- Small molecule inhibitors of plasma kallikrein
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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
- 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
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- Factor VIIa inhibitors: Gaining selectivity within the trypsin family
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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
- 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.
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p. 1596 - 1600
(2007/10/03)
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- Factor VIIa inhibitors: Chemical optimization, preclinical pharmacokinetics, pharmacodynamics, and efficacy in an arterial baboon thrombosis model
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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
- 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.
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p. 2037 - 2041
(2007/10/03)
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- 2- [5- (5-carbamimidoyl-1H-heteroaryl)-6-hydroxybiphenyl-3-yl]-succinic acid derivatives as factor viia inhibitors
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The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders. Processes for preparing these inhibitors are also disclosed.
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