SUBSTITUTED 8'-PYRI(MI)DINYL-DIHYDROSPIRO-[CYCLOALKYLAMINE]-PYRIMIDO[1,2-a]PYRIMIDIN-6-ONE DERIVATIVES
    3.
    发明申请
    SUBSTITUTED 8'-PYRI(MI)DINYL-DIHYDROSPIRO-[CYCLOALKYLAMINE]-PYRIMIDO[1,2-a]PYRIMIDIN-6-ONE DERIVATIVES 失效
    取代的8'-哌嗪(MI)十二烷基二 - [环己基] - 吡咯并[1,2-a]吡啶-6-酮衍生物

    公开(公告)号:US20080081820A1

    公开(公告)日:2008-04-03

    申请号:US11866687

    申请日:2007-10-03

    摘要: The invention relates to a dihydrospiro-[cycloalkylamine]-pyrimidone derivative represented by formula (I) or a salt thereof: wherein: X represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Y represents a bond, a carbonyl group, a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring, the ring being optionally substituted; R2 represents a benzene ring or a naphthalene ring; the rings being optionally substituted; R3 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; R4 represents a hydrogen atom, a C1-4 alkoxy carbonyl group, a C1-5 alkyl group optionally substituted; o and m represent 1 to 2; n represents 0 to 3; p represents 0 to 2; and q represents 0 to 2. 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.

    摘要翻译: 本发明涉及由式(I)表示的二氢螺环 - [环烷基胺] - 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 1-2 - 烷基和氢原子; Y表示键,羰基,任选取代的亚甲基; R1表示2,3或4-吡啶环或2,4或5-嘧啶环,该环任选被取代; R2表示苯环或萘环; 所述环任选被取代; R 3表示氢原子,C 1-6烷基或卤素原子; R4表示氢原子,C 1-4烷氧基羰基,任选取代的C 1-5烷基; o和m表示1〜2; n表示0〜3; p表示0〜2; 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,所述活性成分用于预防和/或治疗由GSK3β如异常活动引起的神经变性疾病,例如阿尔茨海默氏症 疾病。