673-09-6Relevant academic research and scientific papers
ANTI-MUCUS DRUGS AND USES THEREFOR
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Paragraph 0199; 0201, (2015/07/15)
Disclosed are methods of identifying, generating and synthesizing compounds that inhibit MAPK13 activity. In various embodiments, compounds, salts thereof and prodrugs thereof of the present teachings can be useful for the treatment of diseases and disord
Design, synthesis and characterization of N', N''- Diaryl ureas as p38 kinase inhibitors
Kulkarni, Ravindra G.,Laufer, Stefan,Mangannavar, Chandrashekhar,Garlapati, Achaiah
, p. 213 - 221 (2013/07/28)
Kinases have been known as important molecular targets for various diseases and p38 kinase is found to be vital target among all mitogen activated protein kinases for inflammatory diseases. P38 kinase inhibitors bearing urea scaffold have shown potent kinase inhibitory activity and also selectivity over other kinases. We present here the synthesis, p38 kinase inhibitory and anti-inflammatory activities of compounds containing N', N''-diarylurea scaffold. Compound 7f demonstrated IC50 value of 1.09 μM in p38 kinase assay and 79.41% inhibition of rat paw edema at the 2nd hour of carrageenan challenge. The molecular docking studies of synthesized compounds indicated some of the important hydrogen bonding interactions and also revealed the minor change in the binding pose when compared to BIRB796.
QUINOLINE DERIVATIVES FOR MODULATING DNA METHYLATION
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Page/Page column 142, (2008/06/13)
Quinoline derivatives, particularly 4-anilinoquinoline derivatives, are provided. Such quinoline derivatives can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position, for example via selective inhibition of DNA methyltransferase DNMT1. Methods for synthesizing numerous 4-anilinoquinoline derivatives and for modulating DNA methylation are provided. Also provided are methods for formulating and administering these compounds or compositions to treat conditions such as cancer and hematological disorders.
INHIBITION OF RAF KINASE USING ARYL AND HETEROARYL SUBSTITUTED HETEROCYCLIC UREAS
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Page/Page column 15, (2010/11/08)
Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.
ANTIPROLIFERATIVE 2-(SULFO-PHENYL)-AMINOTHIAZOLE DERIVATIVES
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Page 84-85, (2010/02/08)
Aminothiazole compounds substituted with sulfur-containing groups are represented by the Formula (I), and their pharmaceutically acceptable salts, prodrugs, active metabolites, and pharmaceutically acceptable salts of said metabolites are described. These agents modulate and/or inhibit the cell proliferation and activity of protein kinases and are useful as pharmaceuticals for treating malignancies and other disorders.
Rho-kinase inhibitors
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Page/Page column 12-14, (2008/06/13)
Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., c
INHIBITION OF RAF KINASE USING QUINOLYL, ISOQUINOLYL OR PYRIDYL UREAS
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Page/Page column 17, (2010/11/29)
This invention relates to a group of quinolyl, isoquinolyl and pyridyl ureas, their the use in treating raf mediated diseases, and pharmaceutical compositions which contain these ureas for use in such therapy.
Heteroaryl ureas containing nitrogen hetero-atoms as p38 kinase inhibitors
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, (2008/06/13)
This invention relates to the use of a group of heteroaryl ureas containing nitrogen in treating p38 mediated diseases, and pharmaceutical compositions for use in such therapy.
Discovery of FR115092 : A novel antinephritic agent
Ogino, Takashi,Tsuji, Kiyoshi,Tojo, Takashi,Igari, Norihiro,Seki, Nobuo,Sudo, Yu,Manda, Toshitaka,Nishigaki, Fusako,Matsuo, Masaaki
, p. 75 - 80 (2007/10/03)
A series of dapsone-related 4-aminophenyl and 2-aminothiazolyl derivatives was prepared, and their antinephritic activity and blood toxicity were evaluated. 5-(2-Pyridylsulfonyl)-2-thiazolamine (FR115092,26) was effective against two nephritis models, namely graft-versus-host disease (GVHD) and autoimmune W/BF1 mice, and showed none of the blood toxicity observed with dapsone.
