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 C1-6alkanediyl, 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.
申请公布号 WO2008148849(A3) 申请公布日期 2009.04.16
申请号 WO2008EP57008 申请日期 2008.06.05
申请人 JANSSEN PHARMACEUTICA N.V.;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;DE WAEPENAERT, KATHARINA, ANTONIA, GERMANIA, J.M.;ROEVENS, PETER, WALTER, MARIA;DAVIDENKO, PETR, VLADIMIRIVICH 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;DE WAEPENAERT, KATHARINA, ANTONIA, GERMANIA, J.M.;ROEVENS, PETER, WALTER, MARIA;DAVIDENKO, PETR, VLADIMIRIVICH
分类号 A61K31/451;A61K31/495;A61P3/06;A61P9/00;A61P35/00;C07D295/135 主分类号 A61K31/451
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