Structure–activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties

…, M Hadden, D Orton, AR Rendina, JM Luettgen…

Index: Corte, James R.; Fang, Tianan; Pinto, Donald J.P.; Han, Wei; Hu, Zilun; Jiang, Xiang-Jun; Li, Yun-Long; Gauuan, Jolicia F.; Hadden, Mark; Orton, Darren; Rendina, Alan R.; Luettgen, Joseph M.; Wong, Pancras C.; He, Kan; Morin, Paul E.; Chang, Chong-Hwan; Cheney, Daniel L.; Knabb, Robert M.; Wexler, Ruth R.; Lam, Patrick Y.S. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 9 p. 2845 - 2849

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Citation Number: 22

Abstract

Introduction of the phenyl piperidinone and phenyl pyridinone P4 moieties in the anthranilamide scaffold led to potent, selective, and orally bioavailable inhibitors of factor Xa. Anthranilamide 28 displayed comparable efficacy to apixaban in the rabbit arteriovenous-shunt (AV) thrombosis model.

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