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    • 4. 发明公开
    • 치환된 비시클릭 피리미돈 유도체
    • 取代的双环吡啶酮衍生物
    • KR1020080070671A
    • 2008-07-30
    • KR1020087012084
    • 2006-11-21
    • 사노피미쓰비시 타나베 파마 코퍼레이션
    • 쉐헤즈,나탈리록헤드,알리스테어사디,무라드슬로윈스키,프랑크야이체,필리프
    • C07D471/04A61K31/519
    • C07D239/00C07D471/04
    • A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: Y represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Z represents a bond, an oxygen atom, a nitrogen atom substituted by a hydrogen atom or a C1-3 alkyl group, a sulphur atom, a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring, the ring being optionally substituted; R2 represents a benzene ring or a naphthalene ring; the rings being optionally substituted; R3 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; R4 represents a hydrogen atom or a C-1-6 alkyl group; R5 represents a hydrogen atom, a C1-6 alkyl group optionally substituted; R6 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; R7 represents a hydrogen atom or a C1-6 alkyl group; n represents 0 to 3; m represents 0 to 1; o represents 0 to 2. 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 GSK3F, such as Alzheimer disease.
    • 由式(I)表示的嘧啶酮衍生物或其盐或其溶剂合物或其水合物:其中:Y表示2个氢原子,硫原子,氧原子或C 1-2烷基和氢原子; Z表示键,氧原子,被氢原子或C1-3烷基取代的氮原子,硫原子,任选取代的亚甲基; R1表示2,3或4-吡啶环或2,4或5-嘧啶环,该环任选被取代; R2表示苯环或萘环; 所述环任选被取代; R3表示氢原子,C1-6烷基或卤素原子; R 4表示氢原子或C 1-6烷基; R5表示氢原子,任选取代的C 1-6烷基; R6表示氢原子,C1-6烷基或卤素原子; R7表示氢原子或C1-6烷基; n表示0〜3; m表示0〜1; o表示0至2.本发明还涉及包含所述衍生物或其盐作为活性成分的药物,其用于预防和/或治疗由GSK3F异常活动引起的神经变性疾病,例如阿尔茨海默病 。