202208-69-3Relevant articles and documents
Identification and initial structure-activity relationships of a novel class of nonpeptide inhibitors of blood coagulation factor Xa
Klein, Scott I.,Czekaj, Mark,Gardner, Charles J.,Guertin, Kevin R.,Cheney, Daniel L.,Spada, Alfred P.,Bolton, Scott A.,Brown, Karen,Colussi, Dennis,Heran, Christopher L.,Morgan, Suzanne R.,Leadley, Robert J.,Dunwiddie, Christopher T.,Perrone, Mark H.,Chu, Valeria
, p. 437 - 450 (1998)
The discovery and some of the basic structure-activity relationships of a series of novel nonpeptide inhibitors of blood coagulation Factor Xa is described. These inhibitors are functionalized β-alanines, exemplified by 2a. Docking experiments placing 2a in the active site of Factor Xa implied that the most expeditious route to enhancing in vitro potency was to modify the group occupying the S3 site of the enzyme. Increasing the hydrophobic contacts between the inhibitor and the enzyme in this region led to 8, which has served as the prototype for this series. In addition, an enantioselective synthesis of these substituted β-alanines was also developed.
Pyrrolobenzodiazepine pyridine carboxamides and derivatives as follicle-stimulating hormone receptor antagonists
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Page/Page column 34, (2010/11/25)
This invention provides pyrrolobenzodiazepine pyridine carboxamides selected from those of Formula (1), which act as follicle stimulating hormone receptor antagonists. The invention also provides pharmaceutical compositions and methods of treatment utilizing the compounds of Formulae (1) and (2).
