发明授权
US5777114A Spiro�heterocycle-imidazo�1,2-a!indeno�1,2-e!pyrazine!-4'-ones,
preparation thereof and drugs containing same
失效
螺[杂环咪唑并[1,2-a]茚并[1,2-e]吡嗪] -4'-酮，其制备方法和含有它们的药物
- 专利标题： Spiro�heterocycle-imidazo�1,2-a!indeno�1,2-e!pyrazine!-4'-ones, preparation thereof and drugs containing same
- 专利标题（中）： 螺[杂环咪唑并[1,2-a]茚并[1,2-e]吡嗪] -4'-酮，其制备方法和含有它们的药物
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申请号： US836410申请日： 1997-06-30
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公开(公告)号： US5777114A公开(公告)日： 1998-07-07
- 发明人: Jean-Claude Aloup , Fran.cedilla.ois Audiau , Michel Barreau , Dominique Damour , Arielle Genevois-Borella , Patrick Jimonet , Serge Mignani , Yves Ribeill
- 申请人： Jean-Claude Aloup , Fran.cedilla.ois Audiau , Michel Barreau , Dominique Damour , Arielle Genevois-Borella , Patrick Jimonet , Serge Mignani , Yves Ribeill
- 申请人地址： FRX Antony Cedex
- 专利权人： Rhone-Poulenc Rorer S.A.
- 当前专利权人： Rhone-Poulenc Rorer S.A.
- 当前专利权人地址： FRX Antony Cedex
- 优先权： FRX9413060 19941102
- 主分类号： C07D487/04
- IPC分类号： C07D487/04 ; A61K31/495 ; A61P9/02 ; A61P9/08 ; A61P9/10 ; A61P9/14 ; A61P11/00 ; A61P25/00 ; A61P25/28 ; A61P43/00 ; C07D471/20 ; C07D487/20 ; C07D471/235 ; C07D487/241
摘要：
Compounds of formula (I): ##STR1## wherein R.sub.3 and R.sub.4, taken together with the carbon atom to which they are attached, form (a) a 2- or 3-pyrrolidine ring, a 2- or 4-piperidine ring or a 2-azacycloheptane ring, said rings being optionally substituted at the nitrogen atom by an alkyl, --CHO, --COOR.sub.11, --CO--alk--COOR.sub.6, --CO--alk--NR.sub.6 R.sub.12, --CO--alk--CONR.sub.6 R.sub.8, --CO--COOR.sub.6, --CO--CH.sub.2 --O--CH.sub.2 --COOR.sub.6, --CO--CH.sub.2 --S--CH.sub.2 --COOR.sub.6, --CO--CH.dbd.CH--COOR.sub.6, CO--alk, --CO--Ar", --CO--alk--Ar", --CO--NH--Ar", --CO--NH--alk--Ar", --CO--Het, --CO--alk--Het, --CO--NH--Het, --CO--NH--alk--Het, --CO--NH.sub.2, --CO--NH--alk, --CO--N(alk)alk', --CS--NH.sub.2, --CS--NH--alk, --CS--NH--Ar", --CS--NH--Het, --alk--Het, --alk--NR.sub.6 R.sub.8, --alk--COOR.sub.6, --alk--CO--NR.sub.6 R.sub.8, --alk--Ar", --SO.sub.2 --alk or --SO.sub.2 --Ar radical, or a --CO-cycloalkyl radical where the cycloalkyl is optionally 2-substituted by a carboxyl radical; or (b) a 2-pyrrolidin-5-one ring. The compounds of formula (I) have useful pharmacological properties and are .alpha.-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists, said receptor also being known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive N-methyl-D-aspartate (NMDA) receptor antagonists, and especially NMDA receptor glycine modulation site ligands.