910485-24-4

Upstream product

• 939-97-9 4-tert-Butylbenzaldehyde 
• 158010-17-4 ethyl (E)-3-[4-(tert-butylphenyl)]-2-propenoate 
• 105393-24-6 2-[4-(tert-butyl)phenyl]cyclopropylmethanol 
• 117721-77-4 (E)-3-(4-(tert-butyl)phenyl)prop-2-en-1-ol 
• 445029-32-3 2-[4-(tert-butyl)phenyl]cyclopropanecarboxylic acid 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of B-region modified diarylalkyl amide analogues as novel TRPV1 antagonists

Design, synthesis and biological evaluation of B-region, known to be a dipolar interacting pharmacophore, modified diarylalkyl amide analogues for novel TRPV1 (transient receptor potential channel, vanilloid subfamily member 1) antagonists was described. A variety of moieties including guanidines, heterocyclic rings, cinnamides, and α-substituted acetamides were introduced at the B-region. TRPV1 antagonistic activities of these analogues were evaluated by 45Ca2+ uptake assay in rat DRG neuron. In particular, α,α-difluoroamide 53 exhibited 3-fold more potent TRPV1 antagonistic activity (IC50 = 0.058 μM) than the parent amide analogue 6.

NOVEL COMPOUNDS, ISOMER THEREOF OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF AS VANILLOID RECEPTOR ANTAGONIST; AND A PHARMACEUTICAL COMPOSITION CONTAINING THE SAME

This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1 )antagonist; and a pharmaceutical composition containing the same. The present invention