发明公开
EP1460075A1 Substituted 8-Pyridinyl-6,7,8,9-Tetrahydropyrimido[1,2-a]Pyrimidin-4-one and 8-Phenyl-6-7,8,9-Tetrahydropyrimido[1,2-a]Pyrimidin-4-one derivatives
审中-公开
取代基8-全氟-6,7,8,9-四氢嘧啶并[1,2-a]嘧啶-4-酮衍生物
- 专利标题： Substituted 8-Pyridinyl-6,7,8,9-Tetrahydropyrimido[1,2-a]Pyrimidin-4-one and 8-Phenyl-6-7,8,9-Tetrahydropyrimido[1,2-a]Pyrimidin-4-one derivatives
- 专利标题（中）： 取代基8-全氟-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： EP03290727.1申请日： 2003-03-21
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公开(公告)号： EP1460075A1公开(公告)日： 2004-09-22
- 发明人: Lochead, Alistair W. , Saady, Mourad , Slowinski, Franck , 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 ; A61P25/00
摘要：
The invention relates to substituted-pyrimidone derivatives represented by formula (I) or a salt thereof:
wherein:
X represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C 1-2 alkyl group and a hydrogen atom;
Y represents a bond, a carbonyl group, a methylene group optionally substituted;
R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring, the rings being optionally substituted;
R2 represents a phenyl group or a naphthalene ring; the phenyl group and the naphthalene ring being optionally substituted;
R3 represents a hydrogen atom or a C 1-6 alkyl group;
R4 represents a phenyl group, a pyridinyl group or a naphthalene ring, the groups and the ring being optionally substituted;
R5 represents a hydrogen atom, a C 1-6 alkyl group or a halogen atom;
n represents 0 to 3; and p+q=0-3.
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.
wherein:
X represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C 1-2 alkyl group and a hydrogen atom;
Y represents a bond, a carbonyl group, a methylene group optionally substituted;
R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring, the rings being optionally substituted;
R2 represents a phenyl group or a naphthalene ring; the phenyl group and the naphthalene ring being optionally substituted;
R3 represents a hydrogen atom or a C 1-6 alkyl group;
R4 represents a phenyl group, a pyridinyl group or a naphthalene ring, the groups and the ring being optionally substituted;
R5 represents a hydrogen atom, a C 1-6 alkyl group or a halogen atom;
n represents 0 to 3; and p+q=0-3.
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.
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