51363-82-7Relevant academic research and scientific papers
Route Selection and Optimization in the Synthesis of Two Imidazopyridine Inhibitors of DGAT-2
Bader, Scott J.,Herr, Michael,Aspnes, Gary E.,Cabral, Shawn,Li, Qifang,Bian, Jianwei,Coffey, Steven B.,Dowling, Matthew S.,Fernando, Dilinie P.,Jiao, Wenhua,Lavergne, Sophie Y.,Kung, Daniel W.
, p. 360 - 367 (2018)
The scalable syntheses of two imidazopyridine inhibitors of the enzyme diacylglycerol acyltransferase 2 (DGAT-2) are described. 6-Chloro-3-nitro-2-aminopyridine was the starting material for the convergent synthesis of the central imidazopyridine ring. Differentiation in reactivity of the C2- and C3-nitrogen substituents on the pyridine ring and the development of mild cyclodehydration conditions to form the imidazole ring were critical problems that were addressed to deliver a 3-kg batch of compound 1 (PF-06424439) and a 0.1-kg batch of compound 2 (PF-06450561).
Small structural changes of the imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitors produce an improved safety profile
Futatsugi,Huard,Kung,Pettersen,Flynn,Gosset,Aspnes,Barnes,Cabral,Dowling,Fernando,Goosen,Gorczyca,Hepworth,Herr,Lavergne,Li,Niosi,Orr,Pardo,Perez,Purkal,Schmahai,Shirai,Shoieb,Zhou,Goodwin
, p. 771 - 779 (2017)
Small molecule DGAT2 inhibitors have shown promise for the treatment of metabolic diseases in preclinical models. Herein, we report the first toxicological evaluation of imidazopyridine-based DGAT2 inhibitors and show that the arteriopathy associated with
DIACYLGLYCEROL ACYLTRANSFERASE 2 INHIBITORS
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Page/Page column 113, (2013/10/22)
Derivatives of purine, 3H-imidazo[4,5-b]pyrimidine and 1H- imidazo[4,5-d]pyrazine of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.
