Structure-Activity Relationships Of Amide And Sulfonamide Analogs Of Omarigliptin (Mk-3102), A Novel, Long Acting Dpp-4 Inhibitor For Treatment Of Type 2 Diabetes

A series of novel substituted-[(3R)-amino-2-(2,5-difluorophenyl)]tetrahydro-2H-pyran analogs have been prepared and evaluated as potent, selective and orally active DPP-4 inhibitors. These efforts lead to the discovery of a long acting DPP-4 inhibitor, omarigliptin (MK-3102), which recently completed phase III clinical development and has been approved in Japan.