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Structure-activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties |
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| Authors: | 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 |
| Affiliation: | aBristol-Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08543, USA bAlbany Molecular Research, Inc., 21 Corporate Circle, PO Box 15098, Albany, NY 12212, USA |
| 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. |
| Keywords: | Factor Xa Anthranilamide |
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