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Abstract
Factor Xa is a key enzyme in the production of thrombin from its precursor prothrombin and is an important target for antithrombotic drug development. The patent literature for the last four to five years illustrates a variety of peptide and non-peptide Factor Xa inhibitors, including small proteins isolated from natural sources, rationally designed peptides and peptidomimetics based on substrate cleavage sites, and non-peptide small molecules derived from screening and rational design. This report reviews the status of the patent literature in the field of Factor Xa inhibitors through 1998.