| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1371818 | Bioorganic & Medicinal Chemistry Letters | 2012 | 6 Pages |
Abstract
The design and synthesis of a second generation GPR119-agonist clinical candidate for the treatment of diabetes is described. Compound 16 (APD597, JNJ-38431055) was selected for preclinical development based on a good balance between agonist potency, intrinsic activity and in particular on its good solubility and reduced drug–drug interaction potential. In addition, extensive in vivo studies showed a more favorable metabolic profile that may avoid the generation of long lasting metabolites with the potential to accumulate in clinical studies.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Graeme Semple, Juerg Lehmann, Amy Wong, Albert Ren, Marc Bruce, Young-Jun Shin, Carleton R. Sage, Michael Morgan, Wei-Chao Chen, Kristen Sebring, Zhi-Liang Chu, James N. Leonard, Hussein Al-Shamma, Andrew J. Grottick, Fuyong Du, Yin Liang,