140894-62-8Relevant articles and documents
Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors
Huang, Wenrong,Naughton, Mary Ann,Yang, Hua,Su, Ting,Dam, Suiko,Wong, Paul W.,Arfsten, Ann,Edwards, Susan,Sinha, Uma,Hollenbach, Stanley,Scarborough, Robert M.,Zhu, Bing-Yan
, p. 723 - 728 (2007/10/03)
A series of novel transition state factor Xa inhibitors containing a variety of lactam ring systems as central templates was synthesized in an expedient manner and allowed for a great deal of structural variability. Among them, the piperazinone-based inhibitors were found to be not only active against factor Xa but also selective over thrombin. Optimization of the P4 moiety yielded several potent compounds with IC50 below 1 nM against factor Xa.
Selective factor Xa inhibitors
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Example 1, (2008/06/13)
Novel compounds of formula I: including its pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The co
Synthesis of a homologous series of ketomethylene arginyl pseudodipeptides and application to low molecular weight hirudin-like thrombin inhibitors
DiMaio,Gibbs,Lefebvre,Konishi,Munn,Shi Yi Yue,Hornberger
, p. 3331 - 3341 (2007/10/02)
The design of low molecular weight thrombin inhibitors IIa-d (hirutonins) that bind concurrently with the enzyme's catalytic site and auxiliary 'anion- binding exosite' for fibrinogen recognition is reported. A practical synthesis of the required homologo