Indian Patents. 263974:NOVEL VANILLOID RECEPTOR LIGANDS AND THE USE THEREOF FOR THE PRODUCTION OF PHARMACEUTICALS

Title of Invention	NOVEL VANILLOID RECEPTOR LIGANDS AND THE USE THEREOF FOR THE PRODUCTION OF PHARMACEUTICALS
Abstract	The present invention relates to novel vanilloid receptor ligands, to processes for the production thereof, to pharmaceuticals containing said compounds and to the use of said compounds for the production of pharmaceuticals.

Full Text	Novel vanilloid receptor ligands and the use thereof for the production of pharmaceuticals The present invention relates to novel vanilloid receptor ligands, to processes for the production thereof, to pharmaceuticals containing said compounds and to the use of said compounds for the production of pharmaceuticals. The treatment of pain, particularly neuropathic pain, is of great significance in the medical field. There is a global need for effective pain therapies. The urgent need for action to provide a patient-friendly und targeted treatment of chronic and non-chronic states of pain, this being taken to mean the successful und satisfactory treatment of pain for patients, is documented by the large number of scientific papers which have recently appeared in the field of applied analgesics or in basic research concerning nociception. A suitable starting point for the treatment of pain; particularly of pain selected from the group consisting of acute pain, chronic pain, neuropathic pain, and visceral pain, particularly preferably neuropathic pain; is the vanilloid receptor of subtype 1 (VR1/TRPV1), frequently also designated as the capsaicin receptor. This receptor is stimulated, inter alia, by vanilloids such as capsaicin, heat, and protons and plays a central part in the generation of pain. Furthermore, it is significant for a large number of other physiological and pathophysiological processes such as migraine; states of depression; neurodegenerative disorders; cognitive disorders; anxiety; epilepsy; coughing; diarrhea; pruritus; inflammations; disorders of the cardiovascular system; food intake disorders; medicine addiction; medicine abuse and, in particular, urinary incontinence. It is thus an object of the invention to provide novel compounds which are particularly suitable for use as pharmacologically active substances in pharmaceuticals, preferably in pharmaceuticals for treatment of disorders or diseases that are at least partially mediated by vanilloid receptors 1 (VR1/TRPV1 receptors). It has now been found, surprisingly, that the substituted compounds of the general formula I stated below show excellent affinity to the vanilloid receptor of subtype 1 (VR1/TRPV1 receptor) and are therefore particularly suitable for the prophylaxis and/or treatment of disorders or diseases which are at least partially mediated by vanilloid receptors 1 (VR1/TRPV1). The substituted compounds of the general formula I given below also show anti-inflammatory activity. It is thus an object of the present invention to provide substituted compounds of the general formula I, in which 0 stands for 0, 1,2, 3, or 4; R1 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(= O)-NH2; -S(= O)2-NH2; -C(= O)-NH-OH; -C(= O)-OH; -C(= O)-H; -S(= O)2-OH; -C(= NH)- NH2; -C(= NH)-NH-R9; -N= C(NH2)2; -N= C(NHR10)-(NHR11); -O-P(= 0)2-O- R12; -NHR13; -NR14R15; -NH-C(=O)-R13; -OR16; -SR17; -C(= O)-NHR18; -C(= O)-NR19R20; -S(= O)2-NHR21; -S(= O)2-NR22R23; -C(= O)-OR24; -C(= O)-R25; - S(= O)-R26; or -S(= O)2-R27 or for a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical; R2 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(= O)-NH2; -S(= O)2-NH2; -C(= O)-NH-OH; -C(= O)-OH; -C(= O)-H; -S(= O)2-OH; -C(= NH)- NH2; -C(= NH)-NH-R9; -N= C(NH2)2; -N= C(NHR10)-(NHR11); -O-P(= 0)2-O- R12; -NHR13; -NR14R15; -NH-C(= O)-R13; -OR16; -SR17; -C(= O)-NHR18; -C(= O)-NR19R20; -S(= O)2-NHR21; -S(= O)2-NR22R23; -C(= O)-OR24; -C(= O)-R25; - S(= O)-R26; or -S(= O)2-R27 or for a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical; R3 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(= O)-NH2; -S(= O)2-NH2; -C(= O)-NH-OH; -C(= O)-OH; -C(= 0)-H; -S(= O)2-OH; -C(= NH)- NH2; -C(= NH)-NH-R9; -N= C(NH2)2; -N= C(NHR10)-(NHR11); -O-P(= O)2-O- R12; -NHR13; -NR14R15; -NH-C(= O)-R13; -OR16; -SR17; -C(= O)-NHR18; -C(= O)-NR19R20; -S(= O)2-NHR21; -S(= O)2-NR22R23; -C(= O)-OR24; -C(= O)-R25; - S(= O)-R26; or -S(= O)2-R27 or for a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical; R4 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(= O)-NH2; -S(= O)2-NH2; -C(= O)-NH-OH; -C(= O)-OH; -C(= O)-H; -S(= O)2-OH; -C(= NH)- NH2; -C(= NH)-NH-R9; -N= C(NH2)2; -N= C(NHR10)-(NHR11); -O-P(= O)2-O- R12; -NHR13; -NR14R15; -NH-C(= 0)-R13; -OR16; -SR17; -C(= O)-NHR18; -C(= O)-NR19R20; -S(= O)2-NHR21; -S(= O)2-NR22R23; -C(= O)-OR24; -C(= O)-R25; - S(= O)-R26; or -S(= O)2-R27 or for a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical; R5 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(= O)-NH2; -S(= O)2-NH2; -C(= O)-NH-OH; -C(= O)-OH; -C(= O)-H; -S(= O)2-OH; -C(= NH)- NH2; -C(= NH)-NH-R9; -N= C(NH2)2; -N= C(NHR10)-(NHR11); -O-P(= O)2-O- R12; -NHR13; -NR14R15; -NH-C(= O)-R13; -OR16; -SR17; -C(= O)-NHR18; -C(= O)-NR19R20; -S(= O)2-NHR21; -S(= O)2-NR22R23; -C(= O)-OR24; -C(= O)-R25; - S(= O)-R26; or -S(= O)2-R27 or for a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical; R6 stands in each case for hydrogen or for a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical; R7 stands for hydrogen or -OH; or R6 and R7 form, together with the interconnecting carbon atom as ring member, a saturated or unsaturated, unsubstituted or at least monosubstituted three- membered, four-membered, five-membered, or six-membered cycloaliphatic radical; R8 stands for -SF5; -O-CF3; -CF3; -O-CFH2; -O-CF2 H; -CFH2; -CF2 H; or for an unsubstituted or at least monosubstituted tert-butyl radical; T stands for C-R35 and U stands for C-R36 and V stands for N and W stands for C-R38 Or T stands for C-R35 and U stands for N and V stands for C-R37 and W stands for C-R38 Or T stands for N and U stands for C-R36 and V stands for C-R37 and W stands for C-R38 Or T stands for N and U stands for N and V stands for C-R37 and W stands for C-R38 Or T stands for N and U stands for C-R36 and V stands for N and W stands for C-R38 Or T stands for C-R35 and U stands for N and V stands for N and W stands for C-R38 Or T stands for C-R35 and U stands for C-R36 and V stands for C-R37 and W stands for C-R38; R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, R25, R26 and R27 each independently stand for a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical; for an unsaturated or saturated, unsubstituted or at least monosubstituted, three-membered, four-membered, five-membered, six-membered, seven- membered, eight-membered, or nine-membered cycloaliphatic radical optionally containing at least one heteroatom as ring member, which can be condensed with a saturated or unsaturated, unsubstituted or at least monosubstituted monocyclic or polycyclic ring system and/or can be bonded via a linear or branched, unsubstituted or at least monosubstituted C1-6 alkylene group or two to six-membered heteroalkylene group; or for an unsubstituted or at least monosubstituted five-membered to fourteen- membered aryl radical or heteroaryl radical, which can be condensed with a saturated or unsaturated, unsubstituted or at least monosubstituted monocyclic or polycyclic ring system and/or can be bonded via a linear or branched, unsubstituted or at least monosubstituted C1-6 alkylene group or two to six-membered heteroalkylene group; R35, R36, and R37 each independently stand for H; F; CI; Br; I; -SF5; -NO2; -CF3; -CN; - NH2; -OH; -SH; -C(= O)-NH2; -S(= O)2-NH2; -C(= O)-NH-OH; -C(= O)-OH; -C(= O)-H; -S(= O)2-OH; -NHR13; -NR14R15; -NH-C(= O)-R13; -OR16; -SR17; -C(= O)- NHR18; -C(= O)-NR19R20; -S(= O)2-NHR21; -S(= O)2-NR22R23; -C(= O)-OR24; - C(= O)-R25; -S(= O)-R26; -S(= O)2R27 for a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical; or for an unsubstituted or at least monosubstituted five-membered to fourteen- membered aryl radical or heteroaryl radical, which can be condensed with a saturated or unsaturated, unsubstituted or at least monosubstituted monocyclic or polycyclic ring system and/or can be bonded via a linear or branched, unsubstituted or at least monosubstituted C1-6 alkylene group or C2-6 alkenylene group or C2-6-alkynylene group; R38 stands for F; CI; Br; I; -SF5; -NO2; -CF3; -CF2 CI; -CN; -NH2; -OH; -SH; -C(= O)- NH2; -S(= O)2-NH2; -C(= O)-NH-OH; -C(= O)-OH; -C(= O)-H; -S(= O)2-OH; - NHR39; -NR40R41; -OR42; -SR43; -C(= O)-NHR44; -C(= O)-NR45R46; -S(= O)2- NHR47; -S(= O)2-NR48R49; -C(= O)-OR50; -C(= O)-R51; -S(= O)-R52; -S(= O)2- R53; -C(= NH)-NH2; -C(= NH)-NH-R54; -N= C(NH2)2; -N= C(NHR55)-(NHR56); for a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical; for an unsaturated or saturated, unsubstituted or at least monosubstituted three-membered, four-membered, five-membered, six-membered, seven- membered, eight-membered, or nine-membered cycloaliphatic radical optionally exhibiting at least one heteroatom as ring member, each of which is bonded to the parent structure over a carbon atom in the ring of the cycloaliphatic radical and is condensed with a saturated or unsaturated, unsubstituted or at least monosubstituted monocyclic or polycyclic ring system and/or can be bonded via a linear or branched, unsubstituted or at least monosubstituted C1-6 alkylene group or C2-6 alkenylene group or C2-6 alkynylene group; or for an unsubstituted or at least monosubstituted five-membered to fourteen- membered aryl radical or heteroaryl radical, which can be condensed with a saturated or unsaturated, unsubstituted or at least monosubstituted monocyclic or polycyclic ring system and/or can be bonded via a linear or branched, unsubstituted or at least monosubstituted C1-6 alkylene group or C2-6 alkenylene group or C2-6-alkynylene group; R39, R40, R41, R42, R43, R44, R45, R46, R47, R48, R49, R50, R51, R52, R53, R54, R55, and R56 each independently stand for a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical; for an unsaturated or saturated, unsubstituted or at least monosubstituted, three-membered, four-membered, five-membered, six-membered, seven- membered, eight-membered, or nine-membered cycloaliphatic radical optionally containing at least one heteroatom as ring member, which can be condensed with a saturated or unsaturated, unsubstituted or at least monosubstituted monocyclic or polycyclic ring system and/or can be bonded via a linear or branched, unsubstituted or at least monosubstituted C1-6 alkylene group or two to six-membered heteroalkylene group; or for an unsubstituted or at least monosubstituted five-membered to fourteen- membered aryl radical or heteroaryl radical, which can be condensed with a saturated or unsaturated, unsubstituted or at least monosubstituted monocyclic or polycyclic ring system and/or can be bonded via a linear or branched, unsubstituted or at least monosubstituted C1-6 alkylene group or two to six-membered heteroalkylene group; or R40 and R41 form, together with the interconnecting nitrogen atom as ring member, a saturated or unsaturated four-membered, five-membered, six-membered, seven-membered, eight-membered, or nine-membered heterocycloaliphatic radical, which is unsubstituted or substituted by 1, 2, 3, 4, or 5 radicals R57 and optionally exhibits at least one further heteroatom as ring member, and which can be condensed with a saturated or unsaturated, unsubstituted or at least monosubstituted monocyclic or polycyclic ring system; R57 stands for -NHR58, -NR59R60, or for a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical; R58, R59, and R60 each independently stand for -C(= O)-R61; for a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical or for an unsubstituted or at least monosubstituted five-membered to fourteen- membered aryl radical or heteroaryl radical, which can be condensed with a saturated or unsaturated, unsubstituted or at least monosubstituted monocyclic or polycyclic ring system and/or can be bonded via a linear or branched, unsubstituted or at least monosubstituted C1-6 alkylene group or C2-6 alkenylene group or C2-6 alkynylene group; and R61 stands for a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical; each optionally in the form of one of the pure stereoisomers thereof, particularly enantiomers or diastereoisomers thereof, the racemates thereof or in the form of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in an arbitrary mixing ratio, or each in the form of corresponding salts, or each in the form of corresponding solvates; wherein the aforementioned aliphatic C1-10 radicals and tert-butyl radicals can each be optionally substituted by 1, 2, 3, 4, 5, 6, 7, 8, or 9 substituents independently selected from the group consisting of F, CI, Br, I, -CN, -NO2, -OH, -NH2, -SH, -O(C1-5 alkyl), - S(C1-5 alkyl), -NH(C1-5 alkyl), -N(C1-5 alkyl)-(C1-5 alkyl), -C(= O)-O-(C1-5 alkyl), -O-C(= O)-(C1-5 alkyl), -O-phenyl, phenyl, -OCF3, and -SCF3; the aforementioned two to six-membered heteroalkylene groups, C1-6 alkylene groups, and C2-6 alkenylene groups and C2-6 alkynylene groups can each be optionally substituted by 1, 2, 3, 4, 5, 6, 7, 8, or 9 substituents independently selected from the group consisting of F, CI, Br, I, -CN, -NO2, -OH, -NH2, -SH, -O(C1-5 alkyl), - S(C1-5 alkyl), -NH(C1-5 alkyl), -N(C1-5 alkyl)-(C1-5 alkyl), -OCF3, and -SCF3; the aforementioned heteroalkylene groups each optionally exhibit 1, 2, or 3 heteroatom(s) independently selected from the group consisting of oxygen, sulfur, and nitrogen (NH) as link(s); the aforementioned (hetero)cycloaliphatic radicals are optionally each substituted by 1,2,3, 4, or 5 substituents independently selected from the group consisting of -(C1-6 alkylene)-OH, = CH2, -O-(C1-5 alkylene)oxetanyl, -(C1-5 alkylene)-O-(C1-5 alkylene)oxetanyl, -CH2-NH-(C1-5 alkyl), -CH2-N(C1-5 alkyl)2, -N[C(= O)-(C1-5 alkyl)]phenyl, -CH2-O-(C1-5 alkyl), oxo (= O), thioxo (= S), F, CI, Br, I, -CN, -CF3, -SF5, -OH, -O-(C1-5 alkyl), -O-C(= O)-(C1-5 alkyl), -NH2, -NO2, -O-CF3, -S-CF3, -SH, -S-(C1-5 alkyl), -(C1-5 alkyl), -C(= O)-(C1-5 alkyl), -C(= O)-OH, -C(= O)-O-(C1-5 alkyl), -NH-(C1-5 alkyl), -N(C1-5 alkyl)2, -NH-phenyl, -N(C1-5 alkyl)phenyl, cyclohexyl, cyclopentyl, (4,5)- dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, piperidinyl, pyrrolidinyl, -(CH2)-pyridinyl, pyridinyl, -O-phenyl, -O-benzyl, phenyl, and benzyl, and the cyclic moiety of the radicals oxetanyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)- thiadiazolyl, thiophenyl, phenethyl, -N[C(= O)-(C1-5 alkyl)]phenyl, -NH-phenyl, -N(C1-5 alkyl)phenyl, -(CH2)-pyridinyl, pyridinyl, -O-phenyl, -O-benzyl, phenyl, and benzyl can each be substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of F, CI, Br, -OH, -CF3, -SF5, -CN, -NO2, -C1-5-alkyl, -O-C1-5 alkyl, - O-CF3, -S-CF3, phenyl, and -O-benzyl, and, unless otherwise stated, the aforementioned (hetero)cycloaliphatic radicals can each optionally exhibit 1, 2, or 3 (further) heteroatom(s) independently selected from the group consisting of oxygen, nitrogen, and sulfur; the rings of the aforementioned monocyclic or polycyclic ring systems can each be optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of oxo (= O), thioxo (= S), F, CI, Br, I, -CN, -CF3, -SF5, -OH, -O-(C1-5 alkyl), -NH2, -NO2, -O-CF3, -S-CF3, -SH, -S-(C1-5 alkyl), -(C1-5 alkyl), -C(= O)-(C1-5 alkyl), -C(= O)-OH, -C(= O)-O-(C1-5 alkyl), -NH-(C1-5 alkyl), -N(C1-5 alkyl)2, -O-phenyl, -O-benzyl, phenyl, and benzyl, and the cyclic moiety of the radicals -O-phenyl, -O- benzyl, phenyl, and benzyl can each be substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of F, CI, Br, -OH, -CF3, -SF5, -CN, - NO2, -C1-5-alkyl, -O-C1-5-alkyl, -O-CF3, -S-CF3, phenyl, and -O-benzyl, and the rings of the aforementioned monocyclic or polycyclic ring systems are each five-membered, six-membered, or seven-membered and can each optionally exhibit 1, 2, 3, 4, or 5 heteroatom(s) as ring member(s), which are independently selected from the group consisting of oxygen, nitrogen, and sulfur; and the aforementioned aryl radicals or heteroaryl radicals can each be optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of F, CI, Br, I, -CN, -CF3, -SF5, -OH, -O-C1-5-alkyl, -NH2, -NO2, -O-CF3, -S- CF3, -SH, -S-C1-5-alkyl, -C1-5 alkyl, -C(= O)-OH, -C(= O)-O-C1-5-alkyl, -NH-C1-5-alkyl, - N(C1-5-alky)2, -NH-S(= O)2-C1-5 alkyl, -NH-C(= O)-O-C1-5 alkyl, -C(= O)-H, -C(= O)-C1- 5-alkyl, -C(= O)-NH2, -C(= O)-NH-C1-5-alkyl, -C(= O)-N-(C1-5-alkyl)2, -O-phenyl, -O- benzyl, phenyl, and benzyl, and the cyclic moiety of the radicals -O-phenyl, -O- benzyl, phenyl, and benzyl can each be substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of F, CI, Br, -OH, -CF3, -SF5, -CN, - NO2, -C1-5-alkyl, -O-C1-5-alkyl, -O-CF3, -S-CF3, phenyl, and -O-benzyl, and the aforementioned heteroaryl radicals can each optionally exhibit 1, 2, 3, 4, or 5 heteroatom(s) independently selected from the group consisting of oxygen, nitrogen, and sulfur as ring member(s). The term "heteroalkylene" designates an alkylene chain in which one or more C- atoms have each been replaced by a heteroatom independently selected from the group consisting of oxygen, sulfur and nitrogen (NH). Heteroalkylene groups can preferably contain 1, 2, or 3 heteroatom(s) and more preferably one heteroatom, independently selected from the group consisting of oxygen, sulfur and nitrogen (NH), as link(s). Heteroalkylene groups can preferably be two to six-membered and more preferably two or three-membered. Mention may be made, for example, of heteroalkylene groups such as -CH2-CH2-O- CH2-, -CH2-CH(CH3)-O-CH2-, -(CH2)-O-, -(CH2)2-O-, -(CH2)3-O-, -(CH2)4-O -, -O- (CH2)-, -O-(CH2)2-, -O-(CH2)3-, -O-(CH2)4-, -C(C2H5)-(H)-O-, -O-C(C2H5)-(H)-, -CH2-O- CH2-, -CH2-S-CH2-, -CH2-NH-CH2-, -CH2-NH-, and -CH2-CH2-NH-CH2-CH2. If one or more of the aforementioned substituents exhibit a linear or branched C1-6- alkylene group, these can be preferably selected from the group consisting of -(CH2)- , -(CH2)2-, -C(H)-(CH3)-, -(CH2)3-, -(CH2)4-, -(CH2)5-, -C(H)-(C(H)-(CH3)2)-, and - C(C2H5)-(H)-. Saturated or unsaturated C1-10 aliphatic radicals can stand for a C1-10-alkyl, C2-10- alkenyl, or C2-10-alkynyl radical. C2-10-alkenyl radicals have at least one and preferably 1, 2, 3, or 4 C-C-double bonds and C2-10-alkynyl radicals at least one and preferably 1, 2, 3, or 4 C-C-triple bonds. Preference is given to C1-10-alkyl radicals selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3- methylbut-1-yl, 2-pentyl, 3-pentyl, sec-pentyl, neopentyl, 4-methylpent-1-yl, (3,3)- dimethylbut-1-yl, n-hexyl, n-heptyl, 2-heptyi, 3-heptyl, 4-heptyl, n-octyl, n-nonyl, 2- nonyl, 3-nonyl, 4-nonyl, 5-nonyl, and (2,6)-dimethylhept-4-yl, which can be optionally substituted by 1, 2, 3, 4, 5, 6, 7, 8, or 9 substituents independently selected from the group consisting of -O-phenyl, -O-C(= O)-CH3, -O-C(= O)-C2H5, -O-C(= O)-CH(CH3)2, -O-C(= O)-C(CH3)3, -C(= O)-O-CH3, -C(= O)-O-C2H5, -C(= O)-O-CH(CH3)2, -C(= O)- O-C(CH3)3, F, CI, Br, I, -CN, -NO2, -OH, -NH2, -SH, -O-CH3, -O-C2H5, -O-CH(CH3)2, - O-C(CH3)3) -S-CH3, -S-C2H5, -S-CH(CH3)2, -S-C(CH3)3, -NH-CH3, -NH-C2H5, -NH- C(CH3)3, -N(CH3)2, -N(C2H5)2, -N(CH3)-(C2H5), -OCF3, and -SCF3. In another preferred embodiment, C2-10 alkenyl radicals are selected from the group consisting of vinyl, 1-propenyl, 2-propenyl, 1-butenyl, 2-butenyl, 3-butenyl, 2-methyl- propene-1-yl, 3-methyl-but-2-en-1-yl, (3,3)-dimethyl-but-1-enyl, 2-methyl-butene-2-yl, 1-pentenyl, 2-pentenyl, 3-pentenyl, 4-pentenyl, 1-hexenyl, 1-heptenyl, and 1-octenyl, which can be optionally substituted by 1, 2, or 3 substituents independently selected from the group consisting of F, CI, Br, I, -CN, -NO2, -OH, -NH2, -SH, -O-CH3, -O- C2H5, -O-CH(CH3)2, -O-C(CH3)3, -S-CH3, -S-C2H5, -S-CH(CH3)2, -S-C(CH3)3, -NH- CH3, -NH-C2H5, -NH-C(CH3)3, -N(CH3)2, -N(C2H5)2, -N(CH3)-(C2H5), -OCF3, and - SCF3. Preference is also given to C2-10 alkynyl radicals selected from the group consisting of (3,3)-dimethyl-but-1-ynyl, 4-methyl-pent-1-ynyl, 1-hexynyl, ethynyl, 1-propynyl, 2- propynyl, 1-butynyl, 2-butynyl, 3-butynyl, 1-pentynyl, 2-pentynyl, 3-pentynyl, and 4- pentynyl, which can be optionally substituted by 1, 2, or 3 substituents independently selected from the group consisting of F, CI, Br, I, -CN, -NO2, -OH, -NH2, -SH, -O-CH3, -O-C2H5, -O-CH(CH3)2, -O-C(CH3)3, -S-CH3, -S-C2H5, -S-CH(CH3)2, -S-C(CH3)3, -NH- CH3, -NH-C2H5, -NH-C(CH3)3, -N(CH3)2, -N(C2H5)2, -N(CH3)(C2H5), -OCF3, and - SCF3. Particularly preferred optionally substituted C1-10 aliphatic radicals are selected from the group consisting of methyl, -CF3, -CHF2, -CH2F, -CF2CI, -CCI2F, -CCI3, -CBr3, - CH2-CN, -CH2-O-CH3, -CH2-O-CF3, -CH2-SF3, -CH2-NH2, -CH2-OH, -CH2-SH, -CH2- NH-CH3, -CH2-N(CH3)2, -CH2-N(C2H5)2, -CH2-N(CH3)-(C2H5), ethyl, -CF2-CH3, -CHF- CF2CI, -CF2-CFCI2, -CFCI-CF2CI, -CFCI-CFCI2, -CH2-CH2-NH2, -CH2-CH2-OH, -CH2- CH2-SH, -CH2-CH2-NH-CH3, -CH2-CH2-N(CH3)2, -CH2-CH2-N(C2H5)2, -CH2-CH2- N(CH3)-(C2H5), -CH2-CF3, -C2F5, -CH2-CCI3, -CH2-CBr3, -CH2-CH2-CN, n-propyl, - CH2-CH2-CH2-OH, -CH2-CH2-CH2-SH, -CH2-CH2-CH2-NH2, -CH2-CH2-CH2-NH-CH3, - CH2-CH2-CH2-N(CH3)2, -CH2-CH2-CH2-N(C2H5)2, -CH2-CH2-CH2-N(CH3)-(C2H5), - CH2-CH2-O-CH3, -CF2-CF2-CF3, -CF(CF3)2, isopropyl, -CH2-CH2-CH2-CN, -CH2-O- CH2-CH3, -CH2-CH2-SF3, -CH2-CH2-OCF3, -CH(CH3)-(O-CH3), -CH(CH3)-(S-CH3), n- butyl, -CF2-CF2-CF2-CF3, -CH2-CH2-CH2-CH2-CN, -CH2-CH2-CH2-CF3, -CH2-CH2- CH2-CH2-CF3, -CH2-O-C(= O)-CH3, -CH2-O-C(= O)-C2H5, -CH2-O-C(= O)-CH(CH3)2, - CH2-O-C(= O)-C(CH3)3, -CH2-C(= O)-O-CH3, -CH2-C(= O)-O-C2H5, -CH2-C(= O)-O- C(CH3)3, -CH2-CH2-O-CH3, -CH2-CH2-O-C2H5l -CH2-CH2-O-phenyl, -CH2-CH2-CH2- O-CH3, sec-butyl, isobutyl, tert-butyl, n-pentyl, sec-pentyl, neo-pentyl, n-hexyl, vinyl, 1-propenyl, 2-propenyl, 1-butenyl, 2-butenyl, 3-butenyl, 2-methyl-butene-2-yl, (1,1,2)- trifluoro-1 -butenyl, 1-pentenyl, 2-pentenyl, 3-pentenyl, 4-pentenyl, -CF= CF2, -CCI= CCI2, -CH2-CF= CF2, -CH2-CCI= CCI2, -C=C-I, -OC-, and -C=C-CI. If one or more of the aforementioned substituents stand for a (hetero)cycloaliphatic radical, which can be optionally condensed with a saturated or unsaturated, unsubstituted or at least monosubstituted monocyclic or polycyclic ring system, this can preferably be selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclopentenyl, cyclohexenyl, cycloheptenyl, imidazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, thiomorpholinyl, tetrahydropyranyl, oxetanyl, (1,2,3,6)- tetrahydropyridinyl, azepanyl, azocanyl, diazepanyl, dithiolanyl, (1,3,4,5)- tetrahydropyrido[4.3-b]indolyl, (3,4)-dihydro-1 H-isoquinolinyl, (1,3,4,9)- tetrahydro[b]carbolinyl, and (1,3)-thiazolidinyl. As examples of suitable (hetero)cycloaliphatic radicals, which can be unsubstituted or monosubstituted or polysubstituted and are condensed with a monocyclic or bicyclic ring system, there may be mentioned (4,5,6,7)-tetrahydroisoxazolo[5.4- c]pyridinyl, (2,3)-dihydro-1H-indenyl, 3-aza-bicyclo[3.1.1]heptyl, 3-aza- bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl, 8-aza-bicyclo[3.2.1]octyl, isoindolyl, indolyl, (1,2,3,4)-tetrahydroquinolinyl, (1,2,3,4)-tetrahydroisoquinolinyl, (2,3)-dihydro- 1 H-isoindolyl, (1,2,3,4)-tetrahydronaphthyl, (2,3)-dihydro-benzo[1.4]dioxinyl, benzo[1.3]dioxolyl, (1,4)-benzodioxanyl, (2,3)-dihydrothieno[3.4-b][1.4]dioxinyl, (3,4)- dihydro-2H-benzo[1.4]oxazinyl, octahydro-1 H-isoindolyl, and octahydro-pyrrolo[3.4- c]pyrrolyl. (Hetero)cycloaliphatic radicals can form, within the scope of the present invention, a spirocyclic radical with another (hetero)cycloaliphatic radical via a carbon atom common to both rings. As examples of suitable spirocyclic radicals there may be mentioned a 6-aza- spiro[2.5]octyl radical, 8-aza-spiro[4.5]decyl radical and a 1-oxa-2,8-diaza- spiro[4.5]dec-2-enyl radical. More preferably the (hetero)cycloaliphatic radicals can each be optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of oxo (= O), thioxo (= S), F, CI, Br, I, -CN, -CF3, -SF5, -OH, -O-CH3, -O-C2H5, -O- CH(CH3)2, -O-C(CH3)3, -NH2, -NO2, -O-CF3, -S-CF3, -SH, -S-CH3, -S-C2H5, -S- CH(CH3)2, -S-C(CH3)3, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, -C(= O)-CH3, -C(= O)-C2H5, -C(= O)-CH(CH3)2, -C(= O)-C(CH3)3, - C(= O)-0H, -C(= O)-O-CH3, -C(= O)-O-C2H5, -C(= O)-O-CH(CH3)2, -C(= O)-O- C(CH3)3, -NH-CH3, -NH-C2H5, -NH-C(CH3)3, -N(CH3)2, -N(C2H5)2, -N(CH3)-(C2H5), - CH2-OH, -CH2-CH2-OH, = CH2, -CH2-O-CH2-oxetanyl, -O-CH2-oxetanyl, -CH2- N(CH3)2, -CH2-N(C2H5)2, -CH2-NH-CH3, -CH2-NH-C2H5, -N-[C(= O)-C2H5]-phenyl, -N- [C(= O)-CH3]-phenyl, -CH2-O-CH3, -CH2-O-CH2-CH3, -NH-phenyl, -N(CH3)phenyl, - N(C2H5)phenyl, -N(C2H5)phenyl, -O-CH2-CH2-CH2-CH3, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, cyclohexyl, cyclopentyl, piperidinyl, pyrrolidinyl, -O-C(= O)-CH3, -O-C(= O)-C2H5, -O-C(= O)-C(CH3)3, - (CH2)pyridinyl, pyridinyl, -O-phenyl, -O-benzyl, phenyl, and benzyl, and the cyclic moiety of the radicals oxetanyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, -N-[C(= O)-C2H5]phenyl, -N-[C(= O)-CH3]phenyl, -NH-phenyl, - N(CH3)phenyl, -N(C2H5)phenyl, -(CH2)pyridinyl, pyridinyl, -O-phenyl, -O-benzyl, phenyl, and benzyl can each be substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of F, CI, Br, -OH, -CF3, -SF5, -CN, - NO2, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, -O-CH3, -O-C2H5, -O-CH(CH3)2, -O-C(CH3)3, -O-CF3, -S-CF3, phenyl, and -O-benzyl. If one or more of the aforementioned substituents stand for an aryl radical, this can preferably be selected from the group consisting of phenyl and naphthyl (1-naphthyl and 2-naphthyl). If one or more of the aforementioned substituents stand for a heteroaryl radical, this can preferably be selected from the group consisting of tetrazolyl, thiophenyl, furanyl, pyrrolyl, pyrazolyl, pyrazinyl, pyranyl, triazolyl, pyridinyl, imidazolyl, indolyl, isoindolyl, benzo[b]furanyl, benzo[b]thiophenyl, benzoxazolyl, benzisoxazolyl, thiazolyl, oxazolyl, isoxazolyl, pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl, quinoxalinyl, quinolinyl, and isoquinolinyl. As examples of suitable aryl and heteroaryl radicals, which can be unsubstituted or monosubstituted or polysubstituted and are condensed with a monocyclic or bicyclic ring system, there may be mentioned isoindolyl, indolyl, (1,2,3,4)- tetrahydroquinolinyl, (1,2,3,4)-tetrahydroisoquinolinyl, (2,3)-dihydro-1 H-isoindolyl, (1,2,3,4)-tetrahydronaphthyl, (2,3)-dihydrobenzo[1.4]dioxinyl, (2,3)-dihydrothieno[3.4- b][1.4]dioxinyl, benzo[1.3]dioxolyl, and (1,4)-benzodioxanyl. More preferably, the aryl radicals or heteroaryl radicals can each be optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of F, CI, Br, I, -CN, -CF3, -SF5, -OH, -O-CH3, -O-C2H5, -O-CH(CH3)2, -O- C(CH3)3, -NH2, -NO2, -O-CF3, -S-CF3, -SH, -S-CH3, -S-C2H5, -S-CH(CH3)2, -S- C(CH3)3, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n- pentyl, -C(= O)-OH, -C(= O)-O-CH3, -C(= O)-O-C2H5l -C(= O)-O-CH(CH3)2, -C(= O)- O-C(CH3)3, -NH-CH3, -NH-C2H5, -NH-C(CH3)3, -N(CH3)2, -N(C2H5)2, -N(CH3)-(C2H5), - NH-S(= O)2-CH3, -NH-S(= 02)-C2H5, -NH-S(= O)2-CH(CH3)2, -NH-C(= O)-O-CH3, - NH-C(= O)-O-C2H5, -NH-C(= O)-O-C(CH3)3, -C(= O)-H, -C(= O)-CH3, -C(= O)-C2H5, - C(= O)-CH(CH3)2, -C(= O)-C(CH3)3, -C(= O)-NH2, -C(= O)-NH-CH3, -C(= O)-NH- C2H5, -C(= O)-N(CH3)2, -C(= O)-N(C2H5)2, -O-phenyl, -O-benzyl, phenyl, and benzyl, and the cyclic moiety of the radicals -O-phenyl, -O-benzyl, phenyl, and benzyl can each be substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of F, CI, Br, -OH, -CF3, -SF5, -CN, -NO2, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, -O-CH3, -O-C2H5, -O-CH(CH3)2, -O- C(CH3)3, -O-CF3, -S-CF3, phenyl, and -O-benzyl. If a polycyclic ring system such as a bicyclic ring system is present, the different rings can independently exhibit a different degree of saturation, i.e. be saturated or unsaturated. A polycyclic ring system is preferably a bicyclic ring system. As examples of aryl radicals condensed with a monocyclic or polycyclic ring system mention may be made of (1,3)-benzodioxolyl and (1,4)-benzodioxanyl. If one or more of the aforementioned substituents have a monocyclic or polycyclic ring system, this can preferably be substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of oxo (= O), thioxo (= S), F, CI, Br, I, -CN, -CF3, -SF5, -OH, -O-CH3, -O-C2H5, -O-CH(CH3)2, -O-C(CH3)3, -NH2, -NO2, -O- CF3, -S-CF3, -SH, -S-CH3, -S-C2H5, -S-CH(CH3)2, -S-C(CH3)3, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, -C(= O)-OH, -C(= O)-O- CH3, -C(= O)-O-C2H5, -C(= O)-O-CH(CH3)2l -C(= O)-O-C(CH3)3, -NH-CH3, -NH-C2H5, -NH-C(CH3)3, -N(CH3)2, -N(C2H5)2, -N(CH3HC2H5), -NH-C(= O)-O-CH3, -NH-C(= O)- O-C2H5, -NH-C(= O)-O-C(CH3)3, -C(= O)-H, -C(= O)-CH3, -C(= O)-C2H5, -C(= O)- CH(CH3)2, -C(= O)-C(CH3)3, -C(= O)-NH2, -C(= O)-NH-CH3, -C(= O)-nH-C2H5, -C(= O)-N(CH3)2, -C(= O)-N(C2H5)2, -O-phenyl, -O-benzyl, phenyl, and benzyl, and the cyclic moiety of the radicals -O-phenyl, -O-benzyl, phenyl, and benzyl can each be substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of F, CI, Br, -OH, -CF3, -SF5, -CN, -NO2, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, -O-CH3, -O-C2H5, -O-CH(CH3)2, -O-C(CH3)3, - O-CF3l -S-CF3, phenyl, and -O-benzyl. If the radicals R41 and R42, together with the interconnecting nitrogen atom as ring member, form a heterocycloaliphatic radical which is substituted by 1, 2, 3, 4 or 5 radicals R57, these radicals R57 each have, independently of one another, one of the indicated meanings. Preference is given to compounds of the general formula la, in which D stands for N or CH; R1 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; - SR17; -S(=O)2-NR22R23; -S(=O)2-R27 or for a radical selected from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl; R2 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; - SR17; -S(=O)2-NR22R23; -S(=O)2-R27 or for a radical selected from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl; R3 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; - SR17; -S(=O)2-NR22R23; -S(=O)2-R27 or for a radical selected from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl; R4 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; - SR17; -S(=O)2-NR22R23; -S(=O)2-R27 or for a radical selected from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl; R5 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; - SR17; -S(=O)2-NR22R23; -S(=O)2-R27 or for a radical selected from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl; R8 stands for -SF5; -O-CF3; -CF3; tert-butyl; or -C(CH3)2(CH2OH); R13, R16, R17, R22, R23 and R27 each independently stand for a radical selected from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, -CF2-CH3, -CH2-CF3, - C2F5, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n- heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n- hexyl, (3,3)-dimethylbutyl and ethenyl; R42 stands for a radical selected from the group consisting of methyl, -CH2-O-CH3, ethyl, n-propyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-hexyl, (3,3)- dimethylbutyl, -CH2-CH2-O-CH3, -CH2-CH2-O-C2H5l and -CH2-CH2-CH2-O-CH3; or for a radical selected from the group consisting of 2,3-dihydro-1H-indenyl, cyclopropyl, oxetanyl, cyclobutyl, cyclopentyl, cyclohexyl, imidazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl, and thiomorpholinyl, each of which can be optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, and n-pentyl; in each case optionally in the form of one of the pure stereoisomers thereof, particularly enantiomers or diastereoisomers, or the racemates thereof or in the form of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in each case in the form of corresponding solvates. Special preference is given to compounds of the general formula la, in which D stands for N or CH; R1 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(=O)-R13; - OR16; SR17, -S(=O)2-NR22R23 or -(S=O)-R27; R2 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(=O)-R13; - OR16; SR17, -S(=O)2-NR22R23 or-(S=O)-R27; R3 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(=O)-R13; - OR16; SR17, -S(=O)2-NR22R23 or-(S=O)-R27; R4 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(=O)-R13; - OR16; SR17, -S(=O)2-NR22R23 or-(S=O)-R27; R5 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(=O)-R13; - OR16; SR17, -S(=O)2-NR22R23 or-(S=O)-R27; R8 stands for -SF5; -O-CF3; -CF3; tert-butyl; or -C(CH3)2(CH2OH); R13, R16, R17, R22, R23 and R27 each independently stand for a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl and ethenyl; R42 stands for a radical selected from the group consisting of methyl, ethyl, n- propyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-hexyl, and (3,3)-dimethylbutyl; or for a radical selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl, each of which can be optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, and n-pentyl; in each case optionally in the form of one of the pure stereoisomers thereof, particularly enantiomers or diastereoisomers, or the racemates thereof or in the form of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in each case in the form of corresponding solvates. Very particular preference is given to compounds of the general formula la, in which D stands for N or CH; R1 stands for H; F; CI; Br; or I; R2 stands for H; F; CI; Br; I; methyl; -OH; -NH2 or -OR16; R3 stands for H; F; CI; Br; I; -NO2; -OH; -NH2; -NH-C(= O)-R13, -OR16; SR17, - S(=O)2-NR22R23 or-(S=O)-R27; R4 stands for H; F; CI; Br; I; methyl, -OH; -NH2; or -OR16; R5 stands for H; F; CI; Br; or I; R8 stands for -SF5; -O-CF3; -CF3; tert-butyl; or -C(CH3)2(CH2OH); R13, R16, R17, R22, R23 and R27 each independently stand for a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl and ethenyl; R42 stands for a radical selected from the group consisting of methyl, ethyl, n- propyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-hexyl, and (3,3)- dimethylbutyl; or for a radical selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl, each of which can be optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, and n-pentyl; in each case optionally in the form of one of the pure stereoisomers thereof, particularly enantiomers or diastereoisomers, the racemates thereof or in the form of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in each case in the form of corresponding solvates. Preference is given to compounds of the general formula lb, in which D stands for N or CH; R1 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; - SR17; -S(=O)2-NR22R23; -(S=O)-R27 or for a radical selected from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl; R2 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; - SR17; -S(=O)2-NR22R23; -(S=O)-R27 or for a radical selected from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl; R3 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; - SR17; -S(=O)2-NR22R23; -(S=O)-R27 or for a radical selected from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl; R4 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; - SR17; -S(=O)2-NR22R23; -(S=O)-R27 or for a radical selected from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl; R5 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; - SR17; -S(=O)2-NR22R23; -(S=O)-R27 or for a radical selected from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl; R8 stands for -SF5; -O-CF3; -CF3; tert-butyl; or -C(CH3)2(CH2OH); R13, R16, R17, R22, R23 and R27 each independently stand for a radical selected from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, -CF2-CH3, -CH2-CF3, - C2F5, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n- heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n- hexyl, (3,3)-dimethylbutyl and ethenyl; R43 stands for a radical selected from the group consisting of methyl, -CH2-O-CH3, ethyl, n-propyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-hexyl, (3,3)- dimethylbutyl, -CH2-CH2-O-CH3, -CH2-CH2-O-C2H5, and -CH2-CH2-CH2-O-CH3; or for a radical selected from the group consisting of 2,3-dihydro-1 H-indenyl, cyclopropyl, oxetanyl, cyclobutyl, cyclopentyl, cyclohexyl, imidazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl, and thiomorpholinyl, each of which can be optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, and n-pentyl; in each case optionally in the form of one of the pure stereoisomers thereof, particularly enantiomers or diastereoisomers, or the racemates thereof or in the form of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in each case in the form of corresponding solvates. Special preference is given to compounds of the general formula lb, in which D stands for N or CH; R1 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(= O)-R13; - OR16; -SR17; -S(=O)2-NR22R23 or-(S=O)-R27; R2 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(= O)-R13; - OR16; -SR17; -S(=O)2-NR22R23 or -(S=O)-R27; R3 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(= O)-R13; - OR16; -SR17; -S(=O)2-NR22R23 or -(S=O)-R27; R4 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(= O)-R13; - OR16; -SR17; -S(=O)2-NR22R23 or-(S=O)-R27; R5 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(= O)-R13; - OR16; -SR17; -S(=O)2-NR22R23 or -(S=O)-R27; R8 stands for -SF5; -O-CF3; -CF3; tert-butyl; or -C(CH3)2(CH2OH); R13, R16, R17, R22, R23 and R27 each independently stand for a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl and ethenyl; R43 stands for a radical selected from the group consisting of methyl, ethyl, n- propyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-hexyl, and (3,3)- dimethylbutyl; or for a radical selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl, each of which can be optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, and n-pentyl; in each case optionally in the form of one of the pure stereoisomers thereof, particularly enantiomers or diastereoisomers, or the racemates thereof or in the form of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in each case in the form of corresponding solvates. Very particular preference is given to compounds of the general formula lb, in which D stands for N or CH; R1 stands for H; F; CI; Br; or I; R2 stands for H; F; CI; Br; I; methyl; -OH; -NH2; or -OR16; R3 stands for H; F; CI; Br; I; -NO2; -OH; -NH2; -NH-C(= O)-R13, -OR16; SR17; - S(=O)2-NR22R23 or -(S=O)-R27; R4 stands for H; F; CI; Br; I; methyl; -OH; -NH2; or -OR16; R5 stands for H; F; CI; Br; or I; R8 stands for -SF5; -O-CF3; -CF3; tert-butyl; or -C(CH3)2(CH2OH); R13, R16, R17, R22, R23 and R27 each independently stand for a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl and ethenyl; R43 stands for a radical selected from the group consisting of methyl, ethyl, n- propyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-hexyl, and (3,3)- dimethylbutyl; or for a radical selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl, each of which can be optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, and n-pentyl; in each case optionally in the form of one of the pure stereoisomers thereof, particularly enantiomers or diastereoisomers, or the racemates thereof or in the form of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in each case in the form of corresponding solvates. Preference is given to compounds of the general formula Ic, in which D stands for N or CH; R1 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; - SR17; -S(=O)2-NR22R23 or -(S=O)-R27 or for a radical selected from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl; R2 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; - SR17; -S(=O)2-NR22R23 or -(S=O)-R27 or for a radical selected from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl; R3 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; - SR17; -S(=O)2-NR22R23 or -(S=O)-R27 or for a radical selected from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl; R4 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; - SR17; -S(=O)2-NR22R23 or -(S=O)-R27 or for a radical selected from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl; R5 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; - SR17; -S(=O)2-NR22R23 or -(S=O)-R27 or for a radical selected from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl; R8 stands for -SF5; -O-CF3; -CF3; tert-butyl; or -C(CH3)2(CH2OH); R13, R16, R17, R22, R23 and R27 each independently stand for a radical selected from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, -CF2-CH3, -CH2-CF3, - C2F5, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n- heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n- hexyl, (3,3)-dimethylbutyl and ethenyl; R40 and R41 each independently stand for a radical selected from the group consisting of methyl, -CH2-O-CH3, ethyl, n-propyl, n-butyl, sec-butyl, isobutyl, tert- butyl, n-pentyl, 3-pentyl, n-hexyl, (3,3)-dimethylbutyl, -CH2-CH2-O-CH3, -CH2-CH2-O- C2H5, and -CH2-CH2-CH2-O-CH3; for a radical selected from the group consisting of 2,3-dihydro-1H-indenyl, cyclopropyl, oxetanyl, cyclobutyl, cyclopentyl, cyclohexyl, imidazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl, and thiomorpholinyl, each of which can be optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, and n-pentyl; or R40 and R41 form, together with the interconnecting nitrogen atom as ring member, a radical selected from the group consisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza- spiro[2.5]octyl, 3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl, 8-aza- bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl, azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl, (4,5,6,7)-tetrahydroisoxazolo[5.4-c]pyridinyl, pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, azepanyl, diazepanyl, and thiomorpholinyl, of which the heterocycloaliphatic moiety can in each case be unsubstituted or substituted by 1, 2, 3, 4, or 5 radicals R57; R57 stands for -NHR58, -NR59R60, or for an alkyl radical selected from the group consisting of-CF3, -CH2-CF3, methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, and isobutyl; R58, R59, and R60 each independently stand for -C(= O)-R61; for an alkyl radical selected from the group consisting of-CF3, -CH2-CF3, methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, and isobutyl; or for a radical selected from the group consisting of phenyl and naphthyl, and each radical can be bonded via a -(CH2)-, -(CH2)2- or -(CH2)3 group and/or can each be unsubstituted or optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of F, CI, Br, I, -CN, -CF3, -O-CH3, -O-C2H5, -O- CH(CH3)2, -O-C(CH3)3, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, and n-pentyl; and R61 stands for an alkyl radical selected from the group consisting of -CF3, - CH2-CF3, methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, and isobutyl; in each case optionally in the form of one of the pure stereoisomers thereof, particularly enantiomers or diastereoisomers, or the racemates thereof or in the form of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in each case in the form of corresponding solvates. Special preference is given to compounds of the general formula Ic, in which D stands for N or CH; R1 stands for H; F; CI; Br; I; methyl; ethyl; -NO2; -OH; -NH2; -NH-C(= O)-R13; - OR16; -SR17; -S(=O)2-NR22R23 or-(S=O)-R27; R2 stands for H; F; CI; Br; I; methyl; ethyl; -NO2; -OH; -NH2; -NH-C(= O)-R13; - OR16; -SR17; -S(=O)2-NR22R23 or -(S=O)-R27; R3 stands for H; F; CI; Br; I; methyl; ethyl; -NO2; -OH; -NH2; -NH-C(= O)-R13; - OR16; -SR17; -S(=O)2-NR22R23 or-(S=O)-R27; R4 stands for H; F; CI; Br; I; methyl; ethyl; -NO2; -OH; -NH2; -NH-C(= O)-R13; - OR16; -SR17; -S(=O)2-NR22R23 or -(S=O)-R27; R5 stands for H; F; CI; Br; I; methyl; ethyl; -NO2; -OH; -NH2; -NH-C(= O)-R13; - OR16; -SR17; -S(=O)2-NR22R23 or -(S=O)-R27; R8 stands for -SF5; -O-CF3; -CF3; tert-butyl; or -C(CH3)2(CH2OH); R13, R16, R17, R22, R23 and R27 each independently stand for a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl and ethenyl; R40 and R41 form, together with the interconnecting nitrogen atom as ring member, a radical selected from the group consisting of pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, and azepanyl, of which the heterocycloaliphatic moiety can in each case be unsubstituted or substituted by 1, 2, 3, 4, or 5 radicals R57; and R57 stands for an alkyl radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, and isobutyl; in each case optionally in the form of one of the pure stereoisomers thereof, particularly enantiomers or diastereoisomers, or the racemates thereof or in the form of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in each case in the form of corresponding solvates. Very particular preference is given to compounds of the general formula Ic, in which D stands for N or CH; R1 stands for H; F; CI; Br; or I; R2 stands for H; F; CI; Br; I; -OH; -NH2; or -OR16; R3 stands for H; F; CI; Br; I; -NO2; -OH; -NH2; -NH-C(= O)-R13, -OR16; -SR17; - S(=O)2-NR22R23 or -(S=O)-R27; R4 stands for H; F; CI; Br; I; methyl; -OH; -NH2; or -OR16; R5 stands for H; F; CI; Br; or I; R8 stands for -SF5; -O-CF3; -CF3; tert-butyl; or -C(CH3)2(CH2OH); R13, R16, R17, R22, R23 and R27 each independently stand for a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl and ethenyl; R40 and R41 form, together with the interconnecting nitrogen atom as ring member, a radical selected from the group consisting of pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, and azepanyl, of which the heterocycloaliphatic moiety can in each case be unsubstituted or substituted by 1, 2, 3, 4, or 5 radicals R57; and R57 stands for an alkyl radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, and isobutyl; in each case optionally in the form of one of the pure stereoisomers thereof, particularly enantiomers or diastereoisomers, or the racemates thereof or in the form of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in each case in the form of corresponding solvates. Even greater preference is given to compounds of the general formulas I, la, lb, and Ic selected from the group consisting of [1] 2-(4-Amino-3-fluorophenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide; [2] 2-(3,5-Dibromophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin- 3-yl)methyl)acetamide; [3] 2-(4-Amino-3-bromo-5-methoxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)acetamide; [4] 2-(3-Fluorophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-3- yl)methyl)acetamide; [5] 2-(2,4-Difluorophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin- 3-yl)methyl)acetamide; [6] 2-(2,6-Difluorophenyl)-N-((2-(4-fnethylpiperidin-1-yl)-6-(trifluoromethyl)pyridin- 3-yl)methyl)acetamide; [7] 2-(2,5-Difluorophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin- 3-yl)methyl)acetamide; [8] 2-(4-Fluorophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-3- yl)methyl)acetamide; [9] 2-(4-Hydroxy-3-methoxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide; [10] 2-(3,5-Difluorophenyl)-N-((2-(4-methylpiperidin-1 -yl)-6-(trifluoromethyl)pyridin- 3-yl)methyl)propanamide; [11] 2-(3,4-Difluorophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin- 3-yl)methyl)propanamide; [12] 2-(4-Fluorophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-3- yl)methyl)propanamide; [13] 2-(3-Fluorophenyl)-N-((2-(4-methylpiperidin-1 -yl)-6-(trifluoromethyl)pyridin-3- yl)methyl)propanamide; [14] 2-(3,4-Diaminophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin- 3-yl)methyl)propanamide; [15] N-(2-Butoxy-6-tert-butylpyridin-3-ylmethyl)-2-(3,4-diamino-phenyl)- propionamide; [16] N-((6-tert-Butyl-2-(4-methylpiperidin-1 -yl)pyridin-3-yl)methyl)-2-(3,4- diaminophenyl)propanamide; [17] N-((6-tert-Butyl-2-(cyclohexylthio)pyridin-3-yl)methyl)-2-(3,4- diaminophenyl)propanamide; [18] 2-(4-Acetamido-3-fluorophenyl)-N-((2-(4-methylpiperidin-1 -yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide; [19] 2-(3,5-Dibromo-4-hydroxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide; [20] 2-(4-Amino-3,5-dibromophenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide; [21] 2-(3-Bromo-4-hydroxy-5-methoxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)acetamide; [22] 2-(4-Amino-3,5-dibromophenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)acetamide; [23] 2-(3,5-Dibromo-4-hydroxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)acetamide; [24] 2-(3-Amino-4-hydroxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide; and [25] 2-(3,5-Dibromophenyl)-N-(4-methyl-6'-trifluoromethyl-3,4,5,6-tetrahydro-2H- [1,2']bipyridinyl-3'-ylmethyl)acetamide; [26] 2-(4-Amino-3,5-difluorophenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [27] 2-(3-Fluoro-5-hydroxy-4-nitrophenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [28] 2-(3-Chloro-4-(methylthio)phenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [29] 2-(3-Chloro-4-(methylsulfonyl)phenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [30] 2-(3-Fluoro-4-(methylthio)phenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [31] 2-(3-Fluoro-4-(methylsulfonyl)phenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [32] 2-(4-(N,N-Dimethylsulfamoyl)-3-fluorophenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [33] N-(2-Fluoro-4-(1-((2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-3- yl)methylamino)-1-oxopropane-2-yl)phenyl)acrylamide, [34] N-(2-Fluoro-6-iodo-4-(1-((2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-3- yl)methylamino)-1-oxopropane-2-yl)phenyl)acrylamide, [35] 2-(4-Methoxy-3,5-dimethylphenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [36] 2-(3,5-Difluoro-4-methoxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [37] 2-(4-Hydroxy-3,5-dimethylphenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [38] 2-(3,5-Difluoro-4-hydroxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, each optionally in the form of one of the pure stereoisomers thereof, particularly enantiomers or diastereoisomers thereof, the racemates thereof or in the form of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in an arbitrary mixing ratio, or each in the form of corresponding salts, or each in the form of corresponding solvates; Furthermore, preference may be given to compounds according to the invention of the general formulas I, la, lb and Ic, which in the FLIPR assay using CHO-K1 cells, which have been transfected with the human VR1 gene in a concentration below 2000 nM, preferably below 1000 nM, more preferably below 300 nM, even more preferably below 100 nM, still more preferably below 75 nM, \/ery preferably below 50 nM and most preferably below 10 nM, cause a 50 percent displacement of capsaicin present in a concentration of 100 nM. In the FLIPR assay, the Ca2+ influx is quantified with the aid of a Ca2+-sensitive dye (type Fluo-4, Molecular Probes Europe BV, Leiden, Netherlands) in a fluorescent imaging plate reader (FLIPR, Molecular Devices, Sunnyvale, USA), as described below. The invention further relates to a process for the production of compounds of the above general formula I, according to which at least one compound of the general formula II, in which R8, U, T, V, and W have the aforementioned meanings, m stands for 0, 1, 2, or 3, and R stands for hydrogen or for a linear or branched C1-6-alkyl radical, in a reaction medium, in the presence of at least one reducing agent, preferably in the presence of at least one reducing agent selected from the group consisting of sodium hydride, sodium, potassium hydride, lithium aluminum hydride, sodium tetrahydridoborate, and di(isobutyl)aluminum hydride is converted to at least one compound of the general formula III, in which R8, U, T, V, and W have the meanings stated above and m stands for 0, 1, 2, or 3, and this is optionally purified and/or isolated, and at least one compound of the general formula III is converted, in a reaction medium in the presence of diphenylphosphorylazide or in the presence of HN3, to at least one compound of the general formula IV, in which R8, U, T, V, and W have the meanings stated above and m stands for 0,1,2, or 3, and this is optionally purified and/or isolated, and at least one compound of the general formula IV is converted, in a reaction medium in the presence of at least one reducing agent, preferably in the presence of at least one reducing agent selected from the group consisting of sodium hydride, potassium hydride, lithium aluminum hydride, sodium tetrahydridoborate, and di(isobutyl)aluminum hydride, or in a reaction medium in the presence of a catalyst, preferably in the presence of a catalyst based on platinum or palladium, more preferably in the presence of palladium-on-charcoal, and in the presence of hydrogen or in the presence of hydrazine, or in a reaction medium in the presence of triphenylphosphine to at least one compound of the general formula V, in which R8, U, T, V, and W have the meanings stated above and m stands for 0, 1, 2, or 3, and this is optionally purified and/or isolated, or at least one compound of the general formula VI in which R8, U, T, V, and W have the meanings stated above and m stands for 0, 1,2, or 3, in a reaction medium is converted, in the presence of at least one catalyst, preferably in the presence of at least one catalyst based on palladium or platinum, more preferably in the presence of palladium-on-charcoal, under a blanket of hydrogen, optionally in the presence of at least one acid, preferably in the presence of hydrochloric acid, or in the presence of at least one reducing agent selected from the group consisting of BH3.S(CH3)2, lithium aluminum hydride, and sodium tetrahydridoborate, optionally in the presence of NiCl2, to form at least one compound of the general formula V, optionally in the form of a corresponding salt, preferably in the form of a corresponding hydrochloride, and this is optionally purified and/or isolated, and at least one compound of the general formula V is caused to react with at least one compound of the general formula VII, in which R1, R2, R3, R4, R5, R6, and R7 have the meanings stated above, in a reaction medium, optionally in the presence of at least one suitable coupling agent, optionally in the presence of at least one base, or with at least one compound of the general formula VIII, in which R1, R2, R3, R4, R5, R6, and R7 have the meanings stated above and LG stands for a leaving group, preferably for a chlorine or bromine atom, in a reaction medium, optionally in the presence of at least one base, to form at least one compound of the general formula I, in which T, U, V, W, R1, R2, R3, R4, R5, R6, R7, and R8 have the meanings stated above and n stands for 1, 2, 3, or 4, and this is optionally purified and/or isolated. The invention further relates to a process for the production of compounds of the above general formula I, according to which at least one compound of the general formula II, in which R8, U, T, V, and W have the meanings stated above, is caused to react with at least one compound of the general formula VII, in which R1, R2, R3, R4, R5, R6, and R7 have the meanings stated above, in a reaction medium, optionally in the presence of at least one suitable coupling agent, optionally in the presence of at least one base, or with at least one compound of the general formula VIII, in which R1, R2, R3, R4, R5, R6, and R7 have the meanings stated above and LG stands for a leaving group, preferably for a chlorine or bromine atom, in a reaction medium, optionally in the presence of at least one base, to form at least one compound of the general formula Im, in which T, U, V, W, R1, R2, R3, R4, R5, R6, R7, and R8 have the meanings stated above, and this is optionally purified and/or isolated. The reaction of compounds of the above general formulas V or X with carboxylic acids of the above general formula VII to form compounds of the above general formulas I or Im is carried out preferably in a reaction medium selected from the group consisting of diethyl ether, tetrahydrofuran, acetonitrile, methanol, ethanol, (1,2)-dichloroethane, dimethylformamide, dichloromethane and appropriate mixtures thereof, optionally in the presence of at least one coupling agent, preferably selected from the group consisting of 1-benzotriazolyloxy-tris(dimethylamino)phosphonium hexafluorophosphate (BOP), dicyclohexylcarbodiimide (DCC), N'-(3- dimethylaminopropyl)-N-ethylcarbodiimide (EDCI), diisoproylcarbodiimide, 1,1'- carbonyldiimidazole (CDI), N-[(dimethylamino)-1 H-1,2,3-triazolo[4.5-b]pyridino-1- ylmethylene]-N-methylmethanaminium hexafluorophosphate N-oxide (HATU), O- (benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate (HBTU), 0(benzotriazol-1-yl)-N,N,N',N-tetramethyluronium tetrafluoroborate (TBTU), N- hydroxybenzotriazole (HOBT), and 1-hydroxy-7-azabenzotriazole (HOAt), optionally in the presence of at least one organic base, preferably selected from the group consisting of triethylamine, pyridine, dimethylaminopyridine, N-methylmorpholine, and diisopropylethylamine, preferably at temperatures ranging from -70 °C to 100 °C. Alternatively, the reaction of compounds of the above general formulas V or X with carboxylic derivatives of the above general formula VIII, in which LG stands for a leaving group, preferably for a chlorine or bromine atom, to form compounds of the above general formulas Ih or Im is carried out in a reaction medium preferably selected from the group consisting of diethyl ether, tetrahydrofuran, acetonitrile, methanol, ethanol, dimethylformamide, dichloromethane and appropriate mixtures thereof, optionally in the presence of an organic or inorganic base, preferably selected from the group consisting of triethylamine, dimethylaminopyridine, pyridine, and diisopropylamine, at temperatures ranging from -70 °C to 100 °C. The compounds of the above formulas II, III, IV, V, VI, VII, X and VIII are all commercially available and can be obtained by conventional methods known to the person skilled in the art. The synthesis of compounds of the general formula VII is described in the paper "4- (Methylsulfonylamino)phenyl analogues as vanilloid antagonist showing excellent analgesic activity and the pharmaceutical compositions comprising the same" by J. W. Lee et al. [WO 2005/003084-A1]. The appropriate sections of this reference are hereby to be regarded as part of the disclosure. The conversions described above can each be carried out under usual conditions well-known to the person skilled in the art, for example, in respect of pressure or order of addition of the components. Optionally, the optimal procedure under the respective conditions can be determined by the person skilled in the art using simple preliminary tests. The intermediates and end products obtained by the aforementioned reactions can in each case be isolated and/or purified by conventional methods known to the person skilled in the art, if desired and/or necessary. Suitable purification techniques are, for example, extraction processes and chromatographic processes such as column chromatography or preparative chromatography. All of the process steps described above and the purification and/or isolation of intermediate or end products can be carried out partially or completely under a blanket of inert gas, preferably under a blanket of nitrogen. The substituted compounds according to the invention of the aforementioned general formulas I, la, lb and Ic, designated below simply as compounds of the general formula I, and corresponding stereoisomers can be isolated either in the form of the free bases thereof, the free acids thereof or in the form of corresponding salts, particularly physiologically compatible salts. The free bases of the respective substituted compounds according to the invention of the aforementioned general formula I and corresponding stereoisomers can, for example by reaction with an inorganic or organic acid, preferably with hydrochloric acid, hydrobromic acid, sulfuric acid, phosphoric acid, methanesulfonic acid, p- toluenesulfonic acid, carbonic acid, formic acid, acetic acid, oxalic acid, succinic acid, tartaric acid, mandelic acid, fumaric acid, lactic acid, citric acid, glutamic acid, or aspartic acid, be converted to the corresponding salts, preferably physiologically compatible salts. The free bases of the respective substituted compounds of the aforementioned general formula I and corresponding stereoisomers can be likewise caused to react with the free acid or a salt of a sugar substitute, such as saccharin, cyclamate, or acesulfam, to form the corresponding physiologically compatible salts. Similarly, the free acids of the substituted compounds of the aforementioned general formula I and corresponding stereoisomers can be caused to react with a suitable base to form the corresponding physiologically compatible salts. Mention may be made, for example, of the alkali-metal salts, alkaline earth metal salts, or ammonium salts [NHXR4-X]+ in which x is equal to 0, 1, 2, 3, or 4, and R stands for a linear or branched C1-4-alkyl radical. The substituted compounds according to the invention designated by the aforementioned general formula I and corresponding stereoisomers can optionally, like the corresponding acids, the corresponding bases or salts of these compounds, be obtained in the form of the solvates thereof, preferably in the form of the hydrates thereof, by conventional methods known to the person skilled in the art. If the substituted compounds according to the invention designated by the aforementioned general formula I are obtained, following production thereof, in the form of a mixture of the stereoisomers thereof, preferably in the form of the racemates thereof or other mixtures of the various enantiomers and/or diastereoisomers thereof, these compounds can be separated and, if desired, isolated by methods known to the person skilled in the art. Mention may be made, for example, of chromatographic separation methods, particularly liquid- chromatographic methods carried out under standard pressure or at elevated pressure, preferably MPLC and HPLC methods, and also methods of fractional crystallization. In particular, individual enantiomers can be separated from each other, e.g. diastereoisomeric salts formed by means of HPLC on chiral stationary phase or by means of crystallization with chiral acids, say, (+)-tartaric acid, (-)-tartaric acid, or (+)-10-camphorsulfonic acid. The substituted compounds according to the invention designated by the aforementioned general formula I and corresponding stereoisomers and in each case the corresponding acids, bases, salts, and solvates are toxicologically safe and are therefore suitable for use as pharmaceutically active substances in pharmaceuticals. The invention therefore further relates to a pharmaceutical containing at least one compound according to the invention of the above general formula I, each optionally in the form of one of the pure stereoisomers thereof, particularly enantiomers or diastereoisomers thereof, the racemates thereof or in the form