Pyrrolidine and piperidine derivates as nk1 antagonists

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 211/60 (2006.01) A61K 31/4025 (2006.01) A61K 31/407 (2006.01) A61K 31/438 (2006.01) A61K 31/445 (2006.01) A61P 1/08 (2006.01) A61P 11/00 (2006.01) A61P 25/06 (2006.01) A61P 25/24 (2006.01) C07D 207/14 (2006.01) C07D 211/28 (2006.01) C07D 211/32 (2006.01) C07D 211/42 (2006.01) C07D 211/56 (2006.01) C07D 211/72 (2006.01) C07D 211/76 (2006.01) C07D 401/04 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 403/04 (2006.01) C07D 413/12 (2006.01) C07D 471/10 (2006.01) C07D 487/10 (2006.01) C07D 491/1

Patent

CA 2470476

A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 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.

L'invention concerne un antagoniste de NK¿1? Ayant la formule (I), dans laquelle Ar?1¿ et Ar?2¿ représentent facultativement phényle ou hétéroaryle facultativement substitués, X?1¿ représente une liaison éther, thio ou imino, R?4¿ et R?5¿ ne représentent pas tous les deux H ou alkyle, et les variables restantes sont telles que définies dans la description, utile pour traiter un certain nombre de troubles notamment le vomissement, la dépression, l'angoisse et la toux. L'invention concerne également des compositions pharmaceutiques, des méthodes de traitement ainsi que des combinaisons avec d'autres agents.

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