| 摘要 |
The invention relates to a DGAT inhibitor of formula (I) including any st ereochemically isomeric form thereof, wherein A represents CH or N; X repres ents O or NRx; the dotted line represents an optional bond in case A represe nts a carbon atom; Y represents a direct bond; -NRx -C(=O)-; -C(=O)-NRx -; - NRx -C(=O)- Z-; -NRx -C(=O)-Z-NRy -; -NRx -C(=O)-Z-NRy -C(=O)-; -NRx -C(=O)- Z-NRy -C(=O)-O-; -NRx -C(=O)-Z-O-; -NRx -C(=O)-Z-O-C(=O)-; -NRx -C(=O)-Z-C(= O)-; -NRx -C(=O)-Z-C(=O)-O-; -NRx -C(=O)-O-Z-C(=O)-; -NRx -C(=O)-O-Z-C(=O)-O -; -NRx -C(=O)-O-Z- O-C(=O)-; -NRx -C(=O)-Z-C(=O)-NRy -; -NRx -C(=O)-Z-NRy - C(=O)-NRy -; -C(=O)-Z-; -C(=O)-Z-O-; -C(=O)-NRx -Z-; -C(=O)-NRx -Z-O-; -C(=O )-NRx -Z-C(=O)-O-; -C(=O)-NRx -Z-O-C(=O)-; -C(=O)-NRx -O-Z-; -C(=O)-NRx -Z-N Ry -; -C(=O)-NRx -Z- NRy -C(=O)-; -C(=O)-NRx -Z-NRy -C(=O)-O-; R1 represents optionally substituted C1-12alkyl; C2-6alkenyl; C2-6alkynyl; C3-6cycloalkyl ; aryl1; aryl1 C1-6alkyl; Het1; or Het1C1- 6alkyl; provided that when Y repr esents -NRx -C(=O)-Z-; -NRx -C(=O)-Z-NRy; -NRx - C(=O)-Z-C(=O)-NRy -; -C(=O) -Z-; -NRx -C(=O)-Z-NRy -C(=O)-NRy -; -C(=O)-NRx -Z-; -C(=O)-NRx -O-Z-; or -C (=O)-NRx -Z-NRy -; then R1 may also represent hydrogen; R2 and R3 each indep endently represent hydrogen; hydroxyl; carboxyl; halo; C1-6alkyl; polyhaloC1 -6alkyl; C1-6alkyloxyoptionally substituted withC1-4alkyloxy; C1-6alkylthio; polyhaloC1-6alkyloxy; C1-6alkyloxycarbonyl; cyano; aminocarbonyl; mono-or d i(C1-4alkyl)aminocarbonyl; C1-6alkylcarbonyl; nitro; amino; mono-or di(C1-4a lkyl)amino; -S(=O) p-C1-4alkyl; R4 represents hydrogen; hydroxyl; carboxyl; halo; C1-6alkyl; polyhaloC1-6alkyl; optionally substituted C1-6alkyloxy; C1- 6alkylthio; polyhalo-C1-6alkyloxy; C1-6alkyloxycarbonyl wherein C1-6alkyl ma yoptionally be substituted; cyano; C1-6alkylcarbonyl; nitro; amino; mono-or di(C1-4alkyl)amino; C1-4alkylcarbonylamino; -S(=O) p-C1-4alkyl; R6 R5 N-C(=O )-; R6 R5 N-C1-6alkyl; C3-6cycloalkyl; aryl; aryloxy; arylC1-4alkyl; aryl-C( =O)-C1-4alkyl; aryl-C(=O)-; Het; HetC1-4alkyl; Het-C(=O)-C1-4alkyl; Het-C(=O )-; Het-O-; R9 represents hydrogen, halo,C1-4alkyl, C1-4alkyl substituted wi th hydroxyl; a N-oxide thereof, a pharmaceutically acceptable salt thereof o r a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as wel l as the use as a medicine of saidcompounds.
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