of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in an arbitrary mixing ratio, or each in the form of a corresponding salt, or each in the form of a corresponding solvate, and optionally one or more pharmaceutically compatible adjuvants. These pharmaceuticals according to the invention are particularly suitable for vanilloid receptor 1-(VR1/TRPV1) regulation, preferably vanilloid receptor 1- (VR1/TRPV1) inhibition and/or vanilloid receptor 1-(VR1/TRPV1) stimulation. In another preferred embodiment, the pharmaceuticals according to the invention are suitable for prophylaxis and/or treatment of disorders or diseases that are at least partially mediated by vanilloid receptors 1. Preferably, the pharmaceutical according to the invention is suitable for treatment and/or prophylaxis of one or more disorders selected from the group consisting of pain selected from the group consisting of acute pain, chronic pain, neuropathic pain and visceral pain; arthralgia; hyperalgesia; allodynia; causalgia; migraine; states of depression; nervous disorders; neurotraumas; neurodegenerative disorders, preferably selected from the group consisting of multiple sclerosis, Morbus Alzheimer, Morbus Parkinson, and Morbus Huntington; cognitive dysfunctions, preferably cognitive deficiency states, more preferably memory defects; epilepsy; respiratory tract diseases, preferably selected from the group consisting of asthma, bronchitis, and pneumonia; coughing; urinary incontinence; an overactive bladder (OAB); disorders and/or injuries of the gastrointestinal tract; duodenal ulcers; gastric ulcers; colitis syndrome; apoplectic strokes; eye irritations; cutaneous irritations; neurotic skin conditions; allergic skin diseases; psiorasis; vitiligo; Herpes simplex; inflammations, preferably inflammation of the intestine, the eyes, the bladder, the skin, or the nasal mucosa; diarrhea; pruritus; osteoporosis; arthritis; osteo-arthritis; rheumatic disorders; food intake disorders, preferably selected from the group consisting of bulimia, cachexia, anorexia, and obesity; medicine addiction; medicine abuse; withdrawal phenomena following medicine addiction; tolerance development to pharmaceuticals, particularly to natural or synthetic opioids; drug addiction; drug abuse; withdrawal phenomena following drug addiction; alcohol addiction; alcohol abuse and withdrawal phenomena following alcohol addiction; for diuresis; for antinatriuresis; for affection of the cardiovascular system; for vigilance enhancement; for treatment of wounds and/or burning; for treatment of severed nerves; for libido enhancement; for modulation of movement activity; for anxiolysis; for local anesthesia and/or for inhibition of undesirable side effects, preferably selected from the group consisting of hyperthermia, hypertension, and bronchial constriction, as caused by administration of vanilloid receptor 1 (VR1/TRPV1 receptor) agonists, preferably selected from the group consisting of capsaicin, resiniferatoxin, olvanil, arvanil, SDZ-249665, SDZ-249482, nuvanil, and capsavanil. The pharmaceutical according to the invention is particularly preferably suitable for treatment and/or prophylaxis of one or more disorders selected from the group consisting of pain, preferably pain selected from the group consisting of acute pain, chronic pain, neuropathic pain, and visceral pain; arthralgia; migraine; states of depression; neurodegenerative disorders, preferably selected from the group consisting of multiple sclerosis, Morbus Alzheimer, Morbus Parkinson, and Morbus Huntington; cognitive dysfunctions, preferably cognitive deficiency states, more preferably memory defects; inflammation, preferably inflammation of the intestine, the eyes, the bladder, the skin or the nasal mucosa; urinary incontinence; an overactive bladder (OAB); medicine addiction; medicine abuse; withdrawal phenomena following medicine addiction; tolerance development to pharmaceuticals, preferably tolerance development to natural or synthetic opioids; drug addiction; drug abuse; withdrawal phenomena following drug addiction; alcohol addiction; alcohol abuse and withdrawal phenomena following alcohol addiction. The pharmaceutical according to the invention is most preferably suitable for treatment and/or prophylaxis of pain, preferably pain selected from the group consisting of acute pain, chronic pain, neuropathic pain, and visceral pain, and/or urinary incontinence. The invention further relates to the use of at least one compound according to the invention and optionally one or more pharmaceutically compatible adjuvants for the production of a pharmaceutical for vanilloid receptor 1-(VR1/TRPV1) regulation, preferably vanilloid receptor 1-(VR1/TRPV1) inhibition and/or vanilloid receptor 1- (VR1/TRPV1) stimulation. Preference is given to the use of at least one substituted compound according to the invention and optionally one or more pharmaceutically compatible adjuvants for the production of a pharmaceutical for the prophylaxis and/or treatment of disorders or diseases which are at least partially mediated by vanilloid receptors 1. Particular preference is given to the use of at least one compound according to the invention and optionally one or more pharmaceutically compatible adjuvants for the production of a pharmaceutical for treatment and/or prophylaxis of one or more disorders selected from the group consisting of pain, preferably of pain selected from the group consisting of acute pain, chronic pain, neuropathic pain, visceral pain, and arthralgia. Particular preference is given to the use at least one compound according to the invention and optionally one or more pharmaceutically compatible adjuvants for the production of a pharmaceutical for treatment and/or prophylaxis of one or more disorders selected from the group consisting of hyperalgesia; allodynia; causalgia; migraine; states of depression; nervous disorders; neurotraumas; neurodegenerative disorders, preferably selected from the group consisting of multiple sclerosis, Morbus Alzheimer, Morbus Parkinson, and Morbus Huntington; cognitive dysfunctions, preferably cognitive deficiency states, more preferably memory defects; epilepsy; respiratory tract diseases, preferably selected from the group consisting of asthma, bronchitis, and pneumonia; coughing; urinary incontinence; an overactive bladder (OAB); disorders and/or injuries of the gastrointestinal tract; duodenal ulcers; gastric ulcers; colitis syndrome; apoplectic strokes; eye irritations; cutaneous irritations; neurotic skin conditions; allergic skin diseases; psiorasis; vitiligo; Herpes simplex; inflammation, preferably inflammation of the intestine, the eyes, the bladder, the skin, or the nasal mucosa; diarrhea; pruritus; osteoporosis; arthritis; osteo-arthritis; rheumatic disorders; food intake disorders, preferably selected from the group consisting of bulimia, cachexia, anorexia, and obesity; medicine addiction; medicine abuse; withdrawal phenomena following medicine addiction; tolerance development to pharmaceuticals, preferably to natural or synthetic opioids; drug addiction; drug abuse; withdrawal phenomena following drug addiction; alcohol addiction; alcohol abuse and withdrawal phenomena following alcohol addiction; for diuresis; for antinatriuresis; for affection of the cardiovascular system; for vigilance enhancement; for treatment of wounds and/or burning; for treatment of severed nerves; for libido enhancement; for modulation of movement activity; for anxiolysis; for local anesthesia and/or for inhibition of undesirable side effects, preferably selected from the group consisting of hyperthermia, hypertension, and bronchial constriction, as caused by administration of vanilloid receptor 1 (VR1/TRPV1 receptor) agonists, preferably selected from the group consisting of capsaicin, resiniferatoxin, olvanil, arvanil, SDZ-249665, SDZ-249482, nuvanil, and capsavanil. Very particular preference is given to the use of at least one substituted compound according to the invention and optionally one or more pharmaceutically compatible adjuvants for the production of a pharmaceutical for treatment and/or prophylaxis of one or more disorders selected from the group consisting of pain, preferably pain selected from the group consisting of acute pain, chronic pain, neuropathic pain, and visceral pain; arthralgia; migraine; states of depression; neurodegenerative disorders, preferably selected from the group consisting of multiple sclerosis, Morbus Alzheimer, Morbus Parkinson, and Morbus Huntington; cognitive dysfunctions, preferably cognitive deficiency states, more preferably memory defects; inflammation, preferably inflammation of the intestine, the eyes, the bladder, the skin, or the nasal mucosa; urinary incontinence; an overactive bladder (OAB); medicine addiction; medicine abuse; withdrawal phenomena following medicine addiction; tolerance development to pharmaceuticals, preferably tolerance development to natural or synthetic opioids, drug addiction; drug abuse; withdrawal phenomena following drug addiction; alcohol addiction; alcohol abuse and withdrawal phenomena following alcohol addiction. Even more preference is given to the use of at least one substituted compound according to the invention and optionally one or more pharmaceutically compatible adjuvants for the production of a pharmaceutical for treatment and/or prophylaxis of pain, preferably selected from the group consisting of acute pain, chronic pain, neuropathic pain, and visceral pain, and/or urinary incontinence. The pharmaceutical according to the invention is suitable for administration to adults and children including infants and babies. The pharmaceutical according to the invention can exist as a liquid, semisolid, or solid pharmaceutical dosage form, for example, in the form of injection fluids, drops, juices, syrups, sprays, suspensions, tablets, patches, capsules, plasters, suppositories, ointments, creams, lotions, gels, emulsions, or aerosols, or in a multiparticular form, for example, in the form of pellets or granules, optionally compressed to tablets, filled into in capsules, or suspended in a liquid, and can be administered as such. In addition to at least one substituted compound of the above general formula I, optionally in the form of a pure stereoisomer thereof, particularly an enantiomer or diastereoisomer, the racemate thereof or in the form of mixtures of the stereoisomers, particularly the enantiomers or diastereoisomers, in an arbitrary mixing ratio, or optionally in the form of a corresponding salt or each in the form of a corresponding solvate, the pharmaceutical according to the invention usually contains further physiologically compatible pharmaceutical adjuvants, which, for example, can be selected from the group consisting of vehicles, fillers, solvents, diluents, surfactants, dyes, preservatives, blasting agents, slip agents, lubricants, flavors, and binding agents. The selection of the physiologically compatible adjuvants and the amount thereof to be used depends on whether the pharmaceutical is to be applied orally, subcutaneously, parenterally, intravenously, intraperitoneally, intradermally, intramuscularly, intranasally, buccally, rectally or locally, e.g. to infected parts of the skin, the mucous membrane, or the eyes. Preparations suitable for oral administration are preferably in the form of tablets, dragees, capsules, granules, pellets, drops, juices, and syrups, and preparations suitable for parenteral, topical and inhalative administration are solutions, suspensions, readily reconstitutable dry preparations, and sprays. The substituted compounds according to the invention used in the pharmaceutical according to the invention in a depot in dissolved form or in a plaster, optionally with the addition of skin penetration-enhancing agents, are suitable percutaneous administration forms. Formulations for oral or percutaneous application may be such as to effect delayed release of the respective substituted compound according to the invention. The production of the pharmaceutical according to the invention is effected by conventional means, devices, methods, and processes, as are known in the prior art, such as are described, for example, in "Remington's Pharmaceutical Sciences", Editor A.R. Gennaro, 17th Edition, Mack Publishing Company, Easton, Pa, 1985, particularly in Section 8, Chapters 76 to 93. The corresponding description is incorporated herein by reference and is to be regarded as part of the disclosure. The amount of the respective substituted compounds according to the invention of the above general formula I to be administered to the patients can vary and is dependent, for example, on the weight or age of the patient and also on the method of administration, the indication, and the severity of the disorder. Usually from 0.001 to 100 mg/kg, preferably from 0.05 to 75 mg/kg and more preferably from 0.05 to 50 mg/kg, of body weight of the patient of at least one such compound according to the invention are administered. Pharmacological methods: I. Functional investigation on the vanilloid receptor 1 (VRI/TRPV1 receptor) The agonistic or antagonistic action of the substances to be investigated on the vanilloid receptor 1 (VR1/TRPV1) of the species rat can be determined using the following assay. According to this assay, the Ca2+ influx through the receptor channel is quantified with the aid of a Ca2+-sensitive dye (Type Fluo-4, Molecular Probes Europe BV, Leiden Netherlands) in a fluorescent imaging plate reader (FLIPR, Molecular Devices, Sunnyvale, USA). Method: Complete medium: 50 mL of HAMS F12 Nutrient Mixture (Gibco Invitrogen GmbH, Karlsruhe, Germany) with 10% by volume of FCS (fetal calf serum, Gibco Invitrogen GmbH, Karlsruhe, Germany, heat-inactivated); 2mM of L-glutamine (Sigma, Munich, Germany); 1% by weight of AA solution (antibiotics/antimycotics solution, PAA, Pasching, Austria) and 25 ng/mL of Medium NGF (2.5 S, Gibco Invitrogen GmbH, Karlsruhe, Germany) Cell culture plate: Poly-D-lysine-coated, black 96-well plates with a clear bottom (96- well black/clear plate, BD Biosciences, Heidelberg, Germany) are additionally coated with laminin (Gibco Invitrogen GmbH, Karlsruhe, Germany) by diluting laminin to a concentration of 100 µg/mL with PBS (Ca-Mg-free PBS, Gibco Invitrogen GmbH, Karlsruhe, Germany). Aliquots having a concentration of 100 µg/mL of laminin are taken and stored at -20 °C. The aliquots are diluted with PBS in the ratio 1:10 to 10 µg/mL of laminin and in each case 50 uL of the solution is pipeted into a well of the cell culture plate. The cell culture plates are incubated at 37 °C for at least two hours, the supernatant solution is aspirated and the wells are in each case washed twice with PBS. The coated cell culture plates are stored with supernatant PBS and this is removed only directly before the addition of the cells. Preparation of the cells: The vertebral column is removed from decapitated rats and this is laid directly in a cold, i.e. ice bath-surrounded, HBSS buffer (Hank's buffered saline solution, Gibco Invitrogen GmbH, Karlsruhe, Germany) and 1% by volume of an AA solution (antibiotics/antimycotics solution, PAA, Pasching, Austria) is added. The vertebral column is cut in two, longitudinally, and the vertebral canal is removed together with fascias. Subsequently, the dorsal root ganglia (DRGs) are removed and in turn stored in cold HBSS buffer to which 1% by volume of an AA solution has been added. The DRGs completely freed from blood residues and spinal nerves are in each case transferred to 500 µL of cold collagenase Type 2 (PAA, Pasching, Austria) and incubated at 37 °C for 35 minutes. After the addition of 2.5% by volume of trypsin (PAA, Pasching, Austria), the preparation is incubated at 37 °C for a further 10 minutes. On completion of incubation, the enzyme solution is carefully pipeted off and 500 uL of complete medium are added to the DRGs in each case. The DRGs are in each case repeatedly suspended, drawn through No. 1, No. 12, and No. 16 needles by means of a syringe and transferred to 50 mL Falcon tubes and these are filled to 15 mL with complete medium. The contents of each Falcon tube are in each case filtered through a 70 µm Falcon filter insert and centrifuged at 1200 rpm and RT for 10 minutes. The resulting pellet is in each case taken up in 250 µL of complete medium and the cell count is determined. The number of cells in the suspension is adjusted to 3 x 105 per mL and in each case 150 µL of this suspension are added to a well of the cell culture plates coated as described above. The plates are allowed to stand at 37 °C, 5% by volume of CO2 and 95% relative humidity for two to three days in an incubator. Subsequently, the cells are loaded with 2 µM of Fluo-4 and 0.01% by volume of Pluronic F127 (Molecular Probes Europe BV, Leiden Netherlands) in HBSS buffer (Hank's buffered saline solution, Gibco Invitrogen GmbH, Karlsruhe, Germany) at 37°C for 30 min, washed 3 times with HBSS buffer and, after a further incubation of 15 minutes at RT, employed in the FLIPR assay for Ca2+ measurement. The Ca2+- dependent fluorescence is measured before and after addition of substances (λex = 488 nm, λem = 540 nm). Quantification is carried out by measuring the highest fluorescence intensity (FC, fluorescence counts) over time. FLIPR assay: The FLIPR protocol consists of two substance additions. Initially, the compounds to be tested (10 µM) are pipeted onto the cells and the Ca2+ influx is compared with the control (capsaicin 10 µM). Information is gained therefrom in percentage activation relative to the Ca2+ signal after addition of 10 µM of capsaicin (CP). After incubation for 5 minutes, 100 nM of capsaicin are applied and the influx of Ca2+ is likewise determined. Desensitizing agonists and antagonists lead to suppression of the Ca2+ influx. The percentage inhibition is calculated in comparison with the maximum inhibition achieved with 10 µM of capsaicin. Triple determinations (n=3) are carried out and these are repeated in at least 3 independent experiments (N=4). Based on the percentage displacement effected by different concentrations of the compounds of the general formula I to be tested, IC50 inhibition concentrations that cause 50 percent displacement of capsaicin are calculated. Conversion using the Cheng Prusoff equation gave Ki values for the test substances (Cheng, Prusoff; Bioch. Pharmacol. 22, 3099-3108, 1973). II. Functional investigations on the vanilloid receptor (VR1) The agonistic or antagonistic action of the substances to be examined on the vanilloid receptor (VR1) can also be determined by the following assay. According to this assay, the Ca2+ influx through the canal is quantified with the aid of a Ca2+- sensitive dye (type Fluo-4, Molecular Probes, Europe BV, Leiden, Netherlands) in a fluorescent imaging plate reader (FLIPR, Molecular Devices, Sunnyvale, USA). Method: Chinese hamster ovary cells (CHO-K1 cells, European Collection of Cell Cultures (ECACC) UK) are stably transfected with the VR1 gene. For carrying out functional investigations, these cells are plated on poly-D-lysine-coated, black 96-well plates with a clear bottom (BD Biosciences, Heidelberg, Germany) in a density of 25,000 cells/well. The cells are incubated overnight at 37 °C and 5% CO2 in a culture medium (Nutrient Mixture 'am's F12, 10% by volume of FCS (fetal calf serum), 18 µg/mL of L-proline). On the following day the cells are incubated with Fluo-4 (Fluo- 4 2 µM, Pluronic F127 0.01 by volume, Molecular Probes in HBSS (Hank's buffered saline solution), Gibco Invitrogen GmbH, Karlsruhe, Germany) for 30 minutes at 37 °C. The plates are then washed 3 times with HBSS buffer and, after another incubation over a period of 15 minutes at RT, are used in the FLIPR for Ca2+ measurement. The Ca2+-dependent fluorescence is measured prior to and following the addition of the substances being examined (wavelength λex = 488 nm, λem = 540 nm). Quantification is carried out by measuring the highest fluorescence intensity (FC, fluorescence counts) over time. FLIPR assay: The FLIPR protocol consists of two substance additions. First of all, the substances to be tested (10 µM) are pipeted onto the cells and the Ca2+ influx is compared with the control (capsaicin 10 µM) (percentage activation based on the Ca2+ signal following addition of 10 µM of capsaicin). Following incubation over a period of 5 minutes 100 nM of capsaicin are applied and the influx of Ca2+ is likewise determined. Desensitizing agonists and antagonists led to a suppression of the Ca2+ influx. The percentage inhibition compared with the maximum inhibition achieved with 10 µM of capsaicin is calculated. Based on the percentage displacement effected by different concentrations of the compounds of the general formula I to be tested, IC50 inhibition concentrations that cause 50 percent displacement of capsaicin are calculated. Conversion using the Cheng Prusoff equation gave Ki values for the test substances (Cheng, Prusoff; Bioch. Pharmacol. 22, 3099-3108, 1973). III. Formalin test on mice The investigation for the determination of the antinociceptive action of the compounds according to the invention is carried out in the formalin test on male mice (NMRI, of 20 to 30 g body weight, Iffa, Credo, Belgium). In the formalin test, the first (early) phase (0 to 15 minutes after the formalin injection) and the second (late) phase (15 to 60 minutes after the formalin injection) are distinguished according to D. Dubuisson et al., Pain 1977, 4, 161-174. The early phase, as a direct reaction to the formalin injection, is a model of acute pain, whereas the late phase is regarded as a model of persistent (chronic) pain (T.J. Coderre et al., Pain 1993, 52, 259-285). The appropriate literature references are incorporated herein by reference and are to be regarded as part of the disclosure. The compounds according to the invention are examined in the second phase of the formalin test, in order to obtain information concerning a substance's action on chronic/inflammatory pain. The point in time of administration of the compounds according to the invention before the formalin injection is selected according to the method of administration of the compounds according to the invention. Intravenous administration of 10 mg/kg of body weight of the test substances is carried out 5 minutes before the formalin injection. This is carried out by a single subcutaneous formalin injection (20 µL, 1% strength aqueous solution) into the dorsal side of the right hind paw so that in the case of free-moving experimental animals a nociceptive reaction is induced which is manifested by marked licking and biting of the relevant paw. The nociceptive behavior is then continuously registered during an investigation period of three minutes in the second (late) phase of the formalin test (21 to 24 minutes after the formalin injection) by observation of the animals. Quantification of the pain behavior is carried out by summating the seconds during which the animals exhibit licking and biting of the relevant paw during the investigation period. In each case, comparison is carried out with control animals, which receive, instead of the compounds according to the invention, a vehicle (0.9% strength aqueous sodium chloride solution) prior to formalin administration. Based on the quantification of the pain behavior, the substance's action in the formalin test is determined as the degree of change compared with the corresponding control in percent. Following injection of the substances having an antinociceptive action in the formalin test, the aforementioned behavioral patterns of the animals, i.e. licking and biting, decrease or cease. IV. Test for analgesic effectiveness in the writhing test Investigation of the compounds of the general formula I according to the invention for analgetic effectiveness was carried out based on phenylquinone-induced writhing in mice, modified in accordance with I.e. Hendershot and J. Forsaith (1959) J. Pharmacol. Exp. Ther. 125, 237-240. The corresponding literature reference is incorporated herein by reference and is to be regarded as part of the disclosure. For this purpose, male NMRI mice having a weight of from 25 to 30 g were used. Groups of 10 animals per dose of the test compound received by intraperitoneal administration, 10 minutes after intravenous administration of the compounds to be tested, 0.3 mL/mouse of a 0.02% strength aqueous solution of phenylquinone (phenylbenzoquinone, Sigma, Deisenhofen, Germany and produced by adding to the solution 5% by weight of ethanol and storing it in a water bath at 45 °C). The animals were placed individually in observation cages. With the aid of a pushbutton counter, the number of pain-induced stretching movements (so-called writhing reactions - straightening of the body with stretching of the rear extremities) was counted over a period of from 5 to 20 minutes following the administration of the phenylquinone. The control was provided by animals receiving only physiological saline. All of the compounds were tested using the standard dosage of 10 mg/kg. V. Hypothermia assay in mice Description of the method: The hypothermia assay was carried out on male NMRI mice (weight 25-35 gram, breeder IFFA CREDO, Brussels, Belgium). The animals were kept under standardized conditions: light/dark rhythm (from 6:00 to 18:00 hours light phase; from 18:00 to 6:00 hours dark phase), RT 19-22 °C, relative air humidity 35-70 %, 15 air changes per hour, air movement (ssniff R/M-Haltung, ssniff Spezialdiaeten GmbH, Soest, Germany) and tap water. Water and feed were withdrawn during the experiment. All animals were used only once during the experiment. The animals had an acclimatization period of at least 5 days. Acute administration of capsaicin (VR-1 agonist) leads to a drop in the core temperature of the body in rats and mice due to stimulation of heat sensors. Only specifically effective VR-1 receptor antagonists can antagonize the capsaicin-induced hypothermia. By contrast, hypothermia induced by morphine is not antagonized by VR-1 antagonists. This model is therefore suitable for identifying substances with VR- 1 antagonistic properties via their effect on body temperature. Measurement of the core temperature is carried out using a digital thermometer (Thermalert TH-5, physitemp, Clifton NJ, USA). The sensing element is inserted into the rectum of the animals. To give an individual basic value for each animal, the body temperature is measured twice at an interval of approximately half an hour. One group of animals (n = 6 to 10) then receives an intraperitoneal (i.p.) application of capsaicin 3 mg/kg and vehicle (control group). Another group of animals receives the substance to be tested (i.v. or p.o.) and additionally capsaicin (3 mg/kg) i.p. The administration of the test substance is carried out i.v. 10 min, or p.o 15 minutes, prior to capsaicin. The body temperature is then measured 7.5/15 and 30 min following capsaicin (i.v. + i.p.) or 15/30/60/90/120 min (p.o. + i.p.) following capsaicin. In addition, one group of animals is treated with the test substance only and one group with vehicle only. The evaluation or representation of the measured values as mean +/- SEM of the absolute values is presented as a graphical representation. The antagonistic action is calculated as the percentage reduction of the capsaicin-induced hypothermia. VI. Neuropathic pain in mice The investigation on effectiveness on neuropathic pain was examined using the Bennett Model (chronic constriction injury; Bennett und Xie, 1988, Pain 33:87-107). Three loose ligatures are tied around the right ischiadic nerve of Ketavet/Rompun- anesthetized NMRI mice weighing 16-18 g. The animals develop hypersensitivity of the nervate paw caused by the damaged nerve, which hypersensitivity is quantified, following a recovery phase of one week, over a period of approximately three weeks by means of a cold metal plate (temperature 4 °C) (cold allodynia). The animals are observed on this plate over a period of 2 min, and the withdrawal reactions of the damaged paw are counted. Based on the pre-value prior to administration of substance, the substance's action over a certain period of time is determined at various points in time (e.g., 15, 30, 45, or 60 min following administration) and the resultant area under the curve (AUC) and/or the inhibition of cold allodynia at the individual measuring points was/were expressed as percentage action relative to the vehicle control (AUC) or to the starting value (individual measuring points). The group size is n= 10, the significance of an anti-allodynic action (= p with the aid of an analysis of variance with repeated measurement and Bonferroni post hoc analysis. The invention is described below with reference to some examples. These explanations are by way of example only and do not restrict the general inventive concept. Examples: The yields of the compounds produced were not optimized. All temperatures are uncorrected. The statement "equivalents" denotes mol equivalents, "RT" room temperature, "M" and "N" are concentrations in mol/L, "aq." aqueous, "sat." saturated, "soln." solution, Further abbreviations: AcOH acetic acid DCM dichloromethane DMF N,N-dimethylformamide EDCI N-ethyl-N'-(3-dimethylaminopropyl)carbodiimide hydrochloride EA ethyl acetate H2O water HOBt N-hydroxybenzotriazole MeOH methanol THF tetrahydrofuran The chemicals and solvents used were obtained commercially from the usual suppliers (Acros, Avocado, Aldrich, Bachem, Fluka, Lancaster, Maybridge, Merck, Sigma, TCI, Oakwood etc.) or synthesized by usual methods known to the person skilled in the art. The stationary phase used for column chromatography was silica gel 60 (0.0-0 - 0.063 mm) supplied by E. Merck, Darmstadt. The thin-layer chromatographic analyses were carried out using preformed HPTLC plates, Silica Gel 60 F 254, supplied by E. Merck, Darmstadt. The mixing ratios of solvents, mobile solvents, or for chromatographic analyses are always stated in vol/vo!. Analysis was carried out by mass spectroscopy and NMR. 1. General instructions for the preparation of amines of the general formula V- A. Preparation of amines of the general formula V-A is carried out as illustrated by the following scheme 1. Stage 1: Preparation of nitriles of the general formula Vl-B Method A: Compounds of the general formula Vl-A (1 equivalent), in which R8, U, T, and V have the meanings stated above and m stands for 0,1,2, or 3, are stirred with an amine of the general formula HNR40R41 (6 equivalents) over a period of 48 hours at RT. To the reaction mixture there is added 1N hydrochloric acid, and the mixture is extracted with EA a number of times. The aqueous phase is saturated with NaCI and then again extracted with EA. The combined organic phases are washed with 1N hydrochloric acid and with sat. aq. NaCI soln., dried over MgSO4, and the solvent is removed in vacuo. The following compound was obtained by method A: 6'-tert-Butyl-4-methyl-3,4,5,6-tetrahydro-2H-[1,2']bipyridinyl-3'-carbonitrile 1H-NMR(CDCI3) δ 7.65 (d, 1H, J = 7.9 Hz, Ar), 6.70 (d, 1H, J = 8.0 Hz, Ar), 4.45 (m, 2H, piperidine), 2.98 (m, 2H, piperidine), 1.75-1.24 (m, 5H, piperidine), 1.29 (s, 9H, C(CH3)3), 0.98 (d, 3H, J = 5.9 Hz, CHCH3) IR 2956, 2213, 1583, 1550, 1452, 1230, 965 crrT1 Method B: Compounds of the general formula Vl-A (1 equivalent), in which R8, U, T, and V have the meanings stated above and m stands for 0,1,2, or 3, are stirred with an amine of the general formula HNR40R41 (2 equivalents) and DBU [1.8-diaza- bicyclo[5.4.0]undec-7-ene] (2 equivalents) in acetonitrile (7 mL per mmol of the compound of formula Vl-A) over a period of 12 hours at RT. The reaction mixture is extracted with EA a number of times. The combined organic phases are washed with sat. aq. NaCI solution, dried over MgSO4, and the solvent is removed in vacuo. The residue is purified in each case by column chromatography (SiO2, various mixtures of hexane/EA). The following compound was produced by method B. 6-(Trifluoromethyl)-2-(4-methylpiperidin-1-yl)pyridine-3-carbonitrile 1H NMR (300 M Hz, CDCI3) δ 7.87 (d, 1 h, J = 7.8 Hz), 6.95 (d, 1 h, J = 7.8 Hz), 4.53 (m, 2 H), 3.05 (m, 2 H), 1.78 (m, 2 H), 1.64 (m, 1 H), 1.29 (m, 2 H), 1.00 (d, 3 H, J = 6.6 Hz); IR (PUR) 2926, 2852, 2218, 1590, 1497, 1456, 1324, 1237, 1186, 1147, 1082, of 963 cm-1; MS (FAB) m/z 270 (M+H) Step 2: Method 1 Compounds of the general formula Vl-B (5 mmol), in which R8, R40, R41, U, T, and V have the meanings stated above and m stands for 0, 1, 2, or 3, palladium-on- charcoal (10%, 500 mg) and conc, hydrochloric acid (3 mL) are dissolved in MeOH (30 mL) and exposed to a hydrogen atmosphere over a period of 6 hours at RT. The reaction mixture is filtered over Celite and the filtrate is concentrated in vacuo. The residue is purified by means of flash chromatography (SiO2, EA). Method 2: Compounds of the general formula Vl-B (2 mmol), in which R8, R40, R41, U, T, and V have the meanings stated above and m stands for 0, 1, 2, or 3, are dissolved in THF (10 mL, 10 mL), and BH3'S(CH3)2 [2.0 M in THF, 3 mL, 3 equivalents] is added. The reaction mixture is heated under reflux over a period of 8 hours, aq. HCI (2N) is added and the reaction mixture is again heated under reflux for 30 minutes. Aq. sodium hydroxide solution (2N) is added to the reaction mixture, and the mixture is washed with EA. The combined organic phases are washed with sat. aq. NaCI solution and dried over magnesium sulfate. The solvent is removed in vacuo and the residue purified by column chromatography (SiO2, various mixtures of dichloromethane and MeOH as mobile solvent). The following compounds were obtained by method 2. (6-(Trifluoromethyl)-2-(4-methylpiperidin-1-yl)pyridin-3-yl)methanamine 1H NMR (300 M Hz, CDCI3) δ 7.89 (d, 1 H, J = 7.8 Hz), 7.33 (d, 1H, J = 7.8 Hz), 3.88 (s, 2H), 3.39 (m, 2 H), 2.83 (m, 2 H), 1.75 (m, 2 H), 1.55 (m, 1 H), 1.38 (m, 2 H), 1.00 (d, 3 H, J = 6.6 Hz); MS (FAB) m/z 274(M+H) C-(6'-tert-Butyl-4-methyl-3,4,5,6-tetrahydro-2H-[1,2']bipyridinyl-3'-yl)- methylamine 1H-NMR (CDCI3) δ 7.48 (d, 1H, J = 7.7 Hz, Ar), 6.90 (d, 1H, J = 7.7 Hz, Ar), 3.82 (s, 2H, CH2NH2), 3.38 (m, 2H, piperidine), 2.81 (m, 2H, piperidine), 1.73-1.28 (m, 5H, piperidine), 1.31 (s, 9H, C(CH3)3), 0.98 (d, 3H, J = 6.4 Hz, CHCH3) IR 3363, 2954, 1571, 1451, 1400, 1372, 1234, 960 cm"1 2. General instructions for the preparation of amines of the general formula V-E The preparation of amines of the general formula V-E is carried out as illustrated in the following scheme 2. Scheme 2. Step 1: Synthesis of 2-(cyclohexylthio)-6-(trifluoromethyl)nicotinonitrile 1.3 Equivalents of NaH (4.9 g, 0.124 mol) were dissolved in 50 mL of DMF under a blanket of nitrogen. Following the addition of 1.2 equivalents of cyclohexanethiol (14.2 mL, 0.116 mol), the mixture was stirred at RT over a period of 1.5 h. The resulting suspension was cooled to 10 °C and added dropwise to 1 equivalent of 2- chloro-6-(trifluoromethyl)nicotinonitrile (20 g, 0.096 mol) in 50 mL of DMF and stirred over a period of 2 h at RT. To the reaction mixture there was added sat. aq. NH4CI soln. and the mixture was diluted with 1 L of water and extracted with EA (3 x 200 mL) a number of times. The combined organic phases were washed with sat. aq. NaCI solution, dried over MgSO4 and concentrated in vacuo. Column chromatographic purification (silica gel 100-200 mesh, eluant: 2% EA in hexane) yielded 26 g (93.8%) of product. 1H NMR (300 M Hz, CDCI3) δ 7.94 (d ,1 H, J = 7.9 Hz), 7.34 (d, 1 H, J = 7.9 Hz), 4.00 (m, 1 H),1.90-2.14 (m, 2 H), 1.42-1.88 (m, 8 H) IR (neat) 2930, 2854, 2232, 1643, 1573, 1447, 1334, 1245, 1186, 1149, 1107, 851 cm"1 MS (FAB) m/z 287 (M+H) Step 2: Synthesis of (2-(cyclohexylthio)-6-(trifluoromethyl)-pyridin-3-yl)methanamine dihydrochloride The nitrile (26 g, 0.091 mol) was dissolved in 600 mL of THF under a blanket of nitrogen and cooled to 5 °C. BH3-dimethyl sulfide (13.78 g, 0.182 mol) was added dropwise and the mixture was boiled under reflux over a period of 20 h. After cooling to 5 °C, 100 mL of MeOH were added to the reaction batch and the mixture was stirred at RT over a period of 15 minutes. Di-tert-butyldicarbonate (29.7 g, 0.136 mol) was then added and the mixture was stirred at RT for 30 min. Following the removal of the solvent in vacuo, the crude product was purified by column chromatography (silica gel 100-200 mesh, eluant: 10% EA in hexane) and 23.4 g (66%) of product were obtained. The crude product was dissolved in 120 mL of sat. HCI/dioxane soln., and the solution was stirred at RT over a period of 6 h. Following the removal of the solvent in vacuo, the solid matter was washed with 10% EA in hexane (2 x 100 mL) and isolated by filtration. Yield: 17 g (88.8%) 1H NMR (DMSO-d6, 400 M Hz): δ 8.8 (s,2H), 8.05(d,1H), 7.76 (d,1H), 4.01 (s, 1H), 3.86-3.93 (m,1H), 2.02-2.08 (m,2H), 1.71-1.74 (m,2H), 1.40-1.60 (m,6H). 3. General instructions for the preparation of amines of the general formula V-B The preparation of amines of the general formula V-B is carried out as illustrated in the following scheme 3. Step 1: Preparation of nitriles of the general formula Vl-C Compounds of the general formula Vl-A (1 equivalent), in which R8, U, T, and V have the meanings stated above and m stands for 0,1,2, or 3, are stirred with an alcohol of the general formula HO-R42 (3.5 equivalents) and DBU [1,8-diaza- bicyclo[5.4.0]undec-7-ene] (3,5 equivalents) in acetonitrile (7 mL per mmol of the compound of formula Vl-A) over a period of 12 hours at RT. The reaction mixture is extracted with EA a number of times. The combined organic phases are washed with sat. aq. NaCI soln. and dried over MgSO4, and the solvent is removed in vacuo. The residue is purified in each case by column chromatography (SiO2, various mixtures of hexane/EA). Method 2: Compounds of the general formula Vl-C (2 mmol), in which R8, R42, U, T, and V have the meanings stated above and m stands for 0, 1,2, or 3, are dissolved in THF (10 mL, 10 mL) and BH3'S(CH3)2 [2.0 M in THF, 3 mL, 3 equivalent] is added. The reaction mixture is heated under reflux over a period of 8 hours, aq. HCI (2N) is added and the reaction mixture is again heated under reflux for 30 minutes. Aq. sodium hydroxide solution (2N) is added to the reaction mixture, and the mixture is washed with EA. The combined organic phases are washed with sat. aq. NaCI solution and dried over magnesium sulfate. The solvent is removed in vacuo and the residue is purified by column chromatography (SiO2, various mixtures of dichloromethane and methanol as mobile solvent). Method 3: Compounds of the general formula Vl-C (1,5 mmol), in which R8, R42, U, T, and V have the meanings stated above and m stands for 0,1,2, or 3, are dissolved in diethyl ether (3 mL) and a suspension of lithium aluminum hydride (3 mmol) in ether (5 mL) is slowly added dropwise at 0 °C. The reaction mixture is heated under reflux over a period of 4 hours and methanol followed by 1N aq. NaOH solution are slowly added dropwise at 0 °C. The reaction mixture is diluted with methanol and filtered over Celite. The solvent is removed in vacuo and the residue is purified by column chromatography (SiO2, various mixtures of dichloromethane and methanol as mobile solvent). 4. General instructions for the preparation of amines of the general formula V-C The preparation of amines of the general formula V-C is carried out as illustrated in the following scheme 4. Step 1: Preparation of nitriles of the general formula Vl-D Compounds of the general formula Vl-A (1 equivalent), in which R8, U, T, and V have the meanings stated above and m stands for 0,1,2, or 3, are dissolved together with bis(triphenylphosphine)palladium dichloride (7 mol%) and copper(l) iodide (14 mol%) in 1-methyl-2-pyrrolidinone (7 mL per mmol of the compound of the general formula Vl-A). Following a period of 10 minutes the alkyne of the general formula HC=C-R38 (3,5 equivalents) and N,N-diisopropylethylamine (2 equivalents) are added, and the reaction mixture is stirred over a period of 12 h at a temperature between 90 and 110 °C. The reaction mixture is filtered over Celite and extracted with EA a number of times. The combined organic phases are washed with sat. aq. NaCI solution, dried over MgSO4, and the solvent is removed in vacuo. The residue is purified in each case by column chromatography (SiO2, various mixtures of hexane/EA). 5. General instructions for the preparation of amines of the general formula V-D The preparation of amines of the general formula V-D is carried out as illustrated in the following scheme 5. Step 1: Preparation of nitriles of the general formula Vl-E Compounds of the general formula Vl-A (1 equivalent), in which R8, U, T, and V have the aforementioned meanings and m stands for 0, 1, 2, or 3, are stirred with palladium dichloride (5 mol%) and a compound of the general formula R38-B(OH)2 (2 equivalents), in which R38 stands for aryl, heteroaryl, or cycloalkenyl, in a solvent mixture of toluene/dioxane/2N aq. sodium carbonate solution (20 mL per 1 mmol of compounds of the general formula Vl-A). The reaction mixture is heated under reflux over a period of 12 h and filtered over Celite. The combined organic phases are dried over magnesium sulfate, and the solvent is removed in vacuo. The residue is purified by column chromatography (SiO2, various solvent mixtures of hexane and EA). Step 2: Method 1: Compounds of the general formula Vl-E (5 mmol), in which R8, R38, U, T, and V have the meanings stated above and m stands for 0, 1,2, or 3, palladium-on-charcoal (10%, 500 mg) and concentrated hydrochloric acid (3 mL) are dissolved in MeOH (30 mL) and exposed to a hydrogen atmosphere over a period of 6 hours at RT. The reaction mixture is filtered over Celite and the filtrate is concentrated in vacuo. The residue is purified by means of flash chromatography (SiO2, EA). Method 2: Compounds of the general formula Vl-E (2 mmol), in which R8, R38, U, T, and V have the meanings stated above and m stands for 0,1,2, or 3, are dissolved in THF (10 mL, 10 mL), and BH3'S(CH3)2 [2.0 M in THF, 3 mL, 3 equivalent] is added. The reaction mixture is heated under reflux over a period of 8 hours, aq. HCI (2N) is added and the reaction mixture is again heated under reflux for 30 minutes. Aq. sodium hydroxide solution (2N) is added to the reaction mixture, and the mixture is washed with EA. The combined organic phases are washed with sat. aq. NaCI solution and dried over magnesium sulfate. The solvent is removed in vacuo and the residue is purified by column chromatography (SiO2, various mixtures of dichloromethane and methanol as mobile solvent). 6. Preparation of specific acids Preparation of 2-(3-halogenated-4-(methylthio)phenyl)propanoic acids (cf. Examples 28, 29) Substituted methylthiophenylpropanoic acids can be prepared as described in US2003/225283. For this purpose, a solution of AICI3 (54.9 g, 412 mmol) in chloroform (180 mL) is cooled under an argon atmosphere to 0 °C and a solution of methyl-2-chloro-2-oxoacetate (24.3 mL, 264 mmol) in chloroform (180 mL) is added in drops. After this reaction mixture has been stirred for 30 min at 0 °C, a solution of 2-chlorothioanisol (39.4 g, 247 mmol) in chloroform (180 mL) is added in drops. The red-coloured reaction mixture is slowly heated to room temperature and stirred for a further 4 h. The reaction mixture is then slowly stirred in ice water (700 mL) and the obtained yellow mixture is stirred for 15 min and filtered to remove the aluminium salts. The filtrate is extracted with dichloromethane (3 x 50 mL) and the combined organic phases are washed with sat. aq. sodium bicarbonate solution (1 x 50 mL). After drying of the organic phase over MgSO4 and removal of the solvent in vacuo, the (3-chloro-4-methylsulfanyl-phenyl)-oxo-methyl acetate as oil (36.4 g, 60%) is obtained (a). A solution of this ester (61.7 g, 252 mmol) in toluol (120 mL) is heated to 50 °C. While ensuring that the temperature of the reaction mixture does not exceed 60 °C, a 3 M NaOH solution (105 mL, 313 mmol) is now added in drops and subsequently stirred for 1.5 h at 50 °C. After removal of the heat source, cone. HCI (10.6 mL, 290 mmol) is added to the warm solution in drops and once the mixture is cooled to room temperature, it is let to stir for a further 16 h. The resultant precipitate is filtered off, washed with water (50 mL) and toluol (50 mL) and dried. The (3-chloro-4- methylsulfanyl-phenyl)-oxo-acetic acid accumulates as a white solid (57.2 g, 98%) (b). Hydrazine-hydrate (8.5 mL, 273 mmol) is provided in a reaction flask with a mechanical stirrer. After cooling to -50 °C, in one portion, the oxo-acetic acid (12.6 g, 54.6 mmol) is added, which leads to an increase in temperature. The resultant milky mixture is heated to 80 °C and, after removal of the heat source, KOH (2.09 g, 31.7 mmol) is added in one portion. This leads to an exothermal reaction. After cooling to 80 °C, a further portion of KOH (2.09 g, 31.7 mmol) is added and in turn cooled to 80 °C. This procedure is now repeated two further times. After addition of the fourth portion of KOH, the reaction mixture is boiled for 16 h at 100 °C. After cooling of the homogeneous reaction mixture to room temperature, it is diluted with water (12 mL) and, following transfer to a separating funnel, further water (12 mL) and diethylether (40 mL) are added. After phase separation, the organic phase is extracted with water (2x15 mL). Heptane (20 mL) is added to the combined aqueous phases and the mixture is vigorously stirred. While keeping the temperature below 50 °C by means of an ice bath, cone. HCI (26 mL) is added in drops over a period of 30 min and the resultant suspension is stirred for 3 h at room temperature. The resultant precipitate is filtered off and consecutively washed with 1 N aq. HCI solution (2x6 mL), heptane (1x12 mL) and heptane/diethyl ether (15 mL, 4:1). After drying, the (3-chloro-4- methylsulfanyl-phenyl)-acetic acid (10.48 g, 89%) is obtained as a cream-coloured solid (c). This (3-chloro-4-methylsulfanyl-phenyl)-acetic acid is now alkylated in alpha position in an analogous manner to Vazquez et al. Eur. J. Med. Chem. Chim. Ther. (1997), 32, 6, 529-53. A solution of the aryl acetic acid (1.05 mmol) in dry THF (3 mL) is cooled to -78 °C and stirred under an argon atmosphere . For this purpose, a 2 M solution of LDA in hexane (1.6 mL, 3.2 mmol) and TMEDA (0.3 mL, 1.9 mmol) is added in drops over a period of 15 min. After 3 hours of slow stirring at -78 °C, methyl iodide (0.17 mL, 2.7 mmol) is added slowly while stirring. After 16 hours of stirring at room temperature, the reaction mixture is neutralized with sat. aq. NH4CI solution (10 mL) and stirred for 1 h at room temperature. After separation of the organic phase, the aqueous, alkaline phase is acidified with 5 N HCI and the product extracted with ether (3 x 20 mL). The combined organic phases are dried over Na2SO4 and the solvent is removed in vacuo. Purification by means of column chromatography (hexane/ethyl acetate 8:2) produces the desired methylthiophenylpropanoic acid (d). Preparation of 2-(3-halogenated-4-(methylsulfonyl)phenyl)propanoic acids (cf. Examples 29, 31) In an analogous manner to the method described in US2003/225283, the methylthiophenylpropanoic acids are reacted to yield the corresponding methylsulfonylphenylpropanoic acids. In this process, a solution of methylthiophenylpropanoic acid (0.16 mmol) is dissolved in formic acid (0.19 mL, 4.8 mmol) and cooled to 0 °C. After addition of 30% strength aq. hydrogen peroxide solution (0.10 mL, 0.8 mmol), stirring is performed at 0 °C for 30 min and the reaction is then quenched with 10% strength aq. sodium bisulphite solution. The reaction mixture is diluted with water (5 mL) and extracted ethyl acetate (2x5 mL). The combined organic phases are dried over Mg2SO4 and the solvent is removed in vacuo. The residue obtained is dissolved in methanol (1 mL) and a solution of KMNO4 (0.028 g, 0.176 mmol) in water (0.5 mL) is added by drops. The dark brown solution is now stirred for 30 min at room temperature and then diluted with methanol (10 mL). After filtration of the solution, the filtrate is concentrated in vacuo and purified by column chromatography (hexane/ethyl acetate 1:4) (a). Preparation of 2-(4-(N-substituted sulfamoyl)-3-fluorophenyl)propanoic acids (cf. Ex. 32) In an analogous manner to Greig, IR et al. J. Med. Chem. (2006), 49, 4787-7492, the bromo-fluorobenzyl-sulfonylchloride (5 mmol) is dissolved with dimethylamine (5 mmol) in dichloromethane (15 mL). Pyridine (5 mmol) is added to this mixture and the mixture is stirred for 2 h at room temperature. After addition of water (15 mL), the organic phase is separated and the aqueous phase extracted with ethyl acetate (15 mL). The combined organic phases are dried over Na2SO4, the solvent is removed in vacuo and the residue is purified by column chromatography (a). As described in Durandetti M. et al., Tetrahedron (2007), 63, 1146-1153, the sulfamoyl-aryl bromide is converted with ethylchloropropionate into sulfamoyl- arylpropanoic acid ester. Together with ethylchloropropionate (1.6 mL ,13 mmol), sulfamoyl-aryl bromide (10 mmol) is stirred under an argon atmosphere at room temperature in 15 ml DMF. For the purpose of activation, (1.1 g, 20 mmol) Mn, followed by 2,2'-bipyridine)nickel-(ll)-dibromide (0.26 g, 0.7 mmol) and TFA (20 mL) are then added. The reaction mixture is stirred for 1.5 h at 50 °C. After cooling of the reaction mixture, hydrolysis is performed with 25 mL 1 N HCI, the mixture is extracted 3 x with 25 mL diethyl ether, the combined organic phases are washed with 25 mL water and 25 mL sat. NaCI solution, dried over MgSO4 and concentrated in vacuo. The resultant precipitate is removed by suction, washed with diethyl ether and purified by means of column chromatography (b). The propionate (0.81 mmol) is then dissolved in a mixture of THF (1.6 mL, 20 mmol) and water (0.8 mL, 45 mmol). After addition of LiOH (0.058 g, 2.43 mmol), the reaction mixture is refluxed overnight. For the purpose of processing, 25 mL water and 25 mL diethyl ether are added to the mixture and the resultant phases are separated. The aqueous phase is acidified with HCI and extracted 3x with in each case 25 mL dichloromethane. After combination of the organic phases, drying over MgSO4 and concentration in vacuo, the N-substituted sulfamoyl- fluorophenylpropanoic acid can be obtained. Preparation of 2-(4-methoxy- and hydroxy-3,5-dimethylphenyl)propanoic acids (cf. Examples 35-38) In an analogous manner to the method described in WO2006/078834, on the basis of aryl bromides, phenylpropanoic acids can be obtained by reaction with diethylmalonate. For this purpose, in the first step, NaH (60%, 1.45 g, 36.2 mmol) is added to a solution of aryl bromide (16.5 mmol), CuBr (4.72 g, 32.9 mmol) and diethyl malonate (5 mL, 32.9 mmol) in 1,4-dioxane (20 mL) at room temperature while stirring slowly and stirred for 16 h at 100 °C. After filtration, the filtrate is concentrated in vacuo and purified by means of column chromatography (hexane/ethyl acetate 4:1) (a). The obtained phenylmalonic acid diethyl ester (21 mmol) is now dissolved in 2 N NaOH /THF:H20 (1:1) (20 mL) and refluxed for 3 h. After acidification of the reaction mixture to pH 1 with cone HCI, stirring is carried out for a further hour at room temperature. The solution is then adjusted with 1 N NaOH to pH 13 and extracted with diethyl ether. The aqueous phase is adjusted with 1 N HCI to pH 5 and extracted with ethyl acetate (3 x). The combined organic phases are washed with sat. NaCI solution, dried over Na2SO4 and, after filtration, the solvent is removed in vacuo (b). This phenylacetic acid is now alkylated in an analogous manner to Vazquez et al. Eur. J. Med. Chem. Chim. Ther. (1997), 32, 6, 529-53 in alpha position. A solution of arylacetic acid (1.05 mmol) in dry THF (3 mL) is cooled under an argon atmosphere to -78 °C and stirred. For this purpose, a 2 M solution of LDA in hexane (1.6 mL, 3.2 mmol) and TMEDA (0.3 mL, 1.9 mmol) is added in drops over a period of 15 min. After 3 hours of slow stirring at -78 °C, methyl iodide (0.17 mL, 2.7 mmol) is added slowly while stirring. After 16 hours of stirring at room temperature, the reaction mixture is neutralized with sat. aq. NH4CI solution (10 mL) and stirred for 1 h at room temperature. After separation of the organic phase, the aqueous, alkaline phase is acidified with 5 N HCI and the product is extracted with ether (3 x 20 mL). The combined organic phases are dried over Na2SO4 and the solvent is removed in vacuo. Purification by means of column chromatography (hexane/ethyl acetate 8:2) produces the desired substituted phenylmethoxy-propanoic acid (c). According to a method known to the person skilled in the art, the methoxy ether is split by means of HBr in glacial acetic acid and the corresponding phenylhydroxy- propanoic acid is obtained (d). Preparation of 2-(4-amino-3,5-difluorophenyl)propanoic acid (cf. Ex. 26) KOtBu (3.57 g, 31.85 mmol) was dissolved in DMF (30 mL) and cooled to -45 °C. A mixture of ethyl-2-chloropropionate (2 mL, 15.9 mmol) and 2,6-difluoronitrobenzene (2.5 g, 15.7 mmol) were added slowly in drops to the solution kept at -40 °C and stirred for 1 h after addition. For the purpose of processing, the reaction mixture was adjusted with 16% strength HCI to pH 4 and diluted with water (150 mL). The mixture was extracted with ethyl acetate (3 x 50 mL), the combined organic phases washed with water (50 mL) and sat. NaCI solution (2 x 50 mL) and dried over MgSO4. After removal of the solvent in vacuo, the product was obtained as an oil (4.12 g, 99%) (a). The difluoronitropropanoate (2.59 g, 10 mmol) was dissolved in EtOH/acetic acid ester (200 mL, 1 : 1) and hydrated in the H cube (1 bar, 25 °C, 1 mL/min, 0.25 mol/L). After removal of the solvent in vacuo, the difluoroaminopropionate could be obtained as an oil (2.27 g, 99%) (b). The raw product of the hydrogenation (1 g, 4.36 mmol) was dissolved in THF/water (10 mL, 2 :1), LiOH (0.312 g, 13.1 mmol) added and refluxed for 16 h. Water (50 mL) and diethyl ether (25 mL) were added to the reaction mixture. After phase separation, the aqueous phase was acidified with HCI to pH 2 and extracted with dichloromethane (3 x 50 mL). The combined organic phases were dried over MgSO4 and the solvent removed in vacuo. The product was obtained as a white solid (0.72 g, 81%) (c). 