发明名称 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
摘要 The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof: wherein: X represents hydrogen atoms, a sulphur atom, an oxygen atom or a C<SUB>1-2 </SUB>alkyl group and a hydrogen atom; Y represents a bond, an ethenylene group, an ethynylene group, a 1,2-cyclopropylene, an oxygen atom, a sulphur atom, a sulfonyl group, a sulfoxyde group, a carbonyl group, a nitrogen atom being optionally substituted; or a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridyl group optionally substituted by a C<SUB>3-6 </SUB>cycloalkyl group a C<SUB>1-4 </SUB>alkyl group, a C<SUB>1-4 </SUB>alkoxy group, a benzyl group or a halogen atom; when Y represents a bond, a methylene group optionally substituted or a carbonyl group then R2 represents a C<SUB>1-6 </SUB>alkyl group, a C<SUB>3-6 </SUB>cycloalkyl group, a C<SUB>1-4 </SUB>alkylthio group, a C<SUB>1-4 </SUB>alkoxy group, a C<SUB>1-2 </SUB>perhalogenated alkyl group, a C<SUB>1-3 </SUB>halogenated alkyl group, a 5,6,7,8-tetrahydronaphthyl ring, a naphthyl ring, a phenylthio group, a benzyl group, a phenyl ring, a pyridyl ring, an indole ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring; when Y represents an ethenylene group, an ethynylene group, an oxygen atom, a sulphur atom, a sulfonyl group, a sulfoxyde group or a nitrogen atom being optionally substituted then R2 represents a C<SUB>1-6 </SUB>alkyl group, a C<SUB>3-6 </SUB>cycloalkyl group, a C<SUB>1-2 </SUB>perhalogenated alkyl group, a C<SUB>1-3 </SUB>halogenated alkyl group, a naphthyl ring, a 5,6,7,8-tetrahydronaphthyl ring, a benzyl group, a phenyl ring, a pyridyl ring, an indole ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring. 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 diseases caused by abnormal activity of GSK3beta such as Alzheimer's disease.
申请公布号 AU2002212249(B2) 申请公布日期 2006.11.30
申请号 AU20020212249 申请日期 2001.08.31
申请人 发明人
分类号 A61K31/519;A61P3/04;A61P3/10;A61P9/00;A61P9/10;A61P17/14;A61P23/02;A61P25/00;A61P25/02;A61P25/16;A61P25/24;A61P25/28;A61P27/06;A61P35/00;A61P35/02;C07D487/04 主分类号 A61K31/519
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