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

Article abstract of DOI:10.1016/S0960-894X(00)00260-2

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.