| 摘要 |
The present invention relates to a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein R1 represents hydrogen, C1-6alkyl, C3-7cycloalkyl, C1-6alkyloxyC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, aryl or heteroaryl; each R2 independently represents halo, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, polyhaloC1-6alkyl, polyhaloC1-6alkyloxy, cyano, aminocarbonyl, amino, mono- or di(C1-4alkyl)amino, nitro, aryl or aryloxy; R3 represents hydrogen, cyano, C1-6alkyl optionally substituted with hydroxy or C1-6alkyloxy, C(-O)-O-R6, C(-O)-NR7aR7b, C(-S)-NR7aR7b, S(-O)2-NR7aR7b or C(-O)-R8; R4 represents hydrogen, cyano, C1-6alkyl optionally substituted with hydroxy or C1-6alkyloxy, C(-O)-O-R6, C(-O)-NR7aR7b, C(-S)-NR7aR7b, S(-O)2-NR7aR7b or C(-O)-R8; or R3 and R4 taken together may form a bivalent radical of formula -C(-O)-NH-NH-C(-O)-; n is 1, 2, 3, 4 or 5; provided that at least one of R3 or R4 is other than hydrogen; and that if R3 represents C(-O)-OH, C(-O)-O-C1-6alkyl or C(-O)-O-C2-6alkenyl, then R4 is other than hydrogen; and that if R3 represents CH2OH and R1 and R5 represents hydrogen, then R4 is other than hydrogen; and that if R3 represents C(-O)-NH-C1-4alkyl-NH2 and R1 and R5 represents hydrogen, then R4 is other than hydrogen; and that if R3 represents and R1 and R5 represents hydrogen, then R4 is other than hydrogen having CCR2 receptor antagonistic properties. The invention also relates to processes for preparing the compounds of formula (1) and pharmaceutical compositions comprising them. |
