- 专利标题: 1-[alkyl], 1-[(heteroaryl)alkyl] and 1-[(aryl)alkyl]-7pyridinyl-imidazo[1,2-alpha]pyrimidin-5(1H)-one derivatives
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申请号: US10362857申请日: 2001-08-31
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公开(公告)号: US07067521B2公开(公告)日: 2006-06-27
- 发明人: Alistair Lochead , Séverine Marguerie , Mourad Saady , Philippe Yaiche
- 申请人: Alistair Lochead , Séverine Marguerie , Mourad Saady , Philippe Yaiche
- 申请人地址: FR Paris
- 专利权人: sanofi-aventis
- 当前专利权人: sanofi-aventis
- 当前专利权人地址: FR Paris
- 代理商 Balaram Gupta
- 优先权: EP00402411 20000901
- 国际申请: PCT/EP01/10725 WO 20010831
- 国际公布: WO02/18385 WO 20020307
- 主分类号: A61K31/519
- IPC分类号: A61K31/519
摘要:
The invention relates to an imidazo[1,2-a]pyrimidone derivative represented by formula (1) or a salt thereof, wherein: X represents a bond, an ethenylene group, and ethenylene group, a methylene group optionally substituted by one or two groups selected from a C1-6 alkyl group, a hydroxy group and a C1-4 alkoxy group; a carbonyl group, an oxygen atom, a sulfur atom, a sulfonyl group, a sulfoxide group or a nitrogen atom being optionally substituted by a C1-6 alkyl group; R1 represents a 2,3 or 4-pyridyl group optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or a halogen atom; R2 represents a C1-6 alkyl group, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a benzyl group, a phenyl ring, a naphthyl ring, 5,6,7,8-tetrahydronaphthyl ring, a pyridyl ring, an indole ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring, the benzyl group and the rings being optionally substituted by 1 to 4 substituents selected from a C1-6 alkyl group, a phenyl ring, a halogen atom, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a hydroxyl group, a C1-4 alkoxy group, a nitro, a cyano, an amino, a C1-6 monoalkylamino group or a C2-10 dialkylamino group; and n represents 0 to 3. 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, such as Alzheimer disease.