Title of article :
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
Author/Authors :
Marc Gerspacher، نويسنده , , Andreas von Sprecher، نويسنده , , Robert Mah، نويسنده , , Gary P. Anderson، نويسنده , , Jean Claude Bertrand، نويسنده , , Natarajan Subramanian، نويسنده , , Kathleen Hauser، نويسنده , , Howard A. Ball، نويسنده ,
Abstract :
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.
