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    • 9. 发明申请
    • SUBSTITUTED BICYCLIC PYRIMIDONE DERIVATIVES
    • 取代的双环嘧啶酮衍生物
    • WO2007057790A2
    • 2007-05-24
    • PCT/IB2006004046
    • 2006-11-21
    • SANOFI AVENTISMITSUBISHI PHARMA CORPCHEREZE NATHALIELOCHEAD ALISTAIRSAADY MOURADSLOWINSKI FRANCKYAICHE PHILIPPE
    • CHEREZE NATHALIELOCHEAD ALISTAIRSAADY MOURADSLOWINSKI FRANCKYAICHE PHILIPPE
    • 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 C 1-2 alkyl group and a hydrogen atom; Z represents a bond, an oxygen atom, a nitrogen atom substituted by a hydrogen atom or a C 1- 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 C 1-6 alkyl group or a halogen atom; R4 represents a hydrogen atom or a C- 1-6 alkyl group; R5 represents a hydrogen atom, a C 1-6 alkyl group optionally substituted; R6 represents a hydrogen atom, a C 1-6 alkyl group or a halogen atom; R7 represents a hydrogen atom or a C 1-6 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 GSK3ß, such as Alzheimer disease.
    • 式(I)代表的嘧啶酮衍生物或其盐,或其溶剂化物或其水合物:其中:Y代表两个氢原子,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C 1〜3烷基取代的氮原子,硫原子,任选被取代的亚甲基; R1代表2,3或4-吡啶环或2,4或5-嘧啶环,所述环任选被取代; R2代表苯环或萘环; 该环任选被取代; R 3表示氢原子,C 1-6烷基或卤素原子; R4代表氢原子或C1-6烷基; R 5表示氢原子,任选取代的C 1-6烷基; R6代表氢原子,C1-6烷基或卤素原子; R 7代表氢原子或C 1-6烷基; n表示0至3; m代表0至1; o代表0至2.本发明还涉及一种药物,其包含所述衍生物或其盐作为活性成分,其用于预防和/或治疗由GSK3β的异常活性引起的神经退行性疾病,如阿尔茨海默病 。