720702-44-3Relevant academic research and scientific papers
Discovery of 1-[3-(4-Bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxyphenyl]-3-(2, 4-difluorophenyl)urea (Nelotanserin) and Related 5-Hydroxytryptamine 2A Inverse Agonists for the Treatment of Insomnia
Teegarden, Bradley R.,Li, Hongmei,Jayakumar, Honnappa,Strah-Pleynet, Sonja,Dosa, Peter I.,Selaya, Susan D.,Kato, Naomi,Elwell, Katie H.,Davidson, Jarrod,Cheng, Karen,Saldana, Hazel,Frazer, John M.,Whelan, Kevin,Foster, Jonathan,Espitia, Stephan,Webb, Robert R.,Beeley, Nigel R. A.,Thomsen, William,Morairty, Stephen R.,Kilduff, Thomas S.,Al-Shamma, Hussien A.
experimental part, p. 1923 - 1936 (2010/08/05)
Insomnia affects a growing portion of the adult population in the U.S. Most current therapeutic approaches to insomnia primarily address sleep onset latency. Through the 5-hydroxytryptamine2A (5-HT2A) receptor, serotonin (5-HT) plays a role in the regulation of sleep architecture, and antagonists/ inverse-agonists of 5-HT2A have been shown to enhance slow wave sleep (SWS). We describe here a series of 5-HT2A inverse-agonists that when dosed in rats, both consolidate the stages of NREM sleep, resulting in fewer awakenings, and increase a physiological measure of sleep intensity. These studies resulted in the discovery of 1-[3-(4-bromo-2- methyl-2i/-pyrazol-3-yl)-4-methoxyphenyl]-3-(2,4-difluorophenyl)urea (Nelotanserin), a potent inverse-agonist of 5-HT2A that was advanced into clinical trials for the treatment of insomnia.
DIARYL AND ARYLHETEROARYL UREA DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE PROPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERTO
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, (2010/02/10)
The present invention relates to certain pyrazole derivatives of Formula (I) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to
DIARYLAMINE AND ARYLHETEROARYLAMINE PYRAZOLE DERIVATIVES AS MODULATORS OF 5HT2A
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, (2010/02/07)
One aspect of the present invention relates to certain diarylamine and arylheteroarylamine pyrazole derivatives of Formula (A) and pharmaceutical compositions that modulate the activity of the human 5HT2A serotonin receptor. Compounds and pharmaceutical c