7. General instructions for the reaction of amines of the general formulas V or X with carboxylic acids of the general formula VII Method A: The acid of the general formula VII (1 equivalent), the amine of the general formulas V or X (1.2 equivalents) and EDCI (1.2 equivalents) are stirred in DMF (10 mmol of acid in 20 mL) over a period of 12 hours at RT, and water is then added. The reaction mixture is extracted with EA a number of times, the aqueous phase is saturated with NaCI and then again extracted with EA. The combined organic phases are washed with 1N hydrochloric acid and sat. aq. NaCI soln., dried over MgSO4, and the solvent is removed in vacuo. The residue is purified by means of flash chromatography (SiO2, EA/hexane 1:2). Method B: The acid of the general formula VII (1 equivalent) and the amine of the general formula V or X (1.1 equivalents) are dissolved in DCM (1 mmol acid in 6 mL), and to the solution EDCI (1.5 equivalents), HOBt (1.4 equivalents) and triethylamine (3 equivalents) are added at 0 °C. The reaction mixture is stirred at RT for a period of 20 h and purified by column chromatography (2:1 mixture of n-hexane/AE). The following exemplary compounds were obtained in accordance with method B above. Exemplary Compound 3: 2-(4-Amino-3-bromo-5-methoxy-phenyl)-N-(4-methyl-6,-trifluoromethyl-3,4,5,6- tetrahydro-2H-[1,2']bipyridinyl-3'-ylmethyl)acetamide 1H-NMR (CDCl3) δ 7.52 (d, 1H, J = 7.5 Hz), 7.21 (d, 1H, J = 7.5 Hz), 6.93 (d, 1H, J = 1.4 Hz), 6.57 (d, 1H), 6.24 (bt, NH), 4.47 (d, 2H), 4.22 (s, 2H), 3.80 (s, 3H), 3.51 (s, 2H), 3.30-3.26 (m, 2H), 1.70-1.48 (m, 3H), 1.21-1.09 (m, 2H), 0.95 (d, 3H, J = 6.4 Hz) IR 3298, 2924, 1649, 1575, 1500, 1460, 1420, 1338, 1135, 1047 cm-1 Mass (FAB) m/z 515 and 517 [M+H]+ (Base), 537 and 539 [M+Na]+ Exemplary Compound 4: 2-(3-Fluorophenyl)-N-(4-methyl-6'-trifluoromethyl-3,4,5,6-tetrahydro-2H- [1,2']bipyridinyl-3'-ylmethyl)acetamide IR (KBr) 3272, 2923, 1648, 1592, 1552, 1455, 1421, 1374, 1337, 1246, 1138,958, 835, 774 cm-1 MS(FAB) m/z 410(M+H) Exemplary Compound 5: 2-(2,4-Difluoro-phenyl)-N-(4-methyl-6'-trifluoromethyl-3,4,5,6-tetrahydro-2H- [1,2']bipyridinyl-3'-ylmethyl)acetamide IR (KBr) 3270, 2921, 1647, 1558, 1507, 1424, 1330, 1242, 1134, 966, 851 cm-1 MS (FAB) m/z 428 (M+H) Exemplary Compound 6: 2-(2,6-Difluoro-phenyl)-N-(4-methyl-6'-trifluoromethyl-3,4,5,6-tetrahydro-2H- [1,2']bipyridinyl-3'-ylmethyl)acetamide IR (KBr) 3292, 2924, 1656, 1593, 1553, 1468, 1419, 1337, 1238, 1178, 1135, 1017, 945, 834, 784 cm-1 MS (FAB) m/z 428 (M+H) Exemplary Compound 7: 2-(2,5-Difluoro-phenyl)-N-(4-methyl-6'-trifluoromethyl-3,4,5,6-tetrahydro-2H- y[1,2']bipyridinyl-3'-ylmethyl)acetamide IR (KBr) 3271, 2922, 1644, 1593, 1555, 1497, 1424, 1329, 1137, 960, 833, 756 cm-1 MS (FAB) m/z 428 (M+H) Exemplary Compound 8: 2-(4-Fluoro-phenyl)-N-(4-methyl-6,-trifluoromethyl-3,4,5,6-tetrahydro-2H- [1,2']bipyridinyl-3'-ylmethyl)acetamide IR (KBr) 3255, 2920, 1646, 1595, 1558, 1509, 1424, 1330, 1229, 1132, 1043, 960, 828, 755 cm-1 MS(FAB) m/z 410 (M+H) Exemplary Compound 9: 2-(4-Hydroxy-3-methoxy-phenyl)-N-methyl-6'-trifluoromethyl-3,4,5,6- tetrahydro-2H-[1,2']bipyridinyl-3'-ylmethyl)propionamide ' 1H NMR (300 M Hz, CDCl3) δ 7.44 (d, 1 H, J = 7.7 Hz), 7.17 (d, 1 H, J = 7.5 Hz), 6.88 (d, 1 H, J= 7.9 Hz), 6.80-6.70 (m, 2 H), 6.11 (bt, 1 H), 5.60 (s, 1 H), 4.46-4.42 (m, 2 H), 3.84 (s, 3 H), 3.55 (q, 1 H, J = 7.1 Hz), 3.32-3.23 (m, 2 H), 2.83-2.73 (m, 2 H), 1.71-1.66 (m, 2 H), 1.53 (d, 3 H, J= 7.1 Hz), 1.26-1.1 (m, 2 H), 0.96 (d, 3 H, J= 6.6 Hz) IR (KBr) 3301, 2925, 1650, 1516, 1458, 1421, 1373 cm"1 MS (FAB) m/z 452 (M+H) Exemplary Compound 10: 2-(3,5-Difluoro-phenyl)-N-(4-methyl-6'-trifluoromethyl-3,4,5,6-tetrahydro-2H- [1,2']bipyridinyl-3'-ylmethyl)propionamide 1H NMR (300 M Hz, CDCl3) δ 7.47 (d, 1 H, J- 7.5 Hz), 7.21 (d, 1 H, J- 7.7 Hz), 6.85-6.82 (m, 2 H), 6.80-6.70 (m, 2 H), 6.11 (bt, 1 H), 5.60 (s, 1 H), 4.46-4.42 (m, 2 H), 3.84 (s, 3 H), 3.55 (q, 1 H, J = 7.1 Hz), 3.32-3.23 (m, 2 H), 2.83-2.73 (m, 2 H), 1.71-1.66 (m, 2 H), 1.53 (d, 3 H, J= 7.1 Hz), 1.26-1.1 (m, 2 H), 0.96 (d, 3 H, J = 6.6 Hz) IR (KBr) 3293, 2925, 1651, 1596, 1542, 1460, 1335 cm"1 MS (FAB) m/z 442 (M+H) Exemplary Compound 12: 2-(4-Fluoro-phenyl)-N(4-methyl-6'-trifluoromethyl-3,5,4,6-tetrahydro-2H- [1,2']bipyridinyl-3'-ylmethyl)propionamide 1H-NMR(CDCI3) δ 7.43(d, 1H, J = 7.5 Hz), 7.28-7.24(m, 2H), 7.18(d, 1H, J = 7.7 Hz), 7.06-7.00(m, 2H), 6.16 (bs, NH), 4.45(d, 2H), 3.59(q, 1H, J = 7.0 Hz), 3.29(m, 2H), 2.79(m, 2H0, 1.75-1.50(m, 3H), 1.53(d, 3H, J = 7.1 Hz), 1.26-1.10(m, 2H), 0.96(d, 3H, J = 6.4 Hz) IR 3291, 2925, 1650, 1510, 1458, 1419, 1336, 1231, 1177, 1138 cm-1 Mass (FAB) m/z 424 [M+H]+ (Base), 446 [M+Na]+ Exemplary Compound 13: 2-(3-Fluoro-phenyl)-N-(4-methyl-6'-trifluoromethyl-3,4,5,6-tetrahydro-2H- [1,2']bipyridinyl-3'-ylmethyl)propionamide 1H-NMR(CDCI3) δ 7.43(d, 1H, J = 7.7 Hz), 7.31 (m, 1H), 7.18(d, 1H, J = 7.7 Hz), 7.07- 6.95(m, 3H), 6.23(bs, NH), 4.45(d, 2H), 3.60(q, 1H, J = 7.0 Hz), 3.29(m, 2H), 2.79(m, 2H), 1.65-1.50(m, 3H), 1.54(d, 2H, J = 7.0 Hz), 1.24-1.12(m, 2H), 0.96(d, 3H, J = 6.4 Hz) IR 3292, 2925, 1651, 1592, 1542, 1456, 1419, 1177, 1140 cm"1 Mass (FAB) m/z 424 [M+H]+ (Base), 446 [M+Na]+ Exemplary Compound 14: 2-(3,4-Diamino-phenyl)-N-(4-methyl-6'-trifluoromethyl-3,4,5,6-tetrahydro-2H- [1,2']bipyridinyl-3'-ylmethyl)propionamide 1H-NMR(CDCI3) δ 7.42 (d, 1H, J = 7.5 Hz), 7.17 (d, 1H, J = 7.7 Hz), 6.67-6.57 (m, 3H), 6.03 (bt, NH), 4.41 (d, 2H), 3.49 (q, 1H, J = 7.3 Hz), 3.40 (br, NH2), 3.33-3.27 (m, 2H), 2.84-2.74 (m, 2H), 1.73-1.55 (m, 3H), 1.51 (d, 3H, J = 7.1 Hz), 1.30-1.18 (m, 2H), 0.96 (d, 3H, J = 6.6 Hz) IR 3334, 2925, 1651, 1518, 1419, 1176, 1135, 733 cm'1 Mass (FAB) m/z 436 [M+H]+ Exemplary Compound 15: N-(2-Butoxy-6-tert-butyl-pyridin-3-ylmethyl)-2-(3,4-diaminophenyl)propionamide 1H-NMR(CDCI3) δ 7.32 (d, 1H, J = 7.5 Hz, Ar), 6.76 (d, 1H, J = 7.3 Hz, Ar), 6.66-6.57 (m, 3H, Ar), 6.00 (bt, NH), 4.27 (m, 4H, OCH2 & CH2NH), 3.41 (q, 1H, J = 7.1 Hz, CHCH3), 1.64 (m, 2H, OCH2CH2), 1.45 (d, 3H, J = 7.1 Hz, CHCH3), 1.39 (m, 2H, CH2CH3), 1.29 (s, 9H, C(CH3)3), 0.95 (t, 3H, J = 7.3 Hz, CH2CH3) IR 3303, 2960, 1649, 1517, 1456, 1254 cm'1 Mass (FAB) 399 m/z [M+H]+ Exemplary Compound 16: N-(6'-tert-Butyl-4-methyl-3,4,5,6-tetrahydro-2H-[1,2']bipyridinyl-3'-ylmethyl)-2- (3,4-diamino-phenyl)propionamide 1H-NMR(CDCI3) δ 7.26 (d, 1H, J = 7.9 Hz, Ar), 6.85 (d, 1H, J = 7.7 Hz, Ar), 6.66-6.58 (m, 3H, Ar), 6.39 (bt, NH), 4.37 (m, 2H, CH2NH), 3.45 (q, 1H, J = 7.1 Hz, CHCH3), 3.37 (bs, NH22), 3.23 (m, 2H, piperidine), 2.74 (m, 2H, piperidine), 1.65-1.45 (m, 3H, piperidine), 1.49 (d, 3H, J = 7.1 Hz, CHCH3), 1.29 (s, 9H, C(CH3)3), 1.28-1.16 (m, 2H, piperidine), 0.95 (d, 3H, J = 6.4 Hz, piperidine CH3) IR 3338, 2955, 1648, 1517, 1449, 1232 cm-1 Mass (FAB) m/z 424[M+H]+ Exemplary Compound 17: N-(6-tert-Butyl-2-cyclohexylsulfanyl-pyridin-3-ylmethyl)-2-(3,4-diamino-phenyl)- propionamide 1H-NMR(CDCI3) δ 7.27 (d, 1H, Ar), 6.91 (d, 1H, J = 7.9 Hz, Ar), 6.67-6.59 (m, 3H, Ar), 5.90 (bt, NH), 4.26 (m, 2H, CH2NH), 3.96 (m, 1H, SCH), 3.46 (q, 1H, J = 7.3 Hz, CHCH3), 3.37 (bs, NH2*2), 2.06 (m, 2H, cyclohexyl), 1.80-1.20 (m, 8H, cyclohexyl), 1.50 (d, 3H, CHCH3), 1.31 (s, 9H, C(CH3)3) IR 3303, 2929, 2854, 1651, 1517, 1444, 1079cm-1 Mass (FAB) m/z 441[M+H]+ Exemplary Compound 19: 2-(3,5-Dibromo-4-hydroxy-phenyl)-N-(4-methyl-6'-trifluoromethyl-3,4,5,6-tetra- hydro-2H-[1,2']bipyridinyl-3'-ylmethyl)propionamide 1H-NMR(CDCI3) δ 7.48 (m, 1H, Ar), 7.39 (s, 2H, Ar), 7.22 (d, 1H, J = 7.7 Hz, Ar), 6.27 (bt, NH), 4.47 (m, 2H, CH2NH), 3.46 (q, 1H, J = 7.1 Hz, CHCH3), 3.31 (m, 2H, piperidine), 2.81 (m, 2H, piperidine), 2.40 (s, OH), 1.75-1.16 (m, 5H, piperidine), 1.50 (d, 3H, J = 7.1 Hz, CHCH3), 0.98 (d, 3H, J = 6.4 Hz, piperidine CH3) IR 3298, 2924, 1650, 1550, 1462, 1417, 1176, 1138 cm-1 Mass (FAB) m/z 580 [M+H]+ Exemplary Compound 20: 2-(4-Amino-3,5-dibromo-phenyl)-N-(4-methyl-6'-trlfluoromethyl-3,4,5,6-tetra- hydro-2H-[1,2']bipyridinyl-3'-ylmethyl)propionamide 1H-NMR(CDCI3) δ 7.47 (d, 1H, J = 7.7 Hz, Ar), 7.31 (s, 2H, Ar), 7.21 (d, 1H, J = 7.7 Hz, Ar), 6.18 (bt, NH), 4.55 (bs, NH2), 4.46 (m, 2H, CH2NH), 3.43 (q, 1H, J = 7.0 Hz, CHCH3), 3.30 (m, 2H, piperidine), 2.81 (m, 2H, piperidine), 1.75-1.15 (m, 5H, piperidine), 1.48 (d, 3H, J = 7.1 Hz, CH2CH3), 0.97 (d, 3H, J = 6.4 Hz, piperidine CH3) IR 3298, 2924, 1649, 1544, 1474, 1418, 1177, 1136 cm-1 Mass (FAB) m/z 579[M+H]+ Exemplary Compound 21: 2-(3-Bromo-4-hydroxy-5-methoxy-phenyl)-N-(4-methyl-6'-trifluoromethyl-3,4,5,6- tetrahydro-2H-[1,2']bipyridinyl-3'-ylmethyl)acetamide 1H-NMR(CDCI3) δ 7.54 (d, 1H, J = 7.5 Hz, Ar), 7.22 (d, 1H, J = 7.7 Hz, Ar), 6.99 (d, 1H, J = 1.5 Hz, Ar), 6.69 (d, 1H, J = 2.0 Hz, Ar), 6.27 (bt, NH), 5.91 (bs, OH), 4.48 (m, 2H, CH2NH), 3.86 (s, 3H, OCH3), 3.53 (s, 2H, CH2CO), 3.28 (m, 2H, piperidine), 2.80 (m, 2H, piperidine), 1.73-1.07 (m, 5H, piperidine), 0.96 (d, 3H, J = 6.4 Hz, piperidine CH3) IR 3298, 2924, 1649, 1501, 1459, 1421, 1282, 1178, 1136, 1047 cm-1 Mass(FAB)m/z 517[M+H]+ Exemplary Compound 22: 2-(4-Amino-3,5-dibromo-phenyl)-N-(4-methyl-6,-trifluoromethyl-3,4,5,6-tetra- hydro-2H-[1,2']bipyridinyl-3'-ylmethyl)acetamide 1H-NMR(CDCI3) δ 7.53 (d, 1H, J = 7.3 Hz, Ar), 7.29 (s, 2H, Ar), 7.23 (d, 1H, J = 7.7 Hz, Ar), 6.26 (bt, NH), 4.57 (bs, NH2), 4.48 (m, 2H, CH2NH), 3.46 (s, 2H, CH2CO), 3.30 (m, 2H, piperidine), 2.81 (m, 2H, piperidine), 1.75-1.10 (m, 5H, piperidine), 0.97 (d, 3H, J = 6.4 Hz, piperidine CH3) IR 3288, 2923, 1649, 1544, 1478, 1418, 1337, 1177, 1135 cm-1 Mass (FAB) m/z 565 [M+H]+ Exemplary Compound 23: 2-(3,5-Dibromo-4-hydroxy-phenyl)-N-(4-methyl-6'-trifluoromethyl-3,4,5,6-tetra- hydro-2H-[1,2']bipyridinyl-3'-ylmethyl)acetamide 1H-NMR(CDCI3) δ 7.55 (d, 1H, J = 7.7 Hz, Ar), 7.38 (s, 2H, Ar), 7.24 (d, 1H, J = 7.7 Hz, Ar), 6.31 (bt, NH), 4.50 (m, 2H, CH2NH), 3.50 (s, 2H, CH2CO), 3.31 (m, 2H, piperidine), 2.82 (m, 2H, piperidine), 2.40 (s, OH), 1.77-1.10 (m, 5H, piperidine), 0.97 (d, 3H, J = 6.6 Hz, piperidine CH3) IR 3297, 2924, 1650, 1546, 1473, 1419, 1337, 1177, 1137 cm-1 Mass (FAB) m/z 566 [M+H]+ Exemplary Compound 24: 2-(3-Amino-4-hydroxy-phenyl)-N-(4-methyl-6'-trlfluoromethyl-3,4,5,6-tetrahydro- 2H-[1,2']bipyridinyl-3'-ylmethyl)propionamide 1H-NMR(CDCI3) δ 7.42 (d, 1H, J = 7.7 Hz, Ar), 7.17 (d, 1H, J = 7.7 Hz, Ar), 6.69-6.64 (m, 2H, Ar), 6.53 (dd, 1H, J = 8.0, 1.8 Hz, Ar), 6.07 (bt, NH), 4.42 (d, 2H, J = 5.7 Hz, CH2NH), 3.69 (bs, NH2), 3.59 (q, 1H, J = 7.1 Hz, CHCH3), 3.30 (m, 2H, piperidine), 2.79 (m, 2H, piperidine), 1.71-1.50 (m, 6H, piperidine & CHCH3), 1.22 (m, 2H, piperidine), 0.96 (d, 3H, J = 6.6 Hz, CHCH3) IR 3298, 2924, 1649, 1519, 1458, 1420, 1177, 1136 cm-1 Mass (FAB) m/z 437 [M+H]+, 459 [M+Na]+ Exemplary Compound 25: 2-(3,5-Dibromo-phenyl)-N-(4-methyl-6'-trifluoromethyl-3,4,5,6-tetrahydro-2H- [1,2']bipyridinyl-3'-ylmethyl)acetamide 1H-NMR(CDCI3) δ 7.61 (t, 1H, J = 1.7 Hz), 7.54 (d, 1H, J = 7.7 Hz), 7.38 (d, 1H, J = 1.7 Hz), 7.24 (d, 1H, J = 7.7 Hz), 6.34 (bt, NH), 4.50 (d, 2H), 3.54 (s, 3H), 3.32 (m, 2H), 2.83 (m, 2H), 1.75-1.50 (m, 3H), 1.33-1.13 (m, 2H), 0.98 (d, 3H, J = 6.4 Hz) IR 3291, 2924, 1649, 1554, 1458, 1421, 1337, 1176, 1138 cm"1 Mass (FAB) m/z 550[M+H]+ The following further exemplary compounds were obtained by the methods described above: Exemplary compounds 28-32 and 35-33 can likewise be obtained according to the methods described above. Pharmacological Data The affinity of the compounds according to the invention for the vanilloid receptor 1 (VR1/TRPV1 -Receptor) was detected as described above (Pharmacological Methods I and II respectively). The compounds according to the invention of the above formula I exhibit excellent affinity to the VR1/TRPV1 receptor (Table 1). Ne denotes "no effect", i.e. no reaction was observed. The value following the symbol "@" indicates the concentration at which the inhibition (in percent) was determined. Claims 1. Substituted compounds of the general formula I, in which n stands for 0, 1, 2, 3, or 4; R1 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(= O)-NH2; -S(= O)2-NH2; -C(= O)-NH-OH; -C(= O)-OH; -C(= O)-H; -S(= O)2-OH; - C(= NH)-NH2; -C(= NH)-NH-R9; -N= C(NH2)2; -N= C(NHR10)-(NHR11); - O-P(= O)2-O-R12; -NHR13; -NR14R15; -NH-C(= O)-R13; -OR16; -SR17; -C(= O)-NHR18; -C(= O)-NR19R20; -S(= O)2-NHR21; -S(= O)2-NR22R23; -C(= O)-OR24; -C(= O)-R25; -S(= O)-R26; or -S(= O)2-R27 or for a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical; R2 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(= O)-NH2; -S(= O)2-NH2; -C(= O)-NH-OH; -C(= O)-OH; -C(= O)-H; -S(= O)2-OH; - C(= NH)-NH2; -C(= NH)-NH-R9; -N= C(NH2)2; -N= C(NHR10)-(NHR11); - O-P(= O)2-O-R12; -NHR13; -NR14R15; -NH-C(= O)-R13; -OR16; -SR17; -C(= O)-NHR18; -C(= O)-NR19R20; -S(= O)2-NHR21; -S(= O)2-NR22R23; -C(= O)-OR24; -C(= O)-R25; -S(= O)-R26; or -S(= O)2-R27 or for a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical; R3 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(= O)-NH2; -S(= O)2-NH2; -C(= O)-NH-OH; -C(= O)-OH; -C(= O)-H; -S(= O)2-OH; - C(= NH)-NH2; -C(= NH)-NH-R9; -N= C(NH2)2; -N= C(NHR10)-(NHR11); - O-P(= O)2-O-R12; -NHR13; -NR14R15; -NH-C(= O)-R13; -OR16; -SR17, -C(= O)-NHR18; -C(= O)-NR19R20; -S(= O)2-NHR21; -S(= O)2-NR22R23; -C(= O)-OR24; -C(= O)-R25; -S(= O)-R26; or -S(= O)2-R27 or for a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical; R4 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(= O)-NH2; -S(= O)2-NH2; -C(= O)-NH-OH; -C(= O)-OH; -C(= O)-H; -S(= O)2-OH; - C(= NH)-NH2; -C(= NH)-NH-R9; -N= C(NH2)2; -N= C(NHR10)-(NHR11); - O-P(= O)2-O-R12; -NHR13; -NR14R15; -NH-C(= O)-R13; -OR16; -SR17; -C(= O)-NHR18; -C(= O)-NR19R20; -S(= O)2-NHR21; -S(= O)2-NR22R23; -C(= O)-OR24; -C(= O)-R25; -S(= O)-R26; or -S(= O)2-R27 or for a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical; R5 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(= O)-NH2; -S(= O)2-NH2; -C(= O)-NH-OH; -C(= O)-OH; -C(= O)-H; -S(= O)2-OH; - C(= NH)-NH2; -C(= NH)-NH-R9; -N= C(NH2)2; -N= C(NHR10)-(NHR11); - O-P(= O)2-O-R12; -NHR13; -NR14R15; -NH-C(= O)-R13; -OR16; -SR17; -C(= O)-NHR18; -C(= O)-NR19R20; -S(= O)2-NHR21; -S(= O)2-NR22R23; -C(= O)-OR24; -C(= O)-R25; -S(= O)-R26; or -S(= O)2-R27 or for a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical; R6 stands in each case for hydrogen or for a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical; R7 stands for hydrogen or -OH; or R6 and R7 each form, together with the interconnecting carbon atom as ring member, a saturated or unsaturated, unsubstituted or at least monosubstituted three-membered, four-membered, five-membered, or six-membered cycloaliphatic radical; R8 stands for -SF5; -O-CF3; -CF3; -O-CFH2; -O-CF2 H; -CFH2; -CF2 H; or for an unsubstituted or at least monosubstituted tert-butyl radical; T stands for C-R35 and U stands for C-R36 and V stands for N and W stands for C-R38 or T stands for C-R35 and U stands for N and V stands for C-R37 and W stands for C-R38 or T stands for N and U stands for C-R36 and V stands for C-R37 and W stands for C-R38 or T stands for N and U stands for N and V stands for C-R37 and W stands for C-R38 or T stands for N and U stands for C-R36 and V stands for N and W stands for C-R38 or T stands for C-R35 and U stands for N and V stands for N and W stands for C-R38 or T stands for C-R35 and U stands for C-R36 and V stands for C-R37 and W stands for C-R38; R9 R10 p11 R12 R13 R14 R15 R16 R17 R18 R19 p20 R21 R22 R23 R24 R25 R26 and R27 each independently stand for a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical; for an unsaturated or saturated, unsubstituted or at least monosubstituted, three-membered, four-membered, five-membered, six-membered, seven-membered, eight-membered, or nine-mem be red cycloaliphatic radical optionally containing at least one heteroatom as ring member, which can be condensed with a saturated or unsaturated, unsubstituted or at least monosubstituted monocyclic or polycyclic ring system and/or can be bonded via a linear or branched, unsubstituted or at least monosubstituted C1-6 alkylene group or two to six-membered heteroalkylene group; or for an unsubstituted or at least monosubstituted five-membered to fourteen-membered aryl radical or heteroaryl radical, which can be condensed with a saturated or unsaturated, unsubstituted or at least monosubstituted monocyclic or polycyclic ring system and/or can be bonded via a linear or branched, unsubstituted or at least monosubstituted C1-6 alkylene group or two to six-membered heteroalkylene group; R35, R36, and R37 each independently stand for H; F; CI; Br; I; -SF5; -NO2; -CF3; -CN; - NH2; -OH; -SH; -C(= O)-NH2; -S(= O)2-NH2; -C(= O)-NH-OH; -C(= O)- OH; -C(= O)-H; -S(= O)2-OH; -NHR13; -NR14R15; -NH-C(= O)-R13; -OR16; -SR17; -C(= O)-NHR18; -C(= O)-NR19R20; -S(= O)2-NHR21; -S(= O)2- NR22R23; -C(= O)-OR24; -C(= O)-R25; -S(= O)-R26; -S(= O)2R27; for a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical; or for an unsubstituted or at least monosubstituted five-membered to fourteen-membered aryl radical or heteroaryl radical, which can be condensed with a saturated or unsaturated, unsubstituted or at least monosubstituted monocyclic or polycyclic ring system and/or can be bonded via a linear or branched, unsubstituted or at least monosubstituted C1-6-alkylene group or C2-6-alkenylene group or C2_6- alkynylene group; R38 stands for F; CI; Br; I; -SF5; -NO2; -CF3; -CF2 CI; -CN; -NH2; -OH; -SH; - C(= O)-NH2; -S(= O)2-NH2; -C(= O)-NH-OH; and -C(= O)-OH; -C(= O)- H; -S(= O)2-OH; -NHR39; -NR40R41; -OR42; -SR43; -C(= O)-NHR44; -C(= O)-NR45R46; -S(= O)2-NHR47; -S(= O)2-NR48R49; -C(= O)-OR50; -C(= O)- R51; -S(= O)-R52; -S(= O)2-R53; -C(= NH)-NH2; -C(= NH)-NH-R54; -N= C(NH2)2; -N= C(NHR55)-(NHR56) for a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical; for an unsaturated or saturated, unsubstituted or at least monosubstituted three-membered, four-membered, five-membered, six- membered, seven-membered, eight-membered, or nine-membered cycloaliphatic radical optionally exhibiting at least one heteroatom as ring member, each of which is bonded to the parent structure over a carbon atom in the ring of the cycloaliphatic radical and is condensed with a saturated or unsaturated, unsubstituted or at least monosubstituted monocyclic or polycyclic ring system and/or can be bonded via a linear or branched, unsubstituted or at least monosubstituted C1-6 alkylene group or C2-6 alkenylene group or C2-6 alkynylene group; or for an unsubstituted or at least monosubstituted five-membered to fourteen-membered aryl radical or heteroaryl radical, which can be condensed with a saturated or unsaturated, unsubstituted or at least monosubstituted monocyclic or polycyclic ring system and/or can be bonded via a linear or branched, unsubstituted or at least monosubstituted C1-6 alkylene group or C2-6 alkenylene group or C2-6- alkynylene group; R39 R40 R41 R42 R43 R44 R45 R46 R47 R48 R49 R50 R51 R52 R53 R54 R55 and R56 each independently stand for a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical; for an unsaturated or saturated, unsubstituted or at least monosubstituted, three-membered, four-membered, five-membered, six-membered, seven-membered, eight-membered, or nine-membered cycloaliphatic radical optionally containing at least one heteroatom as ring member, which can be condensed with a saturated or unsaturated, unsubstituted or at least monosubstituted monocyclic or polycyclic ring system and/or can be bonded via a linear or branched, unsubstituted or at least monosubstituted C1-6-alkylene group or two to six-membered heteroalkylene group; or for an unsubstituted or at least monosubstituted five-membered to fourteen-membered aryl radical or heteroaryl radical, which can be condensed with a saturated or unsaturated, unsubstituted or at least monosubstituted monocyclic or polycyclic ring system and/or can be bonded via a linear or branched, unsubstituted or at least monosubstituted C1-6-alkylene group or two to six-membered heteroalkylene group; or R40 and R41 form, together with the interconnecting nitrogen atom as ring member, a saturated or unsaturated four-membered, five-membered, six-membered, seven-membered, eight-membered, or nine-membered heterocycloaliphatic radical, which is unsubstituted or substituted by 1, 2, 3, 4, or 5 radicals R57 and optionally exhibits at least one further heteroatom as ring member, and which can be condensed with a saturated or unsaturated, unsubstituted or at least monosubstituted monocyclic or polycyclic ring system; R57 stands for -NHR58, -NR59R60, or for a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical; R58, R59, and R60 each independently stand for -C(= O)-R61; for a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical or for an unsubstituted or at least monosubstituted five-membered to fourteen-membered aryl radical or heteroaryl radical, which can be condensed with a saturated or unsaturated, unsubstituted or at least monosubstituted monocyclic or polycyclic ring system and/or can be bonded via a linear or branched, unsubstituted or at least monosubstituted C1-6 alkylene group or C2-6 alkenylene group or C2-6 alkynylene group; and R61 stands for a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical; each optionally in the form of one of the pure stereoisomers thereof, particularly enantiomers or diastereoisomers thereof, the racemates thereof or in the form of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in an arbitrary mixing ratio, or each in the form of corresponding salts, or each in the form of corresponding solvates; wherein the aforementioned aliphatic C1-10 radicals and tert-butyl radicals can each be optionally substituted by 1, 2, 3, 4, 5, 6, 7, 8, or 9 substituents independently selected from the group consisting of F, CI, Br, I, -CN, -NO2, -OH, -NH2, -SH, - O(C1-5 alkyl), -S(C1-5 alkyl), -NH(C1-5 alkyl), -N(C1-5 alkyl)-(C1-5 alkyl), -C(= O)- O-(C1-5 alkyl), -O-C(= O)-(C1-5 alkyl), -O-phenyl, phenyl, -OCF3, and -SCF3; the aforementioned two to six-membered heteroalkylene groups, C1-6 alkylene groups, and C2-6 alkenylene groups and C2-6 alkynylene groups can each be optionally substituted by 1, 2, 3, 4, 5, 6, 7, 8, or 9 substituents independently selected from the group consisting of F, CI, Br, I, -CN, -NO2, -OH, -NH2, -SH, - 0(C1-5 alkyl), -S(C1-5 alkyl), -NH(C1-5 alkyl), -N(C1-5 alkyl)-(C1-5 alkyl), -OCF3, and -SCF3; the aforementioned heteroalkylene groups each optionally exhibit 1, 2, or 3 heteroatom(s) independently selected from the group consisting of oxygen, sulfur, and nitrogen (NH) as link(s); the aforementioned (hetero)cycloaliphatic radicals are optionally each substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of -C1-6-alkylene-OH, = CH2, -O-C1-5-alkyleneoxetanyl, -C1-5- alkylene-O-C1-5 alkylene-oxetanyl, -CH2-NH-C1-5 alkyl, -CH2-N(C1-5 alkyl)2, - N[C(= O)-C1-5 alkyl]-phenyl, -CH2-O-C1-5-alkyl, oxo (= O), thioxo (= S), F, CI, Br, I, -CN, -CF3, -SF5, -OH, -O-C1-5-alkyl, -O-C(= O)-C1-5-alkyl, -NH2, -NO2, -O- CF3, -S-CF3, -SH, -S-C1-5-alkyI), -C1-5-alkyI, -C(= O)-C1-5-alkyl), -C(= O)-OH, - C(= O)-O-C1-5-alkyl, -NH-C1-5-alkyl), -N(C1-5 alkyl)2, -NH-phenyl, -N(C1-5-alkyl)- phenyl, cyclohexyl, cyclopentyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)- thiadiazolyl, thiophenyl, phenethyl, piperidinyl, pyrrolidinyl, -(CH2)pyridinyl, pyridinyl, -O-phenyl, -O-benzyl, phenyl, and benzyl, and the cyclic moiety of the radicals oxetanyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, -N[C(= O)-C1-5-alkyl]-phenyl, -NH-phenyl, -N(C1-5 alkyl)- phenyl, -(CH2)-pyridinyl, pyridinyl, -O-phenyl, -O-benzyl, phenyl, and benzyl can each be substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of F, CI, Br, -OH, -CF3, -SF5, -CN, -NO2, -d-5-alkyl, - O-C1-5-alkyl, -O-CF3, -S-CF3, phenyl, and -O-benzyl, and, unless otherwise stated, the aforementioned (hetero)cycloaliphatic radicals can each optionally exhibit 1, 2, or 3 (further) heteroatom(s) independently selected from the group consisting of oxygen, nitrogen, and sulfur; the rings of the aforementioned monocyclic or polycyclic ring systems can each be optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of oxo (= O), thioxo (= S), F, CI, Br, I, -CN, - CF3, -SF5, -OH, -O-C1-5-alkyl, -NH2, -NO2, -O-CF3, -S-CF3, -SH, -S-C1-5-alkyl, - C1-5-alkyl, -C(= O)-C1-5-alkyl, -C(= O)-OH, -C(= O)-O-C1-5-alkyl), -NH-C1-5-alkyl, -N(C1-5-alkyl)2, -O-phenyl, -O-benzyl, phenyl, and benzyl, and the cyclic moiety of the radicals -O-phenyl, -O-benzyl, phenyl, and benzyl can each be substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of F, CI, Br, -OH, -CF3, -SF5, -CN, -NO2, -C1-5-alkyl, -O-C1-5- alkyl, -O-CF3, -S-CF3, phenyl, and -O-benzyl, and the rings of the aforementioned monocyclic or polycyclic ring systems are each five-membered, six-membered, or seven-membered and can each optionally exhibit 1, 2, 3, 4, or 5 heteroatom(s) as ring member(s), which are independently selected from the group consisting of oxygen, nitrogen, and sulfur; and the aforementioned aryl radicals or heteroaryl radicals can each be optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of F, CI, Br, I, -CN, -CF3, -SF5, -OH, -O-C1-5-alkyl, - NH2, -NO2, -O-CF3, -S-CF3, -SH, -S-C1-5-alkyI, -C1-5-alkyl, -C(= O)-OH, -C(= O)-O-C1-5-alkyl, -NH-C1-5-alkyl), -N(C1-5-alkyl)2, -NH-S(= O)2-C1-5-alkyl, -NH- C(= O)-O-C1-5-alkyl, -C(= O)-H, -C(= O)-C1-5-alkyl, -C(= O)-NH2, -C(= O)-NH- C1-5-alkyl, -C(= O)-N-(C1-5 alkyl)2, -O-phenyl, -O-benzyl, phenyl, and benzyl, and the cyclic moiety of the radicals -O-phenyl, -O-benzyl, phenyl, and benzyl can each be substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of F, CI, Br, -OH, -CF3, -SF5, -CN, -NO2, -C1-5-alkyl, - O-C1-5-alkyl, -O-CF3, -S-CF3, phenyl, and -O-benzyl, and the aforementioned heteroaryl radicals can each optionally exhibit 1,2,3, 4, or 5 heteroatom(s) independently selected from the group consisting of oxygen, nitrogen, and sulfur as ring member(s). The compounds according to claim 1, characterized in that n stands for 0, 1, 2, 3, or 4; R1 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; and -NH2; -OH; -SH; -C(=O)- NH2; -S(=O)2-NH2; -C(=O)-NH-OH; -C(=O)-OH; -C(=O)-H; -S(=O)2-OH; -NHR13; -NR14R15; -NH-C(=O)-R13; -OR16; -SR17; -S(=O)-NR22R23; - S(=O)-R26; -S(=O)2-R27 or for a radical selected from the group consisting of methyl, -CF3, -CCI3, -CBr3, -CHF2, -CH2F, -CF2CI, -CCI2F, ethyl, -CF2-CH3, -CH2-CF3, -C2F5, -CH2-CCI3, -CH2-CBr3, -CHF-CF2CI, - CF2-CF2CI, -CFCI-CF2CI, n-propyl, -CF2-CF2-CF3, -CF(CF3)2, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl; R2 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(=O)-NH2; -S(=O)2-NH2; -C(=O)-NH-OH; -C(=O)-OH; -C(=O)-H; -S(=O)2-OH; - NHR13; -NR14R15; -NH-C(=O)-R13; -OR16; -SR17; -S(=O)-NR22R23; - S(=O)-R26; -S(=O)2-R27 or for a radical selected from the group consisting of methyl, -CF3, -CCI3, -CBr3, -CHF2, -CH2F, -CF2CI, -CCI2F, ethyl, -CF2-CH3, -CH2-CF3, -C2F5, -CH2-CCI3, -CH2-CBr3, -CHF-CF2CI, - CF2-CF2CI, -CFCI-CF2CI, n-propyl, -CF2-CF2-CF3, -CF(CF3)2, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl; R3 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(=O)-NH2; -S(=O)2-NH2; -C(=O)-NH-OH; -C(=O)-OH; -C(=O)-H; -S(=O)2-OH; - NHR13; -NR14R15; -NH-C(=O)-R13; -OR16; -SR17; -S(=O)-NR22R23; - S(=O)-R26; -S(=O)2-R27 or for a radical selected from the group consisting of methyl, -CF3, -CCI3, -CBr3, -CHF2, -CH2F, -CF2CI, -CCI2F, ethyl, -CF2-CH3, -CH2-CF3, -C2F5, -CH2-CCI3, -CH2-CBr3, -CHF-CF2CI, - CF2-CF2CI, -CFCI-CF2CI, n-propyl, -CF2-CF2-CF3, -CF(CF3)2, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl; R4 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(=O)-NH2; -S(=O)2-NH2; -C(=O)-NH-OH; -C(=O)-OH; -C(=O)-H; -S(=O)2-OH; - NHR13; -NR14R15; -NH-C(=O)-R13; -OR16; -SR17; -S(=O)-NR22R23; - S(=O)-R26; -S(=O)2-R27 or for a radical selected from the group consisting of methyl, -CF3, -CCI3, -CBr3, -CHF2, -CH2F, -CF2CI, -CCI2F, ethyl, -CF2-CH3, -CH2-CF3, -C2F5, -CH2-CCI3, -CH2-CBr3, -CHF-CF2CI, - CF2-CF2CI, -CFCI-CF2CI, n-propyl, -CF2-CF2-CF3, -CF(CF3)2, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl; R5 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(=O)-NH2; -S(=O)2-NH2; -C(=O)-NH-OH; -C(=O)-OH; -C(=O)-H; -S(=O)2-OH; - NHR13; -NR14R15; -NH-C(=O)-R13; -OR16; -SR17; -S(=O)-NR22R23; - S(=O)-R26; -S(=O)2-R27 or for a radical selected from the group consisting of methyl, -CF3, -CCI3, -CBr3, -CHF2, -CH2F, -CF2CI, -CCI2F, ethyl, -CF2-CH3, -CH2-CF3, -C2F5, -CH2-CCI3, -CH2-CBr3, -CHF-CF2CI, - CF2-CF2CI, -CFCI-CF2CI, n-propyl, -CF2-CF2-CF3, -CF(CF3)2, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl; R6 stands for hydrogen or for an alkyl radical selected from the group consisting of-CH2-OH, -CH2-CH2-OH, -CH2-CH2-CH2-OH, -CH2-CH2- CH2-CH2-OH, isopropyl, n-butyl, sec-butyl, isobutyl, methyl, ethyl, and n-propyl; R7 stands for hydrogen or-OH; or R6 and R7 form, together with the interconnecting carbon atom as ring member, a radical selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl; R8 stands for -SF5; -O-CF3; -O-CFH2; -O-CF2H; -CFH2; -CF2H; -CF3; or for a tert-butyl radical, each of which can be unsubstituted or substituted by 1, 2, 3, 4, 5, 6, 7, 8, or 9 substituents independently selected from the group consisting of F, CI, Br, I, -CN, -NO2, -OH, -NH2, -SH, -O-CH3, -O- C2H5, -O-CH(CH3)2, -NH-CH3, and -NH-C2H5; T stands for C-R35 and U stands for C-R36 and V stands for N and W stands for C-R38 or T stands for C-R35 and U stands for N and V stands for C-R37 and W stands for C-R38 or T stands for N and U stands for C-R36 and V stands for C-R37 and W stands for C-R38 or T stands for N and U stands for N and V stands for C-R37 and W stands for C- R38 or T stands for N and U stands for C-R36 and V stands for N and W stands for C- R38 or T stands for C-R35 and U stands for N and V stands for N and W stands for C- R38 or T stands for C-R35 and U stands for C-R36 and V stands for C-R37 and W stands for C-R38 R13, R14, R15, R16, R17, R26, and R27 each independently stand for a radical selected from the group consisting of methyl, -CF3, - CCI3, -CBr3, -CHF2, -CH2F, -CF2CI, -CCI2F, -CH2-CN, -CH2-O-CH3, - CH2-O-CF3, -CH2-SF3, ethyl, -CF2-CH3, -CH2-CF3, -C2F5, -CH2-CCI3, - CH2-CBr3, -CHF-CF2CI, -CF2-CF2CI, -CFCI-CF2CI, -CH2-CH2-CN, n- propyl, -CF2-CF2-CF3, -CF(CF3)2, isopropyl, -CH2-CH2-CH2-CN, -CH2-O- CH2-CH3, -CH2-CH2-SF3, -CH2-CH2-OCF3, -CH(CH3)-(O-CH3), - CH(CH3)-(S-CH3), n-butyl, -CF2-CF2-CF2-CF3, -CH2-CH2-CH2-CH2-CN, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-heptyl, 4-heptyl, n- octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl, -CH2-CH2-O-CH3, -CH2-CH2-O-C2H5, -CH2-CH2- CH2-O-CH3, ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl, and 3- pentenyl; for a radical selected from the group consisting of 2,3-dihydro-1H- indenyl, cyclopropyl, oxetanyl, cyclobutyl, cyclopentyl, cyclohexyl, imidazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl, and thiomorpholinyl, each of which can be bonded via a -CH2-O-, -CH2- CH2-O-, -CH2-CH2-O-CH2-, -CH2-CH(CH3)-O-CH2-, -(CH2)-, -(CH2)2 or - (CH2)3 group and/or can each be unsubstituted or optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of oxo (=O), thioxo (=S), -OH, -O-CH3, -O-C2H5, -O- CH(CH3)2, -O-C(CH3)3, -O-CF3, -S-CF3, -SH, -S-CH3, -S-C2H5, -S- CH(CH3)2, -S-C(CH3)3, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec- butyl, isobutyl, tert-butyl, n-pentyl, -C(=O)-CH3, -C(=O)-C2H5, -C(=O)- CH(CH3)2, -C(=O)-C(CH3)3, -C(=O)-OH, -C(=O)-O-CH3, -C(=O)-O-C2H5, -C(=O)-O-CH(CH3)2, and -C(=O)-O-C(CH3)3; or for a radical selected from the group consisting of phenyl, naphthyl, thiophenyl, furanyl, pyrrolyl, pyrazolyl, pyrazinyl, pyranyl, triazolyl, pyridinyl, imidazolyl, thiazolyl, oxazolyl, and isoxazolyl, and each radical can be bonded via a -(CH2)-, -(CH2)2 or -(CH2)3 group and/or can be unsubstituted or optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of F, CI, Br, I, -CN, - CF3, -SF5, -OH, -O-CH3, -O-C2H5, -O-CH(CH3)2, -O-C(CH3)3, -NH2, - NO2, -O-CF3, -S-CF3, -SH, -S-CH3, -S-C2H5, -S-CH(CH3)2, -S-C(CH3)3, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, -C(=O)-OH, -C(=O)-O-CH3, -C(=O)-O-C2H5, -C(=O)-O- CH(CH3)2, -C(=O)-O-C(CH3)3, -NH-CH3, -NH-C2H5, -NH-C(CH3)3, - N(CH3)2, -N(C2H5)2, -N(CH3)-(C2H5), -NH-C(=O)-O-CH3, -NH-C(=O)-O- C2H5, -NH-C(=O)-O-C(CH3)3, -C(=O)-H, -C(=O)-CH3, -C(=O)-C2H5, - C(=O)-CH(CH3)2, -C(=O)-C(CH3)3, -C(=O)-NH2, -C(=O)-NH-CH3, - C(=O)-NH-C2H5, -C(=O)-N(CH3)2, -C(=O)-N(C2H5)2, -O-phenyl, -O- benzyl, phenyl, and benzyl; R35, R36, and R37 each independently stand for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(=O)-NH2; -S(=O)2-NH2; -C(=O)-NH-OH; -C(=O)-OH; -C(=O)-H; -S(=O)2-OH; -NHR13; -NR14R15; -OR16; -SR17; -S(=O)-R25; - S(=O)2-R26; for a radical selected from the group consisting of-CH2-OH, methyl, -CF3, -CCI3, -CBr3, -CHF2, -CH2F, -CF2CI, -CCI2F, ethyl, -CF2- CH3, -CH2-CF3, -C2F5, -CH2-CCI3, -CH2-CBr3, -CHF-CF2CI, -CF2-CF2CI, -CFCI-CF2CI, n-propyl, -CF2-CF2-CF3, -CF(CF3)2, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl or for a phenyl radical, which are unsubstituted or can optionally be substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of F, CI, Br, I, -CN, -CF3, -SF5, -OH, -O-CH3, -O-C2H5, -O-CH(CH3)2, -O-C(CH3)3, -NH2, -NO2, -O-CF3, -S-CF3, -SH, -S-CH3, -S-C2H5, -S-CH(CH3)2, -S- C(CH3)3, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, and n-pentyl; R38 stands for -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(=O)-NH2; -S(=O)2-NH2; - C(=O)-NH-OH; -C(=O)-OH; -C(=O)-H; -S(=O)2-OH; -NHR39; -NR40R41; - OR42; -SR43; -C(=O)-OR50; -S(=O)-R52; -S(=O)2-R53; -C(=NH)-NH2; - C(=NH)-NH-R54; -N=C(NH2)2; -N=C(NHR55)-(NHR56); for a radical selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, imidazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl, and thiomorpholinyl, each of which is bonded to the basic framework via a carbon atom of the rings of the aforementioned radicals or via a - (CH=CH)-, -C≡C or -C≡C-CH2- group and is unsubstituted or can optionally be substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of-CN, -CH2-N(CH3)2, -CH2- N(C2H5)2, -CH2-NH-CH3, -CH2-NH-C2H5, -N-[C(=O)-C2H5]phenyl, -N- [C(=O)-CH3]phenyl, oxo (=O), thioxo (=S), -OH, -O-CH3, -O-C2H5, -O- CH(CH3)2, -O-C(CH3)3, -O-CF3, -S-CF3, -SH, -S-CH3, -S-C2H5, -S- CH(CH3)2, -S-C(CH3)3, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec- butyl, isobutyl, tert-butyl, n-pentyl, -C(=O)-CH3, -C(=O)-C2H5, -C(=O)- CH(CH3)2, -C(=O)-C(CH3)3, -C(=O)-OH, -C(=O)-O-CH3, -C(=O)-O-C2H5, -C(=O)-O-CH(CH3)2, and -C(=O)-O-C(CH3)3; or for a radical selected from the group consisting of (1,3)- benzodioxolyl, (1,4)-benzodioxanyl, tetrazolyl, (2,3)-dihydrothieno[3.4- b][1.4]dioxinyl, benzo[b]furanyl, phenyl, naphthyl, thiophenyl, furanyl, pyrrolyl, pyrazolyl, pyrazinyl, pyranyl, triazolyl, pyridinyl, imidazolyl, indolyl, isoindolyl, thiazolyl, oxazolyl, isoxazolyl, pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl, quinoxalinyl, quinolinyl, and isoquinolinyl, each of which can be bonded via a -(CH=CH)-, -C=C-, -(CH2)-, -(CH2)2- or - (CH2)3 group and/or is unsubstituted or can optionally be substituted by 1,2,3, 4, or 5 substituents independently selected from the group consisting of F, CI, Br, I, -CN, -CF3, -SF5, -OH, -O-CH3, -O-C2H5, -O- CH(CH3)2, -O-C(CH3)3, -NH2, -NO2, -O-CF3, -S-CF3, -SH, -S-CH3, -S- C2H5, -S-CH(CH3)2, -S-C(CH3)3, methyl, ethyl, n-propyl, isopropyl, n- butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, -C(=O)-OH, -C(=O)-O-CH3, -C(=O)-O-C2H5, -C(=O)-O-CH(CH3)2, -C(=O)-O-C(CH3)3, -NH-CH3, - NH-C2H5, -NH-C(CH3)3, -N(CH3)2, -N(C2H5)2, -N(CH3)-(C2H5), -NH- C(=O)-O-CH3, -NH-S(=O)2-CH3, -NH-S(=O2)-C2H5, -NH-S(=O)2- CH(CH3)2, -NH-C(=O)-O-C2H5, -NH-C(=O)-O-C(CH3)3, -C(=O)-H, - C(=O)-CH3, -C(=O)-C2H5, -C(=O)-CH(CH3)2, -C(=O)-C(CH3)3, -C(=O)- NH2, -C(=O)-NH-CH3, -C(=O)-NH-C2H5, -C(=O)-N(CH3)2) -C(=O)- N(C2H5)2, -O-phenyl, -O-benzyl, phenyl, and benzyl; R39, R40, and R41, R42, R43, R50, R52, R53, R54, R55, and R56 each independently stand for a radical selected from the group consisting of methyl, -CF3, - CCI3, -CBr3, -CHF2, -CH2F, -CF2CI, -CCI2F, -CH2-CN, -CH2-O-CH3, - CH2-O-CF3, -CH2-SF3, ethyl, -CF2-CH3, -CH2-CF3, -C2F5, -CH2-CCI3, - CH2-CBr3, -CHF-CF2CI, -CF2-CF2CI, -CFCI-CF2CI, -CH2-CH2-CN, n- propyl, -CF2-CF2-CF3, -CF(CF3)2, isopropyl, -CH2-CH2-CH2-CN, -CH2-O- CH2-CH3, -CH2-CH2-SF3, -CH2-CH2-OCF3, -CH(CH3)-(O-CH3), - CH(CH3)-(S-CH3), n-butyl, -CF2-CF2-CF2-CF3, -CH2-CH2-CH2-CH2-CN, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-heptyl, 4-heptyl, n- octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl, -CH2-CH2-O-CH3, -CH2-CH2-O-C2H5, -CH2-CH2- CH2-O-CH3, ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl, and 3- pentenyl; for a radical selected from the group consisting of 2,3-dihydro-1H- indenyl, cyclopropyl, oxetanyl, cyclobutyl, cyclopentyl, cyclohexyl, imidazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl, and thiomorpholinyl, each of which can be bonded via a -CH2-O-, -CH2- CH2-O-, -CH2-CH2-O-CH2-, -CH2-CH(CH3)-O-CH2-, -(CH2)-, -(CH2)2- or - (CH2)3 group and/or can each be unsubstituted or optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of oxo (=O), thioxo (=S), -OH, -O-CH3, -O-C2H5, -O- CH(CH3)2, -O-C(CH3)3, -O-CF3, -S-CF3, -SH, -S-CH3, -S-C2H5, -S- CH(CH3)2, -S-C(CH3)3, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec- butyl, isobutyl, tert-butyl, n-pentyl, -C(=O)-CH3, -C(=O)-C2H5, -C(=O)- CH(CH3)2, -C(=O)-C(CH3)3, -C(=O)-OH, -C(=O)-O-CH3, -C(=O)-O-C2H5, -C(=O)-O-CH(CH3)2, and -C(=O)-O-C(CH3)3; or for a radical selected from the group consisting of phenyl, naphthyl, thiophenyl, furanyl, pyrrolyl, pyrazolyl, pyrazinyl, pyranyl, triazolyl, pyridinyl, imidazolyl, thiazolyl, oxazolyl, and isoxazolyl, and each radical can be bonded via a -(CH2)-, -(CH2)2- or -(CH2)3 group and/or can each be unsubstituted or optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of F, CI, Br, I, -CN, - CF3, -SF5, -OH, -O-CH3, -O-C2H5, -O-CH(CH3)2, -O-C(CH3)3, -NH2, - NO2, -O-CF3, -S-CF3, -SH, -S-CH3, -S-C2H5, -S-CH(CH3)2, -S-C(CH3)3, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, -C(=O)-OH, -C(=O)-O-CH3, -C(=O)-O-C2H5, -C(=O)-O- CH(CH3)2, -C(=O)-O-C(CH3)3, -NH-CH3, -NH-C2H5, -NH-C(CH3)3, - N(CH3)2, -N(C2H5)2, -N(CH3)(C2H5), -NH-C(=O)-O-CH3, -NH-C(=O)-O- C2H5, -NH-C(=O)-O-C(CH3)3, -C(=O)-H, -C(=O)-CH3, -C(=O)-C2H5, - C(=O)-CH(CH3)2, -C(=O)-C(CH3)3, -C(=O)-NH2, -C(=O)-NH-CH3, - C(=O)-NH-C2H5, -C(=O)-N(CH3)2, -C(=O)-N(C2H5)2, -O-phenyl, -O- benzyl, phenyl, and benzyl; or R40 and R41 form, together with the interconnecting nitrogen atom as ring member, a radical selected from the group consisting of 3-aza- bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl, 3-aza-bicyclo[3.2.1]octyl, 6- aza-bicyclo[3.3.1]heptyl, 8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8- diazaspiro[4.5]dec-2-enyl, azocanyl, isoindolyl, indolyl, (1,2,3,6)- tetrahydropyridinyl, (4,5,6,7)-tetrahydroisoxazolo[5.4-c]pyridinyl, pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, azepanyl, diazepanyl, and thiomorpholinyl, of which the heterocycloaliphatic portion can in each case be unsubstituted or substituted by 1, 2, 3, 4, or 5 radicals R57; R57 stands for -NHR58, -NR59R60, or for an alkyl radical selected from the group consisting of-CF3, -CH2-CF3, methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, and isobutyl; R58, R59, and R60 each independently stand for -C(=O)-R61; or for an alkyl radical selected from the group consisting of-CF3, -CH2-CF3, methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, and isobutyl; or for a radical selected from the group consisting of phenyl, naphthyl, thiophenyl, furanyl, pyrrolyl, pyrazolyl, pyrazinyl, pyranyl, triazolyl, pyridinyl, imidazolyl, thiazolyl, oxazolyl, and isoxazolyl, and each radical can be bonded via a -(CH2)-, -(CH2)2- or -(CH2)3 group and/or can each be unsubstituted or optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of F, CI, Br, I, -CN, - CF3, -SF5, -OH, -O-CH3, -O-C2H5, -O-CH(CH3)2, -O-C(CH3)3, -NH2, - NO2, -O-CF3, -S-CF3, -SH, -S-CH3, -S-C2H5, -S-CH(CH3)2, -S-C(CH3)3, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, -C(=O)-OH, -C(=O)-O-CH3, -C(=O)-O-C2H5, -C(=O)-O- CH(CH3)2, -C(=O)-O-C(CH3)3, -NH-CH3, -NH-C2H5, -NH-C(CH3)3l - N(CH3)2, -N(C2H5)2, -N(CH3)-(C2H5), -NH-C(=O)-O-CH3, -NH-C(=O)-O- C2H5, -NH-C(=O)-O-C(CH3)3, -C(=O)-H, -C(=O)-CH3, -C(=O)-C2H5, - C(=O)-CH(CH3)2, -C(=O)-C(CH3)3, -C(=O)-NH2, -C(=O)-NH-CH3, - C(=O)-NH-C2H5, -C(=O)-N(CH3)2l -C(=O)-N(C2H5)2, -O-phenyl, -O- benzyl, phenyl, and benzyl; and R61 stands for an alkyl radical selected from the group consisting of - CF3, -CH2-CF3, methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec- butyl, and isobutyl; in each case optionally in the form of one of the pure stereoisomers thereof, particularly enantiomers or diastereoisomers, or the racemates thereof or in the form of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in each case in the form of corresponding solvates. 3. The compounds according to claim 1 or claim 2, characterized in that n stands for 0, 1, or 2; R1 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(=O)-R13; - OR16; -SR17; -S(=O)2-NR22R23; -S(=O)2-R27; or for a radical selected from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n- propyl, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl; R2 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(=O)-R13; - OR16; -SR17; -S(=O)2-NR22R23; -S(=O)2-R27; or for a radical selected from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n- propyl, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl; R3 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(=O)-R13; - OR16; -SR17; -S(=O)2-NR22R23; -S(=O)2-R27; or for a radical selected from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n- propyl, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl; R4 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(=O)-R13; - OR16; -SR17; -S(=O)2-NR22R23; -S(=O)2-R27; or for a radical selected from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n- propyl, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl; R5 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(=O)-R13; - OR16; -SR17; -S(=O)2-NR22R23; -S(=O)2-R27; or for a radical selected from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n- propyl, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl; R6 stands for hydrogen or for an alkyl radical selected from the group consisting of isopropyl, n-butyl, sec-butyl, isobutyl, methyl, ethyl, and n- propyl; R7 stands for hydrogen or -OH; or R6 and R7 form, together with the interconnecting carbon atom as ring member, a radical selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl; R8 stands for -SF5; -O-CF3; -CF3; tert-butyl or -C(CH3)2(CH2OH); T stands for C-R35 and U stands for C-R36 and V stands for N and W stands for C-R38 or T stands for C-R35 and U stands for C-R36 and V stands for C-R37 and W stands for C-R38; R13 R16 R17 R22 R23 and R27 egch independ ently stand for a radical selected from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, -CF2- CH3, -CH2-CF3, -C2F5, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl and ethenyl; R35, R36, and R37 each independently stand for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -OR16; -SR17; or for a radical selected from the group consisting of-CH2-OH, methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl; R38 stands for -SF5; -NO2; -CN; -NH2; -OH; -SH; -NHR39; -NR40R41; -OR42; - SR43; for a radical selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, imidazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl, and thiomorpholinyl, each of which is bonded to the parent structure via a carbon atom of the rings of the aforementioned residues and are unsubstituted or can optionally be substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of -CH2- N(CH3)2, -CH2-N(C2H5)2, -CH2-NH-CH3, -CH2-NH-C2H5, -N-[C(=O)- C2H5]phenyl, -N-[C(=0)-CH3]-phenyl, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl; or for a radical selected from the group consisting of phenyl, thiophenyl, furanyl, pyrrolyl, pyrazolyl, pyrazinyl, pyranyl, triazolyl, pyridinyl, imidazolyl, thiazolyl, oxazolyl, isoxazolyl, pyridazinyl, pyrazinyl, and pyrimidinyl, each of which can be optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of F, CI, Br, I, -CN, -CF3, -SF5, -OH, -O-CH3, -O-C2H5, -O-CH(CH3)2, -O- C(CH3)3, -O-CF3, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, and n-pentyl; R41, R42, R43, R42, and R43, each independently stand for a radical selected from the group consisting of methyl, -CH2- O-CH3, ethyl, n-propyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3- pentyl, n-hexyl, (3,3)-dimethylbutyl, -CH2-CH2-O-CH3, -CH2-CH2-O- C2H5, and -CH2-CH2-CH2-O-CH3; for a radical selected from the group consisting of 2,3-dihydro-1 H- indenyl, cyclopropyl, oxetanyl, cyclobutyl, cyclopentyl, cyclohexyl, imidazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl, and thiomorpholinyl, each of which can be optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert- butyl, and n-pentyl; or R40 and R41 form, together with the interconnecting nitrogen atom as ring member, a radical selected from the group consisting of 3-aza- bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl, 3-aza-bicyclo[3.2.1]octyl, 6- aza-bicyclo[3.3.1]heptyl, 8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8- diazaspiro[4.5]dec-2-enyl, azocanyl, isoindolyl, indolyl, (1,2,3,6)- tetrahydropyridinyl, (4,5,6,7)-tetrahydroisoxazolo[5.4-c]pyridinyl, pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, azepanyl, diazepanyl, and thiomorpholinyl, of which the heterocycloaliphatic moiety can in each case be unsubstituted or substituted by 1, 2, 3, 4, or 5 radicals R57; R57 stands for -NHR58, -NR59R60, or for an alkyl radical selected from the group consisting of-CF3, -CH2-CF3, methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, and isobutyl; R58, R59, and R60 each independently stand for -C(=O)-R61; for an alkyl radical selected from the group consisting of -CF3, -CH2-CF3, methyl, ethyl, n- propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, and isobutyl; or for a radical selected from the group consisting of phenyl and naphthyl, and the radical can each be bonded via a -(CH2)-, -(CH2)2- or -(CH2)3 group and/or can each be unsubstituted or optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of F, CI, Br, I, -CN, -CF3, -O-CH3, -O-C2H5, -O-CH(CH3)2, -O- C(CH3)3, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, and n-pentyl; and R61 stands for an alkyl radical selected from the group consisting of - CF3, -CH2-CF3, methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec- butyl, and isobutyl; in each case optionally in the form of one of the pure stereoisomers thereof, particularly enantiomers or diastereoisomers, or the racemates thereof or in the form of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in each case in the form of corresponding solvates. 4. The compounds according to any one or more of claims 1 to 3, characterized in that n stands for 0, 1, or 2; R1 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(=O)- R13; -OR16; -SR17; -S(=O)2-NR22R23 or-S(=O)2-R27; R2 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(=O)- R13; -OR16; -SR17; -S(=O)2-NR22R23 or -S(=O)2-R27; R3 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(=O)- R13; -OR16; -SR17; -S(=O)2-NR22R23 or-S(=O)2-R27; R4 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(=O)- R13; -OR16; -SR17; -S(=O)2-NR22R23 or-S(=O)2-R27; R5 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(=O)- R13; -OR16; -SR17; -S(=O)2-NR22R23 or-S(=O)2-R27; R6 stands for hydrogen or for an alkyl radical selected from the group consisting of isopropyl, n-butyl, sec-butyl, isobutyl, methyl, ethyl, and n- propyl; R7 stands for hydrogen or -OH; R8 stands for -SF5; -O-CF3; -CF3; tert-butyl; or -C(CH3)2(CH2OH); T stands for C-R35 and U stands for C-R36 and V stands for N and W stands for C-R38 or T stands for C-R35 and U stands for C-R36 and V stands for C-R37 and W stands for C-R38 R13, R16, R17, R22, R23 and R27 each independently stand for a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, and ethenyl; R35, R36, and R37 each stand for H; R38 stands for -NHR39; -NR40R41; -OR42; -SR43; R39, R42, and R43 each independently stand for a radical selected from the group consisting of methyl, ethyl, n-propyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n- hexyl, and (3,3)-dimethylbutyl; or for a radical selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl, each of which can be optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, and n-pentyl; or R40 and R41 form, together with the interconnecting nitrogen atom as ring member, a radical selected from the group consisting of pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, and azepanyl, of which the heterocycloaliphatic moiety can in each case be unsubstituted or substituted by 1, 2, 3, 4, or 5 radicals R57; and R57 stands for an alkyl radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, and isobutyl; each optionally in the form of one of the pure stereoisomers thereof, particularly enantiomers or diastereoisomers thereof, the racemates thereof or in the form of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in an arbitrary mixing ratio, or each in the form of corresponding salts, or each in the form of corresponding solvates. 5. The compounds according to any one or more of claims 1 to 4, characterized in that n stands for 1; R1 stands for H; F; CI; Br; or I; R2 stands for H; F; CI; Br; I; -OH; -NH2 or -OR16; R3 stands for H; F; CI; Br; I; -NO2; -OH; -NH2; -NH-C(=O)-R13; -OR16; - SR17; -S(=O)-NR22R23 or -S(=O)2-R27; R4 stands for H; F; CI; Br; I; methyl, -OH; -NH2 or -OR16; R5 stands for H; F; CI; Br or I; R6 stands for hydrogen or for an alkyl radical selected from the group consisting of isopropyl, n-butyl, sec-butyl, isobutyl, methyl, ethyl, and n- PropyI; R7 stands for hydrogen or -OH; R8 stands for -SF5; -O-CF3; -CF3; tert-butyl or -C(CH3)2(CH2OH); T stands for C-R35 and U stands for C-R36 and V stands for N and W stands for C-R38 or T stands for C-R35 and U stands for C-R36 and V stands for C-R37 and W stands for C-R38; R13 Rie R17 R22 R23 and R27 each independently stand for a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, and ethenyl; R35, R36, and R37 each stand for H; R38 stands for -NHR39; -NR40R41; -OR42; -SR43; R39, R42, and R43 each independently stand for a radical selected from the group consisting of methyl, ethyl, n-propyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n- hexyl, and (3,3)-dimethylbutyl; or for a radical selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl, each of which can be optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, and n-pentyl; or R40 and R41 form, together with the interconnecting nitrogen atom as ring member, a radical selected from the group comprising the group consisting pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, and azepanyl, the heterocycloaliphatic moiety of which can each be unsubstituted or substituted by 1, 2, 3, 4, or 5 radicals R57; and R57 stands for an alkyl radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, and isobutyl; each optionally in the form of one of the pure stereoisomers thereof, particularly enantiomers or diastereoisomers thereof, the racemates thereof or in the form of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in an arbitrary mixing ratio, or each in the form of corresponding salts, or each in the form of corresponding solvates. 6. The compounds of the general formula la according to any one or more of claims 1 to 3, in which D stands for N or CH; and R1, R2, R3, R4, R5, R8, and R42 have the meanings stated in claim 3; in each case optionally in the form of one of the pure stereoisomers thereof, particularly enantiomers or diastereoisomers, or the racemates thereof or in the form of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in each case in the form of corresponding solvates. 7. The compounds of the general formula la according to any one or more of claims 1 to 6, la, in which D stands for N or CH; and R1, R2, R3, R4, R5, R8, and R42 have the meanings stated in claim 4; in each case optionally in the form of one of the pure stereoisomers thereof, particularly enantiomers or diastereoisomers, or the racemates thereof or in the form of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in each case in the form of corresponding solvates. 8. The compounds of the general formula la according to any one or more of claims 1 to 7, in which D stands for N or CH; and R1, R2, R3, R4, R5, R8, and R42 have the meanings stated in claim 5; in each case optionally in the form of one of the pure stereoisomers thereof, particularly enantiomers or diastereoisomers, or the racemates thereof or in the form of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in each case in the form of corresponding solvates. 9. The compounds of the general formula lb according to any one or more of claims 1 to 3, in which D stands for N or CH; and R1, R2, R3, R4, R5, R8, and R42 have the meanings stated in claim 3; in each case optionally in the form of one of the pure stereoisomers thereof, particularly enantiomers or diastereoisomers, or the racemates thereof or in the form of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in each case in the form of corresponding solvates. 10. The compounds of the general formula lb according to any one or more of claims 1 to 9, in which D stands for N or CH; and R1, R2, R3, R4, R5, R8, and R42 have the meanings stated in claim 4; in each case optionally in the form of one of the pure stereoisomers thereof, particularly enantiomers or diastereoisomers, or the racemates thereof or in the form of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in each case in the form of corresponding solvates. 11. The compounds of the general formula lb according to any one or more of claims 1 to 10, in which D stands for N or CH; and R1, R2, R3, R4, R5, R8, and R42 have the meanings stated in claim 5; in each case optionally in the form of one of the pure stereoisomers thereof, particularly enantiomers or diastereoisomers, or the racemates thereof or in the form of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in each case in the form of corresponding solvates. 12. The compounds of the general formula Ic according to any one or more of claims 1 to 3, in which D stands for N or CH; and R1, R2, R3, R4, R5, R8, and R42 have the meanings stated in claim 3; in each case optionally in the form of one of the pure stereoisomers thereof, particularly enantiomers or diastereoisomers, or the racemates thereof or in the form of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in each case in the form of corresponding solvates. 13. The compounds of the general formula Ic according to any one or more of claims 1 to 12, in which D stands for N or CH; and R1, R2, R3, R4, R5, R8, and R42 have the meanings stated in claim 4; in each case optionally in the form of one of the pure stereoisomers thereof, particularly enantiomers or diastereoisomers, or the racemates thereof or in the form of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in each case in the form of corresponding solvates. 14. The compounds of the general formula Ic according to any one or more of claims 1 to 13, Ic, in which D stands for N or CH; and R1, R2, R3, R4, R5, R8, and R42 have the meanings stated in claim 5; in each case optionally in the form of one of the pure stereoisomers thereof, particularly enantiomers or diastereoisomers, or the racemates thereof or in the form of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in each case in the form of corresponding solvates. 15. The compounds according to any one or more of claims 1 to 14, selected from the group consisting of [1 ] 2-(4-Amino-3-fluorophenyl)-N-((2-(4-methylpiperidin-1 -yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [2] 2-(3,5-Dibromophenyl)-N-((2-(4-methylpiperidin-1 -yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)acetamide, [3] 2-(4-Amino-3-bromo-5-methoxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)acetamide, [4] 2-(3-Fluorophenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)acetamide, [5] 2-(2,4-Difluorophenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)acetamide, [6] 2-(2,6-Difluorophenyl)-N-((2-(4-methylpiperidin-1 -yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)acetamide, [7] 2-(2,5-Difluorophenyl)-N-((2-(4-methylpiperidin-1 -yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)acetamide, [8] 2-(4-Fluorophenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)acetamide, [9] 2-(4-Hydroxy-3-methoxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [10] 2-(3,5-Difluorophenyl)-N-((2-(4-methylpiperidin-1 -yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [11] 2-(3,4-Difluorophenyl)-N-((2-(4-methylpiperidin-1 -yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [12] 2-(4-Fluorophenyl)-N-((2-(4-methylpiperidin-1 -yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [13] 2-(3-Fluorophenyl)-N-((2-(4-methylpiperidin-1 -yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [14] 2-(3,4-Diaminophenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [15] N-(2-Butoxy-6-tert-butylpyridin-3-ylmethyl)-2-(3,4-diamino-phenyl)- propionamide, [16] N-((6-tert-Butyl-2-(4-methylpiperidin-1-yl)pyridin-3-yl)methyl)-2-(3,4- diaminophenyl)propanamide, [17] N-((6-tert-Butyl-2-(cyclohexylthio)pyridin-3-yl)methyl)-2-(3,4- diaminophenyl)propanamide, [18] 2-(4-Acetamido-3-fluorophenyl)-N-((2-(4-methylpiperidin-1 -yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [19] 2-(3,5-Dibromo-4-hydroxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [20] 2-(4-Amino-3,5-dibromophenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [21] 2-(3-Bromo-4-hydroxy-5-methoxyphenyl)-N-((2-(4-methylpiperidin-1-yl)- 6-(trifluoromethyl)pyridin-3-yl)methyl)acetamide, [22] 2-(4-Amino-3,5-dibromophenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)acetamide, [23] 2-(3,5-Dibromo-4-hydroxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)acetamide, [24] 2-(3-Amino-4-hydroxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [25] 2-(3,5-Dibromo-phenyl)-N-(4-methyl-6'-trifluoromethyl-3,4,5,6- tetrahydro-2H-[1,2']bipyridinyl-3'-ylmethyl)-acetamide. [26] 2-(4-Amino-3,5-difluorophenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [27] 2-(3-Fluoro-5-hydroxy-4-nitrophenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [28] 2-(3-Chloro-4-(methylthio)phenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [29] 2-(3-Chloro-4-(methylsulfonyl)phenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [30] 2-(3-Fluoro-4-(methylthio)phenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [31] 2-(3-Fluoro-4-(methylsulfonyl)phenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [32] 2-(4-(N,N-Dimethylsulfamoyl)-3-fluorophenyl)-N-((2-(4-methylpiperidin- 1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide, [33] N-(2-Fluoro-4-(1 -((2-(4-methylpiperidin-1 -yl)-6-(trifluoromethyl)pyridin-3- yl)methylamino)-1-oxopropane-2-yl)phenyl)acrylamide, [34] N-(2-Fluoro-6-iodo-4-(1-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methylamino)-1-oxopropane-2- yl)phenyl)acrylamide, [35] 2-(4-Methoxy-3,5-dimethylphenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [36] 2-(3,5-Difluoro-4-methoxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [37] 2-(4-Hydroxy-3,5-dimethylphenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, [38] 2-(3,5-Difluoro-4-hydroxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6- (trifluoromethyl)pyridin-3-yl)methyl)propanamide, in each case optionally in the form of one of the pure stereoisomers thereof, particularly enantiomers or diastereoisomers, or the racemates thereof or in the form of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in each case in the form of corresponding solvates. 16. The compounds according to any one or more of claims 1 to 15, characterized in that, in the FLIPR assay using CHO-K1 cells, which have been transfected with the human VR1 gene in a concentration below 2000 nM, preferably below 1000 nM, more preferably below 300 nM, even more preferably below 100 nM, still more preferably below 75 nM, very preferably below 50 nM and most preferably below 10 nM, they cause a 50 percent displacement of capsaicin present in a concentration of 100 nM. 17. A process for the production of a compound according to any one or more of claims 1 to 16, characterized in that at least one compound of the general formula II, in which R8, U, T, V, and W have the meanings stated in any one or more of claims 1 to 16, m stands for 0, 1, 2, or 3, and R stands for hydrogen or for a linear or branched C1-6 alkyl radical, in a reaction medium, in the presence of at least one reducing agent, preferably in the presence of at least one reducing agent selected from the group consisting of sodium hydride, sodium, potassium hydride, lithium aluminum hydride, sodium tetrahydridoborate, and di(isobutyl)aluminum hydride is converted to at least one compound of the general formula III, in which R8, U, T, V, and W have the meanings stated in any one or more of claims 1 to 16 and m stands for 0, 1, 2, or 3, and this is optionally purified and/or isolated, and at least one compound of the general formula III is converted, in a reaction medium in the presence of diphenylphosphorylazide or in the presence of HN3, to at least one compound of the general formula IV, in which R8, U, T, V, and W have the meanings stated in any one or more of claims 1 to 16 and m stands for 0, 1, 2, or 3, and this is optionally purified and/or isolated, and at least one compound of the general formula IV is converted, in a reaction medium in the presence of at least one reducing agent, preferably in the presence of at least one reducing agent selected from the group consisting of sodium hydride, potassium hydride, lithium aluminum hydride, sodium tetrahydridoborate, and di(isobutyl)aluminum hydride, or in a reaction medium in the presence of a catalyst, preferably in the presence of a catalyst based on platinum or palladium, more preferably in the presence of palladium-on-charcoal, and in the presence of hydrogen or in the presence of hydrazine, or in a reaction medium in the presence of triphenylphosphine to at least one compound of the general formula V, in which R8, U, T, V, and W have the meanings stated in any one or more of claims 1 to 16 and m stands for 0, 1, 2, or 3, and this is optionally purified and/or isolated, or at least one compound of the general formula VI VI, in which R8, U, T, V, and W have the meanings stated in any one or more of claims 1 to 16 and m stands for 0, 1,2, or 3, in a reaction medium is converted, in the presence of at least one catalyst, preferably in the presence of at least one catalyst based on palladium or platinum, more preferably in the presence of palladium-on-charcoal, under a blanket of hydrogen, optionally in the presence of at least one acid, preferably in the presence of hydrochloric acid, or in the presence of at least one reducing agent selected from the group consisting of BH3.S(CH3)2, lithium aluminum hydride, and sodium tetrahydridoborate, optionally in the presence of NiCI2, to form at least one compound of the general formula V, optionally in the form of a corresponding salt, preferably in the form of a corresponding hydrochloride, and this is optionally purified and/or isolated, and at least one compound of the general formula V is caused to react with at least one compound of the general formula VII, VII, in which R1, R2, R3, R4, R5, R6, and R7 have the meanings stated in any one or more of claims 1 to 16, in a reaction medium, optionally in the presence of at least one suitable coupling agent, optionally in the presence of at least one base, or with at least one compound of the general formula VIII, in which R1, R2, R3, R4, R5, R6, and R7 have the meanings stated in any one or more of claims 1 to 16 and LG stands for a leaving group, preferably for a chlorine or bromine atom, in a reaction medium, optionally in the presence of at least one base, to form at least one compound of the general formula I, in which T, U, V, W, R1, R2, R3, R4, R5, R6, R7, and R8, have the meanings stated in any one or more of claims 1 to 16 and n stands for 1, 2, 3, or 4, and this is optionally purified and/or isolated. 18. A process for the production of at least one compound according to any one or more of claims 1 to 16, characterized in that at least one compound of the general formula X, in which R8, U, T, V, and W have the meanings stated in any one or more of claims 1 to 16, is caused to react with at least one compound of the general formula VII, in which R1, R2, R3, R4, R5, R6, and R7, have the meanings stated in any one or more of claims 1 to 16, in a reaction medium, optionally in the presence of at least one suitable coupling agent, optionally in the presence of at least one base, or with at least one compound of the general formula VIII, in which R1, R2, R3, R4, R5, R6, and R7 have the meanings stated in any one or more of claims 1 to 16 and LG stands for a leaving group, preferably for a chlorine or bromine atom, in a reaction medium, optionally in the presence of at least one base, to form at least one compound of the general formula Im, in which T, U, V, W, R1, R2, R3, R4, R5, R6, R7, and R8 have the meanings stated in any one or more of claims 1 to 16, and this is optionally purified and/or isolated. 19. A pharmaceutical comprising at least one compound according to any one or more of claims 1 to 16 and optionally one or more physiologically compatible adjuvants. 20. The pharmaceutical according to claim 19 for the treatment and/or prophylaxis of any one or more of the disorders selected from the group consisting of pain, preferably pain selected from the group consisting of acute pain, chronic pain, neuropathic pain and visceral pain; arthralgia; hyperalgesia; allodynia; causalgia; and migraine. 21. The pharmaceutical according to claim 19 for the treatment and/or prophylaxis of any one or more of the disorders selected from the group consisting of states of depression; nervous disorders; neurotraumas; neurodegenerative disorders, preferably selected from the group consisting of multiple sclerosis, Morbus Alzheimer, Morbus Parkinson, and Morbus Huntington; cognitive dysfunctions, preferably cognitive deficiency states, more preferably memory defects; and epilepsy. 22. The pharmaceutical according to claim 19 for the treatment and/or prophylaxis of any one or more of the disorders selected from the group consisting of respiratory tract diseases, preferably selected from the group consisting of asthma, bronchitis and pneumonia; coughing; urinary incontinence; an overactive bladder (OAB); disorders and/or injuries of the gastrointestinal tract; duodenal ulcers; gastric ulcers; colitis syndrome; apoplectic strokes; eye irritations; cutaneous irritations; neurotic skin conditions; allergic skin diseases; psoriasis; vitiligo; Herpes simplex; inflammations, preferably inflammation of the intestine, the eyes, the bladder, the skin, or the nasal mucosa; diarrhea; pruritus; osteoporosis; arthritis; osteoarthritis; rheumatic disorders; food intake disorders, preferably selected from the group consisting of bulimia, cachexia, anorexia, and obesity; medicine addiction; medicine abuse; withdrawal phenomena following medicine addiction; tolerance development to medicines, particularly to natural or synthetic opioids; drug addiction; drug abuse; withdrawal phenomena following drug addiction; alcohol addiction; alcohol abuse and withdrawal phenomena following alcohol addiction; for diuresis; for antinatriuresis; for affection of the cardiovascular system; for vigilance enhancement; for treatment of wounds and/or burning; for treatment of severed nerves; for libido enhancement; for modulation of movement activity; for anxiolysis; for local anesthesia and/or for inhibition of undesirable side effects, preferably selected from the group consisting of hyperthermia, hypertension, and bronchial constriction, as caused by administration of vanilloid receptor 1 (VR1/TRPV1 receptor) agonists, preferably selected from the group consisting of capsaicin, resiniferatoxin, olvanil, arvanil, SDZ-249665, SDZ-249482, nuvanil, and capsavanil. 23. The use of at least one compound according to any one or more of claims 1 to 16 for the production of a pharmaceutical for the treatment and/or prophylaxis of any one or more of the disorders selected from the group consisting of pain, preferably pain selected from the group consisting of acute pain, chronic pain, neuropathic pain, and visceral pain; arthralgia; hyperalgesia; allodynia; causalgia and migraine. 24. The use of at least one compound according to any one or more of claims 1 to 16 for the production of a pharmaceutical for the treatment and/or prophylaxis of any one or more of the disorders selected from the group consisting of states of depression; nervous disorders; neurotraumas; neurodegenerative disorders, preferably selected from the group consisting of multiple sclerosis, Morbus Alzheimer, Morbus Parkinson, and Morbus Huntington; cognitive dysfunctions, preferably cognitive deficiency states, more preferably memory defects; and epilepsy. 25. The use of at least one compound according to any one or more of claims 1 to 10 for the production of a pharmaceutical for the treatment and/or prophylaxis of any one or more of the disorders selected from the group consisting of. respiratory tract diseases, preferably selected from the group consisting of asthma, bronchitis and pneumonia; coughing; urinary incontinence; an overactive bladder (OAB); disorders and/or injuries of the gastrointestinal tract; duodenal ulcers; gastric ulcers; colitis syndrome; apoplectic strokes; eye irritations; cutaneous irritations; neurotic skin conditions; allergic skin diseases; psoriasis; vitiligo; Herpes simplex; inflammation, preferably inflammation of the intestine, the eyes, the bladder, the skin, or the nasal mucosa; diarrhea; pruritus; osteoporosis; arthritis; osteoarthritis; rheumatic disorders; food intake disorders, preferably selected from the group consisting of bulimia, cachexia, anorexia, and obesity; medicine addiction; medicine abuse; withdrawal phenomena following medicine addiction; tolerance development to pharmaceuticals, particularly to natural or synthetic opioids; drug addiction; drug abuse; withdrawal phenomena following drug addiction; alcohol addiction; alcohol abuse and withdrawal phenomena following alcohol addiction; for diuresis; for antinatriuresis; for affection of the cardiovascular system; for vigilance enhancement; for treatment of wounds and/or burning; for treatment of severed nerves; for libido enhancement; for modulation of movement activity; for anxiolysis; for local anesthesia and/or for inhibition of undesirable side effects, preferably selected from the group consisting of hyperthermia, hypertension, and bronchial constriction, as caused by administration of vanilloid receptor 1 (VR1/TRPV1 receptor) agonists, preferably selected from the group consisting of capsaicin, resiniferatoxin, olvanil, arvanil, SDZ-249665, SDZ-249482, nuvanil, and capsavanil. The present invention relates to novel vanilloid receptor ligands, to processes for the production thereof, to pharmaceuticals containing said compounds and to the use of said compounds for the production of pharmaceuticals.

