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Aminopiperidine-fused imidazoles as dipeptidyl peptidase-IV inhibitors |
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| Authors: | Scott D. Edmondson Anthony Mastracchio Jason M. Cox George J. Eiermann Huaibing He Kathryn A. Lyons Reshma A. Patel Sangita B. Patel Aleksandr Petrov Giovanna Scapin Joseph K. Wu Shiyao Xu Bing Zhu Nancy A. Thornberry Ranabir Sinha Roy Ann E. Weber |
| Affiliation: | 1. Department of Medicinal Chemistry, Merck & Co. Inc., PO Box 2000, Rahway, NJ 07065, USA;2. Lead Optimization Pharmacology, Merck & Co. Inc., PO Box 2000, Rahway, NJ 07065, USA;3. Preclinical Drug Metabolism and Pharmacokinetics, Merck & Co. Inc., PO Box 2000, Rahway, NJ 07065, USA;4. Department of Metabolic Disorders, Merck & Co. Inc., PO Box 2000, Rahway, NJ 07065, USA;5. Global Structural Biology, Merck & Co. Inc., PO Box 2000, Rahway, NJ 07065, USA |
| Abstract: | A new series of DPP-4 inhibitors derived from piperidine-fused benzimidazoles and imidazopyridines is described. Optimization of this class of DPP-4 inhibitors led to the discovery of imidazopyridine 34. The potency, selectivity, cross-species DMPK profiles, and in vivo efficacy of 34 is reported. |
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