The discovery of potent and long-acting oral factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs

The discovery and evaluation of potent and long-acting oral sulfonamidopyrrolidin-2-one factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs are described. Unexpected selectivity issues versus tissue plasminogen activator in the former series were addressed in the later, delivering a robust candidate for progression towards clinical studies.

Graphical abstractThe discovery of potent and long-acting series of orally available factor Xa inhibitors with tetrahydroisoquinoline and benzazepine motifs is described.Figure optionsDownload full-size imageDownload as PowerPoint slide