- 专利标题: Substituted 2-pyridinyl-6,7,8,9-tetrahydropyrimido{1,2-a}pyrimidin-4-one and 7-pyridinyl-2,3-dihydroimidazo{1,2-a}pyrimidin-5(1h)one derivatives
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申请号: US10490135申请日: 2002-09-19
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公开(公告)号: US07214682B2公开(公告)日: 2007-05-08
- 发明人: Thierry Gallet , Patrick Lardenois , Alistair Lochead , Séverine Marguerie , Alain Nedelec , Mourad Saady , Franck Slowinski , Philippe Yaiche
- 申请人: Thierry Gallet , Patrick Lardenois , Alistair Lochead , Séverine Marguerie , Alain Nedelec , Mourad Saady , Franck Slowinski , Philippe Yaiche
- 申请人地址: FR Paris JP Osaka
- 专利权人: Sanofi-aventis,Mitsubishi Pharma Corporation
- 当前专利权人: Sanofi-aventis,Mitsubishi Pharma Corporation
- 当前专利权人地址: FR Paris JP Osaka
- 代理商 Balaram Gupta
- 优先权: EP01402432 20010921; EP02290489 20020228
- 国际申请: PCT/EP02/11128 WO 20020919
- 国际公布: WO03/027116 WO 20030403
- 主分类号: A01N43/90
- IPC分类号: A01N43/90 ; A61K31/519 ; A01N43/62 ; A61K31/55 ; C07D471/00 ; C07D487/00
摘要:
The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein X represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Y represents a bond, an ethenylene group, an ethynylene group an oxygen atom, a sulfur atom, a sulfonyl group, a sulfoxide group, a carbonyl group, a hydroxyiminomethylene group, a dioxolan group, a nitrogen atom being optionally substituted; or a methylene group optionally substituted; or a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring optionally substituted; R2 may represent a C1-6 alkyl group optionally; a C3-6 cycloalkyl group, a C1-4 alkythio group, a C1-4 alkoxy group, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a phenylthio group, a benzyl group, a benzene ring, an indan ring, a 5,6,7,8-tetrahydronaphthalene ring, a naphthalene ring, a pyridine ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring; R3 and R4 represent, each independently, a hydrogen atom, a C1-6 alkyl group, a hydroxy group, a C1-4 alkoxy group or a halogen atom; R5 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; with the proviso that when R3 and R4 represent each a hydrogen atom then R5 is not a hydrogen atom. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β or GSK3β, and cdk5/p25, such as Alzheimer disease
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