Patent Evaluation: Inhibitors and Substrates of Thrombin

Summary

Novelty: Novel peptides, which may be thrombin inhibitors, useful for the treatment or prevention of thromboses, are disclosed.

Biology: The inhibition of human α-thrombin was determined using, these peptides, by the inhibition of the enzyme-catalyzed hydrolysis of three different concentrations of the chromogenic substrate, S-2238. Prolongation of the thrombin time for these new compounds was also demonstrated.

Chemistry: Syntheses of these peptides are by conventional methods and are described in twenty-two examples and eight schemes.