Full Text

Novel vanilloid receptor ligands and the use thereof for the production of
pharmaceuticals
The present invention relates to novel vanilloid receptor ligands, to processes for the
production thereof, to pharmaceuticals containing said compounds and to the use of
said compounds for the production of pharmaceuticals.
The treatment of pain, particularly neuropathic pain, is of great significance in the
medical field. There is a global need for effective pain therapies. The urgent need for
action to provide a patient-friendly und targeted treatment of chronic and non-chronic
states of pain, this being taken to mean the successful und satisfactory treatment of
pain for patients, is documented by the large number of scientific papers which have
recently appeared in the field of applied analgesics or in basic research concerning
nociception.
A suitable starting point for the treatment of pain; particularly of pain selected from
the group consisting of acute pain, chronic pain, neuropathic pain, and visceral pain,
particularly preferably neuropathic pain; is the vanilloid receptor of subtype 1
(VR1/TRPV1), frequently also designated as the capsaicin receptor. This receptor is
stimulated, inter alia, by vanilloids such as capsaicin, heat, and protons and plays a
central part in the generation of pain. Furthermore, it is significant for a large number
of other physiological and pathophysiological processes such as migraine; states of
depression; neurodegenerative disorders; cognitive disorders; anxiety; epilepsy;
coughing; diarrhea; pruritus; inflammations; disorders of the cardiovascular system;

food intake disorders; medicine addiction; medicine abuse and, in particular, urinary
incontinence.
It is thus an object of the invention to provide novel compounds which are particularly
suitable for use as pharmacologically active substances in pharmaceuticals,
preferably in pharmaceuticals for treatment of disorders or diseases that are at least
partially mediated by vanilloid receptors 1 (VR1/TRPV1 receptors).
It has now been found, surprisingly, that the substituted compounds of the general
formula I stated below show excellent affinity to the vanilloid receptor of subtype 1
(VR1/TRPV1 receptor) and are therefore particularly suitable for the prophylaxis
and/or treatment of disorders or diseases which are at least partially mediated by
vanilloid receptors 1 (VR1/TRPV1). The substituted compounds of the general
formula I given below also show anti-inflammatory activity.
It is thus an object of the present invention to provide substituted compounds of the
general formula I,

in which

0 stands for 0, 1,2, 3, or 4;
R1 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(= O)-NH2; -S(=
O)2-NH2; -C(= O)-NH-OH; -C(= O)-OH; -C(= O)-H; -S(= O)2-OH; -C(= NH)-
NH2; -C(= NH)-NH-R9; -N= C(NH2)2; -N= C(NHR10)-(NHR11); -O-P(= 0)2-O-
R12; -NHR13; -NR14R15; -NH-C(=O)-R13; -OR16; -SR17; -C(= O)-NHR18; -C(=
O)-NR19R20; -S(= O)2-NHR21; -S(= O)2-NR22R23; -C(= O)-OR24; -C(= O)-R25; -
S(= O)-R26; or -S(= O)2-R27 or for a linear or branched, saturated or
unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical;
R2 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(= O)-NH2; -S(=
O)2-NH2; -C(= O)-NH-OH; -C(= O)-OH; -C(= O)-H; -S(= O)2-OH; -C(= NH)-
NH2; -C(= NH)-NH-R9; -N= C(NH2)2; -N= C(NHR10)-(NHR11); -O-P(= 0)2-O-
R12; -NHR13; -NR14R15; -NH-C(= O)-R13; -OR16; -SR17; -C(= O)-NHR18; -C(=
O)-NR19R20; -S(= O)2-NHR21; -S(= O)2-NR22R23; -C(= O)-OR24; -C(= O)-R25; -
S(= O)-R26; or -S(= O)2-R27 or for a linear or branched, saturated or
unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical;
R3 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(= O)-NH2; -S(=
O)2-NH2; -C(= O)-NH-OH; -C(= O)-OH; -C(= 0)-H; -S(= O)2-OH; -C(= NH)-
NH2; -C(= NH)-NH-R9; -N= C(NH2)2; -N= C(NHR10)-(NHR11); -O-P(= O)2-O-
R12; -NHR13; -NR14R15; -NH-C(= O)-R13; -OR16; -SR17; -C(= O)-NHR18; -C(=
O)-NR19R20; -S(= O)2-NHR21; -S(= O)2-NR22R23; -C(= O)-OR24; -C(= O)-R25; -
S(= O)-R26; or -S(= O)2-R27 or for a linear or branched, saturated or
unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical;

R4 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(= O)-NH2; -S(=
O)2-NH2; -C(= O)-NH-OH; -C(= O)-OH; -C(= O)-H; -S(= O)2-OH; -C(= NH)-
NH2; -C(= NH)-NH-R9; -N= C(NH2)2; -N= C(NHR10)-(NHR11); -O-P(= O)2-O-
R12; -NHR13; -NR14R15; -NH-C(= 0)-R13; -OR16; -SR17; -C(= O)-NHR18; -C(=
O)-NR19R20; -S(= O)2-NHR21; -S(= O)2-NR22R23; -C(= O)-OR24; -C(= O)-R25; -
S(= O)-R26; or -S(= O)2-R27 or for a linear or branched, saturated or
unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical;
R5 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(= O)-NH2; -S(=
O)2-NH2; -C(= O)-NH-OH; -C(= O)-OH; -C(= O)-H; -S(= O)2-OH; -C(= NH)-
NH2; -C(= NH)-NH-R9; -N= C(NH2)2; -N= C(NHR10)-(NHR11); -O-P(= O)2-O-
R12; -NHR13; -NR14R15; -NH-C(= O)-R13; -OR16; -SR17; -C(= O)-NHR18; -C(=
O)-NR19R20; -S(= O)2-NHR21; -S(= O)2-NR22R23; -C(= O)-OR24; -C(= O)-R25; -
S(= O)-R26; or -S(= O)2-R27 or for a linear or branched, saturated or
unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical;
R6 stands in each case for hydrogen or for a linear or branched, saturated or
unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical;
R7 stands for hydrogen or -OH;
or R6 and R7 form, together with the interconnecting carbon atom as ring member,
a saturated or unsaturated, unsubstituted or at least monosubstituted three-
membered, four-membered, five-membered, or six-membered cycloaliphatic
radical;

