939460-95-4Relevant academic research and scientific papers
Design and synthesis of potent, orally efficacious hydroxyethylamine derived β-Site amyloid precursor protein cleaving enzyme (Bace1) inhibitors
Dineen, Thomas A.,Weiss, Matthew M.,Williamson, Toni,Acton, Paul,Babu-Khan, Safura,Bartberger, Michael D.,Brown, James,Chen, Kui,Cheng, Yuan,Citron, Martin,Croghan, Michael D.,Dunn, Robert T.,Esmay, Joel,Graceffa, Russell F.,Harried, Scott S.,Hickman, Dean,Hitchcock, Stephen A.,Horne, Daniel B.,Huang, Hongbing,Imbeah-Ampiah, Ronke,Judd, Ted,Kaller, Matthew R.,Kreiman, Charles R.,La, Daniel S.,Li, Vivian,Lopez, Patricia,Louie, Steven,Monenschein, Holger,Nguyen, Thomas T.,Pennington, Lewis D.,San Miguel, Tisha,Sickmier, E. Allen,Vargas, Hugo M.,Wahl, Robert C.,Wen, Paul H.,Whittington, Douglas A.,Wood, Stephen,Xue, Qiufen,Yang, Bryant H.,Patel, Vinod F.,Zhong, Wenge
, p. 9025 - 9044 (2013/01/15)
We have previously shown that hydroxyethylamines can be potent inhibitors of the BACE1 enzyme and that the generation of BACE1 inhibitors with CYP 3A4 inhibitory activities in this scaffold affords compounds (e.g., 1) with sufficient bioavailability and p
BETA-SECRETASE MODULATORS AND METHODS OF USE
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Page/Page column 115, (2010/11/27)
The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I); wherein A, B, W, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula (I), methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula (I), or compositions including them, to a subject. The invention also comprises further embodiments of Formulas (II) and (III), intermediates and processes useful for the preparation of compounds of the invention.
