Title of Invention	NOVEL ANTIINFECTIVE COMPOUNDS AND THEIR PHARMACEUTICAL COMPOSITIONS
Abstract	The present invention relates to novel triazole compounds of formula (I), their derivatives, their analogs, their tautomeric forms, their regioisomers, their rotamers, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutical compositions containing them. More particularly, the present invention relates to novel triazoles of the general formula (I) where all symbols are as defined in the specification

Title of Invention

NOVEL ANTIINFECTIVE COMPOUNDS AND THEIR PHARMACEUTICAL COMPOSITIONS

Abstract

The present invention relates to novel triazole compounds of formula (I), their derivatives, their analogs, their tautomeric forms, their regioisomers, their rotamers, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutical compositions containing them. More particularly, the present invention relates to novel triazoles of the general formula (I) where all symbols are as defined in the specification

Full Text	Field of the Invention The present invention provides novel triazole compounds of formula (I), their I derivatives, their analogs, their tautomeric forms, their regioisomers, their rotamers, their 1 stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their prodruge, their metabolites, their pharmaceutically acceptable solvates and pharmaceutical compositions containing them. More particularly, the present invention relates to novel triazoles of the general formula (I). their derivatives, their analogs, their tautomeric forms, their regioisomers, their rotamers, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their prodrugs their metabolites, their pharmaceutically acceptable solvates and pharmaceutical compositions containing them. The present invention also relates to a process for the preparation of the above said novel compounds, their derivatives, their analogs, their tautomeric forms, their regioisomers, their rotamers, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their prodruge, their metabolites, their pharmaceutically acceptable solvates and pharmaceutical compositions containing them. The present invention also relates to novel intermediates, methods for their preparation and their use in the preparation of compounds of formula (I). Background of the Invention Since the discovery of penicillin, pharmaceutical companies have produced more than one hundred antibacterial agents to combat a wide variety of bacterial infections. In the past several years, due to the misuse of these antibiotics there has been rapid emergence of bacterial resistance to several of these antibiotics. The multidrug resistance among these bacterial pathogens may also be due to mutation leading to more virulent clinical isolation, the most disturbing milestone has been the acquisition of resistance to vancomycin, an antibiotic generally regarded as the agent of last resort for serious Gram-positive infections. This growing multidrug resistance has recently rekindled interest in the search for new structural class of antibiotic that inhibit or kill these bacteria possibly by novel mechanisms. A problem of larger dimension is the increasing incidence of the more virulent, Methicillin-Resistant Staphylococcus Aureas (MRSA) among clinical isolates found worldwide. Many MRSA strains are resistant to most of the known antibiotics, but have remained sensitive to vancomycin. However, in view of the increasing reports of vancomycin resistant clinical bacterial isolates and growing problem of bacterial resistance, there is an urgent need for new molecular entities effective against the emerging and currently problematic Gram-positive organisms. Bacterial infections and antibacterial resistance are long term problems that call for innovative new therapeutics. There is an urgent need for novel antibacterial compounds. The wide spread use, rather misuse of antibacteria has led to an increase in multidrug resistant bacteria. This is further escacerbated by the use of antibacterials as feed supplements in farm animals and poultry. Yet new classes are unfortimately difficult to develop and any new drugs may quickly loose effectiveness, for example, the first entirely new antibacterial released in market over the past 30 years like Linezolid (Zyovx , Pharmacia Upjohn) proves the capacity for microorganism to develop resistance. Soon after introduction, clinics reported cases of resistance (Lancet 2001, 358(9277): 207-8) and resistant strains have been selected in the lab where a target site alteration was found to reduce drug binding (Antimicrob. Agents Chemother. 2001, 3(3): 288-294) Advancements have been made by several firms in expanding oxazolidinons (Linezolide class of compounds) SAR (structure activity relationship) as well as the spectrum of activity to include the fastidious Gram negative organisms such as Hemophilus influenzae (H. influenzae) and Morexella catarrhalis (M. catarrhalis). With this background we initiated our research program in the area of triazoles and invented new class of chemical entities such as 1,2,3-triazoles effective against wide variety of infectious pathogens including Gram positive/Gram negative and aerobic, anaerobic bacteria. Various l,2,3-tria2oles, 1,2,4-triazoles and benzotriazoles have been reported to show biological activities ranging from anti-inflammatory to antiproliferative and have therefore found applications in medicinal chemistry. The literature survey particularly reveals the use of 1,2,3-triazoles, for the treatment of neuropathic pain and associated hyperalgesia, including trigeminal and herpectic neuralgia, diabetic neuropathic pain, migraine, causalgia and deafferentation syndromes such as brachial plexus avulsion, an anticoccidiostat, as antiproliferative agents, for antimetastatic activity in a model of ovanan cancer progression, for anti-inflammatory effect, controlling activity against noxious organisms, for the treatment of ischemia, anti-human immunodeficiency virus activity etc. However, there are no reports of l,2,3-tria2ole derivatives of the present invention being used for treating bacterial infections, specifically against multidrug resistant strains. The new class of triazoles of the present invention is useful for the treatment of a number of resistant and sensitive gram-positive strains both in vitro and in vivo. (a) Chem. Pharm. Bull. 48(12), 1935-1946 (2000) discloses the triazoles of formula (ia) and (ib), which are reported as antifungal agents, where X represents N, CH or CH2. U.S. 6,054,471 discloses fluorinated triazoles of the formula (ii), which are reported for the treatment of neuropathic pain and associated hyperalgesia, including trigeminal and herpectic neuralgia, diabetic neuropathic pain, migraine, causalgia and deafferentation syndromes such as brachial plexus avulsion, where Ph is an o-fluorinated phenyl group which may be additionally substituted by 1 or 2 halogen atoms selected from fluorine and chlorine; R11 is hydrogen, carbamoyl, N-(C2-C5) alkanoylcarbamoyl or N,N"di-(C1-C4)alkylcarbamoyl; R21 is carbamoyl, N-(C2-C5) alkanoylcarbamoyl or N,N-di- (C1-C4) alylcarbamoyl. An example of this class of compounds is shown in formula (iia), (c) J. Med. Chem., 2843, 1991 discloses compound of formula (iii), which is an anticoccidiostat and also been found to have antiproliferative activity in several disease models and to posses antimetastatic activity in a model of ovarian cancer progression, (d) J. Heterocycl. Chem., 609, 1989 discloses compound of formula (iv), which is reported for anti-inflammatory effects, (e) EPO publication no 0304221 A2 discloses compounds of formula (v), which are reported as antiproliferative agents, wherein p is 0 to 2; m is 0 to 4; and n is 0 to 5; X is O, S, SO, SO2, CO, CHCN, CH2 or C= NR6 where R6 is hydrogen, loweralkyl, hydroxy, loweralkoxy, amino loweralkylamino. diloweralkylamino or cyano, and, R'4 and R'5 are independently halogen, cyano, trifluoromethyl, loweralkanoyl, nitro, loweralkyl, loweralkoxy, carboxy, carbalkoxy, trifluoromethoxy, acetamido, loweralkylthio, loweralkylsulfonyl, trichlorovinyl, trifluoromethylthio. trifluoromethylsuifmyl, or trifluoromethylsulfonyl; R'2 is amino, mono or diloweralkylamino, acetamido, acetimido, ureido, formamido, or guanidino; and R'a is carbamoyl, cyano. carbazoyl, amidino or N-hydroxycarbamoyl. An example of this class of compounds is shown in formula (va), Summary of the Invention With an objective to develop novel compounds effective against a number of human and veterinary pathogens sensitive as well as resistant to various antiinfectives, including Gram-positive, Gram-negative, aerobic and anerobic bacteria. The pathogens such as MRSA, Streptococci including Str pneumoniae, Str. pyogenes, Enterococci as well as anaerobic organisms such as Bacteroides spp., Clostridia spp. species and Acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp. fastidious Gram negative organisms, H. influenzae, M. catarrhalis and several other bacterial species resistant to fluoroquinolone, Macrolide, Vancomycin, Aminoglycosides, Streptogramin, Lincosamides and (3-Lactam, we focussed our research to develop new compounds effective against the above mentioned organisms, as well as expanded spectra of activity to include community acquired pneumonia (CAP). Efforts in this direction have led to the preparation of compounds having general formula (I) as defined above. The present invention provides novel 1,2,3-triazole derivatives of the general formula (I) as defined above and their derivatives, their analogs, their tautomeric forms, their regioisomers, their rotamers, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their prodruge, their metabolites, their pharmaceutically acceptable solvates and pharmaceutical compositions containing them, or their mixtures having enhanced activities, without toxic effect or with reduced toxic effect. The present invention also provides a process for the preparation of novel 1,2,3-triazole derivatives of the formula (I) as defined above and their derivatives, their analogs, their tautomeric forms, their regioisomers, their rotamers, their stereoisomers, their polymorphs, their prodruge, their metabolites and their pharmaceutically acceptable salts. An aspect of the present invention is to provide pharmaceutical compositions containing compounds of the general formula (I), their analogs, their derivatives, their tautomers, their stereoisomers, their rotamers, their regioisomers, their polymorphs, their salts, solvates or their mixtures in combination with suitable carriers, solvents, diluents and other media normally employed in preparing such compositions. Detailed description of the Invention The present invention provides compounds of general formula (I), where R represents halogen, azido, thioalcohol, isothiocyanate, hydroxy, isoindole-l,3-dione, substituted or unsubstituted (C1-C10)alkylsulfonyloxy, arylsulfonyloxy, (C1-C10)acyloxy group, NHR4 where R4 represents substituted or unsubstituted groups selected from (C1- C10)alkyl, (C1-C10)acyl, thio(C1-C10)acyl, (C1-C10)alkoxycarbonyl, (C3- C10)cycloalkoxycarbonyl, (C3-C10)cycloalkoxythiocarbonyl, (C2-C10)alkenyloxycarbonyl, (C2-C10)alkenylcarbonyl, heteroaryl, aryloxycarbonyl, heteroarylcarbonyl, heteroarylthiocarbonyl, (C1-C10)alkoxythiocarbonyl, (C2-C10)alkenyloxythiocarbonyl, aryloxythiocarbonyl, -C(=O)-C(=O)-(C1-C10)alkyl, -C(=O)-C(=O)-aryl, -C(=O)-C(=O)-(C1-C10) alkoxy, -C(=O)-C(=O)-aryloxy, -C(=O)-C(=S)-(C1-C10)alkyl, -C(=O)-C(=S)-aryl, -C(=S)-S-(C1-C10)alkyl, -C(=S)-NH2, -C(-S)-NH-(CrC,o)alkyl, -C(=S)-N-((C1-C10)alkyl)2, -C(=S)-NH-(C2-C10)alkenyl, -C(-S)-C(=O)- (C1-C10)alkoxy, -C(=S)-C(-0)-aryloxy, -C(=S)-0-C(=O)-(C1-C10) alkyl, -C(=S)-C(=S)-(Ct-C,o)alkyl, -C(=S)-C(=S)-aryl, -C(=S)-NH-C(=O)-aryl, -C(=S)-NH-aralkyl, -C(=S)-NH.heteroaralkyl, -C(=NH)-NH2, -C(=NH)-(C1-C10)alkyl, -C(=NH)-aryl, -S (O)2(C1-C10)alkyl, -S(O)2aryl, thiomorpholinylthiocarbonyl, pyrrolidinylthiocarbonyl or -C(=S)-N(R'R"), where R' and R" together form a substituted or unsubstituted 5 or 6 member heterocycle ring containing nitrogen and optionally having one or two additional hetero atoms selected from O, S or N; R and R may be same or different and independently represent hydrogen, halogen atom, substituted or unsubstituted (C1-C10)alkyl group, halo(C1-C10)aIkyl, aryl, heteroaryl, aralkyl, cyano, nitro, OR4 where Ra represents substituted or unsubstituted (C1-C10)alkyl group; Y1 and Y3 may be same or different and independently represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or unsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(Cr C10)alkyI, (C1-C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (C1-C10)alkylsulfonyl, (C1- C10)alkylcarbonylamino(C1-C10)alkyl arylcarbonylamino(C1-C10)alkyl, (C1-C10) aIkylcarbonyloxy(C1-C10)alkyl, amino(C1-C10)alkyl, mono(C1-C10)alkylaniino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyi, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y1, Y2 may represent =O, =S, substituted or unsubstituted =NOR"' group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyi group; Z represents 0, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates. Suitable groups represented by R4 are described as (C1-C10)alkyl group such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-hntyl and the like, the (CpC10)alkyl group may be substituted; (C1-C10)acyl group such as -C(=O)H, -C(=O)CH3, - C(=O)CH2CH3, -C(=O)(CH2)2CH3, -C(=O)(CH2)3CH3, -C(=O)(CH2),CH3. -C(=O)(CH2)5CH3, -C(=O)Ph and the like, the (C1-C10)acyl group may be substituted; thio(C1-C10)acyl group such as -C(=S)H, -C(=S)CH3, -C (=S)CH2CH3, -C(=S)Ph and the like, the thio(C1-C10)acyl group may be substituted; (C1-C10) alkoxycarbonyl group containing (C1-C10)alkyl group which may be linear or branched such as methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, isopropoxycarbonyl and the like, the (C1 - C10)alkoxycarbonyl group may be substituted; (C3-C10)cycloalkoxycarbonyl such as cyclopropoxycarbonyl, cyclobutoxycarbonyl and the like, the (C3-C10) cycloalkoxycarbonyl may be substituted; (C3-C10)cycloalkoxythiocarbonyl such as cyclopropoxythiocarbonyl, cyclobutoxythiocarbonyl and the like, the (C3-C10) cycloalkoxythiocarbonyl may be substituted; (C2-C10)alkenylcarbonyl such as ethenylcarbonyl, propenylcarbonyl, butenylcarbonyl and the like, the (C2"C10)alkenylcarbonyl may be substituted; heteroaryl group such as pyridyl, furyl, thiophenyl, benzothiazoyl, purinyl, benzimidazoyl, pyrimidinyl, tetrazolyl and the like, the heteroaryl group may be substituted; heteroarylcarbonyl such as pyridylcarbonyl, furylcarbonyl, thiophenylcarbonyl, benzothiazoylcarbonyl, benzimidazoylcarbonyl, pyrimidinylcarbonyl, pyridazinecarbonyl, pyrimidinecarbonyl, pyrazinecarbonyl, tetrazolylcarbonyl and the like, the heteroarylcarbonyl group may be substituted, heteroarylthiocarbonyl such as pyridylthiocarbonyl, furylthiocarbonyl. thiophenyithiocarbonyl, benzothiazoyylhiocarbonyl, benzimidazoylthiocarbonyl, pyrimidinylthiocarbonyl, pyridazinethiocarbonyl, pyrimidinethiocarbonyl, pyrazinethiocarbonyl, tetrazolylthiocarbonyl and the like, the heteroarylthiocarbonyl may be substituted, (C2-C io)alkenyloxycarbonyl group such as ethenyloxycarbonyl, propenyloxycarbonyl, butenyloxycarbonyl and the like, the (C2-C10)alkenyloxycarbonyl may be substituted; aryloxycarbonyl group such as phenoxycarbonyl, benzyloxycarbonyl group and the like, the aryloxycarbonyl group may be substituted; (C1-C10)alkoxythiocarbonyl group such as CH3O-C(-S)-, C2H5O-C(=S)- CBHTO-Q-S)- and the like, (C1-C10)alkoxythiocarbonyl group may be substituted; (C2-C10)alkenyloxythiocarbonyl group such as ethenyloxythiocarbonyl, propenyloxythiocarbonyl, butenyloxythiocarbonyl and the like, the (C2-C10) alkenyloxythiocarbonyl group may be substituted; aryloxythiocarbonyl group such as (phenyl)0-C(=S)-, (benzyI)O-C(=S)- and the like, which may be substituted; -C(=O)-C(=O)-(C1-C10)alkyl group such as -C(=O)-C(=O)methyl, -C(=O)"C(=O)ethyl, -C(=O)-C(=O)propyl and the like, which may be substituted; -C(=O)-C(=O)-aryl group such as -C(=O)-C(=O)phenyl, -C(=O)-C(=O)naphthyl and the like, which may be substituted; -C(=O)-C(=O)-(C1-C10)alkoxy group such as -C(=O)-C(=O)methoxy, -C(=O)-C(=O)ethoxy, -C(-O)" C(=O)propyloxy and the like, which may be substituted; -C(=O)-C(=O)-aryloxy group such as -C(=O)-C(=O)phenyloxy, -C(=O)-C(=O)benzyloxy, which may be substituted; -C(=O)-C(=S)-(C1-C10)alkyl group such as -C(=O)-C(=S)-methyl, -C(=O)-C(=S)-ethyl, -C(=O)" C(=S)-propyl, -C(=O)-C(=S)-butyl and the like, which may be substituted; -C(=O)-C(=S)-aryl group such as -C(-0)-C(=S)-phenyl, -C(=O)-C(=S)-naphthyl and the like, which may be substituted; -(C-S)-S-(C1-C10)alkyl such as -(C=S)"S-methyl, -(C=S)^S-ethyl, ^(C=S)-S-propyl and the like, which may be substituted; -(C=S)-NH2, which may be substituted; -(C=S)-NH-(C1-C10)alkyl such as -(C=S)-NH-methyl, -(C=S)-NH-ethyl, "(C=S)-NH-propyl and the like, which may be substituted; "C(=S)-N-((CrC6)alkyl)2 such as -C(=S)-N-(methyl)2, -C(=S)-N-(ethyl)2, -C(=S)-N-(propyl)2 and the like, which may be substituted; -C(=S)-NH-(C2-C10)alkenyl such as -C(=S)-NH-ethenyl, -C(=S)-NH"propenyl, -C (=S)-NH"butenyI and the like, which may be substituted; -(C=SHC=O)-(C1-C10)alkoxy such as -(C=S)-(C=O)-methoxy, -(C=S)-(C=O)-ethoxy, -(C=S)-(C=O)-propoxy and the like, which may be substituted; -(C=S)-(C=O)-aryloxy such as -(C=S)-(C=O)-phenyloxy, -(C=S)-(C=O)-naphthyloxy and the like, which may be substituted; -C(=S)-O-(C=O)-(C1-C10)alkyl such as -C(=S)-O-(C=O)-methyl, -C(=S)-O-(C=O)-ethyl, -C(=S)-O-(C=O)-propyl and the like, which may be substituted; -C(=S)-C(=S)-(C1-C10)alkyl group such as -C(=S)-C(=S)methyl, -C(=S)-C(=S)ethyl, -C(=S)-C(=S)propyl and the like, which may be substituted; -C(=S)-C(=S)aryl group such as -q=S)-C(=S)phenyl, -C(=S)-C(=S)naphthyl and the like, which may be substituted; -C(=S)-NH-C(=O)-aryl group such as -C(=S)-NH-C(=O)-phenyl, -C(=S)-NH-C(^0)-naphthyl and the like, ^C(=S)-NH-C(=O)-aryl group may be substituted; -C(=S)-NH-aralkyl group such as -C(=S)-NH-benzyl, -C(=S)-NH-phenethyl, -C(=S)-NH-C6H5CH2CH2CH2, -C(=S)-NH-naphthylmethyI and the like, -C(=S)-NH-aralkyl group may be substituted; -C(=S)-NH-heteroaralkyl such as -C(=S)-NH-pyridinemethyl, -C(=S)-NH-furanmethyl, -C(=S)-NH-thiophenylenemethyl, -C(=S)-NH-benzothiazolemethyl, -C(=S)-NH-benzimidazolemethyl, -C(=S)-NH-pyrimidinemethyl, -C(=S)-NH-pyrimidinemethyl, -C(^S)-NH-pyrazinemethyl, -C(=S)-NH-tetrazolemethyl and the like, where -C(=S)-NH-aralkyl group may be substituted; -C(=NH)-NH2, which may be substituted; -C(=NH)-(C1-C10)alkyl such as -C(=NH)-methyI, -C(=NH)-ethyl, -C(=NH)-propyl and the like, which may be substituted; -C(=NH)-aryi such as -C(=NH)-phenyl, -C(=NH)-naphthyl and the like, which may be substituted; S(O)2-(C1-C10)alkyl such as S(O)2-methyl, S(O)2"ethyl, S(O)2-propyl, S(O)2-isopropyl, S(O)2-butyl, S(O)2-isobutyl and the like, which may be substituted; S(O)2-aryl such as S(O)2-phenyl, S(O)2-naphthyl and the like, which may be substituted; thiomorpholinylthiocarbonyl, which may be substituted; pyrrolidinylthiocarbonyl, which may be substituted; or -C(=S)-N(R'R") where R'R' are as defined above. A 5 or 6 member heterocycle ring containing nitrogen, optionally having one or two additional heteroatoms selected from oxygen, nitrogen or sulfur, formed by R' & R" is selected from unsubstituted or substituted pyrrolidinyl, pyrroiyl, morpholinyl, thiomorpholinyl, benzothiazole, benzoimidazolyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl and the like. When the groups represented by R4, R4a 44b, 44d, R4c, R, R2 and heterocycles formed by R'and R" are substituted, the substituents may be selected from halogen atom such as chlorine, fluorine, bromine and iodine; hydroxy, amino, cyano, nitro, (C1-C10)alkyl, which is defined as earlier; hydroxy(C1-C10)alkyl, in which (C1-C10)alkyl groups is as defined earher; (C1-C10)alkoxy group such as methoxy, ethoxy, propoxy and the like; =O, =S, aryl group such as phenyl, naphthyl and the like, hydroxyaryl such as hydroxyphenyi, hydroxynaphthyl and the like, pyridyl, mono(C1-C10)alkylamino such as methylamino, ethylamino, propylamino and the like; di(C1-C10)alkylamino such as dimethyl amino, diethylamino, dipropylamino and the like; (C1-C10)acyl group such as -C(=O)H, -C(=O)CH3, -C(=O)CH2CH3, -C(=O)(CH2)2CH3, -C(=O)(CH2)3CH3, -C(=O)(CH2)4CH3, -C(=O)(CH2)5CH3, ^-C(=O)Ph and the like; thio(C1-C10)acyl group such as -C(=S)H, -C(=S)CH3, -C (=S)CH2CH3, -C(=S)Ph and the like; (C1-C10)alkoxycarbonyl group such as methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, butoxycarbony, tert-butoxycarbonyl(BOC) and the like; (C1-C10)alkoxyaryl group such as methoxyaryl, ethoxyaryl, propoxyaryl, iso-propoxyaryl, butoxyaryl and the like, where aryl group is as defined above or carboxylic acid or its derivatives selected from amides and esters such as CONH2, CONHMe, CONMe2, CONHEt, CONEt2, CONHPh, COOCH3, COOC2H5 or COOC3H7. Suitable groups represented by R and R may be selected from hydrogen, halogen atom such as fluorine, chlorine or bromine; substituted or unsubstituted (C1-C10)alkyl group such as methyl, ethyl, n-propyl, isopropyl, n-butyl, iso-butyl, t-butyl, n-pentyl, iso-pentyl, n-hexyl and the like; halo(C1-C10)alkyl group such as halomethyl, haloethyl, halopropyl, trihalomethyl and the like, wherein the halo group is selected from fluorine, chlorine, bromine or iodine; cyano, nitro; aryl group such as phenyl, napthyl and the like; heteroaryl or aralkyl groups is as defined above; ORa where Ra represents substituted or unsubstituted (C1-C10) alkyl group such as methyl, ethyl, propyl, isopropyl and the like. Suitable substitutents on R1 , R2 and Ra are selected from hydroxy, halogen, nitro, amino, (C1-C10)alkyl, (C1-C10)alkoxy, =O, =S, cyano group, or carboxylic acid or its derivatives. These groups are as defined above. Suitable groups represented by Y and Y are selected from hydrogen, cyano, nitro, formyl, hydroxy, amino, halogen such as fluorine, chlorine, bromine or iodine;, substituted or unsubstituted (C1-C10)alkyl such as methyl, ethyl, n-propyl, isopropyl, n-butyl, iso-butyl, t-butyl and the like, which may be substituted; hydroxy(C1-C10)alkyl such as hydroxymethyl, hydroxyethyl, hydroxypropyl and the like, which may be substituted; (C1-C10)alkoxy(Cj-Cto) alkyl group such as methoxymethyl, methoxyethyl, ethoxyethyl, ethoxymethyl, methoxypropyl, propoxymethyl, propoxyethyl and the like, which may be substituted; (C1-C10)alkoxycarbonyl group such as methoxycarbonyl, ethoxycarbonyl and the like, which may be substituted; carboxy(C1-C10)alkyl such as -OOC-CH3, -OOC-CH2-CH3 and the like, which may be substituted; (C1-C10)alkylsulfonyl group such as methylsulfonyl, ethylsulfonyl and the like, which may be substituted; (C1-C10)alkylcarbonylamino(C1-C10)alkyl groups such as methylcarbonylaminomethyl, ethylcarbonylaminomethyl, methylcarbonylaminoethyl and the like, which may be substituted; arylcarbonylamino(C1-C10)alkyl such as phenylcarbonylaminomethyl, phenylcarbonylaminoethyl and the like, which may be substituted; (C1-C10)aIkylcarbonyloxy(C1-C10)alkyl group such as methylcarbonyloxymethyl, ethylcarbonylxoymethyl, methylcarbonyloxyethyl, propylcarbonyloxymethyl, propylcarbonyloxyethyl, propylcarbonyloxypropyl and the like, which may be substituted; amino(C1-C10)alkyl such as aminomethyl, aminoethyl, aminopropyi and the like, which may be substituted; mono(C1-C10)alkyIamino such as methylamino, ethylamino, propylamino and the like, which may be substituted; di(C1-C10)alkylamino such as dimethylamino, diethylamino, dipropylamino and the like, which may be substituted; arylamino such as phenylamino, benzylamino and the like, which may be substituted; (C1-C10)alkoxy group such as methoxy, ethoxy, propoxy, isopropoxy and the like, which may be substituted; aryl group such as phenyl, naphthyl and the like, which may be substituted; aryloxy group such as phenoxy, naphthyloxy and the like, the aryloxy group may be substituted; aralkyl such as benzyl, phenethyl, C6H5CH2CH2CH2, naphthylmethyl and the like, the aralkyl group may be substituted; heteroaryl groups such as pyridyl, thienyl, furyl, pyrrolyl, oxazolyl, thiazolyl, pyrazolyi, imidazoiyi, oxadiazolyl, tetrazolyl, benzopynanyl, benzofuranyl and the like, which may be substituted; heteroaralkyl such as imidazolemethyl, imidazoleethyl, pyridylmethyl, furyl methyl, oxazolemethyl, imidazoiyi and the like, which may be substituted; heterocyclyl group such as pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl and the like; heterocycloalkyl groups such as pyrrolidinemethyl, piperidinemethyl, morpholinemethyl, piperazinemethyl and the like, which may be substituted. Any of Ya, or Ys may also represent =O, =S, substituted or unsubstituted =NOR"', where R'" represents hydrogen, (Cr C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group. These groups are defined as above. When the groups represented by Y and Y are substituted, the substituents may be selected from hydroxy, nitro, cyano, amino, tert-butyldimethylsilyloxy (TBSO), halogen atom, (C1-C10)alkyl, (C1-C10)alkoxy, cyclo(C3-C10)alkyl, aryl, benzyloxy, acyl or acyloxy group such as formyloxy, acetyloxy and the like. The remaining groups are as defined above. When the groups represented by R4 and Rd as defined below are substituted, the substituents are selected from halogen, hydroxy, nitro, amino, cyano, (C1-C10)alkyl or (C]-C10) alkoxy, (C1-C10) alkyl and (C1-C10) alkoxy are as defined above. In another aspect, the compounds of the invention comprise a compound of formula (I), wherein: W R"^ is (C1-C10)acyl, thio(C1-C10)acyl, (C1-C10)alkoxycarbonyl, (C1- (Q i C10)alkoxythiocarbonyl. (ii) R2 and R3represent hydrogen and halogen, (iii) 'm' represents 1. (iv) ' ' represents a bond. (v) R4 is (C1-C10)acyl, thio(C1-C10)acyl, (C1-C10)alkoxycarbonyl, (d-C10)alkoxythiocarbonyl; m represents 1; '....' represents a bond; R2 and R3represent hydrogen and halogen, (vi) R4 is (C1-C10)acyl, thio(C1-C10)acyl, (C1-C10)alkoxycarbonyl, (C1-C10)alkoxythiocarbonyl; m represents 1; '....' represents a bond; R2 and R3represent hydrogen and halogen; Y1 and Y2 represent hydrogen atom, (vii) R'is(C1-C10)acyl; m represents 1; '....' represents a bond; R and R represent hydrogen and halogen; Y1 and Y2 represent hydrogen atom, (viii) R4 is thio(C1-C10)acyl; m represents 1; '....' represents a bond; R2 and R3represent hydrogen and halogen; Y1 and Y2 represent hydrogen atom, (ix) R4 is (C1-C10)alkoxycarbonyl; m represents 1; '....' represents a bond; One embodiment of the present invention is to provide a process for the preparation of the compound of formula (I) where R1 represents NHR4 wherein R4 represents hydrogen atom, Z represents O or S, and all other symbols are as defined earlier, which is shown in the following Scheme-I, comprising the following steps:: The compound of formula (la) is reacted with a compound of formula (lb), to obtain a compound of formula (Ic), when X represents halogen atom, by using (C1-C10) alkyllithium such as methyllithium (MeLi), n-butyllithium (n-BuLi), secondary butyllithium (sec.BuLi), tertiary butyllithium (ter.BuLi) and the like, and the like. The compound of formula (Ic), where X represents hydrogen atom is obtained by treating with CsF, The solvent used in the reaction may be selected from tetrahydrofuran (THF), hexamethylphosphoramide (HMPA), diethylether and the like. The temperature and duration of the reaction can be maintained in the range of about -78 to about 100 °C and about 30 min to about 1.5 h respectively. The compound of formula (Ic) is reacted with a compound of formula (Id), to obtain a compound of formula (le), by using a reagent (C1-C10) alkyllithium such as methyllithium (MeLi), n-butyUithium (n-BuLi), secondary butyllithium (sec.BuLi), tertiary butyllithium (ter.BuLi) and the like. The solvent used in the reaction may be selected from THF, HMPA, diethyl ether, 1,4-dioxane and the like. The temperature and duration of the reaction can be maintained in the range of about -78 to about 50 °C and about 4 to about 10 h respectively. The compound of formula (le) is treated with any of the reagents selected from cone HCl, p-toluene sulfonic acid (p-TSA), mesyl chloride & triethylamine, 1,2-diazabicyclo[5,4,0]undec-7-ene (DBU), phosphorous oxychloride (POCI3), The solvent used in the reaction is selected from pyridine, dichloromethane, acetonitrile, toluene and the like, to obtain a compound of formula (If), where '....' represents a bond, The temperature and duration of the reaction can be maintained in the range of about 0 to about 150 °C and about 30 min to about 24 h respectively. The above obtained compound of formula (le) is converted to compound of formula (le), where '....' represents no bond, by treating with Et3SiH & BF3.0Et2, EtaSiH & CF3COOH, TMSCl, Nal, Me2Sil2, Bu3SnH and the like, under the above reaction conditions. The compound of formula (If) is reacted with NaNO2, NaN3. t-Butyi nitrile and the like, to obtain a compound of formula (Ig), The temperature and duration of the reaction can be maintained, in the range of about 0 to about 150 °C and about 30 min to about 24 h respectively. The compound of formula (Ig) is reacted with a compound of formula (Ih), to obtain a compound of formula (I), by using a reagent such as cuprous iodide (Cul), cuprous chloride (CuCl) and the like. The solvent used in the reaction may be selected from acetonitrile, toluene, diemthyl formamide (DMF) and the like. The reaction may be carried out in the presence of such as diisoporpylethylamine, triethylamine and the like. The temperature and duration of the reaction can be maintained in the range of about 0 to about 100 °C and about 30 min to about 12 h respectively. The compound of formula (I), where R represents isoindole-l,3-dione to a compound of formula (I) where R1 represents NHR4 wherein R4 represents hydrogen atom, is carried out by using hydrazine hydride. The solvent used in the reaction is selected from (C1-C6)alcohol such as methanol, ethanol, propanol, isopropanol and the like or mixtures thereof. The temperature of the reaction is maintained at the reflux temperature of the solvent used. The duration of the reaction is maintained in the range of about 2-4 h. Another embodiment of the present invention provides, an alternte process for the preparation of compound of formula (I), where R1 represents NHR4 wherein R4 represents hydrogen atom and all other symbols are as defined earlier, which is shown in the following Scheme-II: The conversion of compound of formula (li) to a compound of formula (Ij) and compound of formula (Ij) to a compound of formula (I), is carried out by using a palladium reagent such as PdCl2CPPh2), Pd2(dba)3 and the like. The solvent used in the reaction is selected from DMF, acetonitrile, 1,4-dioxane and the like. The temperature and duration of the reaction are maintained in the range of about 20 to about 100 oC and about 2 to about 12 h respectively. The compound of formula (I), where R1 represents isoindole-l,3-dione, '....' represents a bond, to a compound of formula (I) where R1 represents NHR4wherein R4 represents hydrogen atom, is carried out by using hydrazine hydride. The solvent used in the reaction is selected from (C1-C6)alcohol such as methanol, ethanol, propanol, isopropanol and the like or mixtures thereof. The temperature of the reaction is maintained at the reflux temperature of the solvent used. The duration of the reaction is maintained in the range of 2-4 h. The above obtained compound of formula (I) is converted to a compound of formula (I), where ' ' represents no bond, by conventional hydrogenation methods, by using reagent such as PtO2, Pd/C, Raney nickel, and the like, along with H2 gas. The solvent used in the reaction is selected from methanol, ethanol, sodium acetate, acetic acid and other related reagents. Another embodiment of the present invention provides the alternate process for the preparation of the compound of formula (I), where R' represents NHR4 wherein R4represents hydrogen atom, Z represents SO or SO2, and all other symbols are as defined earlier, which comprises: (i) converting the compound of formula (I) where R1 represents isoindole-l,3-dione, Z represents S, all other symbols are as defined earlier, to a compound of formula (I), where Z represents SO or SO2 and (ii) converting the above obtained compound of formula (I), to a compound of formula (I) where R' represents NHR4 wherein R4represents hydrogen atom and all other symbols are as defined earlier. The compound of formula (I), where Z represent S, to a compound of formula (I), where Z represents SO or SO2, can be carried out by using reagents like Siodiumperiodate (NaIO4), aluminium oxide (AI2O3), m-chloroperbenzoicacid, potassium permanganate (KMnO4), ruthenium chloride (RuCl3), periodic acid (H5IO6), oxone in presence of solvents like dichlromethane, acetonitrile, water and the like The temperature and duration of the reaction can be maintained in the range of about 0 to about 60oC and about 30 min to about 36 h respectively. The compound of formula (I), where R1 represents isoindole-l,3-dione, to a compound of formula (I) where R1 represents NHR4 wherein R4represents hydrogen atom, in the presence of reagents such as hydrazine hydrate, sodiumborohydrate, N-methyl amine, phenyl hydrazine, Dianion WA-20 in presence of solvents like methnol, isopropanol, ethanol.and like. The temperature and duration of the reaction can be maintained in the range of about 0 to about 100oC and about 30 min to about 36 h respectively. Another embodiment of the present invention provides an alternative process for the preparation of the compound of formula (I) where R* represents azido and all other symbols are as defined earlier, which is shown in Scheme-Ill: where R^, R\ Y', Y^, Z and m are defined as earlier. Scheme-Ill The compound of formula (Ig) may be converted to a compound of formula (I), where R^ represents hydroxy group, by treating with propargyl alcohol. The solvent used in the reaction may be selected from benzene, toluene, xylene, acetonitrile, THF, DMF and the like. The temperature of the reaction may be maintained in the range of about 10 to about 200 °C, preferably about 20 to about 70 °C. The duration of the reaction may be in the range of about 1 to about 25 h, preferably in the range of about 5 to about 20 h. The compound of formula (I) where R' represents hydroxy group may be converted to a compound of formula (I) where R1 represents azido group was carried out in two steps. In step (1) the compound of formula (I) where R^ represents OH is converted to compound of formula (I) where R1 represents leaving group such as halogen atom, by treating with CBr4/PPh3, PBr3, sulfonyl chloride (SOCI2) and the like. The reaction may be carried out in the presence of chloroform, dichloromethane, THF, dioxane and the like or mixtures thereof The reaction may be carried out in the presence or absence of a base such as triethylamine (EtsN), diisopropyl ethylamine, sodium carbonate (Na2CO3), potassium carbonate (K2CO3) and the like. The temperature of the reaction may be maintained in the range of 0 to 80°C, preferably in the range of 0 to 50°C. The duration of the reaction may be in the range of about 1-12 h, preferably in the range of about 1-4 h. In step (2), the compound of formula (I) where R' represents halogen atom may be converted to compound of formula (I) where R' represents azido group by treating with sodium azide (NaN3), lithium azide (LiN3), trialkylsilylazide and the like. The solvent used in the reaction may be selected from acetone, THF, DMF, dimethyl sulfoxide (DMSO), methylcyanide and the like. The temperature of the reaction may be maintained in the range of about 20 to about 120°C, preferably about 20 to about 80°C, The duration of the reaction may be in the range of about 1 to about 12 h, preferably about 1 to about 4 h. Another embodiment of the present invention provides a process for the preparation of compound of formula (I) where R^ represents hydroxy group, which is shown in the following Scheme-IV: where R1,R2,Y1,Y2 Z and m are defined as earlier. Scheme-IV The conversion of compound of formula (Ig) to a compound of formula (I) where R1 represents (C1-C10)acyloxy group, may be carried out in the presence of (C1-C10)alkyl or aryl esters of propargyl alcohol. The solvent used in the reaction may be selected from benzene, toluene, xylene, acetonitrile, THF and the like. The temperature of the reaction may be maintained in the range of about 10 to about 200°C, preferably room temperature to the boiling temperature of the solvent. The duration of the reaction may be in the range of about 1 to about 25 h, preferably in the range of about 5 to about 20 h. The hydrolysis of compound of formula (I) where R1 represents (C1-C10)acyloxy group, to a compound of formula (I), where R1 represents hydroxy group, may be carried out by using conventional ester hydrolysis procedures. Yet another embodiment of the present invention provides a process for the preparation of compound of formula (I), where R1represents NHR4, wherein R4represents substituted or unsubstituted acetyl group and all other symbols are as defined earlier, from a compound of formula (I) where R1represents azido group, where Z,Y',Y2,, R1and m are as defined earlier, The compound of formula (I), where R1represents NHR4, wherein R4represents substituted or unsubstituted acetyl group may be prepared from compound of formula (I), where R1 represents azido group may be carried out by using thiolacetic acid with or without using solvent such as THF, DMF, toluene and the like. The reaction may be carried out at a temperature in the range of about 25 to about 40 °C, preferably at room temperature. The duration of the reaction may be in the range from about 3 to about 24 h, preferably from about 4 to about 12 h. Still another embodiment of the present invention provides a process for the preparation of compound of formula (I), where R1represents NHR4, wherein R4 represents substituted or unsubstituted -C(=S)-R4a wherein R4a represents (C1-C10)alkyl, halo(C1-C10)alkyl, aryl, heteroaryl, .C(=O)-(C1-C10)alkoxy, -C(=O)-(C1-C10)alkoxy, -C(=O)-aryloxy, - C(=S)-(C1-C10)alkyl or -C(=S)-aryl; from compound of formula (I), where R1represents NHR4, where R4 represents substituted or unsubstituted -C(=O)-R4a, wherein R4a represents (C1-C10)alkyl, haloCC1-C10)alkyl, aryl, heteroaryl, -C(=O)-(C1-C10)aikoxy, -C(=O)-aryloxy, -C(=S)-(C1-C10)alkyl or -C(=S)-aryl where all symbols are as defined earlier. The compound of formula (I), where R1 represents NHR4, wherein R4represents substituted or unsubstituted -C(=S)-R4a, from compound of formula (I), where R1 represents NHR4, wherein R4 represents substituted or unsubstituted -C(=O)-R4a, wherein R4a is as defined above, may be carried out by taking a solution of the amide and Lawesson's reagent (2,4-bis(methoxyphenyl)-l,3-dithia-2,4-diphosphetane-2,4-disulfide) in dry dioxane, toluene, THF, DMF and the like. The reaction may be carried out at a temperature in the range of about 20 to about 130°C, preferably in the range of about 55 to about 90 °C. The duration of the reaction may be in the range from about 3 to about 24 h, preferably from about 3 to about 10 h. Another embodiment of the present invention provides a process for the preparation of compound of formula (I), where R1 represents NHR4, wherein R4represents substituted or unsubstituted -C(=S)-OR4b wherein R4b represents (C1-C10)alkyl, cyclo(C3-C10)alkyl, aryl, (C2-C10)alkenyl or -C(=O)-(C1-C10)alkyl group,, which comprises: (i) reacting compound of formula (I) where R1 represents azido group; and all other symbols are as defined earlier, with triphenylphosphine/water or H2-Pd/C, to produce a compound of formula (I), where R1represents NHR4, wherein R4represents hydrogen atom and all other symbols are as defined earlier. (ii) reacting compound of formula (I), where R1represents NHR4, wherein R4 represents hydrogen atom, with thiophosgene or carbon disulfide and chloromethylformate, in the presence of a base to produce a compound of formula (I), where R1 represents isothiocyanate group; and all symbols are as defmed earlier, (iii) converting compound of formula (I) where R1 represents isothiocynate group, to a compound of formula (I), where R1 represents NHR4, wherein R4represents substituted or unsubstituted -C(=S)-OR'4b, wherein R1' is as defmed above and all other symbols are as defined earlier. The conversion of compound of formula (I), where R1represents azido to a compound of formula (I), where R1 represents NHR4, wherein R4represents hydrogen atom may be carried out in the presence of gaseous hydrogen and a catalyst such as Ru, Pd, Rh, Pt, Ni on solid beads such as charcoal, alumina, asbestos and the like. The reduction may be conducted in the presence of a solvent such as dioxane, acetic acid, ethyl acetate, THF, alcohol such as methanol, ethanol, propanol, isopropanol and the like or mixtures thereof A pressure between atmospheric pressure to 60 psi may be used. The reaction may be carried out at a temperature in the range of 25 to 60°C, preferably in the range of room temperature to 80°C. The duration of the reaction may be in the range of about 2 to about 48 h, preferably in the range of about 5 to about 15 h. The reduction may also be carried out by employing PPhs and water. The compound of formula (I), where R1 represents NHR4, wherein R4represents hydrogen atom may be converted to a compound of formula (I) where R1 represents isothiocyanate group, by using thiophosgene or carbon disulfide and chloromethylformate in the presence of a base such as EtsN, K2CO3, sodium hydroxide (NaOH) and the like. The reaction may be carried out in the presence of a solvent such as dichloromethane (CH2CI2), acetonitrile, chloroform (CHCI3), DMF, THF and the like. The reaction may be carried at a temperature in the range of 0 to 60°C, preferably at 0°C. The reaction may be carried out in an inert atmosphere using argon or any other inert gas. The duration of the reaction may be in the range of about 1 to about 24 h, preferably about 2 to about 10 h. The conversion of compound of formula (I) where R1 represents isothiocyanate group, to a compound of formula (I), where R1represents NHR4, wherein R4represents substituted or unsubstituted -C(=S)-OR4b, wherein R4b is as defined above, may be carried out by using respective alcohol such as methanol, ethanol, propanol, cyclohexanol and the like, in the absence or presence of a base such as sodiumhydride (NaH), potassiumhydride (KH) and the like. The reaction may be carried out in the presence of a solvent such as THF, toluene, DMF and the like. The reaction may be carried out at a temperature in the range of about 20 to about 130°C, preferably at reflux temperature of the solvent used. The duration of the reaction may be in the range of about 6 to about 24 h. Another embodiment of the present invention provides a process for the preparation of compound of formula (I), where R1 represents NHR4, wherein R4 represents substituted or unsubstituted groups selected from -C(=S)-NH2, -C(=S)-NH-(C1-C10)alkyl, -C(=S)-N-((Cr C10)alkyl)2, -C(=S)-NH-(C2-C10)alkenyl, C(=S)-NH-C(=O)-aryl, -C(=S)-NH-aralkyl, -C(-S)-NH-heteroaralkyl or -C(=S)-N(R'R"), wherein R1and R" groups together form a substituted or unsubstituted 5 or 6 membered cyclic structures containing nitrogen and optionally one or two additional hetero atoms selected from oxygen, nitrogen or sulfur; from a compound of formula (I) where R1 represents isothiocyanate group, where all symbols are as defined earlier. The compound of formula (I), where R1 represents NHR4, wherein R4 represents substituted or unsubstituted -C(=S)-NH2, may be prepared by passing ammonia gas into a solution of compound of formula (I) where R1 represents isothiocyanate group, in the presence of a solvent such as THF, toluene, and the like. The reaction may be carried out at a temperature in the range of about -10 to about 40 °C, preferably at about -10 °C. The duration of the reaction may be in the range from about 20 min to about 4 h, preferably about 30 min. The compound of formula (I), where R1 represents NHR4, wherein R4represents substituted or unsubstituted groups selected from -C(=S)-NH-(C1-C10)alkyl, -C(=S)-N-((C1-C10)alkyl)2, -C(=S)-NH-(C2-C10)alkenyl, C(=S)-NH-C(=O)-aryl, -C(=S)-NH.aralkyl, -C(=S)-NH-heteroaralkyl or -C(=S)-N(R'R"), wherein R1and R" groups together form a substituted or unsubstituted 5 or 6 membered cyclic structures containing nitrogen and optionally one or two additional hetero atoms selected from oxygen, nitrogen or sulfur, may be carried out by treating a compound of formula (I) where R1 represents isothiocyanate group with appropriate amine such as methylamine, ethylamine, diemthvlamine, diethvlamine, benzvlamine, aniline. proline, morpholine, thiomorpholine, pyridiylmethylamine and the like, in the presence of a solvent such as THF, DMF, toluene, and the like. The reaction may be carried out at a temperatxire in the fange of 20 about to about 140 °C, preferably at about 20 to about 100°C, The duration of the reaction may be in the range of about 0.5 to about 24 h, preferably about 0.5 to about 12 h. Yet another embodiment of the present invention provides a process for the preparation of compound of formula (I), where R1 represents NHR4, wherein R4represents substituted or unsubstituted -C(=S)-SR4c, wherein R4d represents (C1-C10)alkyl group, from compound of formula (I), where R1represents NHR4, wherein R'* represents hydrogen atom, where all other symbols are as defined earlier. The compound of fomula (I), where R1 represents NHR , wherein R4represents substituted or unsubstituted -C(=S)-SR4c wherein R44 is as defined above, may be prepared from compound of formula (I), where R1 represents NHR4, wherein R4 represents hydrogen atom, by using CS2 in the presence of a base such as EtsN, diisopropyl ethylamine, K2CO3, NaH, tertiary butylalcohol (t-BuOK) and the like. The reaction may be carried out in the presence of alkyl halide such as methyliodide, ethylbromide, propylbromide and the like. The solvent used in the reaction may be selected from ethanol, methanol, isopropanol, THF, diethylether, acetonitrile and the like, or mixtures thereof. The reaction may be carried out at a temperature in the range of about 20 to about 60 °C, preferably at about 20 to about 40 °C. The duration of the reaction may be in the range of about 6 to about 24 h. Another embodiment of the present invention provides a process for the preparation of compound of formula (I), where R1represents NHR4, wherein R4 represents substituted or unsubstituted -C(=S)-NH-R'4d, wherein R4d represents -C(=O)-aryl group, from compound of formula (I), where R1 represents NHR4, wherein R4 represents hydrogen atom, where all other symbols are as defined earlier. The compound of fomula (I), where R1 represents NHR4, wherein R4 represents substituted or unsubstituted -C(=S)-NH-R4c wherein R4d is as defined above, may be prepared from compound of formula (I), where R1represents NHR4, wherein R4represents hydrogen atom by using benzoylisothiocyanate. The solvent used in the reaction may be selected from acetone, ethanol, methanol, isopropanol, THF, diethylether, acetonitrile and the like. The temperature of the reaction may be maintained in the range of about 0 to about 80°C, preferably in the range of about 20 to about 60 °C. The duration of the reaction may be in the range of about 1 to about 20 h, preferably in the range of about 1 to about 10 h. Yet another embodiment of the present invention provides a process for the preparation of compound of formula (I), where R1 represents NHR4, wherein R4represents substituted or unsubstituted -C(=O)-heteroaryI, from a compound of formula (I), where R1 represents NHR4, wherein R4 represents hydrogen atom, where all other symbols are as defined earlier. The compound of fomula (I), where R1 represents NHR4, wherein R4represents substituted or unsubstituted -C(=O)-heteroaryl, may be prepared from compound of formula (I), where R1represents NHR4, wherein R4represents hydrogen atom by treating with corresponding heteroaroyl acid chloride and base such such as pyridine, triethylamine or diisopropylamine. The reaction may also be carried out by using corresponding heteroaryl acid and dicyclohexylcarbodiimide (DCC) in the presence of dimethylaminopyridine (DMAP). The solvent used in the reaction may be selected from acetonitrile, THF, methylcyanide, Et2O and the like. The temperature of the reaction may be maintained in the range of about -5 to about 100°C, preferably in the range of about 0 to about 80oC. The duration of the reaction may be in the range of about 1 to about 15 h, preferably in the range of about 2 to about 12 h. « Still another embodiment of the present invention provides a process for the preparation of compound of formula (I), where R1 represents NHR4 wherein R4 represents substituted or unsubstituted -C(=O)-R4c wherein R4c represents (C1-C10)alkyl, (C1-C10)alkoxy, (C2-C10)alkenyl, halo(C1-C10)alkyl, aryl, aryloxy, heteroaryl, (C2-C10)alkenyloxy, (C1-C10) alkylcarbonyl, arylcarbonyl, aryloxycarbonyl, (C1-C10)alkoxycarbonyl, (C1-C10) alkylthiocarbonyl or (C1-C10)arylthiocarbonyl; from a compound of formula (I), where R1 represents NHR4, wherein R4represents hydrogen atom, where all other symbols are as defined earlier. The compound of formula (I), where R1represents NHR1, wherein R4represents substituted or unsubstituted -C(=O)-R4c, wherein R4d is as defined above, may be prepared from compound of formula (I), where R1represents NHR4, wherein R4 represents hydrogen atom, by treating with appropriate acid halide such as acetyl chloride, propionyl chloride and the like; alkylchloroformate like methylchloroformate, ethylchloroformate and the like; aralkylchloroformate like benzylchloroformate and the like; or anhydride of the corresponding acid such as acetic anhydride. The reaction may be carried out in the presence of a solvent such as CH2CI2, CHCI3, toluene, THF and the like or mixtures thereof. The reaction may also be carried out in the presence of a base like Et3N, diisopropyl ethylamine, pyridine, K2CO3, NaH, t-BuOK and the like. The temperature of the reaction may be maintained in the range of about -20 to about 60 °C, preferably in the range of about 0 to about 40 °C. The duration of the reaction may be in the range of about 1 to about 12 h, preferably from about 1 to about 4 h. Yet another embodiment of the present invention provides a process for the preparation of compound of formula (I) where R1represents NHR wherein R4represents substituted or unsubstituted -C(=NH)-NH2, by reacting a compound of formula (I), where R1represents NHR4 wherein R4represents hydrogen atom, with di-tert-hntoxy carbonyl thiourea, where all other symbols are as defined earlier. The compound of formula (I) where R1 represents NHR4 where R4represents substituted or unsubstituted group selected from -C(=NH)-NH2, may be prepared by reacting the compound of formula (I), where R1represents NHR4 where R4 represents hydrogen atom, with di-tert-bntoxy carbonyl thiourea in two steps. In the first step, the reaction may be carried out in the presence of solvents such as DMF, acetone, THF, dichloromethane and the like. The base used in the reaction may be selected from triethylamine, diisopropylethylamine, pyridine and the like. The temperature of the reaction may be in the range of 0 to 120°C, preferably in the range of 0 to 90°C. The duration of the reaction may be in the range of 0.2 to 15 h, preferably in the range of 0.5 to 10 h. In the second step, the compound obtained in the first step may be reacted with trifluoroacetic acid in the presence of a solvent such as dichloromethane, chloroform, THF and the like. The temperature of the reaction may be in the range of about 0 to about 110 °C, preferably in the range of about 0 to about 90 °C, The duration of the reaction may be in the range of about 0.5 to about 60 h, preferably in the range of about 0.5 to about 54 h. Another embodiment of the present invention provides an alternative process for the preparation of compound of formula (I) where R1 represents NHR4 where R4represents substituted or unsubstituted group selected from -C(=NH)-NH2, by reacting a compound of formula (I), where R4 represents NHR4 wherein R4represents substituted or unsubstituted group selected from -S(O)2(C1-C10)alkyl or -S(O)2aryl group, with guanidine hydrochloride, where all other symbols are as defined earlier. The compound of formula (I) where R1represents NHR4 where R4 represents substituted or unsubstituted group selected from -C(=NH)-NH2, may be prepared by reacting the compound of formula (I), where R1 represents NHR4 wherein R4represents substituted or unsubstituted group selected from -S(O)2(C1-C10)alkyl or -S(O)2aryl group, with guanidine hydrochloride. The solvent used in the reaction may be seleceted form t-butyl alcohol. The base used in the reaction may be selected from NaH, KH, sodium hexamethyldisilazide (Na-HMDS) and the like. The temperature of the reaction may be in the range of about 0 °C to boiling temperature of the solvent used. The duration of the reaction may be in the range of about 1 to about 30 h, preferably in the range of about 1 to about 24 h. Still another embodiment of the present invention provides a process for the preparation of compound of formula (I) where R1 represents NHR4 where R4 represents substituted or unsubstituted group selected from -C(=NH)-(C1-C10)alkyI or -C(=NH)-aryI, which comprises: (i) reacting the compound of formula (I) where R1repersents NHR4, wherein R4 represents -C(=S)-NH2 and all other symbols are as defined earlier, with di R1rr-butoxy carbonyl ether ((B0C)20), to produce a compound of formula (I) where R1represents NHR4, wherein R4represents -C(=S)-NH2 group substituted with tert- butoxy carbonyl group and all symbols are as defined earlier and (ii) reacting the above compound of formula (I), with a compound of formula (Ik) R1-NH2 (Ik) where R7 represents substituted or unsubstituted (C1-C10)alkyl or aryl group, to produce a compound of formula (I) where R1 represents NHR4 where R4represents substituted or unsubstituted group selected from -C(=NH)-(C]-C10)alkyl or -C(=NH)-aryl group and all other symbols are as defined earlier. The conversion of the compound of formula (I) where R1represents NHR4, wherein R4represents -C(=S)-NH2, to a compound of formula (I), where R1 represents NHR4, wherein R represents -C(=S)-NH2 group substituted with tert-butoxy carbonyl group may be carried out by reacting with (BOC)2O, in the presence of solvent such as THF, diethylether and the like. The base^ used in the reaction may be selected from NaH, KH, sodium hexamethyldisilazane (Na-HMDS) and the like. The temperature of the reaction may be in the range of about 0 to boiling temperature of the solvent. The duration of the reaction may be in the range of about 0.5 to about 14 h, preferably in the range of about 0.5 to about 10 h. The conversion of the compound of formula (I), where R1 represents NHR4, wherein R represents -C(=S)-NH2 group substituted with tert-hntoxy carbonyl group, to a compound of formula (I) may be carried out by reacting with the compound of formula (Ik) in two steps. In the first step, the reaction may be carried out in the presence of a solvent such as DMF, THF, chloroform, dichloromethane and the like. The base used in the reaction may be selected from triethylamine, diisopropylethylamine, pyridine and the like. The temperature of the reaction may be in the range of about 0 to about 120°C, preferably in the range of about 0 to about 90°C. The duration of the reaction may be in the range of about 0.5 to about 24 