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Cyclobutane derivatives as potent NK1 selective antagonists. 2006
Michelle Laci Wrobleski, and
Gregory A Reichard, and
Sunil Paliwal, and
Sapna Shah, and
Hon-Chung Tsui, and
Ruth A Duffy, and
Jean E Lachowicz, and
Cynthia A Morgan, and
Geoffrey B Varty, and
Neng-Yang Shih
Chemical Research Department, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
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.
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