R8 stands for -SF5; -O-CF3; -CF3; -O-CFH2; -O-CF2 H; -CFH2; -CF2 H; or for an
unsubstituted or at least monosubstituted tert-butyl radical;
T stands for C-R35 and U stands for C-R36 and V stands for N and W stands for C-R38
Or
T stands for C-R35 and U stands for N and V stands for C-R37 and W stands for C-R38
Or
T stands for N and U stands for C-R36 and V stands for C-R37 and W stands for C-R38
Or
T stands for N and U stands for N and V stands for C-R37 and W stands for C-R38
Or
T stands for N and U stands for C-R36 and V stands for N and W stands for C-R38
Or
T stands for C-R35 and U stands for N and V stands for N and W stands for C-R38
Or
T stands for C-R35 and U stands for C-R36 and V stands for C-R37 and W stands for
C-R38;
R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, R25, R26 and
R27 each independently
stand for a linear or branched, saturated or unsaturated, unsubstituted or at
least monosubstituted aliphatic C1-10 radical;

for an unsaturated or saturated, unsubstituted or at least monosubstituted,
three-membered, four-membered, five-membered, six-membered, seven-
membered, eight-membered, or nine-membered cycloaliphatic radical
optionally containing at least one heteroatom as ring member, which can be
condensed with a saturated or unsaturated, unsubstituted or at least
monosubstituted monocyclic or polycyclic ring system and/or can be bonded
via a linear or branched, unsubstituted or at least monosubstituted C1-6
alkylene group or two to six-membered heteroalkylene group;
or for an unsubstituted or at least monosubstituted five-membered to fourteen-
membered aryl radical or heteroaryl radical, which can be condensed with a
saturated or unsaturated, unsubstituted or at least monosubstituted
monocyclic or polycyclic ring system and/or can be bonded via a linear or
branched, unsubstituted or at least monosubstituted C1-6 alkylene group or two
to six-membered heteroalkylene group;
R35, R36, and R37 each independently stand for H; F; CI; Br; I; -SF5; -NO2; -CF3; -CN; -
NH2; -OH; -SH; -C(= O)-NH2; -S(= O)2-NH2; -C(= O)-NH-OH; -C(= O)-OH; -C(=
O)-H; -S(= O)2-OH; -NHR13; -NR14R15; -NH-C(= O)-R13; -OR16; -SR17; -C(= O)-
NHR18; -C(= O)-NR19R20; -S(= O)2-NHR21; -S(= O)2-NR22R23; -C(= O)-OR24; -
C(= O)-R25; -S(= O)-R26; -S(= O)2R27
for a linear or branched, saturated or unsaturated, unsubstituted or at least
monosubstituted aliphatic C1-10 radical;

or for an unsubstituted or at least monosubstituted five-membered to fourteen-
membered aryl radical or heteroaryl radical, which can be condensed with a
saturated or unsaturated, unsubstituted or at least monosubstituted
monocyclic or polycyclic ring system and/or can be bonded via a linear or
branched, unsubstituted or at least monosubstituted C1-6 alkylene group or C2-6
alkenylene group or C2-6-alkynylene group;
R38 stands for F; CI; Br; I; -SF5; -NO2; -CF3; -CF2 CI; -CN; -NH2; -OH; -SH; -C(= O)-
NH2; -S(= O)2-NH2; -C(= O)-NH-OH; -C(= O)-OH; -C(= O)-H; -S(= O)2-OH; -
NHR39; -NR40R41; -OR42; -SR43; -C(= O)-NHR44; -C(= O)-NR45R46; -S(= O)2-
NHR47; -S(= O)2-NR48R49; -C(= O)-OR50; -C(= O)-R51; -S(= O)-R52; -S(= O)2-
R53; -C(= NH)-NH2; -C(= NH)-NH-R54; -N= C(NH2)2; -N= C(NHR55)-(NHR56);
for a linear or branched, saturated or unsaturated, unsubstituted or at least
monosubstituted aliphatic C1-10 radical;
for an unsaturated or saturated, unsubstituted or at least monosubstituted
three-membered, four-membered, five-membered, six-membered, seven-
membered, eight-membered, or nine-membered cycloaliphatic radical
optionally exhibiting at least one heteroatom as ring member, each of which is
bonded to the parent structure over a carbon atom in the ring of the
cycloaliphatic radical and is condensed with a saturated or unsaturated,
unsubstituted or at least monosubstituted monocyclic or polycyclic ring system
and/or can be bonded via a linear or branched, unsubstituted or at least
monosubstituted C1-6 alkylene group or C2-6 alkenylene group or C2-6
alkynylene group;

or for an unsubstituted or at least monosubstituted five-membered to fourteen-
membered aryl radical or heteroaryl radical, which can be condensed with a
saturated or unsaturated, unsubstituted or at least monosubstituted
monocyclic or polycyclic ring system and/or can be bonded via a linear or
branched, unsubstituted or at least monosubstituted C1-6 alkylene group or C2-6
alkenylene group or C2-6-alkynylene group;
R39, R40, R41, R42, R43, R44, R45, R46, R47, R48, R49, R50, R51, R52, R53, R54, R55, and R56
each independently
stand for a linear or branched, saturated or unsaturated, unsubstituted or at
least monosubstituted aliphatic C1-10 radical;
for an unsaturated or saturated, unsubstituted or at least monosubstituted,
three-membered, four-membered, five-membered, six-membered, seven-
membered, eight-membered, or nine-membered cycloaliphatic radical
optionally containing at least one heteroatom as ring member, which can be
condensed with a saturated or unsaturated, unsubstituted or at least
monosubstituted monocyclic or polycyclic ring system and/or can be bonded
via a linear or branched, unsubstituted or at least monosubstituted C1-6
alkylene group or two to six-membered heteroalkylene group;
or for an unsubstituted or at least monosubstituted five-membered to fourteen-
membered aryl radical or heteroaryl radical, which can be condensed with a
saturated or unsaturated, unsubstituted or at least monosubstituted

monocyclic or polycyclic ring system and/or can be bonded via a linear or
branched, unsubstituted or at least monosubstituted C1-6 alkylene group or two
to six-membered heteroalkylene group;
or
R40 and R41 form, together with the interconnecting nitrogen atom as ring member,
a saturated or unsaturated four-membered, five-membered, six-membered,
seven-membered, eight-membered, or nine-membered heterocycloaliphatic
radical, which is unsubstituted or substituted by 1, 2, 3, 4, or 5 radicals R57 and
optionally exhibits at least one further heteroatom as ring member, and which
can be condensed with a saturated or unsaturated, unsubstituted or at least
monosubstituted monocyclic or polycyclic ring system;
R57 stands for -NHR58, -NR59R60, or for a linear or branched, saturated or
unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10 radical;
R58, R59, and R60 each independently stand for -C(= O)-R61; for a linear or branched,
saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic
C1-10 radical
or for an unsubstituted or at least monosubstituted five-membered to fourteen-
membered aryl radical or heteroaryl radical, which can be condensed with a
saturated or unsaturated, unsubstituted or at least monosubstituted
monocyclic or polycyclic ring system and/or can be bonded via a linear or

branched, unsubstituted or at least monosubstituted C1-6 alkylene group or C2-6
alkenylene group or C2-6 alkynylene group;
and R61 stands for a linear or branched, saturated or unsaturated, unsubstituted
or at least monosubstituted aliphatic C1-10 radical;
each optionally in the form of one of the pure stereoisomers thereof, particularly
enantiomers or diastereoisomers thereof, the racemates thereof or in the form of a
mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in an
arbitrary mixing ratio, or each in the form of corresponding salts, or each in the form
of corresponding solvates;
wherein
the aforementioned aliphatic C1-10 radicals and tert-butyl radicals can each be
optionally substituted by 1, 2, 3, 4, 5, 6, 7, 8, or 9 substituents independently selected
from the group consisting of F, CI, Br, I, -CN, -NO2, -OH, -NH2, -SH, -O(C1-5 alkyl), -
S(C1-5 alkyl), -NH(C1-5 alkyl), -N(C1-5 alkyl)-(C1-5 alkyl), -C(= O)-O-(C1-5 alkyl), -O-C(=
O)-(C1-5 alkyl), -O-phenyl, phenyl, -OCF3, and -SCF3;
the aforementioned two to six-membered heteroalkylene groups, C1-6 alkylene
groups, and C2-6 alkenylene groups and C2-6 alkynylene groups can each be
optionally substituted by 1, 2, 3, 4, 5, 6, 7, 8, or 9 substituents independently selected
from the group consisting of F, CI, Br, I, -CN, -NO2, -OH, -NH2, -SH, -O(C1-5 alkyl), -
S(C1-5 alkyl), -NH(C1-5 alkyl), -N(C1-5 alkyl)-(C1-5 alkyl), -OCF3, and -SCF3;

the aforementioned heteroalkylene groups each optionally exhibit 1, 2, or 3
heteroatom(s) independently selected from the group consisting of oxygen, sulfur,
and nitrogen (NH) as link(s);
the aforementioned (hetero)cycloaliphatic radicals are optionally each substituted by
1,2,3, 4, or 5 substituents independently selected from the group consisting of -(C1-6
alkylene)-OH, = CH2, -O-(C1-5 alkylene)oxetanyl, -(C1-5 alkylene)-O-(C1-5
alkylene)oxetanyl, -CH2-NH-(C1-5 alkyl), -CH2-N(C1-5 alkyl)2, -N[C(= O)-(C1-5
alkyl)]phenyl, -CH2-O-(C1-5 alkyl), oxo (= O), thioxo (= S), F, CI, Br, I, -CN, -CF3, -SF5,
-OH, -O-(C1-5 alkyl), -O-C(= O)-(C1-5 alkyl), -NH2, -NO2, -O-CF3, -S-CF3, -SH, -S-(C1-5
alkyl), -(C1-5 alkyl), -C(= O)-(C1-5 alkyl), -C(= O)-OH, -C(= O)-O-(C1-5 alkyl), -NH-(C1-5
alkyl), -N(C1-5 alkyl)2, -NH-phenyl, -N(C1-5 alkyl)phenyl, cyclohexyl, cyclopentyl, (4,5)-
dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, piperidinyl,
pyrrolidinyl, -(CH2)-pyridinyl, pyridinyl, -O-phenyl, -O-benzyl, phenyl, and benzyl, and
the cyclic moiety of the radicals oxetanyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-
thiadiazolyl, thiophenyl, phenethyl, -N[C(= O)-(C1-5 alkyl)]phenyl, -NH-phenyl, -N(C1-5
alkyl)phenyl, -(CH2)-pyridinyl, pyridinyl, -O-phenyl, -O-benzyl, phenyl, and benzyl can
each be substituted by 1, 2, 3, 4, or 5 substituents independently selected from the
group consisting of F, CI, Br, -OH, -CF3, -SF5, -CN, -NO2, -C1-5-alkyl, -O-C1-5 alkyl, -
O-CF3, -S-CF3, phenyl, and -O-benzyl,
and, unless otherwise stated, the aforementioned (hetero)cycloaliphatic radicals can
each optionally exhibit 1, 2, or 3 (further) heteroatom(s) independently selected from
the group consisting of oxygen, nitrogen, and sulfur;

the rings of the aforementioned monocyclic or polycyclic ring systems can each be
optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from the
group consisting of oxo (= O), thioxo (= S), F, CI, Br, I, -CN, -CF3, -SF5, -OH, -O-(C1-5
alkyl), -NH2, -NO2, -O-CF3, -S-CF3, -SH, -S-(C1-5 alkyl), -(C1-5 alkyl), -C(= O)-(C1-5
alkyl), -C(= O)-OH, -C(= O)-O-(C1-5 alkyl), -NH-(C1-5 alkyl), -N(C1-5 alkyl)2, -O-phenyl,
-O-benzyl, phenyl, and benzyl, and the cyclic moiety of the radicals -O-phenyl, -O-
benzyl, phenyl, and benzyl can each be substituted by 1, 2, 3, 4, or 5 substituents
independently selected from the group consisting of F, CI, Br, -OH, -CF3, -SF5, -CN, -
NO2, -C1-5-alkyl, -O-C1-5-alkyl, -O-CF3, -S-CF3, phenyl, and -O-benzyl,
and the rings of the aforementioned monocyclic or polycyclic ring systems are each
five-membered, six-membered, or seven-membered and can each optionally exhibit
1, 2, 3, 4, or 5 heteroatom(s) as ring member(s), which are independently selected
from the group consisting of oxygen, nitrogen, and sulfur;
and the aforementioned aryl radicals or heteroaryl radicals can each be optionally
substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group
consisting of F, CI, Br, I, -CN, -CF3, -SF5, -OH, -O-C1-5-alkyl, -NH2, -NO2, -O-CF3, -S-
CF3, -SH, -S-C1-5-alkyl, -C1-5 alkyl, -C(= O)-OH, -C(= O)-O-C1-5-alkyl, -NH-C1-5-alkyl, -
N(C1-5-alky)2, -NH-S(= O)2-C1-5 alkyl, -NH-C(= O)-O-C1-5 alkyl, -C(= O)-H, -C(= O)-C1-
5-alkyl, -C(= O)-NH2, -C(= O)-NH-C1-5-alkyl, -C(= O)-N-(C1-5-alkyl)2, -O-phenyl, -O-
benzyl, phenyl, and benzyl, and the cyclic moiety of the radicals -O-phenyl, -O-
benzyl, phenyl, and benzyl can each be substituted by 1, 2, 3, 4, or 5 substituents
independently selected from the group consisting of F, CI, Br, -OH, -CF3, -SF5, -CN, -
NO2, -C1-5-alkyl, -O-C1-5-alkyl, -O-CF3, -S-CF3, phenyl, and -O-benzyl,

and
the aforementioned heteroaryl radicals can each optionally exhibit 1, 2, 3, 4, or 5
heteroatom(s) independently selected from the group consisting of oxygen, nitrogen,
and sulfur as ring member(s).
The term "heteroalkylene" designates an alkylene chain in which one or more C-
atoms have each been replaced by a heteroatom independently selected from the
group consisting of oxygen, sulfur and nitrogen (NH). Heteroalkylene groups can
preferably contain 1, 2, or 3 heteroatom(s) and more preferably one heteroatom,
independently selected from the group consisting of oxygen, sulfur and nitrogen
(NH), as link(s). Heteroalkylene groups can preferably be two to six-membered and
more preferably two or three-membered.
Mention may be made, for example, of heteroalkylene groups such as -CH2-CH2-O-
CH2-, -CH2-CH(CH3)-O-CH2-, -(CH2)-O-, -(CH2)2-O-, -(CH2)3-O-, -(CH2)4-O -, -O-
(CH2)-, -O-(CH2)2-, -O-(CH2)3-, -O-(CH2)4-, -C(C2H5)-(H)-O-, -O-C(C2H5)-(H)-, -CH2-O-
CH2-, -CH2-S-CH2-, -CH2-NH-CH2-, -CH2-NH-, and -CH2-CH2-NH-CH2-CH2.
If one or more of the aforementioned substituents exhibit a linear or branched C1-6-
alkylene group, these can be preferably selected from the group consisting of -(CH2)-
, -(CH2)2-, -C(H)-(CH3)-, -(CH2)3-, -(CH2)4-, -(CH2)5-, -C(H)-(C(H)-(CH3)2)-, and -
C(C2H5)-(H)-.
Saturated or unsaturated C1-10 aliphatic radicals can stand for a C1-10-alkyl, C2-10-
alkenyl, or C2-10-alkynyl radical. C2-10-alkenyl radicals have at least one and

preferably 1, 2, 3, or 4 C-C-double bonds and C2-10-alkynyl radicals at least one and
preferably 1, 2, 3, or 4 C-C-triple bonds.
Preference is given to C1-10-alkyl radicals selected from the group consisting of
methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-
methylbut-1-yl, 2-pentyl, 3-pentyl, sec-pentyl, neopentyl, 4-methylpent-1-yl, (3,3)-
dimethylbut-1-yl, n-hexyl, n-heptyl, 2-heptyi, 3-heptyl, 4-heptyl, n-octyl, n-nonyl, 2-
nonyl, 3-nonyl, 4-nonyl, 5-nonyl, and (2,6)-dimethylhept-4-yl, which can be optionally
substituted by 1, 2, 3, 4, 5, 6, 7, 8, or 9 substituents independently selected from the
group consisting of -O-phenyl, -O-C(= O)-CH3, -O-C(= O)-C2H5, -O-C(= O)-CH(CH3)2,
-O-C(= O)-C(CH3)3, -C(= O)-O-CH3, -C(= O)-O-C2H5, -C(= O)-O-CH(CH3)2, -C(= O)-
O-C(CH3)3, F, CI, Br, I, -CN, -NO2, -OH, -NH2, -SH, -O-CH3, -O-C2H5, -O-CH(CH3)2, -
O-C(CH3)3) -S-CH3, -S-C2H5, -S-CH(CH3)2, -S-C(CH3)3, -NH-CH3, -NH-C2H5, -NH-
C(CH3)3, -N(CH3)2, -N(C2H5)2, -N(CH3)-(C2H5), -OCF3, and -SCF3.
In another preferred embodiment, C2-10 alkenyl radicals are selected from the group
consisting of vinyl, 1-propenyl, 2-propenyl, 1-butenyl, 2-butenyl, 3-butenyl, 2-methyl-
propene-1-yl, 3-methyl-but-2-en-1-yl, (3,3)-dimethyl-but-1-enyl, 2-methyl-butene-2-yl,
1-pentenyl, 2-pentenyl, 3-pentenyl, 4-pentenyl, 1-hexenyl, 1-heptenyl, and 1-octenyl,
which can be optionally substituted by 1, 2, or 3 substituents independently selected
from the group consisting of F, CI, Br, I, -CN, -NO2, -OH, -NH2, -SH, -O-CH3, -O-
C2H5, -O-CH(CH3)2, -O-C(CH3)3, -S-CH3, -S-C2H5, -S-CH(CH3)2, -S-C(CH3)3, -NH-
CH3, -NH-C2H5, -NH-C(CH3)3, -N(CH3)2, -N(C2H5)2, -N(CH3)-(C2H5), -OCF3, and -
SCF3.

Preference is also given to C2-10 alkynyl radicals selected from the group consisting
of (3,3)-dimethyl-but-1-ynyl, 4-methyl-pent-1-ynyl, 1-hexynyl, ethynyl, 1-propynyl, 2-
propynyl, 1-butynyl, 2-butynyl, 3-butynyl, 1-pentynyl, 2-pentynyl, 3-pentynyl, and 4-
pentynyl, which can be optionally substituted by 1, 2, or 3 substituents independently
selected from the group consisting of F, CI, Br, I, -CN, -NO2, -OH, -NH2, -SH, -O-CH3,
-O-C2H5, -O-CH(CH3)2, -O-C(CH3)3, -S-CH3, -S-C2H5, -S-CH(CH3)2, -S-C(CH3)3, -NH-
CH3, -NH-C2H5, -NH-C(CH3)3, -N(CH3)2, -N(C2H5)2, -N(CH3)(C2H5), -OCF3, and -
SCF3.
Particularly preferred optionally substituted C1-10 aliphatic radicals are selected from
the group consisting of methyl, -CF3, -CHF2, -CH2F, -CF2CI, -CCI2F, -CCI3, -CBr3, -
CH2-CN, -CH2-O-CH3, -CH2-O-CF3, -CH2-SF3, -CH2-NH2, -CH2-OH, -CH2-SH, -CH2-
NH-CH3, -CH2-N(CH3)2, -CH2-N(C2H5)2, -CH2-N(CH3)-(C2H5), ethyl, -CF2-CH3, -CHF-
CF2CI, -CF2-CFCI2, -CFCI-CF2CI, -CFCI-CFCI2, -CH2-CH2-NH2, -CH2-CH2-OH, -CH2-
CH2-SH, -CH2-CH2-NH-CH3, -CH2-CH2-N(CH3)2, -CH2-CH2-N(C2H5)2, -CH2-CH2-
N(CH3)-(C2H5), -CH2-CF3, -C2F5, -CH2-CCI3, -CH2-CBr3, -CH2-CH2-CN, n-propyl, -
CH2-CH2-CH2-OH, -CH2-CH2-CH2-SH, -CH2-CH2-CH2-NH2, -CH2-CH2-CH2-NH-CH3, -
CH2-CH2-CH2-N(CH3)2, -CH2-CH2-CH2-N(C2H5)2, -CH2-CH2-CH2-N(CH3)-(C2H5), -
CH2-CH2-O-CH3, -CF2-CF2-CF3, -CF(CF3)2, isopropyl, -CH2-CH2-CH2-CN, -CH2-O-
CH2-CH3, -CH2-CH2-SF3, -CH2-CH2-OCF3, -CH(CH3)-(O-CH3), -CH(CH3)-(S-CH3), n-
butyl, -CF2-CF2-CF2-CF3, -CH2-CH2-CH2-CH2-CN, -CH2-CH2-CH2-CF3, -CH2-CH2-
CH2-CH2-CF3, -CH2-O-C(= O)-CH3, -CH2-O-C(= O)-C2H5, -CH2-O-C(= O)-CH(CH3)2, -
CH2-O-C(= O)-C(CH3)3, -CH2-C(= O)-O-CH3, -CH2-C(= O)-O-C2H5, -CH2-C(= O)-O-
C(CH3)3, -CH2-CH2-O-CH3, -CH2-CH2-O-C2H5l -CH2-CH2-O-phenyl, -CH2-CH2-CH2-
O-CH3, sec-butyl, isobutyl, tert-butyl, n-pentyl, sec-pentyl, neo-pentyl, n-hexyl, vinyl,
1-propenyl, 2-propenyl, 1-butenyl, 2-butenyl, 3-butenyl, 2-methyl-butene-2-yl, (1,1,2)-

trifluoro-1 -butenyl, 1-pentenyl, 2-pentenyl, 3-pentenyl, 4-pentenyl, -CF= CF2, -CCI=
CCI2, -CH2-CF= CF2, -CH2-CCI= CCI2, -C=C-I, -OC-, and -C=C-CI.
If one or more of the aforementioned substituents stand for a (hetero)cycloaliphatic
radical, which can be optionally condensed with a saturated or unsaturated,
unsubstituted or at least monosubstituted monocyclic or polycyclic ring system, this
can preferably be selected from the group consisting of cyclopropyl, cyclobutyl,
cyclopentyl, cyclohexyl, cycloheptyl, cyclopentenyl, cyclohexenyl, cycloheptenyl,
imidazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl, piperidinyl,
morpholinyl, piperazinyl, thiomorpholinyl, tetrahydropyranyl, oxetanyl, (1,2,3,6)-
tetrahydropyridinyl, azepanyl, azocanyl, diazepanyl, dithiolanyl, (1,3,4,5)-
tetrahydropyrido[4.3-b]indolyl, (3,4)-dihydro-1 H-isoquinolinyl, (1,3,4,9)-
tetrahydro[b]carbolinyl, and (1,3)-thiazolidinyl.
As examples of suitable (hetero)cycloaliphatic radicals, which can be unsubstituted
or monosubstituted or polysubstituted and are condensed with a monocyclic or
bicyclic ring system, there may be mentioned (4,5,6,7)-tetrahydroisoxazolo[5.4-
c]pyridinyl, (2,3)-dihydro-1H-indenyl, 3-aza-bicyclo[3.1.1]heptyl, 3-aza-
bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl, 8-aza-bicyclo[3.2.1]octyl, isoindolyl,
indolyl, (1,2,3,4)-tetrahydroquinolinyl, (1,2,3,4)-tetrahydroisoquinolinyl, (2,3)-dihydro-
1 H-isoindolyl, (1,2,3,4)-tetrahydronaphthyl, (2,3)-dihydro-benzo[1.4]dioxinyl,
benzo[1.3]dioxolyl, (1,4)-benzodioxanyl, (2,3)-dihydrothieno[3.4-b][1.4]dioxinyl, (3,4)-
dihydro-2H-benzo[1.4]oxazinyl, octahydro-1 H-isoindolyl, and octahydro-pyrrolo[3.4-
c]pyrrolyl.

(Hetero)cycloaliphatic radicals can form, within the scope of the present invention, a
spirocyclic radical with another (hetero)cycloaliphatic radical via a carbon atom
common to both rings.
As examples of suitable spirocyclic radicals there may be mentioned a 6-aza-
spiro[2.5]octyl radical, 8-aza-spiro[4.5]decyl radical and a 1-oxa-2,8-diaza-
spiro[4.5]dec-2-enyl radical.
More preferably the (hetero)cycloaliphatic radicals can each be optionally substituted
by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of
oxo (= O), thioxo (= S), F, CI, Br, I, -CN, -CF3, -SF5, -OH, -O-CH3, -O-C2H5, -O-
CH(CH3)2, -O-C(CH3)3, -NH2, -NO2, -O-CF3, -S-CF3, -SH, -S-CH3, -S-C2H5, -S-
CH(CH3)2, -S-C(CH3)3, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,
tert-butyl, n-pentyl, -C(= O)-CH3, -C(= O)-C2H5, -C(= O)-CH(CH3)2, -C(= O)-C(CH3)3, -
C(= O)-0H, -C(= O)-O-CH3, -C(= O)-O-C2H5, -C(= O)-O-CH(CH3)2, -C(= O)-O-
C(CH3)3, -NH-CH3, -NH-C2H5, -NH-C(CH3)3, -N(CH3)2, -N(C2H5)2, -N(CH3)-(C2H5), -
CH2-OH, -CH2-CH2-OH, = CH2, -CH2-O-CH2-oxetanyl, -O-CH2-oxetanyl, -CH2-
N(CH3)2, -CH2-N(C2H5)2, -CH2-NH-CH3, -CH2-NH-C2H5, -N-[C(= O)-C2H5]-phenyl, -N-
[C(= O)-CH3]-phenyl, -CH2-O-CH3, -CH2-O-CH2-CH3, -NH-phenyl, -N(CH3)phenyl, -
N(C2H5)phenyl, -N(C2H5)phenyl, -O-CH2-CH2-CH2-CH3, (4,5)-dihydroisoxazolyl,
thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, cyclohexyl, cyclopentyl,
piperidinyl, pyrrolidinyl, -O-C(= O)-CH3, -O-C(= O)-C2H5, -O-C(= O)-C(CH3)3, -
(CH2)pyridinyl, pyridinyl, -O-phenyl, -O-benzyl, phenyl, and benzyl, and the cyclic
moiety of the radicals oxetanyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl,
thiophenyl, phenethyl, -N-[C(= O)-C2H5]phenyl, -N-[C(= O)-CH3]phenyl, -NH-phenyl, -
N(CH3)phenyl, -N(C2H5)phenyl, -(CH2)pyridinyl, pyridinyl, -O-phenyl, -O-benzyl,

phenyl, and benzyl can each be substituted by 1, 2, 3, 4, or 5 substituents
independently selected from the group consisting of F, CI, Br, -OH, -CF3, -SF5, -CN, -
NO2, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, -O-CH3,
-O-C2H5, -O-CH(CH3)2, -O-C(CH3)3, -O-CF3, -S-CF3, phenyl, and -O-benzyl.
If one or more of the aforementioned substituents stand for an aryl radical, this can
preferably be selected from the group consisting of phenyl and naphthyl (1-naphthyl
and 2-naphthyl).
If one or more of the aforementioned substituents stand for a heteroaryl radical, this
can preferably be selected from the group consisting of tetrazolyl, thiophenyl, furanyl,
pyrrolyl, pyrazolyl, pyrazinyl, pyranyl, triazolyl, pyridinyl, imidazolyl, indolyl, isoindolyl,
benzo[b]furanyl, benzo[b]thiophenyl, benzoxazolyl, benzisoxazolyl, thiazolyl,
oxazolyl, isoxazolyl, pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl, quinoxalinyl,
quinolinyl, and isoquinolinyl.
As examples of suitable aryl and heteroaryl radicals, which can be unsubstituted or
monosubstituted or polysubstituted and are condensed with a monocyclic or bicyclic
ring system, there may be mentioned isoindolyl, indolyl, (1,2,3,4)-
tetrahydroquinolinyl, (1,2,3,4)-tetrahydroisoquinolinyl, (2,3)-dihydro-1 H-isoindolyl,
(1,2,3,4)-tetrahydronaphthyl, (2,3)-dihydrobenzo[1.4]dioxinyl, (2,3)-dihydrothieno[3.4-
b][1.4]dioxinyl, benzo[1.3]dioxolyl, and (1,4)-benzodioxanyl.
More preferably, the aryl radicals or heteroaryl radicals can each be optionally
substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group
consisting of F, CI, Br, I, -CN, -CF3, -SF5, -OH, -O-CH3, -O-C2H5, -O-CH(CH3)2, -O-

C(CH3)3, -NH2, -NO2, -O-CF3, -S-CF3, -SH, -S-CH3, -S-C2H5, -S-CH(CH3)2, -S-
C(CH3)3, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-
pentyl, -C(= O)-OH, -C(= O)-O-CH3, -C(= O)-O-C2H5l -C(= O)-O-CH(CH3)2, -C(= O)-
O-C(CH3)3, -NH-CH3, -NH-C2H5, -NH-C(CH3)3, -N(CH3)2, -N(C2H5)2, -N(CH3)-(C2H5), -
NH-S(= O)2-CH3, -NH-S(= 02)-C2H5, -NH-S(= O)2-CH(CH3)2, -NH-C(= O)-O-CH3, -
NH-C(= O)-O-C2H5, -NH-C(= O)-O-C(CH3)3, -C(= O)-H, -C(= O)-CH3, -C(= O)-C2H5, -
C(= O)-CH(CH3)2, -C(= O)-C(CH3)3, -C(= O)-NH2, -C(= O)-NH-CH3, -C(= O)-NH-
C2H5, -C(= O)-N(CH3)2, -C(= O)-N(C2H5)2, -O-phenyl, -O-benzyl, phenyl, and benzyl,
and the cyclic moiety of the radicals -O-phenyl, -O-benzyl, phenyl, and benzyl can
each be substituted by 1, 2, 3, 4, or 5 substituents independently selected from the
group consisting of F, CI, Br, -OH, -CF3, -SF5, -CN, -NO2, methyl, ethyl, n-propyl,
isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, -O-CH3, -O-C2H5, -O-CH(CH3)2, -O-
C(CH3)3, -O-CF3, -S-CF3, phenyl, and -O-benzyl.
If a polycyclic ring system such as a bicyclic ring system is present, the different rings
can independently exhibit a different degree of saturation, i.e. be saturated or
unsaturated. A polycyclic ring system is preferably a bicyclic ring system.
As examples of aryl radicals condensed with a monocyclic or polycyclic ring system
mention may be made of (1,3)-benzodioxolyl and (1,4)-benzodioxanyl.
If one or more of the aforementioned substituents have a monocyclic or polycyclic
ring system, this can preferably be substituted by 1, 2, 3, 4, or 5 substituents
independently selected from the group consisting of oxo (= O), thioxo (= S), F, CI, Br,
I, -CN, -CF3, -SF5, -OH, -O-CH3, -O-C2H5, -O-CH(CH3)2, -O-C(CH3)3, -NH2, -NO2, -O-
CF3, -S-CF3, -SH, -S-CH3, -S-C2H5, -S-CH(CH3)2, -S-C(CH3)3, methyl, ethyl, n-propyl,

isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, -C(= O)-OH, -C(= O)-O-
CH3, -C(= O)-O-C2H5, -C(= O)-O-CH(CH3)2l -C(= O)-O-C(CH3)3, -NH-CH3, -NH-C2H5,
-NH-C(CH3)3, -N(CH3)2, -N(C2H5)2, -N(CH3HC2H5), -NH-C(= O)-O-CH3, -NH-C(= O)-
O-C2H5, -NH-C(= O)-O-C(CH3)3, -C(= O)-H, -C(= O)-CH3, -C(= O)-C2H5, -C(= O)-
CH(CH3)2, -C(= O)-C(CH3)3, -C(= O)-NH2, -C(= O)-NH-CH3, -C(= O)-nH-C2H5, -C(=
O)-N(CH3)2, -C(= O)-N(C2H5)2, -O-phenyl, -O-benzyl, phenyl, and benzyl, and the
cyclic moiety of the radicals -O-phenyl, -O-benzyl, phenyl, and benzyl can each be
substituted by 1, 2, 3, 4, or 5 substituents independently selected from the group
consisting of F, CI, Br, -OH, -CF3, -SF5, -CN, -NO2, methyl, ethyl, n-propyl, isopropyl,
n-butyl, sec-butyl, isobutyl, tert-butyl, -O-CH3, -O-C2H5, -O-CH(CH3)2, -O-C(CH3)3, -
O-CF3l -S-CF3, phenyl, and -O-benzyl.
If the radicals R41 and R42, together with the interconnecting nitrogen atom as ring
member, form a heterocycloaliphatic radical which is substituted by 1, 2, 3, 4 or 5
radicals R57, these radicals R57 each have, independently of one another, one of the
indicated meanings.
Preference is given to compounds of the general formula la,

in which

D stands for N or CH;
R1 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; -
SR17; -S(=O)2-NR22R23; -S(=O)2-R27 or for a radical selected from the group
consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl,
sec-butyl, isobutyl, and tert-butyl;
R2 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; -
SR17; -S(=O)2-NR22R23; -S(=O)2-R27 or for a radical selected from the group
consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl,
sec-butyl, isobutyl, and tert-butyl;
R3 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; -
SR17; -S(=O)2-NR22R23; -S(=O)2-R27 or for a radical selected from the group
consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl,
sec-butyl, isobutyl, and tert-butyl;
R4 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; -
SR17; -S(=O)2-NR22R23; -S(=O)2-R27 or for a radical selected from the group
consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl,
sec-butyl, isobutyl, and tert-butyl;
R5 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; -
SR17; -S(=O)2-NR22R23; -S(=O)2-R27 or for a radical selected from the group

consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl,
sec-butyl, isobutyl, and tert-butyl;
R8 stands for -SF5; -O-CF3; -CF3; tert-butyl; or -C(CH3)2(CH2OH);
R13, R16, R17, R22, R23 and R27 each independently stand for a radical selected from
the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, -CF2-CH3, -CH2-CF3, -
C2F5, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-
heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-
hexyl, (3,3)-dimethylbutyl and ethenyl;
R42 stands for a radical selected from the group consisting of methyl, -CH2-O-CH3,
ethyl, n-propyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-hexyl, (3,3)-
dimethylbutyl, -CH2-CH2-O-CH3, -CH2-CH2-O-C2H5l and -CH2-CH2-CH2-O-CH3;
or for a radical selected from the group consisting of 2,3-dihydro-1H-indenyl,
cyclopropyl, oxetanyl, cyclobutyl, cyclopentyl, cyclohexyl, imidazolidinyl,
tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl, piperidinyl, morpholinyl,
piperazinyl, azepanyl, diazepanyl, azocanyl, and thiomorpholinyl, each of which can
be optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from
the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,
tert-butyl, and n-pentyl;
in each case optionally in the form of one of the pure stereoisomers thereof,
particularly enantiomers or diastereoisomers, or the racemates thereof or in the form
of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers,

in an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in
each case in the form of corresponding solvates.
Special preference is given to compounds of the general formula la,

in which
D stands for N or CH;
R1 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(=O)-R13; -
OR16; SR17, -S(=O)2-NR22R23 or -(S=O)-R27;
R2 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(=O)-R13; -
OR16; SR17, -S(=O)2-NR22R23 or-(S=O)-R27;
R3 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(=O)-R13; -
OR16; SR17, -S(=O)2-NR22R23 or-(S=O)-R27;
R4 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(=O)-R13; -
OR16; SR17, -S(=O)2-NR22R23 or-(S=O)-R27;

R5 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(=O)-R13; -
OR16; SR17, -S(=O)2-NR22R23 or-(S=O)-R27;
R8 stands for -SF5; -O-CF3; -CF3; tert-butyl; or -C(CH3)2(CH2OH);
R13, R16, R17, R22, R23 and R27 each independently stand for a radical selected from
the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,
tert-butyl, n-pentyl and ethenyl;
R42 stands for a radical selected from the group consisting of methyl, ethyl, n-
propyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-hexyl, and
(3,3)-dimethylbutyl;
or for a radical selected from the group consisting of cyclopropyl, cyclobutyl,
cyclopentyl, cyclohexyl, and cycloheptyl, each of which can be optionally substituted
by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of
methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, and n-pentyl;
in each case optionally in the form of one of the pure stereoisomers thereof,
particularly enantiomers or diastereoisomers, or the racemates thereof or in the form
of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers,
in an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in
each case in the form of corresponding solvates.
Very particular preference is given to compounds of the general formula la,

in which
D stands for N or CH;
R1 stands for H; F; CI; Br; or I;
R2 stands for H; F; CI; Br; I; methyl; -OH; -NH2 or -OR16;
R3 stands for H; F; CI; Br; I; -NO2; -OH; -NH2; -NH-C(= O)-R13, -OR16; SR17, -
S(=O)2-NR22R23 or-(S=O)-R27;
R4 stands for H; F; CI; Br; I; methyl, -OH; -NH2; or -OR16;
R5 stands for H; F; CI; Br; or I;
R8 stands for -SF5; -O-CF3; -CF3; tert-butyl; or -C(CH3)2(CH2OH);
R13, R16, R17, R22, R23 and R27 each independently stand for a radical selected from
the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,
tert-butyl, n-pentyl and ethenyl;

R42 stands for a radical selected from the group consisting of methyl, ethyl, n-
propyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-hexyl, and (3,3)-
dimethylbutyl;
or for a radical selected from the group consisting of cyclopropyl, cyclobutyl,
cyclopentyl, cyclohexyl, and cycloheptyl, each of which can be optionally substituted
by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of
methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, and n-pentyl;
in each case optionally in the form of one of the pure stereoisomers thereof,
particularly enantiomers or diastereoisomers, the racemates thereof or in the form of
a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in
an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in
each case in the form of corresponding solvates.
Preference is given to compounds of the general formula lb,

in which
D stands for N or CH;

R1 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; -
SR17; -S(=O)2-NR22R23; -(S=O)-R27 or for a radical selected from the group consisting
of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,
and tert-butyl;
R2 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; -
SR17; -S(=O)2-NR22R23; -(S=O)-R27 or for a radical selected from the group consisting
of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,
and tert-butyl;
R3 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; -
SR17; -S(=O)2-NR22R23; -(S=O)-R27 or for a radical selected from the group consisting
of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,
and tert-butyl;
R4 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; -
SR17; -S(=O)2-NR22R23; -(S=O)-R27 or for a radical selected from the group consisting
of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,
and tert-butyl;
R5 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; -
SR17; -S(=O)2-NR22R23; -(S=O)-R27 or for a radical selected from the group consisting
of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,
and tert-butyl;

R8 stands for -SF5; -O-CF3; -CF3; tert-butyl; or -C(CH3)2(CH2OH);
R13, R16, R17, R22, R23 and R27 each independently stand for a radical selected from
the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, -CF2-CH3, -CH2-CF3, -
C2F5, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-
heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-
hexyl, (3,3)-dimethylbutyl and ethenyl;
R43 stands for a radical selected from the group consisting of methyl, -CH2-O-CH3,
ethyl, n-propyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-hexyl, (3,3)-
dimethylbutyl, -CH2-CH2-O-CH3, -CH2-CH2-O-C2H5, and -CH2-CH2-CH2-O-CH3;
or for a radical selected from the group consisting of 2,3-dihydro-1 H-indenyl,
cyclopropyl, oxetanyl, cyclobutyl, cyclopentyl, cyclohexyl, imidazolidinyl,
tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl, piperidinyl, morpholinyl,
piperazinyl, azepanyl, diazepanyl, azocanyl, and thiomorpholinyl, each of which can
be optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from
the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,
tert-butyl, and n-pentyl;
in each case optionally in the form of one of the pure stereoisomers thereof,
particularly enantiomers or diastereoisomers, or the racemates thereof or in the form
of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers,
in an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in
each case in the form of corresponding solvates.

Special preference is given to compounds of the general formula lb,

in which
D stands for N or CH;
R1 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(= O)-R13; -
OR16; -SR17; -S(=O)2-NR22R23 or-(S=O)-R27;
R2 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(= O)-R13; -
OR16; -SR17; -S(=O)2-NR22R23 or -(S=O)-R27;
R3 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(= O)-R13; -
OR16; -SR17; -S(=O)2-NR22R23 or -(S=O)-R27;
R4 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(= O)-R13; -
OR16; -SR17; -S(=O)2-NR22R23 or-(S=O)-R27;
R5 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(= O)-R13; -
OR16; -SR17; -S(=O)2-NR22R23 or -(S=O)-R27;

R8 stands for -SF5; -O-CF3; -CF3; tert-butyl; or -C(CH3)2(CH2OH);
R13, R16, R17, R22, R23 and R27 each independently stand for a radical selected from
the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,
tert-butyl, n-pentyl and ethenyl;
R43 stands for a radical selected from the group consisting of methyl, ethyl, n-
propyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-hexyl, and (3,3)-
dimethylbutyl;
or for a radical selected from the group consisting of cyclopropyl, cyclobutyl,
cyclopentyl, cyclohexyl, and cycloheptyl, each of which can be optionally substituted
by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of
methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, and n-pentyl;
in each case optionally in the form of one of the pure stereoisomers thereof,
particularly enantiomers or diastereoisomers, or the racemates thereof or in the form
of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers,
in an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in
each case in the form of corresponding solvates.
Very particular preference is given to compounds of the general formula lb,

in which
D stands for N or CH;
R1 stands for H; F; CI; Br; or I;
R2 stands for H; F; CI; Br; I; methyl; -OH; -NH2; or -OR16;
R3 stands for H; F; CI; Br; I; -NO2; -OH; -NH2; -NH-C(= O)-R13, -OR16; SR17; -
S(=O)2-NR22R23 or -(S=O)-R27;
R4 stands for H; F; CI; Br; I; methyl; -OH; -NH2; or -OR16;
R5 stands for H; F; CI; Br; or I;
R8 stands for -SF5; -O-CF3; -CF3; tert-butyl; or -C(CH3)2(CH2OH);
R13, R16, R17, R22, R23 and R27 each independently stand for a radical selected from
the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,
tert-butyl, n-pentyl and ethenyl;

R43 stands for a radical selected from the group consisting of methyl, ethyl, n-
propyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-hexyl, and (3,3)-
dimethylbutyl;
or for a radical selected from the group consisting of cyclopropyl, cyclobutyl,
cyclopentyl, cyclohexyl, and cycloheptyl, each of which can be optionally substituted
by 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of
methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, and n-pentyl;
in each case optionally in the form of one of the pure stereoisomers thereof,
particularly enantiomers or diastereoisomers, or the racemates thereof or in the form
of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers,
in an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in
each case in the form of corresponding solvates.
Preference is given to compounds of the general formula Ic,

in which

D stands for N or CH;
R1 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; -
SR17; -S(=O)2-NR22R23 or -(S=O)-R27 or for a radical selected from the group
consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl,
isobutyl, and tert-butyl;
R2 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; -
SR17; -S(=O)2-NR22R23 or -(S=O)-R27 or for a radical selected from the group
consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl,
isobutyl, and tert-butyl;
R3 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; -
SR17; -S(=O)2-NR22R23 or -(S=O)-R27 or for a radical selected from the group
consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl,
isobutyl, and tert-butyl;
R4 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; -
SR17; -S(=O)2-NR22R23 or -(S=O)-R27 or for a radical selected from the group
consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl,
isobutyl, and tert-butyl;
R5 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(= O)-R13; -OR16; -
SR17; -S(=O)2-NR22R23 or -(S=O)-R27 or for a radical selected from the group
consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl,
isobutyl, and tert-butyl;

R8 stands for -SF5; -O-CF3; -CF3; tert-butyl; or -C(CH3)2(CH2OH);
R13, R16, R17, R22, R23 and R27 each independently stand for a radical selected from
the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, -CF2-CH3, -CH2-CF3, -
C2F5, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-
heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-
hexyl, (3,3)-dimethylbutyl and ethenyl;
R40 and R41 each independently stand for a radical selected from the group
consisting of methyl, -CH2-O-CH3, ethyl, n-propyl, n-butyl, sec-butyl, isobutyl, tert-
butyl, n-pentyl, 3-pentyl, n-hexyl, (3,3)-dimethylbutyl, -CH2-CH2-O-CH3, -CH2-CH2-O-
C2H5, and -CH2-CH2-CH2-O-CH3;
for a radical selected from the group consisting of 2,3-dihydro-1H-indenyl,
cyclopropyl, oxetanyl, cyclobutyl, cyclopentyl, cyclohexyl, imidazolidinyl,
tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl, piperidinyl, morpholinyl,
piperazinyl, azepanyl, diazepanyl, azocanyl, and thiomorpholinyl, each of which can
be optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected from
the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,
tert-butyl, and n-pentyl;
or
R40 and R41 form, together with the interconnecting nitrogen atom as ring member, a
radical selected from the group consisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-

spiro[2.5]octyl, 3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl, 8-aza-
bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl, azocanyl, isoindolyl, indolyl,
(1,2,3,6)-tetrahydropyridinyl, (4,5,6,7)-tetrahydroisoxazolo[5.4-c]pyridinyl, pyrrolidinyl,
piperidinyl, piperazinyl, morpholinyl, azepanyl, diazepanyl, and thiomorpholinyl, of
which the heterocycloaliphatic moiety can in each case be unsubstituted or
substituted by 1, 2, 3, 4, or 5 radicals R57;
R57 stands for -NHR58, -NR59R60, or for an alkyl radical selected from the group
consisting of-CF3, -CH2-CF3, methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl,
sec-butyl, and isobutyl;
R58, R59, and R60 each independently stand for -C(= O)-R61;
for an alkyl radical selected from the group consisting of-CF3, -CH2-CF3, methyl,
ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, and isobutyl;
or for a radical selected from the group consisting of phenyl and naphthyl, and each
radical can be bonded via a -(CH2)-, -(CH2)2- or -(CH2)3 group and/or can each be
unsubstituted or optionally substituted by 1, 2, 3, 4, or 5 substituents independently
selected from the group consisting of F, CI, Br, I, -CN, -CF3, -O-CH3, -O-C2H5, -O-
CH(CH3)2, -O-C(CH3)3, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,
tert-butyl, and n-pentyl;
and R61 stands for an alkyl radical selected from the group consisting of -CF3, -
CH2-CF3, methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, and isobutyl;

in each case optionally in the form of one of the pure stereoisomers thereof,
particularly enantiomers or diastereoisomers, or the racemates thereof or in the form
of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers,
in an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in
each case in the form of corresponding solvates.
Special preference is given to compounds of the general formula Ic,

in which
D stands for N or CH;
R1 stands for H; F; CI; Br; I; methyl; ethyl; -NO2; -OH; -NH2; -NH-C(= O)-R13; -
OR16; -SR17; -S(=O)2-NR22R23 or-(S=O)-R27;
R2 stands for H; F; CI; Br; I; methyl; ethyl; -NO2; -OH; -NH2; -NH-C(= O)-R13; -
OR16; -SR17; -S(=O)2-NR22R23 or -(S=O)-R27;
R3 stands for H; F; CI; Br; I; methyl; ethyl; -NO2; -OH; -NH2; -NH-C(= O)-R13; -
OR16; -SR17; -S(=O)2-NR22R23 or-(S=O)-R27;

R4 stands for H; F; CI; Br; I; methyl; ethyl; -NO2; -OH; -NH2; -NH-C(= O)-R13; -
OR16; -SR17; -S(=O)2-NR22R23 or -(S=O)-R27;
R5 stands for H; F; CI; Br; I; methyl; ethyl; -NO2; -OH; -NH2; -NH-C(= O)-R13; -
OR16; -SR17; -S(=O)2-NR22R23 or -(S=O)-R27;
R8 stands for -SF5; -O-CF3; -CF3; tert-butyl; or -C(CH3)2(CH2OH);
R13, R16, R17, R22, R23 and R27 each independently stand for a radical selected from
the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,
tert-butyl, n-pentyl and ethenyl;
R40 and R41 form, together with the interconnecting nitrogen atom as ring member, a
radical selected from the group consisting of pyrrolidinyl, piperidinyl, piperazinyl,
morpholinyl, and azepanyl, of which the heterocycloaliphatic moiety can in each case
be unsubstituted or substituted by 1, 2, 3, 4, or 5 radicals R57;
and R57 stands for an alkyl radical selected from the group consisting of methyl,
ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, and isobutyl;
in each case optionally in the form of one of the pure stereoisomers thereof,
particularly enantiomers or diastereoisomers, or the racemates thereof or in the form
of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers,
in an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in
each case in the form of corresponding solvates.

Very particular preference is given to compounds of the general formula Ic,

in which
D stands for N or CH;
R1 stands for H; F; CI; Br; or I;
R2 stands for H; F; CI; Br; I; -OH; -NH2; or -OR16;
R3 stands for H; F; CI; Br; I; -NO2; -OH; -NH2; -NH-C(= O)-R13, -OR16; -SR17; -
S(=O)2-NR22R23 or -(S=O)-R27;
R4 stands for H; F; CI; Br; I; methyl; -OH; -NH2; or -OR16;
R5 stands for H; F; CI; Br; or I;
R8 stands for -SF5; -O-CF3; -CF3; tert-butyl; or -C(CH3)2(CH2OH);

R13, R16, R17, R22, R23 and R27 each independently stand for a radical selected from
the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,
tert-butyl, n-pentyl and ethenyl;
R40 and R41 form, together with the interconnecting nitrogen atom as ring member, a
radical selected from the group consisting of pyrrolidinyl, piperidinyl, piperazinyl,
morpholinyl, and azepanyl, of which the heterocycloaliphatic moiety can in each case
be unsubstituted or substituted by 1, 2, 3, 4, or 5 radicals R57;
and R57 stands for an alkyl radical selected from the group consisting of methyl,
ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, and isobutyl;
in each case optionally in the form of one of the pure stereoisomers thereof,
particularly enantiomers or diastereoisomers, or the racemates thereof or in the form
of a mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers,
in an arbitrary mixing ratio, or in each case in the form of corresponding salts, or in
each case in the form of corresponding solvates.
Even greater preference is given to compounds of the general formulas I, la, lb, and
Ic selected from the group consisting of
[1] 2-(4-Amino-3-fluorophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide;
[2] 2-(3,5-Dibromophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-
3-yl)methyl)acetamide;

[3] 2-(4-Amino-3-bromo-5-methoxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)acetamide;
[4] 2-(3-Fluorophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-3-
yl)methyl)acetamide;
[5] 2-(2,4-Difluorophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-
3-yl)methyl)acetamide;
[6] 2-(2,6-Difluorophenyl)-N-((2-(4-fnethylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-
3-yl)methyl)acetamide;
[7] 2-(2,5-Difluorophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-
3-yl)methyl)acetamide;
[8] 2-(4-Fluorophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-3-
yl)methyl)acetamide;
[9] 2-(4-Hydroxy-3-methoxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide;
[10] 2-(3,5-Difluorophenyl)-N-((2-(4-methylpiperidin-1 -yl)-6-(trifluoromethyl)pyridin-
3-yl)methyl)propanamide;
[11] 2-(3,4-Difluorophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-
3-yl)methyl)propanamide;
[12] 2-(4-Fluorophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-3-
yl)methyl)propanamide;
[13] 2-(3-Fluorophenyl)-N-((2-(4-methylpiperidin-1 -yl)-6-(trifluoromethyl)pyridin-3-
yl)methyl)propanamide;
[14] 2-(3,4-Diaminophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-
3-yl)methyl)propanamide;
[15] N-(2-Butoxy-6-tert-butylpyridin-3-ylmethyl)-2-(3,4-diamino-phenyl)-
propionamide;

[16] N-((6-tert-Butyl-2-(4-methylpiperidin-1 -yl)pyridin-3-yl)methyl)-2-(3,4-
diaminophenyl)propanamide;
[17] N-((6-tert-Butyl-2-(cyclohexylthio)pyridin-3-yl)methyl)-2-(3,4-
diaminophenyl)propanamide;
[18] 2-(4-Acetamido-3-fluorophenyl)-N-((2-(4-methylpiperidin-1 -yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide;
[19] 2-(3,5-Dibromo-4-hydroxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide;
[20] 2-(4-Amino-3,5-dibromophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide;
[21] 2-(3-Bromo-4-hydroxy-5-methoxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)acetamide;
[22] 2-(4-Amino-3,5-dibromophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)acetamide;
[23] 2-(3,5-Dibromo-4-hydroxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)acetamide;
[24] 2-(3-Amino-4-hydroxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide; and
[25] 2-(3,5-Dibromophenyl)-N-(4-methyl-6'-trifluoromethyl-3,4,5,6-tetrahydro-2H-
[1,2']bipyridinyl-3'-ylmethyl)acetamide;
[26] 2-(4-Amino-3,5-difluorophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
[27] 2-(3-Fluoro-5-hydroxy-4-nitrophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
[28] 2-(3-Chloro-4-(methylthio)phenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,

[29] 2-(3-Chloro-4-(methylsulfonyl)phenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
[30] 2-(3-Fluoro-4-(methylthio)phenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
[31] 2-(3-Fluoro-4-(methylsulfonyl)phenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
[32] 2-(4-(N,N-Dimethylsulfamoyl)-3-fluorophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
[33] N-(2-Fluoro-4-(1-((2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-3-
yl)methylamino)-1-oxopropane-2-yl)phenyl)acrylamide,
[34] N-(2-Fluoro-6-iodo-4-(1-((2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-3-
yl)methylamino)-1-oxopropane-2-yl)phenyl)acrylamide,
[35] 2-(4-Methoxy-3,5-dimethylphenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
[36] 2-(3,5-Difluoro-4-methoxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
[37] 2-(4-Hydroxy-3,5-dimethylphenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
[38] 2-(3,5-Difluoro-4-hydroxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
each optionally in the form of one of the pure stereoisomers thereof, particularly
enantiomers or diastereoisomers thereof, the racemates thereof or in the form of a
mixture of stereoisomers, particularly the enantiomers and/or diastereoisomers, in an
arbitrary mixing ratio, or each in the form of corresponding salts, or each in the form
of corresponding solvates;

Furthermore, preference may be given to compounds according to the invention of
the general formulas I, la, lb and Ic, which in the FLIPR assay using CHO-K1 cells,
which have been transfected with the human VR1 gene in a concentration below
2000 nM, preferably below 1000 nM, more preferably below 300 nM, even more
preferably below 100 nM, still more preferably below 75 nM, \/ery preferably below
50 nM and most preferably below 10 nM, cause a 50 percent displacement of
capsaicin present in a concentration of 100 nM.
In the FLIPR assay, the Ca2+ influx is quantified with the aid of a Ca2+-sensitive dye
(type Fluo-4, Molecular Probes Europe BV, Leiden, Netherlands) in a fluorescent
imaging plate reader (FLIPR, Molecular Devices, Sunnyvale, USA), as described
below.
The invention further relates to a process for the production of compounds of the
above general formula I, according to which at least one compound of the general
formula II,

in which R8, U, T, V, and W have the aforementioned meanings, m stands for 0, 1, 2,
or 3, and R stands for hydrogen or for a linear or branched C1-6-alkyl radical, in a
reaction medium, in the presence of at least one reducing agent, preferably in the
presence of at least one reducing agent selected from the group consisting of sodium

hydride, sodium, potassium hydride, lithium aluminum hydride, sodium
tetrahydridoborate, and di(isobutyl)aluminum hydride
is converted to at least one compound of the general formula III,

in which
R8, U, T, V, and W have the meanings stated above and m stands for 0, 1, 2, or 3,
and this is optionally purified and/or isolated,
and at least one compound of the general formula III is converted, in a reaction
medium in the presence of diphenylphosphorylazide or in the presence of HN3, to at
least one compound of the general formula IV,

in which
R8, U, T, V, and W have the meanings stated above and m stands for 0,1,2, or 3,
and this is optionally purified and/or isolated,

and at least one compound of the general formula IV is converted, in a reaction
medium in the presence of at least one reducing agent, preferably in the presence of
at least one reducing agent selected from the group consisting of sodium hydride,
potassium hydride, lithium aluminum hydride, sodium tetrahydridoborate, and
di(isobutyl)aluminum hydride,
or in a reaction medium in the presence of a catalyst, preferably in the presence of a
catalyst based on platinum or palladium, more preferably in the presence of
palladium-on-charcoal, and in the presence of hydrogen or in the presence of
hydrazine,
or in a reaction medium in the presence of triphenylphosphine
to at least one compound of the general formula V,

in which R8, U, T, V, and W have the meanings stated above and m stands for 0, 1,
2, or 3, and this is optionally purified and/or isolated,
or at least one compound of the general formula VI

in which
R8, U, T, V, and W have the meanings stated above and m stands for 0, 1,2, or 3, in
a reaction medium is converted,
in the presence of at least one catalyst, preferably in the presence of at least one
catalyst based on palladium or platinum, more preferably in the presence of
palladium-on-charcoal, under a blanket of hydrogen, optionally in the presence of at
least one acid, preferably in the presence of hydrochloric acid,
or in the presence of at least one reducing agent selected from the group consisting
of BH3.S(CH3)2, lithium aluminum hydride, and sodium tetrahydridoborate, optionally
in the presence of NiCl2,
to form at least one compound of the general formula V, optionally in the form of a
corresponding salt, preferably in the form of a corresponding hydrochloride, and this
is optionally purified and/or isolated,
and at least one compound of the general formula V is caused to react with at least
one compound of the general formula VII,

in which R1, R2, R3, R4, R5, R6, and R7 have the meanings stated above, in a reaction
medium, optionally in the presence of at least one suitable coupling agent, optionally
in the presence of at least one base,
or with at least one compound of the general formula VIII,

in which R1, R2, R3, R4, R5, R6, and R7 have the meanings stated above and LG
stands for a leaving group, preferably for a chlorine or bromine atom, in a reaction
medium, optionally in the presence of at least one base, to form at least one
compound of the general formula I,

in which T, U, V, W, R1, R2, R3, R4, R5, R6, R7, and R8 have the meanings stated
above and n stands for 1, 2, 3, or 4, and this is optionally purified and/or isolated.
The invention further relates to a process for the production of compounds of the
above general formula I, according to which at least one compound of the general
formula II,

in which
R8, U, T, V, and W have the meanings stated above, is caused to react with at least
one compound of the general formula VII,

in which R1, R2, R3, R4, R5, R6, and R7 have the meanings stated above, in a reaction
medium, optionally in the presence of at least one suitable coupling agent, optionally
in the presence of at least one base,
or with at least one compound of the general formula VIII,

in which R1, R2, R3, R4, R5, R6, and R7 have the meanings stated above and LG
stands for a leaving group, preferably for a chlorine or bromine atom, in a reaction
medium, optionally in the presence of at least one base, to form at least one
compound of the general formula Im,

in which
T, U, V, W, R1, R2, R3, R4, R5, R6, R7, and R8 have the meanings stated above, and
this is optionally purified and/or isolated.
The reaction of compounds of the above general formulas V or X with carboxylic
acids of the above general formula VII to form compounds of the above general
formulas I or Im is carried out preferably in a reaction medium selected from the
group consisting of diethyl ether, tetrahydrofuran, acetonitrile, methanol, ethanol,
(1,2)-dichloroethane, dimethylformamide, dichloromethane and appropriate mixtures
thereof, optionally in the presence of at least one coupling agent, preferably selected

from the group consisting of 1-benzotriazolyloxy-tris(dimethylamino)phosphonium
hexafluorophosphate (BOP), dicyclohexylcarbodiimide (DCC), N'-(3-
dimethylaminopropyl)-N-ethylcarbodiimide (EDCI), diisoproylcarbodiimide, 1,1'-
carbonyldiimidazole (CDI), N-[(dimethylamino)-1 H-1,2,3-triazolo[4.5-b]pyridino-1-
ylmethylene]-N-methylmethanaminium hexafluorophosphate N-oxide (HATU), O-
(benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate (HBTU),
0(benzotriazol-1-yl)-N,N,N',N-tetramethyluronium tetrafluoroborate (TBTU), N-
hydroxybenzotriazole (HOBT), and 1-hydroxy-7-azabenzotriazole (HOAt), optionally
in the presence of at least one organic base, preferably selected from the group
consisting of triethylamine, pyridine, dimethylaminopyridine, N-methylmorpholine,
and diisopropylethylamine, preferably at temperatures ranging from -70 °C to 100 °C.
Alternatively, the reaction of compounds of the above general formulas V or X with
carboxylic derivatives of the above general formula VIII, in which LG stands for a
leaving group, preferably for a chlorine or bromine atom, to form compounds of the
above general formulas Ih or Im is carried out in a reaction medium preferably
selected from the group consisting of diethyl ether, tetrahydrofuran, acetonitrile,
methanol, ethanol, dimethylformamide, dichloromethane and appropriate mixtures
thereof, optionally in the presence of an organic or inorganic base, preferably
selected from the group consisting of triethylamine, dimethylaminopyridine, pyridine,
and diisopropylamine, at temperatures ranging from -70 °C to 100 °C.
The compounds of the above formulas II, III, IV, V, VI, VII, X and VIII are all
commercially available and can be obtained by conventional methods known to the
person skilled in the art.

