398147-95-0Relevant academic research and scientific papers
Acylaminoalkenylene-amide derivatives as NK1 and NK2 antagonists
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, (2008/06/13)
Compounds of formula I wherein R1, R1-R3, R4′, R4″ and R5are as defined in the description, have valuable pharmaceutical properties and are effective especially as NK1 and NK2 antagonists.
N-[(R,R)-(E)-1-(4-chloro-benzyl)-3-(2-oxo-azepan-3-ylcarbamoyl)-allyl]-N- methyl-3,5-bis-trifluoromethyl-benzamide: An orally active neurokinin NK1/NK2 antagonist
Gerspacher, Marc,Von Sprecher, Andreas,Mah, Robert,Anderson, Gary P.,Bertrand, Claude,Subramanian, Natarajan,Hauser, Kathleen,Ball, Howard A.
, p. 1467 - 1470 (2007/10/03)
The stereoselective synthesis of N-[(R,R)-(E)-1-(4-chloro-benzyl)-3-(2-oxo-azepan-3-ylcarbamoyl)-allyl]-N-methyl-3 ,5-bis-trifluoromethyl-benzamide (4) and its NK1 and NK2 receptor binding properties are reported. In addition the potent inhibitory effects in vivo on sar9-SP- and β-Ala-NKA-induced airway bronchoconstriction in guinea pigs are demonstrated. (C) 2000 Elsevier Science Ltd. All rights reserved.
