Identification of a novel 1′-[5-((3,5-Dichlorobenzoyl)methylamino)-3-(3,4-dichlorophenyl)-4-(methoxyimino)pentyl]-2-oxo-(1,4′-bipiperidine) as a Dual NK1/NK2 antagonist

Abstract A novel series of dual NK 1 /NK 2 receptor antagonists, based on the 2-oxo-(1,4′-bipiperidine) template, has been prepared. Compound 10R is a potent dual NK 1 /NK 2 antagonist and demonstrates excellent in vivo activity and good oral plasma levels in the dog.