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)-; -NR<sup>X</sup>-C(=O)-; -Z-C(=O)-; -Z-NR<sup>X</sup>-C(=O)-; -C(=O)-Z-; -NR<sup>X</sup>-C(=O)-Z-; -C(=S)-; -NR<sup>X</sup>-C(=S)-; -Z-C(=S)-; -Z-NR<sup>X</sup>-C(=S)-; - C(=S)-Z-; -NR<sup>X</sup>-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)-NR<sup>X</sup>- or -NR<sup>X</sup>-C(=O)-; R<sup>1</sup> represents adamantanyl, C3-6cycloalkyl; aryl<sup>1</sup> or Het<sup>1</sup>; R<sup>2</sup> 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; R<sup>7</sup> 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 MX2009013334(A) 申请公布日期 2010.01.20
申请号 MX20090013334 申请日期 2008.06.05
申请人 JANSSEN PHARMACEUTICA N.V. 发明人 MEERPOEL, LIEVEN;BRAEKEN, MIRIELLE;COESEMANS, ERWIN;LINDERS, JOANNES THEODORUS MARIA;BUYCK, CHRISTOPHE FRANCIS ROBERT NESTOR;ROEVENS, PETER WALTER MARIA;VAN LOMMEN, GUY ROSALIA EUGEEN;BERWAER, MONIQUE JENNY MARIE;BONGARTZ, JEAN-PIERRE ANDRE MARC;DE WAEPENAERT, KATHARINA ANTONIA GERMANIA J.M.;DAVIDENKO, PETR VLADIMIRIVICH
分类号 A61K31/451;A61K31/495;A61P3/06;A61P9/00;A61P35/00;C07D295/135 主分类号 A61K31/451
代理机构 代理人
主权项
地址