839714-33-9Relevant 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.
Pyrazole-substituted arylamides as P2X3 and P2X2/3 antagonists
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Page/Page column 48, (2009/07/17)
Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted pyrazolyl, and R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
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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Page/Page column 129, (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
