1381970-69-9

Upstream product

• 1104546-96-4 5-methyl-2-(2Η-1,2,3-triazol-2-yl)benzoyl chloride 
• 1381972-02-6 N-ethyl-N-(2-hydroxyethyl)-5-methyl-2-(2H-1,2,3-triazol-2-yl)benzamide 
• 1381971-92-1 5-fluoro-2-(1H-pyrazol-4-yl)pyridine 
• 1381972-00-4 N-(2-{[tert-butyl(dimethyl)silyl]oxy}ethyl)-N-ethyl-5-methyl-2-(2H-1,2,3-triazol-2-yl)benzamide 
• 1381971-98-7 N-ethyl-5-methyl-2-(2H-1,2,3-triazol-2-yl)benzamide 
• 956317-36-5 2-(2H-1,2,3-triazol-2-yl)-5-methylbenzoic acid 
• 41404-58-4 2-bromo-5-fluoropyridine 

Relevant academic research and scientific papers

Discovery and in vitro and in vivo profiles of N-ethyl-N-[2-[3-(5-fluoro-2-pyridinyl)-1H-pyrazol-1-yl]ethyl]-2-(2H-1,2,3-triazol-2-yl)-benzamide as a novel class of dual orexin receptor antagonist

Orexins play an important role in sleep/wake regulation, and orexin receptor antagonists are a focus of novel therapy for the treatment of insomnia. We identified 27e (TASP0428980) as a potent dual orexin receptor antagonist through the systematic modification of our original designed lead A. We demonstrated the potent sleep-promoting effects of 27e at ip dose of 3 mg/kg in a rat polysomnogram study. 27e exhibited relatively short half-life profiles in rats and dogs. Furthermore, accumulating evidence regarding ADME profiles indicates that the predicted human half-life of 27e should be 1.2-1.4 h. These data indicated that 27e has a short-acting hypnotic property, suggesting that 27e might be useful for treating primary insomnia while exhibiting a low risk of next-day residual somnolence. Thus, 27e and its related compounds should be further evaluated to enable advancement to clinical trials.

PYRAZOLE DERIVATIVE

A compound represented by formula (IA) or a pharmaceutically acceptable salt thereof, which is useful for the treatment or prevention of diseases such sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependence, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, pain, gastrointestinal diseases, epilepsy, inflammation, immune-related diseases, endocrine-related diseases, and hypertension, and of which the action relies on an orexin (OX) receptor antagonistic activity.