发明申请
US20050222172A1 Heteroaryl substituted 2-pyridinyl and 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one derivatives
失效
杂芳基取代的2-吡啶基和2-嘧啶基-6,7,8,9-四氢嘧啶并[1,2-a]嘧啶-4-酮衍生物
- 专利标题: Heteroaryl substituted 2-pyridinyl and 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one derivatives
- 专利标题(中): 杂芳基取代的2-吡啶基和2-嘧啶基-6,7,8,9-四氢嘧啶并[1,2-a]嘧啶-4-酮衍生物
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申请号: US10504677申请日: 2003-02-26
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公开(公告)号: US20050222172A1公开(公告)日: 2005-10-06
- 发明人: Alistair Lochead , Alain Nedelec , Mourad Saady , Philippe Yaiche
- 申请人: Alistair Lochead , Alain Nedelec , Mourad Saady , Philippe Yaiche
- 优先权: EP02290485.8 20020228; EP02290486.6 20020228
- 国际申请: PCT/EP03/02651 WO 20030226
- 主分类号: A61K31/519
- IPC分类号: A61K31/519 ; A61P3/04 ; A61P3/10 ; A61P9/10 ; A61P17/14 ; A61P21/00 ; A61P25/00 ; A61P25/02 ; A61P25/08 ; A61P25/16 ; A61P25/18 ; A61P25/24 ; A61P25/28 ; A61P25/34 ; A61P27/02 ; A61P27/06 ; A61P35/00 ; A61P43/00 ; C07D487/04 ; C07D519/00
摘要:
The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein: (1) X represents two hydrogen atoms, a sulphur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Y represents a bond, an ethenylene group, an ethynylene group or a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring optionally substituted; R2 represents a heterocyclic bicyclic rings, having 1-4 heteroatoms selected from an oxygen atom, a sulfur atom and a nitrogen atom and having 5-9 carbon atoms, of formula (II) R3 represents a hydrogen atom, a C1-6 alkyl group, a hydroxy group, a C1-4 alkoxy group or a halogen atom; R4 represents a hydrogen atom, a C1-6 alkyl group, a C1-4 alkoxy group or a halogen 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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