Patent ID: 6833375
Filing Date: 2004-12-21
Classification: A61P,C07D

Abstract:
A compound of formula a N-oxide, a pharmaceutically acceptable addition salt or a stereochemically isomeric form thereof, wherein:R1 represents hydrogen, hydroxy, C1-6alkyl aryl; R2 represents hydrogen; C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl; aryl; pyrrolidinyl optionally substituted with C1-4alkyl or C1-4alkyloxycarbonyl; or C1-12alkyl substituted with one or two substituents selected from C3-7cycloalkyl, hydroxy, C1-4alkyloxy, cyano, amino, mono- and di(C1-4alkyl)amino, mono- and di(aryl)amino, arylC1-4alkylamino, (C1-4alkyl)(arylC1-4alkyl)amino, pyrrolidinyl, piperidinyl, perhydro-azepinyl, carboxyl, C1-4alkyloxycarbonyl, aminocarbonyl, mono- and di(C1-4alkyl)aminocarbonyl, aryl, aryloxy and arylthio; R3 represents hydrogen, C1-6alkyl, aryl or C1-6alkyl substituted with aryl; Het represents an unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; each of said unsaturated heterocycles may optionally be substituted with amino, mercapto, C1-6alkyl, C1-6alkylthio or aryl; represents an unsaturated mono- or bicyclic heterocycle selected from the group consisting of pyridinyl, quiuolinyl, and isoquinolinyl; each of said unsaturated mono- or bicyclic heterocycles may optionally be substituted with one, two or three substituents selected from hydroxy, halo, nitro, amino, C1-6alkyl, hydroxyC1-6alkyl, haloC1-6alkyl, C1-6alkyloxy, C1-6alkylthio, formyl, carboxyl, mono- or di(C1-6alkyl)amino, C1-6alkyloxycarbonyl or aryl; or represents a radical of formula wherein each X independently represents NR8, O, S, S(&boxH;O) or S(&boxH;O)2; wherein R8 is hydrogen, C1-6alkyl, aryl or arylC1-6alkyl; R4 and R5 each independently represents hydrogen, hydroxy, halo, cyano, nitro, amino, C1-6-alkyl, hydroxyC1-6alkyl, haloC1-6alkyl, C1-6alkyloxy, formyl, carboxyl, mono- or di(C1-6alkyl)amino, C1-6alkyloxycarbonyl or aryl; â€”R6â€”R7â€” represents a bivalent radical of formula: â€”CR9&boxH;CR9â€”CR9&boxH;CR9â€”â€ƒâ€ƒ(b-1); â€”N&boxH;CR9â€”CR9&boxH;CR9â€”â€ƒâ€ƒ(b-2); â€”CR9&boxH;Nâ€”CR9&boxH;CR9â€”â€ƒâ€ƒ(b-3); â€”CR9&boxH;CR9â€”N&boxH;CR9â€”â€ƒâ€ƒ(b-4); orâ€”CR9&boxH;CR9â€”CR9&boxH;Nâ€”â€ƒâ€ƒ(b-5); wherein each R9 independently represents hydrogen, hydroxy, halo, nitro, amino, C1-6alkyl, hydroxyC1-6alkyl, haloC1-6alkyl, C1-6alkyloxy, formyl, carboxyl, mono- or di(C1-6alkyl)amino, C1-6alkyloxycarbonyl or aryl; and aryl represents phenyl or phenyl substituted with one, two or three substituents selected from hydroxy, halo, cyano, amino, mono- or di(C1-6alkyl)amino, C1-6alkyl, haloC1-6alkyl, hydroxyC1-6alkyl, C1-6alkyloxy, formyl, carboxyl and C1-6alkylcarbonyl; or two adjacent carbon atoms on said phenyl maybe substituted by a single bivalent radical having the formula C1-12alkanediyl or haloC1-12alkanediyl, with the proviso that at least one of and Het comprises a one nitrogen containing 6-membered ring.