Due to its critical role in the coagulation cascade Factor Xa became an important target for antithrombotic drug development. The design of the first generation of Factor Xa inhibitors was based on dibasic inhibitors binding to both the primary specificity pocket of Factor Xa and a putative cation binding site. The high basicity of these compounds limited the oral bioavailability and thus prohibited convenient oral administration in a therapeutic setting. Hence, recent efforts have focused on the development of non-peptide inhibitors of low basicity by screening and rational design. This report provides an overview of the recent patent literature from 1998 to 2000.