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    • 1. 发明申请
    • SUBSTITUTED HETEROARYLAMIDE DIAZEPINOPYRIMIDONE DERIVATIVES
    • 取代的异丁酰胺二氮丙啶衍生物
    • WO2009095792A3
    • 2009-10-08
    • PCT/IB2009000397
    • 2009-01-27
    • SANOFI AVENTISMITSUBISHI TANABE PHARMA CORPFAYOL AUDELOCHEAD ALISTAIRSAADY MOURADVACHE JULIENYAICHE PHILIPPE
    • FAYOL AUDELOCHEAD ALISTAIRSAADY MOURADVACHE JULIENYAICHE PHILIPPE
    • A61K31/519C07D403/04C07D487/04
    • C07D487/04C07D519/00
    • A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof, Formula (I): wherein: Y represents two hydrogen atoms, a sulphur 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 by one or two groups chosen from a C1-6 alkyl group, a hydroxyl group, a C1-6 alkoxy group, a C1-2 perhalogenated alkyl group or an amino group; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring, the ring being optionally substituted by a C1-6 alkyl group, a C1-6 alkoxy group or a halogen atom; R2 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; R3 represents a 4-15 membered heterocyclic group, this group being optionally substituted R4 represents a hydrogen atom, a C1-6 alkyl group optionally substituted by 1 to 4 substituents R5 represents a hydrogen atom or a C1-6 alkyl group; and n represents 0 to 3 and their therapeutic use.
    • 式(I)表示的嘧啶酮衍生物或其盐,或其溶剂化物或其水合物,式(I):其中:Y表示两个氢原子,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C1-3烷基取代的氮原子,硫原子,任选被一个或两个选自C 1-6烷基,羟基的基团取代的亚甲基 基团,C1-6烷氧基,C1-2全卤代烷基或氨基; R1表示2,3或4-吡啶环或2,4或5-嘧啶环,该环任选被C 1-6烷基,C 1-6烷氧基或卤素原子取代; R2表示氢原子,C1-6烷基或卤素原子; R3表示4-15元杂环基,该基团任选被取代,R 4表示氢原子,任选被1至4个取代基取代的C 1-6烷基表示氢原子或C 1-6烷基; n表示0〜3,其治疗用途。
    • 3. 发明申请
    • SUBSTITUTED HETEROARYL PYRIDOPYRIMIDONE DERIVATIVES
    • 取代的杂芳基吡啶并嘧啶酮衍生物
    • WO2008078196A2
    • 2008-07-03
    • PCT/IB2007004409
    • 2007-12-20
    • SANOFI AVENTISMITSUBISHI TANABE PHARMA CORPFAYOL AUDEGALLET THIERRYLOCHEAD ALISTAIRSAADY MOURADVERONIQUE CORINNEYAICHE PHILIPPE
    • FAYOL AUDEGALLET THIERRYLOCHEAD ALISTAIRSAADY MOURADVERONIQUE CORINNEYAICHE PHILIPPE
    • A01N43/90C07D239/70
    • 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 Ci-2 alkyl group and a hydrogen atom; Z represents a bond, an oxygen atom, a nitrogen atom, a sulphur atom, a methylene group optionally substituted by one or two groups chosen from a Ci-6 alkyl group, a hydroxyl group, a Ci-6 alkoxy group, a Ci_2 perhalogenated alkyl group or an amino group; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring; R2 represents an optionally substituted 4-15 membered heterocyclic group; R3 represents a hydrogen atom, a Ci-6 alkyl group or a halogen atom; R4 and R5 represent, each independently, a hydrogen atom, a Ci-6 alkyl group, optionally substituted by 1 to 4 substituents selected from a halogen atom, a phenyl group, a hydroxyl group or a Ci-6 alkoxy group; R6 represents a hydrogen atom, a Ci-6 alkyl group; a cycloalkyl group, or a halogen atom; R7 represents a hydrogen atom or a Ci-6 alkyl group; n represents 0 to 3; m represents 0 to 1; o represents 0 to 2; in the form of a free base or of an addition salt with an acid. 