h, preferably in the range of about 0.5 to about 20 h. In the second step, the compound obtained in the first step may be reacted with trifluoroacetic acid in the presence of a solvent such as dichloromethane, chloroform, THF and the like. The temperature of the reaction may be in the range of about 0 to about 110oC, preferably in the range of about 0 to about 90°C. The duration of the reaction may be in the range of about 0.5 to about 60 h, preferably in the range of about 0.5 to about 54 h. Yet another embodiment of the present invention provides a process for the preparation of a compound of formula (I) where R1 represents halogen, from compound of formula (I) where R1 represents hydroxy group, where all other symbols are as defined above. The compound of formula (I) where R1 represents halogen is prepared from compound of formula (I) where R1 represents hydroxy group may be carried out by treating with SOCI2, PCI5, PBr3, tetrahalomethane group such as carbontetrabromide (CBr4), carbontetrachloride (CCI4) and the like, in the presence of triphenylphonsphine (PPh3), trialkylphosphine (P(alkyl)3) and the like. The reaction may be carried out in the presence of a solvent such as dry dichloromethane, chloroform, tetrachloromethane, benzene, DMF, DMSO, THF and the like. The temperature of the reaction may be maintained in the range of about 0 to about 60 °C, preferably about 20 to about 40 °C. The duration of the reaction may be in the range of about 0.5 to about 24 h, preferably about 1 to about 13 h. Still another embodiment of the present invention provides a process for the preparation of a compound of formula (I) where R1represents 'SH', where all other symbols are as defined above, which comprises: (i) reacting the compound of formula (I) where R1 represents halogen atom, to produce a compound of formula (Im), where all other symbols are as defined earlier, with a base and thiolacetic acid, (ii) reacting the compound of formula (Im), to produce a compound of formula (I) where R1 represents 'SH' group and all other symbols are as defined earlier, with base. The compound of formula (Im) is prepared from compound of formula (I) where R1 represents halogen atom may be prepared by using thiolacetic acid in the presence of a base such as triethylamine, di-isopropylamine, di-isopropylethylamine, pyridine, piperidine, DMAP, DBU, lithium diisopropylamide (LDA), potassium bis-(trimethyl silyl)amide, BuLi, Na2CO3, K2CO3, NaOH, KOH, sodiummethoxide (NaOMe), sodiumethoxide (NaOEt), sodium iso propoxide (NaO-iPr), t-BuOK, NaH, KH and the like. The solvent used in the reaction may be seleceted from THF, benzene, dioxane and the like. The temperature of the reaction may be maintained in the range of about 20 °C to reflux temperature, preferably at reflux temperature. The duration of the reaction may be in the range of about 2 to about 24 h, preferably about 6 h. The compound of formula (I), where R1 represents 'SH' group may be prepared from a compound of formula (Im) by reacting with a base such as K2CO3, NaOH, KOH, BuLi and the like. The reaction may be carried out at a temperature in the range of about 20 oC to reflux temprature. The duration of the reaction may be in the range of about 1 to about 24 h. Still yet another embodiment of the present invention provides a process for the preparation of compound of formula (I), where R* represent NHR4 wherein R4represents substituted or unsubstituted -S(O)2(C1-C10)alkyl or -S(O)2aryl group, from a compound of formula (I) where R represents NHR where R represents hydrogen atom, (i) reacting the compound of formula (I), where R1 represents NHR4 where R4represents hydrogen atom and all other symbols are as defined in the description, to a compound of formula (I), where R1 represents NHR4, wherein R4 represents substituted or unsubstituted group selected from -S(O)2-(C1-C10)alkyl or -S(O)2-aryl group and all other symbols are as defined in the description, to a compound of formula (I). The conversion of compound of formula (I), where R1 represents NHR4 where R4represents hydrogen atom, to a compound of formula (I), where R1 represents NHR4, wherein R4 represents substituted or unsubstituted group selected from -S(O)2-(C1-C10)alkyl or -S(O)2-aryl group, may be carried out by treating with alkylsulfonylchloride or arylsulfonylchloride such as methanesulfonyl chloride, p-toluenesulfonyl chloride and the like. The solvent used may be selected from dichloromethane, tetrahydrofuran, acetonitrile, dimethylformamide, dimethylsulfoxide and the like. The temperature of the reaction may be in the range of about 0 to about 50°C, for duration of about 1 to about 6 h. Another embodiment of the present invention provides a novel intermediate of the formula (Ig), Yet another embodiment of the present invention provides a process for the preparation of novel intermediate of formula (Ig), which comprises: The compound of formula (la) is reacted with a compound of formula (lb), to obtain a compound of formula (Ic), when X represents halogen atom, by using a reagent such as BuLi and the like. The compound of formula (Ic), where X represents hydrogen atom is obtained by treating with CsF. The solvent used in the reaction may be selected from tetrahydrofuran (THF), hexamethylphosphoramide (HMPA), diethylether and the like. The temperature and duration of the reaction can be maintained in the range of about -78 to about 100 °C and about 30 min to about 1.5 h respectively. The compound of formula (Ic) is reacted with a compound of formula (Id), to obtain a compound of formula (le), by using a reagent such as methyllithium (MeLi), n-butyllithium (n-BuLi), secondary butyllithium (sec.BuLi), tertiary butyllithium (ter.BuLi) and the like. The solvent used in the reaction may be selected from THF, HMPA, diethyl ether, 1,4-dioxane and the like. The temperature and duration of the reaction can be maintained in the range of about -78 to about 50 °C and about 4 to about 10 h respectively. The compound of formula (le) is treated with any of the reagents selected from cone HCl, p-toluene sulfonic acid (p-TSA), mesyl chloride & triethylamine, 1,2-diazabicyclo[5,4,0]undec-7-ene (DBU), phosphorous oxychloride (POCI3), The solvent used in the reaction is selected from pyridine, dichloromethane, acetonitrile, toluene and the like, to obtain a compound of formula (If), where '....' represents a bond. The temperature and duration of the reaction can be maintained in the range of about 0 to about 150 °C and about 30 min to about 24 h respectively. The above obtained compound of formula (le) is converted to compound of formula (le), where '....' represents no bond, by treating with EtsSiH & BF3OEt2, EtsSiH & CF3COOH, TMSCl, Nal, Me2Sil2, BusSnH and the like, under the above reaction conditions. The compound of formula (If) is reacted with NaNO2, NaNs, t-Butyl nitrile and the like, to obtain a compound of formula (Ig), The temperature and duration of the reaction can be maintained in the range of about 0 to about 150 °C and about 30 min to about 24 h respectively. CH2NH2, -CH2N(Pthalimide), -CH2NH-C(=S)S-O(C1-C10)alkyl, -CH2NH-C(=O) (C,-C!o)alkyl. Still yet another embodiment of the present invention provides a process for the preparation of novel intermediate of formula (Iq), which is shown in the following Scheme-V: Scheme-V The compound of formula (Iq) may be prepared by reacting the compound of formula (Ig) with a compound of formula (Ir), in the presence of Cu(l)I. and a base such as triethylamine, ethyldiisopropylamine, l,4-diazabicyclo[2,2,2]octane (DABCO) and the like. The reaction may be carried out in the presence of a solvent such as dichloromethane, chloroform, tetrahydrofuran, dimethylformamide, dimethylsulfoxide, acetonitrile and the like. It is appreciated that in any of the above-mentioned reactions, any reactive group in the substrate molecule may be protected according to conventional chemical practice. Suitable protecting groups in any of the above mentioned reactions are tertiarybutyldimethylsilyl, methoxymethyl, triphenyl methyl, benzyloxycarbonyl, tetrahydropyran(THP) etc, to protect hydroxyl or phenolic hydroxy group; N-tert-butoxycarbonyl (N-Boc), N-benzyloxycarbonyl (N-Cbz), N-9-fluorenyl methoxy carbonyl (-N-FMOC), benzophenoneimine, propargyloxy carbonyl (POC) etc, for protection of amino or anilino group, acetal protection for aldehyde, ketal protection for ketone and the like. The methods of formation and removal of such protecting groups are those conventional methods appropriate to the molecule being protected. Regioisomers are isomers that differ by their functional groups. The regioisomers of compound of formula (I) may be prepared by modifying the reaction conditions, use of reagents like acid to base or base to acid or by reaction with free base hydrazine instead of its salt with diketone. The molar proportion also can change the regiosiomer formation. The stereoisomers including enantiomers and geometrical isomers (E and Z isomers or their mixtures in various ratios) may be prepared by using reactants in such a way to obtain a single isomeric form in the process wherever applicable or by conducting the reaction in the presence of reagents or catalysts in their single enantiomeric form. The single enantiomer, wherever application may be prepared by resolving the racemic mixture by conventional methods. The stereoisomers of the compounds forming part of this invention may be prepared by using reactants in their single enantiomeric form in the process wherever possible or by conducting the reaction in the presence of reagents or catalysts in their single enantiomer form or by resolving the mixture of stereoisomers by conventional methods. Some of the preferred methods include use of microbial resolution, resolving the diastereomeric salts formed with chiral acids such as mandelic acid, camphorsulfonic acid, tartaric acid, lactic acid, and the like wherever applicable or chiral bases such as brucine, cinchona alkaloids and their derivatives and the like. Commonly used methods are compiled by Jaques et al in "Enantiomers, Racemates and Resolution" (Wiley Interscience, 1981). Where appropriate the compounds of formula (I) may be resolved by treating with chiral amines, ammoacids, aminoalcohols derived from aminoacids; conventional reaction conditions may be employed to convert acid into an amide; the diastereomers may be separated either by fractional crystallization or chromatography and the stereoisomers of compound of formula (I) may be prepared by hydrolyzing the pure diastereomeric amide. A method of treating or preventing an infectious disorder in a subject is provided by administering an effective amount of oxazolidinone as disclosed herein to the subject, wherein the infectious disorder is characterized by the presence of microbial infection caused by pathogens such as Gram-positive, Gram-negative, aerobic and anerobic bacteria such as MRSA, Pseudomonas aeruginosa, Escherischia spp., Streptococci including Str. pneumoniae, Str. pyogenes, Enterococci as well as anaerobic organisms such as Bacteroides spp., Clostridia spp. species and Acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp. fastidious Gram negative organisms, H. influenzae, M. catarrhalis and several other bacteria resistant to fluoroquinolone, macrolide, Vancomycin, Aminoglycosides, Streptogramin, Lincosamides and p-Lactam resistant species. Such disorders include infections of the middle, internal and external ear including otitis media, infections of the cranial sinuses, eye infections, infections of the oral cavity, central nervous system infections, infections of teeth and gums,, infections of the mucosa, respiratory tract infections, genitourinary tract infections, gastro-intestinal infections, septicemia, bone and joint infections, skin and soft infections, bacterial endocarditis, bums, nosocomical infections, pre- and postsurgical infections, opportunistic infections in the immune compromised, intracellular infections such as Chlamydia and Mycoplasma. Pharmaceutically acceptable salts forming part of this invention include salts derived from inorganic bases such as Li, Na, K, Ca, Mg, Fe, Cu, Zn, Mn; salts of organic bases such as N,N'-diacetylethylenediamine, betaine, caffeine, 2-diethylaminoethanol, 2- dimethylaminoethanol, N-ethylmorpholine, N-ethylpiperidine, glucamine, glucosamine, hydrabamine, isopropylamine, methylglucamine, morpholine, piperazine, piperidine, procaine, purines, theobromine, triethylamine, trimethylamine, tripropyiamine, tromethamine, diethanolamine, meglumine, ethyl enediamine, N,N'-diphenylethylenediamine, N,N'- dibenzylethylenediamine, N-benzyl phenylethylamine, choline, choline hydroxide, dicyclohexylamine, metformin, benzylamine, phenylethylamine, dialkylamine, trialkylamine, thiamine, aminopyrimidine, aminopyridine, purine, spermidine, and the like; chiral bases like alkylphenylamine, glycinol, phenyl glycinol and the like, salts of natural amino acids such as glycine, alanine, valine, leucine, isoleucine, norleucine, tyrosine, cystine, cysteine, methionine, proline, hydroxy proline, histidine, ornithine, lysine, arginine, serine, threonine, phenylalanine; unnatural amino acids such as D-isomers or substituted amino acids; guanidine, substituted guanidine wherein the substituents are selected from nitro, amino, alkyl such as methyl, ethyl, propyl and the like; alkenyl such as ethenyl, propenyl, butenyl and the like; alkynyl such as ethynyl, propynyl and the like; ammonium or substituted ammonium salts and aluminum salts. Salts may include acid addition salts where appropriate which are, ) sulphates, nitrates, phosphates, perchlorates, borates, halides, acetates, tartrates, maleates, citrates, succinates, palmoates, methanesulphonates, benzoates, salicylates, hydroxynaphthoates, benzenesulfonates, ascorbates, glycerophosphates, ketoglutarates and the like. Pharmaceutically acceptable solvates may be hydrates or comprising other solvents of crystalHzation such as alcohols. The pharmaceutically acceptable salts are prepared by reacting the compounds of formula (I) wherever applicable with 1 to 4 equivalents of a base such as sodium hydroxide, sodium methoxide, sodium hydride, potassium t-butoxide, calcium hydroxide, magnesium hydroxide and the like, in the presence of a solvent like ether, THF, methanol, t-butanol, dioxane, isopropanol, ethanol etc. Mixture of solvents may be used. Organic bases like lysine, arginine, diethanolamine, choline, tromethamine, guanidine and their derivatives etc. may also be used. Alternatively, acid addition salts wherever applicable are prepared by treatment with acids such as hydrochloric acid, hydrobromic acid, nitric acid, sulfuric acid, phosphoric acid, p-toluenesulphonic acid, methanesulfonic acid, acetic acid, citric acid, maleic acid salicylic acid, hydroxynaphthoic acid, ascorbic acid, palmitic acid, succinic acid, benzoic acid, benzenesulfonic acid, tartaric acid and the like in the presence of a solvent like ethyl acetate, ether, alcohols, acetone, THF, dioxane etc. Mixture of solvent may also be used. The salts of amino acid groups and other groups may be prepared by reacting the compounds of formula (I) with the respective groups in the presence of a solvent like alcohols, ketones, ether etc. Mixture of solvents may be used. The prodrugs such as esters and amides of the compounds of formula (I) can be prepared by conventional methods. The metabolites, which are formed inside the body of the mammal, are formed by the reaction of various enzymes present in the body with the compounds of formula (I) Various polymorphs of a compound of general formula (I) forming part of this invention may be prepared by crystallization of compound of formula (I) under different conditions. For example, using different solvents commonly used or their mixtures for recrystallization; crystallizations at different temperatures; various modes of cooling, ranging from very fast to very slow cooling during crystallizations. Heating or melting the compound followed by gradual or fast cooling may also obtain polymorphs. The presence of polymorphs may be determined by solid probe nmr spectroscopy, IR spectroscopy, differential scanning calorimetry, powder X-ray diffraction or such other techniques. The present invention also provides pharmaceutical compositions, containing compounds of the general formula (I), as defined above, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceuticaily acceptable salts or their pharmaceuticaily acceptable solvates in combination with the usual pharmaceuticaily employed carriers, diluents and the like. The pharmaceutical compositions according to this invention can be used for the treatment of bacterial infections. They can also be used for the treatment of bacterial infections associated with multidrug resistance. The pharmaceutical compositions according to this invention can also be administered prophylatically for the prevention of bacterial infections in a patient at risk of developing a bacterial infection. Such patients include but are not limited to patients who are pre- or postsurgical, immunocompromised, or hospitalized and can be used for the treatment/prevention of bacterial infections associated with multidrug resistance. Pharmaceutically acceptable solvates of compound of formula (I) forming part of this invention may be prepared by conventional methods such as dissolving the compounds of formula (I) in the presence of a solvent such as water, methanol, ethanol etc., preferably water and recrystallizing by using different crystallization techniques. The regioisomers of compound of formula (I) may be prepared by modifying the reaction conditions, use of reagents like acid to base or base to acid or by reaction with free base hydrazine instead of its salt with diketone. The molar proportion also can change the regioisomer formation. The pharmaceutical compositions may be in the forms normally employed, such as tablets, capsules, powders, syrups, solutions, suspensions and the like, may contain flavorants, sweeteners etc. in suitable solid or liquid carriers or diluents, or in suitable sterile media to form injectable solutions or suspensions. Such compositions typically contain from 1 to 20 %, preferably 1 to 10 % by weight of active compound, the remainder of the composition being pharmaceutically acceptable carriers, diluents or solvents. Suitable pharmaceutically acceptable carriers include solid fillers or diluents and sterile aqueous or organic solutions. The active compounds will be present in such pharmaceutical compositions in the amounts sufficient to provide the desired dosage in the range as described above. Thus, for oral administration, the compounds can be combined with a suitable solid, liquid carrier or diluent to form capsules, tablets, powders, syrups, solutions, suspensions and the like. The pharmaceutical compositions, may, if desired, contain additional components such as flavorants, sweeteners, excipients and the like. For parenteral administration, the compounds can be combined with sterile aqueous or organic media to form injectable solutions or suspensions. For example, solutions in sesame or peanut oil, aqueous propylene glycol and the like can be used, as well as aqueous solutions of water-soluble pharmaceutically-acceptable acid addition salts or salts with base of the compounds. The injectable solutions prepared in this maimer can then be administered intravenously, intraperitoneally, subcutaneously, or intramuscularly, with intramuscular administration being preferred in humans. In addition to the compounds of formula (I) the pharmaceutical compositions of the present invention may also contain or be co-administered with one or more known drugs selected from other clinically useful antibacterial agents such as p-lactams. Aminoglycosides, Oxazolidinones, Fluoroquinolines, Streptogramins, Lincosamides, Macrolides or any other suitable antiinfective agent. These may include penicillins such as oxacillin or flucloxacillin and carbapenems such as meropenem or imiphenem to broaden the therapeutic effectiveness against, for example, methicillin-resistant staphylococci. Compounds of the formula (I) of the present invention may also contain or be co-admistered with bactericidal/permeability-increasing protein product (BPI) or efflux pump inhibitors to improve activity against gram negative bacteria and bacteria resistant to antimicrobial agents. The compounds of the formula (I) as defined above are clinically administered to mammals, including human beings, via either oral or parenteral routes. Administration by the oral route is preferred, being more convenient and avoiding the possible pain and irritation of injection. However, in circumstances where the patient cannot swallow the medication, or absorption following oral administration is impaired, as by disease or other abnormality, it is essential that the drug be administered parenterally. By either route, the dosage is in the range of about 0.5 mg/kg to about 50 mg / kg body weight of the subject per day administered singly or as a divided dose. However, the optimum dosage whether for prevention or treatment for the individual subject being treated will be determined by the person responsible for treatment, generally smaller doses being administered initially and thereafter increments made to determine the most suitable dosage. It is also to be understood that the terminology used herein is for the purpose of describing particular embodiments only, and is not intended to limit the scope of the present invention. The manner in which the compounds of this invention can be prepared is illustrated in the following examples, which demonstrate the preparation of typical species of the invention. In these examples, the identities of compounds, intermediates and final, were confirmed by infrared, nuclear magnetic spectral analyses as necessary. The examples are for the purpose of illustration only and should not be regarded as limiting the invention in any way. «-Butyllithium (124 mL, 1.6 M in hexane, 198.4 mmol) was added drop wise to a solution of 3-fluoroaniline (10 g, 90.1 mmol) in THF (200 mL) at -78 °C under nitrogen atmosphere and stirred for 20 min. A solution of l,2-bis(chlorodimethylsilyl)ethane (21.3 g, 99.1 mmol) in dry THF (200 mL) was added and stirred at the same temperature for 45 min. The reaction mixture was brought to room temperature and then quenched with water (120 mL). The mixture was extracted with diethyl ether. The combined organic layers were washed with brine and dried over Na2SO4. The solvent was removed under vacuum to obtain l-(3-fluorophenyl)-2,2,5,5-tetramethyl-[l,2,5]azadisilolidine (21.2 g) and this crude product was used in the next step without purification. To a solution of l-(3-fluorophenyl)-2,2,5,5-tetramethyl-[l,2,5]azadisilolidine (15 g, 59.3 mmol) in THF (130 mL) was slowly added 55 mL (71.1 mmol) of sec-BuLi (1.3 M in cyclohexane/hexane) at -78 oC under nitrogen and stirred the reaction at the same temperature for 4 h. A solution of tetrahydro-4-pyranone (7.11 g, 71.1 mmol) in dry THF (10 mL) was added to the reaction mixture and allowed to rise to room temperature. The reaction mixture was quenched slowly by the addition of water (150 mL) at 0 °C and was concentrated under vacuum. The resulting residue was acidified with cone. HCl and the acidic solution was extracted with diethyl ether (3 x 500 mL). The aqueous layer was basified with aqueous NaOH solution and extracted with diethyl ether (500 mL). The organic layer was washed with brine, dried over sodium sulfate and evaporated under vacuum. The resulting residue was refluxed with cone. HCl (40 mL) for 3 h and then allowed to cool to room temperature. The reaction mixture was basified with aqueous NH3 (30%) and was extracted with dichloromethane. The solvent was evaporated and the required product (3 g, 26%) was separated as a light brown solid by silica gel column chromatography (ethyl acetate / hexane; 3:17). added to an ice cooled solution of 4-(3,6-dihydro-2i/-pyran-4-yI)-3-fluorophenylanune (4 g, 20.7 mmol) obtained in preparation 1, in 6N HCl (18 mL) and stirred for 0.5 h. Then a saturated solution of sodium azide (2.69 g, 41.4 mmol) and sodium acetate (33.98 g, 414 mmol) in water (100 mL) was added slowly. The reaction mixture was stirred for another 0.5 h, diluted with water and extracted with ethyl acetate (2 x 100 mL). The organic layer was washed with water followed by brine and dried over sodium sulfate. Evaporation of volatiles and purification of the residue by flash chromatography (ethyl acetate/ hexahe; 1:9) yielded the title compound as a yellow solid (3.1 g, 68%). n-Butyllithium (55 mL, 1.6 M in hexane, 7.18 mmol) was added drop wise to a solution of 3,5-difluoroaniline (5 g, 38.76 mmol) in THF (78 mL) at -78°C under nitrogen atmosphere and stirred for 20 min. A solution of l,2-bis(chlorodimethylsilyl)ethane (8.33 g, 38.76 mmol) in THF (78 mL) was added to the reaction mixture and stirred for 45 min and then it was brought to room temperature. The reaction mixture was quenched with water (115 mL) and extracted with diethyl ether. The combined organic layers were washed with water and brine and dried over Na2SO4. The solvent was removed under vacuum to obtain l-(3,5-difluorophenyl)-2,2,5,5-tetramethyl-[l,2,5]azadisilolidine (10.12 g) and this crude product was used in the next step without purification. To a solution of l-(3,5-difluorophenyl)-2,2,5,5-tetramethyl-[l,2,5]azadisilolidine (10.12 g, 37.3 mmol) in THF (60 mL) was slowly added 27 mL (42.96 mmol) of/i-BuLi (1.6 M in hexane) at -78 °C under nitrogen and stirred for 4 h. A solution of tetrahydro-4-pyranone (7.11 g, 71.1 mmol) in dry THF (10 mL) was added to the above mixture and warmed to room temperature. The reaction mixture was stirred for 18 h, then quenched with 100 mL of water and concentrated under vacuum. The resulting residue was acidified with cone. HCl and the acidic solution was extracted with diethyl ether (150 mL). The aqueous layer was basified with 40% aqueous NaOH solution at 0 °C and extracted with diethyl ether. The organic layer was washed with brine, dried over sodium sulfate and evaporated on rotavapor. The resulting residue was refluxed with cone. HCl (40 mL) for 3 h and then allowed to cool to room temperature. The reaction mixture was basified with aqueous NH3 (30%) and was extracted with dichloromethane. The solvent was evaporated on rotavapor and the residue was purified through silica gel column (ethyl acetate / hexane; 3:17) to furnish the required product (2.2 g, 27%) as a pale brown solid. A saturated solution of sodium nitrite (590 mg, 8.55 mmol) in water (5 mL) was slowly added to a solution of 4-(3,6-dihydro-2H-pyran-4-yl)-3,5-difluorophenylamine (900 mg, 4.26 mmol) in HCl (6N, 16 mL), obtained in preparation-3, cooled to 0 °C, and stirred for 0.5 h. Then a saturated solution of sodium azide (550 mg, 8.54 mmol) and sodium acetate (7 g, 85.4 mmol) in water (100 mL) was added slowly at the same temperature. The reaction mixture was stirred for another 0.5 h and then diluted with ethyl acetate (250 mL). The organic layer was washed with water followed by brine and dried over Na2SO4. The solvent was evaporated and the residue was purified by flash chromatography (ethyl acetate/ hexane; 1:9) to get the title compound as a pale yellow solid (560 mg, 58%). n-Butyllithium (62 mL, 1.6 M in hexane, 99.2 mmol) was added drop wise to a solution of 3-fluoroaniline (5 g, 45 mmol) in THF (100 mL) at -78oC under nitrogen atmosphere Then a solution of l,2-bis(chlorodimethylsilyl)ethane (10.65 g, 49.53 mmol) in THF (100 mL) was added drop wise. The reaction mixture was stirred at the same temperature for 0.5 h and then it was brought to room temperature. The reaction mixture was quenched with water (135 mL), extracted with diethyl ether and washed with brine. The solvent was removed under vacuum to obtain l-(3-fluorophenyl)-2,2,5,5-tetramethyl-[l,2,5]azadisilolidine (11.8 g) and this crude product was used in the next step without purification. To a solution of l-(3-fluorophenyl)-2,2,5,5-tetramethyl-[l,2,5]azadisilolidine (11.8 g, 46.6 mmol) in THF (350 mL) was slowly added 43 mL of jec-BuLi (55.9 mmol, 1.6 M in hexane) at -78 °C and stirred for 4 h. A solution of tetrahydro-4-thiopyranone (6 g, 51.75 mmol) in THF (50 mL) was added to the reaction mixture at -78 "^C. The reaction mixture was slowly brought to room temperature and was stirred for further 18 h. It was then quenched with water (60 mL), concentrated under vacuum to remove most of the THF and the residue was acidified with cone. HCl. The acidic solution was extracted with diethyl ether. The aqueous layer was basified with 40% aqueous NaOH solution and extracted with diethyl ether (300 mL). The organic layer was washed with brine, dried over sodium sulfate and evaporated under vacuimi. The resulting residue was refluxed with cone. HCl (70 mL) for 3.5 h and then allowed to cool to room temperature. The reaction mixture was basified with aqueous NH3 (30%) and was extracted with dichloromethane. The solvent was evaporated on rotavapor and the required product (5,1 g, 54%) was separated as a pale brown solid by silica gel column chromatography (ethyl acetate / petroleum ether; 3:17). 1H NMR (CDCI3 + CD3OD): 5 6.99 (t, J = 8.8 Hz, IH), 6.42-6.39 (m, 2H), 5.95-5.87 (m, IH), 3.36-3.28 (m, 2H), 3.18-3.08 (m, 2H), 2.85 (t, J = 5.6 Hz, 2H), 2.68-2.56 (m, 2H); CI-MS(m/e):210(M^+l); IR (neat): 3360, 2916, 1630, 1510, 1444, 1164, 965 cm-1 Preparation-6 4-(4-Azido-2-fluoro-phenyl)-3,6-dihydro-2fl'-thiopyran: A saturated'aqueous solution of sodium nitrite (Ig, 14.6 mmol) was slowly added to an ice cooled solution of 4-(3,6-dihydro-2H-thiopyran-4-yl)-3-fluorophenylamine (1.52 g, 7.3 mmol), obtained in preparation-5, in 6 N HCl (16 mL), and stirred for 0.5 h. Then a solution of sodium azide (945 mg, 14.6 mmol) and sodium acetate (12 g, 146 mmol) in water (50 mL) was added at the same temperature and stirred for another 0.5 h. Then diluted with ethyl acetate (250 mL). The organic layer was washed with water followed by brine and dried over sodium sulfate. Evaporation of solvent and purification of the resulting residue by flash chromatography (ethyl acetate/ hexane; 3:17) yielded the desired compound (752 mg, 43%) as a brown oily material. n-Butyllithium (55 mL, L6 M in hexane, 87.18 mmol) was added drop wise to a solution of 3,5-difluoroaniline (5 g, 38.75 mmol) in THF (78 mL) at -78 °C under nitrogen atmosphere and stirred for 20 min., a solution of l,2-bis(chlorodimethylsilyl)ethane (8.5 g, 39.53 mmol) in THF (78 mL) was added drop wise. The reaction mixture was stirred at the same temperature for 0.5 h and then allowed to warm to room temperature. The reaction mixture was quenched with water (100 mL), extracted with diethyl ether and then the organic layer was washed with brine. The solvent was removed under vacuum to obtain l-(3,5-difluorophenyl)-2,2,5,5-tetramethyl-[l,2,5] azadisilolidine (10.7 g) and this crude product was used in the next step without purification. To a solution of l-(3,5-difluorophenyl)-2,2,5,5-tetramethyl-[ 1,2,5] azadisilolidine (10,7 g, 39.4 mmol)) in THF (80 mL) was slowly added 28.4 mL of n-BuLi (45.3 mmol,L6 M in hexane) at -78 °C under nitrogen and stirred the same for 4 h. Then a solution of tetrahydro-4-thiopyranone (5.26 g, 45.3 nmiol) in THF (30 mL) was added to the reaction mixture and slowly brought to room temperature and stirred for further 18 h. The Reaction mixture was quenched with water (50 mL), concentrated under vacuum and the resulting residue was acidified with cone. HCl. The acidic solution was extracted with diethyl ether. The aqueous layer was basified with 40% aqueous NaOH solution and extracted with diethyl ether (3 x 150 mL). The organic layer was washed with brine, dried over sodium sulfate and evaporated under vacuum. The resulting residue was refluxed with cone. HCl (60 mL) for 3.5 h and then allowed to cool to room temperature. The reaction mixture was basified with aqueous NH3 (30%) and was extracted with dichloromethane. The solvent was evaporated on a rotavapor and the crude product was column chromatographed over silica gel (ethyl acetate / petroleum ether; 3:17) to get the desired compound (3.8 g, 43%)) as a pale brown solid. A saturated solution of sodium nitrite (79 mg, 1.14 mmol) in water (3 mL) was slowly added to an ice cooled solution of 4-(3,6-dihydro-2H-thiopyran-4-yl)-3,5-difluorophenylamine, obtained in preparation-7 (130 mg, 0.57 mmol), in 6N HCl (8 mL), and stirred for 0.5 h. Then a solution of sodium azide (75 mg, 1.15 mmol) and sodium acetate (950 mg, 11.58 mmol) in water (15 mL) were added respectively at the same temperature. The reaction mixture was stirred for additional 0.5 h and then diluted with ethyl acetate (100 mL). The organic layer was washed with water followed by brine and dried over sodium sulfate. Evaporation of volatiles and purification of the resulting residue by flash chromatography (ethyl acetate/ hexane; 3:17) yielded the title compound as a pale orange solid (80 mg, 56%). To a solution of 4-(4-azido-2-fluoro-phenyl)-3,6-dihydro-2H-pyran (3 g, 13.7 mmol), obtained in preparation-2, and N, N -diisopropylethylamine base (4.78 mL, 27.4 mmol) in acetonitrile (100 mL) was added 2-prop-2-ynyl-isoindole-l,3- Hydrazine hydrate (3.1 mL) was added to a solution of 2-{l-[4-(3,6-dihydro-2H-pyran-4-yl)-3-fluoro-phenyl]-lH-[l,2,3]triazol-4-ylmethyl}-isoindole-l,3-dione (2.9 g, 7.18 mmol), obtained in example-1, in methanol (15 mL) and refluxed for 2 h followed by stirring at room temperature for 10 h. The reaction mixture was filtered and the filtrate was concentrated under vacuum. The residue was purified by flash chromatography (ethyl acetate/ hexane; 1:9) to afford the title compound as a white solid (800 mg, 41%). 1H NMR (DMS0-d6): 5 9.28-8.78 (m, 2H), 8.67 (s, IH), 7.93-7.63 (m, 2H), 7.58 (t, 7 = 8.1 Hz, IH), 6.30-6.12 (m, IH), 4.52-3.20 (m, 6H), 2.60-2.39 (m, 2H). MS (m/e): 275 (NT+I), 230, 217. IR(KBr): 3297, 1665, 1517, 1436, 1375, 1233, 1044 cm-1 Example-3 Triethylamine (0.08 mL, 0.73 mmol) was added to a solution of C-{l-[4-(3,6-dihydro-2H^-py^an-4-yl)-3-fluoro-phenyl]-li/-[l,2,3]triazol-4-yl}methylamine (100 mg, 0.365 mmol), obtained in example-2, in dichloromethane (5 mL), cooled to 0 "^C, followed by the addition of acetyl chloride (0.028 mL, 0.4 mmol) and stirred at room temperature for 3 h. The reaction mixture was concentrated on rotavapor and the residue was purified by column chromatography over silica gel (2% methanol in chloroform) to get the required compound (62 mg, 54%) as a white powder, mp 186-188 °C. To a solution of C- {l-[4-(3,6-dihydro-2H-pyran-4-yl)-3-fluoro-phenyl]-lH-[l,2,3]triazol-4-yl}methylamine (100 mg, 0.365 mmol), obtained in example-2, in THF (5 mL) was added triethylamine (0.103 mL, 0.73 mmol) followed by the addition of ethyl dithioacetate (0.05 ml, 0.44 mmol) and stirred at room temperature for 16 h. The reaction mixture was concentrated and the resulting residue was purified by column chromatography using 2% methanol in chloroform as eluent. The desired product was obtained as a creamy white solid (62 mg, 51%), mp 159-16rC. 1H NMR (DMS0-d6): 5 10.60-10.40 (m, IH), 8.82 (s, IH), 7.92-7.50 (m, 2H), 7.60 (t, J= 8.3 Hz, IH), 6.27-6.12 (m, IH), 4.84 (d, J= 4.8 Hz, 2H), 4.32-4.18 (m, 2H), 3.83 (t, J = 5.4 Hz, 2H), 2.60-2.30 (m, 5H). MS (m/e): 333 (M^+1), 304, 230, IR(KBr): 3243, 3055, 2926, 1579, 1460, 1406, 1362, 1231 cm-1 Example-5 To a solution of C-{l-[4-(3,6-dihydro-2H-pyran-4-yl)-3-fluoro-phenyl]-li/-[l,2,3]triazol-4-yl}methylamine (100 mg, 0.365 mmol), obtained in exampIe-2, in dichloromethane (10 mL) was added a solution of sodium bicarbonate (77 mg, 0.92 mmol) in water (3 mL) followed by cooling in ice bath. Thiophosgene (0.034 mL, 0.44 mmol) was added to the mixture at 0 °C and stirred at the same temperature for 0.5 h. The reaction mixture was diluted with dichloromethane (50 mL), washed with water, brine and dried over sodium sulfate. The solvent was evaporated and the residue was refluxed with methanol (15 mL) for 16 h. Removal of methanol and purification of the residue by column chromatography (ethyl acetate/hexane; 3:10) yielded the required compound (65 mg, 51%) as a white powder, mp 116-120 °C. 'H NMR (DMSO-d6): 5 9.79-9.60 (m, IH), 8.76 and 8.70 (two s, IH, rotamers in a ratio of 4:1), 8.01-7.63 (m, 2H), 7.59 (t, J= 8.6 Hz, IH), 6.30-6.13 (m, IH), 4.73 and 4.45 (two d, J= 5.4 Hz, 2H, rotamers in a ratio of 4:1), 4.37-4.14 (m, 2H), 4.00-3.68 (m, 5H), 2.69-2.30 (m, 2H). MS (m/e): 349 (Nf+1), 317, 230. IR(KBr, film): 3438, 3214, 2925, 1619,1512, 1458, 1365, 1218 cm"^ Example-6 {l-(4-(3,6-Dihydro-2iy-pyran-4-yl)-3-fluoro-phenyi]-l/r-[l,2,3]triazol-4-ylmethyl}- carbamic acid methyl ester: To a solution of C- {1 - [4-(3,6-dihydro-2H-pyran-4-yl)-3 -fluoro-phenyl] -1 H-[l,2,3]triazol-4-yl}-methylamine (90 mg, 0.33 mmol), obtained in example-2, in dichloromethane (5 mL), cooled to 0 °C, was added N,N-diisopropylethylamine (0.126 mL, 0.72 mmol) followed by the addition of methyl chloroformate (0.031 mL, 0.39 mmol) and stirred at the same temperature for 2 h. And the organic layer was washed with water followed by brine and dried over sodium sulfate. The solvent was evaporated and the residue was purified by column chromatography over silica gel (methanol/ chloroform; 1:24) to afford the required product (50 mg, 46%) as a creamy white solid, mp 140-144 °C. 'H NMR (DMSO-d^): 5 8.70 (s, IH), 7.97-7.66 (m, 2H), 7.58 (t, J= 8.3 Hz, IH), 6.30-6.16 (m, IH), 4.31 (d, y = 5.9 Hz, 2H), 4.25-4.18 (m, 2H), 3.83 (t, 7 = 5.1 Hz, 2H), 3.56 (s, 3H), 2.60-2.32 (m, 2H). MS(m/e):333(M++l). IR(KBr): 3297, 2924, 1688, 1535, 1463, 1262, 1045 cm-'.1 Example-? 2-{l-[4-(3,6-Dihydro-2H-pyran-4.yl)-3,5-difluoro.phenyl]-ljy-[l,2,3]triazol.4-ylmethyl}-l,3-isoindole-l,3-dione: To a solution of 4-(4-azido-2,6-difluoro-phenyl)-3,6-dihydro-2H-pyran (545 mg, 2.30 mmol), obtained in preparation 4, and N,N -diisipropylethylamine (0.80 mL, 4.59 mmol) in acetonitrile (20 mL) was added 2-prop-2-ynyl-isoindole-l,3-dione (642 mg, 3.47 mmol) followed by the addition of cuprous iodide (655 mg, 3.45 mmol) and stirred at room temperature for 2 h. The reaction mixture was filtered through a celite pad. The filtrate was concentrated under vacuum and the residue was purified by chromatography over silica gel (3% methanol in chloroform) to obtain the required compound (350 mg, 39%) as a pale yellow solid 1H NMR (CDCI3): 5 8.94 (s, IH), 8.08-7.73 (m, 6H), 6.12-6.04 (m, IH), 4.99 (s, 2H), 4.35- 4.22 (m, 2H), 3.88 (t, J= 5.4 Hz, 2H), 3.55-3.20 (m, 2H). MS (m/e): 423 (M++1), 173, 131. IR(KBr): 3442,2925, 1716, 1634, 1395, 1280, 1094 cm-1, £xample-8 C-{l-[4-(3,6-Dihydro-2H-pyran-4-yl)-3,5-difluoro-phenyl]-lH-[l,2,3]triazol-4-yl}- methylamine: To a solution of 2-{l-[4-(3,6-dihydro-2H-pyran-4-yl)-3,5-difluoro-phenyl]-lH-[l,2,3]tria2ol-4-ylmethyl}-l,3-isoindole-l,3-dione (325 mg, 0.768 mmol), obtained in example-7, in methanol (10 mL) was added hydrazine hydrate (0.41 mL) and refluxed for 2 h followed by stirring at room temperature for 10 h. The reaction mixture was filtered and the filtrate was concentrated under vacuum. The product was purified by flash chromatography on silica (5% methanol in chloroform) to afford the desired product (100 mg, 47%). H NMR (DMS0-d6): 5 8.67 (s, IH), 7.75 (d, 7 = 8.3 Hz, 2H), 6.05-5.93 (m, IH), 4.30-4.12 (m, 2H), 3.92-3.72 (m, 4H), 2.63-2.38 (m, 2H). MS (m/e): 293 (M^+1), 236, 163. IR(KBr): 3368, 3127, 2924, 2850, 1631, 1592, 1513, 1448, 1227, 1126, 1025 cm-1 ExampIe-9 n--{l-[4-(3,6-Dihydr(2H-pyran-4.yl)-3,5.difluoro-phenyl]-l/r-[l,2,3]triazol-4-ylmethyl}-thioacetamide: ■ Triethylamine (0.053 mL, 0.38 mmol) was added to a solution of C-{l-[4-(3,6-dihydro-2H-pyran-4-yl)-3,5-difluoro-phenyl]-lH-[l,23]triazol-4-yl}-methylainine (50 mg, 0.17 mmol), obtained in example-8, in THF (5 mL) followed by the addition of ethyl dithioacetate (0.03 ml, 0.26 mmol) and stirred at room temperature for 16 h. The reaction mixture was diluted with ethyl acetate (50 mL), washed with water followed by brine and dried over sodium sulfate. Solvent was evaporated and the residue was purified by column chromatography using 4% methanol in chloroform as eluent. Relevant fractions were combined and evaporated to obtain the desired product as a white powder (28 mg, 47%), mp 138 °C 1H NMR (CDCI3): 5 8.28-8.21 (m, IH), 8.14 (s, IH), 7.35 (d, 7 = 7.8 Hz, 2H), 5.98-5.92 (m, IH), 5.02 (d, 7 = 5.7 Hz, 2H), 4.38-4.31 (m, 2H), 3.95 (t, 7- 5.4 Hz, 2H), 2.61 (s, 3H), 2.48-2.40 (m, 2H). MS (m/e): 351 (M^+1), 335, 323, 252. IR(KBr): 3221,3041,2929, 1631, 1510, 1452, 1386, 1028 cm-1 Example-10 {l-[4-(3,6-Dihydro-2iy-pyran-4.yl)-3,5-difluoro-phenyl]-liy-[l,2,3]triazoI-4-ylmethyl}-thiocarbamic acid O-methyl ester: To a solution of C- {1 -[4-(3,6-dihydro-2H-pyran-4-yl)-3,5-difluoro-phenyl]-1H-[l,2,3]triazol-4-yl}methylamine (50 mg, 0.17 mmol), obtained in example-8, in dichloromethane (4 mL) was added a saturated solution of sodium bicarbonate (35 mg, 0.42 mmol) in water (3 mL) followed by cooling in ice bath. Thiophosgene (0.016 mL, 0.21 mmol) was added to the above mixture at 0 °C and stirred at the same temperature for 0.5 h. The reaction mixture was diluted with dichloromethane (50 mL), and the organic layer with water followed by brine and dried over sodium sulfate. Evaporation of volatiles left a residue, which was refluxed with methanol (5 mL) for 16 h. Methanol was removed under vacuum and the residue was purified by column chromatography over silica gel (methanol/ chloroform; 1:25) to get the title compound as a pale pink solid (41 mg, 72%), mp 132 °C. 1H NMR (CDCI3): 5 8.12 and 7.89 (two s, IH, rotamers in a ratio of 4:1), 7.35 (d, J= 7.3 Hz, 2H), 6.98-6.91 (m, IH), 5.98-5.93 (m, IH), 4.92 and 4.65 (d, J= 6.3 Hz, 2H, rotamers in ratio of 4:1), 4.39-4.32 (m, 2H), 4.10 and 4.00 (two s, 3H, rotamers in a ratio of 1:4), 3.95 (t. 7 = 5.4 Hz, 2H), 2.48-2.41 (m, 2H). MS (m/e): 367 (M"+l), 335, 319, 278. IR(KBr): 3237,3126, 1632, 1586, 1448, 1199 cm-1. ExampIe-11 2-{l-[4-(3,6-Dihydro-2iy-thiopyran-4-yI)-3-fluoro-phenyl]-lJy-[l,2,3]triazol-4-ylmethyl}- isoindole-l,3-dione: To a solution of 4-(4-azido-2-fluoro-phenyl)-3,6-dihydro-2H-thiopyran (630 mg, 2.68 mmol), obtained in preaparation-6, and n,n-diisopropylethylamine (0.936 mL, 5.36 mmol) in acetonitrile (10 mL) was added 2-prop-2-ynyl-isoindole-l,3-dione (691 mg, 3.74 mmol) followed by the addition of cuprous iodide (561 mg, 2.95 mmol) and stirred at room temperature for 1 h. The reaction mixture was filtered through a celite pad and washed thoroughly with MeOH. Concentration of the filtrate under vacuum and purification of the resulting residue by flash chromatography (ethyl acetate/ hexane; 4:6) afforded the title compound as a white solid (550 mg, 49%). 1H NMR (CDCI3): 5 8.02 (s, IH), 7.89-7.86 (m, 2H), 7.75-7.71 (m, 2H), 7.49-7.26 (m, 3H), 6.08-6.02 (m, IH), 5.08 (s, 2H), 3.40-3.25 (m, 2H), 2.87 (t, 7 = 5.6 Hz, 2H), 2.69-2.60 (m, 2H). MS (m/e): 421 (M++1), 389, 276, 248. IR(KBr): 3458, 2921, 1767, 1617, 1512, 1395, 1236, 1045 cm' Example-12 C-{l-[4-(3,6-Dihydro-2H-thiopyran-4.yl)-3-fluoro-phenyl]-lh-[l,2,3]triazol-4-yl}-methylamine: To a solution of 2- {1 -[4-(3,6-dihydro-2H'-thiopyran-4-yl)-3-fluoro-phenyl]-1H-[l,2,3]triazol-4-ylmethyl}-isoindole-l,3-dione (520 mg, 1.24 mmol) in methanol (10 mL), obtained in example-11, was added hydrazine hydrate (0.53 mL) and refluxed for 2 h followed by stirring at room temperature for 10 h. The reaction mixture was filtered and the filtrate was concentrated under vacuum. The residue was purified by flash chromatography (methanol/ chloroform; 1:9) to obtain the desired compound as a creamy white solid (205 mg, 57%). 1H NMR (DMS0-d6): 6 8.67 (s, IH), 7.95-7.62 (m, 2H), 7.62-7.29 (m, IH), 6.20-6.03 (m, IH), 4.10-3.78 (m, 2H), 3.78-3.09 (m, 2H), 2.84 (t, J= 5.5 Hz, 2H), 2.70-2.38 (m, 2H). MS (m/e): 291 (M++1), 246, 233. IR(KBr): 3442, 2929, 1740, 1661, 1575, 1494, 1360, 1231, 1015 cm-1 Example-13 A^-{l-[4-(3,6-Dihydro-2Jy-thiopyran-4-yl)-3-fluoro-phenyl]-1H-[l,2,3]triazol-4-ylmeth thioacetamide: Triethylamine (0.077 mL, 0.55 mmol) was added to a solution of C-{l-[4-(3,6-dihydro-2i^-thiopyran-4-yl)-3-fluoro-phenyl]-lH-[l,2,3]triazol-4-yl}-methylamine (80 mg, ' 0.276 mmol), obtained in ezample-12, in THF (5 mL) followed by the addition of ethyl dithioacetate (0.049 mL, 0.43 mmol) and stirred at ambient temperature for 16 h. The reaction mixture was concentrated under vacuum and the residue was purified by a silica gel column (1% methanol in chloroform) to give the desired product as a white solid (55 mg, 57%), Mp 107-110 °C. 'H NMR (CDCI3): 5 8.19-8.02 (m, 2H), 7.56-7.18 (m, 3H), 6.17-6.05 (m, IH), 5.02 (d, J= 5.3 Hz, 2H), 3.40-3.30 (m, 2H), 2.88 (t, J= 5.6 Hz, 2H), 2.80-2.50 (m, 2H), 260 (s, 3H). MS (m/e): 349 (M++1), 206, 149, 126. IR(KBr): 3496, 3194, 2925, 1621, 1566, 1458, 1366, 1234, 1055 cm-1. Example-14 2-{l-[3-Fluoro-4-(l-oxo-l,2,3,6-tetrahydro-llambda4-thiopyran-4-yl)-phenyl]-liy-[l,2,3]triazol-4ylmethyl}-isoin(lole-l,3-dione: Sodium periodate (915 mg, 4.28 mmol) in water (10 mL) was added to an ice cooled solution of 2-{l-[4-(3,6-dihydro-2H-pyran-4-yl).3-fluoro-phenyl]-lH-[l,2,3]triazol-4-ylmethyl}-isoindole-l,3-dione (400 mg, 0.95 mmol), obtained in example-1, in methanol (12 mL) and ethyl acetate (12 mL) and stirred for 1 h. The reaction mixture was brought to room temperature and stirred for 16 h. The reaction mixture was diluted with MeOH/CHCl} (1:19), filtered and the filtrate was concentrated under vacuum. The residue obtained was dissolved in chloroform, washed with saturated solution of Na2SO3 and NaHCO3 respectively and dried over sodium sulfate. The solvent was evaporated and the residue was purified by column chromatography over silica gel to afford the desired product (55 mg, 33%) as a white solid. 'H NMR (CDCI3): 5 8.04 (s, IH), 7.87-7.78 (m, 2H), 7.78-7.68 (m, 2H), 7.68-7.35 (m, 3H), 5.86-5.82 (m, IH), 5.08 (s, 2H), 3.69-3.43 (m, 2H), 3.26-3.10 (m, 2H), 3.05-2.69 (m, 2H). MS (m/e): 437 (M++1), 421, 405, 148. IR(KBr): 3434, 2923, 2361, 1718, 1513, 1395, 1232, 1032 cm-'. Example-15 C-{l-[3-Fluoro-4-(l-oxo-l,2,3,6-tetrahydro-lIambda4-thiopyran-4-yl)-phenyl]-1H- [l,2,3]tria2ol-4-yl}-methylamine: To a solution of 2-{l-[3-fluoro-4-(l-oxo-l,2,3,6-tet^ahydro-llambda4-thiopyran-4-yl)-phenyl]-lH-[l,2,3]triazol-4ylmethyl}-isoindole-l,3-dione (250 mg, 0.57 mmol), obtained in example-14, in methanol (5 mL) was added hydrazine hydrate (0.24 mL) and refluxed for 3 h followed by stirring at room temperature for 10 h. The reaction mixture was filtered and the filtrate was concentrated under vacuum. The residue was purified by flash chromatography over silica gel (6% methanol in chloroform) to furnish the title compound (105 mg, 60%) as a pale yellow solid. 'H NMR (CDCI3 + DMS0-d6): 5 8.09 (s, IH), 7.75-7.62 (m, 2H), 7.46-7.39 (m, IH), 5.95- 5.85 (m, IH), 4.07 (s, 2H), 3.63-3.51 (m, 2H), 3.19-2.98 (m, 4H). MS (m/e): 307 (W+l), 291, 273, 259. IR(KBr): 3427, 2924, 1618, 1515, 1228, 1029 cm"". Example-16 iV-{l-[3-Fluoro-4-(l-oxo-l,2,3,6-tetrahydro-llambda4-thiopyran-4-yl)-phenyl]-lJ?- [l,2,3]triazol-4-ylmethyl}-thioacetamide: To a solution of C-{l-[3-fluoro-4-(l-oxo-l,2,3,6-tetrahydro-llambda4-thiopyran-4-yl)-phenyl]-lH-[l,2,3]triazol-4-yl}-methylamine (45 mg, 0.15 mmol), obtained in example-15, in THF (5 mL) was added triethylamine (0.045 mL, 0.23 mmol) followed by the addition of ethyl dithioacetate (0.025 mL, 0.23 mmol) and stirred at room temperature for 16 h. The solvent was evaporated and the crude residue was purified by column chromatography over silica gel (3% methanol in chloroform) to obtain the desired product as a white solid (28 mg, 52%), mp 204 °C, 1H NMR (CDCI3 + DMSO-d^): 6 8.40 (s, 2H), 7.66-7.50 (m, 3H), 6.07-5.92 (m, IH), 4.97 (s, 2H), 4.17 (s, 2H), 3.81-3.47 (m, 2H), 3.34-3.08 (m, 2H), 2.55 (s, 3H). ES-MS (m/e): 387 (M^+23), 365 (M"+l). IR (KBr): 3428, 3012, 2924, 1620, 1543, 1391, 1231, 1030 cm'^ Example-17 {l-[3-Fluoro-4-(l-oxo-l,2,3,6-tetrahydro-llambda4-thiopyran-4-yI)-phenyl]-1H-[l,2,3]tria2ol-4-ylmethyI}-thiocarbamic acid O-methyl ester: A saturated aqueous solution of sodium bicarbonate (41 mg, 0.48 mmol) was added to a solution of C- {1 -[3-fluoro-4-( 1 -0x0-1,2,3,6-tetrahydro-1 lambda4-thiopyran-4-yl)-phenyl]-lH-[l,2,3]triazol-4-yl}-methylamine (50 mg, 0.16 mmol), obtained in example-15, in dichloromethane (5 mL) and then cooled to 0 °C. Thiophosgene (0.018 mL, 0.23 mmol) was added to the above mixture and stirred at the same temperature for 0.5 h. The reaction mixture was diluted with dichloromethane (50 mL), washed with water followed by brine and dried over Na2SO4. The solvent was evaporated and the residue was refluxed with methanol (10 mL) for 16 h. After evaporation of solvent, the residue was purified by column chromatography over sihca gel (methanol/chloroform; 1:49) to get the title compound as a white solid (35 mg, 56%), mp 153 °C. 1H NMR (CDCI3 + Methanol-d4): 5 8.27 and 8.08 (two s, IH, rotamers in ratio of 4:1), 7.60- 7.52 (m, 2H), 7.47-7.43 (m, IH), 5.96-5.82 (m, IH), 4.86 and 4.61 (s, 2H, rotamers in ratio of 4:1), 3.99 and 4.10 (two s, 3H, rotamers in ratio of 1:4), 3.72-3.67 (m, IH), 3.54- 3.44 (m, IH), 3.37-3.24 (m, IH), 3.15-2.96 (m, 2H), 2.80-2.75 (m, IH). MS (m/e): 349 (Nr-0CH3), 317, 292, 280. IR(KBr): 3189, 3026, 2927, 1619, 1541, 1408, 1200, 1012 cm"ExampIe-18 2-{l-[4-(14-Dioxo-l,2,3,6-tetrahydro-llambda6-thiopyran-4-yl)-3-fluoro-phenyl]-lH- [l,2,3]triazol-4ylmethyI}-isoindole-l,3-dione: To a solution of 2-{l-[4-(3,6-dihydro-2/f-thiopyran-4-yl)-3-fluoro-phenyl]-lH-[l,2,3]triazol-4-ylmethyl}-isoindole-l,3-dione (620 mg, 1.48 mmol), obtained in example-1, in dichloromethane (25 mL), cooled to 0 °C, was added m-chloroperbenzoic acid (1.1 g, 70% w/w, 4.44 mmol) in portion and stirred at the same temperature for 0.5 h. The reaction mixture was diluted with dichloromethane (50 mL) and washed with saturated aqueous solutions of sodium bisulfite and sodium bicarbonate respectively. The organic layer was dried over sodium sulfate and concentrated under reduced pressure. The residue was purified by column chromatography over silica gel to afford the desired sulfone derivative (400 mg, 60%) as a white solid along with some sulfoxide(28 mg, 28%) 1H NMR (CDCI3): 5 8.42 (s, IH), 7.97-7.76 (m, 4H), 7.71-7.55 (m, 2H), 7.42-7.38 (m, IH), 5,98-5.85 (m, IH), 5.05 (s, 2H), 3.88-3.82 (m, 2H), 3.30-3.27 (m, 2H), 2.86-2.59 (m, 2H). CI-MS(m/e):453(M++l) IR(KBr): 3427,2920, 1713, 1620, 1515, 1396, 1286, 1167, 937 cm-1 Example-19 C-{l-[4-{14-Pioxo-l,2,3,6-tetrahydro-llambda6-thiopyran-4-yl)-3-fluoro-phenyl]-lJ^^ [l,2,3]triazoI-4-yl}-methyIamine: Hydrazine hydrate (0.37 mL) was added to a solution of 2-{l-[4-(l,l-dioxo-l,2,3,6-tetrahydro-llambda6-thiopyran-4-yl)-3-fluoro-phenyl]-lH-[l,2,3]triazol-4ylmethyl}-iso indole-1,3-dione (400 mg, 0.88 mmol), obtained in example-18, in methanol (10 mL) and refluxed for 2 h followed by stirring at room temperature for 0.5 h. The reaction mixture was filtered and the filtrate was concentrated under vacuum. The residue was purified by flash chromatography over silica gel (6% methanol in chloroform) to produce the title compound as a white soUd (220 mg, 77%). 1H NMR (CDCI3 + DMS0-d6): 5 8.14 (s, IH), 7.69-7.52 (m, 2H), 7.47-7.38 (m, IH), 5.96-5.82 (m, IH), 4.08 (s, 2H), 3.96-3.81 (m, 2H), 3.38-3.18 (m, 2H), 3.18-3.05 (m, 2H). MS (m/e): 323 (IVT+l), 285, 259, 187. IR(KBr): 3346,2923, 1619, 1515, 1315, 1285, 1123, 1045 cm-1 Example-20 N-{l-[4-(l,l-Dioxo-l,2,3,6-tetrahydro-llambda6-thiopyran-4-yl)-3-fluoro-phenyl]-lH-[l,2,3]triazol-4-ylmethyl}-thioacetamide: R To a solution of C-{l-[4-(l,l-dioxo-l,2,3,6-tetrahydro-llambda6-thiopyran-4-yl)-3-fluoro-phenyl]-l^-[l,2,3]triazoI-4-yI}-methylamine (100 mg, 0.31 mmol), obtained in example-19, in THF (5 mL) was added triethylamine (0.095 mL, 0.68 mmol) followed by the addifion of ethyl dithioacetate (0.052 mL, 0.45 mmol) and stirred at room temperature for 18 h. The solvent was evaporated and the crude residue was purified by column chromatography over silica gel (3% methanol in chloroform) to obtain the desired product (83 mg, 70%) as a pale yellow solid, mp 188 °C. 1H NMR (CDCI3 + DMS0-d6): 5 10.21-10.15 (m, IH), 8.59 (s, IH), 7.82-7.70 (m, 2H), 7.49 (t, y = 8.6 Hz, IH), 5.96-5.84 (m, IH), 4.92 (d, 7= 4.9 Hz, 2H), 3.99-3.92 (m, 2H), 3.38-3.25 (m, 2H), 3.18-3.10 (m, 2H), 2.51 (s, 3H). CI-MS (mJe): 381 (M++1), 349, 317, 308. IR (KBr): 3292, 2924, 1621, 1515, 1315, 1287, 1167, 1045 cm-1 Example-21 {l-[4-(l,l-Dioxo-l,2,3,6-tetrahydro-llambda6-thiopyran-4-yl)-3-fluoro-phenyl]-lH- [l,2,3]triazol-4-yImethyl}-thiocarbamic acid 0-methyl ester: To a solution of C-{1-[4-( 1,1-dioxo-1,2,3,6-tetrahydro-llambda6-thiopyran-4-yl)-3-fluoro-phenyl]-lif-[ 1,2,3]triazol-4-yl}-methylamine (100 mg, 0.31 mmol), obtained in example-19, in dichloromethane (8 mL) was added a saturated aqueous solution of sodium bicarbonate (65 mg, 0.77 mmol) followed by cooling in ice bath. Thiophosgene (0.029 mL, 0.37 mmol) was added to the reacion mixture at 0 °C and stirred at the same temperature for 0.5 h. The reaction mixture was diluted with dichloromethane (50 mL), washed the organic layer with water, brine and dried over sodium sulfate. The solvent was evaporated and the residue was refluxed with methanol (10 mL) for 16 h. Methanol was evaporated on rotavapor and the residue was purified by column chromatography over silica gel (4% methanol in chloroform) to yield the title compound as a white solid (86 mg, 70%), mp 178 °C. 1H NMR (CDCI3 + DMS0-d6): 6 9.02-8.87 and 8.87-8.80 (two m, IH, rotamers in ratio of 1:4), 8.30 and 8.18 (two s, IH, rotamers in ratio of 4:1), 7.65-7.56 (m, 2H), 7.46-7.39 (m, IH), 5.97-5.88 (m, IH), 4.87 and 4.60 (two d, 7 = 5.6 Hz, 2H, rotamers in ratio of 4:1), 4.10 and 3.98 (two s, 3H, rotamers in ratio of 1:4), 3,89-3.81 (m, 2H), 3.38-3.20 (m, 2H), 3.19-3.01 (m, 2H). MS (m/e): 365 (M+-OCH3), 333, 308, 280, IR(KBr): 3428, 3291, 2924, 2854, 1620, 1515, 1315, 1277, 1041 cm-1 Example-22 2.{l-[4.(3,6-Dihydro-2H-thiopyran.4.yl)-3,5-difluoro-phenyl].liy-[l,2,3]triazol-4. ylmethyl}-isoindole-l,3-dione: To a solution of 4-(4-azido-2,6-difluoro-phenyl)-3,6-dihydro-2H-thiopyran (2.13 g, 8.40 mmol), obtained in preparation-8, and N, N-diisopropylethyiamine (2.9 mL, 16.8 mmol) in acetonitrile (25 mL) was added 2-prop-ynyl-isoindole-l,3-dione (2.35 g, 12.6 mmol) followed by the addition of cuprous iodide (2.40 g, 12.60 mmol) and stirred at room temperature for 1 h. The reaction mixture was filtered through a celite pad and washed thoroughly with MeOH/CHCb (1:10).Concentration of the filtrate under vacuum and purification of the resulting residue by flash chromatography (ethyl acetate/hexane; 4:6) yielded the title compound as a light yellow solid (1.60 g, 44%). 1H NMR (CDCI3): 5 8.02 (s, IH), 7.97-7.82 (m, 2H), 7.81-7.65 (m, 2H), 7.32 (d, J= 7.5 Hz, 2H), 6.05-5.97 (m, IH), 5.08 (s, 2H), 3.39-3.35 (m, 2H), 2.88 (t, J- 5.6 Hz, 2H), 2.61-2.47 (m, 2H). MS (m/e): 439 (M++1), 266, 148. IR(KBr): 3149, 3067, 2922, 1712, 1633, 1512, 1394, 1094 cm"^ Example-23 C-{l-[4-(3,6-Dihydro.2H-thiopyran.4-yl)-3,5-difluoro-phenyl]-l^-[l,2,3]tria2ol-4-yl}- methylamine: To a solution of 2-{l-[4-(3,6-dihydro-2H-thiopyran-4-yl)-3,5-difluoro-phenyl]-li/-[1,2,3] triazol-4-ylmethyl}-isoindole"l,3-dione (400 mg, 0.91 mmol), obtained in example-22, in methanol (12 mL) was added hydrazine hydrate (0.41 mL) and refluxed for 2 h followed by stirring at room temperature for 10 h. The reaction mixture was filtered and the filtrate was concentrated under vacuum. The resultant residue was dissolved in chloroform (100 mL), washed the organic layer with water followed by brine and dried (sodium sulfate). Evaporation of the solvent on a rotavapor and purification of the resulting residue by flash chromatography (ethyl acetate/ hexane; 1:10) afforded the title compound as a pale yellow solid (260 mg, 93%). 