发明名称 Piperidine/Piperazine derivatives
摘要 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 C1-6 alkanediyl, 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 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.
申请公布号 JO2972(B) 申请公布日期 2016.03.15
申请号 JO20080000253 申请日期 2008.06.04
申请人 JANSSEN PHARMACEUTICA N.V. 发明人 BONGARTZ, JEAN-PIERRE ANDRE MARC;LINDERS, JOANNES THEODORUS MARIA;MEERPOEL, LIEVEN;VAN LOMMEN, GUY ROSALIA EUGEEN;COESEMANS, ERWIN;BRAEKEN, MIRIELLE;BUYCK, CHRISTOPHE FRANCIS ROBERT NESTOR;BERWAER, MONIQUE JENNY MARIE;DAVIDENKO, PETR VLADIMIRIVICH;PETER WALTER MARIA ،ROEVENS;DE WAEPENAERT, KATHARINA ANTONIA GERMANIA J.M
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