selective BACE1 protease inhibitor
oral PD demonstrated on A_ in model
from optimization of prior ligand
Bioorg. Med. Chem. Lett., May 1, 2020
Amgen, Thousand Oaks, CA
“Compound 15”
1 min read
“Compound 15” is a BACE1 selective inhibitor with a fluoro-olefin replacement for an N-aryl amide without the liability of a potential aniline metabolite. The compound has good oral PK in rodents, which was likely challenging to obtain with the thioamidine core common to BACE1 inhibitors. As usual for Amgen there’s some pretty cool synthetic chemistry in the cited patents for this thiazine scaffold (ref. 17) that’s worth taking a look through.
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