911430-99-4

Upstream product

• 1761-61-1 5-bromosalicyclaldehyde 
• 457611-34-6 N'-[1-(5-Bromo-2-hydroxy-phenyl)-meth-(E)-ylidene]-hydrazinecarboxylic acid tert-butyl ester 
• 851205-58-8 N'-(5-bromo-2-hydroxy-benzyl)-hydrazinecarboxylic acid tert-butyl ester 

Downstream Products

• 851205-56-6 1-(5-bromo-2-hydroxybenzyl)-5-methyl-1H-pyrazole-3-carboxylic acid ethyl ester 
• 913566-79-7 ethyl 1-[(5-bromo-2-{[(2,4-dichlorophenyl)methyl]oxy}phenyl)methyl]-5-methyl-1H-pyrazole-3-carboxylate 
• 913566-78-6 ethyl 1-[(5-bromo-2-{[(2,4-difluorophenyl)methyl]oxy}phenyl)methyl]-5-methyl-1H-pyrazole-3-carboxylate 

Relevant academic research and scientific papers

Identification of novel pyrazole acid antagonists for the EP1 receptor

The discovery, synthesis and structure-activity relationship (SAR) of a novel series of EP1 receptor antagonists is described. Pyrazole acid 4, identified from a chemical array, had desirable physicochemical properties, an excellent in vitro microsomal inhibition and cytochrome P450 (CYP450) profile and good exposure levels in blood. This compound had an ED50 of 1.3 mg/kg in a rat pain model. A range of more potent analogues in the in vitro assay was identified using efficient array chemistry. These EP1 antagonists have potential as agents in the treatment of PGE2 mediated pain.

PYRAZOLE COMPOUNDS AS PROSTAGLANDIN RECEPTORS LIGANDS

Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein Z, R1 ,R2a, R2b, R10, R11 and Rx are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.