934615-45-9Relevant academic research and scientific papers
Discovery of N-Aryl-2-acylindole human glucagon receptor antagonists
Sinz, Christopher,Bittner, Amy,Brady, Ed,Candelore, Mari,Dallas-Yang, Qing,Ding, Victor,Jiang, Guoqiang,Lin, Zhen,Qureshi, Sajjad,Salituro, Gino,Saperstein, Richard,Shang, Jackie,Szalkowski, Deborah,Tota, Laurie,Vincent, Stella,Wright, Michael,Xu, Shiyao,Yang, Xiaodong,Zhang, Bei,Tata, James,Kim, Ronald,Parmee, Emma R.
, p. 7124 - 7130 (2012/01/13)
A novel class of N-aryl-2-acylindole human glucagon receptor (hGCGR) antagonists is reported. These compounds demonstrate good pharmacokinetic profiles in multiple preclinical species. One compound from this series, indole 33, is orally active in a transgenic murine pharmacodynamic model. Furthermore, a 1 mg/kg oral dose of indole 33 lowers ambient glucose levels in an ob/ob/hGCGR transgenic murine diabetes model. This compound was deemed suitable for preclinical safety studies and was found to be well tolerated in an 8-day experimental rodent tolerability study. The combination of preclinical efficacy and safety observed with compound 33 highlights the potential of this class as a treatment for type 2 diabetes.
Acyl indoles, compositions containing such compounds and methods of use
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Page/Page column 19, (2008/06/13)
The present invention relates to substituted indoles, compositions containing such compounds and methods of treatment The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus and related conditions.
