239462-58-9Relevant articles and documents
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.
Tetrahydroquinoline derivatives as antithrombotic agents
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Page 59, (2010/02/05)
This invention relates generally to tetracyclic tetrahydroquinoline compounds, and analogues thereof, and pharmaceutically acceptable salt forms thereof, which are selective inhibitors of serine protease enzymes, especially factor VIIa; pharmaceutical compositions containing the same; and methods of using the same as anticoagulant agents for modulation of the coagulation cascade.
