530439-89-5Relevant academic research and scientific papers
And as the antagonist aminopyrrolidine deriv. NK1 aminopiperidine (by machine translation)
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, (2016/10/08)
A NK 1 antagonist having the formula (I), wherein Ar 1 and Ar 2 are optionally substituted phenyl or heteroaryl, X 1 is an ether, thio or imino linkage, R 4 and R 5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.
Discovery of a novel, potent and orally active series of γ-lactams as selective NK1 antagonists
Paliwal, Sunil,Reichard, Gregory A.,Shah, Sapna,Wrobleski, Michelle Laci,Wang, Cheng,Stengone, Carmine,Tsui, Hon-Chung,Xiao, Dong,Duffy, Ruth A.,Lachowicz, Jean E.,Nomeir, Amin A.,Varty, Geoffrey B.,Shih, Neng-Yang
scheme or table, p. 4168 - 4171 (2009/04/16)
Strategic replacement of the nitrogen of the lead compound 1 in the original cyclic urea series with a carbon resulted in the discovery of a novel, potent and orally more efficacious γ-lactam series of selective NK1 antagonists. Optimization of the lactam series culminated in the identification of compounds with high binding affinity and excellent oral CNS activity.
