首页> 外国专利> SUBSTITUTED 8'-PYRIDINYL-DIHYDROSPIRO-CYCLOALKYL-PYRIMIDO 1,2-A PYRIMIDIN-6-ONE AND 8'-PYRIMIDINYL-DIHYDROSPIRO-CYCLOALKYL-PYRIMIDO 1,2-A PYRIMIDIN-6-ONE DERIVATIVES AND THEIR USE AGAINST NEUROGENERATIVE DISEASES

SUBSTITUTED 8'-PYRIDINYL-DIHYDROSPIRO-CYCLOALKYL-PYRIMIDO 1,2-A PYRIMIDIN-6-ONE AND 8'-PYRIMIDINYL-DIHYDROSPIRO-CYCLOALKYL-PYRIMIDO 1,2-A PYRIMIDIN-6-ONE DERIVATIVES AND THEIR USE AGAINST NEUROGENERATIVE DISEASES

机译:取代的8'-吡啶基-二吡咯并[环烷基]-嘧啶基[1,2-A]吡咯烷6-1和8'-吡咯基-二羟基吡咯并[[环烷基]-吡咯并酮[1,2-A]吡喃基-6-1衍生物及其在神经发生性疾病中的用途

摘要

The invention relates to a dihydrospiro-ÄcycloalkylÜ-pyrimidone derivative represented by formula (I) or a salt thereof: CHEM 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; m represents 1 to 4 n represent 0 to 3 p represents 0 to 2 q represents 0 to 2, p+ q being inferior to 4. ??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 GSK3 beta , such as Alzheimer disease.
机译:本发明涉及由式(I)表示的二氢螺-β-环烷基-嘧啶酮衍生物或其盐:其中:X代表两个氢原子,一个硫原子,一个氧原子或一个C1-2烷基和一个氢原子; Y表示键,羰基,任选取代的亚甲基; R1代表2、3或4-吡啶环或2、4或5-嘧啶环,该环是任选取代的; R 2表示苯环或萘环。环被任选取代; R 3表示氢原子,碳数1〜6的烷基或卤素原子。 m代表1至4 n代表0至3 p代表0至2 q代表0至2,p + q劣于4。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。用于预防和/或治疗由GSK3β异常活性引起的神经退行性疾病的成分,例如阿尔茨海默氏病。

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