1233508-72-9Relevant academic research and scientific papers
Macrocyclic BACE inhibitors: Optimization of a micromolar hit to nanomolar leads
Huang, Yifang,Strobel, Eric D.,Ho, Chih Y.,Reynolds, Charles H.,Conway, Kelly A.,Piesvaux, Jennifer A.,Brenneman, Douglas E.,Yohrling, George J.,Moore Arnold,Rosenthal, Daniel,Alexander, Richard S.,Tounge, Brett A.,Mercken, Marc,Vandermeeren, Marc,Parker, Michael H.,Reitz, Allen B.,Baxter, Ellen W.
scheme or table, p. 3158 - 3160 (2010/09/18)
We have identified macrocyclic inhibitors of the aspartic protease BACE, implicated in the etiology of Alzheimer's disease. An X-ray structure of screening hit 1 in the BACE active site revealed a hairpin conformation suggesting that constrained macrocycl
MACROCYCLE DERIVATIVES USEFUL AS INHIBITORS OF beta-SECRETASE (BACE)
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Page/Page column 19, (2010/11/28)
The present invention is directed to macrocycle derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of β-secretase, also known as β-site cleaving enzyme and BACE, BACE1, Asp2 and memapsin2.
