| 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<SUB>1-2 </SUB>alkyl group and a hydrogen atom; y represents a bond, an ethenylene group, an ethynylene group, an oxygen atom, a sulphur atom, a sulfonyl group, a sulfoxide group, a carbonyl group, a nitrogen atom being optionally; or a methylene group optionally substituted; R1 represents a pyrimidine group optionally substituted; R2 may represent a C<SUB>1-6 </SUB>alkyl group optionally substituted by a C<SUB>6,10 </SUB>aryloxy or a C<SUB>6,10 </SUB>arylamino 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 phenylthio group, a benzyl group, a benzene ring, an indan ring, a 5,6,7,8-tetrahydronaphthalene ring, a naphthalene ring, a pyridine ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring; R3 and R4 represents each independently a hydrogen atom, C<SUB>1-6 </SUB>alkyl group, a hydroxy group, a C<SUB>1-4 </SUB>alkoxy group or a halogen atom; R5 represents a hydrogen atom, a C<SUB>1-6 </SUB>alkyl 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 GSK3beta3 or GSK3beta3 and cdk5/p25, such as Alzheimer disease.
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