219518-95-3Relevant academic research and scientific papers
Antithrombotic agents
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, (2008/06/13)
This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a prodrug thereof, as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its
Structure-based design of potent, amidine-derived inhibitors of factor Xa: Evaluation of selectivity, anticoagulant activity, and antithrombotic activity
Wiley, Michael R.,Weir, Leonard C.,Briggs, Steven,Bryan, Nancy A.,Buben, John,Campbell, Charles,Chirgadze, Nickolay Y.,Conrad, Richard C.,Craft, Trelia J.,Ficorilli, James V.,Franciskovich, Jeffry B.,Froelich, Larry L.,Gifford-Moore, Donetta S.,Goodson Jr., Theodore,Herron, David K.,Klimkowski, Valentine J.,Kurz, Kenneth D.,Kyle, Jeffery A.,Masters, John J.,Ratz, Andrew M.,Milot, Guy,Shuman, Robert T.,Smith, Tommy,Smith, Gerald F.,Tebbe, Ann Louise,Tinsley, Jennifer M.,Towner, Richard D.,Wilson, Alexander,Yee, Ying K
, p. 883 - 899 (2007/10/03)
To enhance the potency of 1,2-dibenzamidobenzene-derived inhibitors of factor Xa (fXa), an amidine substituent was incorporated on one of the benzoyl side chains to interact with Asp189 in the S1 specificity pocket. Lead molecule I was docked into the act
