960215-02-5

Upstream product

• 113503-90-5 2-hydroxy-4-oxo-4-p-tolylbut-2-enoic acid ethyl ester 
• 850829-14-0 4-(3-formyl-5-p-tolyl-pyrazol-1-yl)-benzenesulfonamide 
• 641639-48-7 4-(3-(hydroxymethyl)-5-(p-tolyl)-1H-pyrazol-1-yl)benzenesulfonamide 
• 170569-23-0 1-(4-sulfamoylphenyl)-5-p-tolyl-1H-pyrazole-3-carboxylic acid ethyl ester 
• 122-00-9 para-methylacetophenone 
• 114150-50-4 4,6-dioxo-6-(4-methylphenyl)hexanoic acid 
• 17852-52-7 4-hydrazinobenzene-1-sulfonamide hydrochloride 

Downstream Products

• 960215-49-0 tert-butyl 2-[3-{1-(4-sulfamoylphenyl)-5-p-tolyl-1H-pyrazol-3-yl}propanamido]ethylcarbamate 
• 1287761-22-1 4-[3-(3-hydroxypropyl)-5-p-tolyl-pyrazol-1-yl]-benzenesulfonamide 
• 1287761-23-2 4-{3-[3-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-propyl]-5-p-tolyl-pyrazol-1-yl}-benzenesulfonamide 
• 1287760-95-5 4-(5-p-tolyl-3-{3-[3-(3-trifluoromethylphenyl)-ureido]-propyl}-pyrazol-1-yl)-benzenesulfonamide 
• 1287761-24-3 C₁₉H₂₂N₄O₂S 

Relevant academic research and scientific papers

3-[1-(4-Sulfamoylphenyl)-5-p-tolyl-1H-pyrazol-3-yl]propanoic acid and 3-[5-(4-bromophenyl)-1-(4-sulfamoylphenyl)-1H-pyrazol-3-yl]propanoic acid-dichloromethane-diethyl etherwater (2/0.72/1/1)

The structures of two related analogues 3-[1-(4-Sulfamoylphenyl)-5-p-tolyl- 1H-pyrazol-3-yl]propanoic acids and 3-[5-(4-bromophenyl)-1-(4-sulfamoylphenyl)- 1H-pyrazol-3-yl]propanoic acid-dichloromathane-diethyl ether-water has been reported. The compound

PYRAZOLE INHIBITORS OF COX-2 AND SEH

The present invention provides compounds and compositions, e.g., a series of compounds wherein a 1,5-biarylpyrazole group is conjugated to a urea group by a non-cleavable covalent chain, that are useful as dual COX-2/sEH inhibitors. The compounds disclosed herein have activity associated with the arachidonate cascade. The activity of these compounds was demonstrated using a lipopolysaccharide (LPS) induced model of pain in the rat. The compounds of the present invention demonstrated superior anti-allodynic activity as compared to the same dose of celecoxib, i.e., a COX-2 inhibitor, also as compared to the same dose of t-AUCB, i.e., a sEH inhibitor, and also as compared to the co-administered same dose of both celecoxib and t-AUCB. The dual inhibitors of the present invention demonstrate enhanced in vivo anti-allodynic activity in a nociceptive behavioral assay. In addition, the compounds of the present invention also demonstrated to have potent anti-angiogenic effects toward endothelial cells (HUVEC) and inhibit angiogenesis in vitro, ex vivo and in vivo. The dual inhibitors of the present invention also demonstrate anti-angiogenic effect to slow breast tumor growth in vivo.

Methods and compositions for diagnostic and therapeutic targeting of COX-2

The presently disclosed subject matter provides compositions that selectively bind cyclooxygenase-2 and comprise a therapeutic and/or diagnostic moiety. Also provided are methods for using the disclosed compositions for diagnosing (i.e., by imaging) a target cell and/or treating a disorder associated with a cyclooxygenase-2 biological activity.