Discovery of a Second Generation Agonist of the Orphan G-protein Coupled Receptor GPR119 with an Improved Profile
Bioorganic & medicinal chemistry letters(2012)
摘要
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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关键词
GPR119,GPCR,Diabetes,Lead optimization
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