1402585-33-4

Upstream product

• 1885-14-9 phenyl chloroformate 
• 840501-15-7 (4-amino-2-fluorophenyl)methanol 
• 403-24-7 2-fluoro-4-nitrobenzoic acid 
• 660432-43-9 (2-fluoro-4-nitrophenyl)methanol 
• 392-09-6 2-fluoro-4-nitro-benzoic acid methyl ester 

Downstream Products

• 1402585-34-5 C₁₃H₁₂F₄N₄O₂ 
• 1402581-33-2 1-[[2-(4-chlorophenyl)-5-(trifluoromethyl)-2H-pyrazol-3-yl]methyl]-3-[3-fluoro-4-(hydroxymethyl)phenyl]urea 
• 1402581-34-3 1-[[2-(2,3-dichlorophenyl)-5-(trifluoromethyl)-2H-pyrazol-3-yl]methyl]-3-[3-fluoro-4-(hydroxymethyl)phenyl]urea 
• 1402582-07-3 1-((1-(3-chlorophenyl)-3-(trifluoromethyl)-1H-pyrazol-5-yl)methyl)-3-(3-fluoro-4-formylphenyl)urea 
• 1402581-36-5 1-[[2-(5-chloro-2-methoxyphenyl)-5-(trifluoromethyl)-2H-pyrazol-3-yl]methyl]-3-[3-fluoro-4-(hydroxymethyl)phenyl]urea 
• 1402581-35-4 1-[[2-(3-chloro-2-methoxyphenyl)-5-(trifluoromethyl)-2H-pyrazol-3-yl]methyl]-3-[3-fluoro-4-(hydroxymethyl)phenyl]urea 
• 1402581-32-1 1-[[2-(3-chlorophenyl)-5-(trifluoromethyl)-2H-pyrazol-3-yl]-methyl]-3-[3-fluoro-4-(hydroxymethyl)-phenyl]-urea 

Relevant academic research and scientific papers

Discovery of Nonpungent Transient Receptor Potential Vanilloid 1 (TRPV1) Agonist as Strong Topical Analgesic

Paradoxically, some TRPV1 agonists are, at the organismal level, both nonpungent and clinically useful as topical analgesics. Here, we describe the scaled-up synthesis and characterization in mouse models of a novel, nonpungent vanilloid. Potent analgesic activity was observed in models of neuropathic pain, and the compound blocked capsaicin induced allodynia, showing dermal accumulation with little transdermal absorption. Finally, it displayed much weaker systemic toxicity compared to capsaicin and was negative in assays of genotoxicity.

Discovery of dual-acting opioid ligand and TRPV1 antagonists as novel therapeutic agents for pain

In order to discover a novel type of analgesic, we investigated dual activity ligands with TRPV1 antagonism and mu-opioid receptor affinity with the goal of eliciting synergistic analgesia while avoiding the side effects associated with single targeting.

SUBSTITUTED PYRAZOLYL-BASED CARBOXAMIDE AND UREA DERIVATIVES BEARING A PHENYL MOIETY SUBSTITUTED WITH AN O-CONTAINING GROUP AS VANILLOID RECEPTOR LIGANDS

The invention relates to substituted pyrazolyl-based carboxamide and urea derivatives of formula (Q) as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.

SUBSTITUTED PYRAZOLYL-BASED CARBOXAMIDE AND UREA DERIVATIVES BEARING A PHENYL MOIETY SUBSTITUTED WITH A CO-CONTAINING GROUP AS VANILLOID RECEPTOR LIGANDS

The invention relates to substituted pyrazolyl-based carboxamide and urea derivatives bearing a phenyl moiety substituted with a CO-containing group as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.