Search

Your search keyword '"Hilpert, Kurt"' showing total 2 results
Start Over Author "Hilpert, Kurt" Topic thromboplastin
2 results on '"Hilpert, Kurt"'

1. Dose-dependent antithrombotic activity of an orally active tissue factor/factor VIIa inhibitor without concomitant enhancement of bleeding propensity.

Author

Groebke Zbinden K, Banner DW, Hilpert K, Himber J, Lavé T, Riederer MA, Stahl M, Tschopp TB, and Obst-Sander U

Subjects
Administration, Oral, Animals, Bleeding Time, Crystallography, X-Ray, Dose-Response Relationship, Drug, Drug Evaluation, Preclinical, Guinea Pigs, Humans, Models, Molecular, Molecular Structure, Prodrugs chemical synthesis, Prodrugs pharmacology, Rats, Stereoisomerism, Structure-Activity Relationship, Thrombosis drug therapy, Thrombosis prevention & control, Anticoagulants chemical synthesis, Anticoagulants pharmacology, Blood Coagulation Factor Inhibitors chemical synthesis, Blood Coagulation Factor Inhibitors pharmacology, Factor VIIa antagonists & inhibitors, Thromboplastin antagonists & inhibitors
Abstract

The discovery of a highly potent and selective tissue factor/factor VIIa inhibitor is described. Upon oral administration of its double prodrug in the guinea pig, a dose-dependent antithrombotic effect is observed in an established model of arterial thrombosis without prolonging bleeding time. The pharmacodynamic properties of this selective inhibitor are compared to the behaviour of a mixed factor VIIa/factor Xa inhibitor.

Published
2006
Full Text
View/download PDF

2. Selective and orally bioavailable phenylglycine tissue factor/factor VIIa inhibitors.

Author

Zbinden KG, Obst-Sander U, Hilpert K, Kühne H, Banner DW, Böhm HJ, Stahl M, Ackermann J, Alig L, Weber L, Wessel HP, Riederer MA, Tschopp TB, and Lavé T

Subjects
Administration, Oral, Animals, Anticoagulants chemical synthesis, Biological Availability, Crystallography, X-Ray, Drug Design, Glycine analogs & derivatives, Glycine chemistry, Humans, Molecular Structure, Rats, Serine Proteinase Inhibitors chemical synthesis, Anticoagulants chemistry, Anticoagulants pharmacology, Factor VIIa antagonists & inhibitors, Serine Proteinase Inhibitors chemistry, Serine Proteinase Inhibitors pharmacology, Thromboplastin antagonists & inhibitors
Abstract

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.

Published
2005
Full Text
View/download PDF

Catalog

Books, media, physical & digital resources
See catalog results