1072802-48-2

Upstream product

• 7210-76-6 ethyl-2-amino-4-methylthiazole-5-carboxylate 
• 1072806-73-5 ethyl 4-methyl-2-(2-oxoimidazolidin-1-yl)thiazole-5-carboxylate 
• 41940-43-6 5-Amino-2-ethoxycarbonyl-3-methyl-thiophen-hydrochlorid 
• 88796-28-5 ethyl 5-amino-3-methylthiophene-2-carboxylate 
• 1072806-37-1 ethyl 5-(3-(2-chloroethyl)ureido)-3-methylthiophene-2-carboxylate 
• 459-46-1 4-Fluorobenzyl bromide 
• 1072806-55-3 ethyl 3-methyl-5-(2-oxoimidazolidin-1-yl)thiophene-2-carboxylate 
• 1072802-27-7 ethyl 2-(3-(4-fluorobenzyl)-2-oxoimidazolidin-1-yl)-4-methylthiazole-5-carboxylate 

Downstream Products

• 1072803-08-7 XEN₇₂₃ 
• 1072805-46-9 2-(3-(4-fluorobenzyl)-2-oxoimidazolidin-1-yl)-4-methyl-N-(pyridin-2-ylmethyl)thiazole-5-carboxamide 
• 1072805-43-6 2-(3-(4-fluorobenzyl)-2-oxoimidazolidin-1-yl)-4-methylthiazole-5-carboxamide 

Relevant academic research and scientific papers

Systematic evaluation of amide bioisosteres leading to the discovery of novel and potent thiazolylimidazolidinone inhibitors of SCD1 for the treatment of metabolic diseases

Several five- and six-membered heterocycles were introduced to replace the C2-position amide bond of the original 2-aminothiazole-based hit compound 5. Specifically, replacement of the amide bond with an imidazolidinone moiety yielded a novel and potent thiazolylimidazolidinone series of SCD1 inhibitors. XEN723 (compound 22) was identified after optimization of the thiazolylimidazolidinone series. This compound demonstrated a 560-fold improvement in in vitro potency and reduced plasma desaturation indices in a dose dependent manner, with an EC50 of 4.5 mg/kg.

HETEROCYCLIC INHIBITORS OF STEAROYL-COA DESATURASE

The present invention provides heterocyclic derivatives of formula (I) that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising

ORGANIC COMPOUNDS

The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.