Patent Evaluation: Isosteric peptides as thrombin inhibitors

Summary

Novelty: Novel isosteric peptides are claimed as competitive inhibitors of thrombin and these are stated to be useful as anticoagulants for prophylaxis and treatment of thromboembolic diseases such as venous thrombosis and myocardial infarction.

Biology: The concentration of inhibitor which doubled the thrombin clotting time for human plasma was determined (IC₅₀). pIC₅₀ value ranged from 6.47–8.69.

Chemistry: The synthesis of thirty-seven compounds is described and these are all specifically claimed. Eight different synthetic procedures are disclosed.