'H NMR (CDCI3): 5 7.87 (s, IH), 7.33 (d, J= 7.8 Hz, 2H), 6.15-5.98 (m, IH), 4.08 (s, 2H), 3.41-3.32 (m, 2H), 2.89 (t, J= 5.6 Hz, 2H), 2.61-2.45 (m, 2H). MS(m/e):309(Mt+l), 280. IR(KBr): 3357, 3128, 2920, 1631, 1595, 1449, 1220, 1028 cm"'. £xampie-24 Ar.{1.[4.(3,6-Dihydro-2H-thiopyran-4-yl)-3,5-difluoro-phenyl]-lH-[l,2,3]triazol-4- ylmethyl}-thioacetamide: To a solution of C-{l-[4-(3,6-dihyclro-2H-thiopyran-4-yl)-3,5-difluoro-phenyl]-lH-[l,2,3]triazol-4-yl}-methylamine (100 mg, 0.32 mmol), obtained in example-23, in THF (5 mL) was added triethylamine (0.1 mL, 0.72 mmol) followed by the addition of ethyl dithioacetate (0.06 ml, 0.49 mmol) and stirred at room temperature for 16 h. The reaction mixture was diluted with ethyl acetate (75 mL), washed the organic layer with water followed by brine and dried over sodium sulfate. Solvent was evaporated and the residue was purified by column chromatography (silica gel), using 15% methanol in chloroform as eluent, to give the desired product as a white powder (58 mg, 50%), mp 178-179 °C. 1H NMR (CDCI3): 5 8.18-8.09 (m, 2H), 7.34 (d, 7= 7.3 Hz, 2H), 6.08-6.01 (m, IH), 5.02 (d, J - 5.4 Hz, 2H), 3.40-3.31 (m, 2H), 2.89 (t, J= 5.4 Hz, 2H), 2.68-2.48 (m, 5H). MS (m/e): 367 (M++1), 339, 189. IR(KBr): 3204,2999, 1632, 1510, 1344, 1050 cm"^ Example-25 {l-[4-(3,6-Dihydro-2H-thiopyran-4-yl)-3,5-difluoro-phenyl]-lH-[l,2,3]triazol-4-ylmethyl}-thiocarbamic acid O-methyl ester: To a solution of C-{l-[4-(3,6-dihydro-2H-thiopyran-4-yl)-3,5-difluoro-phenyl]-l/]r-[ 1,2,3]triazol-4-yl}-methylamine (90 mg, 0.29 mmol), obtained in exampie-23, in dichloromethane (10 mL) was added a solution of sodium bicarbonate (62 mg, 0.73 nimol) in water (3 mL) followed by cooling in ice bath. Thiophosgene (0.03 mL, 0.35 mmol) was added to the above mixture at 0 °C and stirred at the same temperature for 0.5 h. The reaction mixture was diluted with dichloromethane (50 mL), washed the organic layer with water followed by brine and dried over sodium sulfate. Evaporation of volatiles left a residue, which was refluxed with methanol (15 mL) for 16 h. Removal of solvent on rotavapor and purification of the residue by column chromatography (ethyl acetate/ hexane; 3:10) yielded the title compound as a white powder (72 mg, 65%), mp 156-158 °C. 1H NMR (CDCI3): 8 8.10 (s, IH), 7.34 (d, J= 7.8 Hz, 2H), 6.15-5.97 (m, IH), 4.91 and 4.68 (two d, y= 5.9 Hz, 2H, rotamers in ratio of 4:1), 4.12 and 3.99 (two s, 3H, rotamers in ratio of 1:4), 3.40-3.31 (m, 2H), 2.89 (t, / = 5.6 Hz, 2H), 2.61-2.50 (m, 2H). MS (m/e): 383 (M>1), 351, 335, 294. IR(KBr): 3193, 3123,2924, 1633,1593, 1454, 1125 cm'. Example-26 2-{l-[3,5-Difluoro-4-(l-oxo-l,2,3,6-tetrahydro-llambda4-thiopyran-4-yl)-phenyl]-lH- [l,2,3]triazol-4ylmethyl}-isoindole-l,3-dione: Sodium periodate (410 mg, 1.92 mmol) in water (5 mL) was added to an ice cooled solution of 2-{l-[4-(3,6-dihydro-2H-pyran-4-yl)-3,5-difluoro-phenyl]-lH-[l,2,3]triazol-4-ylmethyl}-l,3-isoindole-l,3-dione (350 mg, 0.79 mmol), obtained in example-22, in methanol (12 mL) and ethyl acetate (12 mL) and stirred at the same temperature for 1 h. The reaction mixture was warmed to room temperature and stirred for 16 h. The reaction mixture was diluted with methanol (1 mL) and chloroform (19 mL), and filtered. The filtrate was concentrated under vacuum. The residue obtained was dissolved in chloroform, washed with saturated solutions of Na2SO3 and NaHCO3 and dried over sodium sulfate. Evaporation of solvent and purification of the residue by column chromatography over silica gel (ethyl acetate) afforded the desired product (295 mg, 81%) as a pale yellow solid. 1H NMR (DMSO-d6): δ 8.86 (s, IH), 8.00-7.68 (m, 6H), 5.86-5.76 (m, IH), 4.94 (s, 2H), 4.01-3.92 (m, 2H), 3.45-3.18 (m, 2H), 2.96-2.82 (m, 2H), MS (m/e): 455 (NT+I), 439, 421 IR(KBr): 3459, 1714, 1428, 1395, 1208, 1034 cm-1. Example-27 C-{l-[3,5-Difluoro-4-(l-oxo-l,2,3,6-tetrahydro-llambda4-thiopyran-4-yl)-phenyl]-lH- [l,2,3]triazol-4-yl}-niethylamine: To a solution of 2-{l-[3,5-difIuoro-4-(l-oxo-l,2,3,6-tetrahydro-llambda4-thiopyran-4-yl)-phenyl]-lH-[l,2,3]triazol-4ylmethyi}-isoindole-l,3-dione (290 mg, 0.64 mmol), obtained in example-26, in methanol (10 mL) was added hydrazine hydrate (0.27 mL) and refluxed for 2 h followed by stirring at room temperature for 10 h. The reaction mixture was filtered and washed with chloroform (5% methanol). The filtrate was concentrated under vacuum and the residue was purified by flash chromatography. (3% methanol in chloroform) to afford the title compound (126 mg, 62%) as a white solid. 1H NMR (CDCI3 + DMS0-d6): 5 8.58 (s, IH), 7,66 (d, J= 8.3 Hz, 2H), 5.84-5.80 (m, IH), 3.94 (s,2H), 3.75-2.96 (m,6H). MS (m/e): 325 (M++1), 309, 181. IR(KBr): 3441,2924, 1632, 1583, 1452, 1366, 1207, 1034 cm-1. Example-28 A^-{l-[3,5-Difluoro-4-(l-oxo-l,2,3,6-tetrahydro-llambda4-thiopyran-4-yl)-phenyI]-lH-[l,2,3]triazoI-4-yImethyl}thioacetamide: To a solution of C-{l"[3,5-difluoro-4-(l-oxo-l,2,3,6-tetrahydro-llambda4-thiopyran-4-yl)-phenyl]-lH-[l,2,3]triazol-4-yl}-methylamine (60 mg, 0.185 mmol), obtained in example-27, in THF (5 mL) was added triethylamine (0.058 mL, 0.41 mmol) followed by the addition of ethyl dithioacetate (0.033 mL, 0.28 mmol) and stirred at room temperature for 16 h. The solvent was evaporated from the reaction mixture and the residue was purified by column chromatography (2% methanol in chloroform) to obtain the desired product as a pale yellow solid (40 mg, 57%), mp 182-184 °C. 1HNMR(CDCl3 + DMSO-d6): δ 10.15-10.10 (m, IH), 8.38 (s, IH), 7.50-7.38 (m, 2H), 5.84- 5.81 (m, IH), 4.95 (d, 7 = 5.4 Hz, 2H), 3.71-3.66 (m, 2H), 3.48-3.43 (m, 2H), 3.24-3.18 (m, 2H), 2.58 (s, 3H). MS (m/e): 383 (M++1), 367, 365, 339, 310. IR(KBr): 3184, 3003, 1632, 1562, 1450, 1280, 1023 cm"'. Example-29 {l-[3,5-Difluoro-4-(l-oxo-l,2,3,6-tetrahydro-llambda4-thiopyran-4-yl)-phenyl]-l^- [l,2,3]triazol-4-ylmethyl}-thiocarbainic acid 6>-methyl ester: A solution of sodium bicarbonate (41 mg, 0.48 mmol) in water (5 mL) was added to an ice cooled solution of C-{l-[3,5-difluoro-4-(l-oxo-l,2,3,6-tetrahydro-llambda4-thiopyran-4-yl)-phenyi]-lH-[l,2,3]triazol-4-yl}-methylamine (63 mg, 0.194 mmol), obtained in exampIe-27, in dichloromethane (5 mL). Thiophosgene (0.020 mL, 0.26 mmol) was added to the reaction mixture and stirred for 0.5 h. The reaction mixture was diluted with dichloromethane (50 mL), washed the organic layer with water followed by brine and dried over sodium sulfate. The solvent was evaporated and the residue was refluxed with methanol (15 mL) for 16 h. After evaporation of methanol, the residue was purified by column chromatography over silica gel (methanol/chloroform; 1:25) to furnish the title compound as a white powder (50 mg, 65%), mp 206-208 °C. 'H NMR (CDCI3 + DMS0-d6): 5 8.58-8.54 and 8.46-8.39 (two m, IH, rotamers in ratio of 1:4), 8.14 and 8.00 (two s, IH, rotamers in ratio of 4:1), 7.33 (d, 7= 7.8 Hz, 2H), 5.75-5.71 (m, IH), 4.74 and 4.45 (two d, J = 5.9 Hz, 2H, rotamers in ratio of 4:1), 3.90 and 3.86 (two s, 3H, rotamers in ratio of 1:4), 3.60-3.55 (m, 2H), 3.37-3.32 (m, 2H), 3.11-3.07 (m, 2H). MS (m/e): 367 (M^-OCHa), 351, 335, 325, 294. IR(KBr): 3442, 2924, 1715, 1634, 1518, 1452, 1233, 1030 cm-1 Example-30 N-{l-[3,5-Difluoro-4-(l-oxo-l,2,3,6-tetrahydro-llambda4&-thiopyran-4-yI)-phenyl]-1H [l,2,3]triazol-4-ylmethyl}-acetamide: To a solution of C-{l-[3,5-difluoro-4-(l-oxo-1.2,3,6-tetrahydro-llambda4-thiopyran-4-yl)-phenyl]-lH-[l,2,3]triazol-4-yl}-methylamine (80 mg, 0.25 mmol), obtained in example-27, in dichloromethane (5 mL), cooled to 0 ^C was added triethylamine (0.069 mL, 0.49 mmol) followed by the addition of acetyl chloride (0.02 mL, 0.29 mmol) and stirred at room temperature for 3 h. The solvent was evaporated from the reaction mixture and the residue was purified by column chromatography on silica (4% methanol in chloroform) to afford the required compound as a creamy white solid (45 mg, 50%), mp 177-180 °C. 1H NMR (DMS0-d6): 5 8.74 (s, IH), 8.54-8.39 (m, IH), 7..84 (d, J= 8.3 Hz, 2H), 5.92-5.78 (m, IH), 4.37 (d,y= 5.6 Hz, 2H), 3.80-3.10 (m, 6H), 1.86 (s, 3H). MS (m/e): 367 (NT+I), 318, 290, 231. IR(KBr): 3323, 3128, 2926, 1648, 1532, 1455, 1206, 1026 cm■^ Example-31 {l-[3,5-Difluoro-4-(l-oxo-l,2,3,6-tetrahydro-llambda4-thiopyran-4yl)-phenyI]-lH-[l,2,3]triazol-4-ylmethyl}-carbamic acid methyl ester: H,A^-Diisopropylethylamine (0.11 mL, 0.63 mmol) was added to an ice cooled solution of C-{l-[3,5-difluoro-4-(l-oxo-l,2,3,6-tetrahydro-llambda4-thiopyran-4-yl)-phenyl]-lH-[l,2,3]triazol-4-yl}-methylamine obtained in example-27 (80 mg, 0.25 mmol) in dichloromethane (5 mL), followed by the addition of methyl chloroformate (0.023 mL, 0.29 mmol) and stirred for 2 h. The reaction mixture was concentrated on rotavapor and the resulting residue was purified by column chromatography (3% methanol in chloroform) to yield the desired product (50 mg, 53%) as a creamy white solid, mp 172-174 °C. 1H NMR (DMS0-d6): 5 8.75 (s, IH), 7.98-7,72 (m, 3H), 5.91-5.80 (m, IH), 4.32 (d, y = 5.8 Hz, 2H), 3.80-3.10 (m, 6H), 3.57 (s, 3H). MS(m/e):383(Mt+l), 351. IR(KBr): 3333, 2924, 2854, 1696, 1543, 1454, 1264, 1032 cm-ExampIe-32 2-{l-[4-(l,l-Dioxo-l,2,356-tetrahydro-llambda6-thiopyran-4-yl)-3,5-difluoro-phenyl]-1H-[l,2,3]triazol-4ylmethyI}-isoindole-l,3-dione: u To a solution of 2- {l-[4-(3,6-dihydro-2H-pyran-4-yl)-3,5-difluoro-phenyl]-lH-[l,2,3]triazol-4-ylmethyl}-l,3-isoindole-l,3-dione (710 mg, 1.6 mmol), obtained in example-7, in dichloromethane (25 mL), was added m-chloroperbenzoic acid (1.3 g, 5.26 mmol, 70% w/w) in portion at 0 °C and the mixture was stirred for 0.5 h. The reaction mixture was diluted with dichloromethane (75 mL) and washed with water followed by brine. The organic layer was dried over sodium sulfate and evaporated. The residue was purified by column chromatography over silica gel (4% methanol in chloroform) to afford the desired product (375 mg, 49%) as a white solid. 1H NMR (DMS0-d6): 5 8.85 (s, IH), 7.88-7.78 (m, 4H), 7.75 (d, J= 8.6 Hz, 2H), 5.92-5.79 (m, IH), 4.97 (s, 2H), 3.96-3.89 (m, 2H), 3.32-3.18 (m, 2H), 3.02-2.86 (m, 2H), MS (m/e): 471 (M++1), 391, 298, 185. IR(KBr): 3459, 3146, 1713, 1634, 1396, 1286, 1031 cm'. Example-33 C-{l-[4-(l,l-Dioxo-l,2,3,6-tetrahydro-llambda6-thiopyran-4-yl)-3,5-difluoro-phenyl]- l/r-[l,2,3]triazol-4-yl}-methylamine: Hydrazine hydrate (0.312 mL) was added to a solution of 2-{l-[4-(l,l-dioxo-l,2,3,6-tetrahydro-llambda6-thiopyran-4-yl)-3,5-difluoro-phenyl]-lH-[l,2,3]triazol-4ylmethyl}-isoindole-l,3-dione (350 mg, 0.74 mmol), obtained in example-32, in methanol (15 mL) and refluxed for 2 h followed by stirring at room temperature for 16 h. The reaction mixture was filtered and washed with a mixture of chloroform/methanol. The filtrate was concentrated under vacuum and the residue was purified by flash chromatography over silica gel (4% methanol in chloroform) to get the title compound as a white solid (195 mg, 77%). 'H NMR (CDCI3 + DMS0-d6): 5 8.38 (s, IH), 7.58 (d, J= 7.8 Hz, 2H), 5.92-5.83 (m, IH), 4.03 (s, 2H), 3.93-3.87 (m, 2H), 3.18-2.96 (m, 2H), 2.60-2.58 (m, 2H). MS (m/e): 341 (NT+I), 277, 181. IR(KBr): 3449,2923, 1634, 1599, 1515, 1324, 1288, 1029 cm-'. Example-34 N-{l-[4-(l,l-Dioxo-l,2,3,6-tetrahydro-llambda6-thiopyran-4-yl)-3,5-difluoro-phenyl]- lH-[l,2,3]triazol-4-ylmethyl}thioacetamide: To a solution of C-{l-[4-(l,ldioxo-l,2,3,6-tetrahydro-llambda6-thiopyran-4-yl)-3,5-difluoro-phenyl]-l/f-[l,2,3]triazol-4-yl}-methylamine (100 mg, 0.294 mmol), obtained in example-33, in THF (5 mL) was added triethylamine (0.082 mL, 0.58 mmol) followed by the addition of ethyl dithioacetate (0.051 mL, 0.44 mmol). The reaction mixture was stirred at ambient temperature for 16 h and then concentrated on rotavapor The residue was purified by column chromatography (2% methanol in chloroform) to obtain the desired product (58 mg, 50%) as a pale yellow solid, mp 210 oC. 'H NMR (CDCI3 + DMSO-d6): 6 9.96-9.82 (m, IH), 8.33 (s, IH), 7.46 (d, 7 = 7.8 Hz, 2H), 5.96-5.82 (m, IH), 4.98 (d, J= 5.4 Hz, 2H), 3.95-3.82 (m, 2H), 3.29-3.26 (m, 2H), 3.18-3,06 (m,2H),2.56(s,3H). MS (m/e): 399 (M++1), 371, 271. IR(KBr): 3482,3291,2921, 1632, 1551, 1454, 1282, 1168cm-1 Example-35 N-{l-[4-(l-l-Dioxo-l,2,3,6-tetrahydro-llambda6-thiopyran-4-yl)-3,5-difluoro-phenyl]-lH- [l,2,3]triazol-4-ylmethyl}-acetamide: To a solution of C-{l-[4-(lJ-dioxo-l,23,6-tetrahycko-llambda6-thiopyran-4-yl)-3,5-difluoro-phenyl]-lH-[l,2,3]triazol-4-yl}-methylamine (100 mg, 0.29 mmol), obtained in example-33, in dichloromethane (5 mL), cooled to 0 °C, was added triethylamine (0.91 mL, 0.65 mmol) followed by the addition of acetyl chloride (0.023 mL, 0.320 mmol). The reaction mixture was brought to room temperature and stirred for 3 h. Evaporation of solvent from the reaction mixture and purification of the residue by column chromatography (methanol/ chloroform; 1:24) yielded the title compound (60 mg, 53%) as a white solid, mp 242-246 ""C. 1H NMR (DMS0-d6): 5 8.74 (s, IH), 8.52-8.40 (m, IH), 7.84 (d, 7 = 8.6 Hz, 2H), 5.90-5.84 (m, IH), 4.36 (d, y = 5.6 Hz, 2H), 4.04-3.91 (m, 2H), 3.44-3.13 (m, 2H), 2.98-2.87 (m, 2H), 1.86 (s,3H). MS(m/e):383(Nr+l), 239.. IR(KBr): 3287, 3094, 2926, 1630, 1543, 1286, 1058 cm-1. £xample-36 {l-(4-(l,l-Dioxo-l,2,3,6-tetrahydro-lIambda6-thiopyran-4-yl)-3,5-difluoro-phenyl]-l/?-[l,2,3]triazol-4-ylmethyl}-thiocarbamic acid O-methyl ester: To a solution of C-{l-[4-(l,l-dioxo-l,2,3,6-tetrahydro-llambda6-thiopyran-4-yl)-3,5-difluoro-phenyl]-li/-[l,2,3]triazol-4-yl}-methylamine (90 mg, 0.26 mmol), obtained in example-33, in dichloromethane (5 mL) was added a saturated solution of sodium bicarbonate (64 mg, 0.76 mmol) in water (5 mL) followed by cooling in ice bath. Thiophosgene (0.027 mL, 0.35 mmol) was added to the above mixture at 0 °C and stirred for 0.5 h. The reaction mixture was diluted with dichloromethane (50 mL), washed the organic layer with water, brine and dried over sodium sulfate. The solvent was evaporated and the residue was refluxed with methanol (5 mL) for 16 h. Methanol was evaporated on a rotavapor and the residue was purified by column chromatography over silica gel (4% methanol in chloroform) to yield the title compound as a white powder (54 mg, 50%), mp 196 °C. 'H NMR (CDCI3): 5 8.14 and 7.90 (two s, IH, rotamers in ratio of 4:1), 7.40 (d, J= 7.8 Hz. 2H), 6.96-6.85 (m, IH), 5.90-5.82 (m, IH), 4.92 and 4.65 (two d, 7 = 5.9 Hz, 2H, rotamers in ratio of 4:1), 4.10 and 4.00 (two s, 3H, rotamers in ratio of 1:4), 3.92-3.83 (m, 2H), 3.38-3.21 (m,2H), 3.18-3.08 (m,2H). MS (m/e): 415 (Nf+1), 383, 326, 298. IR(KBr): 3269, 1634, 1530, 1451, 1322, 1282, 1201, 1027 cm-' Example-37 {l-[4-(l,l-Dioxo-l,2,3,6-tetrahyclro-llambda6-thiopyran-4-yl)-3,5-difluoro-phenyl]- lH-[l,2,3]triazoI-4-ylmethyl}-carbamic acid methyl ester: To an ice cooled solution of C-{l-[4-(l,l-dioxo-l,2,3,6-tetrahydro-llambda6-thiopyran-4-yl)-3,5-difluoro-phenyl]-lH--[l,2,3]triazol-4-yl}-methylamine (60 mg, 0.8 mmol), obtained in example-33, in dichloromethane (5 mL), was added N, A'-diisopropylethylamine (0.067 mL, 0.38 mmol) followed by the addition of methyl chloroformate (0.016 mL, 0.21 mmol). The reaction mixture was stirred at the same temperature for 2 h. The solvent was evaporated from the reaction mixture and the residue was purified by column chromatography over silica gel (methanol/ chloroform; 1:9) to afford the required product (42 mg, 60%) as a creamy white solid, mp 190-194 °C. 'H NMR (DMS0-d6): 5 8.77 (s, IH), 7.84-7.75 (m, IH), 7.84 (d, 7 = 7.3 Hz, 2H), 5.92-5.82 (m, IH), 4.33 (d, /= 5.8 Hz, 2H), 4.08-3.90 (m, 2H), 3.57 (s, 3H), 3.50-3.19 (m, 2H), 2.99-2.82 (m, 2H). MS (m/e): 399 (M+l), 367. IR(KBr): 3334, 2925, 1691, 1541,1456, 1263, 1031 cm"'. Example-38 {l-[4-(3,6-Dihydro-2H-pyran-4-yl)-3,5-difluorophenyl]-lH-[l,2,3]triazoI-4-yImethyl}-carbamicacid methyl ester: N-Diisopropylethylamine (0.127 mL, 0.729 mmol) was added to an ice cooled solution of C-{l-[4-(3,6-dihydro-2H-pyran-4-yl)-3,5-difluoro-phenyl]-lH-[1.2,3]triazol-4-yl]--methylamine (100mg, 0.365 mmol), obtained in example-8, in dichloromethane (5 niL), followed by the addition of methyl chioroformate (0.034 mL, 0.438 mmol) and stiiTed at the same temperature for 3 h. The reaction mixture was concentrated on rotavapor and the resulting residue was purified by column chromatography over silica gel (3% methanol in chloroform) yielded the desired product (60 mg, 47%) as a white solid, mp 165-170 °C. 'H NMR (CDCI3): 5 7.99 (s, IH), 7.34(d, J-7.8 Hz, 2H), 6.00-5.96 (m, IH), 4.51 (d, J = 5.6 Hz, 2H), 4.38-4.31 (m, 2H), 3.94 (t, J=5.3 Hz, 2H), 3.69(s, 3H), 2,45-2.38(m, 2H). CI-MS(m/e):351 (M++1). IR (KBr): 3341, 2928, 1698, 1635, 1549, 1454. 1267, 1028, 860, 773 cm"'. Example-39 {l-[4-(3,6-Dihydro-2H-thiopyran-4-yl)-3-fluoro-phenyI]-lH-[l,2,3]triazol-4-ylmethyl} thiocarbamic acid O-methyl ester: A saturated solution of sodium bicarbonate (133mg, 1.58mmol) in water (5ml) was added to an ice cooled solution of C-[l-[4-(3,6-dihydro-2H-thiopyran-4-yl)-3-fluoro-phenyl]-lH-[l,2,3]triazol-4-yl}-methylamine (200 mg, 0.689 mmol), obtained in example-12, in dichloromethane (5 mL). Thiophosgene (0.068 mL, 0.895 mmol) was added to the reaction mixture and stirred at the same temperature for 0.5 h. The reaction mixture was diluted with dichloromethane (50 mL), washed the organic layer with water followed by brine and dried over sodium sulfate. The solvent was evaporated and the residue was refluxed with methanol (15 mL) for 16 h. After evaporation of methanol, the residue was purified by column chromatography over silica gel (methanol/chloroform; 1:25) to furnish the title compound as a creamy white solid (150 mg, 60%), mp 110-113 T. 'H NMR (CDCI3): 5 7.99 (s, IH), 7.56-7.32 (m, 3H), 6.16-6.05 (m, IH). 4.52(d. J=6.3 Hz, 2H), 3.70 (s. 3H), 3.42-3.31(m, 2H), 2.88 (t, J=5.8 Hz, 2H), 2.75-2.63 (m, 2H). CI-MS(m/'e):365(M^+l). IR(KBr): 3329, 3149. 2923, 1619, 1540, 1514, 1458, 1357, 1266, 1229. 1145. 1046. 1011. 872,619 cm-'. In vitro Data Minimum Inhibiton Concentrations (MICs) were determined by broth microdilution technique as per the guidelines prescribed in the fifth edition of Approved Standards, NCCLS document M7-A5 Vol 20 - No 2, 2000 Villinova, PA. Initial stock solution of the test compound was prepared in DMSO. Subsequent two fold dilutions were carried out in sterile Mueller Hinton Broth (Difco) (MHB). Frozen cultures stocks were inoculated into 50 ml sterile MHB in 250 ml Erlyn Meyer flasks. Composition of MHB is as follows: Beef Extract Powder - 2.0 s/litre Acid Digest of Casein - 17.5 g/ litre Soluble Starch - 1.5 e/litre Final pH 7.3 ±0.1 Flasks were incubated for 4 to 5 h at 35 'oC on a rotary shaker at 150 rpm. Inoculum was prepared by diluting the culture in sterile MHB to obtain a turbidity of 0.5 McFarland standard. This corresponds to 1-2 x 10 CFU/ml. The stock was further diluted in sterile broth to obtain 1-2X10 CFU/ml. 50µ1 of the above diluted inoculum was added from 1-10 wells. The plates were incubated overnight at 37 °C. MIC is read as the lowest concentration of the compound that completely inhibits growth of the organism in the microdilution wells as detected by the unaided eye. ATCC; American Type Culture Collection, USA NCTC: National Collections of Type Cultures. Colindale, UK DRCC: Dr. Reddy's Culture Collection, Hyderabad, India. The in vitro antibacterial activity data is shown in TABLE 1. TABLE 1 In vivo efficacy studies: Mice Systemic Infection • S.aureus ATCC 29213 and other tested strains were grown overnight on Columbia Blood agar (DIFCO). • The inoculum was prepared by suspending the culture in 0.9% saline and adjusted to 100 X LD50 dose in 10% Hog Gastric Mucin (DIFCO). 0.5ml was injected intraperitonially to Swiss albino mice weighing 18-22g (n=6) • Test compounds were solubilised in suitable formulation and 0.25ml was administered intra venously or orally or sub-cutaneously at 1 hr and 5 hr post infection by BID or TDD or single dose protocol • The animals were observed for 5-7 days and the survival was noted. • ED50 was calculated by probit analysis. We claim: 1. A compound of formula (I) where R1 represents halogen, azido, thioalcohol, isothiocyanate, hydroxy, isoindole-l,3-dione, substituted or unsubstituted (C1-C10)alkylsulfonyloxy, arylsulfonyloxy, (C1-C10)acyloxy group, NHR4 where R4 represents substituted or unsubstituted groups selected from (C1- C10)alkyl, (CrC)o)acyl, thio(C1-C10)acyl, (C1-C10)alkoxycarbonyl, (C3- Cio)cycloalkoxycarbonyl5 (C3-Cio)cycloalkoxythiocarbonyl, (C2-Cio)alkenyloxycarbonyl, (C2- Cio)alkenylcarbonyl, heteroaryl, aryloxycarbonyl, heteroarylcarbonyl, heteroarylthiocarbonyl, (C1-C10)alkoxythiocarbonyl, (C2-Cio)alkenyloxythiocarbonyl, aryloxythiocarbonyl, -C(=O)- C(=O)-(C1-C10)alkyl, -C(=O)-C(=O)-aryl, -C(=O)-C(=O)-(C1-C10) alkoxy, -C(=O)-C(=O)- aryloxy, -C(=O)-C(=S)-(C1-C10)alkyI, -C(=O)-C(=S)-aryl, -C(=S)-S-(C1-C10)alkyl, -C(=S)- NH2, -C(=S)-NHKC1-C10)alkyl, -C(=S)-N-((C1-C10)alkyl)2, -C(=S)-NH-(C2-Cio)alkenyl, - C(=S)-C(=O)- (C1-C10)alkoxy, -CeS)-C(=O)-aryloxy, -C(=S)-0-C(=O)-(C1-C10) alkyl, - C(-S)-C(=S)-(C1-C10)alkyl, -C(=S)-C(=S)-aryl, -C(-S)-NH-C(=O)-aryl, -C(=S)-NH-aralkyl, - C(=S)-NH-heteroaralkyl, -C(=NH)-NH2, -C(=NH)-(C1-C10)alkyl, -C(=NH)-aryl, -S (O)2(C1- Cio)alkyl, -S(0)2aryl, thiomorpholinylthiocarbonyl, pyrrolidinylthiocarbonyl or -C(=S)- N(R'R"), where R' and R" together form a substituted or unsubstituted 5 or 6 member heterocycle ring containing nitrogen and optionally having one or two additional hetero atoms selected from O, S or N; R and R may be same or different and independently represent hydrogen, halogen atom, substituted or unsubstituted (C1-C10)alkyl group, halo(C1-C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, OR4 where R1 represents substituted or unsubstituted (C1-C10)alkyl group; Y and Y may be same or different and independently represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or unsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(Cr Cio)alkyl, (C1-C10)alkoxycarbonyl, caTboxy(C1-C10)alkyl, (C1-C10)alkylsulfonyl, (Cj- Cio)alkylcarbonylamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10) alkylcarbonyloxy(C1-C10)alkyl, amino(C1-C10)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y , Y may represent =O, =S, substituted or unsubstituted =NOR'" group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates. 2. The compoimd of formula (I), as claimed in claim 1, wherein a 5 or 6 member heterocycle ring containing nitrogen, optionally having one or two additional heteroatoms selected from oxygen, nitrogen or sulfur, formed by R' & R" is selected from imsubstituted or substituted pyrrolidinyl, pyrrolyl, morpholinyl, thiomorpholinyl, benzothiazole, benzoimidazolyl, pyridinyl, pyridazinyl, pyrimidinyl or pyrazinyl. 3. The compoimd of formula (I), as claimed in claim 1, where in the substituents on the groups represented by R4, R4a, R4b, 44c, 44d R4e R, R7 and heterocycles formed by R'and R" are selected from halogen atom, hydroxy, amino, cyano, nitro, (C1-C10)alkyl, hydroxy(Ci-Cio)alkyl, (C1-C10)alkoxy =0, =S, aryl, hydroxyaryl, pyridyl, mono(C1-C10)alkylamino, di(Ci-Cio)alkylamino, (C1-C10)acyl, thio(C1-C10)acyl, (C1-C10)alkoxycarbonyl, (C1-C10)alkoxyaryl, or carboxyhc acid or its derivatives. 4. The compound as claimed in claim 1, wherein the substituents on R2, R3 and R4 are selected from hydroxy, halogen, nitro, amino, (C1-C10)alkyl, (C1-C10)alkoxy, =O, =S, cyano group, or carboxylic acid or its derivatives. 5. The compound as claimed in claim 1, wherein the substituents on Y1 and Y2 are selected from hydroxy, nitro, cyano, amino, tert-butyldimethylsilyloxy (TBSO), halogen atom, (C1-C10)alkyl, (C1-C10)alkoxy, cyclo(C3-Cio)alkyl, aryl, benzyloxy, acyl or acyloxy group. 6. The compound of formula (I) as claimed in claim 1, wherein R4 is (C1-C10)acyl, thio(C1-C10)acyl, (C1-C10)alkoxycarbonyl, (C1-C10)alkoxythiocarbonyl. 7. The compound of formula (I) as claimed in claim 1, wherein R2 and R3 represent hydrogen and halogen. 8. The compound of formula (I) as claimed in claim 1, wherein 'm' represents 1. 9. The compound of formula (I) as claimed in claim 1, wherein ' ' represents a bond. 10. The compound of formula (I) as claimed in claim 1, wherein R4 is (C1-C10)acyl, thio(C1-C10)acyl, (C1-C10)alkoxycarbonyl, (C1-C10)alkoxythiocarbonyl; m represents 1; '....' represents a bond and R & R represent hydrogen and halogen. 11. The compound of formula (I) as claimed in claim 1, wherein R is (C1-C10)acyl, thio(C1-C10)acyl, (C1-C10)alkoxycarbonyl, (C1-C10)alkoxythiocarbonyl; m represents 1; '....' represents a bond; R2 and R1 represent hydrogen and halogen and Y1 & Y2 represent hydrogen atom. 12. The compound of formula (I) as claimed in claim 1, wherein R4 is (C1-C10)acyl; m represents 1; '....' represents a bond; R2 and R3 represent hydrogen and halogen and Y1 &Y^ represent hydrogen atom. 13. The compound of formula (I) as claimed in claim 1, wherein R is thio(C1-C10)acyl; m represents 1; '....' represents a bond; R2 and R3 represent hydrogen and halogen and Y1 & Y represent hydrogen atom. 14. The compound of formula (I) as claimed in claim 1, wherein R4 is (C1- C10)alkoxycarbonyl; m represents 1; '....' represents a bond; R2 and R3 represent hydrogen and halogen and Y* & Y^ represent hydrogen atom. 15. The compound of formula (I) as claimed in claim 1, wherein R"* is (C1- Cio)alkoxythio6arbonyl; m represents 1; '....' represents a bond; R2 and R3 represent hydrogen and halogen and Y1 & Y2 represent hydrogen atom. 16. The compound of formula (I) as claimed in claim 1, wherein R4 is -C(=O)-CH3, - C(=S)-CH3, -C(=O)-OCH3, -C(=S)-0CH3; m represents 1; ..' represents a bond; R2 and R3 represent hydrogen and fluorine and Y^ & Y^ represent hydrogen atom. 17. The compound of the formula (I) or a pharmaceutically aceeptable salts thereof, as claimed in claim 1, selected from: 18. The compound of formula (I), as claimed in claim 1 or 17, wherein the pharmaceutically acceptable salt is selected from the group consisting of Li, Na, K, Ca, Mg, Fe, Cu, Zn, Mn; salts of organic bases, chiral bases, natural amino acids, unnatural amino acids, substituted amino acids, guanidine, substituted guanidine salts; ammonium, substituted ammonium salts, aluminum salts or acid addition salts. 19. The compound of formula (I), as claimed in claim 18, wherein the salts of organic bases are selected from the group consisting of N,N'-diacetylethylenediamine, betaine, caffeine, 2-diethylaminoethanol, 2-dimethylaminoethanol, N-ethylmorpholine. N- ethylpiperidine, glucamine, glucosamine, hydrabamine, isopropylamine, methylglucamine, morpholine, piperazine, piperidine, procaine, purines, theobromine, triethylamine, trimethylamine, tripropylamine, tromethamine, diethanolamine, meglumine, ethylenediamine, N,N'-diphenylethylenediamine, N,N'-dibenzylethylenediamine, N-benzyl phenylethylamine, choline, choline hydroxide, dicyclohexylamine, metformin, benzylamine, phenylethylamine, dialkylamine, trialkylamine, thiamine, aminopyrimidine, aminopyridine, purine, or spermidine. 20. The compound of formula (I) as claimed in claim 18, wherein the salts of chiral bases are selected from the group consisting of alkylphenylamine, glycinol, or phenyl glycinol. 21. The compound of formula (I) as claimed in claim 18, wherein the salts of natural amino acids are selected from the group consisting of glycine, alanine, valine, leucine, isoleucine, norleucine, tyrosine, cystine, cysteine, methionine, proline, hydroxy proline, histidine, ornithine, lysine, arginine, serine, threonine, or phenylalanine. 22. The compound of formula (I), as claimed in claim 18, wherein the salts of unnatural amino acid, substituted amino acids are selected from the group consisting of D-isomers, guanidine, and substituted guanidine wherein the substituents are selected from the group consisting of nitro, amino, alkyl, alkenyl or alkynyl. 23. A compound of formula (I) as claimed in claim 18, wherein the acid addition salt is selected from the group consisting of sulphates, nitrates, phosphates, perchlorates, borates, halides, acetates, tartrates, maleates, citrates, succinates, palmoates, methanesulphonates, benzoates, salicylates, hydroxynaphthoates, benzenesulfonates, ascorbates, glycerophosphates, or ketoglutarates. 24. A process for the preparation of compound of formula (I), as claimed in claim 1, where R4 represents NHR4 wherein R4 represents hydrogen atom; R2 and R3 may be same or different and independently represent hydrogen, halogen atom, substituted or unsubstituted (C1-C10)alkyl group, halo(C1-C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, ORa where R1 represents substituted or unsubstituted (C1-C10)alkyl group; Y1 and Y2 may be same or different and independently represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or unsubstituted groups selected from (C1-C10)alkyl hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1-C10)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1- C10)alkyl, (C1-C10)alkylsulfonyl, (C1-C10)alkylcarbonylamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10) alkylcarbonyloxy(C1-C10)alkyl, ainino(C1 -C10)alkyl, niono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y1, Y2 may represent =O, =S, substituted or unsubstituted =NOR'" group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises: (i) reacting the compound of formula (la) where Z represents O or S; all other symbols are as defined above, (iii) converting the compound of formula (le) to a compound of formula (If) where R1 represents isoindole-l,3-dione, Z represents O or S, all other symbols are as defined above and (vi) converting the above compound of formula (I), to a compound of formula (I) where R1 represents NHR4 wherein R4 represents hydrogen atom. (vii) and if desire converting the compound obtained in to its derivatives, its anolagous, its tutomaric form, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically solvates by conventionals methods. 25. A process for the preparation of compound of formula (I), as claimed in claim 1, where all symbols are as defined in claim 24, which comprises (i) reacing the compound of formula (li) o where X represents halogen atom, R represents isoindole-l,3-dione, R and R are as defined above, with [(R)3Sn]2, wherein R represents (C1-C6)alkyl group, to obtain a compound of formula (Ij) where R1 represents isoindole-l,3-dione; ...' represents a bond and all other symbols are as defined above and (iii) converting the above compound of formula (I), to a compound of formula (I), where R1 represents NHR4 wherein R4 represents hydrogen atom and (iv) converting the above obtained compound of formula (I), to a compound of formula (I), where '....' represents no bond, by conventional hydrogenation methods, by using a reagent selected from Pt02, Pd/C, Raney nickel or other related reagent, along with H2 gas (v) and if desire converting the compound obtained in to its derivatives, its anolagous, its tutomaric form, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically solvates by conventionals methods. 26. A process for the preparation of compound of formula (I), as claimed in claim 1, where R1 represents NHR4 wherein R4 represents hydrogen atom; R2 and R3 n different and independently represent hydrogen, halogen atom, substituted o (C1-C10)alkyl group, halo(C1-C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, ORa where R1 represents substituted or unsubstituted (C1-C10)alkyl group; Y* and Y^ may be same or different and independently represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or unsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1-C10)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1- Cio)aIkyl, (C1-C10)alkylsulfonyl, (C1-C10)alkylcarbonylamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10) alkylcarbonyloxy(C1-C10)alkyl, amino(C1-Cio)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (CrGio)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y , Y may represent =0, =S, substituted or unsubstituted =NOR"' group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents SO or SO2; -..' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises: (i) converting the compound of formula (I) where R1 represents isoindole-l,3-dione, Z represents S, and all other symbols are as defined above, to a compound of formula (I), where R1 represents isoindole-l,3-dione, Z represents SO or SO2 and (ii) converting the compound of formula (I), where R1 represents isoindole-l,3-dione, Z represents SO or SO2, to a compound of formula (I) where R1 represents NHR4 wherein R1 represents hydrogen atom and all other symbols are as defined above; (iii) and if desire converting the compound obtained in to its derivatives, its anolagous, its tutomaric form, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically solvates by conventional methods. 27. A process for the preparation of compound of formula (I), as claimed in claim 1, where R1 represents azido group; R2 and R3 may be same or different and independently represent hydrogen, halogen atom, substituted or unsubstituted (C1-C10)alkyl group, halo(C1- Cio)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, ORa where R1 represents substituted or unsubstituted (C1-C10)alkyl group; Y and Y may be same or different and independently represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or unsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1- Cio)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (C1-C10)alkylsulfonyl, (C1- Cio)alkylcarbonylamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10) alkylcarbonyloxy(C1-C10)alkyl, amino(C1-C10)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y1, Y2 may represent =0, =S, substituted or unsubstituted =NOR"' group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises: (i) converting the compound of formula (Ig) where R1 represents hydroxy; Z, Y1, Y2, R2, R4 and m are as defined above and (ii) reacting the compound of formula (I) where R1 represents hydroxy group, with MsCl, triethylamine and sodium azide to give a compound of formula (I) where R1 represents azido group and all other symbols are as defined above; (iii) and if desire converting the compound obtained in to its derivatives, its anolagous, its tutomaric form, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically solvates by conventionals methods. 28. A process for the preparation of compound of formula (I), as claimed in claim 1, where R1 represents hydroxy group; R2 and R3 may be same or different and independently represent hydrogen, halogen atom, substituted or unsubstituted (C1-C10)alkyl group, halo(C1- C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, OR4 where R1 represents substituted o10 unsubstituted (C1-C10)alkyl group; Y1 and Y2 may be same or different and independently represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or unsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1- Cio)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (C1-C10)alkylsulfonyl, (C1- Cio)alkylcarbonylamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10) alkylcarbonyloxy(C1-C10)alkyl, amino(C1-C10)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaraikyl, heterocyclyl or heterocycloalkyl; or any one or two of Y , Y may represent =0, =S, substituted or unsubstituted =NOR"' group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises: (i) converting the compound of formula (Ig), where R1 represents substituted or unsubstituted (C1-C10)acyloxy group, and all other symbols are as defined above and (ii) hydrolysis of the compound of formula (I) where R1 represents (C1-C10)acyloxy group, to a compoimd of formula (I), where R1 represents hydroxy group and all other symbols are as defined above; (iii) and if desire converting the compound obtained in to its derivatives, its anolagous, its tutomaric form, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically solvates by conventionals methods. 29. A process for the preparation of compound of formula (I), as claimed in claim 1, where R1 represents NHR4, wherein R" represents substituted or unsubstituted acetyl group; R2 and R3 may be same or different and independently represent hydrogen, halogen atom, substituted or unsubstituted (C1-C10)alkyl group, halo(C1-C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, OR^ where R1 represents substituted or unsubstituted (C1-C10)alkyl group; Y^ and Y may be same or different and independently represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or unsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1-C10)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (C1-C10)alkylsulfonyl, (C1-C10)alkylcarbonylamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10) alkylcarbonyloxy(C1-C10)alkyl, amino(C1-Cio)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y\ Y^ may represent =0, =S, substituted or unsubstituted =NOR'" group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises: converting the compound of formula (I), where R' represents azido group and all other symbols are as defined above. 30. A process for the preparation of compoimd of formula (I), as claimed in claim 1, where R1 represents NHR4, wherein R4 represents substituted or unsubstituted -C(=S)-R4a, wherein R4a represents (C1-C10)alkyl, halo(C1-C10)alkyl, aryl, heteroaryl, -C(=O)-(C1-Cio)alkoxy, -C(=O)-(C1-C10)alkoxy, -C(=O)-aryloxy, -C(=S)-(C1-C10)alkyl or -C(=S)-aryl; R^ and R may be same or different and independently represent hydrogen, halogen atom, substituted or unsubstituted (C1-C10)alkyl group, halo(C1-C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, ORa where Rb represents substituted or unsubstituted (C1-C10)alkyl group; Y1 and Y may be same or different and independently represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or unsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1-C10)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (C1-C10)alkylsulfonyl, (C1-C10)alkylcarbonylamino(C1-C]o)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10) alkylcarbonyloxy(C1-C10)alkyl, amino(C1-Cio)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y^ Y^ may represent =0, =S, substituted or unsubstituted =NOR"' group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises: converting the compound of formula (I), where R1 represents NHR4, where R4 represents substituted or unsubstituted -C(=O)-R4a, wherein R4a represents (C1-C10)alkyl, halo(C1-C10)alkyl, aryl, heteroaryl, -C(=O)-(C1-C10)alkoxy, -C(=O)-aryloxy, -C(=S)-(C1-C10)alkyl or -C(=S)-aryl. 31. A process for the preparation of compound of formula (I), as claimed in claim 1, where R' represents NHR4, wherein R4 represents substituted or unsubstituted -C(=S)-OR'4a', wherein R4b represents (C1-C10)alkyl, cyclo(C3-Cio)alkyl, aryl, (C2-Cio)alkenyl or -C(=O)- (C1-C10)alkyl group; R and R may be same or different and independently represent hydrogen, halogen atom, substituted or unsubstituted (C1-C10)alkyl group, halo(C1-C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, OR4 where R' represents substituted or imsubstituted (C1-C10)alkyl group; Y1 and Y2 may be same or different and independently represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or unsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1- Cio)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (C1-C10)alkylsulfonyl, (C1- Cio)alkylcarbonylamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10) alkylcarbonyloxy(C1-C10)alkyl, amino(C 1 -C 10)alkyl, mono(C 1-C 10)alkylamino, di(C 1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y1, Y2 may represent =0, =S, substituted or unsubstituted =NOR'" group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '-.' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises: (i) reacting compound of formula (I) where R1 represents azido group; and all other symbols are as defined above, with triphenylphosphine/water or H2-Pd/C, to produce a compound of formula (I), where R1 represents NHR4, wherein R4 represents hydrogen atom and all other symbols are as defined above, (ii) reacting compound of formula (I), where R1 represents NHR4, wherein R4 represents hydrogen atom, with thiophosgene or carbon disulfide and chloromethylformate, in the presence of a base to produce a compound of formula (I), where R1 represents isothiocyanate group; and all symbols are as defined earlier, (iii) converting compound of formula (I) where R1 represents isothiocynate group, to a compound of formula (I), where R1 represents NHR4, wherein R4 represents substituted or unsubstituted -C(=S)-OR4b, wherein R4b is as defined above and all other symbols are as defined above, (iv) and if desire converting the compound obtained in to its derivatives, its anolagous, its tutomaric form, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically solvates by conventionals methods. 32. A process for the preparation of compound of formula (I), as claimed in claim 1, where R1 represents NHR4, wherein R4 represents substituted or unsubstituted groups selected from -C(=S)-NH2, -C(=S)-NH-(C1-C10)alkyl, -C(-S)-N-((C1-C10)alkyl)2, -C(=S)- NH-(C2-C10)alkenyl, C(=S)-NH-C(=O)-aryl, -C(=S)-NH-aralkyl, -C(=S)-NH-heteroaralkyl or -C(=S)-N(R'R"), wherein R' and R" groups together form a substituted or unsubstituted 5 or 6 membered cyclic structures containing nitrogen and optionally one or two additional hetero atoms selected from oxygen, nitrogen or sulfur; R and R may be same or different and independently represent hydrogen, halogen atom, substituted or unsubstituted (C1- C10)alkyl group, halo(C1-C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, ORa where R1 represents substituted or unsubstituted (C1-C10)alkyl group; Y^ and Y^ may be same or different and independently represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or unsubstituted groups selected from (Ci 'C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1-C10)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1- C io)alkyl, (C1-C10)alkylsulfonyl, (C i -Ci o)alkylcarbonylamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10) alkylcarbonyloxy(C1-C10)alkyl, amino(C1-C10)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Ya, Y2 may represent =O, =S, substituted or unsubstituted =NOR"' group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises: converting the compound of formula (I) where R1 represents isothiocyanate group. 33. A process for the preparation of compound of formula (I), as claimed in claim 1, where R1 represents NHR4, wherein R4 represents substituted or unsubstituted -C(=S)-SR'4c, wherein R ^ represents (C1-C10)alkyl group; R and R may be same or different and independently represent hydrogen, halogen atom, substituted or unsubstituted (C]-C10)alkyl group, halo(C1-C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, OR^ where R1 represents substituted or unsubstituted (C1-C10)alkyl group; Y and Y may be same or different and independently represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or xmsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1-C10)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (C\- C10)alkylsulfonyl, (C1-C10)alkylcarbonylamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10) alkylcarbonyloxy(C1-C10)alkyl, amino(C1-C10)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y , Y may represent =0, =S, substituted or unsubstituted =NOR"' group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents 0, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises: converting the compound of formula (I), where compound of formula (I), where R1 represents NHR4, wherein R1 represents hydrogen atom. 34. A process for the preparation of compound of formula (I), as claimed in claim 1, V where R' represents NHR4, wherein R4 represents substituted or unsubstituted -C(=S)-NH- R4D, wherein R4d represents -C(=O)-aryl group; R2 and R3 may be same or different and independently represent hydrogen, halogen atom, substituted or unsubstituted (C1-C10)alkyl group, haIo(C1-C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, OR4 where R1 represents substituted or unsubstituted (C1-C10)alkyl group; Y and Y may be same or different and independently represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or unsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1-C10)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (Cr C10)alkylsulfonyl, (C1-C10)alkylcarbonylamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10) alkylcarbonyloxy(C1-C10)alkyl, amino(C1-C10)alkyl, mono(Ci" C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y , Y may represent =0, =S, substituted or unsubstituted =NOR"' group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises: converting the compound of formula (I), where R1 represents NHR4, wherein R"^ represents hydrogen atom, 35. A process for the preparation of compound of formula (I), as claimed in claim 1, where R1 represents NHR4, wherein R4 represents substituted or unsubstituted -C(=O)- heteroaryl; R and R may be same or different and independently represent hydrogen, halogen atom, substituted or unsubstituted (C1-C10)alkyl group, halo(C1-C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, OR4 where R1 represents substituted or unsubstituted (C1- C10)alkyl group; Y and Y may be same or different and independently represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or unsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1-C10)alkyl, (C1- C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (C1-C10)alkylsulfonyl, (d- C]o)alkylcarbonylamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10) alkylcarbonyloxy(C1-C10)alkyl, amino(C1-C10)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y , Y may represent =0, ==S, substituted or unsubstituted =NOR'" group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises: converting the compound of formula (I), where R1 represents NHR4, wherein R4 represents hydrogen atom. 36. A process for the preparation of compound of formula (I), as claimed in claim 1, where R1 represents NHR4, wherein R4 represents substituted or unsubstituted -C(=O)-R4a wherein R4d represents (C1-C10)alkyl, (C1-C10)alkoxy, (C2-C10)alkenyl, halo(C1-C10)alkyl, aryl, aryloxy, heteroaryl, (C2-C10)alkenyloxy, (C1-C10) alkylcarbonyl, arylcarbonyl, aryloxycarbonyl, (C1-C10)alkoxycarbonyl, (C1-C10) alkylthiocarbonyl or (C1- C10)arylthiocarbonyl; R and R may be same or different and independently represent hydrogen, halogen atom, substituted or unsubstituted (C1-C10)alkyl group, halo(C1-C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, ORa where R1 represents substituted or unsubstituted (C1-C10)alkyl group; Y and Y may be same or different and independently represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or unsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1- C10)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (C1-C10)alkylsulfonyl, (C1- C10)alkylcarbonylamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10) alkylcarbonyloxy(C1-C10)alkyl, amino(C1-C10)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y\ Y^ may represent =0, =S, substituted or unsubstituted =NOR'" group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises: converting the compound of formula (I), where R1 represents NHR4, wherein R4 represents hydrogen atom. 37. A process for the preparation of compound of formula (I), as claimed in claim 1, where R1 represents NHR4, wherein R4 represents substituted or unsubstituted -C(=NH)-NH2; R2 and R3 may be same or different and independently represent hydrogen, halogen atom, substituted or unsubstituted (C1-C10)alkyl group, halo(C1-C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, ORa where R1 represents substituted or unsubstituted (C1-C10)alkyl group; Ya and Y may be same or different and independently represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or unsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1-C10)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (C1-C10)alkylsulfonyl, (C1-C10)alkylcarbonylamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10) alkylcarbonyloxy(C1-C10)alkyl, amino(C1-C10)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y , Y may represent =O, =S, substituted or unsubstituted =NOR"' group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises: (a) converting the compound of formula (I), where R1 represents NHR4, wherein R"* represents hydrogen atom. (b) and if desire converting the compound obtained in to its derivatives, its anolagous, its tutomaric form, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically solvates by conventionals methods. 38. A process for the preparation of compound of formula (I), as claimed in claim 1, where all symbols are as defined in claim 37, which comprises : (a) converting the compound of formula (I), where R1 represents NHR', wherein R represents substituted or unsubstituted group selected fi"om -S(0)2(C1-C10)alkyl or -S(0)2aryl group. (b) and if desire converting the compound obtained in to its derivatives, its anolagous, its tutomaric form, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically solvates by conventional methods. 39. A process for the preparation of compoimd of formula (I), as claimed in claim 1, where R1 represents NHR4, wherein R4 represents substituted or unsubstituted group selected from -C(=NH)-(C1-C10)alkyl or -C(=NH)-aryl; R2 and R3 may be same or different and independently represent hydrogen, halogen atom, substituted or imsubstituted (C1-C10)alkyl group, halo(C1-C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, ORa where R1 represents substituted or imsubstituted (C1-C10)alkyl group; Y1 and Y2 may be same or different and independently represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or unsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1-C10)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (C1- C10)alkylsulfonyl, (C1-C10)alkylcarbonyIamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10) alkylcarbonyloxy(C1-C10)alkyl, amino(C1-C10)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y1, Y2 may represent =0, =S, substituted or unsubstituted =NOR"' group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises: (i) reacting the compound of formula (I) where R1 repersents NHR'^, wherein R" represents -C(=S)-NH2 and all other symbols are as defined above, with di tert-butoxy carbonyl ether ((B0C)20), to produce a compound of formula (I) where R1 represents NHR4, wherein R4 represents -C(=S)-NH2 group substituted with tert- butoxy carbonyl group and all symbols are as defined above and (ii) reacting the above compound of formula (I), with a compound of formula (Ik) R7-NH2 (Ik) where R1 represents substituted or unsubstituted (C1-C10)alkyl or aryl group, to produce a compound of formula (I) where R1 represents NHR4 where R4 represents substituted or unsubstituted group selected fi-om -C(=NH)-(C1-C10)alkyl or -C(=NH)-aryl group and all other symbols are as defined above (iii) and if desire converting the compound obtained in to its derivatives, its anolagous, its tutomaric form, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically solvates by conventionals methods. 40. A process for the preparation of compound of formula (I), as claimed in claim 1, where R represents halogen atom; R and R may be same or different and independently represent hydrogen, halogen atom, substituted or unsubstituted (C1-C10)alkyl group, halo(Cr C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, ORa where R1 represents substituted or unsubstituted (C1-C10)alkyl group; Y and Y may be same or different and independently represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or unsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1- C10)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (C1-C10)alkylsulfonyl, (C1- C10)alkylcarbonylamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (CpC10) alkylcarbonyloxy(C1-C10)alkyl, amino(C1-C10)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y , Y may represent =O, =S, substituted or unsubstituted =NOR'" group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises: (a) converting the compound of formula (I), where R1 represents hydroxy group (b) and if desire converting the compound obtained in to its derivatives, its anolagous, its tutomaric form, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically solvates by conventional methods. 41. A process for the preparation of compound of formula (I), as claimed in claim 1, • * where R represents thioalcohol; R and R may be same or different and independently represent hydrogen, halogen atom, substituted or unsubstituted (C1-C10)alkyl group, halo(Cr C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, ORa where R1 represents substituted or unsubstituted (C1-C10)alkyl group; Y and Y may be same or different and independently represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or unsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1- C10)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (C1-C10)alkylsulfonyl, (C1- C10)alkylcarbonylamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10) alkylcarbonyloxy(C1-C10)alkyl, amino(C1-C10)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of YA, Y2 may represent =O, =S, substituted or unsubstituted =NOR'" group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises; (i) reacting the compound of formula (I) where R1 represents halogen atom, to produce a compound of formula (Im), where all other symbols are as defined above, with a base and thiolacetic acid and (ii) reacting the compound of formula (Im), to produce a compound of formula (I) where R1 represents 'SH' group and all other symbols are as defined above, (iii) and if desire converting the compound obtained in to its derivatives, its anolagous, its tutomaric form, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically solvates by conventional methods. 42. A process for the preparation of compound of formula (I), as claimed in claim 1, where R1 represents NHR4 wherein R4 represents substituted or unsubstituted -S(O)2(C1- C10)alkyl or -S(0)2aryl group; R and R may be same or different and independently represent hydrogen, halogen atom, substituted or unsubstituted (C1-C10)alkyl group, halo(C1- C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, ORa where R1 represents substituted or unsubstituted (C1-C10)alkyl group; Y1 and Y2 may be same or different and independently represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or unsubstituted groups selected fi"om (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1- C10)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (C1-C10)alkylsulfonyl, (C1- C10)alkylcarbonylamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10) alkylcarbonyloxy(C1-C10)alkyl, amino(C1-C10)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y1, Y2 may represent =O, =S, substituted or unsubstituted =NOR'" group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises: (i) converting the compound of formula (I), where R1 represents NHR4 where R represents hydrogen atom (ii) and if desire converting the compound obtained in to its derivatives, its anolagous, its tutomaric form, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically solvates by conventionals methods. 43. A pharmaceutical composition comprising a compound of formula (I) as claimed in claim 1 and a pharmaceutically acceptable carrier, diluent, excipient or solvate. 44. The pharmaceutical composition as claimed in claim 43, in the form of a tablex, capsule, powder, syrup, solution or suspension. 45. A composition comprising a compound as claimed in claim 17 and a pharmaceutically acceptable carrier, diluent, excipient or solvate. 46 The pharmaceutical composition as claimed in claim 45, in the form of a tablet, capsule, powder, syrup, solution or suspension.

