发明公开
EP1136482A1 2-Amino-3-(alkyl)-pyrimidone derivatives as GSK3beta inhibitors
审中-公开
2-氨基-3-（烷基） - 嘧啶脱氧核糖体GSK3β-血红素
- 专利标题： 2-Amino-3-(alkyl)-pyrimidone derivatives as GSK3beta inhibitors
- 专利标题（中）： 2-氨基-3-（烷基） - 嘧啶脱氧核糖体GSK3β-血红素
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申请号： EP00400800.9申请日： 2000-03-23
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公开(公告)号： EP1136482A1公开(公告)日： 2001-09-26
- 发明人: Almario-Garcia, Antonio , Frost, Jonathan Reid , Li, Adrien-Tak , Ando, Ryoichi , Watanabe, Kazutoshi
- 申请人： SANOFI-SYNTHELABO , Mitsubishi-Tokyo Pharmaceuticals, Inc.
- 申请人地址： 174, Avenue de France 75013 Paris FR
- 专利权人： SANOFI-SYNTHELABO,Mitsubishi-Tokyo Pharmaceuticals, Inc.
- 当前专利权人： SANOFI-SYNTHELABO,Mitsubishi-Tokyo Pharmaceuticals, Inc.
- 当前专利权人地址： 174, Avenue de France 75013 Paris FR
- 代理机构： Thouret-Lemaitre, Elisabeth
- 主分类号： C07D401/04
- IPC分类号： C07D401/04 ; A61K31/505 ; A61P25/28
摘要：
A pyrimidone derivative represented by formula (I) or a salt thereof:
Wherein :
R1 represents a hydrogen atom or a C 1-6 alkyl group;
R2 represents a C 1-6 alkyl group which may be substituted, a C 2-6 alkenyl group which may be substituted, a C 3-6 alkynyl group which may be substituted, a C 3-6 cycloalkyl group which may be substituted, or a C 6-10 ARYL group which may be substituted;
or R1 and R2 form together a C 2-6 alkylene group which may be substituted;
or R1 and R2 form together a chain of formula -(CH 2 ) 2 -X-(CH 2 ) 2 - or
-(CH 2 ) 2 -X-(CH 2 ) 3 - where X represents a oxygen atom, a sulfur atom, or a nitrogen atom which may be substituted;
R3 represents a 2, 3 or 4-pyridyl group optionally substituted by a C 1-4 alkyl group, C 1-4 alkoxy group or a halogen atom; and
R4 represents a C 1-6 alkyl group optionally substituted by a C 6,10 aryl group which may be substituted.
And 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's disease, Parkinson's disease, frontoparietal dementia, corticobasal degeneration, Pick's disease, cerebrovascular accidents, brain and spinal trauma, and peripheral neuropathies.
Wherein :
R1 represents a hydrogen atom or a C 1-6 alkyl group;
R2 represents a C 1-6 alkyl group which may be substituted, a C 2-6 alkenyl group which may be substituted, a C 3-6 alkynyl group which may be substituted, a C 3-6 cycloalkyl group which may be substituted, or a C 6-10 ARYL group which may be substituted;
or R1 and R2 form together a C 2-6 alkylene group which may be substituted;
or R1 and R2 form together a chain of formula -(CH 2 ) 2 -X-(CH 2 ) 2 - or
-(CH 2 ) 2 -X-(CH 2 ) 3 - where X represents a oxygen atom, a sulfur atom, or a nitrogen atom which may be substituted;
R3 represents a 2, 3 or 4-pyridyl group optionally substituted by a C 1-4 alkyl group, C 1-4 alkoxy group or a halogen atom; and
R4 represents a C 1-6 alkyl group optionally substituted by a C 6,10 aryl group which may be substituted.
And 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's disease, Parkinson's disease, frontoparietal dementia, corticobasal degeneration, Pick's disease, cerebrovascular accidents, brain and spinal trauma, and peripheral neuropathies.
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