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

被引：30

作者：

Corte, James R. ^{[1
]}

Fang, Tianan ^{[1
]}

Pinto, Donald J. P. ^{[1
]}

Han, Wei ^{[1
]}

Hu, Zilun ^{[1
]}

Jiang, Xiang-Jun ^{[1
]}

Li, Yun-Long ^{[1
]}

Gauuan, Jolicia F. ^{[2
]}

Hadden, Mark ^{[2
]}

Orton, Darren ^{[2
]}

Rendina, Alan R. ^{[1
]}

Luettgen, Joseph M. ^{[1
]}

Wong, Pancras C. ^{[1
]}

He, Kan ^{[1
]}

Morin, Paul E. ^{[1
]}

Chang, Chong-Hwan ^{[1
]}

Cheney, Daniel L. ^{[1
]}

Knabb, Robert M. ^{[1
]}

Wexler, Ruth R. ^{[1
]}

Lam, Patrick Y. S. ^{[1
]}

机构：

[1] Bristol Myers Squibb Res & Dev, Princeton, NJ 08543 USA

[2] Albany Mol Res Inc, Albany, NY 12212 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 09期

关键词：

factor Xa; anthranilamide;

D O I：

10.1016/j.bmcl.2008.03.092

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (c) 2008 Elsevier Ltd. All rights reserved.

引用

页码：2845 / 2849

页数：5

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