Full Text

Field of the Invention
The present invention provides novel triazole compounds of formula (I), their I derivatives, their analogs, their tautomeric forms, their regioisomers, their rotamers, their 1 stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their prodruge, their metabolites, their pharmaceutically acceptable solvates and pharmaceutical compositions containing them. More particularly, the present invention relates to novel triazoles of the general formula (I).

their derivatives, their analogs, their tautomeric forms, their regioisomers, their rotamers, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their prodrugs their metabolites, their pharmaceutically acceptable solvates and pharmaceutical compositions containing them.
The present invention also relates to a process for the preparation of the above said novel compounds, their derivatives, their analogs, their tautomeric forms, their regioisomers, their rotamers, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their prodruge, their metabolites, their pharmaceutically acceptable solvates and pharmaceutical compositions containing them.
The present invention also relates to novel intermediates, methods for their preparation and their use in the preparation of compounds of formula (I).
Background of the Invention
Since the discovery of penicillin, pharmaceutical companies have produced more than one hundred antibacterial agents to combat a wide variety of bacterial infections. In the past several years, due to the misuse of these antibiotics there has been rapid emergence of bacterial resistance to several of these antibiotics. The multidrug resistance among these bacterial pathogens may also be due to mutation leading to more virulent clinical isolation, the most disturbing milestone has been the acquisition of resistance to vancomycin, an antibiotic generally regarded as the agent of last resort for serious Gram-positive infections. This growing multidrug resistance has recently rekindled interest in the search for new structural class of antibiotic that inhibit or kill these bacteria possibly by novel mechanisms.

