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) or a salt thereof: wherein: X represents hydrogen atoms, a sulphur atom, an oxygen atom or a CSUB1-2 /SUBalkyl 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 CSUB3-6 /SUBcycloalkyl group a CSUB1-4 /SUBalkyl group, a CSUB1-4 /SUBalkoxy 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 CSUB1-6 /SUBalkyl group, a CSUB3-6 /SUBcycloalkyl group, a CSUB1-4 /SUBalkylthio group, a CSUB1-4 /SUBalkoxy group, a CSUB1-2 /SUBperhalogenated alkyl group, a CSUB1-3 /SUBhalogenated 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 CSUB1-6 /SUBalkyl group, a CSUB3-6 /SUBcycloalkyl group, a CSUB1-2 /SUBperhalogenated alkyl group, a CSUB1-3 /SUBhalogenated 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.