ([M-H]") 278.3 (RS)-(3-Benzyloxy-2-fluoro-4-methoxy-phenyl)-methoxy-acetic acid was debenzylated by hydrogenation in analogy to example 16.2 and then coupled with 4-aminobenzonitrile according to general procedure C to give (RS)-N-(4-cyano-benzyl)-2-(2-fluoro-3-hydroxy-4-methoxy-phenyl)-2-methoxy-acetamide. Off-white foam. MS 345.1 ([M+H]"^) 278.4 A mixture of (RS)-N-(4-cyano-bemyl)-2-(2-fluoro-3-hydroxy-4-methoxy-phen)d)-2-methoxy-acetamide (150 mg), phenyl boronic add (58 iR2), copper (11) acetate (79 mg), pyridine (0.18 ml) and activated molecular sieves (4 A) at r.t in CH2CI2 under an argon atmosphere was stirred for 24 h. More copper (II) acetate (40 mg), phen)4 boronic add (29 mg) and pyridine (0.9 ml) were added to the mixture and stirring was continued for 16 h. The mixture was filtered and the cake washed with 15 ml CH2C12, The filtrate was washed with 1.0 N Ha (25 ml), 1.0 N NaOH (25 ml) and brine (25 ml), dried (MgS04). filtered and concentrated (rotavapor) to leave the crude product as a brown gum. The crude produd was purified by flash chromatography (cyclohexane => cydohexane/EtOAc 2:3) to give (RS)-N-(4-Cyano-benzyl)-2-(2-fluoro-4-methoxy-3-phenoxy-phen)d)-2-methoxy-acetamide (107 mg) as an off-white foam. MS 421.2 ([M+H]"^) 278.5 (RS) -N-(4-Cyano-ben2yl) -2~(2-fluoro-4-methoxy-3-phenoxy-phen7[)-2-methoxy-acetamide was converted to (RS)-N-(4-carbamimidoyl-benzyi)-2-(2-fluoro-4-methoxy-3-phenoxy-phenyI)-2-methoxy-acetamide hydrochloride according to general procedure D. Colorless soHd. MS 438.3 ([M+H]"") Example 279 279.1 To a solution of (RS)-N-(4-c7ano-benzyl)-2-(2-fluoro-6-hydroxy-phenyi)-2-metiioxy-acetamide {1 g, example 80.4) in dichloromethane (25 ml) were triethylamine (1.02 ml) and DMAP (39 mg). WhUe maintaining temperature at 0'C by cooling with an ice bath, trifluormethane sxilfonic anhydride (0.63 ml) was added slowly. The ice bath was removed after 15 min. Stirring was continued for 5 hrs at r.t. The reaction mixture was diluted with dichloromethane, and washed with water, KHCO3 solution (10%) and again water. The organich layer was dried over MgS04, filtered and concentrated. The crude product was purified by flash chromatography (cydohexane => cyclohexane/EtOAc 1:1) to give (RS)-trifluoro-methanesulfonic add 2-[(4-cyano-benzyicarbamoyl)-methoxy-methyi]-3-fluQro-phenyl ester (1.16 g) as light yeUow soHd. MS 447.2 ([M+H]"") 279.2 A solution of (RS}-trifluoro-methanesulfonic acid 2-[(4-cyano-benz)^carbamoyl)-methoxy-methyi]-3-fluoro-phenyl ester (600 mg) and PPhs (42 mg) in TEA (10 ml) was deoxygenated by passing a stream of argon through the reaction mixture. Ethynyltrimethylsilane (0.28 ml) and palladium(II)acetate (9 mg) were added- The mixture was stirred for 5 hrs at 50°C. After cooling to r.L, the reaction mixture was diluted with water and extracted with EtOAc. The organic layers were combined, dried over MgSO^, filtrated and concentrated. The crude product was purified by flash chromatography (cydohexane => cydohexane/EtOAc 7:3) to give (RS)-N-(4-cyano-ben2yl)-2-(2-fluoro-6-trimethyisilany]ethynyl-phenyl)-2-methoxy-acetainide (278 mg) as ofif-white soUd. MS 395.2 ([M+H]*) 279.3 A solution of (RS)-N-(4-cyano-benz;)d)-2-(2-fluoro-6-trimethylsilan-)dethynyl-phen}d)-2-methoxy-acetamide (214 mg) inEtOH (10 ml) was treated with KzCOs (82 mg). The reaction mixture was stirred over night at r.t, then concentrated. The residue was taken up in water and extracted with EtOAc The organic layers were combined, dried over MgS04 and concentrated to give (RS)-N-(4-cyano-ben2y])-2-(2-fluoro-6-triniethyisilan5dethynyI-phenyl)-2-methoxy-acetaniide (150 rag) as off-white solid. MS 323.2 ([M+H]*) 279.4 (RS)-N-(4-Cyano-ben2)d)-2-(2-fluoro-6-trimethylsilanyIethynyl-phenyl)-2-methoxy-acetamide was converted to (RS)-N-(4-carbaraimido>d-benzyi)-2-(2-ethynyl-6~fluoro-phenyl)-2-methoxy-acetamide hydrochloride according to general procedure D. Light ydlow soUd. MS 340.1 ([M+H]*) Example 280 (RS) -N- (4-carbaminiidoyl-benzyl)-2 - {2-ethynyl-6-fluoro-phenyl) -2-inethoxy-acetamide hydrochloride according was hydrogenated in analogy to example 16.2 to give (RS)-N-(4-carban]imidoyl-benzyl}-2-(2-ethyl-6-fluoro-phenyI)-2-methoxy-acetamide hydrochloride. Off-white solid. MS 344.2 ([M+H]"") Example 281 281.1 A suspension of (RS)-tri£luoro-methanesuIfonic acid 2-[{4-cyano-ben2yicarbamoyl)-methoxy-methyl]-3-fluoro-phenyl ester (520 mg, example 279.1) in DMF (10 ml) was heated to 100°C and treated with TEA (0.49 ml), tetrahydro-2-(2-propyn>doxy)-2H-pyTane (0.33 ml) and Cu(I)I (18 mg). The reaction mixture was degassed by passing a stream of Argon through the reaction mixture. Then bis(triphenylphosphine)paUadium(II)chloride (32 mg) was added. The reaction was heated for 6 hrs at IOO°C. After cooling to r.t., the mixture was concentrated. The residue was taken up in EtOAc and H20. After filtration through a glass microfibre filter, phases were separated. The organic layer was washed with brine, dried over MgS04, filtered and concentrated. The crude product was purified by flash chromatography (cyclohexane => cyclohexane/EtOAc 3:2) to give (RS)-N-(4-c)^no-benzyl)-2-j2-fluoro-6-[3-(tetrahydro-pyran-2-)doxy)-prop-l-ynyi]-phenyi}-2-methoxy-acetamide as off-white solid. MS 454.3 ([M-i-NH4]^) 28U (RS)-N~(4-Cyano-b«i2yl}-2-{2-fluoro-6-[3-(tetrahydro-pyran-2-yJoxy)-prop-l-ynyl]-phenyI}-2-methoxy-acetaniide was converted to (RS)-N-(4-carbamiimdoyl-benz)d)-2-[2-fluoro-6-(3-hydroxy-prop-l-ynyl)-phenyl]-2-methoxy-acetamide hydrochloride according to procedure D. Light yellow soUd. MS 370.2 ([M+H]"*) Example 282 (RS)-N-(4-carbamimidoyl-benzyl)-2-[2-fluoro-6-(3-hydroxy-prop-l-ynyl)-phenyi]-2-methoxy-acetamide hydrochloride was hydrogenated in analogy to example 16.2 to give (RS)-N-(4-carbamimido5d-benz:)d)-2-[2-fluoro-6-(3-hydroxy-propyl)-phenyl]-2-methoxy-acetamide hydrochloride. White solid. MS 374.2 ([M-t-H]"^) Example 283 283.1 Using a similar procedure as described in example 57.1 (RS)-trifluoro-methanesulfonic acid 2- [(4-cyano-benz)dcarbamoyl)-methoxy-methyl] -3-fluoro-phenyl ester (example 279.1) was reacted with phenyl boronic add to give {RS)-N-{4-cyano-benzyl)-2-(3-fluoro-biphenyl-2-yI)-2-methox)'-acetainide. Solid. MS 375.3 ([M+H]"^) 283.2 {RS}-N-(4-Cyano-benzyl)-2-(3-fliioro-biphenyl-2-yl)-2-methoxy-acetaimde was converted to (RS)-N-(4-carbaminiidoyl-benzyl)-2-(3-fluoro-biphenyl-2-yl)-2-methoxy-acetaimde hydrochloride according to general procedure D. OfF-white solid. MS 392.3 ([M+H]"^) Using a similar procedure as described in example 283 (RS)-trifiuoro-methanesuifomc add 2-[(4-cyano-benzylcarbamoyI)-methoxy-methyl]-3-fluoro-phenyl este (example 279.1) was converted to Example 284: (RS)-2-(3'-Aniino-3-fluoro-biphenyi-2-yl)-N-(4-carbamimidoyl-benzyl)-2-methoxy-acetamide hydrochloride. White soHd, MS 407.4 {[M+H]*) Example 285: (RS)-N-(4-Carbaminiido)d-benzyi)-2-(3-fluoro-3'-nitro-biphenyl-2-yl)-2-methoxj'-acetamide hydrochloride. Off-white solid. MS 437.2 {[M+H]"^) Example 286: (RS)-2-[2-(6-Amino-pyridin-2-yl)-6-fluoro-phen)d]-N-(4-carbamimidoyl-ben2yl)-2-methoxy-acetaniide acetate. Off-white solid. MS 408.3 ([M+H]"^) Example 287 287.1 In analogy to example 16.4 {RS)-N-(4-cyano-ben2yl)-2-(2-fiuoro-6-hydroxy-phen5d)-2-methoxy-acetamide (example 80.4) was reacted with ethyl bromoacetate to give (RS)-{2-[(4-cyano-benz)icarbamo}^)-methoxy-methyl]-3-fluoro-phenoxy}-acetic acid methyl ester. YeUowoil. MS 3872 ([M+HD 287.2 (RS)-{2-[(4-Cyano-benzylcarbamoyl)-methoxy-methyl]-3-Suoro-phenoxy}-acetic acid meth)4 ester was converted to (RS)-{2-[(4-carbamin3idoyl-ben27icarbamoyl)-methoxy-methyi]-3-fluoro-phenoxy]-acetic add methyl ester acetate according to general procedure D. White soUd. MS 404.3 ([M+H]*) Example 288 In analogy to example 20.1 (RS)-{2-[{4-carbainimidoji-benz)4carbamoyl}-methoxy-methyI]-3-fIuoro-phenoxy}-acetic acid methyl ester acetate was converted to (RS)-N-(4-Carbamimidoyl-benzyl) -2- (2-fluoro-6-phenoxy-phenyl)-2-methoxy-acetainide hydrochloride. White soHd. MS 390.2 ([M+H]"") Example 289 Using a similar procedure as describe in example 287 (RS)-N-(4-q'ano-benzyi)-2-(2-fluoro-6-hydroxy-phenyl)-2-methoxy-acetamide (example 80.4) was converted to (RS)-N-{4-carbamimidoyl-benzyl)-2-[2-(3-dimethylamino-propoxy)-6-fluoro-phenyi]-2-methoxy-acetamide hydrochloride. White solid. MS 417.2 ([M+H]^) Example 290 Using a similar procedure as describe in example 278.4 and example 278.5 (RS)-N-(4-cyano-ben2yl)-2-(2-fluoro-6-hydroxy-plienyl)-2-methoxy-acetamide (example 80.4} was converted to (4-carbamimidoyl-beiiZ)d}-2-(2-fluoro-6-plienoxy-phen)d)-2-methoxy-acetamide hydrochloiide. White solid. MS 408.2 {{M+H]"^) Example 291 291.1 (RS)-(2,6-Difluoro-4-methoxy-phenyi)-ethoxy-acetic add (example 101.3) was coupled with 4-amino benzonitrile according to general procsduie B to give (RS)-N-(4-cyano-benzyi)-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide. Colorless oil. 291.2 (RS)-N-(4-Cyano-benz)^)-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide was converted to (RS)-N-(4-carbamimidoyl-beiiz;}d)-2-(2,6-difiuoro-4-methoxy-phen)d)-2-ethoxy-acetamide hydrochloride according to general procedure D. White solid. MS 378.3 ([M+H]^) Example 292 292.1 Using analogous procedures as described in 101.1, 101.2 and 101.3 l-benzyloxy-3,5- difluoro-benzene {CAS 176175-97-6) was converted to (RS)-(4-benzyloxy-2,6-difluoro- phenyl)-ethoxy-acetic acid. Light yellow oil. MS 321.1 ([M-H]") 292.2 (RS)-(4-benz3doxy-2,6-difluoro-phen)^)-ethoxy-acetic acid was converted to (RS)-2-(4-benzyloxy-2,6-difluoro-phenyl)-N-(4-cyano-benzyl)-2-ethoxy-acetainide according to general procedure B. Colorless oil. MS 437.2 ([M+H]^) 292.3 (RS)-2-(4-Beiiz}doxy-2,6-difluoro-phen}4)-N-(4-cyano-benzyl)-2-ethoxy-acetaniide was converted to {RS)-2-(4-beii2ylox)'-2,6-difluoro--phenyl)-N-(4-carbaminiidoyi-benzyl}-2-ethoxy-acetamide hydrochloride according to general procedure D. Colorless solid. MS 454.3 {IM+H]+) Example 293 293.1 In analogy to example 16.2 (RS)-(4-benzyloxy-2,6-difluorO'pheiiyi)-ethoxy~acetic acid (example 292.1) was debenzylated to give {RS)-(2,6-difiuoro-4-hydroxy-phenyl)-ethoxy-acetic add. Light yellow solid. MS 255.1 ([M+Na]"") 293.2 According to general procedure B {RS)-(2,6-difluoro-4-hydroxy-phenyl)-ethoxy-acetic acid was reacted with 4-amino benzonitrile to give (RS}-N'-(4-cyano-benzj^)-2-(2,6-difluoro-4-hydroxy-phen}d)-2-ethoxy-acetamide. Colorless solid. MS 345.0 ([M-H]') 293.3 In analogy to example 16.4 (RS)-N-{4-cyano-beiizyl)-2-(2,6-difluoro-4-hydroxy-phenyl)-2-ethoxy-acetamide was reacted with isopropyl iodide to give (RS}-N-(4-cyano-benzyI}-2-(2,6-difluoro-4-isopropoxy-phenyl)-2-ethoxy-acetamide. Colorless oil. MS 387.1 ([M-H]") 293.4 (RS)-N-(4-Cyano-benzyi)-2-(2,6-difluoro-4-isopropoxy-phen)i)-2-ethoxy-acetamide was converted to (RS)-N-(4-carbamimidoy]-benzyl)-2-(2,6-difluoro-4-isopropoxy-phenyi)-2-ethoxy-acetamide hydrochloride according to general procedure D. Colorless foam. MS 406.2 ([M+H]^) Example 294 294.1 In analogy to example 22.1 (RS)-N-(4-cyano-benzyi)-2-(2,6-difluoro-4-hydroxy-phenyl)- 2-ethoxy-acetamide (example 293.2) was reacted with 2-(hydroKymethyl)-pyridine to give (RS)-(4-cyano-benzyl)-2-[2,6-difluoro-4-(pyridin-2-yimethoxy)-phenyl]-2-ethoxy-acetamide. Colorless oil. 294.2 According to general procedure D (RS)-(4-cyano-benzyl)-2-[2,6-difluoro-4-(pyridin-2-)dniethoxy)-phenyl]-2-ethoxy-acetamide was converted to (RS)-N-(4-carbainimidoyl-benzyl)-2-[2,6-difiuoro-4-(pyridin-2-ylmethoxy)-phenyl]-2-ethoxy-acetamide hydrochloride. Colorless solid. MS 455.2 ([M+H]"^) Example 295 In analogy to example 15.5 {RS)-(4-q^o-benzyl)-2-[2,6-difluoro-4-(pyridin-2-yiniethoxy)-phenyI]-2-etlioxy-acetainide {example 294.1) was converted to (RS)-2-[2,6-difluoro-4-(pyridin-2-ylinethoxy)-plienyl]-2-ethoxy-N-[4-(N-faydroxycarbaHiimidoyl)-benzylj-acetamide. Colorless foam.MS471.2 ([M+H]"^) Example 296 In analogy to example 15.4 (RS)-{4-cyano-ben2;)d)-2-[2,6-difluoro-4-(pyridin-2-ylmethoxy)-phenyl]-2-ethoxy-acetamide (example 294.1} was reacted ethyl chlorofonnate to give (RS)-{ammo-[4-({2-[2,6-difluoro-4-(pyridm-2-ylmethoxy)-phenyl]-2-ethoxy-acetylaniino}-methyl)-phenyi]-methylene}-cafbaroic add ethyl ester. Colorless foam. MS 527.2 ([M+H]^) Using analogous procedures as described in example 294.1 and 294.2 (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-4-hydroxy-phen)i)-2-ethoxy-acetamide (example 293.2) was converted to Example 297: (RS)-N-(4-carbamimidoyl-benzyl)-2-[2,6-difluoro-4-(pyridin-3- )dmethoxy)-phenyl]-2-ethoxy-acetamide hydrochloride. Colorless foam. MS 455.2 {[M+H]^) Example 298: (RS)-N-(4-carbamimido)d-benzyl)-2-[2,6-difluoro-4-(pyridin-4- ylmetboxy)-phenyl]-2-ethoxy-acetamide hydrochloride. Light yeDow foam. MS 455.2 ([M+H]") Example 299 299.1 In analogy to example 278.4 (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-4-hydroxy-phenyI)-2-ethoxy-acetamide {example 293.2) was reacted with phenyl boronic acid to give (RS)-N-(4-cyano-ben2yl)-2-C2,6-difluoro-4-phenoxy-phen)d)-2-ethoxy-acetamide. Light yellow soUd. MS 423.1 ([M+H]^* 299.2 (RS)-N-(4-Cyano-ben2yl)-2-(2,6-difluoro-4-phenoxy-phenyl)-2-ethoxy-acetamide was converted to (RS}-N-(4-carbamimidoyl-benz)d)-2-(2,6-difluoro-4-phenoxy-phen)d)-2-ethoxy-acetamide hydrochloride according to general procedure D. White solid. MS 440.2 {[M+H]") Example 300 Using analogous procedures as described in example 22 (RS)-N-(4-cyano-ben2yl)-2-(2,6-difluoro-4-h7droxy-phenyl)-2-ethox)'-acetainide (example 293.2) was converted to RS)-N- (4-carbainiinidoyl-ben27l)-2-[2,6-difluoro-4-(pyridin-3-yloxy-)-phenyl]-2-etlioxy-acetamide hydrochloride. Colorless foam. MS 441.2 ([M+H]"*") Using analogous procedures as described in example 293.3 and 293.4 {RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-3-hydroxy-phenyl)-2-ethoxy-acetamide (example 213) was converted to Example 301: (RS)-N-(4-Carbamimidoyl-benzyI)-2-(2,6-difluoro-3-isopropoxy-phenyl)-2-ethoxy-acetaniide hydrochloride. Colorless foam. MS 406.3 ([M+H]"*") Example 302: (RS)-N-(4-Carbamimidoyl-benzyl)-2-(3-carbamoylmethoxy-2,6-difluoro-phenyl)-2-ethoxy-acetamide hydrochloride. Colorless foam. MS 421.1 ([M+H]"*") Using analogous procedures as described in example 294 (RS)-N-(4-cyano-ben2yl)-2-(2,6-diSuoro-3-hydroxy-phenyl)-2-ethoxy-acetamide (example 213) was converted to Example 303; (RS)-2-[3-(2-Benzyioxy-ethoxy)-2,6-difluoro-phen^]-N-{4-carbamimidoyl-benzyl)-2-ethoxy-acetamide hydrochloride. Colorless foam. MS 498.3 ([M+H]^) Example 304 was isolated as a side product in the preparation of example 26. (RS)-N-(4-carbamiinidoyl-benzyl)-2-[2,6-difluoro-3-(2-hydroxy-ethoxy)-phenyl]-2-ethoxy-acetamide hydrochloride. Colorless foam. MS 408.3 ([M+H]"^) Example 305 Using analogous procedm-es to example 299 (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-3-hydroxy-phenyl)-2-ethoxy-acetamide (example 213) was converted to (RS)-N-(4-carbamimidojd-benzyl)-2-(2,6-difluoro-3-phenoxy-phenyI)-2-ethoxy-acetamide acetate. SoUd. MS 408.3 ([M+H]') Example 306 Using analogous procedures to example 283 (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-3-hydroxy-phenjd)-2-ethoxy-acetamide (example 213) was converted to (RS)-N-(4-carbamimidoyI-benzyI)-2-(2,4-difluoro-biphenyl-3-yI)-2-ethoxy-acetamide hydrochloride. Colorless soUd. MS 424.2 ([M+H]*) Example 307 307.1 A stirred solution of 2,4-difiuorbenzoic add (20.8 g) and N-ethyldiisopropylamine (26.8 ml) in dioxane (80 ml) was treated with diphenyi phosphory- azide (37.9 ml; very exothermicl) and tert-butanoJ (80 ml) at r.t. and under an argon atmosphere. The mixture was then heated to 90°C and stirring was continued for 16 h. The mixture (brown solution) was cooled to r.t., diluted with EtOAc, washed with water and brine, dried over MgSO^ and treated at the same time with decolorizing charcoal, and finally filtered over a celite pad. The yellow filtrate was concentrated to leave the crude product as an orange oil. The crude product was purified by flash chromatography (cydohexane/EtOAc 85:15). The product-containing fi-actions were combined and concentrated. The residue (yellow oil containing white soUd) was taken up in 50 ml heptane. The solid (symmetric urea which was formed as by-product during the Curtius reaction) was filtered off. The filtrate was concentrated. The residue was destilled in a Kugehohr oven (0.73 mbar, 120'C) to give (2,4-difluoro-phenyl)-carbainic acid tert-butyl ester {24.9 g) as Hght yellow oil. 307.2 To a stirred, cooled (-78°C) solution of (2,4-difluoro-phenyl)-carbamic add tert-butji ester (5 g) in THF (50 ml) under an argon atmosphere was added dropvidse a 1.6 M solution of BuLi in hexanes (28.6 ml) for 20 min (temperature below -68°C during the addition). When addition was complete, the mixture (turning to orange, then to light red) was stirred at -78°C for 1 h 30. DMF (7.55 ml) was then added for 10 min (temperature below -70°C) and stirring at -78°C was continued for 15 min. As the mixture had turned to a compact mas (no more stirring), it was allowed to warm to room temperature. Water (50 ml) was added and the pH was set to 3 by the dropwise addition of 3 N HCl. EtOAc (50 ml) was added. The organic phase was washed with water and brine dried over MgS04, filtered and concentrated. The crude product was purified by flash chromatography (cyclohesane => cydohexane/EtOAc 85:15) to give (2,4-difluoro-3-formyl-phenyl)-carbamic add tert-butyl ester (1.75 g) as an off-white solid. 