发明授权
- 专利标题: Trifluoromethylsulfonamide gamma secretase inhibitor
- 专利标题(中): 三氟甲基磺酰胺γ分泌酶抑制剂
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申请号: US13145190申请日: 2010-01-29
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公开(公告)号: US08609897B2公开(公告)日: 2013-12-17
- 发明人: Matthew Daniels , Jed Hubbs , Thomas Miller
- 申请人: Matthew Daniels , Jed Hubbs , Thomas Miller
- 申请人地址: US NJ Rahway
- 专利权人: Merck Sharp & Dohme Corp.
- 当前专利权人: Merck Sharp & Dohme Corp.
- 当前专利权人地址: US NJ Rahway
- 代理商 Raynard Yuro; John Todaro; Susan Hess
- 国际申请: PCT/US2010/022560 WO 20100129
- 国际公布: WO2010/090954 WO 20100812
- 主分类号: C07C311/01
- IPC分类号: C07C311/01 ; A61K31/18
摘要:
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.
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