1002128-17-7

Upstream product

• 2960-66-9 4-oxo-but-2-enoic acid ethyl ester 
• 1002127-25-4 ethyl (2E,4Z)-5-bromo-5-(4-trifluoromethylphenyl)-2,4-pentadienoate 
• 1002127-15-2 ethyl (E)-5,5-dibromo-2,4-pentadienoate 
• 1002128-15-5 ethyl (2E,4Z)-5-(4-hydroxyphenyl)-5-(4-trifluoromethylphenyl)-2,4-pentadienoate 
• 2919-23-5 cyclobutanol 

Downstream Products

• 1002128-16-6 (2E,4Z)-5-(4-cyclobutoxyphenyl)-5-[4-(trifluoromethyl)phenyl]-2,4-pentadienoic acid 
• 1002125-37-2 (2E,4Z)-5-(4-cyclobutoxyphenyl)-N-(3-hydroxy-2-oxo-1,2,3,4-tetrahydro-5-quinolyl)-5-(4-trifluoromethylphenyl)-2,4-pentadienamide 

Relevant academic research and scientific papers

Discovery of novel 5,5-diarylpentadienamides as orally available transient receptor potential vanilloid 1 (TRPV1) antagonists

We have developed a novel and potent chemical series of 5,5-diphenylpentadienamides for targeting TRPV1 in vitro and in vivo. In this investigation, we examined a variety of replacements for the 5-position of dienamides with the goal of addressing issues related to pharmacokinetics. Our data suggest that substitution with alkoxy groups on the phenyl ring at the 5-position increases their ability to penetrate the blood-brain barrier. This investigation culminated in the discovery of compound (R)-36b, which showed a good pharmacokinetic profile. In vivo, compound (R)-36b was found to be effective at reversing mechanical allodynia in rats in a dose-dependent manner, and it reversed thermal hyperalgesia in a model of neuropathic pain induced by sciatic nerve injury.

PENTADIENAMIDE DERIVATIVE

The present invention provides a pentadienamide derivative represented by the formula (I): (wherein R1 represents substituted or unsubstituted aryl or a substituted or unsubstituted aromatic heterocyclic group; R2 represents substitu