624729-66-4Relevant articles and documents
[heteroshikuridenasetoamido[heteroshikuridenasetoamido] derivative
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Paragraph 0298, (2021/02/18)
The present invention provides, a novel method for producing a compound represented by formula (I) and a novel method for producing a compound represented by formula (B) or a salt thereof, which are intermediates in the production of formula (I).
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.
Selective Catalytic Hydrogenation of Arenols by a Well-Defined Complex of Ruthenium and Phosphorus-Nitrogen PN3-Pincer Ligand Containing a Phenanthroline Backbone
Li, Huaifeng,Wang, Yuan,Lai, Zhiping,Huang, Kuo-Wei
, p. 4446 - 4450 (2017/07/24)
Selective catalytic hydrogenation of aromatic compounds is extremely challenging using transition-metal catalysts. Hydrogenation of arenols to substituted tetrahydronaphthols or cyclohexanols has been reported only with heterogeneous catalysts. Herein, we demonstrate the selective hydrogenation of arenols to the corresponding tetrahydronaphthols or cyclohexanols catalyzed by a phenanthroline-based PN3-ruthenium pincer catalyst.
Tetrahydro-naphthols as orally available TRPV1 inhibitors
Urbahns, Klaus,Yura, Takeshi,Gupta, Jang B.,Tajimi, Masaomi,Fujishima, Hiroshi,Masuda, Tsutomu,Yamamoto, Noriyuki,Ikegami, Yuka,Marumo, Makiko,Yasoshima, Kayo,Yoshida, Nagahiro,Moriwaki, Toshiya,Madge, David,Chan, Fiona,Mogi, Muneto
scheme or table, p. 3408 - 3411 (2012/06/29)
Starting from a naphthol-based lead series with low oral bioavailability, we have identified potent TRPV1 antagonists with oral bioavailability in rats. These compounds emerged from SAR studies aimed at replacing the lead's phenol structure whilst maintai
Synthesis and biological evaluation of 5-substituted and 4,5-disubstituted-2-arylamino oxazole TRPV1 antagonists
Perner, Richard J.,Koenig, John R.,Didomenico, Stanley,Gomtsyan, Arthur,Schmidt, Robert G.,Lee, Chih-Hung,Hsu, Margaret C.,McDonald, Heath A.,Gauvin, Donna M.,Joshi, Shailen,Turner, Teresa M.,Reilly, Regina M.,Kym, Philip R.,Kort, Michael E.
supporting information; experimental part, p. 4821 - 4829 (2010/08/06)
The synthesis and structure-activity relationships of a series of 5-monosubstituted and 4,5-disubstituted 2-arylaminooxazoles as novel antagonists of the transient receptor potential vanilloid 1 (TRPV1) receptor are described. The 7-hydroxy group of the t
TRPV1 ANTAGONISTS
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Page/Page column 41, (2010/04/30)
Disclosed herein are compounds of Formula (I), or pharmaceutically acceptable salts, solvates, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and m are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
TRPV1 ANTAGONISTS
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Page/Page column 39-40, (2010/04/30)
Disclosed herein are compounds of formula (I), or pharmaceutically acceptable salts, solvates, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and m are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
SUBSTITUTED AROMATIC CARBOXAMIDE AND UREA DERIVATIVES AS VANILLOID RECEPTOR LIGANDS
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Page/Page column 148; 150, (2010/11/18)
The invention relates to substituted aromatic carboxamide and urea derivatives, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions (formula (I)).
TRPV1 ANTAGONISTS
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Page/Page column 12, (2009/05/28)
Compounds of formula (I) wherein R1, R2, R4, and W are defined in the description are TRPV 1 antagonists with CNS penetration. Compositions comprising such compounds and methods for treating conditions and disorders using
ANTAGONISTS OF THE TRPV1 RECEPTOR AND USES THEREOF
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Page/Page column 13, (2008/12/06)
The present application is directed to compounds that are TRPV1 antagonists and have formula (I) wherein variables Ar1, L1, R1, R2, R3, R4, R5, Y1, Y2, and Y3, are as defined in the description, which are useful for treating disorders caused by or exacerbated by vanilloid receptor activity.