123532-25-2

Usage

Physical state

Yellow crystalline solid

Uses

Widely used in pharmaceutical and agricultural industries

Functions

Intermediate in organic synthesis, pharmaceutical intermediate, agrochemical intermediate

Known for

Inhibiting various enzymes, precursor for synthesis of other organic compounds

Potential pharmacological properties

Anti-inflammatory and antioxidant effects

Upstream product

• 51484-05-0 6-nitro-chromen-4-one 
• 60-34-4 methylhydrazine 
• 720702-43-2 5-(2-methoxy-5-nitro-phenyl)-1-methyl-1H-pyrazole 

Downstream Products

• 839713-75-6 5-(2-benzyloxy-5-nitrophenyl)-1-methyl-1H-pyrazole 
• 839713-86-9 1-methyl-5-(5-nitro-2-phenethyloxyphenyl)-1H-pyrazole 
• 839713-81-4 5-[2-(4-chlorobenzyloxy)-5-nitrophenyl]-1-methyl-1H-pyrazole 
• 887937-64-6 5-[2-(2-bromo-ethoxy)-5-nitro-phenyl]-1-methyl-1H-pyrazole 
• 839713-62-1 5-(2-ethoxy-5-nitrophenyl)-1-methyl-1H-pyrazole 
• 839713-67-6 5-(2-isopropoxy-5-nitrophenyl)-1-methyl-1H-pyrazole 
• 887938-10-5 4-{2-[2-(2-methyl-2H-pyrazol-3-yl)-4-nitro-phenoxy]-ethyl}morpholine 
• 887937-81-7 2-[2-(2-methyl-2H-pyrazol-3-yl)-4-nitro-phenoxymethyl]-pyridine 

Relevant academic research and scientific papers

Discovery and structure-activity relationship of 3-methoxy-N-(3-(1-methyl-1 H-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide (APD791): A highly selective 5-hydroxytryptamine2A receptor inverse agonist for the treatment of arterial thrombo

Serotonin, which is stored in platelets and is released during thrombosis, activates platelets via the 5-HT2A receptor. 5-HT2A receptor inverse agonists thus represent a potential new class of antithrombotic agents. Our medicinal pro

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

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

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