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 <or=1 nM), and potent inhibition of central NK1 receptor following oral administration. Syntheses of these compounds are also described herein.
Wrobleski
Michelle Laci
ML
Chemical Research Department, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
Reichard
Gregory A
GA
Paliwal
Sunil
S
Shah
Sapna
S
Tsui
Hon-Chung
HC
Duffy
Ruth A
RA
Lachowicz
Jean E
JE
Morgan
Cynthia A
CA
Varty
Geoffrey B
GB
Shih
Neng-Yang
NY