Discovery of potent, selective, and orally bioavailable pyridone-based dipeptidyl peptidase-4 inhibitors

anti-Substituted β-methylphenylalanine derived amides have been shown to be potent DPP-IV inhibitors exhibiting excellent selectivity over both DPP8 and DPP9. The optimized compound exhibited good pharmacokinetic profiles in three preclinical species.

anti-Substituted biaryl β-methylphenylalanine derived amides have been shown to be potent DPP-4 inhibitors exhibiting excellent selectivity over both DPP8 and DPP9. The optimized compound 9 exhibited good pharmacokinetic profiles in three preclinical species.Figure optionsDownload as PowerPoint slide