Cyclobutane derivatives as potent NK1 selective antagonists

A series of novel cyclobutane derivatives as potent and selective NK1 receptor antagonists is described. Several compounds in this series exhibited high in vitro binding affinity (Ki ⩽ 1 nM), and potent inhibition of central NK1 receptor following oral administration. Syntheses of these compounds are also described herein.

Graphical abstractThe discovery of a novel series of cyclobutane derivatives 3 as potent and orally active NK1 selective antagonists is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide