- Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors
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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
- Groebke Zbinden, Katrin,Banner, David W.,Ackermann, Jean,D'Arcy, Allan,Kirchhofer, Daniel,Ji, Yu-Hua,Tschopp, Thomas B.,Wallbaum, Sabine,Weber, Lutz
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p. 817 - 822
(2007/10/03)
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- Acylsulfamide inhibitors of factor VIIa
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Compounds having the general formula I are useful for inhibiting serine protease enzymes, such as Tissue Factor VIIa, factor Xa, thrombin and kallikrein and have improved permeability properties. These compounds may be used in methods of preventing and/or
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- Serine protease inhibitors
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Compounds having the structure shown below wherein A, B, N1, N2, X, Y, Q, R2, R5and R6are as defined herein are useful to inhibit serine protease enzymes, such as TF/factor VIIa factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.
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- N-(4- carbamimidoyl-phenyl) -glycine derivatives
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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.
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- N-(4-carb-amimidophenyl)glycineamide derivatives
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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.
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