1402586-72-4Relevant academic research and scientific papers
Discovery of N-(3-fluoro-4-methylsulfonamidomethylphenyl)urea as a potent TRPV1 antagonistic template
Ann, Jihyae,Sun, Wei,Zhou, Xing,Jung, Aeran,Baek, Jisoo,Lee, Sunho,Kim, Changhoon,Yoon, Suyoung,Hong, Sunhye,Choi, Sun,Turcios, Noe A.,Herold, Brienna K.A.,Esch, Timothy E.,Lewin, Nancy E.,Abramovitz, Adelle,Pearce, Larry V.,Blumberg, Peter M.,Lee, Jeewoo
, p. 3603 - 3607 (2016)
A series of homologous analogues of prototype antagonist 1 and its urea surrogate were investigated as hTRPV1 ligands. Through one-carbon elongation in the respective pharmacophoric regions, N-(3-fluoro-4-methylsulfonamidomethylphenyl)urea was identified as a novel and potent TRPV1 antagonistic template. Its representative compound 27 showed a potency comparable to that of lead compound 1. Docking analysis of compound 27 in our hTRPV1 homology model indicated that its binding mode was similar with that of 1S.
KINASE ANTAGONISTS AND METHODS FOR MAKING AND USING THEM
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Page/Page column 125-126, (2020/02/19)
Disclosed herein are small molecule compounds that are SGK1 antagonists, formulations and pharmaceutical compositions comprising the compounds, and methods of making and using them, for treating, ameliorating, preventing, reversing or slowing the progression of: a cancer, a tumor, a metastasis or a dysplastic or a dysfunctional cell condition responsive to inhibition of a kinase enzyme of the AGC group of kinases including SGK1, by administration of an AGC kinase inhibitor or antagonist.
Aryl or N-heteroaryl Substituted Methanesulfonamide Derivatives as Vanilloid Receptor Ligands
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Paragraph 0441; 0442, (2013/04/10)
The invention relates to aryl or N-heteroaryl substituted methanesulfonamide derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
ARYL OR N-HETEROARYL SUBSTITUTED METHANESULFONAMIDE DERIVATIVES AS VANILLOID RECEPTOR LIGANDS
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Page/Page column 51; 52, (2013/04/13)
The invention relates to aryl or N-heteroaryl substituted methanesulfonamide derivatives of Formula (I) as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
SUBSTITUTED METHANESULFONAMIDE DERIVATIVES AS VANILLOID RECEPTOR LIGANDS
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Page/Page column 42; 43; 45, (2013/04/13)
The invention relates to substituted methanesulfonamide derivatives as vanilloid receptor ligands of formula (I), to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and
AMINE SUBSTITUTED METHANESULFONAMIDE DERIVATIVES AS VANILLOID RECEPTOR LIGANDS
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Page/Page column 59, (2013/04/13)
The invention relates to amine substituted methanesulfonamide derivatives of formula (I) as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
Substituted Methanesulfonamide Derivatives as Vanilloid Receptor Ligands
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Paragraph 0270-0271, (2013/04/10)
The invention relates to substituted methanesulfonamide derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseas
Amine Substituted Methanesulfonamide Derivatives as Vanilloid Receptor Ligands
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Paragraph 0507; 0508, (2013/04/10)
The invention relates to amine substituted methanesulfonamide derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
SUBSTITUTED PYRAZOLYL-BASED CARBOXAMIDE AND UREA DERIVATIVES BEARING A PHENYL MOIETY SUBSTITUTED WITH AN N-CONTAINING GROUP AS VANILLOID RECEPTOR LIGANDS
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Page/Page column 74, (2013/05/23)
The invention relates to substituted pyrazolyl-based carboxamide and urea derivatives of formula (R) bearing a phenyl moiety substituted with an N-containing group as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
