1257126-91-2Relevant academic research and scientific papers
Discovery of a series of potent, orally active α,α- disubstituted piperidine NK1 antagonists
Xiao, Dong,Wang, Cheng,Palani, Anandan,Tsui, Hon-Chung,Reichard, Gregory,Paliwal, Sunil,Shih, Neng-Yang,Aslanian, Robert,Duffy, Ruth,Lachowicz, Jean,Varty, Geoffrey,Morgan, Cynthia,Liu, Fei,Nomeir, Amin
, p. 6313 - 6315 (2010)
Modification of prototype NK1 antagonist 2 resulted in the synthesis of a series of simple amides 6 and retroamides 9. These compounds were shown to be potent and orally active NK1 antagonists.
And as the antagonist aminopyrrolidine deriv. NK1 aminopiperidine (by machine translation)
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Paragraph 0403-0414, (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.
