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    • 6. 发明申请
    • KYNURENINE-AMINOTRANSFERASE INHIBITORS
    • KUNURENINE-AMINOTRANSFERASE抑制剂
    • WO2009064836A3
    • 2009-07-02
    • PCT/US2008083321
    • 2008-11-13
    • UNIV MARYLANDMITSUBISHI TANABE PHARMA CORPSCHWARCZ ROBERTKAJII YASUSHIONO SHIN-ICHIRO
    • SCHWARCZ ROBERTKAJII YASUSHIONO SHIN-ICHIRO
    • C07D401/10C07D401/06C07D403/02
    • C07D498/06C07D215/56C07D401/04
    • Compounds of formula (I) : prodrug derivatives and/or pharmaceutically acceptable salt thereof, selectively inhibit the enzyme kynurenine aminotransferase, thereby reducing the synthesis of kynurenic acid. The compounds are used for the treatment of psychiatric and neurological diseases which benefit from an increase in glutamatergic and/or cholinergic neurotransmission, such as schizophrenia, depression, bipolar illness, anxiety and Alzheimer's disease. Furthermore, the compounds of the invention are useful for stimulating attention, memory and other cognitive processes in normal individuals of any age, including children, adolescents and the elderly. Additionally, the compounds of the invention are also useful for treatment of patients suffering from malaria by preventing parasite gametogenesis and fertility based on reduction of xanthurenic acid formation from its bioprecursor 3 -hydroxy kynurenine.
    • 式(I)化合物:前药衍生物和/或其药学上可接受的盐选择性地抑制犬尿氨酸转氨酶,由此减少犬尿烯酸的合成。 该化合物用于治疗精神病和神经疾病,这些疾病受益于谷氨酸能和/或胆碱能神经传递的增加,如精神分裂症,抑郁症,双相情感障碍,焦虑和阿尔茨海默病。 此外,本发明化合物可用于刺激任何年龄的正常个体,包括儿童,青少年和老年人的注意力,记忆力和其他认知过程。 此外,本发明化合物还可用于通过防止寄生虫配子发生和基于从其生物前体3-羟基犬尿氨酸形成黄原酸形成的可育性来治疗患有疟疾的患者。
    • 9. 发明申请
    • HETEROARYLAMIDE PYRIMIDONE COMPOUNDS
    • 异丁酰胺吡咯烷酮化合物
    • WO2008155668A3
    • 2009-03-12
    • PCT/IB2008002445
    • 2008-05-14
    • SANOFI AVENTISMITSUBISHI TANABE PHARMA CORPLOCHEAD ALISTAIRSAADY MOURADVERONIQUE CORINNEYAICHE PHILIPPE
    • LOCHEAD ALISTAIRSAADY MOURADVERONIQUE CORINNEYAICHE PHILIPPE
    • C07D401/12A61K31/513A61P3/00A61P25/00C07D239/36C07D403/12C07D405/12C07D409/12
    • C07D403/12C07D239/36C07D401/14C07D405/14C07D409/14C07D471/04
    • A pyrimidone derivative represented by Formula (I) or a salt, solvate 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 4-15 membered heterocyclic, group, this group being optionally substituted by 1 to 4 substituents as defined in claim 1; 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; and n represents 0 to 3 and m represents 1 in the form of a free base or of an addition salt with an acid. and a medicament containing the same as a GSKk inhibitor.
    • 由式(I)表示的嘧啶酮衍生物或其盐,溶剂合物或水合物,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4-15元杂环基,该基团任选被1至4个如权利要求1所定义的取代基取代; 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1以游离碱或与酸形成的加成盐的形式。 和含有与GSKk抑制剂相同的药物。
    • 10. 发明申请
    • ARYLAMIDE PYRIMIDONE COMPOUNDS
    • ARYLAMIDE PYRIMIDONE化合物
    • WO2008155670A2
    • 2008-12-24
    • PCT/IB2008002458
    • 2008-05-14
    • SANOFI AVENTISMITSUBISHI TANABE PHARMA CORPLOCHEAD ALISTAIRSAADY MOURADVERONIQUE CORINNEYAICHE PHILIPPE
    • LOCHEAD ALISTAIRSAADY MOURADVERONIQUE CORINNEYAICHE PHILIPPE
    • C07D403/04A61K9/0019A61K9/2018A61K9/4858C07D413/14
    • 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 C1-6alkyl 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 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1以游离碱或与酸的加成盐形式的1。