发明授权
EP1430057B1 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
有权
取代基2-吡啶基-6,7,8,9-四氢吡啶并[1,2-a]嘧啶-4-基] -7-吡啶-2,3-二氢吲哚并[1,2-a]嘧啶-5(1H)O
- 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
- 专利标题(中): 取代基2-吡啶基-6,7,8,9-四氢吡啶并[1,2-a]嘧啶-4-基] -7-吡啶-2,3-二氢吲哚并[1,2-a]嘧啶-5(1H)O
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申请号: EP02785157.5申请日: 2002-09-19
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公开(公告)号: EP1430057B1公开(公告)日: 2005-08-31
- 发明人: GALLET, Thierry , LARDENOIS, Patrick , LOCHEAD, Alistair , MARGUERIE, Séverine , NEDELEC, Alain , SAADY, Mourad , SLOWINSKI, Franck , YAICHE, Philippe
- 申请人: Sanofi-Aventis , Mitsubishi Pharma Corporation
- 申请人地址: 174, Avenue de France 75013 Paris FR
- 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: 174, Avenue de France 75013 Paris FR
- 代理机构: Kugel, Dominique
- 优先权: EP01402432 20010921; EP02290489 20020228
- 国际公布: WO2003027116 20030403
- 主分类号: C07D487/04
- IPC分类号: C07D487/04
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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