121198-78-5Relevant articles and documents
Photoredox Reaction of 2-Mercaptothiazolinium Salts with Silyl Enol Ethers
Zemtsov, Artem A.,Ashirbaev, Salavat S.,Levin, Vitalij V.,Kokorekin, Vladimir A.,Korlyukov, Alexander A.,Dilman, Alexander D.
, (2019/11/29)
A method for the generation of free radicals from thiazolinium salts upon photocatalytic reduction is described. The thiazolinium salts are generated by treatment with methyl triflate of 2-mercaptothiazolines, which can be readily obtained from alkyl bromides and tosylates via a nucleophilic substitution reaction or by hydrothiolation of alkenes. Silyl enol ethers were used to trap the radicals, furnishing ketones after successive single-electron oxidation and elimination of the silyl cation.
Discovery of potent and orally bioavailable indazole-based glucagon receptor antagonists for the treatment of type 2 diabetes
Xu, Guozhang,Gaul, Michael D.,Song, Fengbin,Du, Fuyong,Liang, Yin,DesJarlais, Renee L.,DiLoreto, Karen,Shook, Brian,Rentzeperis, Dennis,Santulli, Rosie,Eckardt, Annette,Demarest, Keith
, (2019/09/12)
Type 2 diabetes mellitus (T2DM) is characterized by chronically elevated plasma glucose levels. The inhibition of glucagon-induced hepatic glucose output via antagonism of the glucagon receptor (GCGR) using a small-molecule antagonist is a promising mecha
INDAZOLE DERIVATIVES USEFUL AS GLUCAGON RECEPTOR ANTAGONISTS
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, (2018/03/25)
The present invention is directed to indazole derivatives, pharmaceutical compositions containing them and their use in the treatment and/or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for e