878673-54-2Relevant academic research and scientific papers
Factor VIIa inhibitors: Gaining selectivity within the trypsin family
Shrader, William D.,Kolesnikov, Aleksandr,Burgess-Henry, Jana,Rai, Roopa,Hendrix, John,Hu, Huiyong,Torkelson, Steve,Ton, Tony,Young, Wendy B.,Katz, Bradley A.,Yu, Christine,Tang, Jie,Cabuslay, Ronnel,Sanford, Ellen,Janc, James W.,Sprengeler, Paul A.
, p. 1596 - 1600 (2007/10/03)
Within the trypsin family of coagulation proteases, obtaining highly selective inhibitors of factor VIIa has been challenging. We report a series of factor VIIa (fVIIa) inhibitors based on the 5-amidino-2-(2-hydroxy-biphenyl-3- yl)-benzimidazole (1) scaff
Factor VIIa inhibitors: Chemical optimization, preclinical pharmacokinetics, pharmacodynamics, and efficacy in an arterial baboon thrombosis model
Young, Wendy B.,Mordenti, Joyce,Torkelson, Steven,Shrader, William D.,Kolesnikov, Aleksandr,Rai, Roopa,Liu, Liang,Hu, Huiyong,Leahy, Ellen M.,Green, Michael J.,Sprengeler, Paul A.,Katz, Bradley A.,Yu, Christine,Janc, James W.,Elrod, Kyle C.,Marzec, Ulla M.,Hanson, Stephen R.
, p. 2037 - 2041 (2007/10/03)
Highly selective and potent factor VIIa-tissue factor (fVIIa · TF) complex inhibitors were generated through structure-based design. The pharmacokinetic properties of an optimized analog (9) were characterized in several preclinical species, demonstrating
Factor VIIa inhibitors: Improved pharmacokinetic parameters
Kolesnikov, Aleksandr,Rai, Roopa,Young, Wendy B.,Mordenti, Joyce,Liu, Liang,Torkelson, Steven,Shrader, William D.,Leahy, Ellen M.,Hu, Huiyong,Gjerstad, Erik,Janc, James,Katz, Bradley A.,Sprengeler, Paul A.
, p. 2243 - 2246 (2007/10/03)
Efforts to improve the potency and pharmacokinetic properties of small molecule factor VIIa inhibitors are described. Small structural modifications to existing leads allow the modulation of half-life and clearance, potentially making these compounds suitable candidates for drug development.
