发明公开
EP2238141A1 SUBSTITUTED ARYLAMIDE DIAZEPINOPYRIMIDONE DERIVATIVES FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES CAUSED BY ABNORMAL ACTIVITY OF GSK3-BETA
有权
取代芳香胺衍生物DIAZEPINOPYRIMIDON神经退行性疾病的治疗异常引起的GSK3-β活度
- 专利标题: SUBSTITUTED ARYLAMIDE DIAZEPINOPYRIMIDONE DERIVATIVES FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES CAUSED BY ABNORMAL ACTIVITY OF GSK3-BETA
- 专利标题(中): 取代芳香胺衍生物DIAZEPINOPYRIMIDON神经退行性疾病的治疗异常引起的GSK3-β活度
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申请号: EP09706634.4申请日: 2009-01-27
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公开(公告)号: EP2238141A1公开(公告)日: 2010-10-13
- 发明人: FAYOL, Aude , LOCHEAD, Alistair , SAADY, Mourad , VACHE, Julien , YAICHE, Philippe
- 申请人: Sanofi-Aventis , Mitsubishi Tanabe Pharma Corporation
- 申请人地址: 174 Avenue de France 75013 Paris FR
- 专利权人: Sanofi-Aventis,Mitsubishi Tanabe Pharma Corporation
- 当前专利权人: Sanofi-Aventis,Mitsubishi Tanabe Pharma Corporation
- 当前专利权人地址: 174 Avenue de France 75013 Paris FR
- 代理机构: Dépré, Marie-Line
- 优先权: EP08290074 20080129
- 国际公布: WO2009095789 20090806
- 主分类号: C07D487/04
- IPC分类号: C07D487/04 ; A61K31/519 ; A61P25/00
摘要:
A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: Y represents two hydrogen atoms, a sulphur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Z represents a bond, an oxygen atom, a nitrogen atom substituted by a hydrogen atom or a C1-3 alkyl group, a sulphur atom, a methylene group optionally substituted by one or two groups chosen from a C1-6 alkyl group, a hydroxyl group, a C1-6 alkoxy group, a C1-2 perhalogenated alkyl group or an amino group; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring, the ring being optionally substituted by a C1-6 alkyl group, a C1-6 alkoxy group or a halogen atom; R2 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; R3 represents a benzene ring or a naphthalene ring; the rings being optionally substituted R4 represents a hydrogen atom, a C1-6 alkyl group, a C3-7 cycloalkyl group, a C3-7 cycloalkyl-C1-6 alkyl group, a COO (C1-6-alkyl) group, these group being optionally substituted; R5 represents a hydrogen atom or a C1-6 alkyl group and n represents 0 to 3 and their therapeutic use for the treatment of neurodegenerative diseases caused by abnormal activity of GSK3β.
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