307.3 According to general procedure A (2,4-difluoro-3-formyi-phen)d)-carbamic add tert-butyl ester was converted to (RS)-(3-tert-butoxycarbonylamino-2,6-difluoro-phenyl)-methoxy-acetic acid. Orange gum. MS 316.1 ([M-H]-) 307.4 According to general procedure C (RS)-(3-tert-butoxycarbonylamino-2,6-difluoro-phenyl)-methoxy-acetic add was reacted with 4-amino benzonitrile to give (RS)-{3-[(4- cyano-benzylcarbamo)'l)-inethoxy-methyl]-2,4-difIuoro-phenyl}-carbainic acid tert-but)d ester. Solid. MS 430.3 {[M-H]0 307.5 To a stirred solution of (RS)-l3-[(4-cyano-benzyicarbamoyl)-inethosy-methyl]-2,4-difluoro-phenyll-carbamic add tert-butyi ester (514 mg) at r.L in dioxane {10 ml) under an argon atmosphere was added 4 M HCI solution in dioxane {6 ml). Stirring at r.t. was then continued for 3 h. The light yellow solution was concentrated. The solid residue was suspended in EtOAc and washed with 1 N NaOH. The organic layer was dried over MgS04, filtered and concentrated. The crude product was purified by flash chromatography (cyclohexane -> cyclohexane/EtOAc 2:3) to give (RS)-2-(3-amino-2,6-difluoro-phenyl)-N-(4-cyano-benzyl)-2-methoxy-acetamide (215 mg) as an off-white sohd MS 332.3 ([M+H]^) 307.6 To a stirred solution of (RS)-2-(3-amino-2,6-difiuoro-phen}d)-N-{4-cyano-benzyl)-2- methoxy-acetamide (130 mg) at r.t. in dichloromethane were added sucessively dry 4A molecular sieves (50 mg), phenyl boronic acid (96 mg), triethylamine (0.11 ml), copper (U) acetate (71 mg) and TEMPO (67 mg). A "CaCl2 trap" was placed over the flask and stirring at r.t. was continued over the week-end. Then the soUds were filtered off and washed with EtOAc. The dark brown filtrate was concentrated to leave a dark brown residue. The crude product was purified by flash chromatography (cyclohexane => cyclohexane/EtOAc 3:2) to give (RS)-N-(4-cyano-benzyI)-2-(2,6-difluoro-3-phenylainino-phenyl)-2-methoxy- acetamide (123 mg) as Ught grey gum. MS 408.3 ([M+H]"^) 307.7 In analogy to example 15.5 (RS)-N-(4-cyano-benzyi)-2-(2,6-difluoro-3-phen^^amino-phenyI)-2-methoxy-acetaraide was converted to (RS)-2-(2,6-difluoro-3-phenylamino-phen)d)-N-[4-(N-hydroxycarbamimidoyl)-benz)d]-2-methoxy-acetamide. Off-white soHd. MS 441.6 ([M+H]"") 307.8 To a stirred solution of (RS)-2-(2,6-dfluoro-3-phenylarmno-phenyl)-N-[4-(N-hydroxycarbaminudoyl)-benzyl]-2-methoxy-acetamide (106 mg) at r.t. in ethanol (5 ml) under an argon atmosphere were added 5 drops of acetic acid and and a catalytic amount of Raney-Nickel. The mixture was then stirred at r.t. under a hydrogen atmosphere for 23 h. The catalyst was filtered off and the filtrate was concentrated. The crude product was purified using flash chromatography (EtOAc/acetone/HjO/HOAc 6:2:1:1) to give (RS)-N- (4--carbamimidoyl-benzyl) -2- (2,6-difIuoro-3-phenyl2inino-pheny]) -2-methoxy-acetarnide acetate (92 mg) as on off-white solid. MS 425.5 ([M+H]"") Example 308 30S.1 To a stirred solution of (RS}-2-(3-amino-2,6-difluoro-phenyl)-N-(4-cyano-benzyl)-2-methoxy-acetamide (example 307.5) 81 mg) at r.t in THF (5 ml) under an argon atmosphere were added N-eth)ddiisopropylamine (0.017 ml) and 2-iodopropane (0.01ml). The mixture was heated to reflux and stirring was continued for 17 h. More 2-iodopropane (0.1 ml) and N-ethyldiisopropylamine (0.17 ml) were added and stirring at reflux was continued for 7 h. DMF (5 ml) was added and the mixture was stirred at HO^C for 21 h. The mixture had turned to light brown. More DMF (5 ml), N-ethyldiisopropjdamine (0.35 ml,) and 2-iodQpropane (0.2 ml) were added and stirring at 90°C was continued for 17 h. The mixture was cooled to r.t., diluted with 20 ml water and extracted widi EtOAc. The combined organics were washed with water and brine , dried (MgS04), filtered and concentrated. The crude product was purified by column chromatography (cyclohexane => cyclohexane/EtOAc 1:1) to give H-(4-cyano-benzyl)-2- (2,6-difluoro-3-isopropyianiJno-phenyi)-2-methoxy-acetamide (28 mg) as light brown gum. 30S.2 In analogy to example 307.7 and 307.8 H-(4-cj^no-benzyi)-2-(2,6-difluoro-3- isopropyiainino-phenyl)-2-methoxy-acetamide was converted to (RS)-N-(4- carbamimido)d-ben2yl)-2-(2,6-difluoro-3-isopropylamino-phen)d)-2-methoxy-acetamide acetate. Light green crystals. MS 391.3 ([M+H]"^) Example 309 309.1 In analogy to example 87.2 (RS)-2-(3-amino-2,6-difluoro-phenyl)-N-(4-cyano-benzyi)-2- methoxy-acetamide (example 30.5) was reacted with acetyl chloride to give (RS)-2-(3- acet7lam!no-2,6-difiuoro-phenyl)-N-(4-cyano-ben2yl)-2-methoxy-acetamideas white foam. 309.2 Using general procedure D (RS)-2-(3-acetylamino-2,6-difluoro-phenyl)-N-(4-cyano-benzyl)-2-methoxy-acetamidewas converted to (RS)-2-(3-acetylamino-2,6-difluoro-phenyl)-N-(4-carbamimidoyI-ben2yl)-2-methoxy-acetamide hydrochloride. OS-white solid. MS 391.3 ([M+H]^) Example 310 In analogy to example 309 (RS)-2-(3-ammo-2,6-di£!ucro-piienyl)-N-(4-c)'ano-faenzyl)-2-methoxy-acetamide (example 30.5) was converted to (RS)-(4-carbamimidoyl-benzyl)-2-{2,6-difluoro-3-plien)dacetylamino-phenyi)-2-methoxy-acetaimde hydrochloride. Off-i white sohd. MS 467.4 {[M+H] ^) Example 311 311.1 A stirred solution of 2,4-difluorobenzaldehyde (15.4 ml) in toluene (200 ml) was treated with eth}iene ^ycol (23.2 ml) and p-toluene sulfonic add (0.53 g). The ruction mixture was heated to reflux during 5 hrs (Dean-Stark trap), then it was cooled to r.t and poured onto ice. The organic layer was separated off, washed with 10% KHCOs-solution and brine, dried over MgS04, filtered and concentrated to give 2-(2,4-difluoro-phenyl)-[l,3]dioxolane (26.8 g) as a light yellow oU. MS 186.1 ([M]"") 311.2 In analogy to procedures 101.1, 101.2 and 101.3 2-(2,4-difluoro-phenyl)-[l,3]dioxolane was converted to (RS)-(3-[l,3]dioxolan-2-yi-2,6-difluoro-phen)d)-ethoxy-acetic add. During the addic work-up after the final ester hydrolysis, the acetal protecting group was pardy lost It was completdy deaved off by treating the mixture of protected and unprotected compoimd with 3N aqueous HCI/THF/H2O 1:10:1 overnight at r.t.. Upon complete deprotection, the THE was distilled off and the product was isolated by extraction with EtOAc No further purification. (RS)-(2,6-Difluoro-3-form)d-phenyl)-ethoxy-acetic add. Ydlow oil. MS 262.0 ([M+NH*]') 311.3 According to general procedure B (RS)-(2,6-difluoro-3-formyl-phenyl)-ethoxy-acetic add was reacted with 4-aminomethyl benzonitrile to give (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-3-formyl-phenyl)-2-ethoxy-acetamide. Amorphous ofif-white solid. MS 359.2 ([M+H]-^) 311.4 A suspension of (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-3-formyI-phenyl)-2-ethoxy-acetamide (300 mg) in EtOH (1 ml) was treated with NaBH4 (66 mg) at 0°. The reaction mixture was stirred for 4 hrs at r.L, then poured onto ice and extracted with EtOAc. The organic layers were combined, dried over MgS04, filtrated and concentrated. The cmde product was isolated by flash chromatography (CH2CHI2 => CH2Cl2/MeOH 4:1) to give {RS)-N-{4-c7^o-berizyl)-2-(2,6-difluoro-3-hydroxymethyl-phenyl)-2-ethoxy--acetamide (174 mg) as amourphous white solid. MS 361.3 ([M+H]"^) 311.5 (RS)-N-{4-Cyano-benz)'l)-2-{2,6-difiuoro-3-hydroxyinethyl-phenyl)-2-ethoxy-acetainide was converted according to general procedure D to give (RS)-N-(4-carbamiinidoyl-benzyI)-2-(2,6-difluoro-3-hydroxymethyi-phenyl)-2-ethoxy-acetamide hydrochloride as amorphous white soiid. MS 378.3 ([M+H]^) Example 312 312.1 In analogy to example 106.2 (RS)-N-(4-cyano-benz)d)-2-(2,6-difluoro-3-form>i-phenyl)-2-ethoxy-acetamide (example 311.3) was converted to (RS)-N-(4-cyano-benzyl)-2-[2,6-difluoro-3-(hydroxyiinino-methjd)-phen)d] -2-ethoxy-acetamide. Off-white amorphous soUd. MS 374.3 ([M+H]*) 312.2 In analogy to example 106.3 (RS)-N-(4-cyano-benz)d)-2-[2,6-difiuoro-3-(hydroxyimino- meth5d)-pben)d]-2-ethoxy-acetainide was converted to (RS)-2-(3-aminomethyl-2,6- difluoro-phenyl)-N-(4-cyano-benzyI)-2-ethoxy-acetamide acetic acid. Yellow oil. MS 360.3 ([M+H]") 312.3 In analogy to example 87.2 (RS)-2-(3-aminomethyl-2,6-difiuoro-phen)i)-N-(4-cyano- benzyl)-2-ethoKy-acetamide acetic acid was reacted with acetyl chloride to give (RS)-2-[3- (acet)^amino-methyl)-2,6-difluoro-phenyI]-N-(4-cyano-benzyi)-2-ethoK7-acetamide. White foam. MS 402.5 ([M+H]"") 312.4 According to general procedure D (RS)-2-[3-{acetylamino-methyI)-2,6-difluoro-phenyl]- N-(4-cyano-benzyl)-2-ethoxy-acetamide was converted to (RS)-2-[3-(acet)^amino- methyl)-2,6-difluoro-phenyl]-N-(4-carbamimidoyl-benzyi)-2-ethoxy-acetamide hydrochloride. White soHd. MS 419.2 ([M+H]"*") Example 313 313.1 In analogy to example 15.5 (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-3-formyI-phenyI)-2-ethoxy-acetamide (example 311.3) was converted to (RS)-2-[2,6-difluoro-3- (hydroxyiinino-meth)d)-phenyl]-2-ethoxy-N-[4-(N-hydroxycarbaimmidoyl)-beiizyl]-acetamide. Amorphous off-white solid. MS 407.2 ([M+H]"^' 313.2 In analogy to example 307.8 (RS)-2-[2,6-difluoro-3-(hydroxyiinino-methyI)-phenyl]-2- ethoxy-N-[4-CN-hydroxycarfaamimidoyI)-ben2yl]-acetamide was hydrogenated to give (RS)-2-{3-aminometh'^-2,6-difluoTO-phenyl)-N-(4-caTbanuinidoyl-benzyi)-2-eiiioxy- acetamide acetic acid 1:4. White soUd. MS 377.3 ([M+H]"^) E3tample 314 314.1 To a solution of (RS)-N-(4-cyano-ben2yi)-2-(2,6-difluoro-3-formyl-phenyl)-2-ethoxy-acetamide (250 mg, example 311.3) in EtOH (5 ml) was added aniline (64 mg). The suspension was stirred over night, then cooled to 0°C and treated with NaBH4 (38 mg). The reaction mixture was stirred 1 fa at 0° and 1 h at r.L, then poured onto ice and extracted with EtOAc. The organic layer was dried over MgS04, filtrated and concentrated. The crude product was purified by flash chromatography (cyclohexane/EtOAc 1:4 => BtOAc) togive(RS)-N-(4-cyano-benz)d)-2-(2,6-difiuoro-3-phenyIaminomethyl-phenyl)-2-ethoxy-acetamide (230 mg) as off-white amourphous solid. MS 436.3 ([M+H]^) 314.2 According to general procedure D (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-3-' phenyiaminomethyi-phen)d)-2-ethoxy-acetaraide was converted to (RS)-(4-carbamiraidoyl-benzyl)-2-(2,6-difluoro-3-phen)daminomethyi-phen)i)-2-ethoxy-acetamide hydrochloride. Amorphous white sohd. MS 453.5 ([M+H]"*") Using analogous procedures as described in example 37 (RS)-N-(4-cyano-benzyi)-2-(2,6-difluoro-3-formyl-phen)i)-2-ethoxj'-acetamide (example 311.3) was converted to Example 315; (RS)-(4-Carbamimidoyi-benzyl)-2-(2,6-difluoro-3-morpholin-4-ylmeth)^-phenyl)-2-ethoxy-acetamide hydrochloride. White solid. MS 447.2 ([M+H] '^) Example 316: (RS)-(4-Carbamimidoyi-benz)d)-2-(2,6-difluoro-3-piperidin-l-ylmethyl-phenyi)-2-ethoxy-acetaniide hydrochloride. Amorphous off-white sohd. MS 445.2 ([M+H]^) Example 317 In analogy to example 307.8 (RS)-2-(3-diethoxymethyi-2,6-difluoro-phenyl)-2-ethoxy-N-[4-(N-hydroxycarbamimidoyl)-beii2yl]-acetamide (obtained side product in the synthesis of example 312.1) was converted to (RS)-(4-carbamimidoyl-benzyl)-2-(2,6-difIuoro-3-formyI-phenyl)-2-ethoxy-acetamide acetic add (1:4). White solid. MS 376.3 ([M+H]"^) Example 318 318.1 In analogy to procedures 106.2 and 106.3 3,5-difluoro-4-formyl-benzonitrile (CAS 467442-15-5) was converted to 4-aniinomethyi-3,5-difluoro-benzomtrile hydrochloride. Off-white soUd. MS 169.2 ([M+H]"") 318.2 According to general procedure C 4-aminomethyl-3,5-difluoro-benzonitrile hydrochloride was reacted with {RS)-(2,6-difluoro-4-methoxy-phenyI)-ethoxy-acetic acid (example 101.3) give to (RS)-N-(4-cyano-2,6-difIuoro-benzyl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetaniide. Off-white soUd. MS 397.1 ([M-i-H]^) 318.3 According to general procedure D (RS)-N-(4-cyano-2,6-difluoro-benzyl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide was converted to (RS)-N-(4-carbamiimdoyl-2,6-difiuoro-benzyl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide hydrochloride. White solid. MS 414.2 ([M+H]^) Using similar procedures &s described in example 318 4-aminomethyl-3,5-difluoro-benzonitrile hydrochloride (example 318.1) was coupled with the appropriate adds and converted to the following arnidine products: Example 319: (RS)-N-(4-Carbamimidoyl-2,6-difluoro-benzyi)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyi)-acetamide acetate (coupling with add (RS)-ethoxy-(2-fluoro-4-methoxy-phenyO-acetic add, example 63.1). Off-white powder. MS 396.1 ([M+H] ) Example 320; (RS)-N-(4-Carbaniimido5d-2,6-difiuoro-ben2yI)-2-(2,6-di£luoro-4- methoxy-phenyI)-2-methoxy-acetamid acetate (coupling with add (RS)-(2,6-difluoro-4-methoxy-phenyl)-methoxy-acetic add, example 66.1). Off-white soUd. MS 400.5 ([M+HD Example 321: (RS)-N-(4-Carbamimidoyl-2,6-difluoro-benz)d)-2-(2-fluoro-4-methoxy-phenyl)-2-methoxy-acetamide acetate (coupling with acid (RS)-(2-fluoro-4-methoxy-phenyD-methoxy-acetic acid, example 15.1). Off-white solid. MS 382.3 ([M-l-H]"^) nxampie m 322.1 To a mechanically stirred solution of 4-bromomethyl-3-nitro-benzomtrile (21.7 g, CAS 223 512-70-7) in chlorofonn (250 ml) under argon atmosphere was added hexamethylenetetramine (7.1 g). A white precipitate appeared a few minutes after the addition. After 3 hrs heating to reflux (oil bath SO^C) he mixture was cooled to r.L. The solid was collected by filtration, washed with chloroform and dried under high vacuum) to give l-(4-cyano-2-nitro-benzyl)-3,5,7-triaza-l-azoma-tricyclodecane hydrobromide (13.8 g). Off-white powder. MS 322.2 To a mechanically stirred suspension of l-(4-cyano-2-mtro-beiizyl)-3,5,7-triaza-l-azonia-tricyclodecane hydrobromide (13.8 g) in ethanol (150 ml) mider argon atmosphere, was added concentrated aqueous HCl (20 ml). After 6 hours stirring at reflux the mixture was concentrated, diluted with NaOH IN until pH>12. The product was extracted with EtOAc. The combined organic phases were washed twice with water and with brine. Then the solution was dried over MgS04), filtered and concentrated to give 4-aminometh)i-3-mtro-benzonitrile (5.8 g) as yellow soUd. MS 322.3 Accordk^ to general procedure B 4-aminomethyl-3-nitro-benzonitrile was reacted with (RS)-ethoxy-(2-fluoro-4-methoxy-phenyi}-acetic acid (example 63.1) to give (RS}-(4-cyano-2-nitro-benzyl)-2-ethoxy-2-(2-fIuoro-4-methoxy-phenyl)-acetamide. Yellow foam. MS 388.1 ([M-hH]^) 322.4 To a stirred solution of (RS)-(4-cyano-2-nitro-benzyl)-2-ethoxy-2-(2-fluoro-4-metfaoxy-phenyl)-acetamide in THF (5 ml) and ethanol (15 ml) was added palladium/C (250 mg). After 24 hrs stirring at r.L under hydrogen atmosphere the mixture was filtered, and the filtrate was concentrated to leave a light yellow foam. The crude product was purified by flash chromatography (cyclohexane => cyclohexane/EtOAc 1:1) to give (RS)-(2-amino-4-cyano-benzjd)~2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide (4.45 g) as light yellow foam. MS 358.7 ([M-hH]*) 322.5 To a stirred solution of (RS)-(2-ainino-4-cyano-benzyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide (470 mg) in DMF (8 ml) were added iodoacetamide (376 mg) and N-ethyldiisoprop>damine (0.34 ml). After 50 hrs stirring at 110°C under argon atmosphere. The mixture was diluted with EtOAc and water. The organic phase was separated and washed with water and brine, dried ovef MgS04, filtered and concentrated. The crude product was purified by flash chromatography CCH2a2 => CHjClj/MeOH 4:1) to give (RS)-[2-(carbamoylmeth]i-ainino)-4-cyano-benzyl]-2-ethoxy-2-(2-fluoro-4-rnethoxy-phenyl)-acetamide (133 mg) as an off-white soUd. MS 415.1{[M+H]'*') 322.6 According to general procedure D CRS)-[2-(carbamoylniethyl-ainino}-4-cyano-beii2yI]-2-ethoxy-2-(2-fluoro-4-methoxy-phenyI)-acetamide was converted to (RS)-[4-carbamimidoyi-2-{carbamoylmethyi-amino)-benzyl]-2-ethoxy-2-(2-fluoro-4-methoxy-phenyi)-acetamide hydrochloride. Off-white soHd. MS 432 ([M+HD Using similar procedures as described in example 322.4 and 322.6 (RS)-(2-amino-4-cyano- benzyl)-2-ethoxy-2-(2-fl.uoro-4-methoxy-phenyl)-acetamide (ecample 322.4) was converted to Example 323: (RS)-N-(2-Benzylamino-4-carbamimidoyl-benzyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phen}d)-acetamide acetate. Off-white soUd. MS 465 ([M+H]"^) Example 324: (RS)-[4-Carbaminiidoyl-2-(2-fluoro-benzylamino)-benz)d]-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide hydrochloride. Off-white soUd. MS 483.3 ([M+H]"^) Example 325; (RS)-{4-CarbamimidoyI-2-[(pyridin-2-yImethyl)-aniino]-ben2yi}-2-ethoxy-2-(2-fluoro-4-methoxy-phenyi)-acetamide