| Literature DB >> 22264481 |
Graeme Semple1, 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, Keith Demarest, Robert M Jones.
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.Entities:
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Year: 2011 PMID： 22264481 DOI： 10.1016/j.bmcl.2011.12.092
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823