8-Tetrahydropyran-2-yl Chromans: Highly Selective Beta-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitors

AA Thomas, KW Hunt, B Newhouse…

文献索引：ARRAY BIOPHARMA INC.; GENENTECH, INC.; COOK, Adam; GUNAWARDANA, Indrani, W.; HUESTIS, Malcolm; HUNT, Kevin, W.; KALLAN, Nicholas, C.; METCALF, Andrew, T.; NEWHOUSE, Brad; SIU, Michael; TANG, Tony, P.; THOMAS, Allen, A.; VOLGRAF, Matthew Patent: WO2012/71458 A1, 2012 ; Location in patent: Page/Page column 119-120 ;

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被引用次数: 5

摘要

A series of 2, 3, 4, 4a, 10, 10a-hexahydropyrano [3, 2-b] chromene analogs was developed that demonstrated high selectivity (> 2000-fold) for BACE1 vs Cathepsin D (CatD). Three different Asp-binding moieties were examined: spirocyclic acyl guanidines,