hydrochloride. Off-white sohd. MS 466.4 ([M+H]-^) ■ Example 326: (RS)-[4-Carbamimidoyl-2-(4-chloro-2-fluoro-benz)danuno)-benzj4]-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide hydrochloride. Off-white solid. MS 517.3 ([M+H]') Example 327: (RS)-(4-Carbamunidoyl-2-phenethyianiino-benzj4}-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamidehydrochloride. Off-white foam. MS 479.5 {[M-i-H]"^) Example 328: (RS)-(5-Carbamimidoyl-2-{[2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acet)damino]-raeth)d}-phenylamino)-acetic add ethyl ester hydrochloride. Off-white solid. MS461.1([M+H]-') Example 329 In analogy to example 20.1 (RS)-(5-carbamimidoyl-2-{[2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acer}'lamino]-methylt-phenylainino)-acetic add ethyl ester hydrochloride (example 328) was hydrolysedto give (RS)-(5-carbamimidoyl-2-{[2-ethoKy-2-(2-fluoro-4- methoxy--phenyl)-acetyiamino]-methyl}-phenyiarnino)-acetic acid acetate. Off-white solid. MS 433.4 {[M+H]^} Example 330 330.1 ; In analogy to example 95.4 (RS)-C2-amino-4-cyano-ben2)d)-2-ethoxy-2-{2-£luoro-4- methoxy-phenyl)-acetamide {example 322.4) was reacted with benzyl sulfonylchloride to give (RS)-(4-cyano-2-phenylmethanesulfonylamino-ben2yl)-2-ethoxy-2-(2-fiuoro-4- methoxy-phenyl)-acetainide. Off-white foam. MS 512.3 ([M+H]"^) 330.2 According to general procedure D (RS)-{4-cyano-2-phenylmethanesulfon}damino-benzyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetaniide was converted to (RS)-{4-carbamimidoyl-2-phenylmetfaanesuIfonylamino-ben2yl)-2-ethoxy-2-{2-fluoro-4-methoxy-phenyl)-acetamide hydrochloride. Off-white soUd. MS 529.2 ([M+H]** Example 331 Using similar procedures as described in example 330 (RS)-(2-amino-4-cyano-benzyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetainide (example 322.4) was reacted with benzylisocyanate and subsequently converted into the corresponding amidine to give (RS)-[2-C3-benzyl-ureido)-4-carbamimidoyl-ben2yl]-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide acetate as a white solid. MS 508.4 ([M+H]"^) Example 332 Using similar procedures as described in example 53 (RS)-(2-amino-4-cyano-ben2yl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyi)-acetamide {example 322.4) was reacted with benzyl chloroformate and subsequently converted into the corresponding amidine to give (RS)-{5-carbamimidoyl-2-{[2-ethoxy-2-{2-fluoro-4-methoxy-phenyl)-acetj4amino]-methyll-phenyl)-carbamic acid benzyl ester hydrochloride. White solid. MS 509.4 ([M+H]^) Example 333 333.1 In analogy to example 30.6 {RS)-{2-amino-4-cyano-benzyl)-2-ethoxy-2-(2-fluoro-4- methoxy-phenyl)-acetaraide (example 322.4) was reacted with phenyl boronic acid to give (RS)-(4-cyano-2-phenylamino-benzyl)-2-ethoxy-2-(2-fluoro-4-inethoxy-phen^)- acetamide. Off-white foam. MS 434.1 ([M+H]"^* 333.2 According to general procedure D (RS)-(4-cyano-2-phenylamino-benzyi)-2-ethoxy-2-(2-fiuoro-4-methoxy-phenyl)-acetamide was converted to (RS)-(4-carbaniiinidoyl-2-phenylamino-benz}'l)-2-ethoxy-2-{2-fluoro-4-metlioxy-phenyl)-acetamide hydrochloride, i light green soUd. MS 451.1 ([M+H]"*") Example 334 334.1 A solution of (RS)-(2,6-difluoro-4-trifluoromethanesulfQnylory-phen^)-ethoxy-acetic add ethyl ester {3.5 g, example 162) in dioxane (115 ml) was treated with bis(pinacolato)diboron (3.43 g) and K2CO3 (2.65 g). The solution vfas deoxj^enated by passing a stream of argon through it Then bis(triphenylphosphine)paIladiuni(II) chloride (0.62 g) was added. The reaction mixuter was heated to 100° for 16 hrs, then cooled to r.t and filtrated. The solids were washed with diosane/EtOAc. The filtrate was concentrated. The crude product was isolated by flash chromatography (cyclohexane/EtOAc 1:1 => EtOAc) to give (RS)-[2,6-difluoro-4-(4,4,5,5-tetramethyl-[l,3,2]dioxaborolan-2-yl)-phenyI]-ethoxy-acetic acid ethyl ester (3.51 g) as yellow oil. MS 388.0 ([M+NH4]'^) 334.2 A solution of (RS)-[2,6-difluoro-4-(4,4,5,5-tetramethyl-[13,2]dioxaborolan-2-yl)-phenyl]-ethoxy-acetic acid ethyl ester in li2-dimetiioxyethane was treated with 2-amino-5-bromopyridine and CsF. The reaction mixture was deoxygenated by passing a stream of argon throi^ it Tetrakis(triphenylphosphine)palladium(0) was added. The reaction mixture was heated to 80° for 2 days, then cooled to r.t and concentrated. The crude product was isolated by flash chromatography (cyclohexane/EtOAc 2:1 => EtOAc) to give (RS)-[4-(6-amino-pyridin-3-yl)-2,6-difluoro-phenyl]-ethosy-acetic acid ethyl ester as amorphous brown solid. This material which was contaminated with triphenyl phosphinoxid was dissolved in THF and treated with 4.5 ml IN NaOH and stirred for 18 hrs at r.t.. The solution was neutralized with IN HCl, then concentrated. The residue was taken up in Et20. The solid was filtered off and washed with ether to give (RS)-[4-(6-amino-pyridin-3-)d)-2,6-difluoro-phenylj-ethoxy-acetic acid (1.36 g, contains 2 equivalent of NaCl). According to general method B this material (350 mg) which was contaminated with triphenyl phosphinoxid was reacted with 2-(2-aniinometh)4-5-cyano-phenoxy)-acetaraide hydrochloride (example 123.2) to give (RS}-2-[4-(6-amino-pyridin-3-yl)-2,6-difluoro-phen)d]-N-(2-carbamoylmethoxy-4-cyano-benzyl)-2-ethoxy-acetamide (186 mg) as off-vfinte soUd. MS 496.3 ([M+H]"") 334.3 According to general procedure D (RS)-2-[4-(6-amino-pyridin-3-yl)-2,6-difluoro-pfaenyl]-N-(2-carbamoylmethoxy-4-cyano-benzyl)-2-ethoxy-acetainide was converted to (RS)-2-[4-{ 6-ainmo-pyridin-3-yI)-2,6-difluoro-phenyl]-N-(4-carbamimidoyl-2-carbamoyl^lethosy-benzyl)-2-ethoxy-acetamide hydrochloride acetic add (1:1:2). Off-white soUd. MS 513.3 ([M+H]"^) Example 335 335.1 In analogy to example 22.1 (RS)-{2,6-difluoro-4-hydroxy-phenyl)-etboxy-acetic acid ethyl ester (example L6) was reacted with 2-(hydroxymethyl)pyridine to give (RS)-[2,6-difluoro-4-(pyTidin-2-ylmethoxy)-phenyl]-ethoxy-acetic acid ethyl ester as a yellow semisolid. This material was hydrolysed in analogy to example 101.3 to give (RS)-[2,6-difluoro-4-(pyridin-2-yhnethoxy)-phenyl]-ethoxy-acetic acid. White soUd. MS 324.1 ([M+H]*) 335.2 According to general procedure C (RS)-[2,6-difluoro-4-(pyridin-2-ylmethoxy)-phenyl]-ethoxy-acetic acid was reacted with 2-(2-aminomethyi-5-cyano-phenoxy)-acetamide hydrochloride (example 123.2) to give (RS)-(2-carbamo)imethoxy-4-cyano-benzyl)-2- [2,6-difluoro-4-(pyridin-2-}dmethoxy}-phenyl]-2-ethoxy-acetamide. Amorpbous off-white soUd. MS 511.3 ([M+H]^) 335.3 According to general procedure D (RS)-(2-carbamo)dmethoxy-4-cyano-benzyl)-2-[2,6- difluoro-4-(pyridin-2-ylmethoxy)-phen)d]-2-ethoxy-acetamide was converted to (RS)-(4- carbamiimdo)4-2-carbamoylmethoxy-ben2yl)-2-[2,6-diSuoro-4-(pyridin-2-3dmethoxy}- phenyl]-2-ethoxy-acetamide hydrochloride. Off-white solid. MS 528.2 ([M+H]"^) Example 336 336.1 According to general procedure C (RS)-[4-(6-amino-pyridin-3-yl)-2,6-difluoro-phenyl]-ethoxy-acetic add (intermediate from example 334.4, contains 2 eqmvalent of NaCl) was reacted with 4-aminomethyl-3,5-difiuoro-ben2omtrile hydrochloride (example 318.1) to give (E.S)-2-[4-(6-aniino-pyridin-3-)d)-2,6-difluoio-phenyl]-N-(4-cyano-2,6-difluoro-benzyl)-2-ethoxy-acetamide as off-white solid. MS 459.6 ([M+H]"^) 336.2 In analogy to example 307.7 and 307.8 (RS)-2-[4-(6-amino-pyridin-3-yl)-2,6-difluoro- phenyl]-N-(4-cyano-2,6-di£luoro-benzyl)-2-ethoxy-acetarmde was converted to (RS)-2-[4-(6-aiiiino-pyTidin-3-yi)-2,6-difluoro-phenyi]-N-{4-carbainiiiiidoyl-2,6-difluoro-ben2yI)-2-ethoxy-acetaniide acetate. White powder. MS 476.5 ([M+H]"^) Example 337 337.1 A suspension of (RS)-N-(4-carbamimido)^-benzyl)-2-(2,6-difluoro-4-inethoxy-phenyl}-2-methoxy-acetamide hydrochloride (600 mg, example 66.3) in CH2CI2 (15 ml), H2O (7.5 ml) and saturated NajCOs-solution (7.5 ml) was treated with B0C2O (333 mg) and stirred for 6 hrs at r.t. The mixture was poured onto ice and extracted with CH2CI2. The organic layers were dried over MgSOi, filtrated and concentrated. The crude product was purified by flash chromatography (cyclohexane/EtOAc 4:1 => EtOAc) to give (RS)-[(4-{[2-(2,6-difluoro-4-methoxy-phenyl)-2-methoxy-acetylamino]-metfayI}-phenyl)-imino-methyl]-carbamic acid tert-butyl ester (630 mg). Amorphous off-white soUd. 337.2 The racemic (I^)-[(4-l[2-(2,6-difiuorQ-4-meJiioxy-phenyl)-2-methoxy-acetylamino]-methyl}-phenyl)-iinino-methyi]-carbamic acid tert-butyl ester (620 mg) was separated