23053-35-2Relevant academic research and scientific papers
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.
Small molecule inhibitors of plasma kallikrein
Young, Wendy B.,Rai, Roopa,Shrader, William D.,Burgess-Henry, Jana,Hu, Huiyong,Elrod, Kyle C.,Sprengeler, Paul A.,Katz, Bradley A.,Sukbuntherng, Juthamas,Mordenti, Joyce
, p. 2034 - 2036 (2007/10/03)
Plasma kallikrein is a serine protease that is involved in pathways of inflammation, complement fixation, coagulation, and fibrinolysis. Herein, we describe the SAR and structural binding modes of a series of inhibitors of plasma kallikrein as well as the
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
Non-steroidal irreversible inhibitors of aromatase based on N-pentyl-3-phenylpyrrolidine-2,5-dione
Saeed,Khodarahmi,Fradgley,Smith,Nicholls,King,Ahmadi
, p. 265 - 277 (2007/10/03)
1-Pentyl-3-(3'-propynyloxyphenyl) pyrrolidine-2,5-dione (20), its 3-propynyl substituted derivative (18), with its corresponding 4'-substituted isomer (21), constitute the first of a new type of non-steroidal mechanism-based inactivators of aromatase with
