218138-60-4Relevant academic research and scientific papers
Factor xa inhibitors with aryl-amidines and derivatives, and prodrugs thereof
-
, (2008/06/13)
The present invention relates to a compound with aryl-amidines, particularly amidinoaryl-cyclopropanes, amidinoarylmethyl-pyrroles, amidinoaryl-benzenes, amidinoaryl-pyridines, or amindonoaryl-alanines, represented by formula (1), a pharmaceutically acceptable salt, a prodrug, a hydrate, a solvate or an isomer thereof, which are inhibitors of coagulation enzyme, factor Xa (FXa). The present invention also relates to a pharmaceutical composition containing the compound, and a method of using the same as an anticoagulant agent for treatment and prevention of thrombosis disorders.
Synthesis and SAR of benzamidine factor Xa inhibitors containing a vicinally-substituted heterocyclic core
Fevig, John M.,Pinto, Donald J.,Han, Qi,Quan, Mimi L.,Pruitt, James R.,Jacobson, Irina C.,Galemmo, Jr, Robert A.,Wang, Shuaige,Orwat, Michael J.,Bostrom, Lori L.,Knabb, Robert M.,Wong, Pancras C.,Lam, Patrick Y.S.,Wexler, Ruth R.
, p. 641 - 645 (2007/10/03)
The selective inhibition of coagulation factor Xa has emerged as an attractive strategy for the discovery of novel antithrombotic agents. Here we describe highly potent benzamidine factor Xa inhibitors based on a vicinally-substituted, heterocyclic core.
