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Bunnage ME, Blagg J, Steele J, Owen DR, Allerton C, McElroy AB, Miller D, Ringer T, Butcher K, Beaumont K, Evans K et al: Discovery of potent & selective inhibitors of activated thrombin-activatable fibrinolysis inhibitor for the treatment of thrombosis. J Med Chem (2007) 50(24):6095-6103. •• Provides a full description of the program to convert a non-selective thiol lead into a selective, imidazole-based development candidate. This is a rare example of published phase I toleration data and human pharmacokinetic data in the research area of TAFI.
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Emayan K, Yuan S, Islam I, Hrvatin PM, West C, Chang Z, Bryant J, Chu K, Sukovich D, Buckman BO: 3-Phosphinoylpropionic acid inhibitors of thrombin activatable fibrinolysis inhibitor (TAFI) 1: Design, synthesis and biological activity. 232nd American Chemical Society National Meeting, San Francisco, CA, USA (2006):MEDI 397.
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Suzuki K, Muto Y, Fushihara K, Kanemoto K, Iida H, Sato E, Kikuchi C, Matsushima T, Kato E, Nomoto M, Yoshioka S et al: Enhancement of fibrinolysis by EF-6265 [(S)-7-amino-2-[[[(R)-2- methyl-1-(3-phenylpropanoylamino)propyl]hydroxyphosphinoyl] methyl]heptanoic acid], a specific inhibitor of plasma carboxypeptidase B. J Pharmacol Exp Ther (2004) 309(2):607-615. •• Provides evidence for the renal protective properties of EF-6265, the TAFIa inhibitor that is being researched by Meiji Seika Kaisha.
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Suzuki K, Muto Y, Fushihara K, Kanemoto K, Iida H, Sato E, Kikuchi C, Matsushima T, Kato E, Nomoto M, Yoshioka S et al: Enhancement of fibrinolysis by EF-6265 [(S)-7-amino-2-[[[(R)-2- methyl-1-(3-phenylpropanoylamino)propyl]hydroxyphosphinoyl] methyl]heptanoic acid], a specific inhibitor of plasma carboxypeptidase B. J Pharmacol Exp Ther (2004) 309(2):607-615. •• Provides evidence for the renal protective properties of EF-6265, the TAFIa inhibitor that is being researched by Meiji Seika Kaisha.
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