- Identification of a nonpeptidic and conformationally restricted bradykinin B1 receptor antagonist with anti-inflammatory activity
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We report the discovery of chroman 28, a potent and selective antagonist of human, nonhuman primate, rat, and rabbit bradykinin B1 receptors (0.4-17 nM). At 90 mg/kg s.c., 28 decreased plasma extravasation in two rodent models of inflammation. A novel met
- D'Amico, Derin C.,Aya, Toshi,Human, Jason,Fotsch, Christopher,Chen, Jian Jeffrey,Biswas, Kaustav,Riahi, Bobby,Norman, Mark H.,Willoughby, Christopher A.,Hungate, Randall,Reider, Paul J.,Biddlecome, Gloria,Lester-Zeiner, Dianna,Van Staden, Carlo,Johnson, Eileen,Kamassah, Augustus,Arik, Leyla,Wang, Judy,Viswanadhan, Vellarkad N.,Groneberg, Robert D.,Zhan, James,Suzuki, Hideo,Toro, Andras,Mareska, David A.,Clarke, David E.,Harvey, Darren M.,Burgess, Laurence E.,Laird, Ellen R.,Askew, Benny,Ng, Gordon
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p. 607 - 610
(2007/10/03)
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- TRIAZOLES AND THEIR USE AS BRADYKININ B1 RECEPTOR ANTAGONISTS
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Compounds of Formula (I): are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
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Page/Page column 50
(2008/06/13)
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