Novel trifluoromethylsulfonamide gamma secretase inhibitor

作者: Jed Hubbs , Matthew Daniels , Thomas Miller

DOI:

关键词: Derivative (chemistry)ChemistryOnce weeklyIntermittent dosingGastrointestinal toxicityGamma secretasePharmacologyPharmacokinetics

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

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