A problem of larger dimension is the increasing incidence of the more virulent, Methicillin-Resistant Staphylococcus Aureas (MRSA) among clinical isolates found worldwide. Many MRSA strains are resistant to most of the known antibiotics, but have remained sensitive to vancomycin. However, in view of the increasing reports of vancomycin resistant clinical bacterial isolates and growing problem of bacterial resistance, there is an urgent need for new molecular entities effective against the emerging and currently problematic Gram-positive organisms.
Bacterial infections and antibacterial resistance are long term problems that call for innovative new therapeutics.
There is an urgent need for novel antibacterial compounds. The wide spread use, rather misuse of antibacteria has led to an increase in multidrug resistant bacteria. This is further escacerbated by the use of antibacterials as feed supplements in farm animals and poultry. Yet new classes are unfortimately difficult to develop and any new drugs may quickly loose effectiveness, for example, the first entirely new antibacterial released in market over the past 30 years like Linezolid (Zyovx , Pharmacia Upjohn) proves the capacity for microorganism to develop resistance. Soon after introduction, clinics reported cases of resistance (Lancet 2001, 358(9277): 207-8) and resistant strains have been selected in the lab where a target site alteration was found to reduce drug binding (Antimicrob. Agents Chemother. 2001, 3(3): 288-294)
Advancements have been made by several firms in expanding oxazolidinons (Linezolide class of compounds) SAR (structure activity relationship) as well as the spectrum of activity to include the fastidious Gram negative organisms such as Hemophilus influenzae (H. influenzae) and Morexella catarrhalis (M. catarrhalis).
With this background we initiated our research program in the area of triazoles and invented new class of chemical entities such as 1,2,3-triazoles effective against wide variety of infectious pathogens including Gram positive/Gram negative and aerobic, anaerobic bacteria.
Various l,2,3-tria2oles, 1,2,4-triazoles and benzotriazoles have been reported to show biological activities ranging from anti-inflammatory to antiproliferative and have therefore found applications in medicinal chemistry. The literature survey particularly reveals the use of 1,2,3-triazoles, for the treatment of neuropathic pain and associated hyperalgesia, including trigeminal and herpectic neuralgia, diabetic neuropathic pain, migraine, causalgia and

deafferentation syndromes such as brachial plexus avulsion, an anticoccidiostat, as antiproliferative agents, for antimetastatic activity in a model of ovanan cancer progression, for anti-inflammatory effect, controlling activity against noxious organisms, for the treatment of ischemia, anti-human immunodeficiency virus activity etc.
However, there are no reports of l,2,3-tria2ole derivatives of the present invention being used for treating bacterial infections, specifically against multidrug resistant strains.
The new class of triazoles of the present invention is useful for the treatment of a number of resistant and sensitive gram-positive strains both in vitro and in vivo. (a) Chem. Pharm. Bull. 48(12), 1935-1946 (2000) discloses the triazoles of formula (ia) and (ib), which are reported as antifungal agents,

where X represents N, CH or CH2.
U.S. 6,054,471 discloses fluorinated triazoles of the formula (ii), which are reported for the treatment of neuropathic pain and associated hyperalgesia, including trigeminal and herpectic neuralgia, diabetic neuropathic pain, migraine, causalgia and deafferentation syndromes such as brachial plexus avulsion,

where Ph is an o-fluorinated phenyl group which may be additionally substituted by 1 or 2 halogen atoms selected from fluorine and chlorine; R11 is hydrogen, carbamoyl, N-(C2-C5) alkanoylcarbamoyl or N,N"di-(C1-C4)alkylcarbamoyl; R21 is carbamoyl, N-(C2-C5) alkanoylcarbamoyl or N,N-di- (C1-C4) alylcarbamoyl.
An example of this class of compounds is shown in formula (iia),

(c) J. Med. Chem., 2843, 1991 discloses compound of formula (iii), which is an
anticoccidiostat and also been found to have antiproliferative activity in several disease
models and to posses antimetastatic activity in a model of ovarian cancer progression,

(d) J. Heterocycl. Chem., 609, 1989 discloses compound of formula (iv), which is reported
for anti-inflammatory effects,

(e) EPO publication no 0304221 A2 discloses compounds of formula (v), which are reported
as antiproliferative agents,

wherein p is 0 to 2; m is 0 to 4; and n is 0 to 5; X is O, S, SO, SO2, CO, CHCN, CH2 or C= NR6 where R6 is hydrogen, loweralkyl, hydroxy, loweralkoxy, amino loweralkylamino. diloweralkylamino or cyano, and, R'4 and R'5 are independently halogen, cyano, trifluoromethyl, loweralkanoyl, nitro, loweralkyl, loweralkoxy, carboxy, carbalkoxy, trifluoromethoxy, acetamido, loweralkylthio, loweralkylsulfonyl, trichlorovinyl, trifluoromethylthio. trifluoromethylsuifmyl, or trifluoromethylsulfonyl;

R'2 is amino, mono or diloweralkylamino, acetamido, acetimido, ureido, formamido, or
guanidino; and
R'a is carbamoyl, cyano. carbazoyl, amidino or N-hydroxycarbamoyl.
An example of this class of compounds is shown in formula (va),

Summary of the Invention
With an objective to develop novel compounds effective against a number of human and veterinary pathogens sensitive as well as resistant to various antiinfectives, including Gram-positive, Gram-negative, aerobic and anerobic bacteria. The pathogens such as MRSA, Streptococci including Str pneumoniae, Str. pyogenes, Enterococci as well as anaerobic organisms such as Bacteroides spp., Clostridia spp. species and Acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp. fastidious Gram negative organisms, H. influenzae, M. catarrhalis and several other bacterial species resistant to fluoroquinolone, Macrolide, Vancomycin, Aminoglycosides, Streptogramin, Lincosamides and (3-Lactam, we focussed our research to develop new compounds effective against the above mentioned organisms, as well as expanded spectra of activity to include community acquired pneumonia (CAP). Efforts in this direction have led to the preparation of compounds having general formula (I) as defined above.
The present invention provides novel 1,2,3-triazole derivatives of the general formula (I) as defined above and their derivatives, their analogs, their tautomeric forms, their regioisomers, their rotamers, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their prodruge, their metabolites, their pharmaceutically acceptable solvates and pharmaceutical compositions containing them, or their mixtures having enhanced activities, without toxic effect or with reduced toxic effect.
The present invention also provides a process for the preparation of novel 1,2,3-triazole derivatives of the formula (I) as defined above and their derivatives, their analogs, their tautomeric forms, their regioisomers, their rotamers, their stereoisomers, their polymorphs, their prodruge, their metabolites and their pharmaceutically acceptable salts.

An aspect of the present invention is to provide pharmaceutical compositions containing compounds of the general formula (I), their analogs, their derivatives, their tautomers, their stereoisomers, their rotamers, their regioisomers, their polymorphs, their salts, solvates or their mixtures in combination with suitable carriers, solvents, diluents and other media normally employed in preparing such compositions.
Detailed description of the Invention
The present invention provides compounds of general formula (I),

where R represents halogen, azido, thioalcohol, isothiocyanate, hydroxy, isoindole-l,3-dione,
substituted or unsubstituted (C1-C10)alkylsulfonyloxy, arylsulfonyloxy, (C1-C10)acyloxy
group, NHR4 where R4 represents substituted or unsubstituted groups selected from (C1-
C10)alkyl, (C1-C10)acyl, thio(C1-C10)acyl, (C1-C10)alkoxycarbonyl, (C3-
C10)cycloalkoxycarbonyl, (C3-C10)cycloalkoxythiocarbonyl, (C2-C10)alkenyloxycarbonyl, (C2-C10)alkenylcarbonyl, heteroaryl, aryloxycarbonyl, heteroarylcarbonyl, heteroarylthiocarbonyl, (C1-C10)alkoxythiocarbonyl, (C2-C10)alkenyloxythiocarbonyl, aryloxythiocarbonyl, -C(=O)-C(=O)-(C1-C10)alkyl, -C(=O)-C(=O)-aryl, -C(=O)-C(=O)-(C1-C10) alkoxy, -C(=O)-C(=O)-aryloxy, -C(=O)-C(=S)-(C1-C10)alkyl, -C(=O)-C(=S)-aryl, -C(=S)-S-(C1-C10)alkyl, -C(=S)-NH2, -C(-S)-NH-(CrC,o)alkyl, -C(=S)-N-((C1-C10)alkyl)2, -C(=S)-NH-(C2-C10)alkenyl, -C(-S)-C(=O)- (C1-C10)alkoxy, -C(=S)-C(-0)-aryloxy, -C(=S)-0-C(=O)-(C1-C10) alkyl, -C(=S)-C(=S)-(Ct-C,o)alkyl, -C(=S)-C(=S)-aryl, -C(=S)-NH-C(=O)-aryl, -C(=S)-NH-aralkyl, -C(=S)-NH.heteroaralkyl, -C(=NH)-NH2, -C(=NH)-(C1-C10)alkyl, -C(=NH)-aryl, -S (O)2(C1-C10)alkyl, -S(O)2aryl, thiomorpholinylthiocarbonyl, pyrrolidinylthiocarbonyl or -C(=S)-N(R'R"), where R' and R" together form a substituted or unsubstituted 5 or 6 member heterocycle ring containing nitrogen and optionally having one or two additional hetero atoms selected from O, S or N; R and R may be same or different and independently represent hydrogen, halogen atom, substituted or unsubstituted (C1-C10)alkyl group, halo(C1-C10)aIkyl, aryl, heteroaryl, aralkyl, cyano, nitro, OR4 where Ra represents substituted or unsubstituted (C1-C10)alkyl group; Y1 and Y3 may be same or different and independently represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or

unsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(Cr
C10)alkyI, (C1-C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (C1-C10)alkylsulfonyl, (C1-
C10)alkylcarbonylamino(C1-C10)alkyl arylcarbonylamino(C1-C10)alkyl, (C1-C10)
aIkylcarbonyloxy(C1-C10)alkyl, amino(C1-C10)alkyl, mono(C1-C10)alkylaniino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyi, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y1, Y2 may represent =O, =S, substituted or unsubstituted =NOR"' group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyi group; Z represents 0, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates.
Suitable groups represented by R4 are described as (C1-C10)alkyl group such as
methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-hntyl and the like, the (CpC10)alkyl
group may be substituted; (C1-C10)acyl group such as -C(=O)H, -C(=O)CH3, -
C(=O)CH2CH3, -C(=O)(CH2)2CH3, -C(=O)(CH2)3CH3, -C(=O)(CH2),CH3.
-C(=O)(CH2)5CH3, -C(=O)Ph and the like, the (C1-C10)acyl group may be substituted;
thio(C1-C10)acyl group such as -C(=S)H, -C(=S)CH3, -C (=S)CH2CH3, -C(=S)Ph and the
like, the thio(C1-C10)acyl group may be substituted; (C1-C10) alkoxycarbonyl group containing
(C1-C10)alkyl group which may be linear or branched such as methoxycarbonyl,
ethoxycarbonyl, propoxycarbonyl, isopropoxycarbonyl and the like, the (C1 -
C10)alkoxycarbonyl group may be substituted; (C3-C10)cycloalkoxycarbonyl such as
cyclopropoxycarbonyl, cyclobutoxycarbonyl and the like, the (C3-C10) cycloalkoxycarbonyl
may be substituted; (C3-C10)cycloalkoxythiocarbonyl such as cyclopropoxythiocarbonyl,
cyclobutoxythiocarbonyl and the like, the (C3-C10) cycloalkoxythiocarbonyl may be
substituted; (C2-C10)alkenylcarbonyl such as ethenylcarbonyl, propenylcarbonyl,
butenylcarbonyl and the like, the (C2"C10)alkenylcarbonyl may be substituted; heteroaryl
group such as pyridyl, furyl, thiophenyl, benzothiazoyl, purinyl, benzimidazoyl, pyrimidinyl,
tetrazolyl and the like, the heteroaryl group may be substituted; heteroarylcarbonyl such as
pyridylcarbonyl, furylcarbonyl, thiophenylcarbonyl, benzothiazoylcarbonyl,
benzimidazoylcarbonyl, pyrimidinylcarbonyl, pyridazinecarbonyl, pyrimidinecarbonyl, pyrazinecarbonyl, tetrazolylcarbonyl and the like, the heteroarylcarbonyl group may be substituted, heteroarylthiocarbonyl such as pyridylthiocarbonyl, furylthiocarbonyl.

thiophenyithiocarbonyl, benzothiazoyylhiocarbonyl, benzimidazoylthiocarbonyl,
pyrimidinylthiocarbonyl, pyridazinethiocarbonyl, pyrimidinethiocarbonyl,
pyrazinethiocarbonyl, tetrazolylthiocarbonyl and the like, the heteroarylthiocarbonyl may be substituted, (C2-C io)alkenyloxycarbonyl group such as ethenyloxycarbonyl, propenyloxycarbonyl, butenyloxycarbonyl and the like, the (C2-C10)alkenyloxycarbonyl may be substituted; aryloxycarbonyl group such as phenoxycarbonyl, benzyloxycarbonyl group and the like, the aryloxycarbonyl group may be substituted; (C1-C10)alkoxythiocarbonyl group such as CH3O-C(-S)-, C2H5O-C(=S)- CBHTO-Q-S)- and the like, (C1-C10)alkoxythiocarbonyl group may be substituted; (C2-C10)alkenyloxythiocarbonyl group such as ethenyloxythiocarbonyl, propenyloxythiocarbonyl, butenyloxythiocarbonyl and the like, the (C2-C10) alkenyloxythiocarbonyl group may be substituted; aryloxythiocarbonyl group such as (phenyl)0-C(=S)-, (benzyI)O-C(=S)- and the like, which may be substituted; -C(=O)-C(=O)-(C1-C10)alkyl group such as -C(=O)-C(=O)methyl, -C(=O)"C(=O)ethyl, -C(=O)-C(=O)propyl and the like, which may be substituted; -C(=O)-C(=O)-aryl group such as -C(=O)-C(=O)phenyl, -C(=O)-C(=O)naphthyl and the like, which may be substituted; -C(=O)-C(=O)-(C1-C10)alkoxy group such as -C(=O)-C(=O)methoxy, -C(=O)-C(=O)ethoxy, -C(-O)" C(=O)propyloxy and the like, which may be substituted; -C(=O)-C(=O)-aryloxy group such as -C(=O)-C(=O)phenyloxy, -C(=O)-C(=O)benzyloxy, which may be substituted; -C(=O)-C(=S)-(C1-C10)alkyl group such as -C(=O)-C(=S)-methyl, -C(=O)-C(=S)-ethyl, -C(=O)" C(=S)-propyl, -C(=O)-C(=S)-butyl and the like, which may be substituted; -C(=O)-C(=S)-aryl group such as -C(-0)-C(=S)-phenyl, -C(=O)-C(=S)-naphthyl and the like, which may be substituted; -(C-S)-S-(C1-C10)alkyl such as -(C=S)"S-methyl, -(C=S)^S-ethyl, ^(C=S)-S-propyl and the like, which may be substituted; -(C=S)-NH2, which may be substituted; -(C=S)-NH-(C1-C10)alkyl such as -(C=S)-NH-methyl, -(C=S)-NH-ethyl, "(C=S)-NH-propyl and the like, which may be substituted; "C(=S)-N-((CrC6)alkyl)2 such as -C(=S)-N-(methyl)2, -C(=S)-N-(ethyl)2, -C(=S)-N-(propyl)2 and the like, which may be substituted; -C(=S)-NH-(C2-C10)alkenyl such as -C(=S)-NH-ethenyl, -C(=S)-NH"propenyl, -C (=S)-NH"butenyI and the like, which may be substituted; -(C=SHC=O)-(C1-C10)alkoxy such as -(C=S)-(C=O)-methoxy, -(C=S)-(C=O)-ethoxy, -(C=S)-(C=O)-propoxy and the like, which may be substituted; -(C=S)-(C=O)-aryloxy such as -(C=S)-(C=O)-phenyloxy, -(C=S)-(C=O)-naphthyloxy and the like, which may be substituted; -C(=S)-O-(C=O)-(C1-C10)alkyl such as -C(=S)-O-(C=O)-methyl, -C(=S)-O-(C=O)-ethyl, -C(=S)-O-(C=O)-propyl and the like, which

may be substituted; -C(=S)-C(=S)-(C1-C10)alkyl group such as -C(=S)-C(=S)methyl, -C(=S)-C(=S)ethyl, -C(=S)-C(=S)propyl and the like, which may be substituted; -C(=S)-C(=S)aryl group such as -q=S)-C(=S)phenyl, -C(=S)-C(=S)naphthyl and the like, which may be substituted; -C(=S)-NH-C(=O)-aryl group such as -C(=S)-NH-C(=O)-phenyl, -C(=S)-NH-C(^0)-naphthyl and the like, ^C(=S)-NH-C(=O)-aryl group may be substituted; -C(=S)-NH-aralkyl group such as -C(=S)-NH-benzyl, -C(=S)-NH-phenethyl, -C(=S)-NH-C6H5CH2CH2CH2, -C(=S)-NH-naphthylmethyI and the like, -C(=S)-NH-aralkyl group may be substituted; -C(=S)-NH-heteroaralkyl such as -C(=S)-NH-pyridinemethyl, -C(=S)-NH-furanmethyl, -C(=S)-NH-thiophenylenemethyl, -C(=S)-NH-benzothiazolemethyl, -C(=S)-NH-benzimidazolemethyl, -C(=S)-NH-pyrimidinemethyl, -C(=S)-NH-pyrimidinemethyl, -C(^S)-NH-pyrazinemethyl, -C(=S)-NH-tetrazolemethyl and the like, where -C(=S)-NH-aralkyl group may be substituted; -C(=NH)-NH2, which may be substituted; -C(=NH)-(C1-C10)alkyl such as -C(=NH)-methyI, -C(=NH)-ethyl, -C(=NH)-propyl and the like, which may be substituted; -C(=NH)-aryi such as -C(=NH)-phenyl, -C(=NH)-naphthyl and the like, which may be substituted; S(O)2-(C1-C10)alkyl such as S(O)2-methyl, S(O)2"ethyl, S(O)2-propyl, S(O)2-isopropyl, S(O)2-butyl, S(O)2-isobutyl and the like, which may be substituted; S(O)2-aryl such as S(O)2-phenyl, S(O)2-naphthyl and the like, which may be substituted; thiomorpholinylthiocarbonyl, which may be substituted; pyrrolidinylthiocarbonyl, which may be substituted; or -C(=S)-N(R'R") where R'R' are as defined above.
A 5 or 6 member heterocycle ring containing nitrogen, optionally having one or two additional heteroatoms selected from oxygen, nitrogen or sulfur, formed by R' & R" is selected from unsubstituted or substituted pyrrolidinyl, pyrroiyl, morpholinyl, thiomorpholinyl, benzothiazole, benzoimidazolyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl and the like.
When the groups represented by R4, R4a 44b, 44d, R4c, R, R2 and heterocycles formed by R'and R" are substituted, the substituents may be selected from halogen atom such as chlorine, fluorine, bromine and iodine; hydroxy, amino, cyano, nitro, (C1-C10)alkyl, which is defined as earlier; hydroxy(C1-C10)alkyl, in which (C1-C10)alkyl groups is as defined earher; (C1-C10)alkoxy group such as methoxy, ethoxy, propoxy and the like; =O, =S, aryl group such as phenyl, naphthyl and the like, hydroxyaryl such as hydroxyphenyi, hydroxynaphthyl and the like, pyridyl, mono(C1-C10)alkylamino such as methylamino, ethylamino, propylamino and the like; di(C1-C10)alkylamino such as dimethyl amino,

diethylamino, dipropylamino and the like; (C1-C10)acyl group such as -C(=O)H, -C(=O)CH3,
-C(=O)CH2CH3, -C(=O)(CH2)2CH3, -C(=O)(CH2)3CH3, -C(=O)(CH2)4CH3,
-C(=O)(CH2)5CH3, ^-C(=O)Ph and the like; thio(C1-C10)acyl group such as -C(=S)H, -C(=S)CH3, -C (=S)CH2CH3, -C(=S)Ph and the like; (C1-C10)alkoxycarbonyl group such as methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, butoxycarbony, tert-butoxycarbonyl(BOC) and the like; (C1-C10)alkoxyaryl group such as methoxyaryl, ethoxyaryl, propoxyaryl, iso-propoxyaryl, butoxyaryl and the like, where aryl group is as defined above or carboxylic acid or its derivatives selected from amides and esters such as CONH2, CONHMe, CONMe2, CONHEt, CONEt2, CONHPh, COOCH3, COOC2H5 or COOC3H7.
Suitable groups represented by R and R may be selected from hydrogen, halogen atom such as fluorine, chlorine or bromine; substituted or unsubstituted (C1-C10)alkyl group such as methyl, ethyl, n-propyl, isopropyl, n-butyl, iso-butyl, t-butyl, n-pentyl, iso-pentyl, n-hexyl and the like; halo(C1-C10)alkyl group such as halomethyl, haloethyl, halopropyl, trihalomethyl and the like, wherein the halo group is selected from fluorine, chlorine, bromine or iodine; cyano, nitro; aryl group such as phenyl, napthyl and the like; heteroaryl or aralkyl groups is as defined above; ORa where Ra represents substituted or unsubstituted (C1-C10) alkyl group such as methyl, ethyl, propyl, isopropyl and the like.
Suitable substitutents on R1 , R2 and Ra are selected from hydroxy, halogen, nitro, amino, (C1-C10)alkyl, (C1-C10)alkoxy, =O, =S, cyano group, or carboxylic acid or its derivatives. These groups are as defined above.
Suitable groups represented by Y and Y are selected from hydrogen, cyano, nitro, formyl, hydroxy, amino, halogen such as fluorine, chlorine, bromine or iodine;, substituted or unsubstituted (C1-C10)alkyl such as methyl, ethyl, n-propyl, isopropyl, n-butyl, iso-butyl, t-butyl and the like, which may be substituted; hydroxy(C1-C10)alkyl such as hydroxymethyl, hydroxyethyl, hydroxypropyl and the like, which may be substituted; (C1-C10)alkoxy(Cj-Cto) alkyl group such as methoxymethyl, methoxyethyl, ethoxyethyl, ethoxymethyl, methoxypropyl, propoxymethyl, propoxyethyl and the like, which may be substituted; (C1-C10)alkoxycarbonyl group such as methoxycarbonyl, ethoxycarbonyl and the like, which may be substituted; carboxy(C1-C10)alkyl such as -OOC-CH3, -OOC-CH2-CH3 and the like, which may be substituted; (C1-C10)alkylsulfonyl group such as methylsulfonyl, ethylsulfonyl and the like, which may be substituted; (C1-C10)alkylcarbonylamino(C1-C10)alkyl groups such as

methylcarbonylaminomethyl, ethylcarbonylaminomethyl, methylcarbonylaminoethyl and the
like, which may be substituted; arylcarbonylamino(C1-C10)alkyl such as
phenylcarbonylaminomethyl, phenylcarbonylaminoethyl and the like, which may be
substituted; (C1-C10)aIkylcarbonyloxy(C1-C10)alkyl group such as methylcarbonyloxymethyl,
ethylcarbonylxoymethyl, methylcarbonyloxyethyl, propylcarbonyloxymethyl,
propylcarbonyloxyethyl, propylcarbonyloxypropyl and the like, which may be substituted; amino(C1-C10)alkyl such as aminomethyl, aminoethyl, aminopropyi and the like, which may be substituted; mono(C1-C10)alkyIamino such as methylamino, ethylamino, propylamino and the like, which may be substituted; di(C1-C10)alkylamino such as dimethylamino, diethylamino, dipropylamino and the like, which may be substituted; arylamino such as phenylamino, benzylamino and the like, which may be substituted; (C1-C10)alkoxy group such as methoxy, ethoxy, propoxy, isopropoxy and the like, which may be substituted; aryl group such as phenyl, naphthyl and the like, which may be substituted; aryloxy group such as phenoxy, naphthyloxy and the like, the aryloxy group may be substituted; aralkyl such as benzyl, phenethyl, C6H5CH2CH2CH2, naphthylmethyl and the like, the aralkyl group may be substituted; heteroaryl groups such as pyridyl, thienyl, furyl, pyrrolyl, oxazolyl, thiazolyl, pyrazolyi, imidazoiyi, oxadiazolyl, tetrazolyl, benzopynanyl, benzofuranyl and the like, which may be substituted; heteroaralkyl such as imidazolemethyl, imidazoleethyl, pyridylmethyl, furyl methyl, oxazolemethyl, imidazoiyi and the like, which may be substituted; heterocyclyl group such as pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl and the like; heterocycloalkyl groups such as pyrrolidinemethyl, piperidinemethyl, morpholinemethyl, piperazinemethyl and the like, which may be substituted. Any of Ya, or Ys may also represent =O, =S, substituted or unsubstituted =NOR"', where R'" represents hydrogen, (Cr C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group. These groups are defined as above.
When the groups represented by Y and Y are substituted, the substituents may be selected from hydroxy, nitro, cyano, amino, tert-butyldimethylsilyloxy (TBSO), halogen atom, (C1-C10)alkyl, (C1-C10)alkoxy, cyclo(C3-C10)alkyl, aryl, benzyloxy, acyl or acyloxy group such as formyloxy, acetyloxy and the like. The remaining groups are as defined above.
When the groups represented by R4 and Rd as defined below are substituted, the substituents are selected from halogen, hydroxy, nitro, amino, cyano, (C1-C10)alkyl or (C]-C10) alkoxy, (C1-C10) alkyl and (C1-C10) alkoxy are as defined above.

In another aspect, the compounds of the invention comprise a compound of formula (I), wherein:
W R"^ is (C1-C10)acyl, thio(C1-C10)acyl, (C1-C10)alkoxycarbonyl, (C1- (Q i
C10)alkoxythiocarbonyl. (ii) R2 and R3represent hydrogen and halogen, (iii) 'm' represents 1.
(iv) ' ' represents a bond.
(v) R4 is (C1-C10)acyl, thio(C1-C10)acyl, (C1-C10)alkoxycarbonyl, (d-C10)alkoxythiocarbonyl;
m represents 1;
'....' represents a bond;
R2 and R3represent hydrogen and halogen, (vi) R4 is (C1-C10)acyl, thio(C1-C10)acyl, (C1-C10)alkoxycarbonyl, (C1-C10)alkoxythiocarbonyl;
m represents 1;
'....' represents a bond;
R2 and R3represent hydrogen and halogen;
Y1 and Y2 represent hydrogen atom, (vii) R'is(C1-C10)acyl;
m represents 1;
'....' represents a bond;
R and R represent hydrogen and halogen;
Y1 and Y2 represent hydrogen atom, (viii) R4 is thio(C1-C10)acyl;
m represents 1;
'....' represents a bond;
R2 and R3represent hydrogen and halogen;
Y1 and Y2 represent hydrogen atom, (ix) R4 is (C1-C10)alkoxycarbonyl;
m represents 1;
'....' represents a bond;

One embodiment of the present invention is to provide a process for the preparation of the compound of formula (I) where R1 represents NHR4 wherein R4 represents hydrogen atom, Z represents O or S, and all other symbols are as defined earlier, which is shown in the following Scheme-I, comprising the following steps::

The compound of formula (la) is reacted with a compound of formula (lb), to obtain a compound of formula (Ic), when X represents halogen atom, by using (C1-C10) alkyllithium such as methyllithium (MeLi), n-butyllithium (n-BuLi), secondary butyllithium (sec.BuLi), tertiary butyllithium (ter.BuLi) and the like, and the like. The compound of formula (Ic), where X represents hydrogen atom is obtained by treating with CsF, The solvent used in the reaction may be selected from tetrahydrofuran (THF), hexamethylphosphoramide (HMPA), diethylether and the like. The temperature and duration of the reaction can be maintained in the range of about -78 to about 100 °C and about 30 min to about 1.5 h respectively.

The compound of formula (Ic) is reacted with a compound of formula (Id), to obtain a compound of formula (le), by using a reagent (C1-C10) alkyllithium such as methyllithium (MeLi), n-butyUithium (n-BuLi), secondary butyllithium (sec.BuLi), tertiary butyllithium (ter.BuLi) and the like. The solvent used in the reaction may be selected from THF, HMPA, diethyl ether, 1,4-dioxane and the like. The temperature and duration of the reaction can be maintained in the range of about -78 to about 50 °C and about 4 to about 10 h respectively.
The compound of formula (le) is treated with any of the reagents selected from cone HCl, p-toluene sulfonic acid (p-TSA), mesyl chloride & triethylamine, 1,2-diazabicyclo[5,4,0]undec-7-ene (DBU), phosphorous oxychloride (POCI3), The solvent used in the reaction is selected from pyridine, dichloromethane, acetonitrile, toluene and the like, to obtain a compound of formula (If), where '....' represents a bond, The temperature and duration of the reaction can be maintained in the range of about 0 to about 150 °C and about 30 min to about 24 h respectively. The above obtained compound of formula (le) is converted to compound of formula (le), where '....' represents no bond, by treating with Et3SiH & BF3.0Et2, EtaSiH & CF3COOH, TMSCl, Nal, Me2Sil2, Bu3SnH and the like, under the above reaction conditions.
The compound of formula (If) is reacted with NaNO2, NaN3. t-Butyi nitrile and the like, to obtain a compound of formula (Ig), The temperature and duration of the reaction can be maintained, in the range of about 0 to about 150 °C and about 30 min to about 24 h respectively.
The compound of formula (Ig) is reacted with a compound of formula (Ih), to obtain a compound of formula (I), by using a reagent such as cuprous iodide (Cul), cuprous chloride (CuCl) and the like. The solvent used in the reaction may be selected from acetonitrile, toluene, diemthyl formamide (DMF) and the like. The reaction may be carried out in the presence of such as diisoporpylethylamine, triethylamine and the like. The temperature and duration of the reaction can be maintained in the range of about 0 to about 100 °C and about 30 min to about 12 h respectively.
The compound of formula (I), where R represents isoindole-l,3-dione to a compound of formula (I) where R1 represents NHR4 wherein R4 represents hydrogen atom, is carried out by using hydrazine hydride. The solvent used in the reaction is selected from (C1-C6)alcohol such as methanol, ethanol, propanol, isopropanol and the like or mixtures thereof. The

temperature of the reaction is maintained at the reflux temperature of the solvent used. The duration of the reaction is maintained in the range of about 2-4 h.
Another embodiment of the present invention provides, an alternte process for the preparation of compound of formula (I), where R1 represents NHR4 wherein R4 represents hydrogen atom and all other symbols are as defined earlier, which is shown in the following Scheme-II:

The conversion of compound of formula (li) to a compound of formula (Ij) and compound of formula (Ij) to a compound of formula (I), is carried out by using a palladium

reagent such as PdCl2CPPh2), Pd2(dba)3 and the like. The solvent used in the reaction is selected from DMF, acetonitrile, 1,4-dioxane and the like. The temperature and duration of the reaction are maintained in the range of about 20 to about 100 oC and about 2 to about 12 h respectively.
The compound of formula (I), where R1 represents isoindole-l,3-dione, '....' represents a bond, to a compound of formula (I) where R1 represents NHR4wherein R4 represents hydrogen atom, is carried out by using hydrazine hydride. The solvent used in the reaction is selected from (C1-C6)alcohol such as methanol, ethanol, propanol, isopropanol and the like or mixtures thereof. The temperature of the reaction is maintained at the reflux temperature of the solvent used. The duration of the reaction is maintained in the range of 2-4 h. The above obtained compound of formula (I) is converted to a compound of formula (I),
where ' ' represents no bond, by conventional hydrogenation methods, by using reagent
such as PtO2, Pd/C, Raney nickel, and the like, along with H2 gas. The solvent used in the reaction is selected from methanol, ethanol, sodium acetate, acetic acid and other related reagents.
Another embodiment of the present invention provides the alternate process for the preparation of the compound of formula (I), where R' represents NHR4 wherein R4represents hydrogen atom, Z represents SO or SO2, and all other symbols are as defined earlier, which comprises: (i) converting the compound of formula (I)

where R1 represents isoindole-l,3-dione, Z represents S, all other symbols are as defined earlier, to a compound of formula (I), where Z represents SO or SO2 and (ii) converting the above obtained compound of formula (I), to a compound of formula (I) where R' represents NHR4 wherein R4represents hydrogen atom and all other symbols are as defined earlier.
The compound of formula (I), where Z represent S, to a compound of formula (I), where Z represents SO or SO2, can be carried out by using reagents like Siodiumperiodate (NaIO4), aluminium oxide (AI2O3), m-chloroperbenzoicacid, potassium permanganate (KMnO4), ruthenium chloride (RuCl3), periodic acid (H5IO6), oxone in presence of

solvents like dichlromethane, acetonitrile, water and the like The temperature and duration of the reaction can be maintained in the range of about 0 to about 60oC and about 30 min to about 36 h respectively.
The compound of formula (I), where R1 represents isoindole-l,3-dione, to a compound of formula (I) where R1 represents NHR4 wherein R4represents hydrogen atom, in the presence of reagents such as hydrazine hydrate, sodiumborohydrate, N-methyl amine, phenyl hydrazine, Dianion WA-20 in presence of solvents like methnol, isopropanol, ethanol.and like. The temperature and duration of the reaction can be maintained in the range of about 0 to about 100oC and about 30 min to about 36 h respectively.
Another embodiment of the present invention provides an alternative process for the preparation of the compound of formula (I) where R* represents azido and all other symbols are as defined earlier, which is shown in Scheme-Ill:

where R^, R\ Y', Y^, Z and m are defined as earlier.
Scheme-Ill
The compound of formula (Ig) may be converted to a compound of formula (I), where R^ represents hydroxy group, by treating with propargyl alcohol. The solvent used in the reaction may be selected from benzene, toluene, xylene, acetonitrile, THF, DMF and the like. The temperature of the reaction may be maintained in the range of about 10 to about 200 °C, preferably about 20 to about 70 °C. The duration of the reaction may be in the range of about 1 to about 25 h, preferably in the range of about 5 to about 20 h.

The compound of formula (I) where R' represents hydroxy group may be converted to a compound of formula (I) where R1 represents azido group was carried out in two steps. In step (1) the compound of formula (I) where R^ represents OH is converted to compound of formula (I) where R1 represents leaving group such as halogen atom, by treating with CBr4/PPh3, PBr3, sulfonyl chloride (SOCI2) and the like. The reaction may be carried out in the presence of chloroform, dichloromethane, THF, dioxane and the like or mixtures thereof The reaction may be carried out in the presence or absence of a base such as triethylamine (EtsN), diisopropyl ethylamine, sodium carbonate (Na2CO3), potassium carbonate (K2CO3) and the like. The temperature of the reaction may be maintained in the range of 0 to 80°C, preferably in the range of 0 to 50°C. The duration of the reaction may be in the range of about 1-12 h, preferably in the range of about 1-4 h. In step (2), the compound of formula (I) where R' represents halogen atom may be converted to compound of formula (I) where R' represents azido group by treating with sodium azide (NaN3), lithium azide (LiN3), trialkylsilylazide and the like. The solvent used in the reaction may be selected from acetone, THF, DMF, dimethyl sulfoxide (DMSO), methylcyanide and the like. The temperature of the reaction may be maintained in the range of about 20 to about 120°C, preferably about 20 to about 80°C, The duration of the reaction may be in the range of about 1 to about 12 h, preferably about 1 to about 4 h.
Another embodiment of the present invention provides a process for the preparation of compound of formula (I) where R^ represents hydroxy group, which is shown in the following Scheme-IV:

where R1,R2,Y1,Y2 Z and m are defined as earlier.
Scheme-IV
The conversion of compound of formula (Ig) to a compound of formula (I) where R1 represents (C1-C10)acyloxy group, may be carried out in the presence of (C1-C10)alkyl or aryl esters of propargyl alcohol. The solvent used in the reaction may be selected from benzene, toluene, xylene, acetonitrile, THF and the like. The temperature of the reaction may be maintained in the range of about 10 to about 200°C, preferably room temperature to the boiling temperature of the solvent. The duration of the reaction may be in the range of about 1 to about 25 h, preferably in the range of about 5 to about 20 h.
The hydrolysis of compound of formula (I) where R1 represents (C1-C10)acyloxy group, to a compound of formula (I), where R1 represents hydroxy group, may be carried out by using conventional ester hydrolysis procedures.
Yet another embodiment of the present invention provides a process for the preparation of compound of formula (I), where R1represents NHR4, wherein R4represents substituted or unsubstituted acetyl group and all other symbols are as defined earlier, from a compound of formula (I) where R1represents azido group,

where Z,Y',Y2,, R1and m are as defined earlier,
The compound of formula (I), where R1represents NHR4, wherein R4represents substituted or unsubstituted acetyl group may be prepared from compound of formula (I), where R1 represents azido group may be carried out by using thiolacetic acid with or without using solvent such as THF, DMF, toluene and the like. The reaction may be carried out at a temperature in the range of about 25 to about 40 °C, preferably at room temperature. The duration of the reaction may be in the range from about 3 to about 24 h, preferably from about 4 to about 12 h.
Still another embodiment of the present invention provides a process for the preparation of compound of formula (I), where R1represents NHR4, wherein R4 represents substituted or unsubstituted -C(=S)-R4a wherein R4a represents (C1-C10)alkyl, halo(C1-C10)alkyl, aryl, heteroaryl, .C(=O)-(C1-C10)alkoxy, -C(=O)-(C1-C10)alkoxy, -C(=O)-aryloxy, -

C(=S)-(C1-C10)alkyl or -C(=S)-aryl; from compound of formula (I), where R1represents NHR4, where R4 represents substituted or unsubstituted -C(=O)-R4a, wherein R4a represents (C1-C10)alkyl, haloCC1-C10)alkyl, aryl, heteroaryl, -C(=O)-(C1-C10)aikoxy, -C(=O)-aryloxy, -C(=S)-(C1-C10)alkyl or -C(=S)-aryl

where all symbols are as defined earlier.
The compound of formula (I), where R1 represents NHR4, wherein R4represents substituted or unsubstituted -C(=S)-R4a, from compound of formula (I), where R1 represents NHR4, wherein R4 represents substituted or unsubstituted -C(=O)-R4a, wherein R4a is as defined above, may be carried out by taking a solution of the amide and Lawesson's reagent (2,4-bis(methoxyphenyl)-l,3-dithia-2,4-diphosphetane-2,4-disulfide) in dry dioxane, toluene, THF, DMF and the like. The reaction may be carried out at a temperature in the range of about 20 to about 130°C, preferably in the range of about 55 to about 90 °C. The duration of the reaction may be in the range from about 3 to about 24 h, preferably from about 3 to about 10 h.
Another embodiment of the present invention provides a process for the preparation of compound of formula (I), where R1 represents NHR4, wherein R4represents substituted or unsubstituted -C(=S)-OR4b wherein R4b represents (C1-C10)alkyl, cyclo(C3-C10)alkyl, aryl, (C2-C10)alkenyl or -C(=O)-(C1-C10)alkyl group,, which comprises: (i) reacting compound of formula (I)

where R1 represents azido group; and all other symbols are as defined earlier, with triphenylphosphine/water or H2-Pd/C, to produce a compound of formula (I), where R1represents NHR4, wherein R4represents hydrogen atom and all other symbols are as defined earlier.

(ii) reacting compound of formula (I), where R1represents NHR4, wherein R4 represents hydrogen atom, with thiophosgene or carbon disulfide and chloromethylformate, in the presence of a base to produce a compound of formula (I), where R1 represents isothiocyanate group; and all symbols are as defmed earlier,
(iii) converting compound of formula (I) where R1 represents isothiocynate group, to a compound of formula (I), where R1 represents NHR4, wherein R4represents substituted or unsubstituted -C(=S)-OR'4b, wherein R1' is as defmed above and all other symbols are as defined earlier.
The conversion of compound of formula (I), where R1represents azido to a compound of formula (I), where R1 represents NHR4, wherein R4represents hydrogen atom may be carried out in the presence of gaseous hydrogen and a catalyst such as Ru, Pd, Rh, Pt, Ni on solid beads such as charcoal, alumina, asbestos and the like. The reduction may be conducted in the presence of a solvent such as dioxane, acetic acid, ethyl acetate, THF, alcohol such as methanol, ethanol, propanol, isopropanol and the like or mixtures thereof A pressure between atmospheric pressure to 60 psi may be used. The reaction may be carried out at a temperature in the range of 25 to 60°C, preferably in the range of room temperature to 80°C. The duration of the reaction may be in the range of about 2 to about 48 h, preferably in the range of about 5 to about 15 h. The reduction may also be carried out by employing PPhs and water.
The compound of formula (I), where R1 represents NHR4, wherein R4represents hydrogen atom may be converted to a compound of formula (I) where R1 represents isothiocyanate group, by using thiophosgene or carbon disulfide and chloromethylformate in the presence of a base such as EtsN, K2CO3, sodium hydroxide (NaOH) and the like. The reaction may be carried out in the presence of a solvent such as dichloromethane (CH2CI2), acetonitrile, chloroform (CHCI3), DMF, THF and the like. The reaction may be carried at a temperature in the range of 0 to 60°C, preferably at 0°C. The reaction may be carried out in an inert atmosphere using argon or any other inert gas. The duration of the reaction may be in the range of about 1 to about 24 h, preferably about 2 to about 10 h.
The conversion of compound of formula (I) where R1 represents isothiocyanate group, to a compound of formula (I), where R1represents NHR4, wherein R4represents substituted or unsubstituted -C(=S)-OR4b, wherein R4b is as defined above, may be carried out by using respective alcohol such as methanol, ethanol, propanol, cyclohexanol and the like, in the

absence or presence of a base such as sodiumhydride (NaH), potassiumhydride (KH) and the like. The reaction may be carried out in the presence of a solvent such as THF, toluene, DMF and the like. The reaction may be carried out at a temperature in the range of about 20 to about 130°C, preferably at reflux temperature of the solvent used. The duration of the reaction may be in the range of about 6 to about 24 h.
Another embodiment of the present invention provides a process for the preparation of compound of formula (I), where R1 represents NHR4, wherein R4 represents substituted or unsubstituted groups selected from -C(=S)-NH2, -C(=S)-NH-(C1-C10)alkyl, -C(=S)-N-((Cr C10)alkyl)2, -C(=S)-NH-(C2-C10)alkenyl, C(=S)-NH-C(=O)-aryl, -C(=S)-NH-aralkyl, -C(-S)-NH-heteroaralkyl or -C(=S)-N(R'R"), wherein R1and R" groups together form a substituted or unsubstituted 5 or 6 membered cyclic structures containing nitrogen and optionally one or two additional hetero atoms selected from oxygen, nitrogen or sulfur; from a compound of formula (I) where R1 represents isothiocyanate group,

where all symbols are as defined earlier.
The compound of formula (I), where R1 represents NHR4, wherein R4 represents substituted or unsubstituted -C(=S)-NH2, may be prepared by passing ammonia gas into a solution of compound of formula (I) where R1 represents isothiocyanate group, in the presence of a solvent such as THF, toluene, and the like. The reaction may be carried out at a temperature in the range of about -10 to about 40 °C, preferably at about -10 °C. The duration of the reaction may be in the range from about 20 min to about 4 h, preferably about 30 min.
The compound of formula (I), where R1 represents NHR4, wherein R4represents substituted or unsubstituted groups selected from -C(=S)-NH-(C1-C10)alkyl, -C(=S)-N-((C1-C10)alkyl)2, -C(=S)-NH-(C2-C10)alkenyl, C(=S)-NH-C(=O)-aryl, -C(=S)-NH.aralkyl, -C(=S)-NH-heteroaralkyl or -C(=S)-N(R'R"), wherein R1and R" groups together form a substituted or unsubstituted 5 or 6 membered cyclic structures containing nitrogen and optionally one or two additional hetero atoms selected from oxygen, nitrogen or sulfur, may be carried out by treating a compound of formula (I) where R1 represents isothiocyanate group with appropriate amine such as methylamine, ethylamine, diemthvlamine, diethvlamine, benzvlamine, aniline.

