388071-37-2Relevant academic research and scientific papers
Design of potent inhibitors of human β-secretase. Part 1
Freskos, John N.,Fobian, Yvette M.,Benson, Timothy E.,Bienkowski, Michael J.,Brown, David L.,Emmons, Thomas L.,Heintz, Robert,Laborde, Alice,McDonald, Joseph J.,Mischke, Brent V.,Molyneaux, John M.,Moon, Joseph B.,Mullins, Patrick B.,Bryan Prince,Paddock, Donna J.,Tomasselli, Alfredo G.,Winterrowd, Gregory
, p. 73 - 77 (2007/10/03)
We describe a novel series of potent inhibitors of human β-secretase. These compounds possess the hydroxyethyl amine transition state isostere. A 2.5 A crystal structure of inhibitor 32 bound to BACE is provided.
NOVEL GAMMA-LACTAMS AS BETA-SECRETASE INHIBITORS
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Page 54, (2008/06/13)
There is provided a series of novel substituted gamma-lactams of Formula (I) wherein R1, R2, R3, R4 and R5 are defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of aβ-peptide. The present invention is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