The synthesis of compounds of the general formula VII is described in the paper "4-
(Methylsulfonylamino)phenyl analogues as vanilloid antagonist showing excellent
analgesic activity and the pharmaceutical compositions comprising the same" by J.
W. Lee et al. [WO 2005/003084-A1]. The appropriate sections of this reference are
hereby to be regarded as part of the disclosure.
The conversions described above can each be carried out under usual conditions
well-known to the person skilled in the art, for example, in respect of pressure or
order of addition of the components. Optionally, the optimal procedure under the
respective conditions can be determined by the person skilled in the art using simple
preliminary tests. The intermediates and end products obtained by the
aforementioned reactions can in each case be isolated and/or purified by
conventional methods known to the person skilled in the art, if desired and/or
necessary. Suitable purification techniques are, for example, extraction processes
and chromatographic processes such as column chromatography or preparative
chromatography. All of the process steps described above and the purification and/or
isolation of intermediate or end products can be carried out partially or completely
under a blanket of inert gas, preferably under a blanket of nitrogen.
The substituted compounds according to the invention of the aforementioned general
formulas I, la, lb and Ic, designated below simply as compounds of the general
formula I, and corresponding stereoisomers can be isolated either in the form of the
free bases thereof, the free acids thereof or in the form of corresponding salts,
particularly physiologically compatible salts.

The free bases of the respective substituted compounds according to the invention of
the aforementioned general formula I and corresponding stereoisomers can, for
example by reaction with an inorganic or organic acid, preferably with hydrochloric
acid, hydrobromic acid, sulfuric acid, phosphoric acid, methanesulfonic acid, p-
toluenesulfonic acid, carbonic acid, formic acid, acetic acid, oxalic acid, succinic acid,
tartaric acid, mandelic acid, fumaric acid, lactic acid, citric acid, glutamic acid, or
aspartic acid, be converted to the corresponding salts, preferably physiologically
compatible salts. The free bases of the respective substituted compounds of the
aforementioned general formula I and corresponding stereoisomers can be likewise
caused to react with the free acid or a salt of a sugar substitute, such as saccharin,
cyclamate, or acesulfam, to form the corresponding physiologically compatible salts.
Similarly, the free acids of the substituted compounds of the aforementioned general
formula I and corresponding stereoisomers can be caused to react with a suitable
base to form the corresponding physiologically compatible salts. Mention may be
made, for example, of the alkali-metal salts, alkaline earth metal salts, or ammonium
salts [NHXR4-X]+ in which x is equal to 0, 1, 2, 3, or 4, and R stands for a linear or
branched C1-4-alkyl radical.
The substituted compounds according to the invention designated by the
aforementioned general formula I and corresponding stereoisomers can optionally,
like the corresponding acids, the corresponding bases or salts of these compounds,
be obtained in the form of the solvates thereof, preferably in the form of the hydrates
thereof, by conventional methods known to the person skilled in the art.

If the substituted compounds according to the invention designated by the
aforementioned general formula I are obtained, following production thereof, in the
form of a mixture of the stereoisomers thereof, preferably in the form of the
racemates thereof or other mixtures of the various enantiomers and/or
diastereoisomers thereof, these compounds can be separated and, if desired,
isolated by methods known to the person skilled in the art. Mention may be made,
for example, of chromatographic separation methods, particularly liquid-
chromatographic methods carried out under standard pressure or at elevated
pressure, preferably MPLC and HPLC methods, and also methods of fractional
crystallization. In particular, individual enantiomers can be separated from each
other, e.g. diastereoisomeric salts formed by means of HPLC on chiral stationary
phase or by means of crystallization with chiral acids, say, (+)-tartaric acid, (-)-tartaric
acid, or (+)-10-camphorsulfonic acid.
The substituted compounds according to the invention designated by the
aforementioned general formula I and corresponding stereoisomers and in each case
the corresponding acids, bases, salts, and solvates are toxicologically safe and are
therefore suitable for use as pharmaceutically active substances in pharmaceuticals.
The invention therefore further relates to a pharmaceutical containing at least one
compound according to the invention of the above general formula I, each optionally
in the form of one of the pure stereoisomers thereof, particularly enantiomers or
diastereoisomers thereof, the racemates thereof or in the form of a mixture of
stereoisomers, particularly the enantiomers and/or diastereoisomers, in an arbitrary
mixing ratio, or each in the form of a corresponding salt, or each in the form of a

corresponding solvate, and optionally one or more pharmaceutically compatible
adjuvants.
These pharmaceuticals according to the invention are particularly suitable for
vanilloid receptor 1-(VR1/TRPV1) regulation, preferably vanilloid receptor 1-
(VR1/TRPV1) inhibition and/or vanilloid receptor 1-(VR1/TRPV1) stimulation.
In another preferred embodiment, the pharmaceuticals according to the invention are
suitable for prophylaxis and/or treatment of disorders or diseases that are at least
partially mediated by vanilloid receptors 1.
Preferably, the pharmaceutical according to the invention is suitable for treatment
and/or prophylaxis of one or more disorders selected from the group consisting of
pain selected from the group consisting of acute pain, chronic pain, neuropathic pain
and visceral pain; arthralgia; hyperalgesia; allodynia; causalgia; migraine; states of
depression; nervous disorders; neurotraumas; neurodegenerative disorders,
preferably selected from the group consisting of multiple sclerosis, Morbus
Alzheimer, Morbus Parkinson, and Morbus Huntington; cognitive dysfunctions,
preferably cognitive deficiency states, more preferably memory defects; epilepsy;
respiratory tract diseases, preferably selected from the group consisting of asthma,
bronchitis, and pneumonia; coughing; urinary incontinence; an overactive bladder
(OAB); disorders and/or injuries of the gastrointestinal tract; duodenal ulcers; gastric
ulcers; colitis syndrome; apoplectic strokes; eye irritations; cutaneous irritations;
neurotic skin conditions; allergic skin diseases; psiorasis; vitiligo; Herpes simplex;
inflammations, preferably inflammation of the intestine, the eyes, the bladder, the
skin, or the nasal mucosa; diarrhea; pruritus; osteoporosis; arthritis; osteo-arthritis;

rheumatic disorders; food intake disorders, preferably selected from the group
consisting of bulimia, cachexia, anorexia, and obesity; medicine addiction; medicine
abuse; withdrawal phenomena following medicine addiction; tolerance development
to pharmaceuticals, particularly to natural or synthetic opioids; drug addiction; drug
abuse; withdrawal phenomena following drug addiction; alcohol addiction; alcohol
abuse and withdrawal phenomena following alcohol addiction; for diuresis; for
antinatriuresis; for affection of the cardiovascular system; for vigilance enhancement;
for treatment of wounds and/or burning; for treatment of severed nerves; for libido
enhancement; for modulation of movement activity; for anxiolysis; for local
anesthesia and/or for inhibition of undesirable side effects, preferably selected from
the group consisting of hyperthermia, hypertension, and bronchial constriction, as
caused by administration of vanilloid receptor 1 (VR1/TRPV1 receptor) agonists,
preferably selected from the group consisting of capsaicin, resiniferatoxin, olvanil,
arvanil, SDZ-249665, SDZ-249482, nuvanil, and capsavanil.
The pharmaceutical according to the invention is particularly preferably suitable for
treatment and/or prophylaxis of one or more disorders selected from the group
consisting of pain, preferably pain selected from the group consisting of acute pain,
chronic pain, neuropathic pain, and visceral pain; arthralgia; migraine; states of
depression; neurodegenerative disorders, preferably selected from the group
consisting of multiple sclerosis, Morbus Alzheimer, Morbus Parkinson, and Morbus
Huntington; cognitive dysfunctions, preferably cognitive deficiency states, more
preferably memory defects; inflammation, preferably inflammation of the intestine, the
eyes, the bladder, the skin or the nasal mucosa; urinary incontinence; an overactive
bladder (OAB); medicine addiction; medicine abuse; withdrawal phenomena
following medicine addiction; tolerance development to pharmaceuticals, preferably

tolerance development to natural or synthetic opioids; drug addiction; drug abuse;
withdrawal phenomena following drug addiction; alcohol addiction; alcohol abuse and
withdrawal phenomena following alcohol addiction.
The pharmaceutical according to the invention is most preferably suitable for
treatment and/or prophylaxis of pain, preferably pain selected from the group
consisting of acute pain, chronic pain, neuropathic pain, and visceral pain, and/or
urinary incontinence.
The invention further relates to the use of at least one compound according to the
invention and optionally one or more pharmaceutically compatible adjuvants for the
production of a pharmaceutical for vanilloid receptor 1-(VR1/TRPV1) regulation,
preferably vanilloid receptor 1-(VR1/TRPV1) inhibition and/or vanilloid receptor 1-
(VR1/TRPV1) stimulation.
Preference is given to the use of at least one substituted compound according to the
invention and optionally one or more pharmaceutically compatible adjuvants for the
production of a pharmaceutical for the prophylaxis and/or treatment of disorders or
diseases which are at least partially mediated by vanilloid receptors 1.
Particular preference is given to the use of at least one compound according to the
invention and optionally one or more pharmaceutically compatible adjuvants for the
production of a pharmaceutical for treatment and/or prophylaxis of one or more
disorders selected from the group consisting of pain, preferably of pain selected from
the group consisting of acute pain, chronic pain, neuropathic pain, visceral pain, and
arthralgia.

Particular preference is given to the use at least one compound according to the
invention and optionally one or more pharmaceutically compatible adjuvants for the
production of a pharmaceutical for treatment and/or prophylaxis of one or more
disorders selected from the group consisting of hyperalgesia; allodynia; causalgia;
migraine; states of depression; nervous disorders; neurotraumas; neurodegenerative
disorders, preferably selected from the group consisting of multiple sclerosis, Morbus
Alzheimer, Morbus Parkinson, and Morbus Huntington; cognitive dysfunctions,
preferably cognitive deficiency states, more preferably memory defects; epilepsy;
respiratory tract diseases, preferably selected from the group consisting of asthma,
bronchitis, and pneumonia; coughing; urinary incontinence; an overactive bladder
(OAB); disorders and/or injuries of the gastrointestinal tract; duodenal ulcers; gastric
ulcers; colitis syndrome; apoplectic strokes; eye irritations; cutaneous irritations;
neurotic skin conditions; allergic skin diseases; psiorasis; vitiligo; Herpes simplex;
inflammation, preferably inflammation of the intestine, the eyes, the bladder, the skin,
or the nasal mucosa; diarrhea; pruritus; osteoporosis; arthritis; osteo-arthritis;
rheumatic disorders; food intake disorders, preferably selected from the group
consisting of bulimia, cachexia, anorexia, and obesity; medicine addiction; medicine
abuse; withdrawal phenomena following medicine addiction; tolerance development
to pharmaceuticals, preferably to natural or synthetic opioids; drug addiction; drug
abuse; withdrawal phenomena following drug addiction; alcohol addiction; alcohol
abuse and withdrawal phenomena following alcohol addiction; for diuresis; for
antinatriuresis; for affection of the cardiovascular system; for vigilance enhancement;
for treatment of wounds and/or burning; for treatment of severed nerves; for libido
enhancement; for modulation of movement activity; for anxiolysis; for local
anesthesia and/or for inhibition of undesirable side effects, preferably selected from

the group consisting of hyperthermia, hypertension, and bronchial constriction, as
caused by administration of vanilloid receptor 1 (VR1/TRPV1 receptor) agonists,
preferably selected from the group consisting of capsaicin, resiniferatoxin, olvanil,
arvanil, SDZ-249665, SDZ-249482, nuvanil, and capsavanil.
Very particular preference is given to the use of at least one substituted compound
according to the invention and optionally one or more pharmaceutically compatible
adjuvants for the production of a pharmaceutical for treatment and/or prophylaxis of
one or more disorders selected from the group consisting of pain, preferably pain
selected from the group consisting of acute pain, chronic pain, neuropathic pain, and
visceral pain; arthralgia; migraine; states of depression; neurodegenerative disorders,
preferably selected from the group consisting of multiple sclerosis, Morbus
Alzheimer, Morbus Parkinson, and Morbus Huntington; cognitive dysfunctions,
preferably cognitive deficiency states, more preferably memory defects;
inflammation, preferably inflammation of the intestine, the eyes, the bladder, the skin,
or the nasal mucosa; urinary incontinence; an overactive bladder (OAB); medicine
addiction; medicine abuse; withdrawal phenomena following medicine addiction;
tolerance development to pharmaceuticals, preferably tolerance development to
natural or synthetic opioids, drug addiction; drug abuse; withdrawal phenomena
following drug addiction; alcohol addiction; alcohol abuse and withdrawal phenomena
following alcohol addiction.
Even more preference is given to the use of at least one substituted compound
according to the invention and optionally one or more pharmaceutically compatible
adjuvants for the production of a pharmaceutical for treatment and/or prophylaxis of

pain, preferably selected from the group consisting of acute pain, chronic pain,
neuropathic pain, and visceral pain, and/or urinary incontinence.
The pharmaceutical according to the invention is suitable for administration to adults
and children including infants and babies.
The pharmaceutical according to the invention can exist as a liquid, semisolid, or
solid pharmaceutical dosage form, for example, in the form of injection fluids, drops,
juices, syrups, sprays, suspensions, tablets, patches, capsules, plasters,
suppositories, ointments, creams, lotions, gels, emulsions, or aerosols, or in a
multiparticular form, for example, in the form of pellets or granules, optionally
compressed to tablets, filled into in capsules, or suspended in a liquid, and can be
administered as such.
In addition to at least one substituted compound of the above general formula I,
optionally in the form of a pure stereoisomer thereof, particularly an enantiomer or
diastereoisomer, the racemate thereof or in the form of mixtures of the
stereoisomers, particularly the enantiomers or diastereoisomers, in an arbitrary
mixing ratio, or optionally in the form of a corresponding salt or each in the form of a
corresponding solvate, the pharmaceutical according to the invention usually
contains further physiologically compatible pharmaceutical adjuvants, which, for
example, can be selected from the group consisting of vehicles, fillers, solvents,
diluents, surfactants, dyes, preservatives, blasting agents, slip agents, lubricants,
flavors, and binding agents.

The selection of the physiologically compatible adjuvants and the amount thereof to
be used depends on whether the pharmaceutical is to be applied orally,
subcutaneously, parenterally, intravenously, intraperitoneally, intradermally,
intramuscularly, intranasally, buccally, rectally or locally, e.g. to infected parts of the
skin, the mucous membrane, or the eyes. Preparations suitable for oral
administration are preferably in the form of tablets, dragees, capsules, granules,
pellets, drops, juices, and syrups, and preparations suitable for parenteral, topical
and inhalative administration are solutions, suspensions, readily reconstitutable dry
preparations, and sprays. The substituted compounds according to the invention
used in the pharmaceutical according to the invention in a depot in dissolved form or
in a plaster, optionally with the addition of skin penetration-enhancing agents, are
suitable percutaneous administration forms. Formulations for oral or percutaneous
application may be such as to effect delayed release of the respective substituted
compound according to the invention.
The production of the pharmaceutical according to the invention is effected by
conventional means, devices, methods, and processes, as are known in the prior art,
such as are described, for example, in "Remington's Pharmaceutical Sciences",
Editor A.R. Gennaro, 17th Edition, Mack Publishing Company, Easton, Pa, 1985,
particularly in Section 8, Chapters 76 to 93. The corresponding description is
incorporated herein by reference and is to be regarded as part of the disclosure. The
amount of the respective substituted compounds according to the invention of the
above general formula I to be administered to the patients can vary and is
dependent, for example, on the weight or age of the patient and also on the method
of administration, the indication, and the severity of the disorder. Usually from 0.001
to 100 mg/kg, preferably from 0.05 to 75 mg/kg and more preferably from 0.05 to 50

mg/kg, of body weight of the patient of at least one such compound according to the
invention are administered.

Pharmacological methods:
I. Functional investigation on the vanilloid receptor 1 (VRI/TRPV1 receptor)
The agonistic or antagonistic action of the substances to be investigated on the
vanilloid receptor 1 (VR1/TRPV1) of the species rat can be determined using the
following assay. According to this assay, the Ca2+ influx through the receptor
channel is quantified with the aid of a Ca2+-sensitive dye (Type Fluo-4, Molecular
Probes Europe BV, Leiden Netherlands) in a fluorescent imaging plate reader
(FLIPR, Molecular Devices, Sunnyvale, USA).
Method:
Complete medium: 50 mL of HAMS F12 Nutrient Mixture (Gibco Invitrogen GmbH,
Karlsruhe, Germany) with
10% by volume of FCS (fetal calf serum, Gibco Invitrogen GmbH, Karlsruhe,
Germany, heat-inactivated);
2mM of L-glutamine (Sigma, Munich, Germany);
1% by weight of AA solution (antibiotics/antimycotics solution, PAA, Pasching,
Austria)
and 25 ng/mL of Medium NGF (2.5 S, Gibco Invitrogen GmbH, Karlsruhe, Germany)
Cell culture plate: Poly-D-lysine-coated, black 96-well plates with a clear bottom (96-
well black/clear plate, BD Biosciences, Heidelberg, Germany) are additionally coated
with laminin (Gibco Invitrogen GmbH, Karlsruhe, Germany) by diluting laminin to a
concentration of 100 µg/mL with PBS (Ca-Mg-free PBS, Gibco Invitrogen GmbH,

Karlsruhe, Germany). Aliquots having a concentration of 100 µg/mL of laminin are
taken and stored at -20 °C. The aliquots are diluted with PBS in the ratio 1:10 to
10 µg/mL of laminin and in each case 50 uL of the solution is pipeted into a well of
the cell culture plate. The cell culture plates are incubated at 37 °C for at least two
hours, the supernatant solution is aspirated and the wells are in each case washed
twice with PBS. The coated cell culture plates are stored with supernatant PBS and
this is removed only directly before the addition of the cells.
Preparation of the cells:
The vertebral column is removed from decapitated rats and this is laid directly in a
cold, i.e. ice bath-surrounded, HBSS buffer (Hank's buffered saline solution, Gibco
Invitrogen GmbH, Karlsruhe, Germany) and 1% by volume of an AA solution
(antibiotics/antimycotics solution, PAA, Pasching, Austria) is added. The vertebral
column is cut in two, longitudinally, and the vertebral canal is removed together with
fascias. Subsequently, the dorsal root ganglia (DRGs) are removed and in turn
stored in cold HBSS buffer to which 1% by volume of an AA solution has been
added. The DRGs completely freed from blood residues and spinal nerves are in
each case transferred to 500 µL of cold collagenase Type 2 (PAA, Pasching, Austria)
and incubated at 37 °C for 35 minutes. After the addition of 2.5% by volume of trypsin
(PAA, Pasching, Austria), the preparation is incubated at 37 °C for a further 10
minutes. On completion of incubation, the enzyme solution is carefully pipeted off
and 500 uL of complete medium are added to the DRGs in each case. The DRGs are
in each case repeatedly suspended, drawn through No. 1, No. 12, and No. 16
needles by means of a syringe and transferred to 50 mL Falcon tubes and these are

filled to 15 mL with complete medium. The contents of each Falcon tube are in each
case filtered through a 70 µm Falcon filter insert and centrifuged at 1200 rpm and RT
for 10 minutes. The resulting pellet is in each case taken up in 250 µL of complete
medium and the cell count is determined.
The number of cells in the suspension is adjusted to 3 x 105 per mL and in each case
150 µL of this suspension are added to a well of the cell culture plates coated as
described above. The plates are allowed to stand at 37 °C, 5% by volume of CO2 and
95% relative humidity for two to three days in an incubator.
Subsequently, the cells are loaded with 2 µM of Fluo-4 and 0.01% by volume of
Pluronic F127 (Molecular Probes Europe BV, Leiden Netherlands) in HBSS buffer
(Hank's buffered saline solution, Gibco Invitrogen GmbH, Karlsruhe, Germany) at
37°C for 30 min, washed 3 times with HBSS buffer and, after a further incubation of
15 minutes at RT, employed in the FLIPR assay for Ca2+ measurement. The Ca2+-
dependent fluorescence is measured before and after addition of substances (λex =
488 nm, λem = 540 nm). Quantification is carried out by measuring the highest
fluorescence intensity (FC, fluorescence counts) over time.
FLIPR assay:
The FLIPR protocol consists of two substance additions. Initially, the compounds to
be tested (10 µM) are pipeted onto the cells and the Ca2+ influx is compared with the
control (capsaicin 10 µM). Information is gained therefrom in percentage activation
relative to the Ca2+ signal after addition of 10 µM of capsaicin (CP). After incubation
for 5 minutes, 100 nM of capsaicin are applied and the influx of Ca2+ is likewise

determined.
Desensitizing agonists and antagonists lead to suppression of the Ca2+ influx. The
percentage inhibition is calculated in comparison with the maximum inhibition
achieved with 10 µM of capsaicin.
Triple determinations (n=3) are carried out and these are repeated in at least 3
independent experiments (N=4).
Based on the percentage displacement effected by different concentrations of the
compounds of the general formula I to be tested, IC50 inhibition concentrations that
cause 50 percent displacement of capsaicin are calculated. Conversion using the
Cheng Prusoff equation gave Ki values for the test substances (Cheng, Prusoff;
Bioch. Pharmacol. 22, 3099-3108, 1973).
II. Functional investigations on the vanilloid receptor (VR1)
The agonistic or antagonistic action of the substances to be examined on the
vanilloid receptor (VR1) can also be determined by the following assay. According to
this assay, the Ca2+ influx through the canal is quantified with the aid of a Ca2+-
sensitive dye (type Fluo-4, Molecular Probes, Europe BV, Leiden, Netherlands) in a
fluorescent imaging plate reader (FLIPR, Molecular Devices, Sunnyvale, USA).
Method:
Chinese hamster ovary cells (CHO-K1 cells, European Collection of Cell Cultures
(ECACC) UK) are stably transfected with the VR1 gene. For carrying out functional
investigations, these cells are plated on poly-D-lysine-coated, black 96-well plates

with a clear bottom (BD Biosciences, Heidelberg, Germany) in a density of 25,000
cells/well. The cells are incubated overnight at 37 °C and 5% CO2 in a culture
medium (Nutrient Mixture 'am's F12, 10% by volume of FCS (fetal calf serum),
18 µg/mL of L-proline). On the following day the cells are incubated with Fluo-4 (Fluo-
4 2 µM, Pluronic F127 0.01 by volume, Molecular Probes in HBSS (Hank's buffered
saline solution), Gibco Invitrogen GmbH, Karlsruhe, Germany) for 30 minutes at
37 °C. The plates are then washed 3 times with HBSS buffer and, after another
incubation over a period of 15 minutes at RT, are used in the FLIPR for Ca2+
measurement. The Ca2+-dependent fluorescence is measured prior to and following
the addition of the substances being examined (wavelength λex = 488 nm, λem = 540
nm). Quantification is carried out by measuring the highest fluorescence intensity
(FC, fluorescence counts) over time.
FLIPR assay:
The FLIPR protocol consists of two substance additions. First of all, the substances
to be tested (10 µM) are pipeted onto the cells and the Ca2+ influx is compared with
the control (capsaicin 10 µM) (percentage activation based on the Ca2+ signal
following addition of 10 µM of capsaicin). Following incubation over a period of 5
minutes 100 nM of capsaicin are applied and the influx of Ca2+ is likewise
determined.
Desensitizing agonists and antagonists led to a suppression of the Ca2+ influx. The
percentage inhibition compared with the maximum inhibition achieved with 10 µM of
capsaicin is calculated.

Based on the percentage displacement effected by different concentrations of the
compounds of the general formula I to be tested, IC50 inhibition concentrations that
cause 50 percent displacement of capsaicin are calculated. Conversion using the
Cheng Prusoff equation gave Ki values for the test substances (Cheng, Prusoff;
Bioch. Pharmacol. 22, 3099-3108, 1973).
III. Formalin test on mice
The investigation for the determination of the antinociceptive action of the
compounds according to the invention is carried out in the formalin test on male mice
(NMRI, of 20 to 30 g body weight, Iffa, Credo, Belgium).
In the formalin test, the first (early) phase (0 to 15 minutes after the formalin injection)
and the second (late) phase (15 to 60 minutes after the formalin injection) are
distinguished according to D. Dubuisson et al., Pain 1977, 4, 161-174. The early
phase, as a direct reaction to the formalin injection, is a model of acute pain, whereas
the late phase is regarded as a model of persistent (chronic) pain (T.J. Coderre et al.,
Pain 1993, 52, 259-285). The appropriate literature references are incorporated
herein by reference and are to be regarded as part of the disclosure.
The compounds according to the invention are examined in the second phase of the
formalin test, in order to obtain information concerning a substance's action on
chronic/inflammatory pain.
The point in time of administration of the compounds according to the invention
before the formalin injection is selected according to the method of administration of

the compounds according to the invention. Intravenous administration of 10 mg/kg of
body weight of the test substances is carried out 5 minutes before the formalin
injection. This is carried out by a single subcutaneous formalin injection (20 µL, 1%
strength aqueous solution) into the dorsal side of the right hind paw so that in the
case of free-moving experimental animals a nociceptive reaction is induced which is
manifested by marked licking and biting of the relevant paw.
The nociceptive behavior is then continuously registered during an investigation
period of three minutes in the second (late) phase of the formalin test (21 to 24
minutes after the formalin injection) by observation of the animals. Quantification of
the pain behavior is carried out by summating the seconds during which the animals
exhibit licking and biting of the relevant paw during the investigation period.
In each case, comparison is carried out with control animals, which receive, instead
of the compounds according to the invention, a vehicle (0.9% strength aqueous
sodium chloride solution) prior to formalin administration. Based on the quantification
of the pain behavior, the substance's action in the formalin test is determined as the
degree of change compared with the corresponding control in percent.
Following injection of the substances having an antinociceptive action in the formalin
test, the aforementioned behavioral patterns of the animals, i.e. licking and biting,
decrease or cease.
IV. Test for analgesic effectiveness in the writhing test

Investigation of the compounds of the general formula I according to the invention for
analgetic effectiveness was carried out based on phenylquinone-induced writhing in
mice, modified in accordance with I.e. Hendershot and J. Forsaith (1959) J.
Pharmacol. Exp. Ther. 125, 237-240. The corresponding literature reference is
incorporated herein by reference and is to be regarded as part of the disclosure.
For this purpose, male NMRI mice having a weight of from 25 to 30 g were used.
Groups of 10 animals per dose of the test compound received by intraperitoneal
administration, 10 minutes after intravenous administration of the compounds to be
tested, 0.3 mL/mouse of a 0.02% strength aqueous solution of phenylquinone
(phenylbenzoquinone, Sigma, Deisenhofen, Germany and produced by adding to the
solution 5% by weight of ethanol and storing it in a water bath at 45 °C). The animals
were placed individually in observation cages. With the aid of a pushbutton counter,
the number of pain-induced stretching movements (so-called writhing reactions -
straightening of the body with stretching of the rear extremities) was counted over a
period of from 5 to 20 minutes following the administration of the phenylquinone. The
control was provided by animals receiving only physiological saline. All of the
compounds were tested using the standard dosage of 10 mg/kg.
V. Hypothermia assay in mice
Description of the method:
The hypothermia assay was carried out on male NMRI mice (weight 25-35 gram,
breeder IFFA CREDO, Brussels, Belgium). The animals were kept under
standardized conditions: light/dark rhythm (from 6:00 to 18:00 hours light phase; from
18:00 to 6:00 hours dark phase), RT 19-22 °C, relative air humidity 35-70 %, 15 air

changes per hour, air movement (ssniff R/M-Haltung, ssniff Spezialdiaeten GmbH, Soest, Germany) and tap water.
Water and feed were withdrawn during the experiment. All animals were used only
once during the experiment. The animals had an acclimatization period of at least 5
days.
Acute administration of capsaicin (VR-1 agonist) leads to a drop in the core
temperature of the body in rats and mice due to stimulation of heat sensors. Only
specifically effective VR-1 receptor antagonists can antagonize the capsaicin-induced
hypothermia. By contrast, hypothermia induced by morphine is not antagonized by
VR-1 antagonists. This model is therefore suitable for identifying substances with VR-
1 antagonistic properties via their effect on body temperature.
Measurement of the core temperature is carried out using a digital thermometer
(Thermalert TH-5, physitemp, Clifton NJ, USA). The sensing element is inserted into
the rectum of the animals.
To give an individual basic value for each animal, the body temperature is measured
twice at an interval of approximately half an hour. One group of animals (n = 6 to 10)
then receives an intraperitoneal (i.p.) application of capsaicin 3 mg/kg and vehicle
(control group). Another group of animals receives the substance to be tested (i.v. or
p.o.) and additionally capsaicin (3 mg/kg) i.p. The administration of the test
substance is carried out i.v. 10 min, or p.o 15 minutes, prior to capsaicin. The body
temperature is then measured 7.5/15 and 30 min following capsaicin (i.v. + i.p.) or
15/30/60/90/120 min (p.o. + i.p.) following capsaicin. In addition, one group of
animals is treated with the test substance only and one group with vehicle only. The

evaluation or representation of the measured values as mean +/- SEM of the
absolute values is presented as a graphical representation. The antagonistic action is
calculated as the percentage reduction of the capsaicin-induced hypothermia.
VI. Neuropathic pain in mice
The investigation on effectiveness on neuropathic pain was examined using the
Bennett Model (chronic constriction injury; Bennett und Xie, 1988, Pain 33:87-107).
Three loose ligatures are tied around the right ischiadic nerve of Ketavet/Rompun-
anesthetized NMRI mice weighing 16-18 g. The animals develop hypersensitivity of
the nervate paw caused by the damaged nerve, which hypersensitivity is quantified,
following a recovery phase of one week, over a period of approximately three weeks
by means of a cold metal plate (temperature 4 °C) (cold allodynia). The animals are
observed on this plate over a period of 2 min, and the withdrawal reactions of the
damaged paw are counted. Based on the pre-value prior to administration of
substance, the substance's action over a certain period of time is determined at
various points in time (e.g., 15, 30, 45, or 60 min following administration) and the
resultant area under the curve (AUC) and/or the inhibition of cold allodynia at the
individual measuring points was/were expressed as percentage action relative to the
vehicle control (AUC) or to the starting value (individual measuring points). The group
size is n= 10, the significance of an anti-allodynic action (*= p with the aid of an analysis of variance with repeated measurement and Bonferroni
post hoc analysis.

The invention is described below with reference to some examples. These
explanations are by way of example only and do not restrict the general inventive
concept.

Examples:
The yields of the compounds produced were not optimized.
All temperatures are uncorrected.
The statement "equivalents" denotes mol equivalents, "RT" room temperature, "M"
and "N" are concentrations in mol/L, "aq." aqueous, "sat." saturated, "soln." solution,
Further abbreviations:
AcOH acetic acid
DCM dichloromethane
DMF N,N-dimethylformamide
EDCI N-ethyl-N'-(3-dimethylaminopropyl)carbodiimide hydrochloride
EA ethyl acetate
H2O water
HOBt N-hydroxybenzotriazole
MeOH methanol
THF tetrahydrofuran
The chemicals and solvents used were obtained commercially from the usual
suppliers (Acros, Avocado, Aldrich, Bachem, Fluka, Lancaster, Maybridge, Merck,
Sigma, TCI, Oakwood etc.) or synthesized by usual methods known to the person
skilled in the art.

The stationary phase used for column chromatography was silica gel 60 (0.0-0 -
0.063 mm) supplied by E. Merck, Darmstadt.
The thin-layer chromatographic analyses were carried out using preformed HPTLC
plates, Silica Gel 60 F 254, supplied by E. Merck, Darmstadt.
The mixing ratios of solvents, mobile solvents, or for chromatographic analyses are
always stated in vol/vo!.
Analysis was carried out by mass spectroscopy and NMR.
1. General instructions for the preparation of amines of the general formula V-
A.
Preparation of amines of the general formula V-A is carried out as illustrated by the
following scheme 1.

Stage 1: Preparation of nitriles of the general formula Vl-B
Method A:

Compounds of the general formula Vl-A (1 equivalent), in which R8, U, T, and V have
the meanings stated above and m stands for 0,1,2, or 3, are stirred with an amine of
the general formula HNR40R41 (6 equivalents) over a period of 48 hours at RT. To the
reaction mixture there is added 1N hydrochloric acid, and the mixture is extracted
with EA a number of times. The aqueous phase is saturated with NaCI and then
again extracted with EA. The combined organic phases are washed with 1N
hydrochloric acid and with sat. aq. NaCI soln., dried over MgSO4, and the solvent is
removed in vacuo.
The following compound was obtained by method A:
6'-tert-Butyl-4-methyl-3,4,5,6-tetrahydro-2H-[1,2']bipyridinyl-3'-carbonitrile

1H-NMR(CDCI3) δ 7.65 (d, 1H, J = 7.9 Hz, Ar), 6.70 (d, 1H, J = 8.0 Hz, Ar), 4.45 (m,
2H, piperidine), 2.98 (m, 2H, piperidine), 1.75-1.24 (m, 5H, piperidine), 1.29 (s, 9H,
C(CH3)3), 0.98 (d, 3H, J = 5.9 Hz, CHCH3)
IR 2956, 2213, 1583, 1550, 1452, 1230, 965 crrT1
Method B:
Compounds of the general formula Vl-A (1 equivalent), in which R8, U, T, and V have
the meanings stated above and m stands for 0,1,2, or 3, are stirred with an amine of

the general formula HNR40R41 (2 equivalents) and DBU [1.8-diaza-
bicyclo[5.4.0]undec-7-ene] (2 equivalents) in acetonitrile (7 mL per mmol of the
compound of formula Vl-A) over a period of 12 hours at RT. The reaction mixture is
extracted with EA a number of times. The combined organic phases are washed with
sat. aq. NaCI solution, dried over MgSO4, and the solvent is removed in vacuo. The
residue is purified in each case by column chromatography (SiO2, various mixtures of
hexane/EA).
The following compound was produced by method B.
6-(Trifluoromethyl)-2-(4-methylpiperidin-1-yl)pyridine-3-carbonitrile

1H NMR (300 M Hz, CDCI3) δ 7.87 (d, 1 h, J = 7.8 Hz), 6.95 (d, 1 h, J = 7.8 Hz), 4.53
(m, 2 H), 3.05 (m, 2 H), 1.78 (m, 2 H), 1.64 (m, 1 H), 1.29 (m, 2 H), 1.00 (d, 3 H, J =
6.6 Hz); IR (PUR) 2926, 2852, 2218, 1590, 1497, 1456, 1324, 1237, 1186, 1147,
1082, of 963 cm-1; MS (FAB) m/z 270 (M+H)
Step 2:
Method 1
Compounds of the general formula Vl-B (5 mmol), in which R8, R40, R41, U, T, and V
have the meanings stated above and m stands for 0, 1, 2, or 3, palladium-on-
charcoal (10%, 500 mg) and conc, hydrochloric acid (3 mL) are dissolved in MeOH

(30 mL) and exposed to a hydrogen atmosphere over a period of 6 hours at RT. The
reaction mixture is filtered over Celite and the filtrate is concentrated in vacuo. The
residue is purified by means of flash chromatography (SiO2, EA).
Method 2:
Compounds of the general formula Vl-B (2 mmol), in which R8, R40, R41, U, T, and V
have the meanings stated above and m stands for 0, 1, 2, or 3, are dissolved in THF
(10 mL, 10 mL), and BH3'S(CH3)2 [2.0 M in THF, 3 mL, 3 equivalents] is added. The
reaction mixture is heated under reflux over a period of 8 hours, aq. HCI (2N) is
added and the reaction mixture is again heated under reflux for 30 minutes. Aq.
sodium hydroxide solution (2N) is added to the reaction mixture, and the mixture is
washed with EA. The combined organic phases are washed with sat. aq. NaCI
solution and dried over magnesium sulfate. The solvent is removed in vacuo and the
residue purified by column chromatography (SiO2, various mixtures of
dichloromethane and MeOH as mobile solvent).
The following compounds were obtained by method 2.
(6-(Trifluoromethyl)-2-(4-methylpiperidin-1-yl)pyridin-3-yl)methanamine

1H NMR (300 M Hz, CDCI3) δ 7.89 (d, 1 H, J = 7.8 Hz), 7.33 (d, 1H, J = 7.8 Hz), 3.88
(s, 2H), 3.39 (m, 2 H), 2.83 (m, 2 H), 1.75 (m, 2 H), 1.55 (m, 1 H), 1.38 (m, 2 H), 1.00
(d, 3 H, J = 6.6 Hz); MS (FAB) m/z 274(M+H)
C-(6'-tert-Butyl-4-methyl-3,4,5,6-tetrahydro-2H-[1,2']bipyridinyl-3'-yl)-
methylamine

1H-NMR (CDCI3) δ 7.48 (d, 1H, J = 7.7 Hz, Ar), 6.90 (d, 1H, J = 7.7 Hz, Ar), 3.82 (s,
2H, CH2NH2), 3.38 (m, 2H, piperidine), 2.81 (m, 2H, piperidine), 1.73-1.28 (m, 5H,
piperidine), 1.31 (s, 9H, C(CH3)3), 0.98 (d, 3H, J = 6.4 Hz, CHCH3)
IR 3363, 2954, 1571, 1451, 1400, 1372, 1234, 960 cm"1
2. General instructions for the preparation of amines of the general formula V-E
The preparation of amines of the general formula V-E is carried out as illustrated in
the following scheme 2.

Scheme 2.

Step 1:
Synthesis of 2-(cyclohexylthio)-6-(trifluoromethyl)nicotinonitrile

1.3 Equivalents of NaH (4.9 g, 0.124 mol) were dissolved in 50 mL of DMF under a
blanket of nitrogen. Following the addition of 1.2 equivalents of cyclohexanethiol
(14.2 mL, 0.116 mol), the mixture was stirred at RT over a period of 1.5 h. The
resulting suspension was cooled to 10 °C and added dropwise to 1 equivalent of 2-
chloro-6-(trifluoromethyl)nicotinonitrile (20 g, 0.096 mol) in 50 mL of DMF and stirred
over a period of 2 h at RT. To the reaction mixture there was added sat. aq. NH4CI
soln. and the mixture was diluted with 1 L of water and extracted with EA (3 x 200
mL) a number of times. The combined organic phases were washed with sat. aq.
NaCI solution, dried over MgSO4 and concentrated in vacuo. Column
chromatographic purification (silica gel 100-200 mesh, eluant: 2% EA in hexane)
yielded 26 g (93.8%) of product.
1H NMR (300 M Hz, CDCI3) δ 7.94 (d ,1 H, J = 7.9 Hz), 7.34 (d, 1 H, J = 7.9 Hz), 4.00
(m, 1 H),1.90-2.14 (m, 2 H), 1.42-1.88 (m, 8 H)
IR (neat) 2930, 2854, 2232, 1643, 1573, 1447, 1334, 1245, 1186, 1149, 1107, 851
cm"1
MS (FAB) m/z 287 (M+H)
Step 2:
Synthesis of (2-(cyclohexylthio)-6-(trifluoromethyl)-pyridin-3-yl)methanamine
dihydrochloride

The nitrile (26 g, 0.091 mol) was dissolved in 600 mL of THF under a blanket of
nitrogen and cooled to 5 °C. BH3-dimethyl sulfide (13.78 g, 0.182 mol) was added
dropwise and the mixture was boiled under reflux over a period of 20 h. After cooling
to 5 °C, 100 mL of MeOH were added to the reaction batch and the mixture was
stirred at RT over a period of 15 minutes. Di-tert-butyldicarbonate (29.7 g, 0.136 mol)
was then added and the mixture was stirred at RT for 30 min. Following the removal
of the solvent in vacuo, the crude product was purified by column chromatography
(silica gel 100-200 mesh, eluant: 10% EA in hexane) and 23.4 g (66%) of product
were obtained.
The crude product was dissolved in 120 mL of sat. HCI/dioxane soln., and the
solution was stirred at RT over a period of 6 h. Following the removal of the solvent in
vacuo, the solid matter was washed with 10% EA in hexane (2 x 100 mL) and
isolated by filtration.
Yield: 17 g (88.8%)
1H NMR (DMSO-d6, 400 M Hz): δ 8.8 (s,2H), 8.05(d,1H), 7.76 (d,1H), 4.01 (s, 1H),
3.86-3.93 (m,1H), 2.02-2.08 (m,2H), 1.71-1.74 (m,2H), 1.40-1.60 (m,6H).
3. General instructions for the preparation of amines of the general formula V-B
The preparation of amines of the general formula V-B is carried out as illustrated in
the following scheme 3.

Step 1: Preparation of nitriles of the general formula Vl-C
Compounds of the general formula Vl-A (1 equivalent), in which R8, U, T, and V have
the meanings stated above and m stands for 0,1,2, or 3, are stirred with an alcohol
of the general formula HO-R42 (3.5 equivalents) and DBU [1,8-diaza-
bicyclo[5.4.0]undec-7-ene] (3,5 equivalents) in acetonitrile (7 mL per mmol of the
compound of formula Vl-A) over a period of 12 hours at RT. The reaction mixture is
extracted with EA a number of times. The combined organic phases are washed with
sat. aq. NaCI soln. and dried over MgSO4, and the solvent is removed in vacuo. The
residue is purified in each case by column chromatography (SiO2, various mixtures of
hexane/EA).
Method 2:
Compounds of the general formula Vl-C (2 mmol), in which R8, R42, U, T, and V have
the meanings stated above and m stands for 0, 1,2, or 3, are dissolved in THF
(10 mL, 10 mL) and BH3'S(CH3)2 [2.0 M in THF, 3 mL, 3 equivalent] is added. The
reaction mixture is heated under reflux over a period of 8 hours, aq. HCI (2N) is
added and the reaction mixture is again heated under reflux for 30 minutes. Aq.
sodium hydroxide solution (2N) is added to the reaction mixture, and the mixture is
washed with EA. The combined organic phases are washed with sat. aq. NaCI
solution and dried over magnesium sulfate. The solvent is removed in vacuo and the

residue is purified by column chromatography (SiO2, various mixtures of
dichloromethane and methanol as mobile solvent).
Method 3:
Compounds of the general formula Vl-C (1,5 mmol), in which R8, R42, U, T, and V
have the meanings stated above and m stands for 0,1,2, or 3, are dissolved in
diethyl ether (3 mL) and a suspension of lithium aluminum hydride (3 mmol) in ether
(5 mL) is slowly added dropwise at 0 °C. The reaction mixture is heated under reflux
over a period of 4 hours and methanol followed by 1N aq. NaOH solution are slowly
added dropwise at 0 °C. The reaction mixture is diluted with methanol and filtered
over Celite. The solvent is removed in vacuo and the residue is purified by column
chromatography (SiO2, various mixtures of dichloromethane and methanol as mobile
solvent).
4. General instructions for the preparation of amines of the general formula V-C
The preparation of amines of the general formula V-C is carried out as illustrated in
the following scheme 4.

Step 1:
Preparation of nitriles of the general formula Vl-D
Compounds of the general formula Vl-A (1 equivalent), in which R8, U, T, and V have
the meanings stated above and m stands for 0,1,2, or 3, are dissolved together with
bis(triphenylphosphine)palladium dichloride (7 mol%) and copper(l) iodide (14 mol%)
in 1-methyl-2-pyrrolidinone (7 mL per mmol of the compound of the general formula
Vl-A). Following a period of 10 minutes the alkyne of the general formula HC=C-R38
(3,5 equivalents) and N,N-diisopropylethylamine (2 equivalents) are added, and the
reaction mixture is stirred over a period of 12 h at a temperature between 90 and
110 °C. The reaction mixture is filtered over Celite and extracted with EA a number of
times. The combined organic phases are washed with sat. aq. NaCI solution, dried
over MgSO4, and the solvent is removed in vacuo. The residue is purified in each
case by column chromatography (SiO2, various mixtures of hexane/EA).
5. General instructions for the preparation of amines of the general formula V-D
The preparation of amines of the general formula V-D is carried out as illustrated in
the following scheme 5.

Step 1: Preparation of nitriles of the general formula Vl-E
Compounds of the general formula Vl-A (1 equivalent), in which R8, U, T, and V have
the aforementioned meanings and m stands for 0, 1, 2, or 3, are stirred with
palladium dichloride (5 mol%) and a compound of the general formula R38-B(OH)2 (2
equivalents), in which R38 stands for aryl, heteroaryl, or cycloalkenyl, in a solvent
mixture of toluene/dioxane/2N aq. sodium carbonate solution (20 mL per 1 mmol of
compounds of the general formula Vl-A). The reaction mixture is heated under reflux
over a period of 12 h and filtered over Celite. The combined organic phases are dried
over magnesium sulfate, and the solvent is removed in vacuo. The residue is purified
by column chromatography (SiO2, various solvent mixtures of hexane and EA).
Step 2:
Method 1:
Compounds of the general formula Vl-E (5 mmol), in which R8, R38, U, T, and V have
the meanings stated above and m stands for 0, 1,2, or 3, palladium-on-charcoal
(10%, 500 mg) and concentrated hydrochloric acid (3 mL) are dissolved in MeOH (30
mL) and exposed to a hydrogen atmosphere over a period of 6 hours at RT. The
reaction mixture is filtered over Celite and the filtrate is concentrated in vacuo. The
residue is purified by means of flash chromatography (SiO2, EA).
Method 2:
Compounds of the general formula Vl-E (2 mmol), in which R8, R38, U, T, and V have
the meanings stated above and m stands for 0,1,2, or 3, are dissolved in THF
(10 mL, 10 mL), and BH3'S(CH3)2 [2.0 M in THF, 3 mL, 3 equivalent] is added. The
reaction mixture is heated under reflux over a period of 8 hours, aq. HCI (2N) is
added and the reaction mixture is again heated under reflux for 30 minutes. Aq.

sodium hydroxide solution (2N) is added to the reaction mixture, and the mixture is
washed with EA. The combined organic phases are washed with sat. aq. NaCI
solution and dried over magnesium sulfate. The solvent is removed in vacuo and the
residue is purified by column chromatography (SiO2, various mixtures of
dichloromethane and methanol as mobile solvent).
6. Preparation of specific acids
Preparation of 2-(3-halogenated-4-(methylthio)phenyl)propanoic acids
(cf. Examples 28, 29)

Substituted methylthiophenylpropanoic acids can be prepared as described in
US2003/225283. For this purpose, a solution of AICI3 (54.9 g, 412 mmol) in
chloroform (180 mL) is cooled under an argon atmosphere to 0 °C and a solution of
methyl-2-chloro-2-oxoacetate (24.3 mL, 264 mmol) in chloroform (180 mL) is added
in drops. After this reaction mixture has been stirred for 30 min at 0 °C, a solution of
2-chlorothioanisol (39.4 g, 247 mmol) in chloroform (180 mL) is added in drops. The
red-coloured reaction mixture is slowly heated to room temperature and stirred for a

further 4 h. The reaction mixture is then slowly stirred in ice water (700 mL) and the
obtained yellow mixture is stirred for 15 min and filtered to remove the aluminium
salts. The filtrate is extracted with dichloromethane (3 x 50 mL) and the combined
organic phases are washed with sat. aq. sodium bicarbonate solution (1 x 50 mL).
After drying of the organic phase over MgSO4 and removal of the solvent in vacuo,
the (3-chloro-4-methylsulfanyl-phenyl)-oxo-methyl acetate as oil (36.4 g, 60%) is
obtained (a).
A solution of this ester (61.7 g, 252 mmol) in toluol (120 mL) is heated to 50 °C.
While ensuring that the temperature of the reaction mixture does not exceed 60 °C, a
3 M NaOH solution (105 mL, 313 mmol) is now added in drops and subsequently
stirred for 1.5 h at 50 °C. After removal of the heat source, cone. HCI (10.6 mL, 290
mmol) is added to the warm solution in drops and once the mixture is cooled to room
temperature, it is let to stir for a further 16 h. The resultant precipitate is filtered off,
washed with water (50 mL) and toluol (50 mL) and dried. The (3-chloro-4-
methylsulfanyl-phenyl)-oxo-acetic acid accumulates as a white solid (57.2 g, 98%)
(b).
Hydrazine-hydrate (8.5 mL, 273 mmol) is provided in a reaction flask with a
mechanical stirrer. After cooling to -50 °C, in one portion, the oxo-acetic acid (12.6 g,
54.6 mmol) is added, which leads to an increase in temperature. The resultant milky
mixture is heated to 80 °C and, after removal of the heat source, KOH (2.09 g, 31.7
mmol) is added in one portion. This leads to an exothermal reaction. After cooling to
80 °C, a further portion of KOH (2.09 g, 31.7 mmol) is added and in turn cooled to 80
°C. This procedure is now repeated two further times. After addition of the fourth
portion of KOH, the reaction mixture is boiled for 16 h at 100 °C. After cooling of the
homogeneous reaction mixture to room temperature, it is diluted with water (12 mL)
and, following transfer to a separating funnel, further water (12 mL) and diethylether

(40 mL) are added. After phase separation, the organic phase is extracted with water
(2x15 mL). Heptane (20 mL) is added to the combined aqueous phases and the
mixture is vigorously stirred. While keeping the temperature below 50 °C by means of
an ice bath, cone. HCI (26 mL) is added in drops over a period of 30 min and the
resultant suspension is stirred for 3 h at room temperature. The resultant precipitate
is filtered off and consecutively washed with 1 N aq. HCI solution (2x6 mL), heptane
(1x12 mL) and heptane/diethyl ether (15 mL, 4:1). After drying, the (3-chloro-4-
methylsulfanyl-phenyl)-acetic acid (10.48 g, 89%) is obtained as a cream-coloured
solid (c).
This (3-chloro-4-methylsulfanyl-phenyl)-acetic acid is now alkylated in alpha position
in an analogous manner to Vazquez et al. Eur. J. Med. Chem. Chim. Ther. (1997),
32, 6, 529-53. A solution of the aryl acetic acid (1.05 mmol) in dry THF (3 mL) is
cooled to -78 °C and stirred under an argon atmosphere . For this purpose, a 2 M
solution of LDA in hexane (1.6 mL, 3.2 mmol) and TMEDA (0.3 mL, 1.9 mmol) is
added in drops over a period of 15 min. After 3 hours of slow stirring at -78 °C,
methyl iodide (0.17 mL, 2.7 mmol) is added slowly while stirring. After 16 hours of
stirring at room temperature, the reaction mixture is neutralized with sat. aq. NH4CI
solution (10 mL) and stirred for 1 h at room temperature. After separation of the
organic phase, the aqueous, alkaline phase is acidified with 5 N HCI and the product
extracted with ether (3 x 20 mL). The combined organic phases are dried over
Na2SO4 and the solvent is removed in vacuo. Purification by means of column
chromatography (hexane/ethyl acetate 8:2) produces the desired
methylthiophenylpropanoic acid (d).

