Discovery of the novel antithrombotic agent 5-chloro-N-({(5 S)-2-oxo-3-[4-(3-oxomorpholin-4-yl) phenyl]-1, 3-oxazolidin-5-yl} methyl) thiophene-2-carboxamide (BAY …

…, T Lampe, J Pernerstorfer, KH Schlemmer…

文献索引：Roehrig, Susanne; Straub, Alexander; Pohlmann, Jens; Lampe, Thomas; Pernerstorfer, Josef; Schlemmer, Karl-Heinz; Reinemer, Peter; Perzborn, Elisabeth Journal of Medicinal Chemistry, 2005 , vol. 48, # 19 p. 5900 - 5908

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被引用次数: 352

摘要

Despite recent progress in antithrombotic therapy, there is still an unmet medical need for safe and orally available anticoagulants. The coagulation enzyme Factor Xa (FXa) is a particularly promising target, and recent efforts in this field have focused on the identification of small-molecule inhibitors with good oral bioavailability. We identified oxazolidinone derivatives as a new class of potent FXa inhibitors. Lead optimization led to the discovery ...