Potent 4-amino-5-azaindole factor VIIa inhibitors

The 4-amino-5-azaindole as an amidino-benzimidazole replacement is described. A series of potent and selective analogs were discovered and showed desirable ex vivo efficacy as measured by PT.

In our continued effort to develop orally bioavailable factor VIIa inhibitors based on the 2-[5-(5-carbamimidoyl-1H-benzoimidazol-2-yl)-6-hydroxy-biphenyl-3-yl]- succinic acid scaffold, we have identified potent and selective analogs with 4-amino-5-azaindole (1H-pyrrolo[3,2-c]pyridin-4-ylamine) as a less basic amidine replacement.Figure optionsDownload as PowerPoint slide