1002126-19-3

Upstream product

• 280566-45-2 2-chloro-6-(trifluoromethyl)pyridine-3-carboxylic acid 
• 184956-71-6 6'-Trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2']bipyridinyl-3'-carboxylic acid 
• 1002129-21-6 C₂₂H₂₀F₄N₂O₂ 
• 292143-04-5 5-amino-3-hydroxy-3,4-dihydroquinolin-2(1H)-one 
• 1002129-27-2 C₂₃H₂₂F₄N₂O₂ 
• 1002129-26-1 C₂₀H₁₈F₄N₂O 
• 1002129-25-0 C₂₀H₂₀F₄N₂O 
• 1002129-24-9 C₂₂H₂₂F₄N₂O₂ 
• 1002129-23-8 C₁₈H₁₆F₄N₂O 
• 1002129-22-7 C₁₄H₁₈F₃N₃O₂ 
• 110-89-4 piperidine 

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