Bioorganic and Medicinal Chemistry Letters p. 5767 - 5771 (2015)
Update date:2022-08-10
Topics:
Chen, Ping
Feng, Dennis
Qian, Xiaoxia
Apgar, James
Wilkening, Robert
Kuethe, Jeffrey T.
Gao, Ying-Duo
Scapin, Giovanna
Cox, Jason
Doss, George
Eiermann, George
He, Huaibing
Li, Xiaohua
Lyons, Kathryn A.
Metzger, Joseph
Petrov, Aleksandr
Wu, Joseph K.
Xu, Shiyao
Weber, Ann E.
Yan, Youwei
Roy, Ranabir Sinha
Biftu, Tesfaye
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.
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