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,或其溶剂合物或其水合物: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代表键,氧原子,氮原子,硫原子,任选被选自C 1-6烷基基团,羟基,C 1-6烷氧基的组中选择一个或两个基团取代的亚甲基,C 1-2氟烷全卤代 烷基或氨基; R1代表2,3或4-吡啶环或2,4或5-嘧啶环; R2代表任选取代的4-15元杂环基; R 3代表氢原子,C 1-6烷基或卤素原子; R 4和R 5各自独立地表示氢原子,任选被1至4个选自卤素原子,苯基,羟基或C 1-6烷氧基的取代基取代的C 1-6烷基; R6代表氢原子,C1-6烷基; 环烷基或卤素原子; 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; 以游离碱或与酸加成盐的形式存在。 本发明还涉及包含其所述衍生物或其盐作为用于引起GSK3ß的异常活性,如阿尔茨海默病的神经变性疾病的预防性和/或治疗性治疗的有效成分的药物。
    • 7. 发明申请
    • ARYLAMIDE PYRIMIDONE DERIVATIVES FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
    • 用于治疗神经损伤性疾病的亚胺酰吡咯烷酮衍生物
    • WO2008155669A3
    • 2009-06-04
    • PCT/IB2008002446
    • 2008-05-14
    • SANOFI AVENTISMITSUBISHI TANABE PHARMA CORPCHEREZE NATHALIEGALLET THIERRYLOCHEAD ALISTAIRSAADY MOURADVERONIQUE CORINNEYAICHE PHILIPPE
    • CHEREZE NATHALIEGALLET THIERRYLOCHEAD ALISTAIRSAADY MOURADVERONIQUE CORINNEYAICHE PHILIPPE
    • C07D239/36A61K31/513A61P25/00
    • C07D239/36
    • A pyrimidone derivative represented by Formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: X represents two hydrogen atoms, a sulphur 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 by one or two groups chosen from a C1-6 alkyl group, a hydroxyl group, a C1-6 alkoxy group, a C1-2 perhalogenated alkyl group or an amino group; R1 represents a 2, 4 or 5-pyrimidine ring or a 4-pyridine ring, the ring being optionally substituted by a C1-6 alkyl group, a C1-6 alkoxy group or a halogen atom; R2 represents a benzene ring, a naphthalene ring or a benzyl group; the rings being optionally substituted by 1 to 4 substituents selected from a C1-6 alkyl group, C3-7 cycloalkyl group, a C3-7 cycloalkyl-C1-6 alkyl group, a halogen atom, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a hydroxyl group, an heteroaryl group optionally substituted by a C1-6 alkyl group, C3-7 cycloalkyl group, a C3-7 cycloalkyl-C1-6 alkyl group, C1-6 alkoxy group optionally substituted by a C3-5 cycloalkyl group, a C1-2 perhalogenated alkoxy group, a C1-6 alkylsulfonyl group, a nitro, a cyano, an amino, a C1-6 monoalkylamino group or a C2-12 dialkylamino group, an acetoxy group or an aminosulfonyl group; R3 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; R4 represents a hydrogen atom or a C1-6 alkyl group; R5 represents a hydrogen atom, a C1-6 alkyl group; R6 represents a hydrogen atom, a C1-6 alkyl group; R7 represents a hydrogen atom or a C1-6 alkyl group; n represents 0 to 3 and m represents 0 in the form of a free base or of an addition salt with an acid.
    • 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:X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,任选被一个或两个选自C 1-6烷基,羟基的基团取代的亚甲基 基团,C1-6烷氧基,C1-2全卤代烷基或氨基; R1表示2,4或5-嘧啶环或4-吡啶环,该环任选被C 1-6烷基,C 1-6烷氧基或卤素原子取代; R2表示苯环,萘环或苄基; 该环任选被1至4个选自C 1-6烷基,C 3-7环烷基,C 3-7环烷基-C 1-6烷基,卤素原子,C 1-2全卤代烷基, C 1-3卤代烷基,羟基,任选被C 1-6烷基取代的杂芳基,C 3-7环烷基,C 3-7环烷基-C 1-6烷基,任选被 C3-5环烷基,C1-2全卤代烷氧基,C1-6烷基磺酰基,硝基,氰基,氨基,C1-6单烷基氨基或C2-12二烷基氨基,乙酰氧基或 氨基磺酰基; R3表示氢原子,C1-6烷基或卤素原子; R4表示氢原子或C1-6烷基; R5表示氢原子,C1-6烷基; R6表示氢原子,C1-6烷基; R7表示氢原子或C1-6烷基; n表示0〜3,m表示0以游离碱或与酸形成的加成盐形式。