by HPLC on ChiralPak AD (15% EtOH in heptane) to give (S)-[(4-{[2-(2,6-difluoro-4-methoxy-phenyI)-2-methoxy-acetylamino]-methyl}-phenyl)-inmio-methyl]-carbamic add tert-butyl ester (193 mg) as a white foam and (R)-[(4-{[2-(2,6-difluoro-4-methoxy-phenyl)-2-methoxy-acetyianiino]-meth)d}-phenyI)-imino-methyl]-carbamic acid tert-butyl ester (223 mg) as a white foam. 337.3 A suspension of (S)-[(4-{[2-(2,6-difluoro-4-methoxy-ph.enyl)-2-methoxy-acetylaimno]- methyi}-phenyl)-iniino-meth>i]-carbamic add tert-butyl ester in water was treated with formic add. The solution was stirred for 8 hrs at r.t, then concentrated, redissolved twice in water, concentrated and dried to give (S)-N-(4-carbaniiinidoyl-benzyl)-2-(2,6-di£luoro- 4-methoxy-phenyl)-2-methoxy-acetainide formiate (78 mg) as white foam. MS 364.1 ([M+H]^) 337.4 In analogy to example 341-3 (R)-[(4-{[2-(2,6-difluoro-4-methoxy-phenyl)-2-methoxy- acetylaniinol-methyl}-phenyl)-imino-methyll-carbainic add tert-butyl ester was converted to (R)-N-(4-carbamimidoyl-benzyl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-methoxy- acetamide formiate. White foam. MS 364.1 ([M+H]"^) 338.1 A solution of (RS)-ethoxy-(2-fiuoro-4-methoxy-phenyl)-acetic add {7.26 g, example 63.1), ethanol (16.7 ml) and DMAP (1.57 g) in dichlororaethane (120 ml) was cooled to 0* and treated with EDCI (6.59 g). The reaction stirred was stirred at r.t for 18 hrs, then washed with 0.5 N HQ, H2O, saturated NaHCOs and brine. The organic layer was dried over MgSO^, filtrated and concentrated. The crude product was purified by flash chromatography (cyclohexane => cyclohexane/EtOAc 85:15) to give (RS)-ethoxy-(2-fiuoro-4-methoxy-phen}i)-acetic add ethyl ester (4.42 g) as yellow oil. MS 256.2 ([M]"^) 338.2 An emulsion of (RS)-ethoxy-{2-fluoro-4-methoxy-phenyI)-acetic add ethyi ester (1.11 g) in O.IM NaQ, 3 mM Natriumphosphat buffer pH 7.0 (260 ml) was cooled to 4-5°C and treated with lipase from Rhizomucor miehei. The reaction mixture was stirred for 4 days at 4-5° while maintaining the pH at 7 by gradual addition of O.lN NaOH (totally 25.5 ml), then extracted with CH2CI2 and then EtOAc. The organic layers were dried over Na2S04, then concentrated to give (R)-ethoxy-(2-fluoro-4-methoxy-phenyl)-acetic acid ethyl ester (330 mg, 98.9% ee). An emulsion of (R)~ethoxy-(2-fluoro-4-methoxy-phenyi)-acetic add ethyl ester (416 mg) in O.lM NaCl, 3 mM Natriumphosphat buffer pH 7.0 (75 ml) was cooled to 4-5'=C was treated with hog hver esterase suspension (0.175 ml). The reaction mixture was stirred for 4 days while maintaining the pH at 7 by gradual addition of O.lN NaOH (totally 12.8 ml). The reaction mixture was washed with CH2CI2, then brought to pH 2 by the addition of 2N HCl and extracted with EtOAc. The EtOAc layer was dried over Na2S04, filtrated and concentrated to give (R)-ethoxy-(2-fluoro-4-methoxy-phenyI)-acetic add (304 mg, 97.1% ee) as yellow semisoUd. 338.3 According to general procedure B (R)-ethoxy-(2-fluoro-4-methoxy-phenyl)-acetic add was reacted with [aniino-(4-aminomethyl-phenyi)-mediylene]-carbamic add berizyl ester hydrochloride 1:2 (prepared according to Ch. Lila, Ph. Gloanec, L. Cadet, Y. Herve, J. Foumier, F. Leborgne, T. J. Verbeuren, G. De Nanteuil, Synthetic Commimications 1998, 28, 23, 4419-4429) to give [l-amino-l-(4-{[(R)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyi)-acetylamino]-me^yi}-phenyl)-meth-(E)-ylidene]-carbamic add benzyl ester (96.5% ee). Off-white solid. 338.4 A solution of [l-amino-l-(4-{[(R)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)- acelylamino]-methyl}-phen)d)-meth-(E)-ylidene]-carbamic acid benzyl ester (1.95 mg) in EtOH (20 ml) was treated with HOAc (0.05 ml) and Pd/C 10% (20 mg) and hydrogenated over night at normal pressure. The catalyst was filtered off, the filtrate was concentrated to give (R)-N-(4-carbamimidoyl-benzyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)- acetamide acetate (151 mg, 96.3% ee) as white sohd. Example 339 Using general procedure C (RS)-ethoxy-(2-fluoro-4-methoxy-phenyl)-acetic acid (example 63.1) was reacted with [amino-(4-aminocnethyl-phenyl)-methylene]-carbamic acid benzyl ester hydrochloride 1:2 (prepared according to Ch. Lila, Ph. Gloanec, L. Cadet, Y. Herv^, J. Fournier, F. Leborgne, T. J. Verbeuren, G. De Nanteuil, Synthetic Communications 1998, 28, 23, 4419-4429) to give (RS)-[amino-(4-{[2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetylamino]-methyl}-phenyl)-methylenel-carbamic acid benzyl ester. White solid. MS 494.3 ([M+H]^) Referential Example 340 (RS)-[(4-{[2-(2,6-Difiuoro-4-methoxy-phenyl)-2-methoxy-acetyiamino]-methyi]-phenyl)-imino-methyl]-carbamic acid benzyl ester was prepared using a similar procedure as described in example 339. MS 498.4 ([M-t-H]"") Example 341 341.1 Using analogous procedures as described in examples LI - L4 3,5-difluoro-phenol was converted to (RS)-(2,6-difluoro-4-hydroxy-phenyl)-methoxy-acetic acid ethyl ester. White solid. MS 245.2 ([M-H]") 341.2 Using analoguous procedures as describen in examples 279.1 and 334.3 (RS)-(2,6-difluoro-4-hydroxy-phenyl)-methoxy-acetic acid ethyl ester was converted to (RS)-[2,6-difluoro-4-(4,4,5,5-tetramethyl-[ 1,3,2jdioxaborolan-2-yl)-phenyl]-methoxy-acetic add ethyl ester. YeUowoU. MS 356.2 ([M]"^) 341.3 Using a similar procedure as describe in example 57.1 (RS)-[2,6-difluoro-4-(4,4,5,5-tetramethyl-| 1,3,2] dioxaborolan-2-yl)-phenyl]-methoxy-acetic acid ethyl ester was converted to (RS)-(2,6-difluoro-4-pyridin-4-yl-phenyl)-methoxy-acetic acid ethyl ester. Waxy off-white solid. 341.4 A solution of (RS)-{2,6-difluoro-4-pyridm-4-)d-phenyl)-methox7-acetic acid ethyl ester (1.83 g) in CH2CI2 (25 ml) was treated with mCPBA (1.61 g). After stirring overnight at r.t. additional mCPBA (0.6 g) was added and stirring continued for 24 hrs. The reaction mixture was poured onto ice and saturated Na2C03-solution, then extraaed with dichloromethane. The organic layer was washed mit saturated NaiCOs-solution and brine, dried over MgS04, filtered and concentrated. The crude product was isolated by flash chromatography (cydohexane/EtOAc 1:4 => EtOAc; then CUtCh/MeOH 9:1 => 4:1) to give (RS)-[2,6-difluoro-4-(l-oxy-pyTidin-4-yl)-phenyl]-metho3Cy-acetic acid ethyl ester (474 mg) as yeUow oil. MS 324.2 ([M+H]^) 343.5 A solution of (RS)-[2,6-dfluoro-4-(l-oxy-pyridin-4-yl)-phenyl]-methoxy-acetic add ethyl ester (509 mg) in THF was treated with IN NaOH (3.15 ml) and stirred for 5 hrs at r.L. Then, the reaction mixture was neutralized with IN HQ (1.57 ml) and concentrated. The residue was taken up in diethyl ether. The soKd was filtered off, washed with diethyl ether and dried to give (RS)-[2,6-difluoro-4-(l-oxy-pyridin-4-)d)-phenyl]~methoxy-acetic add (599 mg, contains 1 equivalent of NaCl) as off-white sohd. MS 296.2 ([M+H]"") 341.6 (RS)-[2,6-Difluoro-4-(l-oxy-pyridin-4-yl)-phenyl]-methoxy-acetic add vras coupled with 4-aminomethyl-benzamidine hydrochloride (CAS 217313-79-6) according to general procedure C to give (RS)-(4-carbamimidoyl-ben2yl)-2-[2,6-difiuoro-4-(l-oxy-pyridin-4- yl)-phenyl]-2-methoxy-acetamide hydrochloride as amorphous white solid. MS 427.4 ([M+H]^) Example 342 342.1 To a stirred solution of (RS}-N-(4-Cyano-benzyl)-2-[2,6-difiuoro-4-(4,4,5,5-tetrameth)4-[l,3,2]dioxaborolan-2-yI)-phenyi]-2-ethoxy-acetamide (350 mg, example 262.1) at i.t. in dioxane (3 ml) under an argon atmosphere were added trifluoro-methanesulfonic add 3,6-dihydro-2H-pyran-4-yl ester (196 mg, CAS 188975-30-6, solution in 2 ml dioxane), KOH (86 mg), PdCMdppf) (31 mg) and l,l'-bis(diphen5dphosphino)ferrocene (21 mg). The mixtuie was then heated to SO^C for 6 hrs. The mixture was concentrated to leave a dark brown solid. The crude product was isolated by column chromatography (cydohexane => cyclohexane/EtOAc 55:45) to give (RS)-(4-cyano-benzyl)-2-[4-(3,6-dihydro-2H-pyran-4-yl)-2,6-difluoro-phenyl]-2-ethoxy-acetamide {107 mg) as Ught yellow gum. MS 413.1 ([M+HD 342.2 In analog)' to example 307.7 and 307.8 (RS)-(4-cyano-benzyl)-2-[4-(3,6-dihydro-2H- pyran-4-yl)-2,6-difIuoro-phenyll-2-ethoxy-acetainide was converted to (RS)-(4- carbamimidoyl-benzyl)-2-[2,6-difluoro-4-(tetrahydjo-pyran-4-yl)-phenyl]-2-ethox}'- acetamide acetate. Off-white powder. MS 432.4 ([M+H] +) Example 343 Using similar procedures as described in example 342 (RS)-N-(4-cyano-benz)4)-2-[2,6-difiuoro-4-(4,4,5,5-tetramethyl-[l,3)2]dioxaborolan-2-yl)-phenyl]-2-ethoxy-acetamide (example 262.1) was