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    • 2. 发明公开
    • Arylamide pyrimidone compounds
    • Arylamid-Pyrimidon-Verbindungen
    • EP1992625A1
    • 2008-11-19
    • EP07290626.6
    • 2007-05-16
    • Sanofi-AventisMitsubishi Pharma Corporation
    • Lochead, Alistair.Saady, Mourad.Veronique, Corinne.Yaiche, Philippe.
    • C07D403/04C07D413/14A61K31/495A61P25/00
    • C07D403/04A61K9/0019A61K9/2018A61K9/4858C07D413/14Y02A50/411
    • 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 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 by one or two groups chosen from a C 1-6 alkyl group, a hydroxyl group, a C 1-6 alkoxy group, a C 1-2 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 C 1-6 alkyl group, a C 1-6 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 C 1-6 alkyl group, C 3-7 cycloalkyl group, a C 3-7 cycloalkyl-C 1-6 alkyl group, a halogen atom, a C 1-2 perhalogenated alkyl group, a C 1-3 halogenated alkyl group, a hydroxyl group, an heteroaryl group optionally substituted by a C 1-6 alkyl group, C 3-7 cycloalkyl group, a C 3-7 cycloalkyl-C 1-6 alkyl group, C 1-6 alkoxy group optionally substituted by a C 3-5 cycloalkyl group, a C 1-2 perhalogenated alkoxy group, a C 1-6 alkylsulfonyl group, a nitro, a cyano, an amino, a C 1-6 monoalkylamino group or a C 2-12 dialkylamino group, an acetoxy group or an aminosulfonyl group; 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; R6 represents a hydrogen atom, a C 1-6 alkyl group; R7 represents a hydrogen atom or a C 1-6 alkyl group; n represents 0 to 3 and m represents 1 in the form of a free base or of an addition salt with an acid.
    • 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X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C 1-3烷基取代的氮原子,硫原子,任选被一个或两个选自C 1-6烷基的基团取代的亚甲基, 羟基,C 1-6烷氧基,C 1-2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 基团,任选被C 3-5环烷基取代的C 1-6烷氧基,C 1-2全卤代烷氧基,C 1-6烷基磺酰基,硝基,氰基,氨基,C 1-6 单烷基氨基或C 2-12二烷基氨基,乙酰氧基或氨基磺酰基; R 3表示氢原子,C 1-6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,C 1-6烷基; R6表示氢原子,C 1-6烷基; R 7表示氢原子或C 1-6烷基; n表示0〜3,m表示1以游离碱或与酸的加成盐形式的1。