short T1/2 dual orexin 1/2 receptor antagonist
in clinical dev. for insomnia (Ph. II)
from ligand-based drug design
Bioorg. Med. Chem., Apr. 11, 2020
Taisho Pharmaceutical Co., Saitama, JP
ORN0829 is a dual inhibitor of orexins 1 and 2, designed to have a relatively short half life in humans for application in insomnia (to reduce side effects after waking up). Chemically it has an interesting chiral 1,3-oxazinane amide motif, which is resolved in their med. chem. route through an enzymatic resolution.