发明公开
EP1340758A1 Heteroaryl 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
审中-公开
杂芳基取代基2-吡啶基-6,7,8,9-四氢-1,2-a吡啶-4-酮和7-吡啶基-2,3-二氢咪唑并[1,2-a嘧啶-5（1H）
- 专利标题： Heteroaryl 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）： 杂芳基取代基2-吡啶基-6,7,8,9-四氢-1,2-a吡啶-4-酮和7-吡啶基-2,3-二氢咪唑并[1,2-a嘧啶-5（1H）
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申请号： EP02290485.8申请日： 2002-02-28
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公开(公告)号： EP1340758A1公开(公告)日： 2003-09-03
- 发明人: Lochhead, Alistair, W. , Nedelec, Alain , Saady, Mourad , Yaiche, Philippe
- 申请人： SANOFI-SYNTHELABO , MITSUBISHI PHARMA CORPORATION
- 申请人地址： 174, Avenue de France 75013 Paris FR
- 专利权人： SANOFI-SYNTHELABO,MITSUBISHI PHARMA CORPORATION
- 当前专利权人： SANOFI-SYNTHELABO,MITSUBISHI PHARMA CORPORATION
- 当前专利权人地址： 174, Avenue de France 75013 Paris FR
- 代理机构： Kugel, Dominique
- 主分类号： C07D487/04
- IPC分类号： C07D487/04 ; C07D519/00 ; A61K31/519 ; A61P25/00
摘要：
The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein:
X represents two hydrogen atoms, a sulphur atom, an oxygen atom or a C 1-2 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 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
R3 represents a hydrogen atom, a C 1-6 alkyl group, a hydroxy group, a C 1-4 alkoxy group or a halogen atom;
R4 represents a hydrogen atom, a C 1-6 alkyl group, a C 1-4 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.
X represents two hydrogen atoms, a sulphur atom, an oxygen atom or a C 1-2 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 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
R3 represents a hydrogen atom, a C 1-6 alkyl group, a hydroxy group, a C 1-4 alkoxy group or a halogen atom;
R4 represents a hydrogen atom, a C 1-6 alkyl group, a C 1-4 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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