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    • 3. 发明授权
    • Substituted 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one and 7-pyrimidinyl-2,3-dihydroimidazo [1,2-a]pyrimidin-5(1H)one derivatives for neurodegenerative disorders
    • 取代的2-嘧啶基-6,7,8,9-四氢嘧啶并[1,2-a]嘧啶-4-酮和7-嘧啶基-2,3-二氢咪唑并[1,2-a]嘧啶-5(1H) 神经变性疾病的衍生物
    • US07388005B2
    • 2008-06-17
    • US10490136
    • 2002-09-19
    • Thierry GalletPatrick LardenoisAlistair LocheadSéverine MarguerieAlain NedelecMourad SaadyFranck SlowinskiPhilippe Yaiche
    • Thierry GalletPatrick LardenoisAlistair LocheadSéverine MarguerieAlain NedelecMourad SaadyFranck SlowinskiPhilippe Yaiche
    • A61K31/551A61K31/519C07D487/04A61P25/28
    • A61K31/519A61K31/551C07D487/04
    • The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein: X represents two hydrogen atoms, a sulphur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; y represents a bond, an ethenylene group, an ethynylene group, an oxygen atom, a sulphur atom, a sulfonyl group, a sulfoxide group, a carbonyl group, a nitrogen atom being optionally; or a methylene group optionally substituted; R1 represents a pyrimidine group optionally substituted; R2 may represent a C1-6 alkyl group optionally substituted by a C6,10 aryloxy or a C6,10 arylamino group; a C3-6 cycloalkyl group, a C1-4 alkylthio group, a C1-4 alkoxy group, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a phenylthio group, a benzyl group, a benzene ring, an indan ring, a 5,6,7,8-tetrahydronaphthalene ring, a naphthalene ring, a pyridine ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring; R3 and R4 represents each independently a hydrogen atom, C1-6 alkyl group, a hydroxy group, a C1-4 alkoxy group or a halogen atom; R5 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom. 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 GSK3β3 or GSK3β3 and cdk5/p25, such as Alzheimer disease.
    • 本发明涉及由式(I)表示的嘧啶酮衍生物或其盐,其中:X表示两个氢原子,硫原子,氧原子或C 1-12烷基和氢 原子; y表示键,亚乙烯基,亚乙炔基,氧原子,硫原子,磺酰基,亚砜基,羰基,任选的氮原子; 或任选取代的亚甲基; R1表示任选取代的嘧啶基团; R 2可以表示任选被C 6,10芳氧基或C 6,10芳基氨基取代的C 1-6烷基; C 3-6环烷基,C 1-4烷硫基,C 1-4烷氧基,C 1 -C 4烷氧基, 1-2个全卤代烷基,C 1-3卤代烷基,苯硫基,苄基,苯环,茚满环,5,6,7, 8-四氢萘环,萘环,吡啶环,吡咯环,噻吩环,呋喃环或咪唑环; R 3和R 4各自独立地表示氢原子,C 1-6烷基,羟基,C 1-4烷氧基或卤素原子; R5表示氢原子,C 1-6烷基或卤素原子。 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GSK3β3或GSK3β3和cdk5 / p25的异常活性引起的神经变性疾病,例如阿尔茨海默病 。