Patent ID: 6124330
Filing Date: 2000-09-26
Classification: A61P,C07D

Abstract:
A compound of formula ##STR127## a N-oxide, a pharmaceutically acceptable addition salt or a stereochemically isomeric form thereof, wherein:R.sup.1 represents hydrogen, hydroxy, C.sub.1-6 alkyl or aryl;R.sup.2 represents hydrogen; C.sub.1-12 alkyl; C.sub.3-7 cycloalkyl; C.sub.2-8 alkenyl; aryl; pyrrolidinyl optionally substituted with C.sub.1-4 alkyl or C.sub.1-4 alkyloxycarbonyl; or C.sub.1-12 alkyl substituted with one or two substituents selected from C.sub.3-7 cycloalkyl, hydroxy, C.sub.1-4 alkyloxy, cyano, amino, mono- and di(C.sub.1-4 alkyl)amino, mono- and di(aryl)amino, arylC.sub.1-4 alkylamino, (C.sub.1-4 alkyl) (arylC.sub.1-4 alkyl)amino, pyrrolidinyl, piperidinyl, piperazinyl optionally substituted with C.sub.1-4 alkyl, morpholinyl, perhydro-azepinyl, carboxyl, C.sub.1-4 alkyloxycarbonyl, aminocarbonyl, mono- and di(C.sub.1-4 alkyl)aminocarbonyl, aryl, aryloxy and arylthio;R.sup.3 represents hydrogen, C.sub.1-6 alkyl, aryl or C.sub.1-6 alkyl substituted with aryl;Het represents an unsaturated heterocycle selected from imidazolyl, triazolyl, and tetrazolyl; each of said unsaturated heterocycles may optionally be substituted with amino, mercapto, C.sub.1-6 alkyl, C.sub.1-6 alkylthio or aryl; ##STR128## represents a radical of formula ##STR129## wherein each X independently represents S, S(.dbd.O) or S(.dbd.O).sub.2 ; R.sup.4 and R.sup.5 each independently represent hydrogen, hydroxy, halo, cyano, nitro, amino, C.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, haloC.sub.1-6 alkyl, C.sub.1-6 alkyloxy, formyl, carboxyl, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkyloxycarbonyl or aryl;--R.sup.6 --R.sup.7 -- represents a bivalent radical of formula:--CR.sup.9 .dbd.CR.sup.9 --CR.sup.9 .dbd.CR.sup.9 -- (b-1);wherein each R.sup.9 independently represents hydrogen, hydroxy, halo, nitro, amino, C.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, haloC.sub.1-6 alkyl, C.sub.1-6 alkyloxy, formyl, carboxyl, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkyloxycarbonyl or aryl; andaryl represents phenyl or phenyl substituted with one, two or three substituents selected from hydroxy, halo, cyano, amino, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkyl, haloC.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, C.sub.1-6 alkyloxy, formyl, carboxyl and C.sub.1-6 alkylcarbonyl; or two adjacent carbon atoms on said phenyl may be substituted by a single bivalent radical having the formula C.sub.1-12 alkanediyl or haloC.sub.1-12 alkanediyl.