Cyclic urea derivatives as potent NK 1 selective antagonists

…, JH Schwerdt, S Shah, GA Reichard, JJ Piwinski…

Index: Shue, Ho-Jane; Chen, Xiao; Shih, Neng-Yang; Blythin, David J.; Paliwal, Sunil; Lin, Ling; Gu, Danlin; Schwerdt, John H.; Shah, Sapna; Reichard, Gregory A.; Piwinski, John J.; Duffy, Ruth A.; Lachowicz, Jean E.; Coffin, Vicki L.; Liu, Fei; Nomeir, Amin A.; Morgan, Cynthia A.; Varty, Geoffrey B. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 17 p. 3896 - 3899

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Citation Number: 45

Abstract

A series of novel five-and six-membered ring urea derivatives have been described as potent and selective NK1 receptor antagonists. Several compounds in this series exhibited good oral activity and brain penetration. Syntheses of these compounds are also described herein.