431048-92-9Relevant academic research and scientific papers
Discovery of nonbenzamidine factor VIIa inhibitors using a biaryl acid scaffold
Bolton, Scott A.,Sutton, James C.,Anumula, Rushith,Bisacchi, Gregory S.,Jacobson, Bruce,Slusarchyk, William A.,Treuner, Uwe D.,Wu, Shung C.,Zhao, Guohua,Pi, Zulan,Sheriff, Steven,Smirk, Rebecca A.,Bisaha, Sharon,Cheney, Daniel L.,Wei, Anzhi,Schumacher, William A.,Hartl, Karen S.,Liu, Eddie,Zahler, Robert,Seiler, Steven M.
, p. 5239 - 5243 (2013/09/12)
In this Letter, we describe the synthesis of several nonamidine analogs of biaryl acid factor VIIa inhibitor 1 containing weakly basic or nonbasic P1 groups. 2-Aminoisoquinoline was found to be an excellent surrogate for the benzamidine group (compound 2) wherein potent inhibition of factor VIIa is maintained relative to most other related serine proteases. In an unanticipated result, the m-benzamide P1 (compounds 21a and 21b) proved to be a viable benzamidine replacement, albeit with a 20-40 fold loss in potency against factor VIIa.
Amidino derivatives and drugs containing the same as the active ingredient
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Page column 411, (2010/01/30)
The novel amidino derivatives of the formula (I): wherein all the symbols are as in specification defined; have an inhibitory activity of a blood coagulation factor VIIa and are useful for treatment and/or prevention of several angiopathy caused by enhanc
