Structure–activity-relationship of amide and sulfonamide analogs of omarigliptin. Issue 24 (15th December 2015)

• Record Type: Journal Article
• Authors: 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
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 25:Issue 24(2015)
• Page Start: 5767
• Page End: 5771
• Publication Date: 2015-12-15
• Subjects: DPP-4 inhibitor -- Type 2 diabetes -- DPP-8 -- DPP-9 -- Sitagliptin -- Pyrazolopyrolidine -- Omarigliptin -- X-ray; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.10.070
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: A series of novel substituted-[(3 R )-amino-2-(2, 5-difluorophenyl)]tetrahydro-2 H -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.