878673-54-2Relevant articles and documents
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: 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.