molecules of the month

“Compound 15”

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

Chemical structure of the "Compound 15" BACE1 selective inhibitor
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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