发明授权
EP0880522B1 DERIVES DE 5H,10H-IMIDAZO[1,2-a]INDENO[1,2-e]PYRAZINE-4-ONE ANTAGONISTES DES RECEPTEURS AMPA ET NMDA, LEUR PREPARATION, LEURS INTERMEDIAIRES ET LES MEDICAMENTS LES CONTENANT
失效
5H,10H - 咪唑并[1,2-α]茚并[1,2-e]吡嗪将-4-酮衍生物及其NMDA AMPA受体拮抗剂,它们的制备及中间体和药物含有它们
- 专利标题: DERIVES DE 5H,10H-IMIDAZO[1,2-a]INDENO[1,2-e]PYRAZINE-4-ONE ANTAGONISTES DES RECEPTEURS AMPA ET NMDA, LEUR PREPARATION, LEURS INTERMEDIAIRES ET LES MEDICAMENTS LES CONTENANT
- 专利标题(英): 5H,10H-IMIDAZO[1,2-a]INDENO[1,2-e]PYRAZINE-4-ONE DERIVATIVES AMPA AND NMDA RECEPTORS ANTAGONISTS, PREPARATION THEREOF, INTERMEDIATES THEREOF AND DRUGS CONTAINING SAME
- 专利标题(中): 5H,10H - 咪唑并[1,2-α]茚并[1,2-e]吡嗪将-4-酮衍生物及其NMDA AMPA受体拮抗剂,它们的制备及中间体和药物含有它们
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申请号: EP97900236.7申请日: 1997-01-06
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公开(公告)号: EP0880522B1公开(公告)日: 2001-09-19
- 发明人: ALOUP, Jean-Claude , BOUQUEREL, Jean , DAMOUR, Dominique , HARDY, Jean-Claude , JIMONET, Patrick , MANFRE, Franco , MIGNANI, Serge , NEMECEK, Patrick
- 申请人: Aventis Pharma S.A.
- 申请人地址: 20, avenue Raymond Aron 92160 Antony FR
- 专利权人: Aventis Pharma S.A.
- 当前专利权人: Aventis Pharma S.A.
- 当前专利权人地址: 20, avenue Raymond Aron 92160 Antony FR
- 优先权: FR9600192 19960110
- 国际公布: WO9725328 19970717
- 主分类号: C07D487/04
- IPC分类号: C07D487/04 ; C07D233/90 ; A61K31/495 ; C07F9/6561 ; C07F9/6506
摘要:
Compounds of formula (I), wherein R is a hydrogen atom or a -COOH, -alk-COOH, -PO3H2, -CH2-PO3H2, or -CH=CH-COOH radical, or a phenyl radical substituted by a carboxy radical, R1 is an alk-CN, -alk-COOH, -alk-Het, alk-PO3H2 or -alk-CO-NH-SO2R2 radical, R2 is an alkyl or phenyl radical, alk is an alkyl radical, Het is a saturated or unsaturated mono- or polycyclic heterocyclic ring containing 1-9 carbon atoms and one or more heteroatoms selected from O, S and N, said heterocyclic ring optionally being substituted by one or more alkyl, phenyl or phenylalkyl radicals, with the proviso that when R is a hydrogen atom or a -COOH or -PO3H2 radical, R1 cannot be -alk-COOH, isomers, racemic mixtures, enantiomers and diastereoisomers thereof, salts thereof, the preparation thereof, intermediates thereof and drugs containing said compounds, are disclosed. The compounds of formula (I) have valuable pharmacological properties and are antagonists of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor also known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive antagonists of the N-methyl-D-aspartate (NMDA) receptor, and specifically ligands for NMDA receptor glycine modulator sites.
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