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
M. Gerspacher et al., 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, BIOORG MED, 10(13), 2000, pp. 1467-1470
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 sar(9)-SP- and -beta-Ala-NKA-induc
ed airway bronchoconstriction in guinea pigs are demonstrated. (C) 2000 Els
evier Science Ltd. All rights reserved.