- 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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