- 专利标题: PIPERIDINE/PIPERAZINE DERIVATIVES
-
申请号: US12663011申请日: 2008-06-06
-
公开(公告)号: US20100210618A1公开(公告)日: 2010-08-19
- 发明人: Jean-Pierre Andre Marc Bongartz , Joannes Theodorus Maria Linders , Lieven Mieerpoel , Guy Rosalia Eugeen Van Lommen , Erwin Coesemans , Mirielle Braeken , Christophe Francis Robert Nestor Buyck , Monique Jenny Marie Berwaer , Katharina Antonia Germania J.M. De Waepenaret , Peter Walter Maria Roevens , Petr Vladimirivich Davidenko
- 申请人: Jean-Pierre Andre Marc Bongartz , Joannes Theodorus Maria Linders , Lieven Mieerpoel , Guy Rosalia Eugeen Van Lommen , Erwin Coesemans , Mirielle Braeken , Christophe Francis Robert Nestor Buyck , Monique Jenny Marie Berwaer , Katharina Antonia Germania J.M. De Waepenaret , Peter Walter Maria Roevens , Petr Vladimirivich Davidenko
- 优先权: EP07109866.9 20070608
- 国际申请: PCT/EP2008/057008 WO 20080606
- 主分类号: A61K31/397
- IPC分类号: A61K31/397 ; C07D401/12 ; C07D417/12 ; A61K31/497 ; A61K31/454 ; C07D405/12 ; C07D241/04 ; A61K31/4965 ; C07D211/78 ; A61K31/451 ; C07D403/12 ; C07D413/12 ; A61K31/5377 ; C07D279/02 ; A61K31/541 ; C07D279/12 ; A61P3/04 ; A61P3/06 ; A61P3/10 ; A61P1/16
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.
公开/授权文献
- US08946228B2 Piperidine/piperazine derivatives 公开/授权日:2015-02-03
信息查询