| 摘要 |
<p>This invention concerns a compound of formula (I),a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A represents a 6-membered heterocycle; R1 is hydrogen; aryl; formyl; C¿1-6?alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyloxyC1-6alkylcarbonyl; X is a direct bond or a linker atom or group; Z is O or S; R?2¿ is hydrogen, C¿1-10?alkyl, C2-10alkenyl, C2-10alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R?3¿ is hydrogen; hydroxy; halo; optionally substituted C¿1-6?alkyl or C2-6alkenyl or C2-6alkynyl; C1-6alkyloxy; C1-6alkylthio; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; R?21; R21-C¿1-6alkyl; R?21-O-; R21-S-; R21¿-C(=O)-; R21-S(=O)¿p-; R?7-S(=O)¿p-; R?7-S(=O)¿p?-NH-; R?21¿-S(=O)¿p?-NH-; R?7¿-C(=O)-; -NHC(=O)H; -C(=O)NHNH¿2; R?7-C(=O)-NH-; R21-C(=O)-NH-; -C(=NH)R7; -C(=NH)R?21 ; R4a or R4b¿ each independently represent hydrogen, R8, -Y1-NR9-Y2-NR?10R11, -Y¿1-NR9-Y1-R8, -Y1-NR9R10; provided that -X-R2 and/or R3 is other than hydrogen;their use, pharmaceutical compositions comprising them and processes for their preparation.</p> |
