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The invention relates to a DGAT inhibitor of formula (I): including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents -C(=O)-; -O-C(=O)-; -C(=O)-C(=O)-; -NRx-C(=O)-; -Z1-C(O)-; -Z1-NRx-C(=O)-; -C(=O)-Z1-; -NRx-C(=O)-Z1-; -S(=O)p-; -C(=S)-; -NRx-C(=S)-; -Z1-C(=S)-; -Z1-NRX-C(=S)-; -C(=S)-Z1-; -NRx-C(=S)-Z1-; Y represents NRx-C(=0)- Z2-; -NRx-C(=0)-Z2-NRy-; -NRx-C(=0)-Z2-NRy-C(=0)-; -NRx-C(=0)-Z2-NRy-C(=0)- O-; -NRx-C(=0)-Z2-0-; -NRx-C(=0)-Z2-0-C(=0)-; -NRx-C(=0)-Z2-C(=0)-; -NRx-C(=0)-Z2-C(=0)-0-; -NRx-C(=0)-0-Z2-C(=0)-; -NRx-C(=0)-0-Z2-C(=0)-0-; -NRx-C(=O)-O-Z2-O-C(=O)-; -NRx-C(=O)-Z2-C(=O)-NRy-; -NRx-C(=O)-Z2-NRy- C(=0)-NRy-; -C(=O)-Z2-; -C(=O)-Z2-O-; -C(=0)-NRx-Z2-; -C(=0)-NRx-Z2-0-; -C(=0)-NRx-Z2-C(=0)-0-; -C(=0)-NRx-Z2-0-C(=0)-; -C(=0)-NRx-0-Z2-; -C(=O)- NRx-Z2-NRy-; -C(=0)-NRx-Z2-NRy-C(=0)-; -C(=0)-NRx-Z2-NRy-C(=0)-0-; R1 represents C1-12alkyl optionally substituted with cyano, C1-4alkyloxy, C1-4alkyl-oxyC1-4alkyloxy, C3-6Cy cloalkyl or aryl; C2-6alkenyl; C2-6alkynyl; C3-6cycloalkyl; adamantanyl; aryl1; aryl1C1-6alkyl; Het1; or Het1C1-6alkyl; provided that when Y represents -NRX-C(=O)-Z2-; -NRx-C(=0)-Z2-NRy; -NRX-C(=O)-Z2-C(=O)- NRy-; -C(=O)-Z2-; -NRx-C(=0)-Z2-NRy-C(=0)-NRy-; -C(=O)-NRX-Z2-; -C(=O)-NRX- O-Z2-; or -C(=0)-NRx-Z2-NRy-; then R1 may also represent hydrogen; R2 represents hydrogen, C1-12alkyl, C2-6alkenyl or R3; provided that if X represents -O-C(=O)-, then R2 represents R3; and provided that is excluded; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.
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- PIPERIDINE/PIPERAZINE DERIVATIVES
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The invention relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents -O-C(=O)-; -C(=O)-C(=O)-; -NRX-C(=O)-; -Z-C(=O)-; -Z-NRX-C(=O)-; -C(=O)-Z-; -NRX-C(=O)-Z-; -C(=S)-; -NRX-C(=S)-; -Z-C(=S)-; -Z-NRX-C(=S)-; - C(=S)-Z-; -NRX-C(=S)-Z-; Z represents a bivalent radical selected from C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl; wherein each of said C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl may optionally be substituted; and wherein two hydrogen atoms attached to the same carbon atom in C1-6alkanediyl may optionally be replaced by C1-6alkanediyl; Y represents -C(=O)-NRX- or -NRX-C(=O)-; R1 represents adamantanyl, C3-6cycloalkyl; aryl1 or Het1; R2 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3- dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6Cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl or heterocycle may optionally be substituted; R7 represents hydrogen, halo, C1-4alkyl, C1-4alkyl substituted with hydroxyl; provided that the following compounds (II), (III) are excluded; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine, as a DGAT inhibitor, of said compounds.
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