Trifluoromethylsulfonamide gamma secretase inhibitor
    11.
    发明授权
    Trifluoromethylsulfonamide gamma secretase inhibitor 有权
    三氟甲基磺酰胺γ分泌酶抑制剂

    公开(公告)号:US08609897B2

    公开(公告)日:2013-12-17

    申请号:US13145190

    申请日:2010-01-29

    CPC classification number: C07D233/42 C07C317/30 C07C2601/14 C07D295/185

    Abstract: The present invention is directed to a novel trifluoromethylsulfonamide derivative which inhibits the processing of APP by the putative γ-secretase and thus is useful in the treatment or prevention of Alzheimer's disease. This compound possesses favorable pharmacokinetic properties in higher species (rhesus) and thus can be dosed on an intermittent dosing regiment (e.g., once weekly). When dosed on such a regiment the compound exhibits significant and continuous Aβ lowering without the manifestation of Notch associated gastrointestinal toxicity for extended periods, e.g., 7 days. Pharmaceutical compositions and methods of use are also included.

    Abstract translation: 本发明涉及一种新的三氟甲基磺酰胺衍生物,其抑制由推定的γ-分泌酶处理APP,因此可用于治疗或预防阿尔茨海默氏病。 该化合物在较高种类(恒河猴)中具有有利的药代动力学性质,因此可以间歇给药剂量(例如每周一次)给药。 当给予这样一个团体时,该化合物显示出显着和连续的Abeta降低,而不延长Notch相关的胃肠道毒性的表现,例如7天。 还包括药物组合物和使用方法。

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