An update on recent patents on thrombin inhibitors (2010 - 2013).

摘要: Introduction: Thromboembolic incidences have increased nearly 33% in the past decade and directly affect 0.5% of population. Heparin, warfarin current direct thrombin inhibitors (DTIs), primary anticoagulants choice, suffer from several drawbacks. Thus, search for an antithrombotic devoid adverse effect continues earnest. Areas covered: Literature covering PubMed, SciFinder™ Scholar, Web Knowledge, Espacenet, PatentScope Google Patent Search was used to uncover > 35 patents describing new chemical entities advances DTI technologies. Our uncovered considerable emphasis on development larger more complex molecules such as peptide-based inhibitors, prodrug derivatives, bivalent tryptophan zippers, triple action allosteric inhibitors. Advances formulation technologies clinically relevant DTIs also been made. Expert opinion: Thrombin is a multifaceted, dynamic enzyme with both coagulant anticoagulant functions. Ne...