发明公开
- 专利标题： 2-[(Heteroaryl)alkylamino]pyrimidone derivatives
- 专利标题（中）： 2-烯基芳基烷基氨基嘧啶二酮
-
申请号： EP00400806.6申请日： 2000-03-23
-
公开(公告)号： EP1136491A1公开(公告)日： 2001-09-26
- 发明人: Almario-Garcia, Antonio , Frost, Jonathan Reid , Li, Adrien-Tak
- 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： C07D405/14
- IPC分类号： C07D405/14 ; C07D409/14 ; C07D401/14 ; A61K31/506 ; A61P25/28
摘要：
The invention relates to 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 furan ring, thiophene ring, pyrrole ring or imidazole ring, the rings being optionally substituted by 1 to 3 substituents selected from a C 1-6 alkyl group, a halogen atom, a C 1 - 2 perhalogenated alkyl group, a C 1 - 3 halogenated alkyl group, a hydroxyl group, a C 1-6 alkoxy group, a nitro, a cyano an amino, a C 1-6 monoalkylamino group, a C 2-10 dialkylamino group, a C 1-6 alkylcarbonylamino group, a C 6,10 arylcarbonylamino group or a phenyl group;
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;
n represents 1 to 5.
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'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 furan ring, thiophene ring, pyrrole ring or imidazole ring, the rings being optionally substituted by 1 to 3 substituents selected from a C 1-6 alkyl group, a halogen atom, a C 1 - 2 perhalogenated alkyl group, a C 1 - 3 halogenated alkyl group, a hydroxyl group, a C 1-6 alkoxy group, a nitro, a cyano an amino, a C 1-6 monoalkylamino group, a C 2-10 dialkylamino group, a C 1-6 alkylcarbonylamino group, a C 6,10 arylcarbonylamino group or a phenyl group;
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;
n represents 1 to 5.
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's disease, Parkinson's disease, frontoparietal dementia, corticobasal degeneration, Pick's disease, cerebrovascular accidents, brain and spinal trauma, and peripheral neuropathies.
信息查询
