GAMMA-SECRETASE MODULATORS
    3.
    发明申请
    GAMMA-SECRETASE MODULATORS 审中-公开
    GAMMA秘密调节器

    公开(公告)号:WO2014165263A1

    公开(公告)日:2014-10-09

    申请号:PCT/US2014/025016

    申请日:2014-03-12

    CPC classification number: C07D417/14 C07D487/04

    Abstract: There are provided, imer alia, compounds and methods for lowering total AB peptide production by inhibiting the catalytic activity of gamma-secretase. Since all of the major AB peptide variants, including the pathogenic AB42 as known in the art, are ultimately generated by gamma-secretase-mediated proteolysis of APP-C99 (i.e., the beta-secretase-mediated cleavage product of the amyloid protein precursor IAPPI), one approach to therapeutic intervention (e.g., intervention in Alzheimer's Disease, AD) relates to lowering total AB peptide production by inhibiting the catalytic activity of gamma-secretase.

    Abstract translation: 尤其提供通过抑制γ-分泌酶的催化活性降低总AB肽产生的化合物和方法。 由于所有主要的AB肽变体(包括本领域已知的致病性AB42)最终都通过APP- C99的γ-分泌酶介导的蛋白水解产生(即,β-分泌酶介导的淀粉样蛋白前体IAPPI的切割产物 ),治疗性干预的一种方法(例如,介入阿尔茨海默氏病,AD)涉及通过抑制γ-分泌酶的催化活性来降低总AB肽的产生。

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