SUBSTITUTED 2-PYRIDINYL-6,7,8,9-TETRAHYDROPYRIMIDO1,2-APYRIMIDIN-4-ONE AND 7-PYRIDINYL-2,3-DIHYDROIMIDAZO1,2-APYRIMIDIN-5(1H)ONE DERIVATIVES

摘要

The invention relates to a pyrimidone derivative represented by formula (I) ora salt thereof wherein X represents two hydrogen atoms, a sulfur atom, anoxygen atom or a C~1-2 alkyl group and a hydrogen atom; Y represents a bond,an ethenylene group, an ethynylene group an oxygen atom, a sulfur atom, asulfonyl group, a sulfoxide group, a carbonyl group, a hydroxyiminomethylenegroup, a dioxolan group, a nitrogen atom being optionally substituted; or amethylene group optionally substituted; or a methylene group optionallysubstituted; R1 represents a 2, 3 or 4-pyridine ring optionally substituted;R2 may represent a C~1-6 alkyl group optionally; a C~3-6 cycloalkyl group, aC~1-4 alkythio group, a C~1-4 alkoxy group, a C~1-2 perhalogenated alkylgroup, a C~1-3 halogenated alkyl group, a phenylthio group, a benzyl group, abenzene ring, an indan ring, a 5,6,7,8-tetrahydronaphthalene ring, anaphthalene ring, a pyridine ring, a pyrrole ring, a thiophene ring, a furanring or an imidazole ring; R3 and R4 represent, each independently, a hydrogenatom, a C~1-6 alkyl group, a hydroxy group, a C~1-4 alkoxy group or a halogenatom; R5 represents a hydrogen atom, a C~1-6 alkyl group or a halogen atom;with the proviso that when R3 and R4 represent each a hydrogen atom then R5 isnot a hydrogen atom. The invention relates also to a medicament comprising thesaid derivative or a salt thereof as an active ingredient which is used forpreventive and/or therapeutic treatment of a neurodegenerative disease causedby abnormal activity of GSK3.beta. or GSK3.beta. and cdk5/p25, such asAlzheimer disease.