227021-83-2Relevant academic research and scientific papers
Selective and orally bioavailable phenylglycine tissue factor/factor VIIa inhibitors
Zbinden, Katrin Groebke,Obst-Sander, Ulrike,Hilpert, Kurt,Kuehne, Holger,Banner, David W.,Boehm, Hans-Joachim,Stahl, Martin,Ackermann, Jean,Alig, Leo,Weber, Lutz,Wessel, Hans Peter,Riederer, Markus A.,Tschopp, Thomas B.,Lave, Thierry
, p. 5344 - 5352 (2007/10/03)
We describe the structure-based design and synthesis of highly potent, orally bioavailable tissue factor/factor VIIa inhibitors which interfere with the coagulation cascade by selective inhibition of the extrinsic pathway.
Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors
Groebke Zbinden, Katrin,Banner, David W.,Ackermann, Jean,D'Arcy, Allan,Kirchhofer, Daniel,Ji, Yu-Hua,Tschopp, Thomas B.,Wallbaum, Sabine,Weber, Lutz
, p. 817 - 822 (2007/10/03)
Proof of concept experiments have shown that tissue factor/factor VIIa inhibitors have antithrombotic activity without enhancing bleeding propensity. Starting from lead compounds generated by a biased combinatorial approach, phenylglycine amide tissue fac
N-(4- carbamimidoyl-phenyl) -glycine derivatives
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, (2008/06/13)
The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula: wherein R1, E, X1 to X4 and G1 and G2 are as defined in the description and the claims, as well as hydrates or solvates and physiologically usable salts thereof.
N-(4-carb-amimidophenyl)glycineamide derivatives
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, (2008/06/13)
N-(4-carbamimidophenylamino) phenylglycineamide derivative compounds having the formula: in which E, g1, g2, Q, R and X1 to X4 are each as defined in the description, and hydrates or solvates and physiologically acceptable salts thereof can be used as inhibitors of the formation of the coagulation factors Xa, IXa and thrombin induced by the factor VIIa and by the tissue factor. These compounds can be used as medicaments for the treatment and/or prevention of thromboses, apoplexy, cardiac infarction, inflammation and arteriosclerosis or as antitumor agents.
