Discovery of 6, 7-Dihydro-5 H-pyrrolo [2, 3-a] pyrimidines as Orally Available G Protein-Coupled Receptor 119 Agonists

…, AJ Carpenter, CE Ammala, EE Boros…

文献索引：Katamreddy, Subba R.; Carpenter, Andrew J.; Ammala, Carina E.; Boros, Eric E.; Brashear, Ron L.; Briscoe, Celia P.; Bullard, Sarah R.; Caldwell, Richard D.; Conlee, Christopher R.; Croom, Dallas K.; Hart, Shane M.; Heyer, Dennis O.; Johnson, Paul R.; Kashatus, Jennifer A.; Minick, Doug J.; Peckham, Gregory E.; Ross, Sean A.; Roller, Shane G.; Samano, Vicente A.; Sauls, Howard R.; Tadepalli, Sarva M.; Thompson, James B.; Xu, Yun; Way, James M. Journal of Medicinal Chemistry, 2012 , vol. 55, # 24 p. 10972 - 10994

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被引用次数: 6

摘要

GPR119 is a 7-transmembrane receptor that is expressed in the enteroendocrine cells in the intestine and in the islets of Langerhans in the pancreas. Indolines and 6, 7-dihydro-5 H- pyrrolo [2, 3-a] pyrimidines were discovered as G protein-coupled receptor 119 (GPR119) agonists, and lead optimization efforts led to the identification of 1-methylethyl 4-({7-[2-fluoro- 4-(methylsulfonyl) phenyl]-6, 7-dihydro-5 H-pyrrolo [2, 3-d] pyrimidin-4-yl} oxy)-1- ...