8-Substituted-6,7,8,9-tetrahydropyrimido [1,2-a] pyrimidin-4-one derivatives.
    55.
    发明授权
    8-Substituted-6,7,8,9-tetrahydropyrimido [1,2-a] pyrimidin-4-one derivatives. 失效
    8-取代的6,7,8,9-四氢嘧啶并[1,2-a]嘧啶-4-酮衍生物。

    公开(公告)号:US07247638B2

    公开(公告)日:2007-07-24

    申请号:US11225218

    申请日:2005-09-13

    IPC分类号: C07D487/04 A61K31/519

    CPC分类号: A61K31/519 C07D487/04

    摘要: The invention relates to substituted-pyrimidone derivatives represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, R4, R5, n, p and q are as defined herein. 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 GSK3β, such as Alzheimer's disease.

    摘要翻译: 本发明涉及由式(I)表示的取代嘧啶酮衍生物或其盐:其中X,Y,R 1,R 2,R 3,R 4,R 5,n,p和q如本文所定义。 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GSK3β如阿尔茨海默病异常活动引起的神经变性疾病。

    1-[alkyl], 1-[(heteroaryl)alkyl] and 1-[(aryl)alkyl]-7pyridinyl-imidazo[1,2-alpha]pyrimidin-5(1H)-one derivatives

    公开(公告)号:US07067521B2

    公开(公告)日:2006-06-27

    申请号:US10362857

    申请日:2001-08-31

    IPC分类号: A61K31/519

    CPC分类号: A61K31/519 C07D487/04

    摘要: The invention relates to an imidazo[1,2-a]pyrimidone derivative represented by formula (1) or a salt thereof, wherein: X represents a bond, an ethenylene group, and ethenylene group, a methylene group optionally substituted by one or two groups selected from a C1-6 alkyl group, a hydroxy group and a C1-4 alkoxy group; a carbonyl group, an oxygen atom, a sulfur atom, a sulfonyl group, a sulfoxide group or a nitrogen atom being optionally substituted by a C1-6 alkyl group; R1 represents a 2,3 or 4-pyridyl group optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or a halogen atom; R2 represents a C1-6 alkyl group, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a benzyl group, a phenyl ring, a naphthyl ring, 5,6,7,8-tetrahydronaphthyl ring, a pyridyl ring, an indole ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring, the benzyl group and the rings being optionally substituted by 1 to 4 substituents selected from a C1-6 alkyl group, a phenyl ring, a halogen atom, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a hydroxyl group, a C1-4 alkoxy group, a nitro, a cyano, an amino, a C1-6 monoalkylamino group or a C2-10 dialkylamino group; and n represents 0 to 3. 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 GSK3β, such as Alzheimer disease.