molecules of the month


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

1 min read

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.

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