95798-23-5Relevant articles and documents
Discovery of a potent G-protein-coupled receptor 119 agonist for the treatment of type 2 diabetes
Pola, Suresh,Shah, Shailesh R.,Pingali, Harikishore,Zaware, Pandurang,Thube, Baban,Makadia, Pankaj,Patel, Hoshang,Bandyopadhyay, Debdutta,Rath, Akshyaya,Giri, Suresh,Patel, Jitendra H.,Ranvir,Sundar,Patel, Harilal,Kumar, Jeevan,Jain, Mukul R.
, (2021/03/30)
The ever-growing prevalence of Type-2 diabetes in the world has an urgent need for multiple orally effective agents that can regulate glucose homeostasis. G-Protein coupled receptor 119 (GPR 119) agonists have demonstrated the glucose-dependent insulin secretion and showed beneficial effects on glycemic control in humans and/or relevant animal models. Herein, we describe our efforts towards identification of a potent and oral GPR 119 agonist 13c (ZY-G19), which showed in vitro potency in the cell-based assay and in vivo efficacy without exerting any significant signs of toxicity in relevant animal models.
CONJUGATED CHEMICAL INDUCERS OF DEGRADATION AND METHODS OF USE
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Page/Page column 485-486, (2020/05/28)
The subject matter described herein is directed to antibody-CIDE conjugates (Ab-CIDEs), to pharmaceutical compositions containing them, and to their use in treating diseases and conditions where targeted protein degradation is beneficial.
Chemoselective Oxidation of p-Methoxybenzyl Ethers by an Electronically Tuned Nitroxyl Radical Catalyst
Hamada, Shohei,Sugimoto, Koichi,Elboray, Elghareeb E.,Kawabata, Takeo,Furuta, Takumi
supporting information, p. 5486 - 5490 (2020/07/24)
The oxidation of p-methoxy benzyl (PMB) ethers was achieved using nitroxyl radical catalyst 1, which contains electron-withdrawing ester groups adjacent to the nitroxyl group. The oxidative deprotection of the PMB moieties on the hydroxy groups was observed upon treatment of 1 with 1 equiv of the co-oxidant phenyl iodonium bis(trifluoroacetate) (PIFA). The corresponding carbonyl compounds were obtained by treating the PMB-protected alcohols with 1 and an excess of PIFA.