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 ,
Issue Information
روزنامه با شماره پیاپی سال 2000
Pages
4
From page
1467
To page
1470
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.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2000
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
790898
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