(3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes |
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| Authors: | Biftu Tesfaye Feng Dennis Qian Xiaoxia Liang Gui-Bai Kieczykowski Gerard Eiermann George He Huaibing Leiting Barbara Lyons Kathy Petrov Aleksandr Sinha-Roy Ranabir Zhang Bei Scapin Giovanna Patel Sangita Gao Ying-Duo Singh Suresh Wu Joseph Zhang Xiaoping Thornberry Nancy A Weber Ann E |
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| Affiliation: | Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065, USA. Tesfaye_Biftu@merck.com |
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| Abstract: | Replacement of the triazolopiperazine ring of sitagliptin (DPP-4 IC(50)=18nM) with 3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one gave dipeptidyl peptidase IV (DPP-4) inhibitor 1 which is potent (DPP-4 IC(50)=2.6nM), selective, and efficacious in an oral glucose tolerance test in mice. It was selected for extensive preclinical development as a potential back-up candidate to sitagliptin. |
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