Novel 5-azaindole factor VIIa inhibitors

The discovery and development of 5-azaindole factor VIIa inhibitors will be described.

Graphical abstractWe have developed a series of potent and selective factor VIIa inhibitors based on the 2-[5-(5-carbamimidoyl-1H-benzoimidazol-2-yl)-6-hydroxy-biphenyl-3-yl]- succinic acid scaffold. These biaryl amidine-containing compounds suffer from low oral bioavailability. In an attempt to apply the knowledge we have gained from our amidine fVIIa inhibitor parenteral program to an oral program, we began with our 5-amidinobenzimidazole scaffold and replaced the amidine with a less basic 5-azaindole (1H-pyrrolo[3,2-c]pyridine, 2). The discovery and development of 5-azaindole factor VIIa inhibitors will be described.Figure optionsDownload full-size imageDownload as PowerPoint slide