Novel lactam NK1 antagonists with anti-emetic activity

A series of 4,4-disubstituted cyclohexylamine NK1 antagonists containing a lactam ring is described. The compounds are brain penetrant and activity is demonstrated in a ferret emesis model.

The discovery of potent NK1 antagonists such as 8a is reported. Compound 8a displays good activity in a ferret emesis model.Figure optionsDownload as PowerPoint slide