Discovery of 3-aminopiperidines as potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitors |
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| Authors: | Cox Jason M Harper Bart Mastracchio Anthony Leiting Barbara Sinha Roy Ranabir Patel Reshma A Wu Joseph K Lyons Kathryn A He Huaibing Xu Shiyao Zhu Bing Thornberry Nancy A Weber Ann E Edmondson Scott D |
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| Affiliation: | Merck Research Laboratories, Department of Medicinal Chemistry, PO Box 2000, Rahway, NJ 07065, USA. jason_cox@merck.com |
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| Abstract: | Substituted 3-aminopiperidines 3 were evaluated as DPP-4 inhibitors. The inhibitors showed good DPP-4 potency with superb selectivity over other peptidases (QPP, DPP8, and DPP9). Selected DPP-4 inhibitors were further evaluated for their hERG potassium channel, calcium channel, Cyp2D6, and pharmacokinetic profiles. |
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