| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10591011 | Bioorganic & Medicinal Chemistry Letters | 2014 | 4 Pages |
Abstract
A series of 5-fluoro-4,6-dialkoxypyrimidine GPR119 modulators were discovered and optimized for in vitro agonist activity. A lead molecule was identified that has improved agonist efficacy relative to our clinical compound (APD597) and possesses reduced CYP2C9 inhibitory potential. This optimized lead was found to be efficacious in rodent models of glucose control both alone and in combination with a Dipeptidyl peptidase-4 (DPP-4) inhibitor.
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Authors
Daniel J. Buzard, Sun Hee Kim, Juerg Lehmann, Sangdon Han, Imelda Calderon, Amy Wong, Andrew Kawasaki, Sanju Narayanan, Rohit Bhat, Tawfik Gharbaoui, Luis Lopez, Dawei Yue, Kevin Whelan, Hussien Al-Shamma, David J. Unett, Hsin-Hui Shu, Shiu-Feng Tung,