151067-74-2Relevant academic research and scientific papers
Heteroaryl β-tetralin ureas as novel antagonists of human TRPV1
Jetter, Michele C.,Youngman, Mark A.,McNally, James J.,McDonnell, Mark E.,Zhang, Sui-Po,Dubin, Adrienne E.,Nasser, Nadia,Codd, Ellen E.,Flores, Christopher M.,Dax, Scott L.
, p. 6160 - 6163 (2007)
We report on a series of α-substituted-β-tetralin-derived and related phenethyl-based isoquinolinyl and hydroxynaphthyl ureas as potent antagonists of the human TRPV1 receptor. The synthesis and Structure-activity relationships (SAR) of the series are described.
7-Hydroxynaphthalen-1-yl-urea and -amide antagonists of human vanilloid receptor 1
McDonnell, Mark E.,Zhang, Sui-Po,Nasser, Nadia,Dubin, Adrienne E.,Dax, Scott L.
, p. 531 - 534 (2004)
A series of structurally simple 7-hydroxynaphthalenyl ureas and amides were discovered to be potent ligands of human vanilloid receptor 1 (VR1). 1-(7-Hydroxynaphthalen-1-yl)-3-(4-trifluoromethylbenzyl)urea 5f exhibited nanomolar binding affinity (Ki=1.0 nM) and upon capsaicin challenge, behaved as a potent functional antagonist (IC50=4 nM). The synthesis and structure-activity relationships (SARs) for the series are described.
Discovery of dual-acting opioid ligand and TRPV1 antagonists as novel therapeutic agents for pain
Lee, Hobin,Ahn, Songyeon,Ann, Jihyae,Ha, Heejin,Yoo, Young Dong,Kim, Young Ho,Hwang, Ji-Young,Hur, Kwang-Hyun,Jang, Choon-Gon,Pearce, Larry V.,Esch, Timothy E.,Lewin, Nancy E.,Blumberg, Peter M.,Lee, Jeewoo
, (2019/09/03)
In order to discover a novel type of analgesic, we investigated dual activity ligands with TRPV1 antagonism and mu-opioid receptor affinity with the goal of eliciting synergistic analgesia while avoiding the side effects associated with single targeting.
ETHER DERIVATIVE
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Page/Page column 33, (2008/06/13)
The present invention relates to an ether derivative represented by the formula (I), a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof wherein each symbol is as defined in the description, and an ether derivative represented by the formula (III), a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof wherein each symbol is as defined in the description; a pharmaceutical composition containing the ether derivative; and a package containing the pharmaceutical composition and a description of use thereof. A pharmaceutical composition of the present invention, which contains this compound of the present invention has a superior anti-inflammatory and analgesic activity and is useful as various pharmaceutical agents such as an anti-inflammatory agent, an analgesic, a therapeutic agent for inflammatory bowel disease, a therapeutic agent for pollakiuria and/or incontinentia, a therapeutic agent for asthma and the like.
Heat-sensitive recording materials and phenol compounds
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, (2008/06/13)
Heat-sensitive recording materials contain an electron-donating chromogenic compound and an electron-attracting compound. The recording materials also contain at least one compound represented by the following formula: STR1 wherein R1 and R3 mean a hydrogen atom or an alkyl, aralkyl or aryl group, R2 and R4 denote an alkyl, alkenyl, aralkyl or aryl group, X1, X2, Y1 and Y2 stand for an oxygen or a sulfur atom, and --Z1 -- and --Z2 -- are a specific aromatic group. Also provided are phenol compounds represented by the following formula: STR2 wherein R1, R2, X1 and Y1 have the same meanings as defined above; R5 and R6 are a hydrogen or halogen atom or an alkyl, alkoxy, aralkyl, aryl or hydroxyl group; p and q stand for an integer of 1-4; R5 and R6 may be either the same or different when p and q represent an integer of 2 or greater; and --Z3 -- means a specific divalent group.
