1410040-87-7

Upstream product

• 884494-34-2 2-ethynyl-5-fluoropyridine 
• 1410040-82-2 N-[(3E)-3-(hydroxyimino)propyl]-5-methyl-2-(2H-1,2,3-triazol-2-yl)benzamide 
• 1410040-78-6 N-(3,3-diethoxypropyl)-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 

Downstream Products

• 1410039-22-3 N-ethyl-N-{2-[5-(5-fluoropyridin-2-yl)-1,2-oxazol-3-yl]ethyl}-5-methyl-2-(2H-1,2,3-triazol-2-yl)benzamide 

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.

HETEROAROMATIC RING DERIVATIVE

The compound represented by formula (IA) or a pharmaceutically acceptable salt thereof is based on orexin (OX) receptor antagonist activity, is useful in the treatment and prevention of illnesses including sleep disorder, depression, anxiety disorder, pan