Piperidine-derived γ-secretase modulators

…, GMP Giblin, I Hussain, J Musgrave, A Naylor…

文献索引：Hall, Adrian; Elliott, Richard L.; Giblin, Gerard M.P.; Hussain, Ishrut; Musgrave, James; Naylor, Alan; Sasse, Rosemary; Smith, Beverley Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 3 p. 1306 - 1311

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被引用次数: 39

摘要

This Letter details the SAR of a novel series of piperidine-derived γ-secretase modulators. Compound 10h was found to be a potent modulator in vitro, which on further profiling, was found to decrease Aβ42, increase Aβ38 and have no effect on Aβ40 levels. Furthermore, 10h demonstrated excellent pharmacokinetic parameters in the mouse, rat and dog in addition to good CNS penetration in the mouse.