Patent ID: 6265401
Filing Date: 2001-07-24
Classification: A61K,A61P,C07D

Abstract:
A compound of formula (I) ##STR85##its tautomeric forms, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts, or its pharmaceutically acceptable solvates, wherein the groups R.sup.1, R.sup.2, R.sup.3, R.sup.4, and the groups R.sup.5 and R.sup.6 when attached to a carbon atom, may be same or different and represent hydrogen, halogen, hydroxy, nitro, cyano, formyl or optionally substituted groups selected from alkyl, cycloalkyl, alkoxy, cycloalkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl selected from aziridinyl, pyrrolidinyl, morpholinyl, piperidinyl or piperazinyl; heteroaryl group selected from pyridyl, thienyl, furyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, oxadiazolyl, tetrazolyl, benzopyranyl, or benzofuranyl; heteroaralkyl group selected from furanmethyl, pyridinemethyl, oxazolemethyl, or oxazolethyl; heteroaryloxy wherein the heteroaryl moiety is as defined above; heteroaralkoxy; wherein the heteroaralkyl moiety is as defined above; acyl selected from acetyl, propionyl or benzoyl; acyloxy, hydroxyalkyl, amino, acylamino, alkylamino, arylamino, aralkylamino, aminoalkyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, alkoxyalkyl, aryloxyalkyl, aralkoxyalkyl, alkylthio, thioalkyl, alkoxycarbonylamino, aryloxycarbonylamino, aralkoxycarbonylamino, carboxylic acid or its esters or amides, or sulfonic acid or its esters or amides; one or both of R.sup.5 and R.sup.6 may represent an oxo group when attached to a carbon atom; R.sup.5 and R.sup.6 when attached to a nitrogen atom may be the same or different and represent hydrogen, hydroxy, formyl or optionally substituted groups selected from alkyl, cycloalkyl, alkoxy, cycloalkoxy, aryl, aralkyl, heterocyclyl selected from aziridinyl, pyrrolidinyl, morpholinyl, piperidinyl or piperazinyl; heteroaryl group selected from pyridyl, thienyl, furyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, oxadiazolyl, tetrazolyl, benzopyranyl, or benzofuranyl; heteroaralkyl group selected from furanmethyl, pyridinemethyl, oxazolemethyl, or oxazolethyl; acyl selected from acetyl, propionyl or benzoyl; acyloxy, hydroxyalkyl, amino, acylamino, alkylamino, arylamino, aralkylamino, aminoalkyl, aryloxy, aralkoxy, heteroaryloxy wherein the heteroaryl moiety is as defined above; heteroaralkoxy, wherein the heteroaralkyl moiety is as defined above; alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, alkoxyalkyl, aryloxyalkyl, aralkoxyalkyl, alkylthio, thioalkyl groups, esters or amides of carboxylic acid or esters or amides of sulfonic acid; X represents oxygen or sulfur; Ar represents an optionally substituted divalent single aromatic or fused aromatic or heterocyclic group; R.sup.7 represents hydrogen atom, hydroxy, alkoxy, halogen, lower alkyl, optionally substituted aralkyl group or forms a bond together with R.sup.8 ; R.sup.8 represents hydrogen, hydroxy, alkoxy, halogen, lower alkyl group, acyl, or optionally substituted aralkyl or R.sup.8 forms a bond together with R.sup.7 ; R.sup.9 represents hydrogen, or optionally substituted groups selected from alkyl, cycloalkyl, aryl, aralkyl, alkoxyalkyl, alkoxycarbonyl, aryloxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl, acyl selected from acetyl, propionyl or benzoyl; heterocyclyl selected from aziridinyl, pyrrolidinyl, morpholinyl, piperidinyl or piperazinyl; heteroaryl group selected from pyridyl, thienyl, furyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, oxadiazolyl, tetrazolyl, benzopyranyl, or benzofuranyl; or heteroaralkyl group selected from furanmethyl, pyridinemethyl, oxazolemethyl, or oxazolethyl; R.sup.10 represents hydrogen or optionally substituted groups selected from alkyl, cycloalkyl, aryl, aralkyl, heterocyclyl selected from aziridinyl, pyrrolidinyl, morpholinyl, piperidinyl or piperazinyl; heteroaryl group selected from pyridyl, thienyl, furyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, oxadiazolyl, tetrazolyl, benzopyranyl, or benzofuranyl; or heteroaralkyl group selected from furanmethyl, pyridinemethyl, oxazolemethyl or oxazolethyl; Y represents oxygen or NR.sup.12, where R.sup.12 represents hydrogen, alkyl, aryl, hydroxyalkyl, aralkyl, heterocyclyl selected from aziridinyl, pyrrolidinyl, morpholinyl, piperidinyl or piperazinyl; heteroaryl group selected from pyridyl, thienyl, furyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, oxadiazolyl, tetrazolyl, benzopyranyl, or benzofuranyl; or heteroaralkyl group selected from furanmethyl, pyridinemethyl, oxazolemethyl or oxazolethyl; R.sup.10 and R.sup.12 together may form a 5 or 6 membered cyclic structure containing carbon atoms, which may optionally contain one or more heteroatoms selected from oxygen, sulfur or nitrogen; the linking group represented by --(CH.sub.2).sub.n --(O).sub.m -- may be attached either through a nitrogen atom or a carbon atom; n is an integer ranging from 1-4 and m is an integer 0 or 1, with the proviso that when the linking group is attached through a carbon atom and either of R.sup.5 or R.sup.6 represents an oxo group and Y is an oxygen atom, R.sup.9 does not represent a hydrogen atom.