25195-52-2Relevant academic research and scientific papers
NHC-Catalyzed Deamination of Primary Sulfonamides: A Platform for Late-Stage Functionalization
Fier, Patrick S.,Maloney, Kevin M.
supporting information, p. 1441 - 1445 (2019/01/30)
Herein we describe the development and application of a method for the mild, late-stage conversion of primary sulfonamides to several other other functional groups. These reactions occur via initial reductive deamination of sulfonamides to sulfinates via an NHC-catalyzed reaction of transiently formed N-sulfonylimines. The method described here is tolerant of nearly all common functional groups, as exemplified by the late-stage derivatization of several complex pharmaceutical compounds. On the basis of the prevalence of sulfonamide-containing drugs and building blocks, we have developed a method to enable sulfonamides to be applied as versatile synthetic handles for synthetic chemsitry.
Discovery of TUG-770: A highly potent free fatty acid receptor 1 (FFA1/GPR40) agonist for treatment of type 2 diabetes
Christiansen, Elisabeth,Hansen, Steffen V. F.,Urban, Christian,Hudson, Brian D.,Wargent, Edward T.,Grundmann, Manuel,Jenkins, Laura,Zaibi, Mohamed,Stocker, Claire J.,Ullrich, Susanne,Kostenis, Evi,Kassack, Matthias U.,Milligan, Graeme,Cawthorne, Michael A.,Ulven, Trond
supporting information, p. 441 - 445 (2013/07/11)
Free fatty acid receptor 1 (FFA1 or GPR40) enhances glucose-stimulated insulin secretion from pancreatic β-cells and currently attracts high interest as a new target for the treatment of type 2 diabetes. We here report the discovery of a highly potent FFA1 agonist with favorable physicochemical and pharmacokinetic properties. The compound efficiently normalizes glucose tolerance in diet-induced obese mice, an effect that is fully sustained after 29 days of chronic dosing.
ORTHO-FLUORO SUBSTITUTED COMPOUNDS FOR THE TREATMENT OF METABOLIC DISEASES
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Page/Page column 41, (2012/10/18)
There is provided novel fluoro-substituted compounds capable of modulating the G- protein-coupled receptor GPR40, compositions comprising the compounds, and methods for their use for controlling insulin levels in vivo and for the treatment of conditions such as type II diabetes, hypertension, ketoacidosis, obesity, glucose intolerance, and hypercholesterolemia and related disorders associated with abnormally high or low plasma lipoprotein, triglyceride or glucose levels.
