21709-39-7

Upstream product

• 302963-94-6 2-[[(tert-butyloxy)carbonyl]amino]-4-methyl-1,3-thiazole-5-carboxylic acid 
• 244236-52-0 ethyl 2-[[(tert-butyloxy)carbonyl]amino]-4-methyl-1,3-thiazole-5-carboxylate 
• 7210-76-6 ethyl-2-amino-4-methylthiazole-5-carboxylate 
• 67899-00-7 2-amino-4-methyl-thiazole-5-carboxylic acid 
• 100-46-9 benzylamine 

Downstream Products

• 1034981-12-8 N-benzyl-2-cyano-4-methylthiazole-5-carboxamide 
• 1034981-16-2 2-azido-N-benzyl-4-methylthiazole-5-carboxamide 
• 1072802-20-0 N-benzyl-2-(3-(4-fluorophenyl)-5-methoxy-2-oxoimidazolidin-1-yl)-4-methylthiazole-5-carboxamide 
• 1072802-21-1 N-benzyl-2-(3-(4-fluorophenyl)-5-hydroxy-2-oxoimidazolidin-1-yl)-4-methylthiazole-5-carboxamide 
• 1072803-99-6 N-benzyl-2-(3-(4-fluorobenzyl)-2-oxo-2,3-dihydro-1H-imidazol-1-yl)-4-methylthiazole-5-carboxamide 
• 1072802-22-2 N-benzyl-2-(3-(4-fluorophenyl)-2,5-dioxoimidazolidin-1-yl)-4-methylthiazole-5-carboxamide 
• 1072804-44-4 N-benzyl-2-(3-(4-cyanobenzyl)-2-oxoimidazolidin-1-yl)-4-methylthiazole-5-carboxamide 
• 1072805-53-8 N-benzyl-2-(3-(4-fluorobenzoyl)-2-oxoimidazolidin-1-yl)-4-methylthiazole-5-carboxamide 
• 1072803-94-1 N-benzyl-2-(3-(4-fluorobenzyl)-5-hydroxy-2-oxoimidazolidin-1-yl)-4-methylthiazole-5-carboxamide 

Relevant academic research and scientific papers

Synthesis of GluN2A-selective NMDA receptor antagonists with an electron-rich aromatic B-ring

Glutamatergic N-Methyl-D-aspartate (NMDA) receptors are heterotetrameric ion channels that can be comprised of different subunits. GluN2A subunit-containing NMDA receptors are associated with diseases like anxiety, depression, and schizophrenia. However,

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.

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.

2-SUBSTITUTED 5-MEMBERED HETEROCYCLES AS SCD INHIBITORS

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

HETEROCYCLIC ORGANIC COMPOUNDS

The present application provides compounds 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 such derivatives are also encompassed.

AMINOTHIAZOLE DERIVATIVES AS HUMAN STEAROYL-COA DESATURASE INHIBITORS

Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I), where V, W, R1, R2, R3 and R4 are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.