Preparation of 2-(3-halogenated-4-(methylsulfonyl)phenyl)propanoic acids
(cf. Examples 29, 31)

In an analogous manner to the method described in US2003/225283, the
methylthiophenylpropanoic acids are reacted to yield the corresponding
methylsulfonylphenylpropanoic acids. In this process, a solution of
methylthiophenylpropanoic acid (0.16 mmol) is dissolved in formic acid (0.19 mL, 4.8
mmol) and cooled to 0 °C. After addition of 30% strength aq. hydrogen peroxide
solution (0.10 mL, 0.8 mmol), stirring is performed at 0 °C for 30 min and the reaction
is then quenched with 10% strength aq. sodium bisulphite solution. The reaction
mixture is diluted with water (5 mL) and extracted ethyl acetate (2x5 mL). The
combined organic phases are dried over Mg2SO4 and the solvent is removed in
vacuo. The residue obtained is dissolved in methanol (1 mL) and a solution of
KMNO4 (0.028 g, 0.176 mmol) in water (0.5 mL) is added by drops. The dark brown
solution is now stirred for 30 min at room temperature and then diluted with methanol
(10 mL). After filtration of the solution, the filtrate is concentrated in vacuo and
purified by column chromatography (hexane/ethyl acetate 1:4) (a).

Preparation of 2-(4-(N-substituted sulfamoyl)-3-fluorophenyl)propanoic acids
(cf. Ex. 32)

In an analogous manner to Greig, IR et al. J. Med. Chem. (2006), 49, 4787-7492, the
bromo-fluorobenzyl-sulfonylchloride (5 mmol) is dissolved with dimethylamine (5
mmol) in dichloromethane (15 mL). Pyridine (5 mmol) is added to this mixture and
the mixture is stirred for 2 h at room temperature. After addition of water (15 mL), the
organic phase is separated and the aqueous phase extracted with ethyl acetate (15
mL). The combined organic phases are dried over Na2SO4, the solvent is removed in
vacuo and the residue is purified by column chromatography (a).
As described in Durandetti M. et al., Tetrahedron (2007), 63, 1146-1153, the
sulfamoyl-aryl bromide is converted with ethylchloropropionate into sulfamoyl-
arylpropanoic acid ester. Together with ethylchloropropionate (1.6 mL ,13 mmol),
sulfamoyl-aryl bromide (10 mmol) is stirred under an argon atmosphere at room
temperature in 15 ml DMF. For the purpose of activation, (1.1 g, 20 mmol) Mn,
followed by 2,2'-bipyridine)nickel-(ll)-dibromide (0.26 g, 0.7 mmol) and TFA (20 mL)
are then added. The reaction mixture is stirred for 1.5 h at 50 °C.

After cooling of the reaction mixture, hydrolysis is performed with 25 mL 1 N HCI, the
mixture is extracted 3 x with 25 mL diethyl ether, the combined organic phases are
washed with 25 mL water and 25 mL sat. NaCI solution, dried over MgSO4 and
concentrated in vacuo. The resultant precipitate is removed by suction, washed with
diethyl ether and purified by means of column chromatography (b).
The propionate (0.81 mmol) is then dissolved in a mixture of THF (1.6 mL, 20 mmol)
and water (0.8 mL, 45 mmol). After addition of LiOH (0.058 g, 2.43 mmol), the
reaction mixture is refluxed overnight. For the purpose of processing, 25 mL water
and 25 mL diethyl ether are added to the mixture and the resultant phases are
separated. The aqueous phase is acidified with HCI and extracted 3x with in each
case 25 mL dichloromethane. After combination of the organic phases, drying over
MgSO4 and concentration in vacuo, the N-substituted sulfamoyl-
fluorophenylpropanoic acid can be obtained.

Preparation of 2-(4-methoxy- and hydroxy-3,5-dimethylphenyl)propanoic acids
(cf. Examples 35-38)

In an analogous manner to the method described in WO2006/078834, on the basis of
aryl bromides, phenylpropanoic acids can be obtained by reaction with
diethylmalonate. For this purpose, in the first step, NaH (60%, 1.45 g, 36.2 mmol) is
added to a solution of aryl bromide (16.5 mmol), CuBr (4.72 g, 32.9 mmol) and
diethyl malonate (5 mL, 32.9 mmol) in 1,4-dioxane (20 mL) at room temperature
while stirring slowly and stirred for 16 h at 100 °C. After filtration, the filtrate is
concentrated in vacuo and purified by means of column chromatography
(hexane/ethyl acetate 4:1) (a).
The obtained phenylmalonic acid diethyl ester (21 mmol) is now dissolved in 2 N
NaOH /THF:H20 (1:1) (20 mL) and refluxed for 3 h. After acidification of the reaction
mixture to pH 1 with cone HCI, stirring is carried out for a further hour at room
temperature. The solution is then adjusted with 1 N NaOH to pH 13 and extracted
with diethyl ether. The aqueous phase is adjusted with 1 N HCI to pH 5 and extracted

with ethyl acetate (3 x). The combined organic phases are washed with sat. NaCI
solution, dried over Na2SO4 and, after filtration, the solvent is removed in vacuo (b).
This phenylacetic acid is now alkylated in an analogous manner to Vazquez et al.
Eur. J. Med. Chem. Chim. Ther. (1997), 32, 6, 529-53 in alpha position. A solution of
arylacetic acid (1.05 mmol) in dry THF (3 mL) is cooled under an argon atmosphere
to -78 °C and stirred. For this purpose, a 2 M solution of LDA in hexane (1.6 mL, 3.2
mmol) and TMEDA (0.3 mL, 1.9 mmol) is added in drops over a period of 15 min.
After 3 hours of slow stirring at -78 °C, methyl iodide (0.17 mL, 2.7 mmol) is added
slowly while stirring. After 16 hours of stirring at room temperature, the reaction
mixture is neutralized with sat. aq. NH4CI solution (10 mL) and stirred for 1 h at room
temperature. After separation of the organic phase, the aqueous, alkaline phase is
acidified with 5 N HCI and the product is extracted with ether (3 x 20 mL). The
combined organic phases are dried over Na2SO4 and the solvent is removed in
vacuo. Purification by means of column chromatography (hexane/ethyl acetate 8:2)
produces the desired substituted phenylmethoxy-propanoic acid (c).
According to a method known to the person skilled in the art, the methoxy ether is
split by means of HBr in glacial acetic acid and the corresponding phenylhydroxy-
propanoic acid is obtained (d).
Preparation of 2-(4-amino-3,5-difluorophenyl)propanoic acid
(cf. Ex. 26)

KOtBu (3.57 g, 31.85 mmol) was dissolved in DMF (30 mL) and cooled to -45 °C. A
mixture of ethyl-2-chloropropionate (2 mL, 15.9 mmol) and 2,6-difluoronitrobenzene
(2.5 g, 15.7 mmol) were added slowly in drops to the solution kept at -40 °C and
stirred for 1 h after addition. For the purpose of processing, the reaction mixture was
adjusted with 16% strength HCI to pH 4 and diluted with water (150 mL). The mixture
was extracted with ethyl acetate (3 x 50 mL), the combined organic phases washed
with water (50 mL) and sat. NaCI solution (2 x 50 mL) and dried over MgSO4. After
removal of the solvent in vacuo, the product was obtained as an oil (4.12 g, 99%) (a).
The difluoronitropropanoate (2.59 g, 10 mmol) was dissolved in EtOH/acetic acid
ester (200 mL, 1 : 1) and hydrated in the H cube (1 bar, 25 °C, 1 mL/min, 0.25 mol/L).
After removal of the solvent in vacuo, the difluoroaminopropionate could be obtained
as an oil (2.27 g, 99%) (b).
The raw product of the hydrogenation (1 g, 4.36 mmol) was dissolved in THF/water
(10 mL, 2 :1), LiOH (0.312 g, 13.1 mmol) added and refluxed for 16 h.
Water (50 mL) and diethyl ether (25 mL) were added to the reaction mixture. After
phase separation, the aqueous phase was acidified with HCI to pH 2 and extracted
with dichloromethane (3 x 50 mL). The combined organic phases were dried over

MgSO4 and the solvent removed in vacuo. The product was obtained as a white solid
(0.72 g, 81%) (c).
7. General instructions for the reaction of amines of the general formulas V or
X with carboxylic acids of the general formula VII
Method A:
The acid of the general formula VII (1 equivalent), the amine of the general formulas
V or X (1.2 equivalents) and EDCI (1.2 equivalents) are stirred in DMF (10 mmol of
acid in 20 mL) over a period of 12 hours at RT, and water is then added. The reaction
mixture is extracted with EA a number of times, the aqueous phase is saturated with
NaCI and then again extracted with EA. The combined organic phases are washed
with 1N hydrochloric acid and sat. aq. NaCI soln., dried over MgSO4, and the solvent
is removed in vacuo. The residue is purified by means of flash chromatography
(SiO2, EA/hexane 1:2).
Method B:
The acid of the general formula VII (1 equivalent) and the amine of the general
formula V or X (1.1 equivalents) are dissolved in DCM (1 mmol acid in 6 mL), and to
the solution EDCI (1.5 equivalents), HOBt (1.4 equivalents) and triethylamine (3
equivalents) are added at 0 °C. The reaction mixture is stirred at RT for a period of
20 h and purified by column chromatography (2:1 mixture of n-hexane/AE).
The following exemplary compounds were obtained in accordance with method B
above.

Exemplary Compound 3:
2-(4-Amino-3-bromo-5-methoxy-phenyl)-N-(4-methyl-6,-trifluoromethyl-3,4,5,6-
tetrahydro-2H-[1,2']bipyridinyl-3'-ylmethyl)acetamide

1H-NMR (CDCl3) δ 7.52 (d, 1H, J = 7.5 Hz), 7.21 (d, 1H, J = 7.5 Hz), 6.93 (d, 1H, J =
1.4 Hz), 6.57 (d, 1H), 6.24 (bt, NH), 4.47 (d, 2H), 4.22 (s, 2H), 3.80 (s, 3H), 3.51 (s,
2H), 3.30-3.26 (m, 2H), 1.70-1.48 (m, 3H), 1.21-1.09 (m, 2H), 0.95 (d, 3H, J = 6.4 Hz)
IR 3298, 2924, 1649, 1575, 1500, 1460, 1420, 1338, 1135, 1047 cm-1
Mass (FAB) m/z 515 and 517 [M+H]+ (Base), 537 and 539 [M+Na]+
Exemplary Compound 4:
2-(3-Fluorophenyl)-N-(4-methyl-6'-trifluoromethyl-3,4,5,6-tetrahydro-2H-
[1,2']bipyridinyl-3'-ylmethyl)acetamide

IR (KBr) 3272, 2923, 1648, 1592, 1552, 1455, 1421, 1374, 1337, 1246, 1138,958,
835, 774 cm-1
MS(FAB) m/z 410(M+H)
Exemplary Compound 5:
2-(2,4-Difluoro-phenyl)-N-(4-methyl-6'-trifluoromethyl-3,4,5,6-tetrahydro-2H-
[1,2']bipyridinyl-3'-ylmethyl)acetamide

IR (KBr) 3270, 2921, 1647, 1558, 1507, 1424, 1330, 1242, 1134, 966, 851 cm-1
MS (FAB) m/z 428 (M+H)
Exemplary Compound 6:
2-(2,6-Difluoro-phenyl)-N-(4-methyl-6'-trifluoromethyl-3,4,5,6-tetrahydro-2H-
[1,2']bipyridinyl-3'-ylmethyl)acetamide

IR (KBr) 3292, 2924, 1656, 1593, 1553, 1468, 1419, 1337, 1238, 1178, 1135, 1017,
945, 834, 784 cm-1
MS (FAB) m/z 428 (M+H)
Exemplary Compound 7:
2-(2,5-Difluoro-phenyl)-N-(4-methyl-6'-trifluoromethyl-3,4,5,6-tetrahydro-2H-
y[1,2']bipyridinyl-3'-ylmethyl)acetamide

IR (KBr) 3271, 2922, 1644, 1593, 1555, 1497, 1424, 1329, 1137, 960, 833, 756 cm-1

MS (FAB) m/z 428 (M+H)
Exemplary Compound 8:
2-(4-Fluoro-phenyl)-N-(4-methyl-6,-trifluoromethyl-3,4,5,6-tetrahydro-2H-
[1,2']bipyridinyl-3'-ylmethyl)acetamide

IR (KBr) 3255, 2920, 1646, 1595, 1558, 1509, 1424, 1330, 1229, 1132, 1043, 960,
828, 755 cm-1
MS(FAB) m/z 410 (M+H)
Exemplary Compound 9:
2-(4-Hydroxy-3-methoxy-phenyl)-N-methyl-6'-trifluoromethyl-3,4,5,6-
tetrahydro-2H-[1,2']bipyridinyl-3'-ylmethyl)propionamide

' 1H NMR (300 M Hz, CDCl3) δ 7.44 (d, 1 H, J = 7.7 Hz), 7.17 (d, 1 H, J = 7.5 Hz), 6.88
(d, 1 H, J= 7.9 Hz), 6.80-6.70 (m, 2 H), 6.11 (bt, 1 H), 5.60 (s, 1 H), 4.46-4.42 (m, 2
H), 3.84 (s, 3 H), 3.55 (q, 1 H, J = 7.1 Hz), 3.32-3.23 (m, 2 H), 2.83-2.73 (m, 2 H),
1.71-1.66 (m, 2 H), 1.53 (d, 3 H, J= 7.1 Hz), 1.26-1.1 (m, 2 H), 0.96 (d, 3 H, J= 6.6
Hz)
IR (KBr) 3301, 2925, 1650, 1516, 1458, 1421, 1373 cm"1
MS (FAB) m/z 452 (M+H)

Exemplary Compound 10:
2-(3,5-Difluoro-phenyl)-N-(4-methyl-6'-trifluoromethyl-3,4,5,6-tetrahydro-2H-
[1,2']bipyridinyl-3'-ylmethyl)propionamide

1H NMR (300 M Hz, CDCl3) δ 7.47 (d, 1 H, J- 7.5 Hz), 7.21 (d, 1 H, J- 7.7 Hz),
6.85-6.82 (m, 2 H), 6.80-6.70 (m, 2 H), 6.11 (bt, 1 H), 5.60 (s, 1 H), 4.46-4.42 (m, 2
H), 3.84 (s, 3 H), 3.55 (q, 1 H, J = 7.1 Hz), 3.32-3.23 (m, 2 H), 2.83-2.73 (m, 2 H),
1.71-1.66 (m, 2 H), 1.53 (d, 3 H, J= 7.1 Hz), 1.26-1.1 (m, 2 H), 0.96 (d, 3 H, J = 6.6
Hz)
IR (KBr) 3293, 2925, 1651, 1596, 1542, 1460, 1335 cm"1
MS (FAB) m/z 442 (M+H)
Exemplary Compound 12:
2-(4-Fluoro-phenyl)-N(4-methyl-6'-trifluoromethyl-3,5,4,6-tetrahydro-2H-
[1,2']bipyridinyl-3'-ylmethyl)propionamide

1H-NMR(CDCI3) δ 7.43(d, 1H, J = 7.5 Hz), 7.28-7.24(m, 2H), 7.18(d, 1H, J = 7.7 Hz),
7.06-7.00(m, 2H), 6.16 (bs, NH), 4.45(d, 2H), 3.59(q, 1H, J = 7.0 Hz), 3.29(m, 2H),
2.79(m, 2H0, 1.75-1.50(m, 3H), 1.53(d, 3H, J = 7.1 Hz), 1.26-1.10(m, 2H), 0.96(d,
3H, J = 6.4 Hz)
IR 3291, 2925, 1650, 1510, 1458, 1419, 1336, 1231, 1177, 1138 cm-1
Mass (FAB) m/z 424 [M+H]+ (Base), 446 [M+Na]+
Exemplary Compound 13:
2-(3-Fluoro-phenyl)-N-(4-methyl-6'-trifluoromethyl-3,4,5,6-tetrahydro-2H-
[1,2']bipyridinyl-3'-ylmethyl)propionamide

1H-NMR(CDCI3) δ 7.43(d, 1H, J = 7.7 Hz), 7.31 (m, 1H), 7.18(d, 1H, J = 7.7 Hz), 7.07-
6.95(m, 3H), 6.23(bs, NH), 4.45(d, 2H), 3.60(q, 1H, J = 7.0 Hz), 3.29(m, 2H), 2.79(m,
2H), 1.65-1.50(m, 3H), 1.54(d, 2H, J = 7.0 Hz), 1.24-1.12(m, 2H), 0.96(d, 3H, J = 6.4
Hz)
IR 3292, 2925, 1651, 1592, 1542, 1456, 1419, 1177, 1140 cm"1
Mass (FAB) m/z 424 [M+H]+ (Base), 446 [M+Na]+
Exemplary Compound 14:
2-(3,4-Diamino-phenyl)-N-(4-methyl-6'-trifluoromethyl-3,4,5,6-tetrahydro-2H-
[1,2']bipyridinyl-3'-ylmethyl)propionamide

1H-NMR(CDCI3) δ 7.42 (d, 1H, J = 7.5 Hz), 7.17 (d, 1H, J = 7.7 Hz), 6.67-6.57 (m,
3H), 6.03 (bt, NH), 4.41 (d, 2H), 3.49 (q, 1H, J = 7.3 Hz), 3.40 (br, NH2), 3.33-3.27
(m, 2H), 2.84-2.74 (m, 2H), 1.73-1.55 (m, 3H), 1.51 (d, 3H, J = 7.1 Hz), 1.30-1.18 (m,
2H), 0.96 (d, 3H, J = 6.6 Hz)
IR 3334, 2925, 1651, 1518, 1419, 1176, 1135, 733 cm'1
Mass (FAB) m/z 436 [M+H]+
Exemplary Compound 15:
N-(2-Butoxy-6-tert-butyl-pyridin-3-ylmethyl)-2-(3,4-diaminophenyl)propionamide

1H-NMR(CDCI3) δ 7.32 (d, 1H, J = 7.5 Hz, Ar), 6.76 (d, 1H, J = 7.3 Hz, Ar), 6.66-6.57
(m, 3H, Ar), 6.00 (bt, NH), 4.27 (m, 4H, OCH2 & CH2NH), 3.41 (q, 1H, J = 7.1 Hz,
CHCH3), 1.64 (m, 2H, OCH2CH2), 1.45 (d, 3H, J = 7.1 Hz, CHCH3), 1.39 (m, 2H,
CH2CH3), 1.29 (s, 9H, C(CH3)3), 0.95 (t, 3H, J = 7.3 Hz, CH2CH3)
IR 3303, 2960, 1649, 1517, 1456, 1254 cm'1
Mass (FAB) 399 m/z [M+H]+
Exemplary Compound 16:
N-(6'-tert-Butyl-4-methyl-3,4,5,6-tetrahydro-2H-[1,2']bipyridinyl-3'-ylmethyl)-2-
(3,4-diamino-phenyl)propionamide

1H-NMR(CDCI3) δ 7.26 (d, 1H, J = 7.9 Hz, Ar), 6.85 (d, 1H, J = 7.7 Hz, Ar), 6.66-6.58
(m, 3H, Ar), 6.39 (bt, NH), 4.37 (m, 2H, CH2NH), 3.45 (q, 1H, J = 7.1 Hz, CHCH3),
3.37 (bs, NH2*2), 3.23 (m, 2H, piperidine), 2.74 (m, 2H, piperidine), 1.65-1.45 (m, 3H,
piperidine), 1.49 (d, 3H, J = 7.1 Hz, CHCH3), 1.29 (s, 9H, C(CH3)3), 1.28-1.16 (m, 2H,
piperidine), 0.95 (d, 3H, J = 6.4 Hz, piperidine CH3)
IR 3338, 2955, 1648, 1517, 1449, 1232 cm-1
Mass (FAB) m/z 424[M+H]+
Exemplary Compound 17:
N-(6-tert-Butyl-2-cyclohexylsulfanyl-pyridin-3-ylmethyl)-2-(3,4-diamino-phenyl)-
propionamide

1H-NMR(CDCI3) δ 7.27 (d, 1H, Ar), 6.91 (d, 1H, J = 7.9 Hz, Ar), 6.67-6.59 (m, 3H, Ar),
5.90 (bt, NH), 4.26 (m, 2H, CH2NH), 3.96 (m, 1H, SCH), 3.46 (q, 1H, J = 7.3 Hz,
CHCH3), 3.37 (bs, NH2*2), 2.06 (m, 2H, cyclohexyl), 1.80-1.20 (m, 8H, cyclohexyl),
1.50 (d, 3H, CHCH3), 1.31 (s, 9H, C(CH3)3)
IR 3303, 2929, 2854, 1651, 1517, 1444, 1079cm-1
Mass (FAB) m/z 441[M+H]+

Exemplary Compound 19:
2-(3,5-Dibromo-4-hydroxy-phenyl)-N-(4-methyl-6'-trifluoromethyl-3,4,5,6-tetra-
hydro-2H-[1,2']bipyridinyl-3'-ylmethyl)propionamide

1H-NMR(CDCI3) δ 7.48 (m, 1H, Ar), 7.39 (s, 2H, Ar), 7.22 (d, 1H, J = 7.7 Hz, Ar),
6.27 (bt, NH), 4.47 (m, 2H, CH2NH), 3.46 (q, 1H, J = 7.1 Hz, CHCH3), 3.31 (m, 2H,
piperidine), 2.81 (m, 2H, piperidine), 2.40 (s, OH), 1.75-1.16 (m, 5H, piperidine), 1.50
(d, 3H, J = 7.1 Hz, CHCH3), 0.98 (d, 3H, J = 6.4 Hz, piperidine CH3)
IR 3298, 2924, 1650, 1550, 1462, 1417, 1176, 1138 cm-1
Mass (FAB) m/z 580 [M+H]+
Exemplary Compound 20:
2-(4-Amino-3,5-dibromo-phenyl)-N-(4-methyl-6'-trlfluoromethyl-3,4,5,6-tetra-
hydro-2H-[1,2']bipyridinyl-3'-ylmethyl)propionamide

1H-NMR(CDCI3) δ 7.47 (d, 1H, J = 7.7 Hz, Ar), 7.31 (s, 2H, Ar), 7.21 (d, 1H, J = 7.7
Hz, Ar), 6.18 (bt, NH), 4.55 (bs, NH2), 4.46 (m, 2H, CH2NH), 3.43 (q, 1H, J = 7.0 Hz,
CHCH3), 3.30 (m, 2H, piperidine), 2.81 (m, 2H, piperidine), 1.75-1.15 (m, 5H,
piperidine), 1.48 (d, 3H, J = 7.1 Hz, CH2CH3), 0.97 (d, 3H, J = 6.4 Hz, piperidine CH3)
IR 3298, 2924, 1649, 1544, 1474, 1418, 1177, 1136 cm-1
Mass (FAB) m/z 579[M+H]+

Exemplary Compound 21:
2-(3-Bromo-4-hydroxy-5-methoxy-phenyl)-N-(4-methyl-6'-trifluoromethyl-3,4,5,6-
tetrahydro-2H-[1,2']bipyridinyl-3'-ylmethyl)acetamide

1H-NMR(CDCI3) δ 7.54 (d, 1H, J = 7.5 Hz, Ar), 7.22 (d, 1H, J = 7.7 Hz, Ar), 6.99 (d,
1H, J = 1.5 Hz, Ar), 6.69 (d, 1H, J = 2.0 Hz, Ar), 6.27 (bt, NH), 5.91 (bs, OH), 4.48 (m,
2H, CH2NH), 3.86 (s, 3H, OCH3), 3.53 (s, 2H, CH2CO), 3.28 (m, 2H, piperidine), 2.80
(m, 2H, piperidine), 1.73-1.07 (m, 5H, piperidine), 0.96 (d, 3H, J = 6.4 Hz, piperidine
CH3)
IR 3298, 2924, 1649, 1501, 1459, 1421, 1282, 1178, 1136, 1047 cm-1
Mass(FAB)m/z 517[M+H]+
Exemplary Compound 22:
2-(4-Amino-3,5-dibromo-phenyl)-N-(4-methyl-6,-trifluoromethyl-3,4,5,6-tetra-
hydro-2H-[1,2']bipyridinyl-3'-ylmethyl)acetamide

1H-NMR(CDCI3) δ 7.53 (d, 1H, J = 7.3 Hz, Ar), 7.29 (s, 2H, Ar), 7.23 (d, 1H, J = 7.7
Hz, Ar), 6.26 (bt, NH), 4.57 (bs, NH2), 4.48 (m, 2H, CH2NH), 3.46 (s, 2H, CH2CO),
3.30 (m, 2H, piperidine), 2.81 (m, 2H, piperidine), 1.75-1.10 (m, 5H, piperidine), 0.97
(d, 3H, J = 6.4 Hz, piperidine CH3)

IR 3288, 2923, 1649, 1544, 1478, 1418, 1337, 1177, 1135 cm-1
Mass (FAB) m/z 565 [M+H]+
Exemplary Compound 23:
2-(3,5-Dibromo-4-hydroxy-phenyl)-N-(4-methyl-6'-trifluoromethyl-3,4,5,6-tetra-
hydro-2H-[1,2']bipyridinyl-3'-ylmethyl)acetamide

1H-NMR(CDCI3) δ 7.55 (d, 1H, J = 7.7 Hz, Ar), 7.38 (s, 2H, Ar), 7.24 (d, 1H, J = 7.7
Hz, Ar), 6.31 (bt, NH), 4.50 (m, 2H, CH2NH), 3.50 (s, 2H, CH2CO), 3.31 (m, 2H,
piperidine), 2.82 (m, 2H, piperidine), 2.40 (s, OH), 1.77-1.10 (m, 5H, piperidine), 0.97
(d, 3H, J = 6.6 Hz, piperidine CH3)
IR 3297, 2924, 1650, 1546, 1473, 1419, 1337, 1177, 1137 cm-1
Mass (FAB) m/z 566 [M+H]+
Exemplary Compound 24:
2-(3-Amino-4-hydroxy-phenyl)-N-(4-methyl-6'-trlfluoromethyl-3,4,5,6-tetrahydro-
2H-[1,2']bipyridinyl-3'-ylmethyl)propionamide

1H-NMR(CDCI3) δ 7.42 (d, 1H, J = 7.7 Hz, Ar), 7.17 (d, 1H, J = 7.7 Hz, Ar), 6.69-6.64
(m, 2H, Ar), 6.53 (dd, 1H, J = 8.0, 1.8 Hz, Ar), 6.07 (bt, NH), 4.42 (d, 2H, J = 5.7 Hz,
CH2NH), 3.69 (bs, NH2), 3.59 (q, 1H, J = 7.1 Hz, CHCH3), 3.30 (m, 2H, piperidine),

2.79 (m, 2H, piperidine), 1.71-1.50 (m, 6H, piperidine & CHCH3), 1.22 (m, 2H,
piperidine), 0.96 (d, 3H, J = 6.6 Hz, CHCH3)
IR 3298, 2924, 1649, 1519, 1458, 1420, 1177, 1136 cm-1
Mass (FAB) m/z 437 [M+H]+, 459 [M+Na]+
Exemplary Compound 25:
2-(3,5-Dibromo-phenyl)-N-(4-methyl-6'-trifluoromethyl-3,4,5,6-tetrahydro-2H-
[1,2']bipyridinyl-3'-ylmethyl)acetamide

1H-NMR(CDCI3) δ 7.61 (t, 1H, J = 1.7 Hz), 7.54 (d, 1H, J = 7.7 Hz), 7.38 (d, 1H, J =
1.7 Hz), 7.24 (d, 1H, J = 7.7 Hz), 6.34 (bt, NH), 4.50 (d, 2H), 3.54 (s, 3H), 3.32 (m,
2H), 2.83 (m, 2H), 1.75-1.50 (m, 3H), 1.33-1.13 (m, 2H), 0.98 (d, 3H, J = 6.4 Hz)
IR 3291, 2924, 1649, 1554, 1458, 1421, 1337, 1176, 1138 cm"1
Mass (FAB) m/z 550[M+H]+
The following further exemplary compounds were obtained by the methods described
above:

Exemplary compounds 28-32 and 35-33 can likewise be obtained according to the
methods described above.
Pharmacological Data
The affinity of the compounds according to the invention for the vanilloid receptor 1
(VR1/TRPV1 -Receptor) was detected as described above (Pharmacological Methods
I and II respectively).

The compounds according to the invention of the above formula I exhibit excellent
affinity to the VR1/TRPV1 receptor (Table 1).

Ne denotes "no effect", i.e. no reaction was observed.
The value following the symbol "@" indicates the concentration at which the inhibition (in percent) was
determined.

Claims
1. Substituted compounds of the general formula I,

in which
n stands for 0, 1, 2, 3, or 4;
R1 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(= O)-NH2;
-S(= O)2-NH2; -C(= O)-NH-OH; -C(= O)-OH; -C(= O)-H; -S(= O)2-OH; -
C(= NH)-NH2; -C(= NH)-NH-R9; -N= C(NH2)2; -N= C(NHR10)-(NHR11); -
O-P(= O)2-O-R12; -NHR13; -NR14R15; -NH-C(= O)-R13; -OR16; -SR17; -C(=
O)-NHR18; -C(= O)-NR19R20; -S(= O)2-NHR21; -S(= O)2-NR22R23; -C(=
O)-OR24; -C(= O)-R25; -S(= O)-R26; or -S(= O)2-R27 or for a linear or
branched, saturated or unsaturated, unsubstituted or at least
monosubstituted aliphatic C1-10 radical;
R2 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(= O)-NH2;
-S(= O)2-NH2; -C(= O)-NH-OH; -C(= O)-OH; -C(= O)-H; -S(= O)2-OH; -
C(= NH)-NH2; -C(= NH)-NH-R9; -N= C(NH2)2; -N= C(NHR10)-(NHR11); -

O-P(= O)2-O-R12; -NHR13; -NR14R15; -NH-C(= O)-R13; -OR16; -SR17; -C(=
O)-NHR18; -C(= O)-NR19R20; -S(= O)2-NHR21; -S(= O)2-NR22R23; -C(=
O)-OR24; -C(= O)-R25; -S(= O)-R26; or -S(= O)2-R27 or for a linear or
branched, saturated or unsaturated, unsubstituted or at least
monosubstituted aliphatic C1-10 radical;
R3 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(= O)-NH2;
-S(= O)2-NH2; -C(= O)-NH-OH; -C(= O)-OH; -C(= O)-H; -S(= O)2-OH; -
C(= NH)-NH2; -C(= NH)-NH-R9; -N= C(NH2)2; -N= C(NHR10)-(NHR11); -
O-P(= O)2-O-R12; -NHR13; -NR14R15; -NH-C(= O)-R13; -OR16; -SR17, -C(=
O)-NHR18; -C(= O)-NR19R20; -S(= O)2-NHR21; -S(= O)2-NR22R23; -C(=
O)-OR24; -C(= O)-R25; -S(= O)-R26; or -S(= O)2-R27 or for a linear or
branched, saturated or unsaturated, unsubstituted or at least
monosubstituted aliphatic C1-10 radical;
R4 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(= O)-NH2;
-S(= O)2-NH2; -C(= O)-NH-OH; -C(= O)-OH; -C(= O)-H; -S(= O)2-OH; -
C(= NH)-NH2; -C(= NH)-NH-R9; -N= C(NH2)2; -N= C(NHR10)-(NHR11); -
O-P(= O)2-O-R12; -NHR13; -NR14R15; -NH-C(= O)-R13; -OR16; -SR17; -C(= O)-NHR18; -C(=
O)-NR19R20; -S(= O)2-NHR21; -S(= O)2-NR22R23; -C(=
O)-OR24; -C(= O)-R25; -S(= O)-R26; or -S(= O)2-R27 or for a linear or
branched, saturated or unsaturated, unsubstituted or at least
monosubstituted aliphatic C1-10 radical;
R5 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(= O)-NH2;
-S(= O)2-NH2; -C(= O)-NH-OH; -C(= O)-OH; -C(= O)-H; -S(= O)2-OH; -

C(= NH)-NH2; -C(= NH)-NH-R9; -N= C(NH2)2; -N= C(NHR10)-(NHR11); -
O-P(= O)2-O-R12; -NHR13; -NR14R15; -NH-C(= O)-R13; -OR16; -SR17; -C(=
O)-NHR18; -C(= O)-NR19R20; -S(= O)2-NHR21; -S(= O)2-NR22R23; -C(=
O)-OR24; -C(= O)-R25; -S(= O)-R26; or -S(= O)2-R27 or for a linear or
branched, saturated or unsaturated, unsubstituted or at least
monosubstituted aliphatic C1-10 radical;
R6 stands in each case for hydrogen or for a linear or branched, saturated
or unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10
radical;
R7 stands for hydrogen or -OH;
or R6 and R7 each form, together with the interconnecting carbon atom
as ring member, a saturated or unsaturated, unsubstituted or at least
monosubstituted three-membered, four-membered, five-membered, or
six-membered cycloaliphatic radical;
R8 stands for -SF5; -O-CF3; -CF3; -O-CFH2; -O-CF2 H; -CFH2; -CF2 H; or for
an unsubstituted or at least monosubstituted tert-butyl radical;
T stands for C-R35 and U stands for C-R36 and V stands for N and W
stands for C-R38
or
T stands for C-R35 and U stands for N and V stands for C-R37 and W
stands for C-R38

or
T stands for N and U stands for C-R36 and V stands for C-R37 and W
stands for C-R38
or
T stands for N and U stands for N and V stands for C-R37 and W stands
for C-R38
or
T stands for N and U stands for C-R36 and V stands for N and W stands
for C-R38
or
T stands for C-R35 and U stands for N and V stands for N and W stands
for C-R38
or
T stands for C-R35 and U stands for C-R36 and V stands for C-R37 and
W stands for C-R38;
R9 R10 p11 R12 R13 R14 R15 R16 R17 R18 R19 p20 R21 R22 R23 R24 R25
R26 and R27 each independently
stand for a linear or branched, saturated or unsaturated, unsubstituted
or at least monosubstituted aliphatic C1-10 radical;
for an unsaturated or saturated, unsubstituted or at least
monosubstituted, three-membered, four-membered, five-membered,
six-membered, seven-membered, eight-membered, or nine-mem be red
cycloaliphatic radical optionally containing at least one heteroatom as

ring member, which can be condensed with a saturated or unsaturated,
unsubstituted or at least monosubstituted monocyclic or polycyclic ring
system and/or can be bonded via a linear or branched, unsubstituted or
at least monosubstituted C1-6 alkylene group or two to six-membered
heteroalkylene group;
or for an unsubstituted or at least monosubstituted five-membered to
fourteen-membered aryl radical or heteroaryl radical, which can be
condensed with a saturated or unsaturated, unsubstituted or at least
monosubstituted monocyclic or polycyclic ring system and/or can be
bonded via a linear or branched, unsubstituted or at least
monosubstituted C1-6 alkylene group or two to six-membered
heteroalkylene group;
R35, R36, and R37 each independently stand for H; F; CI; Br; I; -SF5; -NO2; -CF3; -CN; -
NH2; -OH; -SH; -C(= O)-NH2; -S(= O)2-NH2; -C(= O)-NH-OH; -C(= O)-
OH; -C(= O)-H; -S(= O)2-OH; -NHR13; -NR14R15; -NH-C(= O)-R13; -OR16;
-SR17; -C(= O)-NHR18; -C(= O)-NR19R20; -S(= O)2-NHR21; -S(= O)2-
NR22R23; -C(= O)-OR24; -C(= O)-R25; -S(= O)-R26; -S(= O)2R27;
for a linear or branched, saturated or unsaturated, unsubstituted or at
least monosubstituted aliphatic C1-10 radical;
or for an unsubstituted or at least monosubstituted five-membered to
fourteen-membered aryl radical or heteroaryl radical, which can be
condensed with a saturated or unsaturated, unsubstituted or at least

monosubstituted monocyclic or polycyclic ring system and/or can be
bonded via a linear or branched, unsubstituted or at least
monosubstituted C1-6-alkylene group or C2-6-alkenylene group or C2_6-
alkynylene group;
R38 stands for F; CI; Br; I; -SF5; -NO2; -CF3; -CF2 CI; -CN; -NH2; -OH; -SH; -
C(= O)-NH2; -S(= O)2-NH2; -C(= O)-NH-OH; and -C(= O)-OH; -C(= O)-
H; -S(= O)2-OH; -NHR39; -NR40R41; -OR42; -SR43; -C(= O)-NHR44; -C(=
O)-NR45R46; -S(= O)2-NHR47; -S(= O)2-NR48R49; -C(= O)-OR50; -C(= O)-
R51; -S(= O)-R52; -S(= O)2-R53; -C(= NH)-NH2; -C(= NH)-NH-R54; -N=
C(NH2)2; -N= C(NHR55)-(NHR56)
for a linear or branched, saturated or unsaturated, unsubstituted or at
least monosubstituted aliphatic C1-10 radical;
for an unsaturated or saturated, unsubstituted or at least
monosubstituted three-membered, four-membered, five-membered, six-
membered, seven-membered, eight-membered, or nine-membered
cycloaliphatic radical optionally exhibiting at least one heteroatom as
ring member, each of which is bonded to the parent structure over a
carbon atom in the ring of the cycloaliphatic radical and is condensed
with a saturated or unsaturated, unsubstituted or at least
monosubstituted monocyclic or polycyclic ring system and/or can be
bonded via a linear or branched, unsubstituted or at least
monosubstituted C1-6 alkylene group or C2-6 alkenylene group or C2-6
alkynylene group;

or for an unsubstituted or at least monosubstituted five-membered to
fourteen-membered aryl radical or heteroaryl radical, which can be
condensed with a saturated or unsaturated, unsubstituted or at least
monosubstituted monocyclic or polycyclic ring system and/or can be
bonded via a linear or branched, unsubstituted or at least
monosubstituted C1-6 alkylene group or C2-6 alkenylene group or C2-6-
alkynylene group;
R39 R40 R41 R42 R43 R44 R45 R46 R47 R48 R49 R50 R51 R52 R53 R54 R55
and R56 each independently
stand for a linear or branched, saturated or unsaturated, unsubstituted
or at least monosubstituted aliphatic C1-10 radical;
for an unsaturated or saturated, unsubstituted or at least
monosubstituted, three-membered, four-membered, five-membered,
six-membered, seven-membered, eight-membered, or nine-membered
cycloaliphatic radical optionally containing at least one heteroatom as
ring member, which can be condensed with a saturated or unsaturated,
unsubstituted or at least monosubstituted monocyclic or polycyclic ring
system and/or can be bonded via a linear or branched, unsubstituted or
at least monosubstituted C1-6-alkylene group or two to six-membered
heteroalkylene group;

or for an unsubstituted or at least monosubstituted five-membered to
fourteen-membered aryl radical or heteroaryl radical, which can be
condensed with a saturated or unsaturated, unsubstituted or at least
monosubstituted monocyclic or polycyclic ring system and/or can be
bonded via a linear or branched, unsubstituted or at least
monosubstituted C1-6-alkylene group or two to six-membered
heteroalkylene group;
or
R40 and R41 form, together with the interconnecting nitrogen atom as ring
member, a saturated or unsaturated four-membered, five-membered,
six-membered, seven-membered, eight-membered, or nine-membered
heterocycloaliphatic radical, which is unsubstituted or substituted by 1,
2, 3, 4, or 5 radicals R57 and optionally exhibits at least one further
heteroatom as ring member, and which can be condensed with a
saturated or unsaturated, unsubstituted or at least monosubstituted
monocyclic or polycyclic ring system;
R57 stands for -NHR58, -NR59R60, or for a linear or branched, saturated or
unsaturated, unsubstituted or at least monosubstituted aliphatic C1-10
radical;
R58, R59, and R60 each independently stand for -C(= O)-R61; for a linear or
branched, saturated or unsaturated, unsubstituted or at least
monosubstituted aliphatic C1-10 radical

or for an unsubstituted or at least monosubstituted five-membered to
fourteen-membered aryl radical or heteroaryl radical, which can be
condensed with a saturated or unsaturated, unsubstituted or at least
monosubstituted monocyclic or polycyclic ring system and/or can be
bonded via a linear or branched, unsubstituted or at least
monosubstituted C1-6 alkylene group or C2-6 alkenylene group or C2-6
alkynylene group;
and
R61 stands for a linear or branched, saturated or unsaturated, unsubstituted
or at least monosubstituted aliphatic C1-10 radical;
each optionally in the form of one of the pure stereoisomers thereof,
particularly enantiomers or diastereoisomers thereof, the racemates thereof or
in the form of a mixture of stereoisomers, particularly the enantiomers and/or
diastereoisomers, in an arbitrary mixing ratio, or each in the form of
corresponding salts, or each in the form of corresponding solvates;
wherein
the aforementioned aliphatic C1-10 radicals and tert-butyl radicals can each be
optionally substituted by 1, 2, 3, 4, 5, 6, 7, 8, or 9 substituents independently
selected from the group consisting of F, CI, Br, I, -CN, -NO2, -OH, -NH2, -SH, -

O(C1-5 alkyl), -S(C1-5 alkyl), -NH(C1-5 alkyl), -N(C1-5 alkyl)-(C1-5 alkyl), -C(= O)-
O-(C1-5 alkyl), -O-C(= O)-(C1-5 alkyl), -O-phenyl, phenyl, -OCF3, and -SCF3;
the aforementioned two to six-membered heteroalkylene groups, C1-6 alkylene
groups, and C2-6 alkenylene groups and C2-6 alkynylene groups can each be
optionally substituted by 1, 2, 3, 4, 5, 6, 7, 8, or 9 substituents independently
selected from the group consisting of F, CI, Br, I, -CN, -NO2, -OH, -NH2, -SH, -
0(C1-5 alkyl), -S(C1-5 alkyl), -NH(C1-5 alkyl), -N(C1-5 alkyl)-(C1-5 alkyl), -OCF3,
and -SCF3;
the aforementioned heteroalkylene groups each optionally exhibit 1, 2, or 3
heteroatom(s) independently selected from the group consisting of oxygen,
sulfur, and nitrogen (NH) as link(s);
the aforementioned (hetero)cycloaliphatic radicals are optionally each
substituted by 1, 2, 3, 4, or 5 substituents independently selected from the
group consisting of -C1-6-alkylene-OH, = CH2, -O-C1-5-alkyleneoxetanyl, -C1-5-
alkylene-O-C1-5 alkylene-oxetanyl, -CH2-NH-C1-5 alkyl, -CH2-N(C1-5 alkyl)2, -
N[C(= O)-C1-5 alkyl]-phenyl, -CH2-O-C1-5-alkyl, oxo (= O), thioxo (= S), F, CI,
Br, I, -CN, -CF3, -SF5, -OH, -O-C1-5-alkyl, -O-C(= O)-C1-5-alkyl, -NH2, -NO2, -O-
CF3, -S-CF3, -SH, -S-C1-5-alkyI), -C1-5-alkyI, -C(= O)-C1-5-alkyl), -C(= O)-OH, -
C(= O)-O-C1-5-alkyl, -NH-C1-5-alkyl), -N(C1-5 alkyl)2, -NH-phenyl, -N(C1-5-alkyl)-
phenyl, cyclohexyl, cyclopentyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-
thiadiazolyl, thiophenyl, phenethyl, piperidinyl, pyrrolidinyl, -(CH2)pyridinyl,
pyridinyl, -O-phenyl, -O-benzyl, phenyl, and benzyl, and the cyclic moiety of
the radicals oxetanyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl,

thiophenyl, phenethyl, -N[C(= O)-C1-5-alkyl]-phenyl, -NH-phenyl, -N(C1-5 alkyl)-
phenyl, -(CH2)-pyridinyl, pyridinyl, -O-phenyl, -O-benzyl, phenyl, and benzyl
can each be substituted by 1, 2, 3, 4, or 5 substituents independently selected
from the group consisting of F, CI, Br, -OH, -CF3, -SF5, -CN, -NO2, -d-5-alkyl, -
O-C1-5-alkyl, -O-CF3, -S-CF3, phenyl, and -O-benzyl,
and, unless otherwise stated, the aforementioned (hetero)cycloaliphatic
radicals can each optionally exhibit 1, 2, or 3 (further) heteroatom(s)
independently selected from the group consisting of oxygen, nitrogen, and
sulfur;
the rings of the aforementioned monocyclic or polycyclic ring systems can
each be optionally substituted by 1, 2, 3, 4, or 5 substituents independently
selected from the group consisting of oxo (= O), thioxo (= S), F, CI, Br, I, -CN, -
CF3, -SF5, -OH, -O-C1-5-alkyl, -NH2, -NO2, -O-CF3, -S-CF3, -SH, -S-C1-5-alkyl, -
C1-5-alkyl, -C(= O)-C1-5-alkyl, -C(= O)-OH, -C(= O)-O-C1-5-alkyl), -NH-C1-5-alkyl,
-N(C1-5-alkyl)2, -O-phenyl, -O-benzyl, phenyl, and benzyl, and the cyclic moiety
of the radicals -O-phenyl, -O-benzyl, phenyl, and benzyl can each be
substituted by 1, 2, 3, 4, or 5 substituents independently selected from the
group consisting of F, CI, Br, -OH, -CF3, -SF5, -CN, -NO2, -C1-5-alkyl, -O-C1-5-
alkyl, -O-CF3, -S-CF3, phenyl, and -O-benzyl,
and the rings of the aforementioned monocyclic or polycyclic ring systems are
each five-membered, six-membered, or seven-membered and can each
optionally exhibit 1, 2, 3, 4, or 5 heteroatom(s) as ring member(s), which are

independently selected from the group consisting of oxygen, nitrogen, and
sulfur;
and the aforementioned aryl radicals or heteroaryl radicals can each be
optionally substituted by 1, 2, 3, 4, or 5 substituents independently selected
from the group consisting of F, CI, Br, I, -CN, -CF3, -SF5, -OH, -O-C1-5-alkyl, -
NH2, -NO2, -O-CF3, -S-CF3, -SH, -S-C1-5-alkyI, -C1-5-alkyl, -C(= O)-OH, -C(=
O)-O-C1-5-alkyl, -NH-C1-5-alkyl), -N(C1-5-alkyl)2, -NH-S(= O)2-C1-5-alkyl, -NH-
C(= O)-O-C1-5-alkyl, -C(= O)-H, -C(= O)-C1-5-alkyl, -C(= O)-NH2, -C(= O)-NH-
C1-5-alkyl, -C(= O)-N-(C1-5 alkyl)2, -O-phenyl, -O-benzyl, phenyl, and benzyl,
and the cyclic moiety of the radicals -O-phenyl, -O-benzyl, phenyl, and benzyl
can each be substituted by 1, 2, 3, 4, or 5 substituents independently selected
from the group consisting of F, CI, Br, -OH, -CF3, -SF5, -CN, -NO2, -C1-5-alkyl, -
O-C1-5-alkyl, -O-CF3, -S-CF3, phenyl, and -O-benzyl,
and
the aforementioned heteroaryl radicals can each optionally exhibit 1,2,3, 4, or
5 heteroatom(s) independently selected from the group consisting of oxygen,
nitrogen, and sulfur as ring member(s).
The compounds according to claim 1, characterized in that
n stands for 0, 1, 2, 3, or 4;

R1 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; and -NH2; -OH; -SH; -C(=O)-
NH2; -S(=O)2-NH2; -C(=O)-NH-OH; -C(=O)-OH; -C(=O)-H; -S(=O)2-OH;
-NHR13; -NR14R15; -NH-C(=O)-R13; -OR16; -SR17; -S(=O)-NR22R23; -
S(=O)-R26; -S(=O)2-R27 or for a radical selected from the group
consisting of methyl, -CF3, -CCI3, -CBr3, -CHF2, -CH2F, -CF2CI, -CCI2F,
ethyl, -CF2-CH3, -CH2-CF3, -C2F5, -CH2-CCI3, -CH2-CBr3, -CHF-CF2CI, -
CF2-CF2CI, -CFCI-CF2CI, n-propyl, -CF2-CF2-CF3, -CF(CF3)2, isopropyl,
n-butyl, sec-butyl, isobutyl, and tert-butyl;
R2 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(=O)-NH2;
-S(=O)2-NH2; -C(=O)-NH-OH; -C(=O)-OH; -C(=O)-H; -S(=O)2-OH; -
NHR13; -NR14R15; -NH-C(=O)-R13; -OR16; -SR17; -S(=O)-NR22R23; -
S(=O)-R26; -S(=O)2-R27 or for a radical selected from the group
consisting of methyl, -CF3, -CCI3, -CBr3, -CHF2, -CH2F, -CF2CI, -CCI2F,
ethyl, -CF2-CH3, -CH2-CF3, -C2F5, -CH2-CCI3, -CH2-CBr3, -CHF-CF2CI, -
CF2-CF2CI, -CFCI-CF2CI, n-propyl, -CF2-CF2-CF3, -CF(CF3)2, isopropyl,
n-butyl, sec-butyl, isobutyl, and tert-butyl;
R3 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(=O)-NH2;
-S(=O)2-NH2; -C(=O)-NH-OH; -C(=O)-OH; -C(=O)-H; -S(=O)2-OH; -
NHR13; -NR14R15; -NH-C(=O)-R13; -OR16; -SR17; -S(=O)-NR22R23; -
S(=O)-R26; -S(=O)2-R27 or for a radical selected from the group
consisting of methyl, -CF3, -CCI3, -CBr3, -CHF2, -CH2F, -CF2CI, -CCI2F,
ethyl, -CF2-CH3, -CH2-CF3, -C2F5, -CH2-CCI3, -CH2-CBr3, -CHF-CF2CI, -
CF2-CF2CI, -CFCI-CF2CI, n-propyl, -CF2-CF2-CF3, -CF(CF3)2, isopropyl,
n-butyl, sec-butyl, isobutyl, and tert-butyl;

R4 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(=O)-NH2;
-S(=O)2-NH2; -C(=O)-NH-OH; -C(=O)-OH; -C(=O)-H; -S(=O)2-OH; -
NHR13; -NR14R15; -NH-C(=O)-R13; -OR16; -SR17; -S(=O)-NR22R23; -
S(=O)-R26; -S(=O)2-R27 or for a radical selected from the group
consisting of methyl, -CF3, -CCI3, -CBr3, -CHF2, -CH2F, -CF2CI, -CCI2F,
ethyl, -CF2-CH3, -CH2-CF3, -C2F5, -CH2-CCI3, -CH2-CBr3, -CHF-CF2CI, -
CF2-CF2CI, -CFCI-CF2CI, n-propyl, -CF2-CF2-CF3, -CF(CF3)2, isopropyl,
n-butyl, sec-butyl, isobutyl, and tert-butyl;
R5 stands for H; F; CI; Br; I; -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(=O)-NH2;
-S(=O)2-NH2; -C(=O)-NH-OH; -C(=O)-OH; -C(=O)-H; -S(=O)2-OH; -
NHR13; -NR14R15; -NH-C(=O)-R13; -OR16; -SR17; -S(=O)-NR22R23; -
S(=O)-R26; -S(=O)2-R27 or for a radical selected from the group
consisting of methyl, -CF3, -CCI3, -CBr3, -CHF2, -CH2F, -CF2CI, -CCI2F,
ethyl, -CF2-CH3, -CH2-CF3, -C2F5, -CH2-CCI3, -CH2-CBr3, -CHF-CF2CI, -
CF2-CF2CI, -CFCI-CF2CI, n-propyl, -CF2-CF2-CF3, -CF(CF3)2, isopropyl,
n-butyl, sec-butyl, isobutyl, and tert-butyl;
R6 stands for hydrogen or for an alkyl radical selected from the group
consisting of-CH2-OH, -CH2-CH2-OH, -CH2-CH2-CH2-OH, -CH2-CH2-
CH2-CH2-OH, isopropyl, n-butyl, sec-butyl, isobutyl, methyl, ethyl, and
n-propyl;
R7 stands for hydrogen or-OH;

or R6 and R7 form, together with the interconnecting carbon atom as ring
member, a radical selected from the group consisting of cyclopropyl,
cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl;
R8 stands for -SF5; -O-CF3; -O-CFH2; -O-CF2H; -CFH2; -CF2H; -CF3; or for
a tert-butyl radical, each of which can be unsubstituted or substituted by
1, 2, 3, 4, 5, 6, 7, 8, or 9 substituents independently selected from the
group consisting of F, CI, Br, I, -CN, -NO2, -OH, -NH2, -SH, -O-CH3, -O-
C2H5, -O-CH(CH3)2, -NH-CH3, and -NH-C2H5;
T stands for C-R35 and U stands for C-R36 and V stands for N and W stands
for C-R38
or
T stands for C-R35 and U stands for N and V stands for C-R37 and W stands
for C-R38
or
T stands for N and U stands for C-R36 and V stands for C-R37 and W stands
for C-R38
or
T stands for N and U stands for N and V stands for C-R37 and W stands for C-
R38
or
T stands for N and U stands for C-R36 and V stands for N and W stands for C-
R38
or

