720702-45-4Relevant academic research and scientific papers
COMPOSITION OF A 5-HT2A SEROTONIN RECEPTOR MODULATOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
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, (2016/04/20)
The present invention relates to certain compositions of a 5-HT2A serotonin receptor modulator and methods for their preparation. The compositions disclosed herein are useful for increasing slow wave sleep, improvise sleep consolidation, improv
PROCESSES USEFUL FOR THE PREPARATION OF 1-[3-(4-BROMO-2-METHYL-2H-PYRAZOL-3-YL)-4-METHOXY-PHENYL]-3-(2,4-DIFLUORO-PHENYL)-UREA AND CRYSTALLINE FORMS RELATED THERETO
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Page/Page column 75, (2010/06/17)
The present invention is directed to processes and intermediates useful for the preparation of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea (Compound I), crystalline forms and solvate forms thereof; and compositio
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.
PROCESSES FOR PREPARING SUBSTITUTED PHENYLPYRAZOLE UREAS
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Page/Page column 34-36, (2008/06/13)
The present invention is directed to processes for the preparation of substituted phenylpyrazole ureas of Formula (I) that are useful as 5-HT2A serotonin receptor modulators for the treatment of disease.
PROCESSES FOR PREPARING SUBSTITUTED N-ARYL-N’-[3-(1H-PYRAZOL-5-YL) PHENYL] UREAS AND INTERMEDIATES THEREOF
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Page/Page column 47, (2008/06/13)
The present invention is directed to processes for the preparation of substituted phenylpyrazole ureas of Formula (I), that are useful as 5-HT2A serotonin receptor modulators for the treatment of disease.
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
