1032767-83-1Relevant academic research and scientific papers
Sulfamide as Zinc Binding Motif in Small Molecule Inhibitors of Activated Thrombin Activatable Fibrinolysis Inhibitor (TAFIa)
Halland, Nis,Czech, J?rg,Czechtizky, Werngard,Evers, Andreas,Follmann, Markus,Kohlmann, Markus,Schreuder, Herman A.,Kallus, Christopher
, p. 9567 - 9573 (2016/11/11)
Previously disclosed TAFIa inhibitors having a urea zinc-binding motif were used as the starting point for the development of a novel class of highly potent inhibitors having a sulfamide zinc-binding motif. High-resolution X-ray cocrystal structures were used to optimize the structures and reveal a highly unusual sulfamide configuration. A selected sulfamide was profiled in vitro and in vivo and displayed a promising ADMET profile.
UREA AND SULFAMIDE DERIVATIVES AS INHIBITORS OF TAFIa
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Page/Page column 69, (2010/03/02)
The invention relates to compounds of the formula I as defined herein, which are inhibitors of activated thrombin-activatable fibrinolysis inhibitor. The compounds of the formula I are suitable for manufacturing medicaments for the prophylaxis, secondary prevention and therapy of one or more disorders which are associated with thromboses, embolisms, hypercoagulability or fibrotic changes.
