Patent ID: 6288073
Filing Date: 2001-09-11
Classification: A61P,C07D

Abstract:
A compound selected from those of formula (I): ##STR46##in whichX and Y, which may be identical or different, each independently of the other represents a group selected from hydrogen, halogen, hydroxy, mercapto, cyano, nitro, linear or branched (C.sub.1 -C.sub.6)alkyl, linear or branched (C.sub.1 -C.sub.6)alkoxy, linear or branched (C.sub.1 -C.sub.6)trihaloalkyl, and amino which is optionally substituted by one or two, identical or different, linear or branched (C.sub.1 -C.sub.6)alkyl which are themselves optionally substituted by linear or branched (C.sub.1 -C.sub.6)alkoxy or by --NR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8, which may be identical or different, each independently of the other represents hydrogen or linear or branched (C.sub.1 -C.sub.6)alkyl, or X and Y together form methylenedioxy or ethylenedioxy,R.sub.1 represents hydrogen or linear or branched (C.sub.1 -C.sub.6)alkyl,R.sub.2 represents a group selected from:hydrogen,hydroxy,linear or branched (C.sub.1 -C.sub.6)alkyl,linear or branched (C.sub.1 -C.sub.6)alkoxy which is optionally substituted:by NR'.sub.7 R'.sub.8 wherein R'.sub.7 and R'.sub.8, which may be identical or different, each independently of the other represent a group selected from hydrogen, linear or branched (C.sub.1 -C.sub.6)alkyl, and linear or branched (C.sub.1 -C.sub.6)hydroxyalkyl,or by a saturated or unsaturated, monocyclic or bicyclic heterocycle having 5 to 7 ring members, and containing one or two hetero atoms selected from oxygen, nitrogen, and sulphur,linear or branched (C.sub.1 -C.sub.6)alkylcarbonyloxy,and amino which is optionally substituted:by one or two, identical or different, linear or branched (C.sub.1 -C.sub.6)alkyl,by linear or branched (C.sub.1 -C.sub.6)alkylcarbonyl which is optionally substituted by --NR'.sub.7 R'.sub.8 wherein R'.sub.7 and R'.sub.8 are as defined above,by --R.sub.9 --NR'.sub.7 R'.sub.8 wherein R.sub.9 represents linear or branched (C.sub.1 -C.sub.6)alkylene and R'.sub.7 and R'.sub.8, which may be identical or different, each independently of the other represents a group selected from hydrogen, linear or branched (C.sub.1 -C.sub.6)alkyl, and linear or branched (C.sub.1 -C.sub.6)hydroxyalkyl,by linear or branched (C.sub.1 -C.sub.6)alkylene which is substituted by a saturated or unsaturated, monocyclic or bicyclic heterocycle having 5 to 7 ring members and containing one or two hetero atoms selected from oxygen, nitrogen, and sulphur,or by ##STR47##wherein R.sub.9 is as defined above, and R.sub.10 represents hydroxy or linear or branched (C.sub.1 -C.sub.6)alkoxy,R.sub.3 and R.sub.4, which may be identical or different, each independently of the other represents hydrogen or linear or branched (C.sub.1 -C.sub.6)alkyl,A represents --CH.dbd.CH--, or ethylene with the formula --CH(R.sub.5)--CH(R.sub.6) wherein R.sub.5 and R.sub.6, which may be identical or different, each independently of the other represents:hydrogen,hydroxy,linear or branched (C.sub.1 -C.sub.6)alkoxy,linear or branched (C.sub.1 -C.sub.6)alkylcarbonyloxy,arylcarbonyloxy,amino optionally substituted by one or two, identical or different, linear or branched (C.sub.1 -C.sub.6)alkyl, or linear or branched (C.sub.1 -C.sub.6)acyl,mercapto, linear or branched (C.sub.1 -C.sub.6)alkylthio, or arylthio,or R.sub.5 and R.sub.6 together form: ##STR48##wherein Z represents oxygen or sulphur,--O--(CH.sub.2).sub.n --O-- wherein n is 1 to 4 inclusibve, ##STR49##(C.sub.1 -C.sub.6)alkylene or linear (C.sub.2 -C.sub.6)alkylene,or R.sub.5 and R.sub.6 form, together with the carbons carrying them, oxirane or azirideine, optionally substituted on nitrogen by linear or branched (C.sub.1 -C.sub.6)alkyl,wherein the term ""aryl"" denotes phenyl or naphthyl, optionally containing one or more, identical or different, substituents selected from hydroxy, halogen, carboxy, nitro, amino, linear or branched (C.sub.1 -C.sub.6)alkylamino, linear or branched di-(C.sub.1 -C.sub.6)alkylamino, linear or branched (C.sub.1 -C.sub.6)alkoxy, linear or branched (C.sub.1 -C.sub.6)acyl, and linear or branched (C.sub.1 -C.sub.6)alkylcarbonyloxy,its optical isomers, diastereomers, N-oxides, and pharmaceutically-acceptable acid or base addition salts thereof.