converted to (RS)-(4-carbaEQimidoyl-ben2yl)-2-(4-cycloliexyl-2,6-difluoro-phenyl)-2-ethoxy-acetamide acetate. Off-white powder. MS 430.4 ([M+H]"^) Example A Film coated tablets containing the following ingredients can be manufactured in a conventional manner: Ingredients Per tablet Kernel: Compound of formula (I) 10.0 mg 200.0 mg Microcrystalline cellulose 23.5 mg 43.5 mg Lactose hydrous 60.0 mg 70.0 mg Povidone K30 12.5 mg 15.0 mg Sodium starch glycolate 12.5 mg 17.0 mg Magnesium stearate 1.5 mg 4.5 mg (Kernel Weight) 120.0 mg 350.0 mg Film Coat Hydroxypropyi methyl cellulose 3.5 mg 7.0 mg Polyethylene glycol 6000 0.8 mg 1.6 mg Talc 1.3 mg 2.6 mg Iron oxyde (yellow) 0.8 mg 1.6 mg Titan dioxide 0.8 mg 1.6 mg The active ingredient is sieved and mixed with microcristalline cellulose and the mixture is granulated with a solution of polyvinylpyrrolidon in water. The granulate is mixed with sodium starch glycolate and magesiumstearate and compressed to yield kernels of 120 or 350 mg respectively. The kernels are lacquered with an aqueous solution / suspension of the above mentioned film coat Example B Capsules containing the following ingredients can be manufactured in a conventional manner: Ingredients Per capsule Compound of formula (I) 25.0 mg Lactose 150.0 mg Maize starch 20.0 mg Talc 5.0 mg The components are sieved and mixed and filled into capsules of size 2. Example C Injection solutions can have the following composition: Compound of formula (I) 3.0 mg Polyethylene Glycol 400 150.0 mg Acetic Acid q.s. ad pH 5.0 Water for injection solutions ad 1.0 ml The active ingredient is dissolved in a mixture of Polyethylene Glycol 400 and water for injection (part). The pH is adjusted to 5.0 by Acetic Acid. The volume is adjusted to 1.0 ml by addition of the residual amount of water. The solution is filtered, filled into vials using an appropriate overage and sterilized. Example D Soft gelatin capsules containing the following ingredients can be manufactured in a conventional manner: Capsule contents Compound of formula (I) 5.0 mg Yellow wax 8,0 mg Hydrogenated Soya bean oil 8.0 mg Partially hydrogenated plant oils 34.0 mg Soya bean oil 110.0 mg Weight of capsule contents 165.0 mg Gelatin capsule Gelatin 75.0 mg Glycerol 85 % 32.0 mg Karion 83 8.0 mg (dry matter) Titan dioxide 0.4 mg Iron oxide yellow 1-1 mg The active ingredient is dissolved in a warm melting of the other ingredients and the mixtm-e is filled into soft gelatin capsules of appropriate size. The filled soft gelatin capsules are treated according to the usual procedures. Example E Sachets containing the following ingredients can be manufectured in a conventional manner: Compound of formula (1) 50.0 mg Lactose, fine powder 1015-0 mg MicrocristalHne cellulose (AVICEL PH 102) 1400.0 mg Sodium carboxymethyl cellulose 14.0 mg Polyvin)ipyrrolidon K 30 10.0 mg Magnesiumstearate 10.0 mg Flavoring additives 1,0 mg The active ingredient is mixed with lactose, microcristalline cellulose and sodium carboxymethyl cellulose and granulated with a mixture of polyvinylpyrrolidon in water. The granulate is mixed with magnesiumstearate and the flavouring additives and filled into sachets. WE CLAIM : wherein R1 is hydrogen. OH, NHj, C1,7 aUcoxy-carbonyl, aryI-C[.7 alkoxy-carbonyl, aryloxy-carbonyi, C1.7 alkyl-carbonyl, aryl-carbonyl, or C1.7 alkoxy-carfaonyl which is substituted with halogen; R2, R3 and R4 independently from each other are selected from the group consisting of hydrogen, halogen, hydroxy, carboxy-C1.7 alkyl-NH, carbamoyl-C 1.7 alkyl-NH, C1.7 alkoxy-carbon)d-C1.7 alkyl-NH, hydroxy- Cj-iocycloalkyl-oxy, dihydroxy-C3.10 cyc!oallcyl-oxy, aryl, aryloxy, aryl-NH, aryl-C1,? alkyl-NH, aryl-C1.? alkyl-SO2-NH, aryl-C1.7 alkoxy-carbonyl-NH, aryl-C1.7 alkyl-NH-carbonyl-NH, heteroaryloxy, heteroaryl-Cj.? alkyl-NH, and C1-7 alkoxy, whichQ.? alkox/can optionally be substituted with hydroxy, carboxy, carbamoyl, carbamimidoylt CF3, aryl, heteroaryl, C1.7 alkyl-carbamoyi, C1.7 aikoxy-carbonjd, aryl-carbamoyl, C1.7 alkoxy-C1.7 alkyl-carbamoyl, heterocycl)d-C|.7 alkyi-carbamoyl, or N(C!.7 aIkyl)2-C1.7 alkyl-carbamoyl; R1 isC1.7alkyi orCj-iocycloalkyl, or, ifXis O or NR12R5 can also be hydrogen; R1 is hydrogen, C1-7 alkyl, or fluoro- C1.7 alkyl; Y isNorC-R11; R7, R9, R9, R10 and R" independently from each other are selected from the group consisting of hydrogenj hydroxy, halogen, amino, C^.j alkyl-amino, di- C1.7 alkyl-amino, C1-7 alkyl-carbonyl-amino, NO2, fluoro- C1-7 alkyt, C1.7 alkoxy, hydroxy- C1.7 alkoxy. fluoro- C1.7 alkoxy, C2-7 alkinyl, hydroxy- C2.7 alkinyl. aryl, aryi- Q.? alkoxy, aryloxy, aryloxy- C|.7alkoxy, heterocyclyl, heterocydylo3cy. Ct.7 alkoxy-carbonyl- C1.7 alkoxy. carbamoyl- C1.7 alkoxy, carboxy- C;.? alkoxy, C3.10 cycloalkyloxy, heteroaryl, amino- C1-7 alkoxy. d .7 alkyl-amino-C1.jalkoxy, and di-C1-7alkyl-amino-C1.7alkoxy, C1./alkyl-carbonyI-amino-C1.7alkyl, H0'1>}=CH, HCO, fluoro-C1.j alkyi-SOi-O, {C1.7 alkoxy)2^. CH(C1-7 alkoxy)], hydroxy-CH2oro-C1.7alkoxy, atyl-C1-7alkoxy-Q.? alkoxy, aryl-NH, aryl-NH-C1.7 alkyi, aryl-C1-; aikyl-carbonyi-NH, heterocyclyl-C1.7alkyl, heterocyclyl-carbonyl,heterocydyl-C1.7 alkoxy, C1.7alkyl-carbamoyI, fluoro-C1.7alkyI-carbamoyI, Cj-iQi^C1oaikyi-carbamoyi, C3_iocyC1oalkyi-C1.7 alkyl-carbamoyl, di-C1-^alkyl-carbamoyl, Cj,7alkDxy-C1-7alkyl-carbamoyl, di-Ct.7 alkyl-carbamoyl-C1^? alkoxy, heteroaryloxy, heteroaryl-C1-7 alkoxy, amino-C|.7allc)d, C1.7alk^, hydroxy-C1.7alkyl, Cj-iocydoalkyl.and Cj.iocycloalkyl- Q. 7 alkoxy which is optionally substituted with C1-7 alkyl; or R* and R9 or R7 and R9 are bound to each other to form a ring together with the carbon atoms to which they are attached and R and R together or R and R together are -0-CHj-O-. -O-CH2-CO-NH-, -O-CHj-CHrCH2-. or -CH=CH-CH=CH-, which can optionally be substituted with C1.7 alkyl or C(_7 alkoxy, and R"', R" andR1 or R9 respectively are as definde above; X isO R1^ is hydrogen, C1.7 alkyl, or C1.7 alkyl-carbonyl; and pharmaceutically acceptable salts thereof wherein the term "aryl" means a phenyl or naphthyl group, which can optionally be substituted by 1 to 5 substituents independently selected from the group consisting of C2.7 alkenyl, C2.7 alkinyl, dioxo-C1.7alk)dene, halogen, hydroxy, CN, CF3, NHi, N(H, C1.7 alkyl). N{C1-7 alkyDz, aminocarbonyl. carboxy, NO2, C1-7 alkoxy, thio- C1-7alkoxy, C1.7 alkylcarbonyl, C).? aUcylcarbon)dOxy, C1.7 alkoxycarbonyl, C1.7 alkyl-carbonyi-NH, fluoro-C1.7 alkyl, fluoro-C1.7 alkoxy, C|.7 allcoxy-carbonyl- C1.7alkoxy, carboxy-C|-7alkoxy, carfaamoyl-C1.? alkoxy, hydroxy-C1.7 alkoxy, NHrC1.7 alkoxy, N(H, Q.? alk)4)-C1.7 aUcoxy, NCC1.7 alkyl)3-C,.7 alkoxy, benz>^oxy-C,-7 alkoxy, HO-N=:CH-, and C1.? alkyl which can optionaUy be substituted with haJogen, hydroxy, NH2, N(H, C1.7 aikyl) or N(C1.7a]kyl)2: the term "heteroaryl" means an aromatic 5 to 6 membered monocyclic ring or 9 to 10 membered bicyclic ring which can comprise 1, 2 or 3 atoms selected from nitrogen, oxygen and/or sulphur, and the heteroaryl group may have a substituent described in connection with the term "aryl"; the term "heterocyclyi" means non-aromatic monocyclic heterocycles with 5 or 6 ring members, which comprise 1, 2 or 3 hetero atoms selected from nitrogen, oxygen and sulfur, and the heterocyclyi group may have a substituent described in connection with the term "aryl". 2. The compounds according to claim 1, wherein R1 is hydrogen, OH, NH2, C1.7alkoxy-carbonyl, aryl-Cj.? alkoxy-carbonyl, aryloxy- carbony!, C1-7 alkyl-carbonyi, aryl-carbonyl, or C].? alfcoxy-carbonyl which is substituted with halogen; R7, R7 and R* independently from each other are selected from the group consisting of hydrogen, halogen, hydroxy, and C1.7 alkoxy, which C1.7 alkoxy can optionaUy be substituted with hydroxy, carboxy or carbamoyl; R1 ■ isC1.7alkyIorC3.iocycloalkyi, or, ifXisOorNR1^, R7can also behydrogen; R* is hydrogen, C1.7 alkyl, or 9uoro-C|.7 alkyi; Y isNorC-R7; R1, R", R9, R10 and R9 ' independently from each other are selected, from the group consisting of hydrogen, hydroxy, halogen, amino, C(.7alkyl-amino, di-Cj.? alkyl-amino, C1.7alkyl-carbonyl-amino, NOz, fluoro-C1.7alkyl, C1_7alkoxy, hydroxy-C1-7 alkoxy, fluoro-C)-7alkoxy, C1.j alkin>i, hydroxy-C2.7 alkinyt, aryl, aryl-Cj.7 alkoxy, aryloxy, aryloxy-C1.7alkoxy, heterocyclyi, heterocydyloxy, C1.7 alkoxy-carbonyl-C1.7 alkoxy, carbamoyl-C1.7 alkoxy, carboxy-C|.7 alkoxy, Cs-io cycJoalkyJoxy, heteroaryl, amino-C1-?alkoxy, Cj-7 alkyl-amino-C1.? alkoxy, and di-C1.7 alkyl-amino-C1.7 alkoxy. or R* and R9 or R* and R9' are bound to each other to form a ring together with the carbon atoms to which they are attached and R* and R9 together or R* and R7 together are -0-CH2-0-, -O-CH3-CO-NH-, -O-CH2-CH2-CH2-, or -CH=CH-CH=CH-, which can optionally be substituted with C1 .7 alkyl or C1.7 alkoxy, and R10, R9 ' and R7 or R* respectively are as definde above; X isO R1^ is hydrogen, C1.7 alkyl, or C1.7 alkyl-carbonyl; and pharmaceutically acceptable salts thereof. 