Discovery of a Partial Glucokinase Activator Clinical Candidate: Diethyl ((3-(3-((5-(Azetidine-1-carbonyl)pyrazin-2-yl)oxy)-5-isopropoxybenzamido)‑1H‑pyrazol-1-yl)methyl)phosphonate (BMS-820132)

Glucokinase (GK) is a key regulator of glucose homeostasis, and its small-molecule activators represent a promising opportunity for the treatment of type 2 diabetes. Several GK activators have been advanced into clinical trials and have demonstrated promising efficacy; however, hypoglycemia represen...

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Veröffentlicht in:Journal of medicinal chemistry 2022-03, Vol.65 (5), p.4291-4317
Hauptverfasser: Shi, Yan, Wang, Ying, Meng, Wei, Brigance, Robert P, Ryono, Denis E, Bolton, Scott, Zhang, Hao, Chen, Sean, Smirk, Rebecca, Tao, Shiwei, Tino, Joseph A, Williams, Kristin N, Sulsky, Richard, Nielsen, Laura, Ellsworth, Bruce, Wong, Michael K. Y, Sun, Jung-Hui, Leith, Leslie W, Sun, Dawn, Wu, Dauh-Rurng, Gupta, Anuradha, Rampulla, Richard, Mathur, Arvind, Chen, Bang-Chi, Wang, Aiying, Fuentes-Catanio, Helen G, Kunselman, Lori, Cap, Michael, Zalaznick, Jacob, Ma, Xiaohui, Liu, Heng, Taylor, Joseph R, Zebo, Rachel, Jones, Beverly, Kalinowski, Stephen, Swartz, Joann, Staal, Ada, O’Malley, Kevin, Kopcho, Lisa, Muckelbauer, Jodi K, Krystek, Stanley R, Spronk, Steven A, Marcinkeviciene, Jovita, Everlof, Gerry, Chen, Xue-Qing, Xu, Carrie, Li, Yi-Xin, Langish, Robert A, Yang, Yanou, Wang, Qi, Behnia, Kamelia, Fura, Aberra, Janovitz, Evan B, Pannacciulli, Nicola, Griffen, Steven, Zinker, Bradley A, Krupinski, John, Kirby, Mark, Whaley, Jean, Zahler, Robert, Barrish, Joel C, Robl, Jeffrey A, Cheng, Peter T. W
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Sprache:eng
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