1146699-59-3Relevant articles and documents
Discovery and evaluation of BMS-708163, a potent, selective and orally bioavailable γ-secretase inhibitor
Gillman, Kevin W.,Starrett Jr., John E.,Parker, Michael F.,Xie, Kai,Bronson, Joanne J.,Marcin, Lawrence R.,McElhone, Kate E.,Bergstrom, Carl P.,Mate, Robert A.,Williams, Richard,Meredith, Jere E.,Burton, Catherine R.,Barten, Donna M.,Toyn, Jeremy H.,Roberts, Susan B.,Lentz, Kimberley A.,Houston, John G.,Zaczek, Robert,Albright, Charles F.,Decicco, Carl P.,MacOr, John E.,Olson, Richard E.
scheme or table, p. 120 - 124 (2010/12/20)
During the course of our research efforts to develop a potent and selective γ-secretase inhibitor for the treatment of Alzheimer's disease, we investigated a series of carboxamide-substituted sulfonamides. Optimization based on potency, Notch/amyloid-β precursor protein selectivity, and brain efficacy after oral dosing led to the discovery of 4 (BMS-708163). Compound 4 is a potent inhibitor of γ-secretase (Aβ40 IC50 = 0.30 nM), demonstrating a 193-fold selectivity against Notch. Oral administration of 4 significantly reduced Aβ40 levels for sustained periods in brain, plasma, and cerebrospinal fluid in rats and dogs.
Novel Alpha-(N-Sulfonamido)Acetamide Compound as an Inhibitor of Beta Amyloid Peptide Production
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Page/Page column 14-15, (2009/05/28)
The present invention provides a novel alpha-(N-sulfonamido)acetamide compound, its pharmaceutical composition, processes thereof and a method for the treatment of Alzheimer's disease and other conditions associated with β-amyloid peptide.