| abstract |
The present invention is concerned with the compounds of formula (I) the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomerics forms thereof, p and q are 0, 1, 2, 3 or 4 and q is also 5; X is O, S, NR3 or a direct bond; R1 is hydrogen, hydroxy, halo, optionally substituted amino, optionally substituted C¿1-6?alkyl, C1-6alkyloxy, C3-7cycloalkyl or aryl; R?2¿ is aryl, Het1, C3-7cycloalkyl, optionally substituted C1-6alkyl; and if X is O, S or NR3, then R2 may also be a carbonyl or thiocarbonyl linked substituent; R3 is hydrogen or C¿1-4?alkyl; R?4 and R5¿ independently are optionally substituted C¿1-6?alkyl, halo, hydroxy, mercapto, C1-6alkyloxy, C1-6alkylthio, C1-6 alkylcarbonyloxy, aryl, cyano, nitro, Het?3, R6 or NR7R8; R6¿ is substituted sulfonyl or sulfinyl; R?7 and R8¿ are hydrogen, optionally substituted C¿1-4?alkyl, aryl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl, Het?3 and R6; R9 and R10¿ are each independently selected from hydrogen, optionally substituted C¿1-4?alkyl, phenyl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl, Het?3 and R6; R11¿ is hydroxy, mercapto, cyano, nitro, halo, trihalomethyl, C¿1-4?alkyloxy, carboxyl, C1-4alkyloxycarbonyl, trihaloC1-4alkylsulfonyloxy, R?6, NR7R8¿, C(=O)NR7R8, aryl, aryloxy, arylcarbonyl, C¿3-7?cycloalkyl, C3-7cycloalkyloxy, phthalimide-2-yl, Het?3¿ and C(=O)Het?3; R12 and R13¿ are each independently selected from hydrogen, optionally substituted C¿1-4?alkyl, phenyl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl and R?6¿; aryl is optionally substituted phenyl; Het1, Het2 and Het3 are optionally substituted heterocycles; to processes for their preparation and compositions comprising them. It further relates to their use as a medicine. |