- Pyrazole N-alkylation method
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The invention provides a pyrazole N-alkylation method. Pyrazole or pyrazole derivatives and alkyl halogenated hydrocarbons react in a solvent under the existence of quaternary ammonium salt catalysts;N-alkyl substituted pyrazole is obtained. The method provided by the invention has the advantages that the operation is simple; the cost is low; the anhydrous oxygen-free environment is not needed; heating is not needed; the yield is high; the amplified industrialized production can be easily realized.
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Paragraph 0023; 0024
(2018/12/14)
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- NEW THIENOPYRIMIDINE DERIVATIVES, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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Compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R12, X, A and n are as defined in the description.
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Page/Page column 132; 165
(2015/07/15)
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- Synthesis of heterocyclic compounds from 4-formylpyrazoles
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Formylation of pyrazole and 2,5-dimethylpyrazole gave a number of pyrazole-containing aldehydes, which can be used to obtain chromenes, tetrahydrochromenes, 1,4-dihydropyrano[2,3-c]pyrazoles, pyrano[3,2-c]chromenes, thiochromeno[4,3-b]pyrans, pyrano[3,2-c
- Mortikov,Rodinovskaya,Fedorov,Shestopalov,Belyakov
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p. 443 - 456
(2015/02/02)
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- 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
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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.
- 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.
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experimental part
p. 1923 - 1936
(2010/08/05)
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- Pyrazole-substituted arylamides as P2X3 and P2X2/3 antagonists
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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.
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Page/Page column 48
(2009/07/17)
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- 1H-QUINAZ0LINE-2,4-DIONES AND THEIR USE AS AMPA-RECEPTOR LIGANDS
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The present invention relates to l H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as AMPA-receptor ligands, in particular for the treatment of epilepsy or schizophrenia, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) and combinations comprising compounds of formula (I) are disclosed.
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Page/Page column 112
(2010/11/24)
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- 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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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
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Page/Page column 129
(2010/02/10)
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