| 摘要 |
The present invention is concerned with the compounds of formula (I), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein p is 0 to 4; q is 0 to 5; X is O, S, NR<3 >or a direct bond; or -X-R<2 >is CN; R<1 >is H, OH, halo, NH2, mono- or di(C1-4alkyl)NH2, C1-6alkyl, C1-6alkylO, C3-7cycloalkyl, aryl, arylC1-6alkyl, NH2C1-4akyl, mono- or di(C1-4alkyl)NH2C1-4akyl or mono- or di(C1-4alkyl)NH2C1-4alkylNH2; R<2 >is aryl, Het<1>, optionally substituted C3-7cycloalkyl, optionally substituted C1-6alkyl; R<3 >is H or C1-4alkyl; R<4 >and R<5 >are -C(=O)-Z-R<14>, C1-6alkyl, halo, polyhaloC1-6alkyl, OH, mercapto, C1-6alkylO, C1-6alkylthio, C1-6alkylC(=O)O, aryl, cyano, nitro, Het<3>, R<6>, NR<7>R<8 >or C1-4alkyl substituted with -C(=O)-Z-R<14>, Het<3>, R<6 >or NR<7>R<8>; Z is O, S, NH, -CH2O or -CH2-S-; R<14 >is H, C1-20acyl, optionally substituted C1-20alkyl, optionally substituted C3-20alkenyl, C3-20alkynyl, C3-7cycloalkyl, polyhaloC1-20alkyl, Het<5>, phenyl; or R<14 >is an oxygen containing radical; aryl is optionally substituted phenyl; Het<1>, Het<2>, Het<3 >and Het<5 >are optionally substituted heterocycles; Het<4 >is a monocyclic heterocycle; provided however that R<2 >is other than NH<PD |