proline, morpholine, thiomorpholine, pyridiylmethylamine and the like, in the presence of a solvent such as THF, DMF, toluene, and the like. The reaction may be carried out at a temperatxire in the fange of 20 about to about 140 °C, preferably at about 20 to about 100°C, The duration of the reaction may be in the range of about 0.5 to about 24 h, preferably about 0.5 to about 12 h.
Yet another embodiment of the present invention provides a process for the preparation of compound of formula (I), where R1 represents NHR4, wherein R4represents substituted or unsubstituted -C(=S)-SR4c, wherein R4d represents (C1-C10)alkyl group, from compound of formula (I), where R1represents NHR4, wherein R'* represents hydrogen atom,

where all other symbols are as defined earlier.
The compound of fomula (I), where R1 represents NHR , wherein R4represents substituted or unsubstituted -C(=S)-SR4c wherein R44 is as defined above, may be prepared from compound of formula (I), where R1 represents NHR4, wherein R4 represents hydrogen atom, by using CS2 in the presence of a base such as EtsN, diisopropyl ethylamine, K2CO3, NaH, tertiary butylalcohol (t-BuOK) and the like. The reaction may be carried out in the presence of alkyl halide such as methyliodide, ethylbromide, propylbromide and the like. The solvent used in the reaction may be selected from ethanol, methanol, isopropanol, THF, diethylether, acetonitrile and the like, or mixtures thereof. The reaction may be carried out at a temperature in the range of about 20 to about 60 °C, preferably at about 20 to about 40 °C. The duration of the reaction may be in the range of about 6 to about 24 h.
Another embodiment of the present invention provides a process for the preparation of compound of formula (I), where R1represents NHR4, wherein R4 represents substituted or unsubstituted -C(=S)-NH-R'4d, wherein R4d represents -C(=O)-aryl group, from compound of formula (I), where R1 represents NHR4, wherein R4 represents hydrogen atom,

where all other symbols are as defined earlier.
The compound of fomula (I), where R1 represents NHR4, wherein R4 represents substituted or unsubstituted -C(=S)-NH-R4c wherein R4d is as defined above, may be prepared from compound of formula (I), where R1represents NHR4, wherein R4represents hydrogen atom by using benzoylisothiocyanate. The solvent used in the reaction may be selected from acetone, ethanol, methanol, isopropanol, THF, diethylether, acetonitrile and the like. The temperature of the reaction may be maintained in the range of about 0 to about 80°C, preferably in the range of about 20 to about 60 °C. The duration of the reaction may be in the range of about 1 to about 20 h, preferably in the range of about 1 to about 10 h.
Yet another embodiment of the present invention provides a process for the preparation of compound of formula (I), where R1 represents NHR4, wherein R4represents substituted or unsubstituted -C(=O)-heteroaryI, from a compound of formula (I), where R1 represents NHR4, wherein R4 represents hydrogen atom,

where all other symbols are as defined earlier.
The compound of fomula (I), where R1 represents NHR4, wherein R4represents substituted or unsubstituted -C(=O)-heteroaryl, may be prepared from compound of formula (I), where R1represents NHR4, wherein R4represents hydrogen atom by treating with corresponding heteroaroyl acid chloride and base such such as pyridine, triethylamine or diisopropylamine. The reaction may also be carried out by using corresponding heteroaryl acid and dicyclohexylcarbodiimide (DCC) in the presence of dimethylaminopyridine (DMAP). The solvent used in the reaction may be selected from acetonitrile, THF, methylcyanide, Et2O and the like. The temperature of the reaction may be maintained in the range of about -5 to about 100°C, preferably in the range of about 0 to about 80oC. The

duration of the reaction may be in the range of about 1 to about 15 h, preferably in the range of about 2 to about 12 h.
« Still another embodiment of the present invention provides a process for the
preparation of compound of formula (I), where R1 represents NHR4 wherein R4 represents
substituted or unsubstituted -C(=O)-R4c wherein R4c represents (C1-C10)alkyl, (C1-C10)alkoxy,
(C2-C10)alkenyl, halo(C1-C10)alkyl, aryl, aryloxy, heteroaryl, (C2-C10)alkenyloxy, (C1-C10)
alkylcarbonyl, arylcarbonyl, aryloxycarbonyl, (C1-C10)alkoxycarbonyl, (C1-C10)
alkylthiocarbonyl or (C1-C10)arylthiocarbonyl; from a compound of formula (I), where R1
represents NHR4, wherein R4represents hydrogen atom,

where all other symbols are as defined earlier.
The compound of formula (I), where R1represents NHR1, wherein R4represents substituted or unsubstituted -C(=O)-R4c, wherein R4d is as defined above, may be prepared from compound of formula (I), where R1represents NHR4, wherein R4 represents hydrogen atom, by treating with appropriate acid halide such as acetyl chloride, propionyl chloride and the like; alkylchloroformate like methylchloroformate, ethylchloroformate and the like; aralkylchloroformate like benzylchloroformate and the like; or anhydride of the corresponding acid such as acetic anhydride. The reaction may be carried out in the presence of a solvent such as CH2CI2, CHCI3, toluene, THF and the like or mixtures thereof. The reaction may also be carried out in the presence of a base like Et3N, diisopropyl ethylamine, pyridine, K2CO3, NaH, t-BuOK and the like. The temperature of the reaction may be maintained in the range of about -20 to about 60 °C, preferably in the range of about 0 to about 40 °C. The duration of the reaction may be in the range of about 1 to about 12 h, preferably from about 1 to about 4 h.
Yet another embodiment of the present invention provides a process for the preparation of compound of formula (I) where R1represents NHR wherein R4represents substituted or unsubstituted -C(=NH)-NH2, by reacting a compound of formula (I), where R1represents NHR4 wherein R4represents hydrogen atom, with di-tert-hntoxy carbonyl thiourea,

where all other symbols are as defined earlier.
The compound of formula (I) where R1 represents NHR4 where R4represents substituted or unsubstituted group selected from -C(=NH)-NH2, may be prepared by reacting the compound of formula (I), where R1represents NHR4 where R4 represents hydrogen atom, with di-tert-bntoxy carbonyl thiourea in two steps. In the first step, the reaction may be carried out in the presence of solvents such as DMF, acetone, THF, dichloromethane and the like. The base used in the reaction may be selected from triethylamine, diisopropylethylamine, pyridine and the like. The temperature of the reaction may be in the range of 0 to 120°C, preferably in the range of 0 to 90°C. The duration of the reaction may be in the range of 0.2 to 15 h, preferably in the range of 0.5 to 10 h. In the second step, the compound obtained in the first step may be reacted with trifluoroacetic acid in the presence of a solvent such as dichloromethane, chloroform, THF and the like. The temperature of the reaction may be in the range of about 0 to about 110 °C, preferably in the range of about 0 to about 90 °C, The duration of the reaction may be in the range of about 0.5 to about 60 h, preferably in the range of about 0.5 to about 54 h.
Another embodiment of the present invention provides an alternative process for the preparation of compound of formula (I) where R1 represents NHR4 where R4represents substituted or unsubstituted group selected from -C(=NH)-NH2, by reacting a compound of formula (I), where R4 represents NHR4 wherein R4represents substituted or unsubstituted group selected from -S(O)2(C1-C10)alkyl or -S(O)2aryl group, with guanidine hydrochloride,

where all other symbols are as defined earlier.
The compound of formula (I) where R1represents NHR4 where R4 represents substituted or unsubstituted group selected from -C(=NH)-NH2, may be prepared by reacting the compound of formula (I), where R1 represents NHR4 wherein R4represents substituted or

unsubstituted group selected from -S(O)2(C1-C10)alkyl or -S(O)2aryl group, with guanidine hydrochloride. The solvent used in the reaction may be seleceted form t-butyl alcohol. The base used in the reaction may be selected from NaH, KH, sodium hexamethyldisilazide (Na-HMDS) and the like. The temperature of the reaction may be in the range of about 0 °C to boiling temperature of the solvent used. The duration of the reaction may be in the range of about 1 to about 30 h, preferably in the range of about 1 to about 24 h.
Still another embodiment of the present invention provides a process for the preparation of compound of formula (I) where R1 represents NHR4 where R4 represents substituted or unsubstituted group selected from -C(=NH)-(C1-C10)alkyI or -C(=NH)-aryI, which comprises: (i) reacting the compound of formula (I)

where R1repersents NHR4, wherein R4 represents -C(=S)-NH2 and all other symbols are as defined earlier, with di R1rr-butoxy carbonyl ether ((B0C)20), to produce a compound of formula (I)

where R1represents NHR4, wherein R4represents -C(=S)-NH2 group substituted with tert-
butoxy carbonyl group and all symbols are as defined earlier and
(ii) reacting the above compound of formula (I), with a compound of formula (Ik)
R1-NH2 (Ik)
where R7 represents substituted or unsubstituted (C1-C10)alkyl or aryl group, to produce a compound of formula (I) where R1 represents NHR4 where R4represents substituted or unsubstituted group selected from -C(=NH)-(C]-C10)alkyl or -C(=NH)-aryl group and all other symbols are as defined earlier.
The conversion of the compound of formula (I) where R1represents NHR4, wherein R4represents -C(=S)-NH2, to a compound of formula (I), where R1 represents NHR4, wherein

R represents -C(=S)-NH2 group substituted with tert-butoxy carbonyl group may be carried out by reacting with (BOC)2O, in the presence of solvent such as THF, diethylether and the like. The base^ used in the reaction may be selected from NaH, KH, sodium hexamethyldisilazane (Na-HMDS) and the like. The temperature of the reaction may be in the range of about 0 to boiling temperature of the solvent. The duration of the reaction may be in the range of about 0.5 to about 14 h, preferably in the range of about 0.5 to about 10 h.
The conversion of the compound of formula (I), where R1 represents NHR4, wherein R represents -C(=S)-NH2 group substituted with tert-hntoxy carbonyl group, to a compound of formula (I) may be carried out by reacting with the compound of formula (Ik) in two steps. In the first step, the reaction may be carried out in the presence of a solvent such as DMF, THF, chloroform, dichloromethane and the like. The base used in the reaction may be selected from triethylamine, diisopropylethylamine, pyridine and the like. The temperature of the reaction may be in the range of about 0 to about 120°C, preferably in the range of about 0 to about 90°C. The duration of the reaction may be in the range of about 0.5 to about 24 h, preferably in the range of about 0.5 to about 20 h. In the second step, the compound obtained in the first step may be reacted with trifluoroacetic acid in the presence of a solvent such as dichloromethane, chloroform, THF and the like. The temperature of the reaction may be in the range of about 0 to about 110oC, preferably in the range of about 0 to about 90°C. The duration of the reaction may be in the range of about 0.5 to about 60 h, preferably in the range of about 0.5 to about 54 h.
Yet another embodiment of the present invention provides a process for the preparation of a compound of formula (I) where R1 represents halogen, from compound of formula (I) where R1 represents hydroxy group,

where all other symbols are as defined above.
The compound of formula (I) where R1 represents halogen is prepared from compound of formula (I) where R1 represents hydroxy group may be carried out by treating with SOCI2, PCI5, PBr3, tetrahalomethane group such as carbontetrabromide (CBr4), carbontetrachloride (CCI4) and the like, in the presence of triphenylphonsphine (PPh3), trialkylphosphine

(P(alkyl)3) and the like. The reaction may be carried out in the presence of a solvent such as dry dichloromethane, chloroform, tetrachloromethane, benzene, DMF, DMSO, THF and the like. The temperature of the reaction may be maintained in the range of about 0 to about 60 °C, preferably about 20 to about 40 °C. The duration of the reaction may be in the range of about 0.5 to about 24 h, preferably about 1 to about 13 h.
Still another embodiment of the present invention provides a process for the preparation of a compound of formula (I) where R1represents 'SH',

where all other symbols are as defined above, which comprises:
(i) reacting the compound of formula (I) where R1 represents halogen atom, to produce a
compound of formula (Im),

where all other symbols are as defined earlier, with a base and thiolacetic acid,
(ii) reacting the compound of formula (Im), to produce a compound of formula (I) where
R1 represents 'SH' group and all other symbols are as defined earlier, with base.
The compound of formula (Im) is prepared from compound of formula (I) where R1 represents halogen atom may be prepared by using thiolacetic acid in the presence of a base such as triethylamine, di-isopropylamine, di-isopropylethylamine, pyridine, piperidine, DMAP, DBU, lithium diisopropylamide (LDA), potassium bis-(trimethyl silyl)amide, BuLi, Na2CO3, K2CO3, NaOH, KOH, sodiummethoxide (NaOMe), sodiumethoxide (NaOEt), sodium iso propoxide (NaO-iPr), t-BuOK, NaH, KH and the like. The solvent used in the reaction may be seleceted from THF, benzene, dioxane and the like. The temperature of the reaction may be maintained in the range of about 20 °C to reflux temperature, preferably at reflux temperature. The duration of the reaction may be in the range of about 2 to about 24 h, preferably about 6 h.

The compound of formula (I), where R1 represents 'SH' group may be prepared from a compound of formula (Im) by reacting with a base such as K2CO3, NaOH, KOH, BuLi and the like. The reaction may be carried out at a temperature in the range of about 20 oC to reflux temprature. The duration of the reaction may be in the range of about 1 to about 24 h.
Still yet another embodiment of the present invention provides a process for the preparation of compound of formula (I), where R* represent NHR4 wherein R4represents substituted or unsubstituted -S(O)2(C1-C10)alkyl or -S(O)2aryl group, from a compound of formula (I) where R represents NHR where R represents hydrogen atom, (i) reacting the compound of formula (I),

where R1 represents NHR4 where R4represents hydrogen atom and all other symbols are as defined in the description, to a compound of formula (I), where R1 represents NHR4, wherein R4 represents substituted or unsubstituted group selected from -S(O)2-(C1-C10)alkyl or -S(O)2-aryl group and all other symbols are as defined in the description, to a compound of formula (I).
The conversion of compound of formula (I), where R1 represents NHR4 where R4represents hydrogen atom, to a compound of formula (I), where R1 represents NHR4, wherein R4 represents substituted or unsubstituted group selected from -S(O)2-(C1-C10)alkyl or -S(O)2-aryl group, may be carried out by treating with alkylsulfonylchloride or arylsulfonylchloride such as methanesulfonyl chloride, p-toluenesulfonyl chloride and the like. The solvent used may be selected from dichloromethane, tetrahydrofuran, acetonitrile, dimethylformamide, dimethylsulfoxide and the like. The temperature of the reaction may be in the range of about 0 to about 50°C, for duration of about 1 to about 6 h.
Another embodiment of the present invention provides a novel intermediate of the formula (Ig),

Yet another embodiment of the present invention provides a process for the preparation of novel intermediate of formula (Ig), which comprises:

The compound of formula (la) is reacted with a compound of formula (lb), to obtain a compound of formula (Ic), when X represents halogen atom, by using a reagent such as BuLi and the like. The compound of formula (Ic), where X represents hydrogen atom is obtained by treating with CsF. The solvent used in the reaction may be selected from tetrahydrofuran (THF), hexamethylphosphoramide (HMPA), diethylether and the like. The temperature and duration of the reaction can be maintained in the range of about -78 to about 100 °C and about 30 min to about 1.5 h respectively.

The compound of formula (Ic) is reacted with a compound of formula (Id), to obtain a compound of formula (le), by using a reagent such as methyllithium (MeLi), n-butyllithium (n-BuLi), secondary butyllithium (sec.BuLi), tertiary butyllithium (ter.BuLi) and the like. The solvent used in the reaction may be selected from THF, HMPA, diethyl ether, 1,4-dioxane and the like. The temperature and duration of the reaction can be maintained in the range of about -78 to about 50 °C and about 4 to about 10 h respectively.
The compound of formula (le) is treated with any of the reagents selected from cone HCl, p-toluene sulfonic acid (p-TSA), mesyl chloride & triethylamine, 1,2-diazabicyclo[5,4,0]undec-7-ene (DBU), phosphorous oxychloride (POCI3), The solvent used in the reaction is selected from pyridine, dichloromethane, acetonitrile, toluene and the like, to obtain a compound of formula (If), where '....' represents a bond. The temperature and duration of the reaction can be maintained in the range of about 0 to about 150 °C and about 30 min to about 24 h respectively. The above obtained compound of formula (le) is converted to compound of formula (le), where '....' represents no bond, by treating with EtsSiH & BF3OEt2, EtsSiH & CF3COOH, TMSCl, Nal, Me2Sil2, BusSnH and the like, under the above reaction conditions.
The compound of formula (If) is reacted with NaNO2, NaNs, t-Butyl nitrile and the like, to obtain a compound of formula (Ig), The temperature and duration of the reaction can be maintained in the range of about 0 to about 150 °C and about 30 min to about 24 h respectively.

CH2NH2, -CH2N(Pthalimide), -CH2NH-C(=S)S-O(C1-C10)alkyl, -CH2NH-C(=O) (C,-C!o)alkyl.
Still yet another embodiment of the present invention provides a process for the preparation of novel intermediate of formula (Iq), which is shown in the following Scheme-V:

Scheme-V
The compound of formula (Iq) may be prepared by reacting the compound of formula (Ig) with a compound of formula (Ir), in the presence of Cu(l)I. and a base such as triethylamine, ethyldiisopropylamine, l,4-diazabicyclo[2,2,2]octane (DABCO) and the like. The reaction may be carried out in the presence of a solvent such as dichloromethane, chloroform, tetrahydrofuran, dimethylformamide, dimethylsulfoxide, acetonitrile and the like.
It is appreciated that in any of the above-mentioned reactions, any reactive group in the substrate molecule may be protected according to conventional chemical practice. Suitable protecting groups in any of the above mentioned reactions are tertiarybutyldimethylsilyl, methoxymethyl, triphenyl methyl, benzyloxycarbonyl, tetrahydropyran(THP) etc, to protect hydroxyl or phenolic hydroxy group; N-tert-butoxycarbonyl (N-Boc), N-benzyloxycarbonyl (N-Cbz), N-9-fluorenyl methoxy carbonyl (-N-FMOC), benzophenoneimine, propargyloxy carbonyl (POC) etc, for protection of amino or anilino group, acetal protection for aldehyde, ketal protection for ketone and the like. The methods of formation and removal of such protecting groups are those conventional methods appropriate to the molecule being protected.
Regioisomers are isomers that differ by their functional groups. The regioisomers of compound of formula (I) may be prepared by modifying the reaction conditions, use of reagents like acid to base or base to acid or by reaction with free base hydrazine instead of its salt with diketone. The molar proportion also can change the regiosiomer formation.
The stereoisomers including enantiomers and geometrical isomers (E and Z isomers or their mixtures in various ratios) may be prepared by using reactants in such a way to obtain a

single isomeric form in the process wherever applicable or by conducting the reaction in the presence of reagents or catalysts in their single enantiomeric form. The single enantiomer, wherever application may be prepared by resolving the racemic mixture by conventional methods. The stereoisomers of the compounds forming part of this invention may be prepared by using reactants in their single enantiomeric form in the process wherever possible or by conducting the reaction in the presence of reagents or catalysts in their single enantiomer form or by resolving the mixture of stereoisomers by conventional methods. Some of the preferred methods include use of microbial resolution, resolving the diastereomeric salts formed with chiral acids such as mandelic acid, camphorsulfonic acid, tartaric acid, lactic acid, and the like wherever applicable or chiral bases such as brucine, cinchona alkaloids and their derivatives and the like. Commonly used methods are compiled by Jaques et al in "Enantiomers, Racemates and Resolution" (Wiley Interscience, 1981). Where appropriate the compounds of formula (I) may be resolved by treating with chiral amines, ammoacids, aminoalcohols derived from aminoacids; conventional reaction conditions may be employed to convert acid into an amide; the diastereomers may be separated either by fractional crystallization or chromatography and the stereoisomers of compound of formula (I) may be prepared by hydrolyzing the pure diastereomeric amide.
A method of treating or preventing an infectious disorder in a subject is provided by administering an effective amount of oxazolidinone as disclosed herein to the subject, wherein the infectious disorder is characterized by the presence of microbial infection caused by pathogens such as Gram-positive, Gram-negative, aerobic and anerobic bacteria such as MRSA, Pseudomonas aeruginosa, Escherischia spp., Streptococci including Str. pneumoniae, Str. pyogenes, Enterococci as well as anaerobic organisms such as Bacteroides spp., Clostridia spp. species and Acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp. fastidious Gram negative organisms, H. influenzae, M. catarrhalis and several other bacteria resistant to fluoroquinolone, macrolide, Vancomycin, Aminoglycosides, Streptogramin, Lincosamides and p-Lactam resistant species. Such disorders include infections of the middle, internal and external ear including otitis media, infections of the cranial sinuses, eye infections, infections of the oral cavity, central nervous system infections, infections of teeth and gums,, infections of the mucosa, respiratory tract infections, genitourinary tract infections, gastro-intestinal infections, septicemia, bone and joint infections, skin and soft infections, bacterial endocarditis, bums, nosocomical

infections, pre- and postsurgical infections, opportunistic infections in the immune compromised, intracellular infections such as Chlamydia and Mycoplasma.
Pharmaceutically acceptable salts forming part of this invention include salts derived
from inorganic bases such as Li, Na, K, Ca, Mg, Fe, Cu, Zn, Mn; salts of organic bases such
as N,N'-diacetylethylenediamine, betaine, caffeine, 2-diethylaminoethanol, 2-
dimethylaminoethanol, N-ethylmorpholine, N-ethylpiperidine, glucamine, glucosamine,
hydrabamine, isopropylamine, methylglucamine, morpholine, piperazine, piperidine,
procaine, purines, theobromine, triethylamine, trimethylamine, tripropyiamine, tromethamine,
diethanolamine, meglumine, ethyl enediamine, N,N'-diphenylethylenediamine, N,N'-
dibenzylethylenediamine, N-benzyl phenylethylamine, choline, choline hydroxide,
dicyclohexylamine, metformin, benzylamine, phenylethylamine, dialkylamine, trialkylamine,
thiamine, aminopyrimidine, aminopyridine, purine, spermidine, and the like; chiral bases like
alkylphenylamine, glycinol, phenyl glycinol and the like, salts of natural amino acids such as
glycine, alanine, valine, leucine, isoleucine, norleucine, tyrosine, cystine, cysteine,
methionine, proline, hydroxy proline, histidine, ornithine, lysine, arginine, serine, threonine,
phenylalanine; unnatural amino acids such as D-isomers or substituted amino acids;
guanidine, substituted guanidine wherein the substituents are selected from nitro, amino, alkyl
such as methyl, ethyl, propyl and the like; alkenyl such as ethenyl, propenyl, butenyl and the
like; alkynyl such as ethynyl, propynyl and the like; ammonium or substituted ammonium
salts and aluminum salts. Salts may include acid addition salts where appropriate which are,
) sulphates, nitrates, phosphates, perchlorates, borates, halides, acetates, tartrates, maleates,
citrates, succinates, palmoates, methanesulphonates, benzoates, salicylates,
hydroxynaphthoates, benzenesulfonates, ascorbates, glycerophosphates, ketoglutarates and
the like. Pharmaceutically acceptable solvates may be hydrates or comprising other solvents
of crystalHzation such as alcohols.
The pharmaceutically acceptable salts are prepared by reacting the compounds of formula (I) wherever applicable with 1 to 4 equivalents of a base such as sodium hydroxide, sodium methoxide, sodium hydride, potassium t-butoxide, calcium hydroxide, magnesium hydroxide and the like, in the presence of a solvent like ether, THF, methanol, t-butanol, dioxane, isopropanol, ethanol etc. Mixture of solvents may be used. Organic bases like lysine, arginine, diethanolamine, choline, tromethamine, guanidine and their derivatives etc. may also be used. Alternatively, acid addition salts wherever applicable are prepared by

treatment with acids such as hydrochloric acid, hydrobromic acid, nitric acid, sulfuric acid, phosphoric acid, p-toluenesulphonic acid, methanesulfonic acid, acetic acid, citric acid, maleic acid salicylic acid, hydroxynaphthoic acid, ascorbic acid, palmitic acid, succinic acid, benzoic acid, benzenesulfonic acid, tartaric acid and the like in the presence of a solvent like ethyl acetate, ether, alcohols, acetone, THF, dioxane etc. Mixture of solvent may also be used. The salts of amino acid groups and other groups may be prepared by reacting the compounds of formula (I) with the respective groups in the presence of a solvent like alcohols, ketones, ether etc. Mixture of solvents may be used.
The prodrugs such as esters and amides of the compounds of formula (I) can be prepared by conventional methods.
The metabolites, which are formed inside the body of the mammal, are formed by the reaction of various enzymes present in the body with the compounds of formula (I)
Various polymorphs of a compound of general formula (I) forming part of this invention may be prepared by crystallization of compound of formula (I) under different conditions. For example, using different solvents commonly used or their mixtures for recrystallization; crystallizations at different temperatures; various modes of cooling, ranging from very fast to very slow cooling during crystallizations. Heating or melting the compound followed by gradual or fast cooling may also obtain polymorphs. The presence of polymorphs may be determined by solid probe nmr spectroscopy, IR spectroscopy, differential scanning calorimetry, powder X-ray diffraction or such other techniques.
The present invention also provides pharmaceutical compositions, containing compounds of the general formula (I), as defined above, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceuticaily acceptable salts or their pharmaceuticaily acceptable solvates in combination with the usual pharmaceuticaily employed carriers, diluents and the like. The pharmaceutical compositions according to this invention can be used for the treatment of bacterial infections. They can also be used for the treatment of bacterial infections associated with multidrug resistance. The pharmaceutical compositions according to this invention can also be administered prophylatically for the prevention of bacterial infections in a patient at risk of developing a bacterial infection. Such patients include but are not limited to patients who are pre- or postsurgical, immunocompromised, or hospitalized and can be used for the treatment/prevention of bacterial infections associated with multidrug resistance.

Pharmaceutically acceptable solvates of compound of formula (I) forming part of this invention may be prepared by conventional methods such as dissolving the compounds of formula (I) in the presence of a solvent such as water, methanol, ethanol etc., preferably water and recrystallizing by using different crystallization techniques.
The regioisomers of compound of formula (I) may be prepared by modifying the reaction conditions, use of reagents like acid to base or base to acid or by reaction with free base hydrazine instead of its salt with diketone. The molar proportion also can change the regioisomer formation.
The pharmaceutical compositions may be in the forms normally employed, such as tablets, capsules, powders, syrups, solutions, suspensions and the like, may contain flavorants, sweeteners etc. in suitable solid or liquid carriers or diluents, or in suitable sterile media to form injectable solutions or suspensions. Such compositions typically contain from 1 to 20 %, preferably 1 to 10 % by weight of active compound, the remainder of the composition being pharmaceutically acceptable carriers, diluents or solvents.
Suitable pharmaceutically acceptable carriers include solid fillers or diluents and sterile aqueous or organic solutions. The active compounds will be present in such pharmaceutical compositions in the amounts sufficient to provide the desired dosage in the range as described above. Thus, for oral administration, the compounds can be combined with a suitable solid, liquid carrier or diluent to form capsules, tablets, powders, syrups, solutions, suspensions and the like. The pharmaceutical compositions, may, if desired, contain additional components such as flavorants, sweeteners, excipients and the like. For parenteral administration, the compounds can be combined with sterile aqueous or organic media to form injectable solutions or suspensions. For example, solutions in sesame or peanut oil, aqueous propylene glycol and the like can be used, as well as aqueous solutions of water-soluble pharmaceutically-acceptable acid addition salts or salts with base of the compounds. The injectable solutions prepared in this maimer can then be administered intravenously, intraperitoneally, subcutaneously, or intramuscularly, with intramuscular administration being preferred in humans.
In addition to the compounds of formula (I) the pharmaceutical compositions of the present invention may also contain or be co-administered with one or more known drugs selected from other clinically useful antibacterial agents such as p-lactams. Aminoglycosides, Oxazolidinones, Fluoroquinolines, Streptogramins, Lincosamides, Macrolides or any other

suitable antiinfective agent. These may include penicillins such as oxacillin or flucloxacillin and carbapenems such as meropenem or imiphenem to broaden the therapeutic effectiveness against, for example, methicillin-resistant staphylococci. Compounds of the formula (I) of the present invention may also contain or be co-admistered with bactericidal/permeability-increasing protein product (BPI) or efflux pump inhibitors to improve activity against gram negative bacteria and bacteria resistant to antimicrobial agents.
The compounds of the formula (I) as defined above are clinically administered to mammals, including human beings, via either oral or parenteral routes. Administration by the oral route is preferred, being more convenient and avoiding the possible pain and irritation of injection. However, in circumstances where the patient cannot swallow the medication, or absorption following oral administration is impaired, as by disease or other abnormality, it is essential that the drug be administered parenterally. By either route, the dosage is in the range of about 0.5 mg/kg to about 50 mg / kg body weight of the subject per day administered singly or as a divided dose. However, the optimum dosage whether for prevention or treatment for the individual subject being treated will be determined by the person responsible for treatment, generally smaller doses being administered initially and thereafter increments made to determine the most suitable dosage.
It is also to be understood that the terminology used herein is for the purpose of describing particular embodiments only, and is not intended to limit the scope of the present invention.
The manner in which the compounds of this invention can be prepared is illustrated in the following examples, which demonstrate the preparation of typical species of the invention. In these examples, the identities of compounds, intermediates and final, were confirmed by infrared, nuclear magnetic spectral analyses as necessary. The examples are for the purpose of illustration only and should not be regarded as limiting the invention in any way.

«-Butyllithium (124 mL, 1.6 M in hexane, 198.4 mmol) was added drop wise to a solution of 3-fluoroaniline (10 g, 90.1 mmol) in THF (200 mL) at -78 °C under nitrogen atmosphere and stirred for 20 min. A solution of l,2-bis(chlorodimethylsilyl)ethane (21.3 g, 99.1 mmol) in dry THF (200 mL) was added and stirred at the same temperature for 45 min. The reaction mixture was brought to room temperature and then quenched with water (120 mL). The mixture was extracted with diethyl ether. The combined organic layers were washed with brine and dried over Na2SO4. The solvent was removed under vacuum to obtain l-(3-fluorophenyl)-2,2,5,5-tetramethyl-[l,2,5]azadisilolidine (21.2 g) and this crude product was used in the next step without purification. To a solution of l-(3-fluorophenyl)-2,2,5,5-tetramethyl-[l,2,5]azadisilolidine (15 g, 59.3 mmol) in THF (130 mL) was slowly added 55 mL (71.1 mmol) of sec-BuLi (1.3 M in cyclohexane/hexane) at -78 oC under nitrogen and stirred the reaction at the same temperature for 4 h. A solution of tetrahydro-4-pyranone (7.11 g, 71.1 mmol) in dry THF (10 mL) was added to the reaction mixture and allowed to rise to room temperature. The reaction mixture was quenched slowly by the addition of water (150 mL) at 0 °C and was concentrated under vacuum. The resulting residue was acidified with cone. HCl and the acidic solution was extracted with diethyl ether (3 x 500 mL). The aqueous layer was basified with aqueous NaOH solution and extracted with diethyl ether (500 mL). The organic layer was washed with brine, dried over sodium sulfate and evaporated under vacuum. The resulting residue was refluxed with cone. HCl (40 mL) for 3 h and then allowed to cool to room temperature. The reaction mixture was basified with aqueous NH3 (30%) and was extracted with dichloromethane. The solvent was evaporated and the required product (3 g, 26%) was separated as a light brown solid by silica gel column chromatography (ethyl acetate / hexane; 3:17).

added to an ice cooled solution of 4-(3,6-dihydro-2i/-pyran-4-yI)-3-fluorophenylanune (4 g, 20.7 mmol) obtained in preparation 1, in 6N HCl (18 mL) and stirred for 0.5 h. Then a saturated solution of sodium azide (2.69 g, 41.4 mmol) and sodium acetate (33.98 g, 414 mmol) in water (100 mL) was added slowly. The reaction mixture was stirred for another 0.5 h, diluted with water and extracted with ethyl acetate (2 x 100 mL). The organic layer was washed with water followed by brine and dried over sodium sulfate. Evaporation of volatiles and purification of the residue by flash chromatography (ethyl acetate/ hexahe; 1:9) yielded the title compound as a yellow solid (3.1 g, 68%).

n-Butyllithium (55 mL, 1.6 M in hexane, 7.18 mmol) was added drop wise to a solution of 3,5-difluoroaniline (5 g, 38.76 mmol) in THF (78 mL) at -78°C under nitrogen atmosphere and stirred for 20 min. A solution of l,2-bis(chlorodimethylsilyl)ethane (8.33 g, 38.76 mmol) in THF (78 mL) was added to the reaction mixture and stirred for 45 min and then it was brought to room temperature. The reaction mixture was quenched with water (115 mL) and extracted with diethyl ether. The combined organic layers were washed with water and brine and dried over Na2SO4. The solvent was removed under vacuum to obtain l-(3,5-difluorophenyl)-2,2,5,5-tetramethyl-[l,2,5]azadisilolidine (10.12 g) and this crude product was used in the next step without purification. To a solution of l-(3,5-difluorophenyl)-2,2,5,5-tetramethyl-[l,2,5]azadisilolidine (10.12 g, 37.3 mmol) in THF (60 mL) was slowly added 27 mL (42.96 mmol) of/i-BuLi (1.6 M in hexane) at -78 °C under nitrogen and stirred for 4 h. A solution of tetrahydro-4-pyranone (7.11 g, 71.1 mmol) in dry THF (10 mL) was added to the above mixture and warmed to room temperature. The reaction mixture was stirred for 18 h, then quenched with 100 mL of water and concentrated under vacuum. The resulting residue

was acidified with cone. HCl and the acidic solution was extracted with diethyl ether (150 mL). The aqueous layer was basified with 40% aqueous NaOH solution at 0 °C and extracted with diethyl ether. The organic layer was washed with brine, dried over sodium sulfate and evaporated on rotavapor. The resulting residue was refluxed with cone. HCl (40 mL) for 3 h and then allowed to cool to room temperature. The reaction mixture was basified with aqueous NH3 (30%) and was extracted with dichloromethane. The solvent was evaporated on rotavapor and the residue was purified through silica gel column (ethyl acetate / hexane; 3:17) to furnish the required product (2.2 g, 27%) as a pale brown solid.

A saturated solution of sodium nitrite (590 mg, 8.55 mmol) in water (5 mL) was slowly added to a solution of 4-(3,6-dihydro-2H-pyran-4-yl)-3,5-difluorophenylamine (900 mg, 4.26 mmol) in HCl (6N, 16 mL), obtained in preparation-3, cooled to 0 °C, and stirred for 0.5 h. Then a saturated solution of sodium azide (550 mg, 8.54 mmol) and sodium acetate (7 g, 85.4 mmol) in water (100 mL) was added slowly at the same temperature. The reaction mixture was stirred for another 0.5 h and then diluted with ethyl acetate (250 mL). The organic layer was washed with water followed by brine and dried over Na2SO4. The solvent was evaporated and the residue was purified by flash chromatography (ethyl acetate/ hexane; 1:9) to get the title compound as a pale yellow solid (560 mg, 58%).

n-Butyllithium (62 mL, 1.6 M in hexane, 99.2 mmol) was added drop wise to a solution of 3-fluoroaniline (5 g, 45 mmol) in THF (100 mL) at -78oC under nitrogen atmosphere Then a solution of l,2-bis(chlorodimethylsilyl)ethane (10.65 g, 49.53 mmol) in THF (100 mL) was added drop wise. The reaction mixture was stirred at the same temperature for 0.5 h and then it was brought to room temperature. The reaction mixture was quenched with water (135 mL), extracted with diethyl ether and washed with brine. The solvent was removed under vacuum to obtain l-(3-fluorophenyl)-2,2,5,5-tetramethyl-[l,2,5]azadisilolidine (11.8 g) and this crude product was used in the next step without purification. To a solution of l-(3-fluorophenyl)-2,2,5,5-tetramethyl-[l,2,5]azadisilolidine (11.8 g, 46.6 mmol) in THF (350 mL) was slowly added 43 mL of jec-BuLi (55.9 mmol, 1.6 M in hexane) at -78 °C and stirred for 4 h. A solution of tetrahydro-4-thiopyranone (6 g, 51.75 mmol) in THF (50 mL) was added to the reaction mixture at -78 "^C. The reaction mixture was slowly brought to room temperature and was stirred for further 18 h. It was then quenched with water (60 mL), concentrated under vacuum to remove most of the THF and the residue was acidified with cone. HCl. The acidic solution was extracted with diethyl ether. The aqueous layer was basified with 40% aqueous NaOH solution and extracted with diethyl ether (300 mL). The organic layer was washed with brine, dried over sodium sulfate and evaporated under vacuimi. The resulting residue was refluxed with cone. HCl (70 mL) for 3.5 h and then allowed to cool to room temperature. The reaction mixture was basified with aqueous NH3 (30%) and was extracted with dichloromethane. The solvent was evaporated on rotavapor and the required product (5,1 g, 54%) was separated as a pale brown solid by silica gel column chromatography (ethyl acetate / petroleum ether; 3:17).
1H NMR (CDCI3 + CD3OD): 5 6.99 (t, J = 8.8 Hz, IH), 6.42-6.39 (m, 2H), 5.95-5.87 (m, IH), 3.36-3.28 (m, 2H), 3.18-3.08 (m, 2H), 2.85 (t, J = 5.6 Hz, 2H), 2.68-2.56 (m, 2H); CI-MS(m/e):210(M^+l);
IR (neat): 3360, 2916, 1630, 1510, 1444, 1164, 965 cm-1 Preparation-6 4-(4-Azido-2-fluoro-phenyl)-3,6-dihydro-2fl'-thiopyran:

A saturated'aqueous solution of sodium nitrite (Ig, 14.6 mmol) was slowly added to an ice cooled solution of 4-(3,6-dihydro-2H-thiopyran-4-yl)-3-fluorophenylamine (1.52 g, 7.3 mmol), obtained in preparation-5, in 6 N HCl (16 mL), and stirred for 0.5 h. Then a solution of sodium azide (945 mg, 14.6 mmol) and sodium acetate (12 g, 146 mmol) in water (50 mL) was added at the same temperature and stirred for another 0.5 h. Then diluted with ethyl acetate (250 mL). The organic layer was washed with water followed by brine and dried over sodium sulfate. Evaporation of solvent and purification of the resulting residue by flash chromatography (ethyl acetate/ hexane; 3:17) yielded the desired compound (752 mg, 43%) as a brown oily material.

n-Butyllithium (55 mL, L6 M in hexane, 87.18 mmol) was added drop wise to a solution of 3,5-difluoroaniline (5 g, 38.75 mmol) in THF (78 mL) at -78 °C under nitrogen atmosphere and stirred for 20 min., a solution of l,2-bis(chlorodimethylsilyl)ethane (8.5 g, 39.53 mmol) in THF (78 mL) was added drop wise. The reaction mixture was stirred at the same temperature for 0.5 h and then allowed to warm to room temperature. The reaction mixture was quenched with water (100 mL), extracted with diethyl ether and then the organic layer was washed with brine. The solvent was removed under vacuum to obtain l-(3,5-difluorophenyl)-2,2,5,5-tetramethyl-[l,2,5] azadisilolidine (10.7 g) and this crude product was used in the next step without purification. To a solution of l-(3,5-difluorophenyl)-2,2,5,5-tetramethyl-[ 1,2,5] azadisilolidine (10,7 g, 39.4 mmol)) in THF (80 mL) was slowly added 28.4 mL of n-BuLi (45.3 mmol,L6 M in hexane) at -78 °C under nitrogen and stirred the

same for 4 h. Then a solution of tetrahydro-4-thiopyranone (5.26 g, 45.3 nmiol) in THF (30 mL) was added to the reaction mixture and slowly brought to room temperature and stirred for further 18 h. The Reaction mixture was quenched with water (50 mL), concentrated under vacuum and the resulting residue was acidified with cone. HCl. The acidic solution was extracted with diethyl ether. The aqueous layer was basified with 40% aqueous NaOH solution and extracted with diethyl ether (3 x 150 mL). The organic layer was washed with brine, dried over sodium sulfate and evaporated under vacuum. The resulting residue was refluxed with cone. HCl (60 mL) for 3.5 h and then allowed to cool to room temperature. The reaction mixture was basified with aqueous NH3 (30%) and was extracted with dichloromethane. The solvent was evaporated on a rotavapor and the crude product was column chromatographed over silica gel (ethyl acetate / petroleum ether; 3:17) to get the desired compound (3.8 g, 43%)) as a pale brown solid.

A saturated solution of sodium nitrite (79 mg, 1.14 mmol) in water (3 mL) was slowly added to an ice cooled solution of 4-(3,6-dihydro-2H-thiopyran-4-yl)-3,5-difluorophenylamine, obtained in preparation-7 (130 mg, 0.57 mmol), in 6N HCl (8 mL), and stirred for 0.5 h. Then a solution of sodium azide (75 mg, 1.15 mmol) and sodium acetate (950 mg, 11.58 mmol) in water (15 mL) were added respectively at the same temperature. The reaction mixture was stirred for additional 0.5 h and then diluted with ethyl acetate (100 mL). The organic layer was washed with water followed by brine and dried over sodium sulfate. Evaporation of volatiles and purification of the resulting residue by flash chromatography (ethyl acetate/ hexane; 3:17) yielded the title compound as a pale orange solid (80 mg, 56%).

To a solution of 4-(4-azido-2-fluoro-phenyl)-3,6-dihydro-2H-pyran (3 g, 13.7 mmol), obtained in preparation-2, and N, N -diisopropylethylamine base (4.78 mL, 27.4 mmol) in acetonitrile (100 mL) was added 2-prop-2-ynyl-isoindole-l,3-
Hydrazine hydrate (3.1 mL) was added to a solution of 2-{l-[4-(3,6-dihydro-2H-pyran-4-yl)-3-fluoro-phenyl]-lH-[l,2,3]triazol-4-ylmethyl}-isoindole-l,3-dione (2.9 g, 7.18 mmol), obtained in example-1, in methanol (15 mL) and refluxed for 2 h followed by stirring

at room temperature for 10 h. The reaction mixture was filtered and the filtrate was
concentrated under vacuum. The residue was purified by flash chromatography (ethyl acetate/
hexane; 1:9) to afford the title compound as a white solid (800 mg, 41%).
1H NMR (DMS0-d6): 5 9.28-8.78 (m, 2H), 8.67 (s, IH), 7.93-7.63 (m, 2H), 7.58 (t, 7 = 8.1
Hz, IH), 6.30-6.12 (m, IH), 4.52-3.20 (m, 6H), 2.60-2.39 (m, 2H).
MS (m/e): 275 (NT+I), 230, 217.
IR(KBr): 3297, 1665, 1517, 1436, 1375, 1233, 1044 cm-1
Example-3

Triethylamine (0.08 mL, 0.73 mmol) was added to a solution of C-{l-[4-(3,6-dihydro-2H^-py^an-4-yl)-3-fluoro-phenyl]-li/-[l,2,3]triazol-4-yl}methylamine (100 mg, 0.365 mmol), obtained in example-2, in dichloromethane (5 mL), cooled to 0 "^C, followed by the addition of acetyl chloride (0.028 mL, 0.4 mmol) and stirred at room temperature for 3 h. The reaction mixture was concentrated on rotavapor and the residue was purified by column chromatography over silica gel (2% methanol in chloroform) to get the required compound (62 mg, 54%) as a white powder, mp 186-188 °C.