T stands for C-R35 and U stands for N and V stands for N and W stands for C-
R38
or
T stands for C-R35 and U stands for C-R36 and V stands for C-R37 and W
stands for C-R38
R13, R14, R15, R16, R17, R26, and R27 each independently
stand for a radical selected from the group consisting of methyl, -CF3, -
CCI3, -CBr3, -CHF2, -CH2F, -CF2CI, -CCI2F, -CH2-CN, -CH2-O-CH3, -
CH2-O-CF3, -CH2-SF3, ethyl, -CF2-CH3, -CH2-CF3, -C2F5, -CH2-CCI3, -
CH2-CBr3, -CHF-CF2CI, -CF2-CF2CI, -CFCI-CF2CI, -CH2-CH2-CN, n-
propyl, -CF2-CF2-CF3, -CF(CF3)2, isopropyl, -CH2-CH2-CH2-CN, -CH2-O-
CH2-CH3, -CH2-CH2-SF3, -CH2-CH2-OCF3, -CH(CH3)-(O-CH3), -
CH(CH3)-(S-CH3), n-butyl, -CF2-CF2-CF2-CF3, -CH2-CH2-CH2-CH2-CN,
sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-heptyl, 4-heptyl, n-
octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl,
(3,3)-dimethylbutyl, -CH2-CH2-O-CH3, -CH2-CH2-O-C2H5, -CH2-CH2-
CH2-O-CH3, ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl, and 3-
pentenyl;
for a radical selected from the group consisting of 2,3-dihydro-1H-
indenyl, cyclopropyl, oxetanyl, cyclobutyl, cyclopentyl, cyclohexyl,
imidazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl,
piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl,
and thiomorpholinyl, each of which can be bonded via a -CH2-O-, -CH2-

CH2-O-, -CH2-CH2-O-CH2-, -CH2-CH(CH3)-O-CH2-, -(CH2)-, -(CH2)2 or -
(CH2)3 group and/or can each be unsubstituted or optionally substituted
by 1, 2, 3, 4, or 5 substituents independently selected from the group
consisting of oxo (=O), thioxo (=S), -OH, -O-CH3, -O-C2H5, -O-
CH(CH3)2, -O-C(CH3)3, -O-CF3, -S-CF3, -SH, -S-CH3, -S-C2H5, -S-
CH(CH3)2, -S-C(CH3)3, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-
butyl, isobutyl, tert-butyl, n-pentyl, -C(=O)-CH3, -C(=O)-C2H5, -C(=O)-
CH(CH3)2, -C(=O)-C(CH3)3, -C(=O)-OH, -C(=O)-O-CH3, -C(=O)-O-C2H5,
-C(=O)-O-CH(CH3)2, and -C(=O)-O-C(CH3)3;
or for a radical selected from the group consisting of phenyl, naphthyl,
thiophenyl, furanyl, pyrrolyl, pyrazolyl, pyrazinyl, pyranyl, triazolyl,
pyridinyl, imidazolyl, thiazolyl, oxazolyl, and isoxazolyl, and each radical
can be bonded via a -(CH2)-, -(CH2)2 or -(CH2)3 group and/or can be
unsubstituted or optionally substituted by 1, 2, 3, 4, or 5 substituents
independently selected from the group consisting of F, CI, Br, I, -CN, -
CF3, -SF5, -OH, -O-CH3, -O-C2H5, -O-CH(CH3)2, -O-C(CH3)3, -NH2, -
NO2, -O-CF3, -S-CF3, -SH, -S-CH3, -S-C2H5, -S-CH(CH3)2, -S-C(CH3)3,
methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl,
n-pentyl, -C(=O)-OH, -C(=O)-O-CH3, -C(=O)-O-C2H5, -C(=O)-O-
CH(CH3)2, -C(=O)-O-C(CH3)3, -NH-CH3, -NH-C2H5, -NH-C(CH3)3, -
N(CH3)2, -N(C2H5)2, -N(CH3)-(C2H5), -NH-C(=O)-O-CH3, -NH-C(=O)-O-
C2H5, -NH-C(=O)-O-C(CH3)3, -C(=O)-H, -C(=O)-CH3, -C(=O)-C2H5, -
C(=O)-CH(CH3)2, -C(=O)-C(CH3)3, -C(=O)-NH2, -C(=O)-NH-CH3, -
C(=O)-NH-C2H5, -C(=O)-N(CH3)2, -C(=O)-N(C2H5)2, -O-phenyl, -O-
benzyl, phenyl, and benzyl;

R35, R36, and R37 each independently stand for H; F; CI; Br; I; -SF5; -NO2; -CN;
-NH2; -OH; -SH; -C(=O)-NH2; -S(=O)2-NH2; -C(=O)-NH-OH; -C(=O)-OH;
-C(=O)-H; -S(=O)2-OH; -NHR13; -NR14R15; -OR16; -SR17; -S(=O)-R25; -
S(=O)2-R26; for a radical selected from the group consisting of-CH2-OH,
methyl, -CF3, -CCI3, -CBr3, -CHF2, -CH2F, -CF2CI, -CCI2F, ethyl, -CF2-
CH3, -CH2-CF3, -C2F5, -CH2-CCI3, -CH2-CBr3, -CHF-CF2CI, -CF2-CF2CI,
-CFCI-CF2CI, n-propyl, -CF2-CF2-CF3, -CF(CF3)2, isopropyl, n-butyl,
sec-butyl, isobutyl, and tert-butyl or for a phenyl radical, which are
unsubstituted or can optionally be substituted by 1, 2, 3, 4, or 5
substituents independently selected from the group consisting of F, CI,
Br, I, -CN, -CF3, -SF5, -OH, -O-CH3, -O-C2H5, -O-CH(CH3)2, -O-C(CH3)3,
-NH2, -NO2, -O-CF3, -S-CF3, -SH, -S-CH3, -S-C2H5, -S-CH(CH3)2, -S-
C(CH3)3, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,
tert-butyl, and n-pentyl;
R38 stands for -SF5; -NO2; -CN; -NH2; -OH; -SH; -C(=O)-NH2; -S(=O)2-NH2; -
C(=O)-NH-OH; -C(=O)-OH; -C(=O)-H; -S(=O)2-OH; -NHR39; -NR40R41; -
OR42; -SR43; -C(=O)-OR50; -S(=O)-R52; -S(=O)2-R53; -C(=NH)-NH2; -
C(=NH)-NH-R54; -N=C(NH2)2; -N=C(NHR55)-(NHR56);
for a radical selected from the group consisting of cyclopropyl,
cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, imidazolidinyl,
tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl, piperidinyl,
morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl, and
thiomorpholinyl, each of which is bonded to the basic framework via a

carbon atom of the rings of the aforementioned radicals or via a -
(CH=CH)-, -C≡C or -C≡C-CH2- group and is unsubstituted or can
optionally be substituted by 1, 2, 3, 4, or 5 substituents independently
selected from the group consisting of-CN, -CH2-N(CH3)2, -CH2-
N(C2H5)2, -CH2-NH-CH3, -CH2-NH-C2H5, -N-[C(=O)-C2H5]phenyl, -N-
[C(=O)-CH3]phenyl, oxo (=O), thioxo (=S), -OH, -O-CH3, -O-C2H5, -O-
CH(CH3)2, -O-C(CH3)3, -O-CF3, -S-CF3, -SH, -S-CH3, -S-C2H5, -S-
CH(CH3)2, -S-C(CH3)3, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-
butyl, isobutyl, tert-butyl, n-pentyl, -C(=O)-CH3, -C(=O)-C2H5, -C(=O)-
CH(CH3)2, -C(=O)-C(CH3)3, -C(=O)-OH, -C(=O)-O-CH3, -C(=O)-O-C2H5,
-C(=O)-O-CH(CH3)2, and -C(=O)-O-C(CH3)3;
or for a radical selected from the group consisting of (1,3)-
benzodioxolyl, (1,4)-benzodioxanyl, tetrazolyl, (2,3)-dihydrothieno[3.4-
b][1.4]dioxinyl, benzo[b]furanyl, phenyl, naphthyl, thiophenyl, furanyl,
pyrrolyl, pyrazolyl, pyrazinyl, pyranyl, triazolyl, pyridinyl, imidazolyl,
indolyl, isoindolyl, thiazolyl, oxazolyl, isoxazolyl, pyridazinyl, pyrazinyl,
pyrimidinyl, indazolyl, quinoxalinyl, quinolinyl, and isoquinolinyl, each of
which can be bonded via a -(CH=CH)-, -C=C-, -(CH2)-, -(CH2)2- or -
(CH2)3 group and/or is unsubstituted or can optionally be substituted by
1,2,3, 4, or 5 substituents independently selected from the group
consisting of F, CI, Br, I, -CN, -CF3, -SF5, -OH, -O-CH3, -O-C2H5, -O-
CH(CH3)2, -O-C(CH3)3, -NH2, -NO2, -O-CF3, -S-CF3, -SH, -S-CH3, -S-
C2H5, -S-CH(CH3)2, -S-C(CH3)3, methyl, ethyl, n-propyl, isopropyl, n-
butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, -C(=O)-OH, -C(=O)-O-CH3,
-C(=O)-O-C2H5, -C(=O)-O-CH(CH3)2, -C(=O)-O-C(CH3)3, -NH-CH3, -

NH-C2H5, -NH-C(CH3)3, -N(CH3)2, -N(C2H5)2, -N(CH3)-(C2H5), -NH-
C(=O)-O-CH3, -NH-S(=O)2-CH3, -NH-S(=O2)-C2H5, -NH-S(=O)2-
CH(CH3)2, -NH-C(=O)-O-C2H5, -NH-C(=O)-O-C(CH3)3, -C(=O)-H, -
C(=O)-CH3, -C(=O)-C2H5, -C(=O)-CH(CH3)2, -C(=O)-C(CH3)3, -C(=O)-
NH2, -C(=O)-NH-CH3, -C(=O)-NH-C2H5, -C(=O)-N(CH3)2) -C(=O)-
N(C2H5)2, -O-phenyl, -O-benzyl, phenyl, and benzyl;
R39, R40, and R41, R42, R43, R50, R52, R53, R54, R55, and R56 each independently
stand for a radical selected from the group consisting of methyl, -CF3, -
CCI3, -CBr3, -CHF2, -CH2F, -CF2CI, -CCI2F, -CH2-CN, -CH2-O-CH3, -
CH2-O-CF3, -CH2-SF3, ethyl, -CF2-CH3, -CH2-CF3, -C2F5, -CH2-CCI3, -
CH2-CBr3, -CHF-CF2CI, -CF2-CF2CI, -CFCI-CF2CI, -CH2-CH2-CN, n-
propyl, -CF2-CF2-CF3, -CF(CF3)2, isopropyl, -CH2-CH2-CH2-CN, -CH2-O-
CH2-CH3, -CH2-CH2-SF3, -CH2-CH2-OCF3, -CH(CH3)-(O-CH3), -
CH(CH3)-(S-CH3), n-butyl, -CF2-CF2-CF2-CF3, -CH2-CH2-CH2-CH2-CN,
sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-heptyl, 4-heptyl, n-
octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl,
(3,3)-dimethylbutyl, -CH2-CH2-O-CH3, -CH2-CH2-O-C2H5, -CH2-CH2-
CH2-O-CH3, ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl, and 3-
pentenyl;
for a radical selected from the group consisting of 2,3-dihydro-1H-
indenyl, cyclopropyl, oxetanyl, cyclobutyl, cyclopentyl, cyclohexyl,
imidazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl,
piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl,

and thiomorpholinyl, each of which can be bonded via a -CH2-O-, -CH2-
CH2-O-, -CH2-CH2-O-CH2-, -CH2-CH(CH3)-O-CH2-, -(CH2)-, -(CH2)2- or -
(CH2)3 group and/or can each be unsubstituted or optionally substituted
by 1, 2, 3, 4, or 5 substituents independently selected from the group
consisting of oxo (=O), thioxo (=S), -OH, -O-CH3, -O-C2H5, -O-
CH(CH3)2, -O-C(CH3)3, -O-CF3, -S-CF3, -SH, -S-CH3, -S-C2H5, -S-
CH(CH3)2, -S-C(CH3)3, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-
butyl, isobutyl, tert-butyl, n-pentyl, -C(=O)-CH3, -C(=O)-C2H5, -C(=O)-
CH(CH3)2, -C(=O)-C(CH3)3, -C(=O)-OH, -C(=O)-O-CH3, -C(=O)-O-C2H5,
-C(=O)-O-CH(CH3)2, and -C(=O)-O-C(CH3)3;
or for a radical selected from the group consisting of phenyl, naphthyl,
thiophenyl, furanyl, pyrrolyl, pyrazolyl, pyrazinyl, pyranyl, triazolyl,
pyridinyl, imidazolyl, thiazolyl, oxazolyl, and isoxazolyl, and each radical
can be bonded via a -(CH2)-, -(CH2)2- or -(CH2)3 group and/or can each
be unsubstituted or optionally substituted by 1, 2, 3, 4, or 5 substituents
independently selected from the group consisting of F, CI, Br, I, -CN, -
CF3, -SF5, -OH, -O-CH3, -O-C2H5, -O-CH(CH3)2, -O-C(CH3)3, -NH2, -
NO2, -O-CF3, -S-CF3, -SH, -S-CH3, -S-C2H5, -S-CH(CH3)2, -S-C(CH3)3,
methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl,
n-pentyl, -C(=O)-OH, -C(=O)-O-CH3, -C(=O)-O-C2H5, -C(=O)-O-
CH(CH3)2, -C(=O)-O-C(CH3)3, -NH-CH3, -NH-C2H5, -NH-C(CH3)3, -
N(CH3)2, -N(C2H5)2, -N(CH3)(C2H5), -NH-C(=O)-O-CH3, -NH-C(=O)-O-
C2H5, -NH-C(=O)-O-C(CH3)3, -C(=O)-H, -C(=O)-CH3, -C(=O)-C2H5, -
C(=O)-CH(CH3)2, -C(=O)-C(CH3)3, -C(=O)-NH2, -C(=O)-NH-CH3, -

C(=O)-NH-C2H5, -C(=O)-N(CH3)2, -C(=O)-N(C2H5)2, -O-phenyl, -O-
benzyl, phenyl, and benzyl;
or
R40 and R41 form, together with the interconnecting nitrogen atom as ring
member,
a radical selected from the group consisting of 3-aza-
bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl, 3-aza-bicyclo[3.2.1]octyl, 6-
aza-bicyclo[3.3.1]heptyl, 8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-
diazaspiro[4.5]dec-2-enyl, azocanyl, isoindolyl, indolyl, (1,2,3,6)-
tetrahydropyridinyl, (4,5,6,7)-tetrahydroisoxazolo[5.4-c]pyridinyl,
pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, azepanyl, diazepanyl,
and thiomorpholinyl, of which the heterocycloaliphatic portion can in
each case be unsubstituted or substituted by 1, 2, 3, 4, or 5 radicals
R57;
R57 stands for -NHR58, -NR59R60, or for an alkyl radical selected from the
group consisting of-CF3, -CH2-CF3, methyl, ethyl, n-propyl, isopropyl,
tert-butyl, n-butyl, sec-butyl, and isobutyl;
R58, R59, and R60 each independently stand for -C(=O)-R61; or for an alkyl
radical selected from the group consisting of-CF3, -CH2-CF3, methyl,
ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, and isobutyl;

or for a radical selected from the group consisting of phenyl, naphthyl,
thiophenyl, furanyl, pyrrolyl, pyrazolyl, pyrazinyl, pyranyl, triazolyl,
pyridinyl, imidazolyl, thiazolyl, oxazolyl, and isoxazolyl, and each radical
can be bonded via a -(CH2)-, -(CH2)2- or -(CH2)3 group and/or can each
be unsubstituted or optionally substituted by 1, 2, 3, 4, or 5 substituents
independently selected from the group consisting of F, CI, Br, I, -CN, -
CF3, -SF5, -OH, -O-CH3, -O-C2H5, -O-CH(CH3)2, -O-C(CH3)3, -NH2, -
NO2, -O-CF3, -S-CF3, -SH, -S-CH3, -S-C2H5, -S-CH(CH3)2, -S-C(CH3)3,
methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl,
n-pentyl, -C(=O)-OH, -C(=O)-O-CH3, -C(=O)-O-C2H5, -C(=O)-O-
CH(CH3)2, -C(=O)-O-C(CH3)3, -NH-CH3, -NH-C2H5, -NH-C(CH3)3l -
N(CH3)2, -N(C2H5)2, -N(CH3)-(C2H5), -NH-C(=O)-O-CH3, -NH-C(=O)-O-
C2H5, -NH-C(=O)-O-C(CH3)3, -C(=O)-H, -C(=O)-CH3, -C(=O)-C2H5, -
C(=O)-CH(CH3)2, -C(=O)-C(CH3)3, -C(=O)-NH2, -C(=O)-NH-CH3, -
C(=O)-NH-C2H5, -C(=O)-N(CH3)2l -C(=O)-N(C2H5)2, -O-phenyl, -O-
benzyl, phenyl, and benzyl;
and R61 stands for an alkyl radical selected from the group consisting of -
CF3, -CH2-CF3, methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-
butyl, and isobutyl;
in each case optionally in the form of one of the pure stereoisomers thereof,
particularly enantiomers or diastereoisomers, or the racemates thereof or in
the form of a mixture of stereoisomers, particularly the enantiomers and/or
diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of
corresponding salts, or in each case in the form of corresponding solvates.

3. The compounds according to claim 1 or claim 2, characterized in that
n stands for 0, 1, or 2;
R1 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(=O)-R13; -
OR16; -SR17; -S(=O)2-NR22R23; -S(=O)2-R27; or for a radical selected
from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-
propyl, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl;
R2 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(=O)-R13; -
OR16; -SR17; -S(=O)2-NR22R23; -S(=O)2-R27; or for a radical selected
from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-
propyl, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl;
R3 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(=O)-R13; -
OR16; -SR17; -S(=O)2-NR22R23; -S(=O)2-R27; or for a radical selected
from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-
propyl, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl;
R4 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(=O)-R13; -
OR16; -SR17; -S(=O)2-NR22R23; -S(=O)2-R27; or for a radical selected
from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-
propyl, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl;

R5 stands for H; F; CI; Br; I; -NO2; -CF3; -CN; -NH2; -OH; -NH-C(=O)-R13; -
OR16; -SR17; -S(=O)2-NR22R23; -S(=O)2-R27; or for a radical selected
from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, n-
propyl, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl;
R6 stands for hydrogen or for an alkyl radical selected from the group
consisting of isopropyl, n-butyl, sec-butyl, isobutyl, methyl, ethyl, and n-
propyl;
R7 stands for hydrogen or -OH;
or
R6 and R7 form, together with the interconnecting carbon atom as ring
member, a radical selected from the group consisting of cyclopropyl,
cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl;
R8 stands for -SF5; -O-CF3; -CF3; tert-butyl or -C(CH3)2(CH2OH);
T stands for C-R35 and U stands for C-R36 and V stands for N and W stands
for C-R38
or
T stands for C-R35 and U stands for C-R36 and V stands for C-R37 and W
stands for C-R38;

R13 R16 R17 R22 R23 and R27 egch independ ently stand for a radical selected
from the group consisting of methyl, -CF3, -CHF2, -CH2F, ethyl, -CF2-
CH3, -CH2-CF3, -C2F5, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,
tert-butyl, n-pentyl, 3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl,
(2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl and
ethenyl;
R35, R36, and R37 each independently stand for H; F; CI; Br; I; -SF5; -NO2; -CN;
-NH2; -OH; -SH; -OR16; -SR17; or for a radical selected from the group
consisting of-CH2-OH, methyl, -CF3, -CHF2, -CH2F, ethyl, n-propyl,
isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl;
R38 stands for -SF5; -NO2; -CN; -NH2; -OH; -SH; -NHR39; -NR40R41; -OR42; -
SR43;
for a radical selected from the group consisting of cyclopropyl,
cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, imidazolidinyl,
tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl, piperidinyl,
morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl, and
thiomorpholinyl, each of which is bonded to the parent structure via a
carbon atom of the rings of the aforementioned residues and are
unsubstituted or can optionally be substituted by 1, 2, 3, 4, or 5
substituents independently selected from the group consisting of -CH2-
N(CH3)2, -CH2-N(C2H5)2, -CH2-NH-CH3, -CH2-NH-C2H5, -N-[C(=O)-
C2H5]phenyl, -N-[C(=0)-CH3]-phenyl, methyl, ethyl, n-propyl, isopropyl,
n-butyl, sec-butyl, isobutyl, and tert-butyl;

or for a radical selected from the group consisting of phenyl, thiophenyl,
furanyl, pyrrolyl, pyrazolyl, pyrazinyl, pyranyl, triazolyl, pyridinyl,
imidazolyl, thiazolyl, oxazolyl, isoxazolyl, pyridazinyl, pyrazinyl, and
pyrimidinyl, each of which can be optionally substituted by 1, 2, 3, 4, or
5 substituents independently selected from the group consisting of F,
CI, Br, I, -CN, -CF3, -SF5, -OH, -O-CH3, -O-C2H5, -O-CH(CH3)2, -O-
C(CH3)3, -O-CF3, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl,
isobutyl, tert-butyl, and n-pentyl;
R41, R42, R43, R42, and R43, each independently
stand for a radical selected from the group consisting of methyl, -CH2-
O-CH3, ethyl, n-propyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-
pentyl, n-hexyl, (3,3)-dimethylbutyl, -CH2-CH2-O-CH3, -CH2-CH2-O-
C2H5, and -CH2-CH2-CH2-O-CH3;
for a radical selected from the group consisting of 2,3-dihydro-1 H-
indenyl, cyclopropyl, oxetanyl, cyclobutyl, cyclopentyl, cyclohexyl,
imidazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl,
piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl,
and thiomorpholinyl, each of which can be optionally substituted by 1, 2,
3, 4, or 5 substituents independently selected from the group consisting
of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-
butyl, and n-pentyl;

or
R40 and R41 form, together with the interconnecting nitrogen atom as ring
member, a radical selected from the group consisting of 3-aza-
bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl, 3-aza-bicyclo[3.2.1]octyl, 6-
aza-bicyclo[3.3.1]heptyl, 8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-
diazaspiro[4.5]dec-2-enyl, azocanyl, isoindolyl, indolyl, (1,2,3,6)-
tetrahydropyridinyl, (4,5,6,7)-tetrahydroisoxazolo[5.4-c]pyridinyl,
pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, azepanyl, diazepanyl,
and thiomorpholinyl, of which the heterocycloaliphatic moiety can in
each case be unsubstituted or substituted by 1, 2, 3, 4, or 5 radicals
R57;
R57 stands for -NHR58, -NR59R60, or for an alkyl radical selected from the
group consisting of-CF3, -CH2-CF3, methyl, ethyl, n-propyl, isopropyl,
tert-butyl, n-butyl, sec-butyl, and isobutyl;
R58, R59, and R60 each independently stand for -C(=O)-R61; for an alkyl radical
selected from the group consisting of -CF3, -CH2-CF3, methyl, ethyl, n-
propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, and isobutyl;
or for a radical selected from the group consisting of phenyl and
naphthyl, and the radical can each be bonded via a -(CH2)-, -(CH2)2- or
-(CH2)3 group and/or can each be unsubstituted or optionally substituted
by 1, 2, 3, 4, or 5 substituents independently selected from the group
consisting of F, CI, Br, I, -CN, -CF3, -O-CH3, -O-C2H5, -O-CH(CH3)2, -O-

C(CH3)3, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,
tert-butyl, and n-pentyl;
and R61 stands for an alkyl radical selected from the group consisting of -
CF3, -CH2-CF3, methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-
butyl, and isobutyl;
in each case optionally in the form of one of the pure stereoisomers thereof,
particularly enantiomers or diastereoisomers, or the racemates thereof or in
the form of a mixture of stereoisomers, particularly the enantiomers and/or
diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of
corresponding salts, or in each case in the form of corresponding solvates.
4. The compounds according to any one or more of claims 1 to 3, characterized
in that
n stands for 0, 1, or 2;
R1 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(=O)-
R13; -OR16; -SR17; -S(=O)2-NR22R23 or-S(=O)2-R27;
R2 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(=O)-
R13; -OR16; -SR17; -S(=O)2-NR22R23 or -S(=O)2-R27;
R3 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(=O)-
R13; -OR16; -SR17; -S(=O)2-NR22R23 or-S(=O)2-R27;

R4 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(=O)-
R13; -OR16; -SR17; -S(=O)2-NR22R23 or-S(=O)2-R27;
R5 stands for H; F; CI; Br; I; methyl, ethyl, -NO2; -OH; -NH2; -NH-C(=O)-
R13; -OR16; -SR17; -S(=O)2-NR22R23 or-S(=O)2-R27;
R6 stands for hydrogen or for an alkyl radical selected from the group
consisting of isopropyl, n-butyl, sec-butyl, isobutyl, methyl, ethyl, and n-
propyl;
R7 stands for hydrogen or -OH;
R8 stands for -SF5; -O-CF3; -CF3; tert-butyl; or -C(CH3)2(CH2OH);
T stands for C-R35 and U stands for C-R36 and V stands for N and W stands
for C-R38
or
T stands for C-R35 and U stands for C-R36 and V stands for C-R37 and W
stands for C-R38
R13, R16, R17, R22, R23 and R27 each independently stand for a radical selected
from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl,
sec-butyl, isobutyl, tert-butyl, n-pentyl, and ethenyl;
R35, R36, and R37 each stand for H;

R38 stands for -NHR39; -NR40R41; -OR42; -SR43;
R39, R42, and R43 each independently
stand for a radical selected from the group consisting of methyl, ethyl,
n-propyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-
hexyl, and (3,3)-dimethylbutyl;
or for a radical selected from the group consisting of cyclopropyl,
cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl, each of which can
be optionally substituted by 1, 2, 3, 4, or 5 substituents independently
selected from the group consisting of methyl, ethyl, n-propyl, isopropyl,
n-butyl, sec-butyl, isobutyl, tert-butyl, and n-pentyl;
or
R40 and R41 form, together with the interconnecting nitrogen atom as ring
member, a radical selected from the group consisting of pyrrolidinyl,
piperidinyl, piperazinyl, morpholinyl, and azepanyl, of which the
heterocycloaliphatic moiety can in each case be unsubstituted or
substituted by 1, 2, 3, 4, or 5 radicals R57;
and R57 stands for an alkyl radical selected from the group consisting of
methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, and
isobutyl;

each optionally in the form of one of the pure stereoisomers thereof,
particularly enantiomers or diastereoisomers thereof, the racemates thereof or
in the form of a mixture of stereoisomers, particularly the enantiomers and/or
diastereoisomers, in an arbitrary mixing ratio, or each in the form of
corresponding salts, or each in the form of corresponding solvates.
5. The compounds according to any one or more of claims 1 to 4, characterized
in that
n stands for 1;
R1 stands for H; F; CI; Br; or I;
R2 stands for H; F; CI; Br; I; -OH; -NH2 or -OR16;
R3 stands for H; F; CI; Br; I; -NO2; -OH; -NH2; -NH-C(=O)-R13; -OR16; -
SR17; -S(=O)-NR22R23 or -S(=O)2-R27;
R4 stands for H; F; CI; Br; I; methyl, -OH; -NH2 or -OR16;
R5 stands for H; F; CI; Br or I;
R6 stands for hydrogen or for an alkyl radical selected from the group
consisting of isopropyl, n-butyl, sec-butyl, isobutyl, methyl, ethyl, and n-
PropyI;

R7 stands for hydrogen or -OH;
R8 stands for -SF5; -O-CF3; -CF3; tert-butyl or -C(CH3)2(CH2OH);
T stands for C-R35 and U stands for C-R36 and V stands for N and W stands
for C-R38
or
T stands for C-R35 and U stands for C-R36 and V stands for C-R37 and W
stands for C-R38;
R13 Rie R17 R22 R23 and R27 each independently stand for a radical selected
from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl,
sec-butyl, isobutyl, tert-butyl, n-pentyl, and ethenyl;
R35, R36, and R37 each stand for H;
R38 stands for -NHR39; -NR40R41; -OR42; -SR43;
R39, R42, and R43 each independently
stand for a radical selected from the group consisting of methyl, ethyl,
n-propyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-
hexyl, and (3,3)-dimethylbutyl;

or for a radical selected from the group consisting of cyclopropyl,
cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl, each of which can
be optionally substituted by 1, 2, 3, 4, or 5 substituents independently
selected from the group consisting of methyl, ethyl, n-propyl, isopropyl,
n-butyl, sec-butyl, isobutyl, tert-butyl, and n-pentyl;
or
R40 and R41 form, together with the interconnecting nitrogen atom as ring
member, a radical selected from the group comprising the group
consisting pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, and
azepanyl, the heterocycloaliphatic moiety of which can each be
unsubstituted or substituted by 1, 2, 3, 4, or 5 radicals R57;
and R57 stands for an alkyl radical selected from the group consisting of
methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, and
isobutyl;
each optionally in the form of one of the pure stereoisomers thereof,
particularly enantiomers or diastereoisomers thereof, the racemates thereof or
in the form of a mixture of stereoisomers, particularly the enantiomers and/or
diastereoisomers, in an arbitrary mixing ratio, or each in the form of
corresponding salts, or each in the form of corresponding solvates.
6. The compounds of the general formula la according to any one or more of
claims 1 to 3,

in which
D stands for N or CH;
and
R1, R2, R3, R4, R5, R8, and R42 have the meanings stated in claim 3;
in each case optionally in the form of one of the pure stereoisomers thereof,
particularly enantiomers or diastereoisomers, or the racemates thereof or in
the form of a mixture of stereoisomers, particularly the enantiomers and/or
diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of
corresponding salts, or in each case in the form of corresponding solvates.
7. The compounds of the general formula la according to any one or more of
claims 1 to 6,

la,
in which
D stands for N or CH;
and
R1, R2, R3, R4, R5, R8, and R42 have the meanings stated in claim 4;
in each case optionally in the form of one of the pure stereoisomers thereof,
particularly enantiomers or diastereoisomers, or the racemates thereof or in
the form of a mixture of stereoisomers, particularly the enantiomers and/or
diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of
corresponding salts, or in each case in the form of corresponding solvates.
8. The compounds of the general formula la according to any one or more of
claims 1 to 7,

in which
D stands for N or CH;

and
R1, R2, R3, R4, R5, R8, and R42 have the meanings stated in claim 5;
in each case optionally in the form of one of the pure stereoisomers thereof,
particularly enantiomers or diastereoisomers, or the racemates thereof or in
the form of a mixture of stereoisomers, particularly the enantiomers and/or
diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of
corresponding salts, or in each case in the form of corresponding solvates.
9. The compounds of the general formula lb according to any one or more of
claims 1 to 3,

in which
D stands for N or CH;
and
R1, R2, R3, R4, R5, R8, and R42 have the meanings stated in claim 3;

in each case optionally in the form of one of the pure stereoisomers thereof,
particularly enantiomers or diastereoisomers, or the racemates thereof or in
the form of a mixture of stereoisomers, particularly the enantiomers and/or
diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of
corresponding salts, or in each case in the form of corresponding solvates.
10. The compounds of the general formula lb according to any one or more of
claims 1 to 9,

in which
D stands for N or CH;
and
R1, R2, R3, R4, R5, R8, and R42 have the meanings stated in claim 4;
in each case optionally in the form of one of the pure stereoisomers thereof,
particularly enantiomers or diastereoisomers, or the racemates thereof or in
the form of a mixture of stereoisomers, particularly the enantiomers and/or

diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of
corresponding salts, or in each case in the form of corresponding solvates.
11. The compounds of the general formula lb according to any one or more of
claims 1 to 10,

in which
D stands for N or CH;
and
R1, R2, R3, R4, R5, R8, and R42 have the meanings stated in claim 5;
in each case optionally in the form of one of the pure stereoisomers thereof,
particularly enantiomers or diastereoisomers, or the racemates thereof or in
the form of a mixture of stereoisomers, particularly the enantiomers and/or
diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of
corresponding salts, or in each case in the form of corresponding solvates.

12. The compounds of the general formula Ic according to any one or more of
claims 1 to 3,

in which
D stands for N or CH;
and
R1, R2, R3, R4, R5, R8, and R42 have the meanings stated in claim 3;
in each case optionally in the form of one of the pure stereoisomers thereof,
particularly enantiomers or diastereoisomers, or the racemates thereof or in
the form of a mixture of stereoisomers, particularly the enantiomers and/or
diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of
corresponding salts, or in each case in the form of corresponding solvates.
13. The compounds of the general formula Ic according to any one or more of
claims 1 to 12,

in which
D stands for N or CH;
and
R1, R2, R3, R4, R5, R8, and R42 have the meanings stated in claim 4;
in each case optionally in the form of one of the pure stereoisomers thereof,
particularly enantiomers or diastereoisomers, or the racemates thereof or in
the form of a mixture of stereoisomers, particularly the enantiomers and/or
diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of
corresponding salts, or in each case in the form of corresponding solvates.
14. The compounds of the general formula Ic according to any one or more of
claims 1 to 13,

Ic,
in which
D stands for N or CH;
and
R1, R2, R3, R4, R5, R8, and R42 have the meanings stated in claim 5;
in each case optionally in the form of one of the pure stereoisomers thereof,
particularly enantiomers or diastereoisomers, or the racemates thereof or in
the form of a mixture of stereoisomers, particularly the enantiomers and/or
diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of
corresponding salts, or in each case in the form of corresponding solvates.
15. The compounds according to any one or more of claims 1 to 14, selected from
the group consisting of
[1 ] 2-(4-Amino-3-fluorophenyl)-N-((2-(4-methylpiperidin-1 -yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
[2] 2-(3,5-Dibromophenyl)-N-((2-(4-methylpiperidin-1 -yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)acetamide,
[3] 2-(4-Amino-3-bromo-5-methoxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)acetamide,
[4] 2-(3-Fluorophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)acetamide,

[5] 2-(2,4-Difluorophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)acetamide,
[6] 2-(2,6-Difluorophenyl)-N-((2-(4-methylpiperidin-1 -yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)acetamide,
[7] 2-(2,5-Difluorophenyl)-N-((2-(4-methylpiperidin-1 -yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)acetamide,
[8] 2-(4-Fluorophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)acetamide,
[9] 2-(4-Hydroxy-3-methoxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
[10] 2-(3,5-Difluorophenyl)-N-((2-(4-methylpiperidin-1 -yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
[11] 2-(3,4-Difluorophenyl)-N-((2-(4-methylpiperidin-1 -yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
[12] 2-(4-Fluorophenyl)-N-((2-(4-methylpiperidin-1 -yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
[13] 2-(3-Fluorophenyl)-N-((2-(4-methylpiperidin-1 -yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
[14] 2-(3,4-Diaminophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
[15] N-(2-Butoxy-6-tert-butylpyridin-3-ylmethyl)-2-(3,4-diamino-phenyl)-
propionamide,
[16] N-((6-tert-Butyl-2-(4-methylpiperidin-1-yl)pyridin-3-yl)methyl)-2-(3,4-
diaminophenyl)propanamide,
[17] N-((6-tert-Butyl-2-(cyclohexylthio)pyridin-3-yl)methyl)-2-(3,4-
diaminophenyl)propanamide,

[18] 2-(4-Acetamido-3-fluorophenyl)-N-((2-(4-methylpiperidin-1 -yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
[19] 2-(3,5-Dibromo-4-hydroxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
[20] 2-(4-Amino-3,5-dibromophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
[21] 2-(3-Bromo-4-hydroxy-5-methoxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-
6-(trifluoromethyl)pyridin-3-yl)methyl)acetamide,
[22] 2-(4-Amino-3,5-dibromophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)acetamide,
[23] 2-(3,5-Dibromo-4-hydroxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)acetamide,
[24] 2-(3-Amino-4-hydroxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
[25] 2-(3,5-Dibromo-phenyl)-N-(4-methyl-6'-trifluoromethyl-3,4,5,6-
tetrahydro-2H-[1,2']bipyridinyl-3'-ylmethyl)-acetamide.
[26] 2-(4-Amino-3,5-difluorophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
[27] 2-(3-Fluoro-5-hydroxy-4-nitrophenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
[28] 2-(3-Chloro-4-(methylthio)phenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
[29] 2-(3-Chloro-4-(methylsulfonyl)phenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
[30] 2-(3-Fluoro-4-(methylthio)phenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,

[31] 2-(3-Fluoro-4-(methylsulfonyl)phenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
[32] 2-(4-(N,N-Dimethylsulfamoyl)-3-fluorophenyl)-N-((2-(4-methylpiperidin-
1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
[33] N-(2-Fluoro-4-(1 -((2-(4-methylpiperidin-1 -yl)-6-(trifluoromethyl)pyridin-3-
yl)methylamino)-1-oxopropane-2-yl)phenyl)acrylamide,
[34] N-(2-Fluoro-6-iodo-4-(1-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methylamino)-1-oxopropane-2-
yl)phenyl)acrylamide,
[35] 2-(4-Methoxy-3,5-dimethylphenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
[36] 2-(3,5-Difluoro-4-methoxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
[37] 2-(4-Hydroxy-3,5-dimethylphenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
[38] 2-(3,5-Difluoro-4-hydroxyphenyl)-N-((2-(4-methylpiperidin-1-yl)-6-
(trifluoromethyl)pyridin-3-yl)methyl)propanamide,
in each case optionally in the form of one of the pure stereoisomers thereof,
particularly enantiomers or diastereoisomers, or the racemates thereof or in
the form of a mixture of stereoisomers, particularly the enantiomers and/or
diastereoisomers, in an arbitrary mixing ratio, or in each case in the form of
corresponding salts, or in each case in the form of corresponding solvates.
16. The compounds according to any one or more of claims 1 to 15, characterized
in that, in the FLIPR assay using CHO-K1 cells, which have been transfected

with the human VR1 gene in a concentration below 2000 nM, preferably below
1000 nM, more preferably below 300 nM, even more preferably below 100 nM,
still more preferably below 75 nM, very preferably below 50 nM and most
preferably below 10 nM, they cause a 50 percent displacement of capsaicin
present in a concentration of 100 nM.
17. A process for the production of a compound according to any one or more of
claims 1 to 16, characterized in that at least one compound of the general
formula II,

in which R8, U, T, V, and W have the meanings stated in any one or more of
claims 1 to 16, m stands for 0, 1, 2, or 3, and R stands for hydrogen or for a
linear or branched C1-6 alkyl radical, in a reaction medium, in the presence of
at least one reducing agent, preferably in the presence of at least one
reducing agent selected from the group consisting of sodium hydride, sodium,
potassium hydride, lithium aluminum hydride, sodium tetrahydridoborate, and
di(isobutyl)aluminum hydride
is converted to at least one compound of the general formula III,

in which R8, U, T, V, and W have the meanings stated in any one or more of
claims 1 to 16 and m stands for 0, 1, 2, or 3, and this is optionally purified
and/or isolated,
and at least one compound of the general formula III is converted, in a
reaction medium in the presence of diphenylphosphorylazide or in the
presence of HN3, to at least one compound of the general formula IV,

in which R8, U, T, V, and W have the meanings stated in any one or more of
claims 1 to 16 and m stands for 0, 1, 2, or 3, and this is optionally purified
and/or isolated,
and at least one compound of the general formula IV is converted, in a
reaction medium in the presence of at least one reducing agent, preferably in
the presence of at least one reducing agent selected from the group consisting

of sodium hydride, potassium hydride, lithium aluminum hydride, sodium
tetrahydridoborate, and di(isobutyl)aluminum hydride,
or in a reaction medium in the presence of a catalyst, preferably in the
presence of a catalyst based on platinum or palladium, more preferably in the
presence of palladium-on-charcoal, and in the presence of hydrogen or in the
presence of hydrazine,
or in a reaction medium in the presence of triphenylphosphine
to at least one compound of the general formula V,

in which R8, U, T, V, and W have the meanings stated in any one or more of
claims 1 to 16 and m stands for 0, 1, 2, or 3, and this is optionally purified
and/or isolated,
or at least one compound of the general formula VI

VI,
in which R8, U, T, V, and W have the meanings stated in any one or more of
claims 1 to 16 and m stands for 0, 1,2, or 3, in a reaction medium is
converted,
in the presence of at least one catalyst, preferably in the presence of at least
one catalyst based on palladium or platinum, more preferably in the presence
of palladium-on-charcoal, under a blanket of hydrogen, optionally in the
presence of at least one acid, preferably in the presence of hydrochloric acid,
or in the presence of at least one reducing agent selected from the group
consisting of BH3.S(CH3)2, lithium aluminum hydride, and sodium
tetrahydridoborate, optionally in the presence of NiCI2,
to form at least one compound of the general formula V, optionally in the form
of a corresponding salt, preferably in the form of a corresponding
hydrochloride, and this is optionally purified and/or isolated,
and at least one compound of the general formula V is caused to react with at
least one compound of the general formula VII,

VII,
in which R1, R2, R3, R4, R5, R6, and R7 have the meanings stated in any one or
more of claims 1 to 16, in a reaction medium, optionally in the presence of at
least one suitable coupling agent, optionally in the presence of at least one
base,
or with at least one compound of the general formula VIII,

in which R1, R2, R3, R4, R5, R6, and R7 have the meanings stated in any one or
more of claims 1 to 16 and LG stands for a leaving group, preferably for a
chlorine or bromine atom, in a reaction medium, optionally in the presence of
at least one base, to form at least one compound of the general formula I,

in which T, U, V, W, R1, R2, R3, R4, R5, R6, R7, and R8, have the meanings
stated in any one or more of claims 1 to 16 and n stands for 1, 2, 3, or 4, and
this is optionally purified and/or isolated.
18. A process for the production of at least one compound according to any one or
more of claims 1 to 16, characterized in that at least one compound of the
general formula X,

in which R8, U, T, V, and W have the meanings stated in any one or more of
claims 1 to 16, is caused to react with at least one compound of the general
formula VII,

in which R1, R2, R3, R4, R5, R6, and R7, have the meanings stated in any one
or more of claims 1 to 16, in a reaction medium, optionally in the presence of
at least one suitable coupling agent, optionally in the presence of at least one
base,

or with at least one compound of the general formula VIII,

in which R1, R2, R3, R4, R5, R6, and R7 have the meanings stated in any one or
more of claims 1 to 16 and LG stands for a leaving group, preferably for a
chlorine or bromine atom, in a reaction medium, optionally in the presence of
at least one base, to form at least one compound of the general formula Im,

in which T, U, V, W, R1, R2, R3, R4, R5, R6, R7, and R8 have the meanings
stated in any one or more of claims 1 to 16, and this is optionally purified
and/or isolated.
19. A pharmaceutical comprising at least one compound according to any one or
more of claims 1 to 16 and optionally one or more physiologically compatible
adjuvants.

20. The pharmaceutical according to claim 19 for the treatment and/or prophylaxis
of any one or more of the disorders selected from the group consisting of pain,
preferably pain selected from the group consisting of acute pain, chronic pain,
neuropathic pain and visceral pain; arthralgia; hyperalgesia; allodynia;
causalgia; and migraine.
21. The pharmaceutical according to claim 19 for the treatment and/or prophylaxis
of any one or more of the disorders selected from the group consisting of
states of depression; nervous disorders; neurotraumas; neurodegenerative
disorders, preferably selected from the group consisting of multiple sclerosis,
Morbus Alzheimer, Morbus Parkinson, and Morbus Huntington; cognitive
dysfunctions, preferably cognitive deficiency states, more preferably memory
defects; and epilepsy.
22. The pharmaceutical according to claim 19 for the treatment and/or prophylaxis
of any one or more of the disorders selected from the group consisting of
respiratory tract diseases, preferably selected from the group consisting of
asthma, bronchitis and pneumonia; coughing; urinary incontinence; an
overactive bladder (OAB); disorders and/or injuries of the gastrointestinal tract;
duodenal ulcers; gastric ulcers; colitis syndrome; apoplectic strokes; eye
irritations; cutaneous irritations; neurotic skin conditions; allergic skin diseases;
psoriasis; vitiligo; Herpes simplex; inflammations, preferably inflammation of
the intestine, the eyes, the bladder, the skin, or the nasal mucosa; diarrhea;
pruritus; osteoporosis; arthritis; osteoarthritis; rheumatic disorders; food intake

disorders, preferably selected from the group consisting of bulimia, cachexia,
anorexia, and obesity; medicine addiction; medicine abuse; withdrawal
phenomena following medicine addiction; tolerance development to
medicines, particularly to natural or synthetic opioids; drug addiction; drug
abuse; withdrawal phenomena following drug addiction; alcohol addiction;
alcohol abuse and withdrawal phenomena following alcohol addiction; for
diuresis; for antinatriuresis; for affection of the cardiovascular system; for
vigilance enhancement; for treatment of wounds and/or burning; for treatment
of severed nerves; for libido enhancement; for modulation of movement
activity; for anxiolysis; for local anesthesia and/or for inhibition of undesirable
side effects, preferably selected from the group consisting of hyperthermia,
hypertension, and bronchial constriction, as caused by administration of
vanilloid receptor 1 (VR1/TRPV1 receptor) agonists, preferably selected from
the group consisting of capsaicin, resiniferatoxin, olvanil, arvanil, SDZ-249665,
SDZ-249482, nuvanil, and capsavanil.
23. The use of at least one compound according to any one or more of claims 1 to
16 for the production of a pharmaceutical for the treatment and/or prophylaxis
of any one or more of the disorders selected from the group consisting of pain,
preferably pain selected from the group consisting of acute pain, chronic pain,
neuropathic pain, and visceral pain; arthralgia; hyperalgesia; allodynia;
causalgia and migraine.
24. The use of at least one compound according to any one or more of claims 1 to
16 for the production of a pharmaceutical for the treatment and/or prophylaxis

of any one or more of the disorders selected from the group consisting of
states of depression; nervous disorders; neurotraumas; neurodegenerative
disorders, preferably selected from the group consisting of multiple sclerosis,
Morbus Alzheimer, Morbus Parkinson, and Morbus Huntington; cognitive
dysfunctions, preferably cognitive deficiency states, more preferably memory
defects; and epilepsy.
25. The use of at least one compound according to any one or more of claims 1 to
10 for the production of a pharmaceutical for the treatment and/or prophylaxis
of any one or more of the disorders selected from the group consisting of.
respiratory tract diseases, preferably selected from the group consisting of
asthma, bronchitis and pneumonia; coughing; urinary incontinence; an
overactive bladder (OAB); disorders and/or injuries of the gastrointestinal tract;
duodenal ulcers; gastric ulcers; colitis syndrome; apoplectic strokes; eye
irritations; cutaneous irritations; neurotic skin conditions; allergic skin diseases;
psoriasis; vitiligo; Herpes simplex; inflammation, preferably inflammation of the
intestine, the eyes, the bladder, the skin, or the nasal mucosa; diarrhea;
pruritus; osteoporosis; arthritis; osteoarthritis; rheumatic disorders; food intake
disorders, preferably selected from the group consisting of bulimia, cachexia,
anorexia, and obesity; medicine addiction; medicine abuse; withdrawal
phenomena following medicine addiction; tolerance development to
pharmaceuticals, particularly to natural or synthetic opioids; drug addiction;
drug abuse; withdrawal phenomena following drug addiction; alcohol
addiction; alcohol abuse and withdrawal phenomena following alcohol
addiction; for diuresis; for antinatriuresis; for affection of the cardiovascular
system; for vigilance enhancement; for treatment of wounds and/or burning;

for treatment of severed nerves; for libido enhancement; for modulation of
movement activity; for anxiolysis; for local anesthesia and/or for inhibition of
undesirable side effects, preferably selected from the group consisting of
hyperthermia, hypertension, and bronchial constriction, as caused by
administration of vanilloid receptor 1 (VR1/TRPV1 receptor) agonists,
preferably selected from the group consisting of capsaicin, resiniferatoxin,
olvanil, arvanil, SDZ-249665, SDZ-249482, nuvanil, and capsavanil.

The present invention relates to novel vanilloid receptor ligands, to processes for the
production thereof, to pharmaceuticals containing said compounds and to the use of
said compounds for the production of pharmaceuticals.

Documents:

3972-KOLNP-2009-(05-02-2014)-ANNEXURE TO FORM 3.pdf

3972-KOLNP-2009-(05-02-2014)-CORRESPONDENCE.pdf

3972-KOLNP-2009-(13-08-2014)ABSTRACT.pdf

3972-KOLNP-2009-(13-08-2014)ANNEXURE TO FORM 3.pdf

3972-KOLNP-2009-(13-08-2014)CLAIMS.pdf

3972-KOLNP-2009-(13-08-2014)CORRESPONDENCE..pdf

3972-KOLNP-2009-(13-08-2014)CORRESPONDENCE.pdf

3972-KOLNP-2009-(13-08-2014)OTHERS.pdf

3972-KOLNP-2009-(13-08-2014)PETITION UNDER RULE 137.pdf

3972-kolnp-2009-abstract.pdf

3972-kolnp-2009-claims.pdf

3972-KOLNP-2009-CORRESPONDENCE 1.1.pdf

3972-KOLNP-2009-CORRESPONDENCE 1.2.pdf

3972-kolnp-2009-correspondence.pdf

3972-kolnp-2009-description (complete).pdf

3972-kolnp-2009-form 1.pdf

3972-KOLNP-2009-FORM 18.pdf

3972-kolnp-2009-form 2.pdf

3972-KOLNP-2009-FORM 3.1.1.pdf

3972-kolnp-2009-form 3.pdf

3972-kolnp-2009-form 5.pdf

3972-kolnp-2009-international preliminary examination report.pdf

3972-kolnp-2009-international publication.pdf

3972-kolnp-2009-international search report.pdf

3972-KOLNP-2009-PA.pdf

3972-kolnp-2009-pct priority document notification.pdf

3972-kolnp-2009-pct request form.pdf

3972-kolnp-2009-specification.pdf

3972-kolnp-2009-translated copy of priority document.pdf

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Patent Number

263974

Indian Patent Application Number

3972/KOLNP/2009

PG Journal Number

49/2014

Publication Date

05-Dec-2014

Grant Date

28-Nov-2014

Date of Filing

16-Nov-2009

Name of Patentee

GRÜNENTHAL GMBH

Applicant Address

ZIEGLERSTRASSE 6, 52078 AACHEN, GERMANY

Inventors:

#	Inventor's Name	Inventor's Address
1	BAHRENBERG, GREGOR	KLEINBAHNSTR. 7A, D-52078 AACHEN, GERMANY
2	SUNDERMANN, BERND	TANNENMÜHLENWEG 8, D-61381 FRIEDRICHSDORF, GERMANY
3	DE VRY, JEAN	MÜHLENROTSCHEN 40, D-52223 STOLBERG, GERMANY
4	SAUNDERS, DEREK	FÖRSTERSTRASSE 19, D-52072 AACHEN, GERMANY
5	PRZEWOSNY, MICHAEL	BORNGASSE 43, D-52062 AACHEN, GERMANY
6	FRANK, ROBERT	LUISENSTRASSE 28, D-52070 AACHEN, GERMANY
7	CHRISTOPH, THOMAS	SCHILDERSTRASSE 42, D-52080 AACHEN, GERMANY
8	SCHIENE, KLAUS	SCHAAN 51, D-41363 JÜCHEN, GERMANY
9	LEE, JEEWOO	DIGITALBIOTECH CO., LTD. 1227 SHINGIL-DONG, ANSAN-SI, GYENGGI-DO 425-838, KOREA

PCT International Classification Number

C07D213/64; A61K31/44; A61K31/4545

PCT International Application Number

PCT/EP2008/002994

PCT International Filing date

2008-04-15

PCT Conventions:

#	PCT Application Number	Date of Convention	Priority Country
1	10 2007 018 151.7	2007-04-16	Germany