3. The compounds according to any of claims 1-2, wherein R is hydrogen, OH, NH2, or Cj.jalkoxy-carbonyl. 4 The compounds according lo any of claims 1-3, v^erein R9is hydrogen, OH, or C1.,alkoxy-carDonyi. 5, The compounds according 10 any of claims 1 - 4, wherein R is hydrogen, OH, or ethoxycarbonyl. 6. The compounds according to any of claims I -5, wherein R is hydrogen. y_ The compounds according lo any of claims 1-6, wherein R7, R9and R* independently from each other are hydrogen or halogen. 8. The compounds according to any of claims I - 7, wherein R , R and R are hydrogen. 9. The compounds according to any of claims 1 - 6, wherein R andR are hydrogen. IQ The compounds according to claim I, wherein R7 is hydrogen, halogen, hydroxy, caiboxy-C1-yalkyl-NH, carbamoyl-C1-yaM-NH, C1.7alkoxy-carbonyl- C1.7a!kyl-NH,hydroxy-C3.iocycloalkyl-oxy, dihydroxy-C3.iocydoalkyl-oxy,aryl, aryloxy, aryl-NH, aryl-C1.7 alkyl-NH, aryI-C1.7 alkyl-S02-NH, aryl-C,.? alkoxy-carbonyl-NH, aryi- C,.? alkyl-NH-carbonyl-NH, heteroaryloxy, heteroar)d-C1.7 alkyl-NH, or C1-7 alkoxy, which C1.7 alkojcy can optionally be substituted with hydroxy, carboxy, carbamoyl, carbamimidoyl, CFs, ary], heteroaryl. C1.7alk>^-carbamo)4, C1.7 alkoxy-carbonyl, aryl-carbamoyl, C1.7 alkoxy-C1.yalkyl-carbamoyl, heteroq'dyl-C|.7alkyl-carbamoyLorN{C|.7alkyl)2-C|.7aIk)'l-caibamoyl. U. The compounds according to claim I, wherein R7 is hydrogen, halogen, carboKy-C1.7aIfc)4-NH, aryUC1-? alkyl-NH, heteroaryt-C1.jalkyl-NH, or Q.y alkoxy, which C1-Talkoxycan optionally be substituted with carbamoyl, heteroar)d, or C1-Talkoxy-C1.y alkyl-carbamoyl. 12, The compounds according to claim J, wherein R7 i* hydrogen, fluorine, carbamoyimelhoxy, (2-methoxy-ethylcarbainoyI}-methoxy, pyridin-2-y!-methoxy, benzylamino, carboxymethl-amino, or pyridin-2-yImethyl-amino. 13. The compounds accordingto any of claims 1 - 12, wherein R7 is C1-7alkyl. 14. The compounds according to any of claims 1-13, wherein R7 is methyl or ethyl. 15. The compounds according to any of claims 1 - 14, wherein R* is hydrogen, methyl, or CFs. 16. Thecompounds according to any of claims I - r5, wherein R* is hydrogen. 17. The compounds according to any of claims 1 -16. wherein Y is C-R" and R9 R*, R9, R9° and R9 ' independently from each other are selected from the group consisting of hydrogen, hydroxy, halogen, di-C1-yallcyl-amino, C1.7aikyl-carbonyl-amino, NO3, fluoro-C1-7 alkyl, C1.7 alkoxy, hydroxy- C1.7 aUtoxy, fluoro- C1-7 aDcojfy, aryl, aryl-C1.7alkoxy, aryloxy, aryloxy-C1-? alkoxy, heterocyclyl, hcterocydyloxy, Cj-7 alkoxy-carbonyl-C1.? alkoxy, carbamoyl-C1-7 alkoxy, carboKy-C1.7 alkoxy, C3.10 cycloalkyloxy, heteroaryl, and di-C1-? atkyl-amino-C1.7 alkoxy. 18. The compounds according to any of claims I -17, wherein Y is C-R" and R7 R*, R9, R10 and R" independently from each other are selected from the group consisting of hydrogen, halogen, C1.7 alkoxy, and pyridyL 19. The compounds according to any of claims 1-18, wherein Y is C-R" and R"", R7, R9, R10 and R" independently from each other are selected from the group consisting of hydrogen, fluoro, bromo, methoxy, and pyridyl. 20. The compounds according to claim 1, wherein Y is C-R1\ R7 andR7or R9and R9 are bound to each other to form a ring together with the carbon atoms to which they are attached and R7 and R7 together or R* and R7 together are -O-CH2-O-, -O-CH2-CO-NH-. -O-CH2-CH2-CH2-, or -CH=CH-CH=CH-. which can optionally be substituted with C1.7 alley] or C1.7 aJkoxy, and R10, R7 and R7 or R7 respectiveiy are hydrogen. 21. The compounds according to any of claims I -16, wherein Y is C-R" and R9 R8, R9, R10 and R7 independently from each other are selected from the group consisting of hydrogen, halogen, Cj.? alkcoxy and heteroaryl. 22. The compounds according to any of claims 1 - 16, wherein Y is C-R" R7 is halogen, R* is hydrogen, R9 is C1.7 alkoxy, heteroaryl or heteroaryl-Cj.? alkoxy, R10is hydrogen and R" is hydrogen or halogen. 23. The compounds according to any of claims 1 - 16, wherein Y is C-R", R9 is fluorine, R7 is hydrogen, R9 is methoxy, pyridin-3-yI, 5-amino-pyridin-2-yI, 6-amJno-pyridin-3-yl, pyTidin-2-ylmethoKy, or 2-amino-pyTimidin-5-yl, R9° is hydrogen and R" is hydrogen or fluorine. 24. The compounds according to claim 1, selected from the group consisting of (S)-N-(4-Carbamimidoyl-benzyl)-2-methoxy-2-phenyi-acetamide hydrochloride, (RS)-N-(4-Carbamimidoyl-ben2yI)-2-(2-fluoro-4-methoxy-phenyl)-2-methoxy-acetamide hydrochloride, (RS)-lAniino-(4-l[2-{2-fluoro-4-methoxy-phenyi)-2-methoxy-acetylamino]-methyl}-phenyl)-methylene]-carbamic aC1d ethyl ester, (RS)-2-C2-Fluoro-4-methoJcy-phenyl)-N-[4-(N-hydroxycarbamimidoyl)-beiizyl]-2-methoxy-acetamide, (RS)-N-(4-Carbamimidoyl-ben2yI)-2-(3-fluoro-3'-methoxy-biphenyl-4-yl)-2-methoxy-acetamide hydrochloride, (RS)-N-(4-Carbamimidoyl-benzyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyI)-acetamide hydrochloride, {RS)-N-(4-Carbamimidoyl-benzyl)-2-(2,6-difluoro-4-methoxy-phenyl)-2-methoxy-acetamide hydrochloride, (RS)-N-(4-Carbamimido)1-benzyI)-2-(2-fluoro-4-pyridin-3-yl-phenyi)-2-methoxy-acetamide hydrochloride, and (RS)-2-{4-Bronio-2,6-difluoro-phenyl )-N-(4-carbamimidoyl-benzyi)-2-ethoxy-acetamide hydrochloride, and pharmaceuticaily acceptable salts thereof. 25. The compounds according to claim I, selected from the group consisting of (RS)-N-(4-Carbamimidoyl-2-carbaraoylmethoxy-benzyl)-2-(2,6-difluoro-4-methoxy-phenyI)-2-ethoxy-acetainide hydrochloride, (RS)-N-{4-Carbaminiidoyl-2-[{2-rnethOxy-eth7lcarbamoy!)-melhoxy]-benzyl}-2-(2,6-difluoro-4-methoxy-phenyl)-2-ethoxy-acetamide hydrochloride, (RS)-N-l4-Carbamim!doyl-2-(pyridin-2-y!inetho);y)-benzyl]-2-{2,6-difluoro-4-niethoxy-phcny3)-2-jiietbQxy-acetaniidehydroc]3]oride, (RS)-2-[4-(2-Ainino-pyrimidin-5-yl)-2,6-difluaro-phen)d]-N-(4-caibamimidoyl-benzyl)-2-ethDxy-acetamidc hydrochloride, (RS)-N-(4-Carbaminiidoyl-benzyl)-2-{2,6-difluoro-4"pyTidin-3-yl-phenyt)-2-ethoxy-acetamide hydrochloride, (RS)-2-[4-{5-Amino-pyridin-2-yl)-2,6-diQuoro-phenyll-N-(4-carbamimidoyI-benzyl)-2-ethoxy-acetamide hydrochloride, (RS)-(2-[4-(6-Amino-pyridin-3-yl)-2,6-difluoro-phenyI]-N-(4-carbamimidoyl-benzyl)-2-ethoxy-acetamide hydrochloride, (RS)-N-C4-Carbamimidoyl-benzyl)-2-l2,6-difluoro-4-(pyridin-2-ylmethoxy)-phenyl]-2-ethoxy-acetamide hydrochloride, (RS)-N-(2-Benzylamino-4-carbaniiinidoy!-benzyl}-2-ethoxy-2-(2-fluoro-4'inethoxy-phenyO-acetamide acetate, (RS)-(5-CarbamimidoyI-2-{[2-ethoxy-2-{2-fluoro-4-methoxy-phenyl)-acety!araino)-methyil-phenytainino)-acetic aC1d acetate, (RS)-(4-Carbaniimidoyl-2-carbamo)dmelhoxy-benzyl)-2-[2,6-difluoro-4~(pyTidin-2-yImethoxy)-phenyI]-2-ethoxy-acetamide hydrochloride, (RS)-2-[4-(6-Amino-pyridin-3-yl)-2,6-difluoro-phenyll-N-(4-carbamimidoyl-2,6-difluoro^benzy])-2-ethoxj'-acetamide acetate, and (RS)-i4-Carbamimido>d-2-[(pyridiii-2-yiinethyl)-aminol-benzyl}-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide hydrochloride, and pharmaceylicajly acceptable salts thereof. 26. A process for the manufacture of compounds of formula {I) as defined in any of claims I -25 which process comprises converting the nitrile group in a compound of formula (11) wherein R2 R3 R4 R5 R6 R7, R8, R9, R10, X and Y have the significances given in any of claims 1-25 into a carbamimidoyl group, or into a N-hydroxy-carbamimidoyl group, or into a N-amino-carbamimidoyl group, and, if desired, converting an obtained compound of formula (I) into a pharmaceutically acceptable "salt. 27. The Compounds according to any of claims 1 - 26, when manufectured by a process according to claim 26. 28. Compounds of formula (II) wherein R7 R7 R*, R7 R*, R9, R*, R9, R9*". X and Y have the significances given in claim 1. 29, Pharmaceutical compositions comprising a compound according to any of claims 1-25, and a pharmaceutically acceptable carrier and/or adjuvant

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