To a solution of C- {l-[4-(3,6-dihydro-2H-pyran-4-yl)-3-fluoro-phenyl]-lH-[l,2,3]triazol-4-yl}methylamine (100 mg, 0.365 mmol), obtained in example-2, in THF (5 mL) was added triethylamine (0.103 mL, 0.73 mmol) followed by the addition of ethyl dithioacetate (0.05 ml, 0.44 mmol) and stirred at room temperature for 16 h. The reaction mixture was concentrated and the resulting residue was purified by column chromatography using 2% methanol in chloroform as eluent. The desired product was obtained as a creamy white solid (62 mg, 51%), mp 159-16rC.
1H NMR (DMS0-d6): 5 10.60-10.40 (m, IH), 8.82 (s, IH), 7.92-7.50 (m, 2H), 7.60 (t, J= 8.3 Hz, IH), 6.27-6.12 (m, IH), 4.84 (d, J= 4.8 Hz, 2H), 4.32-4.18 (m, 2H), 3.83 (t, J = 5.4 Hz, 2H), 2.60-2.30 (m, 5H). MS (m/e): 333 (M^+1), 304, 230,
IR(KBr): 3243, 3055, 2926, 1579, 1460, 1406, 1362, 1231 cm-1 Example-5

To a solution of C-{l-[4-(3,6-dihydro-2H-pyran-4-yl)-3-fluoro-phenyl]-li/-[l,2,3]triazol-4-yl}methylamine (100 mg, 0.365 mmol), obtained in exampIe-2, in dichloromethane (10 mL) was added a solution of sodium bicarbonate (77 mg, 0.92 mmol) in water (3 mL) followed by cooling in ice bath. Thiophosgene (0.034 mL, 0.44 mmol) was added to the mixture at 0 °C and stirred at the same temperature for 0.5 h. The reaction mixture was diluted with dichloromethane (50 mL), washed with water, brine and dried over sodium sulfate. The solvent was evaporated and the residue was refluxed with methanol (15 mL) for 16 h. Removal of methanol and purification of the residue by column chromatography (ethyl acetate/hexane; 3:10) yielded the required compound (65 mg, 51%) as a white powder, mp 116-120 °C.
'H NMR (DMSO-d6): 5 9.79-9.60 (m, IH), 8.76 and 8.70 (two s, IH, rotamers in a ratio of 4:1), 8.01-7.63 (m, 2H), 7.59 (t, J= 8.6 Hz, IH), 6.30-6.13 (m, IH), 4.73 and 4.45 (two d, J=

5.4 Hz, 2H, rotamers in a ratio of 4:1), 4.37-4.14 (m, 2H), 4.00-3.68 (m, 5H), 2.69-2.30 (m,
2H).
MS (m/e): 349 (Nf+1), 317, 230.
IR(KBr, film): 3438, 3214, 2925, 1619,1512, 1458, 1365, 1218 cm"^
Example-6
{l-(4-(3,6-Dihydro-2iy-pyran-4-yl)-3-fluoro-phenyi]-l/r-[l,2,3]triazol-4-ylmethyl}-
carbamic acid methyl ester:

To a solution of C- {1 - [4-(3,6-dihydro-2H-pyran-4-yl)-3 -fluoro-phenyl] -1 H-[l,2,3]triazol-4-yl}-methylamine (90 mg, 0.33 mmol), obtained in example-2, in dichloromethane (5 mL), cooled to 0 °C, was added N,N-diisopropylethylamine (0.126 mL, 0.72 mmol) followed by the addition of methyl chloroformate (0.031 mL, 0.39 mmol) and stirred at the same temperature for 2 h. And the organic layer was washed with water followed by brine and dried over sodium sulfate. The solvent was evaporated and the residue was purified by column chromatography over silica gel (methanol/ chloroform; 1:24) to afford the required product (50 mg, 46%) as a creamy white solid, mp 140-144 °C. 'H NMR (DMSO-d^): 5 8.70 (s, IH), 7.97-7.66 (m, 2H), 7.58 (t, J= 8.3 Hz, IH), 6.30-6.16 (m, IH), 4.31 (d, y = 5.9 Hz, 2H), 4.25-4.18 (m, 2H), 3.83 (t, 7 = 5.1 Hz, 2H), 3.56 (s, 3H), 2.60-2.32 (m, 2H). MS(m/e):333(M++l).
IR(KBr): 3297, 2924, 1688, 1535, 1463, 1262, 1045 cm-'.1 Example-?
2-{l-[4-(3,6-Dihydro-2H-pyran-4.yl)-3,5-difluoro.phenyl]-ljy-[l,2,3]triazol.4-ylmethyl}-l,3-isoindole-l,3-dione:

To a solution of 4-(4-azido-2,6-difluoro-phenyl)-3,6-dihydro-2H-pyran (545 mg, 2.30 mmol), obtained in preparation 4, and N,N -diisipropylethylamine (0.80 mL, 4.59 mmol) in

acetonitrile (20 mL) was added 2-prop-2-ynyl-isoindole-l,3-dione (642 mg, 3.47 mmol)
followed by the addition of cuprous iodide (655 mg, 3.45 mmol) and stirred at room
temperature for 2 h. The reaction mixture was filtered through a celite pad. The filtrate was
concentrated under vacuum and the residue was purified by chromatography over silica gel
(3% methanol in chloroform) to obtain the required compound (350 mg, 39%) as a pale
yellow solid
1H NMR (CDCI3): 5 8.94 (s, IH), 8.08-7.73 (m, 6H), 6.12-6.04 (m, IH), 4.99 (s, 2H), 4.35-
4.22 (m, 2H), 3.88 (t, J= 5.4 Hz, 2H), 3.55-3.20 (m, 2H).
MS (m/e): 423 (M++1), 173, 131.
IR(KBr): 3442,2925, 1716, 1634, 1395, 1280, 1094 cm-1,
£xample-8
C-{l-[4-(3,6-Dihydro-2H-pyran-4-yl)-3,5-difluoro-phenyl]-lH-[l,2,3]triazol-4-yl}-
methylamine:

To a solution of 2-{l-[4-(3,6-dihydro-2H-pyran-4-yl)-3,5-difluoro-phenyl]-lH-[l,2,3]tria2ol-4-ylmethyl}-l,3-isoindole-l,3-dione (325 mg, 0.768 mmol), obtained in example-7, in methanol (10 mL) was added hydrazine hydrate (0.41 mL) and refluxed for 2 h followed by stirring at room temperature for 10 h. The reaction mixture was filtered and the filtrate was concentrated under vacuum. The product was purified by flash chromatography on silica (5% methanol in chloroform) to afford the desired product (100 mg, 47%). *H NMR (DMS0-d6): 5 8.67 (s, IH), 7.75 (d, 7 = 8.3 Hz, 2H), 6.05-5.93 (m, IH), 4.30-4.12 (m, 2H), 3.92-3.72 (m, 4H), 2.63-2.38 (m, 2H). MS (m/e): 293 (M^+1), 236, 163.
IR(KBr): 3368, 3127, 2924, 2850, 1631, 1592, 1513, 1448, 1227, 1126, 1025 cm-1 ExampIe-9
n--{l-[4-(3,6-Dihydr(2H-pyran-4.yl)-3,5.difluoro-phenyl]-l/r-[l,2,3]triazol-4-ylmethyl}-thioacetamide:

■
Triethylamine (0.053 mL, 0.38 mmol) was added to a solution of C-{l-[4-(3,6-dihydro-2H-pyran-4-yl)-3,5-difluoro-phenyl]-lH-[l,23]triazol-4-yl}-methylainine (50 mg, 0.17 mmol), obtained in example-8, in THF (5 mL) followed by the addition of ethyl dithioacetate (0.03 ml, 0.26 mmol) and stirred at room temperature for 16 h. The reaction mixture was diluted with ethyl acetate (50 mL), washed with water followed by brine and dried over sodium sulfate. Solvent was evaporated and the residue was purified by column chromatography using 4% methanol in chloroform as eluent. Relevant fractions were combined and evaporated to obtain the desired product as a white powder (28 mg, 47%), mp 138 °C
1H NMR (CDCI3): 5 8.28-8.21 (m, IH), 8.14 (s, IH), 7.35 (d, 7 = 7.8 Hz, 2H), 5.98-5.92 (m, IH), 5.02 (d, 7 = 5.7 Hz, 2H), 4.38-4.31 (m, 2H), 3.95 (t, 7- 5.4 Hz, 2H), 2.61 (s, 3H), 2.48-2.40 (m, 2H).
MS (m/e): 351 (M^+1), 335, 323, 252.
IR(KBr): 3221,3041,2929, 1631, 1510, 1452, 1386, 1028 cm-1 Example-10
{l-[4-(3,6-Dihydro-2iy-pyran-4.yl)-3,5-difluoro-phenyl]-liy-[l,2,3]triazoI-4-ylmethyl}-thiocarbamic acid O-methyl ester:

To a solution of C- {1 -[4-(3,6-dihydro-2H-pyran-4-yl)-3,5-difluoro-phenyl]-1H-[l,2,3]triazol-4-yl}methylamine (50 mg, 0.17 mmol), obtained in example-8, in dichloromethane (4 mL) was added a saturated solution of sodium bicarbonate (35 mg, 0.42 mmol) in water (3 mL) followed by cooling in ice bath. Thiophosgene (0.016 mL, 0.21 mmol) was added to the above mixture at 0 °C and stirred at the same temperature for 0.5 h. The reaction mixture was diluted with dichloromethane (50 mL), and the organic layer with water followed by brine and dried over sodium sulfate. Evaporation of volatiles left a residue, which was refluxed with methanol (5 mL) for 16 h. Methanol was removed under vacuum and the

residue was purified by column chromatography over silica gel (methanol/ chloroform; 1:25)
to get the title compound as a pale pink solid (41 mg, 72%), mp 132 °C.
1H NMR (CDCI3): 5 8.12 and 7.89 (two s, IH, rotamers in a ratio of 4:1), 7.35 (d, J= 7.3 Hz,
2H), 6.98-6.91 (m, IH), 5.98-5.93 (m, IH), 4.92 and 4.65 (d, J= 6.3 Hz, 2H, rotamers in ratio
of 4:1), 4.39-4.32 (m, 2H), 4.10 and 4.00 (two s, 3H, rotamers in a ratio of 1:4), 3.95 (t. 7 =
5.4 Hz, 2H), 2.48-2.41 (m, 2H).
MS (m/e): 367 (M"+l), 335, 319, 278.
IR(KBr): 3237,3126, 1632, 1586, 1448, 1199 cm-1.
ExampIe-11
2-{l-[4-(3,6-Dihydro-2iy-thiopyran-4-yI)-3-fluoro-phenyl]-lJy-[l,2,3]triazol-4-ylmethyl}-
isoindole-l,3-dione:
To a solution of 4-(4-azido-2-fluoro-phenyl)-3,6-dihydro-2H-thiopyran (630 mg, 2.68 mmol), obtained in preaparation-6, and n,n-diisopropylethylamine (0.936 mL, 5.36 mmol) in acetonitrile (10 mL) was added 2-prop-2-ynyl-isoindole-l,3-dione (691 mg, 3.74 mmol) followed by the addition of cuprous iodide (561 mg, 2.95 mmol) and stirred at room temperature for 1 h. The reaction mixture was filtered through a celite pad and washed thoroughly with MeOH. Concentration of the filtrate under vacuum and purification of the resulting residue by flash chromatography (ethyl acetate/ hexane; 4:6) afforded the title compound as a white solid (550 mg, 49%).
1H NMR (CDCI3): 5 8.02 (s, IH), 7.89-7.86 (m, 2H), 7.75-7.71 (m, 2H), 7.49-7.26 (m, 3H), 6.08-6.02 (m, IH), 5.08 (s, 2H), 3.40-3.25 (m, 2H), 2.87 (t, 7 = 5.6 Hz, 2H), 2.69-2.60 (m, 2H).
MS (m/e): 421 (M++1), 389, 276, 248.
IR(KBr): 3458, 2921, 1767, 1617, 1512, 1395, 1236, 1045 cm' Example-12
C-{l-[4-(3,6-Dihydro-2H-thiopyran-4.yl)-3-fluoro-phenyl]-lh-[l,2,3]triazol-4-yl}-methylamine:

To a solution of 2- {1 -[4-(3,6-dihydro-2H'-thiopyran-4-yl)-3-fluoro-phenyl]-1H-[l,2,3]triazol-4-ylmethyl}-isoindole-l,3-dione (520 mg, 1.24 mmol) in methanol (10 mL), obtained in example-11, was added hydrazine hydrate (0.53 mL) and refluxed for 2 h followed by stirring at room temperature for 10 h. The reaction mixture was filtered and the filtrate was concentrated under vacuum. The residue was purified by flash chromatography (methanol/ chloroform; 1:9) to obtain the desired compound as a creamy white solid (205 mg, 57%).
1H NMR (DMS0-d6): 6 8.67 (s, IH), 7.95-7.62 (m, 2H), 7.62-7.29 (m, IH), 6.20-6.03 (m, IH), 4.10-3.78 (m, 2H), 3.78-3.09 (m, 2H), 2.84 (t, J= 5.5 Hz, 2H), 2.70-2.38 (m, 2H). MS (m/e): 291 (M++1), 246, 233.
IR(KBr): 3442, 2929, 1740, 1661, 1575, 1494, 1360, 1231, 1015 cm-1 Example-13
A^-{l-[4-(3,6-Dihydro-2Jy-thiopyran-4-yl)-3-fluoro-phenyl]-1H-[l,2,3]triazol-4-ylmeth thioacetamide:
Triethylamine (0.077 mL, 0.55 mmol) was added to a solution of C-{l-[4-(3,6-dihydro-2i^-thiopyran-4-yl)-3-fluoro-phenyl]-lH-[l,2,3]triazol-4-yl}-methylamine (80 mg, ' 0.276 mmol), obtained in ezample-12, in THF (5 mL) followed by the addition of ethyl dithioacetate (0.049 mL, 0.43 mmol) and stirred at ambient temperature for 16 h. The reaction mixture was concentrated under vacuum and the residue was purified by a silica gel column (1% methanol in chloroform) to give the desired product as a white solid (55 mg, 57%), Mp 107-110 °C.
'H NMR (CDCI3): 5 8.19-8.02 (m, 2H), 7.56-7.18 (m, 3H), 6.17-6.05 (m, IH), 5.02 (d, J= 5.3 Hz, 2H), 3.40-3.30 (m, 2H), 2.88 (t, J= 5.6 Hz, 2H), 2.80-2.50 (m, 2H), 260 (s, 3H). MS (m/e): 349 (M++1), 206, 149, 126.
IR(KBr): 3496, 3194, 2925, 1621, 1566, 1458, 1366, 1234, 1055 cm-1. Example-14

2-{l-[3-Fluoro-4-(l-oxo-l,2,3,6-tetrahydro-llambda*4-thiopyran-4-yl)-phenyl]-liy-[l,2,3]triazol-4ylmethyl}-isoin(lole-l,3-dione:

Sodium periodate (915 mg, 4.28 mmol) in water (10 mL) was added to an ice cooled solution of 2-{l-[4-(3,6-dihydro-2H-pyran-4-yl).3-fluoro-phenyl]-lH-[l,2,3]triazol-4-ylmethyl}-isoindole-l,3-dione (400 mg, 0.95 mmol), obtained in example-1, in methanol (12 mL) and ethyl acetate (12 mL) and stirred for 1 h. The reaction mixture was brought to room temperature and stirred for 16 h. The reaction mixture was diluted with MeOH/CHCl} (1:19), filtered and the filtrate was concentrated under vacuum. The residue obtained was dissolved in chloroform, washed with saturated solution of Na2SO3 and NaHCO3 respectively and dried over sodium sulfate. The solvent was evaporated and the residue was purified by column chromatography over silica gel to afford the desired product (55 mg, 33%) as a white solid.
'H NMR (CDCI3): 5 8.04 (s, IH), 7.87-7.78 (m, 2H), 7.78-7.68 (m, 2H), 7.68-7.35 (m, 3H),
5.86-5.82 (m, IH), 5.08 (s, 2H), 3.69-3.43 (m, 2H), 3.26-3.10 (m, 2H), 3.05-2.69 (m, 2H).
MS (m/e): 437 (M++1), 421, 405, 148.
IR(KBr): 3434, 2923, 2361, 1718, 1513, 1395, 1232, 1032 cm-'.
Example-15
C-{l-[3-Fluoro-4-(l-oxo-l,2,3,6-tetrahydro-lIambda*4*-thiopyran-4-yl)-phenyl]-1H-
[l,2,3]tria2ol-4-yl}-methylamine:

To a solution of 2-{l-[3-fluoro-4-(l-oxo-l,2,3,6-tet^ahydro-llambda*4*-thiopyran-4-yl)-phenyl]-lH-[l,2,3]triazol-4ylmethyl}-isoindole-l,3-dione (250 mg, 0.57 mmol), obtained in example-14, in methanol (5 mL) was added hydrazine hydrate (0.24 mL) and refluxed for 3 h followed by stirring at room temperature for 10 h. The reaction mixture was filtered and the filtrate was concentrated under vacuum. The residue was purified by flash chromatography over silica gel (6% methanol in chloroform) to furnish the title compound (105 mg, 60%) as a pale yellow solid.

'H NMR (CDCI3 + DMS0-d6): 5 8.09 (s, IH), 7.75-7.62 (m, 2H), 7.46-7.39 (m, IH), 5.95-
5.85 (m, IH), 4.07 (s, 2H), 3.63-3.51 (m, 2H), 3.19-2.98 (m, 4H).
MS (m/e): 307 (W+l), 291, 273, 259.
IR(KBr): 3427, 2924, 1618, 1515, 1228, 1029 cm"".
Example-16
iV-{l-[3-Fluoro-4-(l-oxo-l,2,3,6-tetrahydro-llambda*4*-thiopyran-4-yl)-phenyl]-lJ?-
[l,2,3]triazol-4-ylmethyl}-thioacetamide:

To a solution of C-{l-[3-fluoro-4-(l-oxo-l,2,3,6-tetrahydro-llambda*4*-thiopyran-4-yl)-phenyl]-lH-[l,2,3]triazol-4-yl}-methylamine (45 mg, 0.15 mmol), obtained in example-15, in THF (5 mL) was added triethylamine (0.045 mL, 0.23 mmol) followed by the addition of ethyl dithioacetate (0.025 mL, 0.23 mmol) and stirred at room temperature for 16 h. The solvent was evaporated and the crude residue was purified by column chromatography over silica gel (3% methanol in chloroform) to obtain the desired product as a white solid (28 mg, 52%), mp 204 °C,
1H NMR (CDCI3 + DMSO-d^): 6 8.40 (s, 2H), 7.66-7.50 (m, 3H), 6.07-5.92 (m, IH), 4.97 (s, 2H), 4.17 (s, 2H), 3.81-3.47 (m, 2H), 3.34-3.08 (m, 2H), 2.55 (s, 3H). ES-MS (m/e): 387 (M^+23), 365 (M"+l). IR (KBr): 3428, 3012, 2924, 1620, 1543, 1391, 1231, 1030 cm'^ Example-17
{l-[3-Fluoro-4-(l-oxo-l,2,3,6-tetrahydro-llambda*4*-thiopyran-4-yI)-phenyl]-1H-[l,2,3]tria2ol-4-ylmethyI}-thiocarbamic acid O-methyl ester:

A saturated aqueous solution of sodium bicarbonate (41 mg, 0.48 mmol) was added to a solution of C- {1 -[3-fluoro-4-( 1 -0x0-1,2,3,6-tetrahydro-1 lambda*4*-thiopyran-4-yl)-phenyl]-lH-[l,2,3]triazol-4-yl}-methylamine (50 mg, 0.16 mmol), obtained in example-15, in

dichloromethane (5 mL) and then cooled to 0 °C. Thiophosgene (0.018 mL, 0.23 mmol) was
added to the above mixture and stirred at the same temperature for 0.5 h. The reaction mixture
was diluted with dichloromethane (50 mL), washed with water followed by brine and dried
over Na2SO4. The solvent was evaporated and the residue was refluxed with methanol (10
mL) for 16 h. After evaporation of solvent, the residue was purified by column
chromatography over sihca gel (methanol/chloroform; 1:49) to get the title compound as a
white solid (35 mg, 56%), mp 153 °C.
1H NMR (CDCI3 + Methanol-d4): 5 8.27 and 8.08 (two s, IH, rotamers in ratio of 4:1), 7.60-
7.52 (m, 2H), 7.47-7.43 (m, IH), 5.96-5.82 (m, IH), 4.86 and 4.61 (s, 2H, rotamers in ratio of
4:1), 3.99 and 4.10 (two s, 3H, rotamers in ratio of 1:4), 3.72-3.67 (m, IH), 3.54- 3.44 (m,
IH), 3.37-3.24 (m, IH), 3.15-2.96 (m, 2H), 2.80-2.75 (m, IH).
MS (m/e): 349 (Nr-0CH3), 317, 292, 280.
IR(KBr): 3189, 3026, 2927, 1619, 1541, 1408, 1200, 1012 cm"ExampIe-18
2-{l-[4-(14-Dioxo-l,2,3,6-tetrahydro-llambda*6*-thiopyran-4-yl)-3-fluoro-phenyl]-lH-
[l,2,3]triazol-4ylmethyI}-isoindole-l,3-dione:

To a solution of 2-{l-[4-(3,6-dihydro-2/f-thiopyran-4-yl)-3-fluoro-phenyl]-lH-[l,2,3]triazol-4-ylmethyl}-isoindole-l,3-dione (620 mg, 1.48 mmol), obtained in example-1, in dichloromethane (25 mL), cooled to 0 °C, was added m-chloroperbenzoic acid (1.1 g, 70% w/w, 4.44 mmol) in portion and stirred at the same temperature for 0.5 h. The reaction mixture was diluted with dichloromethane (50 mL) and washed with saturated aqueous solutions of sodium bisulfite and sodium bicarbonate respectively. The organic layer was dried over sodium sulfate and concentrated under reduced pressure. The residue was purified by column chromatography over silica gel to afford the desired sulfone derivative (400 mg, 60%) as a white solid along with some sulfoxide(28 mg, 28%)
1H NMR (CDCI3): 5 8.42 (s, IH), 7.97-7.76 (m, 4H), 7.71-7.55 (m, 2H), 7.42-7.38 (m, IH), 5,98-5.85 (m, IH), 5.05 (s, 2H), 3.88-3.82 (m, 2H), 3.30-3.27 (m, 2H), 2.86-2.59 (m, 2H). CI-MS(m/e):453(M++l)

IR(KBr): 3427,2920, 1713, 1620, 1515, 1396, 1286, 1167, 937 cm-1
Example-19
C-{l-[4-{14-Pioxo-l,2,3,6-tetrahydro-llambda*6*-thiopyran-4-yl)-3-fluoro-phenyl]-lJ^^
[l,2,3]triazoI-4-yl}-methyIamine:

Hydrazine hydrate (0.37 mL) was added to a solution of 2-{l-[4-(l,l-dioxo-l,2,3,6-tetrahydro-llambda*6*-thiopyran-4-yl)-3-fluoro-phenyl]-lH-[l,2,3]triazol-4ylmethyl}-iso indole-1,3-dione (400 mg, 0.88 mmol), obtained in example-18, in methanol (10 mL) and refluxed for 2 h followed by stirring at room temperature for 0.5 h. The reaction mixture was filtered and the filtrate was concentrated under vacuum. The residue was purified by flash chromatography over silica gel (6% methanol in chloroform) to produce the title compound as a white soUd (220 mg, 77%).
1H NMR (CDCI3 + DMS0-d6): 5 8.14 (s, IH), 7.69-7.52 (m, 2H), 7.47-7.38 (m, IH), 5.96-5.82 (m, IH), 4.08 (s, 2H), 3.96-3.81 (m, 2H), 3.38-3.18 (m, 2H), 3.18-3.05 (m, 2H). MS (m/e): 323 (IVT+l), 285, 259, 187.
IR(KBr): 3346,2923, 1619, 1515, 1315, 1285, 1123, 1045 cm-1 Example-20
N-{l-[4-(l,l-Dioxo-l,2,3,6-tetrahydro-llambda*6*-thiopyran-4-yl)-3-fluoro-phenyl]-lH-[l,2,3]triazol-4-ylmethyl}-thioacetamide:
R

To a solution of C-{l-[4-(l,l-dioxo-l,2,3,6-tetrahydro-llambda*6*-thiopyran-4-yl)-3-fluoro-phenyl]-l^-[l,2,3]triazoI-4-yI}-methylamine (100 mg, 0.31 mmol), obtained in example-19, in THF (5 mL) was added triethylamine (0.095 mL, 0.68 mmol) followed by the addifion of ethyl dithioacetate (0.052 mL, 0.45 mmol) and stirred at room temperature for 18 h. The solvent was evaporated and the crude residue was purified by column chromatography over silica gel (3% methanol in chloroform) to obtain the desired product (83 mg, 70%) as a pale yellow solid, mp 188 °C.

1H NMR (CDCI3 + DMS0-d6): 5 10.21-10.15 (m, IH), 8.59 (s, IH), 7.82-7.70 (m, 2H), 7.49
(t, y = 8.6 Hz, IH), 5.96-5.84 (m, IH), 4.92 (d, 7= 4.9 Hz, 2H), 3.99-3.92 (m, 2H), 3.38-3.25
(m, 2H), 3.18-3.10 (m, 2H), 2.51 (s, 3H).
CI-MS (mJe): 381 (M++1), 349, 317, 308.
IR (KBr): 3292, 2924, 1621, 1515, 1315, 1287, 1167, 1045 cm-1
Example-21
{l-[4-(l,l-Dioxo-l,2,3,6-tetrahydro-llambda*6*-thiopyran-4-yl)-3-fluoro-phenyl]-lH-
[l,2,3]triazol-4-yImethyl}-thiocarbamic acid 0-methyl ester:

To a solution of C-{1-[4-( 1,1-dioxo-1,2,3,6-tetrahydro-llambda*6*-thiopyran-4-yl)-3-fluoro-phenyl]-lif-[ 1,2,3]triazol-4-yl}-methylamine (100 mg, 0.31 mmol), obtained in example-19, in dichloromethane (8 mL) was added a saturated aqueous solution of sodium bicarbonate (65 mg, 0.77 mmol) followed by cooling in ice bath. Thiophosgene (0.029 mL, 0.37 mmol) was added to the reacion mixture at 0 °C and stirred at the same temperature for 0.5 h. The reaction mixture was diluted with dichloromethane (50 mL), washed the organic layer with water, brine and dried over sodium sulfate. The solvent was evaporated and the residue was refluxed with methanol (10 mL) for 16 h. Methanol was evaporated on rotavapor and the residue was purified by column chromatography over silica gel (4% methanol in chloroform) to yield the title compound as a white solid (86 mg, 70%), mp 178 °C.
1H NMR (CDCI3 + DMS0-d6): 6 9.02-8.87 and 8.87-8.80 (two m, IH, rotamers in ratio of
1:4), 8.30 and 8.18 (two s, IH, rotamers in ratio of 4:1), 7.65-7.56 (m, 2H), 7.46-7.39 (m, IH),
5.97-5.88 (m, IH), 4.87 and 4.60 (two d, 7 = 5.6 Hz, 2H, rotamers in ratio of 4:1), 4.10 and
3.98 (two s, 3H, rotamers in ratio of 1:4), 3,89-3.81 (m, 2H), 3.38-3.20 (m, 2H), 3.19-3.01 (m,
2H).
MS (m/e): 365 (M+-OCH3), 333, 308, 280,
IR(KBr): 3428, 3291, 2924, 2854, 1620, 1515, 1315, 1277, 1041 cm-1
Example-22
2.{l-[4.(3,6-Dihydro-2H-thiopyran.4.yl)-3,5-difluoro-phenyl].liy-[l,2,3]triazol-4.
ylmethyl}-isoindole-l,3-dione:

To a solution of 4-(4-azido-2,6-difluoro-phenyl)-3,6-dihydro-2H-thiopyran (2.13 g, 8.40 mmol), obtained in preparation-8, and N, N-diisopropylethyiamine (2.9 mL, 16.8 mmol) in acetonitrile (25 mL) was added 2-prop-ynyl-isoindole-l,3-dione (2.35 g, 12.6 mmol) followed by the addition of cuprous iodide (2.40 g, 12.60 mmol) and stirred at room temperature for 1 h. The reaction mixture was filtered through a celite pad and washed thoroughly with MeOH/CHCb (1:10).Concentration of the filtrate under vacuum and purification of the resulting residue by flash chromatography (ethyl acetate/hexane; 4:6) yielded the title compound as a light yellow solid (1.60 g, 44%).
1H NMR (CDCI3): 5 8.02 (s, IH), 7.97-7.82 (m, 2H), 7.81-7.65 (m, 2H), 7.32 (d, J= 7.5 Hz,
2H), 6.05-5.97 (m, IH), 5.08 (s, 2H), 3.39-3.35 (m, 2H), 2.88 (t, J- 5.6 Hz, 2H), 2.61-2.47
(m, 2H).
MS (m/e): 439 (M++1), 266, 148.
IR(KBr): 3149, 3067, 2922, 1712, 1633, 1512, 1394, 1094 cm"^
Example-23
C-{l-[4-(3,6-Dihydro.2H-thiopyran.4-yl)-3,5-difluoro-phenyl]-l^-[l,2,3]tria2ol-4-yl}-
methylamine:
To a solution of 2-{l-[4-(3,6-dihydro-2H-thiopyran-4-yl)-3,5-difluoro-phenyl]-li/-[1,2,3] triazol-4-ylmethyl}-isoindole"l,3-dione (400 mg, 0.91 mmol), obtained in example-22, in methanol (12 mL) was added hydrazine hydrate (0.41 mL) and refluxed for 2 h followed by stirring at room temperature for 10 h. The reaction mixture was filtered and the filtrate was concentrated under vacuum. The resultant residue was dissolved in chloroform (100 mL), washed the organic layer with water followed by brine and dried (sodium sulfate). Evaporation of the solvent on a rotavapor and purification of the resulting residue by flash chromatography (ethyl acetate/ hexane; 1:10) afforded the title compound as a pale yellow solid (260 mg, 93%).

'H NMR (CDCI3): 5 7.87 (s, IH), 7.33 (d, J= 7.8 Hz, 2H), 6.15-5.98 (m, IH), 4.08 (s, 2H),
3.41-3.32 (m, 2H), 2.89 (t, J= 5.6 Hz, 2H), 2.61-2.45 (m, 2H).
MS(m/e):309(Mt+l), 280.
IR(KBr): 3357, 3128, 2920, 1631, 1595, 1449, 1220, 1028 cm"'.
£xampie-24
Ar.{1.[4.(3,6-Dihydro-2H-thiopyran-4-yl)-3,5-difluoro-phenyl]-lH-[l,2,3]triazol-4-
ylmethyl}-thioacetamide:

To a solution of C-{l-[4-(3,6-dihyclro-2H-thiopyran-4-yl)-3,5-difluoro-phenyl]-lH-[l,2,3]triazol-4-yl}-methylamine (100 mg, 0.32 mmol), obtained in example-23, in THF (5 mL) was added triethylamine (0.1 mL, 0.72 mmol) followed by the addition of ethyl dithioacetate (0.06 ml, 0.49 mmol) and stirred at room temperature for 16 h. The reaction mixture was diluted with ethyl acetate (75 mL), washed the organic layer with water followed by brine and dried over sodium sulfate. Solvent was evaporated and the residue was purified by column chromatography (silica gel), using 15% methanol in chloroform as eluent, to give the desired product as a white powder (58 mg, 50%), mp 178-179 °C.
1H NMR (CDCI3): 5 8.18-8.09 (m, 2H), 7.34 (d, 7= 7.3 Hz, 2H), 6.08-6.01 (m, IH), 5.02 (d, J - 5.4 Hz, 2H), 3.40-3.31 (m, 2H), 2.89 (t, J= 5.4 Hz, 2H), 2.68-2.48 (m, 5H). MS (m/e): 367 (M++1), 339, 189. IR(KBr): 3204,2999, 1632, 1510, 1344, 1050 cm"^ Example-25
{l-[4-(3,6-Dihydro-2H-thiopyran-4-yl)-3,5-difluoro-phenyl]-lH-[l,2,3]triazol-4-ylmethyl}-thiocarbamic acid O-methyl ester:

To a solution of C-{l-[4-(3,6-dihydro-2H-thiopyran-4-yl)-3,5-difluoro-phenyl]-l/]r-[ 1,2,3]triazol-4-yl}-methylamine (90 mg, 0.29 mmol), obtained in exampie-23, in

dichloromethane (10 mL) was added a solution of sodium bicarbonate (62 mg, 0.73 nimol) in
water (3 mL) followed by cooling in ice bath. Thiophosgene (0.03 mL, 0.35 mmol) was added
to the above mixture at 0 °C and stirred at the same temperature for 0.5 h. The reaction
mixture was diluted with dichloromethane (50 mL), washed the organic layer with water
followed by brine and dried over sodium sulfate. Evaporation of volatiles left a residue, which
was refluxed with methanol (15 mL) for 16 h. Removal of solvent on rotavapor and
purification of the residue by column chromatography (ethyl acetate/ hexane; 3:10) yielded
the title compound as a white powder (72 mg, 65%), mp 156-158 °C.
1H NMR (CDCI3): 8 8.10 (s, IH), 7.34 (d, J= 7.8 Hz, 2H), 6.15-5.97 (m, IH), 4.91 and 4.68
(two d, y= 5.9 Hz, 2H, rotamers in ratio of 4:1), 4.12 and 3.99 (two s, 3H, rotamers in ratio of
1:4), 3.40-3.31 (m, 2H), 2.89 (t, / = 5.6 Hz, 2H), 2.61-2.50 (m, 2H).
MS (m/e): 383 (M>1), 351, 335, 294.
IR(KBr): 3193, 3123,2924, 1633,1593, 1454, 1125 cm'.
Example-26
2-{l-[3,5-Difluoro-4-(l-oxo-l,2,3,6-tetrahydro-llambda*4*-thiopyran-4-yl)-phenyl]-lH-
[l,2,3]triazol-4ylmethyl}-isoindole-l,3-dione:

Sodium periodate (410 mg, 1.92 mmol) in water (5 mL) was added to an ice cooled solution of 2-{l-[4-(3,6-dihydro-2H-pyran-4-yl)-3,5-difluoro-phenyl]-lH-[l,2,3]triazol-4-ylmethyl}-l,3-isoindole-l,3-dione (350 mg, 0.79 mmol), obtained in example-22, in methanol (12 mL) and ethyl acetate (12 mL) and stirred at the same temperature for 1 h. The reaction mixture was warmed to room temperature and stirred for 16 h. The reaction mixture was diluted with methanol (1 mL) and chloroform (19 mL), and filtered. The filtrate was concentrated under vacuum. The residue obtained was dissolved in chloroform, washed with saturated solutions of Na2SO3 and NaHCO3 and dried over sodium sulfate. Evaporation of solvent and purification of the residue by column chromatography over silica gel (ethyl acetate) afforded the desired product (295 mg, 81%) as a pale yellow solid. 1H NMR (DMSO-d6): δ 8.86 (s, IH), 8.00-7.68 (m, 6H), 5.86-5.76 (m, IH), 4.94 (s, 2H), 4.01-3.92 (m, 2H), 3.45-3.18 (m, 2H), 2.96-2.82 (m, 2H),

MS (m/e): 455 (NT+I), 439, 421
IR(KBr): 3459, 1714, 1428, 1395, 1208, 1034 cm-1.
Example-27
C-{l-[3,5-Difluoro-4-(l-oxo-l,2,3,6-tetrahydro-llambda*4*-thiopyran-4-yl)-phenyl]-lH-
[l,2,3]triazol-4-yl}-niethylamine:

To a solution of 2-{l-[3,5-difIuoro-4-(l-oxo-l,2,3,6-tetrahydro-llambda*4*-thiopyran-4-yl)-phenyl]-lH-[l,2,3]triazol-4ylmethyi}-isoindole-l,3-dione (290 mg, 0.64 mmol), obtained in example-26, in methanol (10 mL) was added hydrazine hydrate (0.27 mL) and refluxed for 2 h followed by stirring at room temperature for 10 h. The reaction mixture was filtered and washed with chloroform (5% methanol). The filtrate was concentrated under vacuum and the residue was purified by flash chromatography. (3% methanol in chloroform) to afford the title compound (126 mg, 62%) as a white solid. 1H NMR (CDCI3 + DMS0-d6): 5 8.58 (s, IH), 7,66 (d, J= 8.3 Hz, 2H), 5.84-5.80 (m, IH), 3.94 (s,2H), 3.75-2.96 (m,6H). MS (m/e): 325 (M++1), 309, 181.
IR(KBr): 3441,2924, 1632, 1583, 1452, 1366, 1207, 1034 cm-1. Example-28
A^-{l-[3,5-Difluoro-4-(l-oxo-l,2,3,6-tetrahydro-llambda*4*-thiopyran-4-yl)-phenyI]-lH-[l,2,3]triazoI-4-yImethyl}thioacetamide:

To a solution of C-{l"[3,5-difluoro-4-(l-oxo-l,2,3,6-tetrahydro-llambda*4*-thiopyran-4-yl)-phenyl]-lH-[l,2,3]triazol-4-yl}-methylamine (60 mg, 0.185 mmol), obtained in example-27, in THF (5 mL) was added triethylamine (0.058 mL, 0.41 mmol) followed by the addition of ethyl dithioacetate (0.033 mL, 0.28 mmol) and stirred at room temperature for 16 h. The solvent was evaporated from the reaction mixture and the residue was purified by

column chromatography (2% methanol in chloroform) to obtain the desired product as a pale
yellow solid (40 mg, 57%), mp 182-184 °C.
1HNMR(CDCl3 + DMSO-d6): δ 10.15-10.10 (m, IH), 8.38 (s, IH), 7.50-7.38 (m, 2H), 5.84-
5.81 (m, IH), 4.95 (d, 7 = 5.4 Hz, 2H), 3.71-3.66 (m, 2H), 3.48-3.43 (m, 2H), 3.24-3.18 (m,
2H), 2.58 (s, 3H).
MS (m/e): 383 (M++1), 367, 365, 339, 310.
IR(KBr): 3184, 3003, 1632, 1562, 1450, 1280, 1023 cm"'.
Example-29
{l-[3,5-Difluoro-4-(l-oxo-l,2,3,6-tetrahydro-llambda*4*-thiopyran-4-yl)-phenyl]-l^-
[l,2,3]triazol-4-ylmethyl}-thiocarbainic acid 6>-methyl ester:

A solution of sodium bicarbonate (41 mg, 0.48 mmol) in water (5 mL) was added to an ice cooled solution of C-{l-[3,5-difluoro-4-(l-oxo-l,2,3,6-tetrahydro-llambda*4*-thiopyran-4-yl)-phenyi]-lH-[l,2,3]triazol-4-yl}-methylamine (63 mg, 0.194 mmol), obtained in exampIe-27, in dichloromethane (5 mL). Thiophosgene (0.020 mL, 0.26 mmol) was added to the reaction mixture and stirred for 0.5 h. The reaction mixture was diluted with dichloromethane (50 mL), washed the organic layer with water followed by brine and dried over sodium sulfate. The solvent was evaporated and the residue was refluxed with methanol (15 mL) for 16 h. After evaporation of methanol, the residue was purified by column chromatography over silica gel (methanol/chloroform; 1:25) to furnish the title compound as a white powder (50 mg, 65%), mp 206-208 °C.
'H NMR (CDCI3 + DMS0-d6): 5 8.58-8.54 and 8.46-8.39 (two m, IH, rotamers in ratio of
1:4), 8.14 and 8.00 (two s, IH, rotamers in ratio of 4:1), 7.33 (d, 7= 7.8 Hz, 2H), 5.75-5.71
(m, IH), 4.74 and 4.45 (two d, J = 5.9 Hz, 2H, rotamers in ratio of 4:1), 3.90 and 3.86 (two s,
3H, rotamers in ratio of 1:4), 3.60-3.55 (m, 2H), 3.37-3.32 (m, 2H), 3.11-3.07 (m, 2H).
MS (m/e): 367 (M^-OCHa), 351, 335, 325, 294.
IR(KBr): 3442, 2924, 1715, 1634, 1518, 1452, 1233, 1030 cm-1
Example-30

N-{l-[3,5-Difluoro-4-(l-oxo-l,2,3,6-tetrahydro-llambda*4*&-thiopyran-4-yI)-phenyl]-1H [l,2,3]triazol-4-ylmethyl}-acetamide:

To a solution of C-{l-[3,5-difluoro-4-(l-oxo-1.2,3,6-tetrahydro-llambda*4*-thiopyran-4-yl)-phenyl]-lH-[l,2,3]triazol-4-yl}-methylamine (80 mg, 0.25 mmol), obtained in example-27, in dichloromethane (5 mL), cooled to 0 ^C was added triethylamine (0.069 mL, 0.49 mmol) followed by the addition of acetyl chloride (0.02 mL, 0.29 mmol) and stirred at room temperature for 3 h. The solvent was evaporated from the reaction mixture and the residue was purified by column chromatography on silica (4% methanol in chloroform) to afford the required compound as a creamy white solid (45 mg, 50%), mp 177-180 °C. 1H NMR (DMS0-d6): 5 8.74 (s, IH), 8.54-8.39 (m, IH), 7..84 (d, J= 8.3 Hz, 2H), 5.92-5.78 (m, IH), 4.37 (d,y= 5.6 Hz, 2H), 3.80-3.10 (m, 6H), 1.86 (s, 3H). MS (m/e): 367 (NT+I), 318, 290, 231.
IR(KBr): 3323, 3128, 2926, 1648, 1532, 1455, 1206, 1026 cm■^ Example-31
{l-[3,5-Difluoro-4-(l-oxo-l,2,3,6-tetrahydro-llambda*4*-thiopyran-4*yl)-phenyI]-lH-[l,2,3]triazol-4-ylmethyl}-carbamic acid methyl ester:

H,A^-Diisopropylethylamine (0.11 mL, 0.63 mmol) was added to an ice cooled solution of C-{l-[3,5-difluoro-4-(l-oxo-l,2,3,6-tetrahydro-llambda*4*-thiopyran-4-yl)-phenyl]-lH-[l,2,3]triazol-4-yl}-methylamine obtained in example-27 (80 mg, 0.25 mmol) in dichloromethane (5 mL), followed by the addition of methyl chloroformate (0.023 mL, 0.29 mmol) and stirred for 2 h. The reaction mixture was concentrated on rotavapor and the resulting residue was purified by column chromatography (3% methanol in chloroform) to yield the desired product (50 mg, 53%) as a creamy white solid, mp 172-174 °C.

1H NMR (DMS0-d6): 5 8.75 (s, IH), 7.98-7,72 (m, 3H), 5.91-5.80 (m, IH), 4.32 (d, y = 5.8
Hz, 2H), 3.80-3.10 (m, 6H), 3.57 (s, 3H).
MS(m/e):383(Mt+l), 351.
IR(KBr): 3333, 2924, 2854, 1696, 1543, 1454, 1264, 1032 cm-ExampIe-32
2-{l-[4-(l,l-Dioxo-l,2,356-tetrahydro-llambda*6*-thiopyran-4-yl)-3,5-difluoro-phenyl]-1H-[l,2,3]triazol-4ylmethyI}-isoindole-l,3-dione:

u To a solution of 2- {l-[4-(3,6-dihydro-2H-pyran-4-yl)-3,5-difluoro-phenyl]-lH-[l,2,3]triazol-4-ylmethyl}-l,3-isoindole-l,3-dione (710 mg, 1.6 mmol), obtained in example-7, in dichloromethane (25 mL), was added m-chloroperbenzoic acid (1.3 g, 5.26 mmol, 70% w/w) in portion at 0 °C and the mixture was stirred for 0.5 h. The reaction mixture was diluted with dichloromethane (75 mL) and washed with water followed by brine. The organic layer was dried over sodium sulfate and evaporated. The residue was purified by column chromatography over silica gel (4% methanol in chloroform) to afford the desired product (375 mg, 49%) as a white solid.
1H NMR (DMS0-d6): 5 8.85 (s, IH), 7.88-7.78 (m, 4H), 7.75 (d, J= 8.6 Hz, 2H), 5.92-5.79
(m, IH), 4.97 (s, 2H), 3.96-3.89 (m, 2H), 3.32-3.18 (m, 2H), 3.02-2.86 (m, 2H),
MS (m/e): 471 (M++1), 391, 298, 185.
IR(KBr): 3459, 3146, 1713, 1634, 1396, 1286, 1031 cm'.
Example-33
C-{l-[4-(l,l-Dioxo-l,2,3,6-tetrahydro-llambda*6*-thiopyran-4-yl)-3,5-difluoro-phenyl]-
l/r-[l,2,3]triazol-4-yl}-methylamine:

Hydrazine hydrate (0.312 mL) was added to a solution of 2-{l-[4-(l,l-dioxo-l,2,3,6-tetrahydro-llambda*6*-thiopyran-4-yl)-3,5-difluoro-phenyl]-lH-[l,2,3]triazol-4ylmethyl}-isoindole-l,3-dione (350 mg, 0.74 mmol), obtained in example-32, in methanol (15 mL) and

refluxed for 2 h followed by stirring at room temperature for 16 h. The reaction mixture was filtered and washed with a mixture of chloroform/methanol. The filtrate was concentrated under vacuum and the residue was purified by flash chromatography over silica gel (4% methanol in chloroform) to get the title compound as a white solid (195 mg, 77%).
'H NMR (CDCI3 + DMS0-d6): 5 8.38 (s, IH), 7.58 (d, J= 7.8 Hz, 2H), 5.92-5.83 (m, IH),
4.03 (s, 2H), 3.93-3.87 (m, 2H), 3.18-2.96 (m, 2H), 2.60-2.58 (m, 2H).
MS (m/e): 341 (NT+I), 277, 181.
IR(KBr): 3449,2923, 1634, 1599, 1515, 1324, 1288, 1029 cm-'.
Example-34
N-{l-[4-(l,l-Dioxo-l,2,3,6-tetrahydro-llambda*6*-thiopyran-4-yl)-3,5-difluoro-phenyl]-
lH-[l,2,3]triazol-4-ylmethyl}thioacetamide:

To a solution of C-{l-[4-(l,ldioxo-l,2,3,6-tetrahydro-llambda*6*-thiopyran-4-yl)-3,5-difluoro-phenyl]-l/f-[l,2,3]triazol-4-yl}-methylamine (100 mg, 0.294 mmol), obtained in example-33, in THF (5 mL) was added triethylamine (0.082 mL, 0.58 mmol) followed by the addition of ethyl dithioacetate (0.051 mL, 0.44 mmol). The reaction mixture was stirred at ambient temperature for 16 h and then concentrated on rotavapor The residue was purified by column chromatography (2% methanol in chloroform) to obtain the desired product (58 mg, 50%) as a pale yellow solid, mp 210 oC.
'H NMR (CDCI3 + DMSO-d6): 6 9.96-9.82 (m, IH), 8.33 (s, IH), 7.46 (d, 7 = 7.8 Hz, 2H), 5.96-5.82 (m, IH), 4.98 (d, J= 5.4 Hz, 2H), 3.95-3.82 (m, 2H), 3.29-3.26 (m, 2H), 3.18-3,06 (m,2H),2.56(s,3H). MS (m/e): 399 (M++1), 371, 271.
IR(KBr): 3482,3291,2921, 1632, 1551, 1454, 1282, 1168cm-1 Example-35
N-{l-[4-(l-l-Dioxo-l,2,3,6-tetrahydro-llambda*6*-thiopyran-4-yl)-3,5-difluoro-phenyl]-lH- [l,2,3]triazol-4-ylmethyl}-acetamide:

To a solution of C-{l-[4-(lJ-dioxo-l,23,6-tetrahycko-llambda*6*-thiopyran-4-yl)-3,5-difluoro-phenyl]-lH-[l,2,3]triazol-4-yl}-methylamine (100 mg, 0.29 mmol), obtained in example-33, in dichloromethane (5 mL), cooled to 0 °C, was added triethylamine (0.91 mL, 0.65 mmol) followed by the addition of acetyl chloride (0.023 mL, 0.320 mmol). The reaction mixture was brought to room temperature and stirred for 3 h. Evaporation of solvent from the reaction mixture and purification of the residue by column chromatography (methanol/ chloroform; 1:24) yielded the title compound (60 mg, 53%) as a white solid, mp 242-246 ""C. 1H NMR (DMS0-d6): 5 8.74 (s, IH), 8.52-8.40 (m, IH), 7.84 (d, 7 = 8.6 Hz, 2H), 5.90-5.84 (m, IH), 4.36 (d, y = 5.6 Hz, 2H), 4.04-3.91 (m, 2H), 3.44-3.13 (m, 2H), 2.98-2.87 (m, 2H), 1.86 (s,3H).
MS(m/e):383(Nr+l), 239..
IR(KBr): 3287, 3094, 2926, 1630, 1543, 1286, 1058 cm-1. £xample-36
{l-(4-(l,l-Dioxo-l,2,3,6-tetrahydro-lIambda*6*-thiopyran-4-yl)-3,5-difluoro-phenyl]-l/?-[l,2,3]triazol-4-ylmethyl}-thiocarbamic acid O-methyl ester:

To a solution of C-{l-[4-(l,l-dioxo-l,2,3,6-tetrahydro-llambda*6*-thiopyran-4-yl)-3,5-difluoro-phenyl]-li/-[l,2,3]triazol-4-yl}-methylamine (90 mg, 0.26 mmol), obtained in example-33, in dichloromethane (5 mL) was added a saturated solution of sodium bicarbonate (64 mg, 0.76 mmol) in water (5 mL) followed by cooling in ice bath. Thiophosgene (0.027 mL, 0.35 mmol) was added to the above mixture at 0 °C and stirred for 0.5 h. The reaction mixture was diluted with dichloromethane (50 mL), washed the organic layer with water, brine and dried over sodium sulfate. The solvent was evaporated and the residue was refluxed with methanol (5 mL) for 16 h. Methanol was evaporated on a rotavapor and the residue was purified by column chromatography over silica gel (4% methanol in chloroform) to yield the title compound as a white powder (54 mg, 50%), mp 196 °C.

