183308-17-0

Upstream product

• 74-88-4 methyl iodide 
• 183307-56-4 3-[(4-methyl-3,5,6-trifluoropyridin-2-yl)amino]benzonitrile 
• 183308-14-7 3-(4-methyl-3,5,6-trifluoropyridin-2-yl)methylaminobenzonitrile 
• 2237-30-1 m-cyanoaniline 
• 16297-14-6 2,3,5,6-tetrafluoro-4-methylpyridine 
• 183307-65-5 3-[6-(3-cyanophenyl)amino-3,5-difluoro-4-methylpyridin-2-yl(methylamino)]-benzonitrile 

Relevant academic research and scientific papers

Benzamidine derivatives and their use as anti-coagulants

This invention is directed to benzamidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.

Design, synthesis, and activity of 2,6-diphenoxypyridine-derived factor Xa inhibitors

A novel series of 2,6-diphenoxypyridines has been designed to inhibit factor Xa, a serine protease strategically located in the coagulation cascade. The evolution from the photochemically unstable bisamidine (Z,Z)- BABCH to potent bisamidine compounds with a pyridine heterocycle as the core scaffold has been achieved. The most potent compound in the series, 6h, has a K(i) for human factor Xa of 12 nM. The selectivity of 6h against bovine trypsin and human thrombin was greater than 90- and 1000-fold, respectively. Two proposed modes of binding of 6h to factor Xa are made based on the crystal structures of 6h by itself and of 6h bound to bovine trypsin.