| abstract |
The present invention is concerned with the compounds of formulan nthe N -oxides, the pharmaceutically acceptable addition salts and the stereochemicallynisomeric forms thereof, wherein p is 0 to 4; X is O, S, NR 5 or a direct bond; Y is O, S,nNR 5 or S(O) 2 ; R 1 independently is C 1-6 alkyl, halo, polyhaloC 1-6 alkyl, hydroxy, mercapto,nC 1-6 alkyloxy, C 1-6 alkylthio, C 1-6 alkylcarbonyloxy, aryl, cyano, nitro, Het 3 , R 6 , NR 7 R 8 ornsubstituted C 1-4 alkyl; R 2 is Het 1 , C 3-7 cycloalkyl or optionally substituted C 1-6 alkyl and ifnX is O, S or NR 5 , then R 2 may also represent aminocarbonyl, aminothiocarbonyl,nC 1-4 alkylcarbonyl, C 1-4 alkylthiocarbonyl, arylcarbonyl, arylthiocarbonyl, Het 1 carbonyl ornHet 1 thiocarbonyl; R 3 and R 4 independently are hydrogen, C 1-6 alkyl or C 3-7 cycloalkyl; R 3 nand R 4 form a C 2-6 alkanediyl; R 5 is hydrogen or C 1-4 alkyl; R 6 a sulfonyl or sulfinylnderivative; R 7 and R 8 are independently hydrogen, optionally substituted C 1-4 alkyl, aryl, ancarbonyl containing moiety, C 3-7 cycloalkyl, -Y-C 1-4 alkanediyl-C(=O)-O-R 14 , Het 3 and R 6 ;nR 11 is hydroxy, mercapto, cyano, nitro, halo, trihalomethyl, C 1-4 alkyloxy, formyl,ntrihaloC 1-4 alkylsulfonyloxy, R 6 , NR 7 R 8 , C(=O)NR 7 R 8 , C 1-4 alkanediyl-C(=O)-O-R 14 , -nC(=O)-O-R 14 , -Y-C 1-4 alkanediyl-C(=O)-O-R 14 , aryl, aryloxy, arylcarbonyl, C 3-7 cycloalkyl,nC 3-7 cycloalkyloxy, phthalimide-2-yl, Het 3 , Het 4 and C(=O)Het 3 ; R 14 is hydrogen, C 1-4 alkyl,nC 3-7 cycloalkyl, aminocarbonylmethylene or mono-or di(C 1-4 alkyl)aminocarbonylmethylene;naryl is optionally substituted phenyl; Het 1 , Het 2 , Het 3 and Het 4 are optionally substitutednheterocycles; to processes for their preparation and compositions comprising them. Itnfurther relates to their use as a medicine. |