'H NMR (CDCI3): 5 8.14 and 7.90 (two s, IH, rotamers in ratio of 4:1), 7.40 (d, J= 7.8 Hz.
2H), 6.96-6.85 (m, IH), 5.90-5.82 (m, IH), 4.92 and 4.65 (two d, 7 = 5.9 Hz, 2H, rotamers in
ratio of 4:1), 4.10 and 4.00 (two s, 3H, rotamers in ratio of 1:4), 3.92-3.83 (m, 2H), 3.38-3.21
(m,2H), 3.18-3.08 (m,2H).
MS (m/e): 415 (Nf+1), 383, 326, 298.
IR(KBr): 3269, 1634, 1530, 1451, 1322, 1282, 1201, 1027 cm-'
Example-37
{l-[4-(l,l-Dioxo-l,2,3,6-tetrahyclro-llambda*6*-thiopyran-4-yl)-3,5-difluoro-phenyl]-
lH-[l,2,3]triazoI-4-ylmethyl}-carbamic acid methyl ester:

To an ice cooled solution of C-{l-[4-(l,l-dioxo-l,2,3,6-tetrahydro-llambda*6*-thiopyran-4-yl)-3,5-difluoro-phenyl]-lH--[l,2,3]triazol-4-yl}-methylamine (60 mg, 0.8 mmol), obtained in example-33, in dichloromethane (5 mL), was added N, A'-diisopropylethylamine (0.067 mL, 0.38 mmol) followed by the addition of methyl chloroformate (0.016 mL, 0.21 mmol). The reaction mixture was stirred at the same temperature for 2 h. The solvent was evaporated from the reaction mixture and the residue was purified by column chromatography over silica gel (methanol/ chloroform; 1:9) to afford the required product (42 mg, 60%) as a creamy white solid, mp 190-194 °C.
'H NMR (DMS0-d6): 5 8.77 (s, IH), 7.84-7.75 (m, IH), 7.84 (d, 7 = 7.3 Hz, 2H), 5.92-5.82 (m, IH), 4.33 (d, /= 5.8 Hz, 2H), 4.08-3.90 (m, 2H), 3.57 (s, 3H), 3.50-3.19 (m, 2H), 2.99-2.82 (m, 2H).
MS (m/e): 399 (M*+l), 367.
IR(KBr): 3334, 2925, 1691, 1541,1456, 1263, 1031 cm"'. Example-38
{l-[4-(3,6-Dihydro-2H-pyran-4-yl)-3,5-difluorophenyl]-lH-[l,2,3]triazoI-4-yImethyl}-carbamicacid methyl ester:

N-Diisopropylethylamine (0.127 mL, 0.729 mmol) was added to an ice cooled solution of C-{l-[4-(3,6-dihydro-2H-pyran-4-yl)-3,5-difluoro-phenyl]-lH-[1.2,3]triazol-4-yl]--methylamine (100mg, 0.365 mmol), obtained in example-8, in dichloromethane (5 niL), followed by the addition of methyl chioroformate (0.034 mL, 0.438 mmol) and stiiTed at the same temperature for 3 h. The reaction mixture was concentrated on rotavapor and the resulting residue was purified by column chromatography over silica gel (3% methanol in chloroform) yielded the desired product (60 mg, 47%) as a white solid, mp 165-170 °C. 'H NMR (CDCI3): 5 7.99 (s, IH), 7.34(d, J-7.8 Hz, 2H), 6.00-5.96 (m, IH), 4.51 (d, J = 5.6 Hz, 2H), 4.38-4.31 (m, 2H), 3.94 (t, J=5.3 Hz, 2H), 3.69(s, 3H), 2,45-2.38(m, 2H). CI-MS(m/e):351 (M++1).
IR (KBr): 3341, 2928, 1698, 1635, 1549, 1454. 1267, 1028, 860, 773 cm"'. Example-39
{l-[4-(3,6-Dihydro-2H-thiopyran-4-yl)-3-fluoro-phenyI]-lH-[l,2,3]triazol-4-ylmethyl} thiocarbamic acid O-methyl ester:

A saturated solution of sodium bicarbonate (133mg, 1.58mmol) in water (5ml) was added to an ice cooled solution of C-[l-[4-(3,6-dihydro-2H-thiopyran-4-yl)-3-fluoro-phenyl]-lH-[l,2,3]triazol-4-yl}-methylamine (200 mg, 0.689 mmol), obtained in example-12, in dichloromethane (5 mL). Thiophosgene (0.068 mL, 0.895 mmol) was added to the reaction mixture and stirred at the same temperature for 0.5 h. The reaction mixture was diluted with dichloromethane (50 mL), washed the organic layer with water followed by brine and dried over sodium sulfate. The solvent was evaporated and the residue was refluxed with methanol (15 mL) for 16 h. After evaporation of methanol, the residue was purified by column chromatography over silica gel (methanol/chloroform; 1:25) to furnish the title compound as a creamy white solid (150 mg, 60%), mp 110-113 T.
'H NMR (CDCI3): 5 7.99 (s, IH), 7.56-7.32 (m, 3H), 6.16-6.05 (m, IH). 4.52(d. J=6.3 Hz, 2H), 3.70 (s. 3H), 3.42-3.31(m, 2H), 2.88 (t, J=5.8 Hz, 2H), 2.75-2.63 (m, 2H). CI-MS(m/'e):365(M^+l).

IR(KBr): 3329, 3149. 2923, 1619, 1540, 1514, 1458, 1357, 1266, 1229. 1145. 1046. 1011. 872,619 cm-'.
In vitro Data
Minimum Inhibiton Concentrations (MICs) were determined by broth microdilution technique as per the guidelines prescribed in the fifth edition of Approved Standards, NCCLS document M7-A5 Vol 20 - No 2, 2000 Villinova, PA.
Initial stock solution of the test compound was prepared in DMSO. Subsequent two fold dilutions were carried out in sterile Mueller Hinton Broth (Difco) (MHB).
Frozen cultures stocks were inoculated into 50 ml sterile MHB in 250 ml Erlyn Meyer flasks.
Composition of MHB is as follows: Beef Extract Powder - 2.0 s/litre Acid Digest of Casein - 17.5 g/ litre Soluble Starch - 1.5 e/litre Final pH 7.3 ±0.1
Flasks were incubated for 4 to 5 h at 35 'oC on a rotary shaker at 150 rpm. Inoculum was prepared by diluting the culture in sterile MHB to obtain a turbidity of 0.5 McFarland standard. This corresponds to 1-2 x 10 CFU/ml. The stock was further diluted in sterile broth to obtain 1-2X10 CFU/ml. 50µ1 of the above diluted inoculum was added from 1-10 wells. The plates were incubated overnight at 37 °C.
MIC is read as the lowest concentration of the compound that completely inhibits growth of the organism in the microdilution wells as detected by the unaided eye.

ATCC; American Type Culture Collection, USA
NCTC: National Collections of Type Cultures. Colindale, UK
DRCC: Dr. Reddy's Culture Collection, Hyderabad, India.
The in vitro antibacterial activity data is shown in TABLE 1.
TABLE 1

In vivo efficacy studies: Mice Systemic Infection
• S.aureus ATCC 29213 and other tested strains were grown overnight on Columbia
Blood agar (DIFCO).
• The inoculum was prepared by suspending the culture in 0.9% saline and adjusted to
100 X LD50 dose in 10% Hog Gastric Mucin (DIFCO). 0.5ml was injected
intraperitonially to Swiss albino mice weighing 18-22g (n=6)

• Test compounds were solubilised in suitable formulation and 0.25ml was administered intra venously or orally or sub-cutaneously at 1 hr and 5 hr post infection by BID or TDD or single dose protocol
• The animals were observed for 5-7 days and the survival was noted.
• ED50 was calculated by probit analysis.

We claim:
1. A compound of formula (I)

where R1 represents halogen, azido, thioalcohol, isothiocyanate, hydroxy, isoindole-l,3-dione,
substituted or unsubstituted (C1-C10)alkylsulfonyloxy, arylsulfonyloxy, (C1-C10)acyloxy
group, NHR4 where R4 represents substituted or unsubstituted groups selected from (C1-
C10)alkyl, (CrC)o)acyl, thio(C1-C10)acyl, (C1-C10)alkoxycarbonyl, (C3-
Cio)cycloalkoxycarbonyl5 (C3-Cio)cycloalkoxythiocarbonyl, (C2-Cio)alkenyloxycarbonyl, (C2-
Cio)alkenylcarbonyl, heteroaryl, aryloxycarbonyl, heteroarylcarbonyl, heteroarylthiocarbonyl,
(C1-C10)alkoxythiocarbonyl, (C2-Cio)alkenyloxythiocarbonyl, aryloxythiocarbonyl, -C(=O)-
C(=O)-(C1-C10)alkyl, -C(=O)-C(=O)-aryl, -C(=O)-C(=O)-(C1-C10) alkoxy, -C(=O)-C(=O)-
aryloxy, -C(=O)-C(=S)-(C1-C10)alkyI, -C(=O)-C(=S)-aryl, -C(=S)-S-(C1-C10)alkyl, -C(=S)-
NH2, -C(=S)-NHKC1-C10)alkyl, -C(=S)-N-((C1-C10)alkyl)2, -C(=S)-NH-(C2-Cio)alkenyl, -
C(=S)-C(=O)- (C1-C10)alkoxy, -CeS)-C(=O)-aryloxy, -C(=S)-0-C(=O)-(C1-C10) alkyl, -
C(-S)-C(=S)-(C1-C10)alkyl, -C(=S)-C(=S)-aryl, -C(-S)-NH-C(=O)-aryl, -C(=S)-NH-aralkyl, -
C(=S)-NH-heteroaralkyl, -C(=NH)-NH2, -C(=NH)-(C1-C10)alkyl, -C(=NH)-aryl, -S (O)2(C1-
Cio)alkyl, -S(0)2aryl, thiomorpholinylthiocarbonyl, pyrrolidinylthiocarbonyl or -C(=S)-
N(R'R"), where R' and R" together form a substituted or unsubstituted 5 or 6 member
heterocycle ring containing nitrogen and optionally having one or two additional hetero atoms
selected from O, S or N; R and R may be same or different and independently represent
hydrogen, halogen atom, substituted or unsubstituted (C1-C10)alkyl group, halo(C1-C10)alkyl,
aryl, heteroaryl, aralkyl, cyano, nitro, OR4 where R1 represents substituted or unsubstituted
(C1-C10)alkyl group; Y and Y may be same or different and independently represent
hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or
unsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(Cr
Cio)alkyl, (C1-C10)alkoxycarbonyl, caTboxy(C1-C10)alkyl, (C1-C10)alkylsulfonyl, (Cj-
Cio)alkylcarbonylamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10)
alkylcarbonyloxy(C1-C10)alkyl, amino(C1-C10)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y , Y may represent =O, =S,

substituted or unsubstituted =NOR'" group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates.
2. The compoimd of formula (I), as claimed in claim 1, wherein a 5 or 6 member heterocycle ring containing nitrogen, optionally having one or two additional heteroatoms selected from oxygen, nitrogen or sulfur, formed by R' & R" is selected from imsubstituted or substituted pyrrolidinyl, pyrrolyl, morpholinyl, thiomorpholinyl, benzothiazole, benzoimidazolyl, pyridinyl, pyridazinyl, pyrimidinyl or pyrazinyl.
3. The compoimd of formula (I), as claimed in claim 1, where in the substituents on the groups represented by R4, R4a, R4b, 44c, 44d R4e R, R7 and heterocycles formed by R'and R" are selected from halogen atom, hydroxy, amino, cyano, nitro, (C1-C10)alkyl, hydroxy(Ci-Cio)alkyl, (C1-C10)alkoxy =0, =S, aryl, hydroxyaryl, pyridyl, mono(C1-C10)alkylamino, di(Ci-Cio)alkylamino, (C1-C10)acyl, thio(C1-C10)acyl, (C1-C10)alkoxycarbonyl, (C1-C10)alkoxyaryl, or carboxyhc acid or its derivatives.
4. The compound as claimed in claim 1, wherein the substituents on R2, R3 and R4 are selected from hydroxy, halogen, nitro, amino, (C1-C10)alkyl, (C1-C10)alkoxy, =O, =S, cyano group, or carboxylic acid or its derivatives.
5. The compound as claimed in claim 1, wherein the substituents on Y1 and Y2 are selected from hydroxy, nitro, cyano, amino, tert-butyldimethylsilyloxy (TBSO), halogen atom, (C1-C10)alkyl, (C1-C10)alkoxy, cyclo(C3-Cio)alkyl, aryl, benzyloxy, acyl or acyloxy group.
6. The compound of formula (I) as claimed in claim 1, wherein R4 is (C1-C10)acyl, thio(C1-C10)acyl, (C1-C10)alkoxycarbonyl, (C1-C10)alkoxythiocarbonyl.
7. The compound of formula (I) as claimed in claim 1, wherein R2 and R3 represent hydrogen and halogen.
8. The compound of formula (I) as claimed in claim 1, wherein 'm' represents 1.
9. The compound of formula (I) as claimed in claim 1, wherein ' ' represents a bond.
10. The compound of formula (I) as claimed in claim 1, wherein R4 is (C1-C10)acyl, thio(C1-C10)acyl, (C1-C10)alkoxycarbonyl, (C1-C10)alkoxythiocarbonyl; m represents 1; '....' represents a bond and R & R represent hydrogen and halogen.

11. The compound of formula (I) as claimed in claim 1, wherein R is (C1-C10)acyl,
thio(C1-C10)acyl, (C1-C10)alkoxycarbonyl, (C1-C10)alkoxythiocarbonyl; m represents 1; '....'
represents a bond; R2 and R1 represent hydrogen and halogen and Y1 & Y2 represent
hydrogen atom.
12. The compound of formula (I) as claimed in claim 1, wherein R4 is (C1-C10)acyl; m
represents 1; '....' represents a bond; R2 and R3 represent hydrogen and halogen and Y1 &Y^
represent hydrogen atom.
13. The compound of formula (I) as claimed in claim 1, wherein R is thio(C1-C10)acyl; m
represents 1; '....' represents a bond; R2 and R3 represent hydrogen and halogen and Y1 & Y
represent hydrogen atom.
14. The compound of formula (I) as claimed in claim 1, wherein R4 is (C1-
C10)alkoxycarbonyl; m represents 1; '....' represents a bond; R2 and R3 represent hydrogen
and halogen and Y* & Y^ represent hydrogen atom.
15. The compound of formula (I) as claimed in claim 1, wherein R"* is (C1-
Cio)alkoxythio6arbonyl; m represents 1; '....' represents a bond; R2 and R3 represent
hydrogen and halogen and Y1 & Y2 represent hydrogen atom.
16. The compound of formula (I) as claimed in claim 1, wherein R4 is -C(=O)-CH3, -
C(=S)-CH3, -C(=O)-OCH3, -C(=S)-0CH3; m represents 1; ..' represents a bond; R2 and R3 represent hydrogen and fluorine and Y^ & Y^ represent hydrogen atom.
17. The compound of the formula (I) or a pharmaceutically aceeptable salts thereof, as
claimed in claim 1, selected from:

18. The compound of formula (I), as claimed in claim 1 or 17, wherein the
pharmaceutically acceptable salt is selected from the group consisting of Li, Na, K, Ca, Mg,
Fe, Cu, Zn, Mn; salts of organic bases, chiral bases, natural amino acids, unnatural amino
acids, substituted amino acids, guanidine, substituted guanidine salts; ammonium, substituted
ammonium salts, aluminum salts or acid addition salts.
19. The compound of formula (I), as claimed in claim 18, wherein the salts of organic
bases are selected from the group consisting of N,N'-diacetylethylenediamine, betaine,
caffeine, 2-diethylaminoethanol, 2-dimethylaminoethanol, N-ethylmorpholine. N-

ethylpiperidine, glucamine, glucosamine, hydrabamine, isopropylamine, methylglucamine, morpholine, piperazine, piperidine, procaine, purines, theobromine, triethylamine, trimethylamine, tripropylamine, tromethamine, diethanolamine, meglumine, ethylenediamine, N,N'-diphenylethylenediamine, N,N'-dibenzylethylenediamine, N-benzyl phenylethylamine, choline, choline hydroxide, dicyclohexylamine, metformin, benzylamine, phenylethylamine, dialkylamine, trialkylamine, thiamine, aminopyrimidine, aminopyridine, purine, or spermidine.
20. The compound of formula (I) as claimed in claim 18, wherein the salts of chiral bases are selected from the group consisting of alkylphenylamine, glycinol, or phenyl glycinol.
21. The compound of formula (I) as claimed in claim 18, wherein the salts of natural amino acids are selected from the group consisting of glycine, alanine, valine, leucine, isoleucine, norleucine, tyrosine, cystine, cysteine, methionine, proline, hydroxy proline, histidine, ornithine, lysine, arginine, serine, threonine, or phenylalanine.
22. The compound of formula (I), as claimed in claim 18, wherein the salts of unnatural amino acid, substituted amino acids are selected from the group consisting of D-isomers, guanidine, and substituted guanidine wherein the substituents are selected from the group consisting of nitro, amino, alkyl, alkenyl or alkynyl.

23. A compound of formula (I) as claimed in claim 18, wherein the acid addition salt is selected from the group consisting of sulphates, nitrates, phosphates, perchlorates, borates, halides, acetates, tartrates, maleates, citrates, succinates, palmoates, methanesulphonates, benzoates, salicylates, hydroxynaphthoates, benzenesulfonates, ascorbates, glycerophosphates, or ketoglutarates.
24. A process for the preparation of compound of formula (I), as claimed in claim 1,

where R4 represents NHR4 wherein R4 represents hydrogen atom; R2 and R3 may be same or different and independently represent hydrogen, halogen atom, substituted or unsubstituted (C1-C10)alkyl group, halo(C1-C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, ORa
where R1 represents substituted or unsubstituted (C1-C10)alkyl group; Y1 and Y2 may be same or different and independently represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or unsubstituted groups selected from (C1-C10)alkyl

hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1-C10)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1-
C10)alkyl, (C1-C10)alkylsulfonyl, (C1-C10)alkylcarbonylamino(C1-C10)alkyl,
arylcarbonylamino(C1-C10)alkyl, (C1-C10) alkylcarbonyloxy(C1-C10)alkyl, ainino(C1 -C10)alkyl, niono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y1, Y2 may represent =O, =S, substituted or unsubstituted =NOR'" group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises: (i) reacting the compound of formula (la)

where Z represents O or S; all other symbols are as defined above,

(iii) converting the compound of formula (le) to a compound of formula (If)

where R1 represents isoindole-l,3-dione, Z represents O or S, all other symbols are as defined
above and
(vi) converting the above compound of formula (I), to a compound of formula (I) where R1
represents NHR4 wherein R4 represents hydrogen atom.
(vii) and if desire converting the compound obtained in to its derivatives, its anolagous, its
tutomaric form, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its
pharmaceutically solvates by conventionals methods.
25. A process for the preparation of compound of formula (I), as claimed in claim 1,

where all symbols are as defined in claim 24, which comprises

(i) reacing the compound of formula (li)
o

where X represents halogen atom, R represents isoindole-l,3-dione, R and R are as defined above, with [(R)3Sn]2, wherein R represents (C1-C6)alkyl group, to obtain a compound of formula (Ij)

where R1 represents isoindole-l,3-dione; ...' represents a bond and all other symbols are as
defined above and
(iii) converting the above compound of formula (I), to a compound of formula (I), where
R1 represents NHR4 wherein R4 represents hydrogen atom and
(iv) converting the above obtained compound of formula (I), to a compound of formula (I),
where '....' represents no bond, by conventional hydrogenation methods, by using a reagent
selected from Pt02, Pd/C, Raney nickel or other related reagent, along with H2 gas (v) and if desire converting the compound obtained in to its derivatives, its anolagous, its tutomaric form, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically solvates by conventionals methods.
26. A process for the preparation of compound of formula (I), as claimed in claim 1,

where R1 represents NHR4 wherein R4 represents hydrogen atom; R2 and R3 n
different and independently represent hydrogen, halogen atom, substituted o
(C1-C10)alkyl group, halo(C1-C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, ORa where R1 represents substituted or unsubstituted (C1-C10)alkyl group; Y* and Y^ may be same or
different and independently represent hydrogen, halogen, cyano, nitro, formyl, hydroxy,
amino, carboxyl or substituted or unsubstituted groups selected from (C1-C10)alkyl,
hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1-C10)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1-
Cio)aIkyl, (C1-C10)alkylsulfonyl, (C1-C10)alkylcarbonylamino(C1-C10)alkyl,
arylcarbonylamino(C1-C10)alkyl, (C1-C10) alkylcarbonyloxy(C1-C10)alkyl, amino(C1-Cio)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (CrGio)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y , Y may represent =0, =S, substituted or unsubstituted =NOR"' group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents SO or SO2; *-..' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises: (i) converting the compound of formula (I)

where R1 represents isoindole-l,3-dione, Z represents S, and all other symbols are as defined above, to a compound of formula (I), where R1 represents isoindole-l,3-dione, Z represents SO or SO2 and
(ii) converting the compound of formula (I), where R1 represents isoindole-l,3-dione, Z represents SO or SO2, to a compound of formula (I) where R1 represents NHR4 wherein R1 represents hydrogen atom and all other symbols are as defined above;

(iii) and if desire converting the compound obtained in to its derivatives, its anolagous, its tutomaric form, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically solvates by conventional methods. 27. A process for the preparation of compound of formula (I), as claimed in claim 1,

where R1 represents azido group; R2 and R3 may be same or different and independently
represent hydrogen, halogen atom, substituted or unsubstituted (C1-C10)alkyl group, halo(C1-
Cio)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, ORa where R1 represents substituted or
unsubstituted (C1-C10)alkyl group; Y and Y may be same or different and independently
represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or
unsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1-
Cio)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (C1-C10)alkylsulfonyl, (C1-
Cio)alkylcarbonylamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10)
alkylcarbonyloxy(C1-C10)alkyl, amino(C1-C10)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y1, Y2 may represent =0, =S, substituted or unsubstituted =NOR"' group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises: (i) converting the compound of formula (Ig)

where R1 represents hydroxy; Z, Y1, Y2, R2, R4 and m are as defined above and (ii) reacting the compound of formula (I) where R1 represents hydroxy group, with MsCl, triethylamine and sodium azide to give a compound of formula (I) where R1 represents azido group and all other symbols are as defined above;
(iii) and if desire converting the compound obtained in to its derivatives, its anolagous, its tutomaric form, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically solvates by conventionals methods. 28. A process for the preparation of compound of formula (I), as claimed in claim 1,

where R1 represents hydroxy group; R2 and R3 may be same or different and independently
represent hydrogen, halogen atom, substituted or unsubstituted (C1-C10)alkyl group, halo(C1-
C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, OR4 where R1 represents substituted o10
unsubstituted (C1-C10)alkyl group; Y1 and Y2 may be same or different and independently
represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or
unsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1-
Cio)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (C1-C10)alkylsulfonyl, (C1-
Cio)alkylcarbonylamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10)
alkylcarbonyloxy(C1-C10)alkyl, amino(C1-C10)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaraikyl, heterocyclyl or heterocycloalkyl; or any one or two of Y , Y may represent =0, =S, substituted or unsubstituted =NOR"' group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises: (i) converting the compound of formula (Ig),

where R1 represents substituted or unsubstituted (C1-C10)acyloxy group, and all other symbols
are as defined above and
(ii) hydrolysis of the compound of formula (I) where R1 represents (C1-C10)acyloxy
group, to a compoimd of formula (I), where R1 represents hydroxy group and all other
symbols are as defined above;
(iii) and if desire converting the compound obtained in to its derivatives, its anolagous,
its tutomaric form, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or
its pharmaceutically solvates by conventionals methods.
29. A process for the preparation of compound of formula (I), as claimed in claim 1,

where R1 represents NHR4, wherein R"* represents substituted or unsubstituted acetyl group; R2 and R3 may be same or different and independently represent hydrogen, halogen atom, substituted or unsubstituted (C1-C10)alkyl group, halo(C1-C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, OR^ where R1 represents substituted or unsubstituted (C1-C10)alkyl group; Y^ and Y may be same or different and independently represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or unsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1-C10)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (C1-C10)alkylsulfonyl, (C1-C10)alkylcarbonylamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10) alkylcarbonyloxy(C1-C10)alkyl, amino(C1-Cio)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y\ Y^ may represent =0, =S, substituted or unsubstituted =NOR'" group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its

regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises: converting the compound of formula (I), where R' represents azido group and all other symbols are as defined above.
30. A process for the preparation of compoimd of formula (I), as claimed in claim 1,

where R1 represents NHR4, wherein R4 represents substituted or unsubstituted -C(=S)-R4a, wherein R4a represents (C1-C10)alkyl, halo(C1-C10)alkyl, aryl, heteroaryl, -C(=O)-(C1-Cio)alkoxy, -C(=O)-(C1-C10)alkoxy, -C(=O)-aryloxy, -C(=S)-(C1-C10)alkyl or -C(=S)-aryl; R^ and R may be same or different and independently represent hydrogen, halogen atom, substituted or unsubstituted (C1-C10)alkyl group, halo(C1-C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, ORa where Rb represents substituted or unsubstituted (C1-C10)alkyl group; Y1 and Y may be same or different and independently represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or unsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1-C10)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (C1-C10)alkylsulfonyl, (C1-C10)alkylcarbonylamino(C1-C]o)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10) alkylcarbonyloxy(C1-C10)alkyl, amino(C1-Cio)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y^ Y^ may represent =0, =S, substituted or unsubstituted =NOR"' group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises: converting the compound of formula (I), where R1 represents NHR4, where R4 represents substituted or unsubstituted -C(=O)-R4a, wherein R4a represents (C1-C10)alkyl, halo(C1-C10)alkyl, aryl, heteroaryl, -C(=O)-(C1-C10)alkoxy, -C(=O)-aryloxy, -C(=S)-(C1-C10)alkyl or -C(=S)-aryl.
31. A process for the preparation of compound of formula (I), as claimed in claim 1,

where R' represents NHR4, wherein R4 represents substituted or unsubstituted -C(=S)-OR'4a',
wherein R4b represents (C1-C10)alkyl, cyclo(C3-Cio)alkyl, aryl, (C2-Cio)alkenyl or -C(=O)-
(C1-C10)alkyl group; R and R may be same or different and independently represent
hydrogen, halogen atom, substituted or unsubstituted (C1-C10)alkyl group, halo(C1-C10)alkyl,
aryl, heteroaryl, aralkyl, cyano, nitro, OR4 where R' represents substituted or imsubstituted
(C1-C10)alkyl group; Y1 and Y2 may be same or different and independently represent
hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or
unsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1-
Cio)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (C1-C10)alkylsulfonyl, (C1-
Cio)alkylcarbonylamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10)
alkylcarbonyloxy(C1-C10)alkyl, amino(C 1 -C 10)alkyl, mono(C 1-C 10)alkylamino, di(C 1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y1, Y2 may represent =0, =S, substituted or unsubstituted =NOR'" group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '-.' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises: (i) reacting compound of formula (I)

where R1 represents azido group; and all other symbols are as defined above, with
triphenylphosphine/water or H2-Pd/C, to produce a compound of formula (I), where R1
represents NHR4, wherein R4 represents hydrogen atom and all other symbols are as defined
above,
(ii) reacting compound of formula (I), where R1 represents NHR4, wherein R4 represents
hydrogen atom, with thiophosgene or carbon disulfide and chloromethylformate, in the

presence of a base to produce a compound of formula (I), where R1 represents isothiocyanate
group; and all symbols are as defined earlier,
(iii) converting compound of formula (I) where R1 represents isothiocynate group, to a
compound of formula (I), where R1 represents NHR4, wherein R4 represents substituted or
unsubstituted -C(=S)-OR4b, wherein R4b is as defined above and all other symbols are as
defined above,
(iv) and if desire converting the compound obtained in to its derivatives, its anolagous, its
tutomaric form, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its
pharmaceutically solvates by conventionals methods.
32. A process for the preparation of compound of formula (I), as claimed in claim 1,

where R1 represents NHR4, wherein R4 represents substituted or unsubstituted groups
selected from -C(=S)-NH2, -C(=S)-NH-(C1-C10)alkyl, -C(-S)-N-((C1-C10)alkyl)2, -C(=S)-
NH-(C2-C10)alkenyl, C(=S)-NH-C(=O)-aryl, -C(=S)-NH-aralkyl, -C(=S)-NH-heteroaralkyl
or -C(=S)-N(R'R"), wherein R' and R" groups together form a substituted or unsubstituted 5
or 6 membered cyclic structures containing nitrogen and optionally one or two additional
hetero atoms selected from oxygen, nitrogen or sulfur; R and R may be same or different
and independently represent hydrogen, halogen atom, substituted or unsubstituted (C1-
C10)alkyl group, halo(C1-C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, ORa where R1 represents substituted or unsubstituted (C1-C10)alkyl group; Y^ and Y^ may be same or
different and independently represent hydrogen, halogen, cyano, nitro, formyl, hydroxy,
amino, carboxyl or substituted or unsubstituted groups selected from (Ci 'C10)alkyl,
hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1-C10)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1-
C io)alkyl, (C1-C10)alkylsulfonyl, (C i -Ci o)alkylcarbonylamino(C1-C10)alkyl,
arylcarbonylamino(C1-C10)alkyl, (C1-C10) alkylcarbonyloxy(C1-C10)alkyl, amino(C1-C10)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Ya, Y2 may represent =O, =S, substituted or unsubstituted =NOR"' group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its

derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises: converting the compound of formula (I) where R1 represents isothiocyanate group.
33. A process for the preparation of compound of formula (I), as claimed in claim 1,

where R1 represents NHR4, wherein R4 represents substituted or unsubstituted -C(=S)-SR'4c,
wherein R ^ represents (C1-C10)alkyl group; R and R may be same or different and
independently represent hydrogen, halogen atom, substituted or unsubstituted (C]-C10)alkyl
group, halo(C1-C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, OR^ where R1 represents
substituted or unsubstituted (C1-C10)alkyl group; Y and Y may be same or different and
independently represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl
or substituted or xmsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl,
(C1-C10)alkoxy(C1-C10)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (C\-
C10)alkylsulfonyl, (C1-C10)alkylcarbonylamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10) alkylcarbonyloxy(C1-C10)alkyl, amino(C1-C10)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y , Y may represent =0, =S, substituted or unsubstituted =NOR"' group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents 0, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises: converting the compound of formula (I), where compound of formula (I), where R1 represents NHR4, wherein R1 represents hydrogen atom.
34. A process for the preparation of compound of formula (I), as claimed in claim 1,

V
where R' represents NHR4, wherein R4 represents substituted or unsubstituted -C(=S)-NH-
R4D, wherein R4d represents -C(=O)-aryl group; R2 and R3 may be same or different and
independently represent hydrogen, halogen atom, substituted or unsubstituted (C1-C10)alkyl
group, haIo(C1-C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, OR4 where R1 represents
substituted or unsubstituted (C1-C10)alkyl group; Y and Y may be same or different and
independently represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl
or substituted or unsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl,
(C1-C10)alkoxy(C1-C10)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (Cr
C10)alkylsulfonyl, (C1-C10)alkylcarbonylamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10) alkylcarbonyloxy(C1-C10)alkyl, amino(C1-C10)alkyl, mono(Ci" C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y , Y may represent =0, =S, substituted or unsubstituted =NOR"' group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises: converting the compound of formula (I), where R1 represents NHR4, wherein R"^ represents hydrogen atom, 35. A process for the preparation of compound of formula (I), as claimed in claim 1,

where R1 represents NHR4, wherein R4 represents substituted or unsubstituted -C(=O)-
heteroaryl; R and R may be same or different and independently represent hydrogen,
halogen atom, substituted or unsubstituted (C1-C10)alkyl group, halo(C1-C10)alkyl, aryl,
heteroaryl, aralkyl, cyano, nitro, OR4 where R1 represents substituted or unsubstituted (C1-
C10)alkyl group; Y and Y may be same or different and independently represent hydrogen,
halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or unsubstituted
groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1-C10)alkyl, (C1-
C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (C1-C10)alkylsulfonyl, (d-
C]o)alkylcarbonylamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10)

alkylcarbonyloxy(C1-C10)alkyl, amino(C1-C10)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y , Y may represent =0, ==S, substituted or unsubstituted =NOR'" group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises: converting the compound of formula (I), where R1 represents NHR4, wherein R4 represents hydrogen atom. 36. A process for the preparation of compound of formula (I), as claimed in claim 1,

where R1 represents NHR4, wherein R4 represents substituted or unsubstituted -C(=O)-R4a
wherein R4d represents (C1-C10)alkyl, (C1-C10)alkoxy, (C2-C10)alkenyl, halo(C1-C10)alkyl,
aryl, aryloxy, heteroaryl, (C2-C10)alkenyloxy, (C1-C10) alkylcarbonyl, arylcarbonyl,
aryloxycarbonyl, (C1-C10)alkoxycarbonyl, (C1-C10) alkylthiocarbonyl or (C1-
C10)arylthiocarbonyl; R and R may be same or different and independently represent
hydrogen, halogen atom, substituted or unsubstituted (C1-C10)alkyl group, halo(C1-C10)alkyl,
aryl, heteroaryl, aralkyl, cyano, nitro, ORa where R1 represents substituted or unsubstituted
(C1-C10)alkyl group; Y and Y may be same or different and independently represent
hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or
unsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1-
C10)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (C1-C10)alkylsulfonyl, (C1-
C10)alkylcarbonylamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10)
alkylcarbonyloxy(C1-C10)alkyl, amino(C1-C10)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y\ Y^ may represent =0, =S, substituted or unsubstituted =NOR'" group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically

acceptable salts or its pharmaceutically acceptable solvates; which comprises: converting the compound of formula (I), where R1 represents NHR4, wherein R4 represents hydrogen atom. 37. A process for the preparation of compound of formula (I), as claimed in claim 1,

where R1 represents NHR4, wherein R4 represents substituted or unsubstituted -C(=NH)-NH2; R2 and R3 may be same or different and independently represent hydrogen, halogen atom, substituted or unsubstituted (C1-C10)alkyl group, halo(C1-C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, ORa where R1 represents substituted or unsubstituted (C1-C10)alkyl group; Ya and Y may be same or different and independently represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or unsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1-C10)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (C1-C10)alkylsulfonyl, (C1-C10)alkylcarbonylamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10) alkylcarbonyloxy(C1-C10)alkyl, amino(C1-C10)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y , Y may represent =O, =S, substituted or unsubstituted =NOR"' group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises:
(a) converting the compound of formula (I), where R1 represents NHR4, wherein R"* represents hydrogen atom.
(b) and if desire converting the compound obtained in to its derivatives, its anolagous, its tutomaric form, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically solvates by conventionals methods. 38. A process for the preparation of compound of formula (I), as claimed in claim 1,

where all symbols are as defined in claim 37, which comprises :
(a) converting the compound of formula (I), where R1 represents NHR'*, wherein R represents substituted or unsubstituted group selected fi"om -S(0)2(C1-C10)alkyl or -S(0)2aryl group.
(b) and if desire converting the compound obtained in to its derivatives, its anolagous, its tutomaric form, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically solvates by conventional methods.
39. A process for the preparation of compoimd of formula (I), as claimed in claim 1,

where R1 represents NHR4, wherein R4 represents substituted or unsubstituted group selected
from -C(=NH)-(C1-C10)alkyl or -C(=NH)-aryl; R2 and R3 may be same or different and
independently represent hydrogen, halogen atom, substituted or imsubstituted (C1-C10)alkyl
group, halo(C1-C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, ORa where R1 represents
substituted or imsubstituted (C1-C10)alkyl group; Y1 and Y2 may be same or different and
independently represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl
or substituted or unsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl,
(C1-C10)alkoxy(C1-C10)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (C1-
C10)alkylsulfonyl, (C1-C10)alkylcarbonyIamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10) alkylcarbonyloxy(C1-C10)alkyl, amino(C1-C10)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y1, Y2 may represent =0, =S, substituted or unsubstituted =NOR"' group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers,

its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which
comprises:
(i) reacting the compound of formula (I)

where R1 repersents NHR'^, wherein R"* represents -C(=S)-NH2 and all other symbols are as defined above, with di tert-butoxy carbonyl ether ((B0C)20), to produce a compound of formula (I)
where R1 represents NHR4, wherein R4 represents -C(=S)-NH2 group substituted with tert-
butoxy carbonyl group and all symbols are as defined above and
(ii) reacting the above compound of formula (I), with a compound of formula (Ik)
R7-NH2 (Ik)
where R1 represents substituted or unsubstituted (C1-C10)alkyl or aryl group, to produce a compound of formula (I) where R1 represents NHR4 where R4 represents substituted or unsubstituted group selected fi-om -C(=NH)-(C1-C10)alkyl or -C(=NH)-aryl group and all other symbols are as defined above
(iii) and if desire converting the compound obtained in to its derivatives, its anolagous, its tutomaric form, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically solvates by conventionals methods. 40. A process for the preparation of compound of formula (I), as claimed in claim 1,

where R represents halogen atom; R and R may be same or different and independently represent hydrogen, halogen atom, substituted or unsubstituted (C1-C10)alkyl group, halo(Cr C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, ORa where R1 represents substituted or unsubstituted (C1-C10)alkyl group; Y and Y may be same or different and independently

represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or
unsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1-
C10)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (C1-C10)alkylsulfonyl, (C1-
C10)alkylcarbonylamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (CpC10)
alkylcarbonyloxy(C1-C10)alkyl, amino(C1-C10)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y , Y may represent =O, =S, substituted or unsubstituted =NOR'" group, where R'" represents hydrogen, (C1-C10)alkyl, (C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises: (a) converting the compound of formula (I), where R1 represents hydroxy group (b) and if desire converting the compound obtained in to its derivatives, its anolagous, its tutomaric form, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically solvates by conventional methods. 41. A process for the preparation of compound of formula (I), as claimed in claim 1,
• *
where R represents thioalcohol; R and R may be same or different and independently
represent hydrogen, halogen atom, substituted or unsubstituted (C1-C10)alkyl group, halo(Cr
C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, ORa where R1 represents substituted or
unsubstituted (C1-C10)alkyl group; Y and Y may be same or different and independently
represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or
unsubstituted groups selected from (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1-
C10)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (C1-C10)alkylsulfonyl, (C1-
C10)alkylcarbonylamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10)
alkylcarbonyloxy(C1-C10)alkyl, amino(C1-C10)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of YA, Y2 may represent =O, =S, substituted or unsubstituted =NOR'" group, where R'" represents hydrogen, (C1-C10)alkyl,

(C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '...' represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates; which comprises; (i) reacting the compound of formula (I) where R1 represents halogen atom, to produce a compound of formula (Im),

where all other symbols are as defined above, with a base and thiolacetic acid and
(ii) reacting the compound of formula (Im), to produce a compound of formula (I) where
R1 represents 'SH' group and all other symbols are as defined above,
(iii) and if desire converting the compound obtained in to its derivatives, its anolagous, its
tutomaric form, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its
pharmaceutically solvates by conventional methods.
42. A process for the preparation of compound of formula (I), as claimed in claim 1,

where R1 represents NHR4 wherein R4 represents substituted or unsubstituted -S(O)2(C1-
C10)alkyl or -S(0)2aryl group; R and R may be same or different and independently
represent hydrogen, halogen atom, substituted or unsubstituted (C1-C10)alkyl group, halo(C1-
C10)alkyl, aryl, heteroaryl, aralkyl, cyano, nitro, ORa where R1 represents substituted or
unsubstituted (C1-C10)alkyl group; Y1 and Y2 may be same or different and independently
represent hydrogen, halogen, cyano, nitro, formyl, hydroxy, amino, carboxyl or substituted or
unsubstituted groups selected fi"om (C1-C10)alkyl, hydroxy(C1-C10)alkyl, (C1-C10)alkoxy(C1-
C10)alkyl, (C1-C10)alkoxycarbonyl, carboxy(C1-C10)alkyl, (C1-C10)alkylsulfonyl, (C1-
C10)alkylcarbonylamino(C1-C10)alkyl, arylcarbonylamino(C1-C10)alkyl, (C1-C10)
alkylcarbonyloxy(C1-C10)alkyl, amino(C1-C10)alkyl, mono(C1-C10)alkylamino, di(C1-C10) alkylamino, arylamino, (C1-C10)alkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl or heterocycloalkyl; or any one or two of Y1, Y2 may represent =O, =S,

substituted or unsubstituted =NOR'" group, where R'" represents hydrogen, (C1-C10)alkyl,
(C1-C10)alkoxy, aryl, heteroaryl or aralkyl group; Z represents O, S, SO or SO2; '...'
represents a bond or no bond; 'm' represents 0-3; its derivatives, its analogs, its tautomeric
forms, its stereoisomers, its polymorphs, it rotamers, its regioisomers, its pharmaceutically
acceptable salts or its pharmaceutically acceptable solvates; which comprises:
(i) converting the compound of formula (I), where R1 represents NHR4 where R
represents hydrogen atom
(ii) and if desire converting the compound obtained in to its derivatives, its anolagous, its
tutomaric form, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its
pharmaceutically solvates by conventionals methods.
43. A pharmaceutical composition comprising a compound of formula (I)
as claimed in claim 1 and a pharmaceutically acceptable carrier, diluent, excipient or solvate.
44. The pharmaceutical composition as claimed in claim 43, in the form of a tablex, capsule, powder, syrup, solution or suspension.
45. A composition comprising a compound as claimed in claim 17 and a pharmaceutically acceptable carrier, diluent, excipient or solvate.
46 The pharmaceutical composition as claimed in claim 45, in the form of a tablet, capsule, powder, syrup, solution or suspension.

Documents:

0448-che-2003 claims-duplicate.pdf

0448-che-2003 description (complete)-duplicate.pdf

448-che-2003-abstract.pdf

448-che-2003-claims.pdf

448-che-2003-correspondnece-others.pdf

448-che-2003-correspondnece-po.pdf

448-che-2003-description(complete).pdf

448-che-2003-form 1.pdf

448-che-2003-form 18.pdf

448-che-2003-form 3.pdf

448-che-2003-pct.pdf

abs-448-che-2003.jpg

hh1.jpg

« Previous Patent

Next Patent »

Patent Number

221690

Indian Patent Application Number

448/CHE/2003

PG Journal Number

37/2008

Publication Date

12-Sep-2008

Grant Date

01-Jul-2008

Date of Filing

03-Jun-2003

Name of Patentee

DR. REDDY'S LABORATORIES LTD.

Applicant Address

7-1-27, AMEERPET, HYDERABAD 500 016,

Inventors:

#	Inventor's Name	Inventor's Address
1	MOHAMED TAKHI	7-1-27, AMEERPET, HYDERABAD 500 016,
2	JAGATTARAN DAS	7-1-27, AMEERPET, HYDERABAD 500 016,
3	NATESAN SELVAKUMAR	7-1-27, AMEERPET, HYDERABAD 500 016,
4	SANJAY TREHAN	7-1-27, AMEERPET, HYDERABAD 500 016,
5	JAVED IQBAL	7-1-27, AMEERPET, HYDERABAD 500 016,
6	MAGADI SITARAM KUMAR	7-1-27, AMEERPET, HYDERABAD 500 016,

PCT International Classification Number

A61K 031/41

PCT International Application Number

N/A

PCT International Filing date

PCT Conventions:

#	PCT Application Number	Date of Convention	Priority Country
1			NA