218301-61-2Relevant academic research and scientific papers
Nonbenzamidine isoxazoline derivatives as factor Xa inhibitors
Quan, Mimi L.,Ellis, Christopher D.,He, Ming Y.,Liauw, Ann Y.,Lam, Patrick Y. S.,Rossi, Karen A.,Knabb, Robert M.,Luettgen, Joseph M.,Wright, Matthew R.,Wong, Pancras C.,Wexler, Ruth R.
, p. 1023 - 1028 (2007/10/03)
Factor Xa (fXa) is an important serine protease in the blood coagulation cascade. Inhibition of fXa has emerged as an attractive target for potential therapeutic applications in the treatments of both arterial and venous thrombosis. Herein, we describe a series of non-benzamidine isoxazoline derivatives as fXa inhibitors. The chloroaniline group was found to be the most potent benzamidine mimic in this series. Chloroaniline 1 (ST368) has a Ki value of 1.5 nM against fXa and is highly selective for fXa relative to thrombin and trypsin.
Guanidine mimics as factor Xa inhibitors
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Page column 105, (2010/02/04)
The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings D—E represent guanidine mimics, which are useful as inhibitors of factor Xa.
