285984-47-6Relevant academic research and scientific papers
MITOGEN-ACTIVATED PROTEIN KINASE INHIBITORS, METHODS OF MAKING, AND METHODS OF USE THEREOF
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, (2019/12/25)
Compounds that inhibit mitogen-activated protein kinases (MAPKs) are disclosed. Some inhibitor compounds specifically target a single MAPK such as MAPK13, while others target multiple MAPKs such as MAPK13 and MAPK12. The compounds can be used therapeutica
ANTI-MUCUS DRUGS AND USES THEREFOR
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, (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
INHIBITOR OF p38 MAP KINASE
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, (2015/09/22)
A compound has the following formula: The compound is a p38 MAP kinase inhibitor. The compound and its pharmaceutically acceptable salts can be used for treatment of conditions, such as inflammatory diseases.
PYRAZOLE DERIVATIVES AS P38 MAP INHIBITORS
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Paragraph 0557; 0558, (2015/07/27)
Compounds of formula (I): wherein R1, R2, J, Q, V, X, Y and Z are defined herein are disclosed. The compounds are inhibitors of the family of p38 mitogen-activated protein kinase enzymes (referred to herein as p38 MAP kinase inhibitors), particularly the alpha sub-type thereof, and of Syk kinase and the Src family of tyrosine kinases. The compounds may be used in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, in particular inflammatory diseases of the lung, such as asthma and COPD, as well as those of the gastrointestinal tract, such as ulcerative colitis and Crohn's disease and of the eye, such as uveitis.
INTERMEDIATES FOR USE IN THE PREPARATION OF INDAZOLE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF
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Paragraph 00169, (2014/09/16)
Provided herein are novel processes for preparing a compound of Formula (I) to the use of said compound as an intermediate in novel processes for the synthesis of indazole derivatives, and to indazole intermediates and derivatives prepared by the processe
PYRAZOLE DERIVATIVES AS P38 MAP INHIBITORS
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Page/Page column 70, (2014/03/25)
Compounds of formula (I) wherein R1, R2, J, Q, V, X, Y and Z are defined herein are disclosed. The compounds are inhibitors of the family of p38 mitogen-activated protein kinase enzymes (referred to herein as p38 MAP kinase inhibitors), particularly the alpha sub-type thereof, and of Syk kinase and the Src family of tyrosine kinases. The compounds may be used in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, in particular inflammatory diseases of the lung, such as asthma and COPD, as well as those of the gastrointestinal tract, such as ulcerative colitis and Crohn's disease and of the eye, such as uveitis.
Fragment-based discovery of focal adhesion kinase inhibitors
Graedler, Ulrich,Bomke, Joerg,Musil, Djordje,Dresing, Verena,Lehmann, Martin,Hoelzemann, Guenter,Greiner, Hartmut,Esdar, Christina,Krier, Mireille,Heinrich, Timo
, p. 5401 - 5409 (2013/09/23)
Chemically diverse fragment hits of focal adhesion kinase (FAK) were discovered by surface plasmon resonance (SPR) screening of our in-house fragment library. Site specific binding of the primary hits was confirmed in a competition setup using a high-affi
1-Pyrazolyl-3-(4-((2-anilinopyrimidin-4-yl)oxy)napththalen-1-yl)ureas as p38 MAP kinase inhibitors
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Paragraph 0088; 0089, (2013/04/23)
There are provided compounds of formula (I) which are inhibitors of the family of p38 mitogen-activated protein kinase enzymes, and to their use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, in
Development of novel, highly potent inhibitors of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF): Increasing cellular potency through optimization of a distal heteroaromatic group
Suijkerbuijk, Bart M.J.M.,Niculescu-Duvaz, Ion,Gaulon, Catherine,Dijkstra, Harmen P.,Niculescu-Duvaz, Dan,Ménard, Delphine,Zambon, Alfonso,Nourry, Arnaud,Davies, Lawrence,Manne, Helen A.,Friedlos, Frank,Ogilvie, Lesley M.,Hedley, Douglas,Lopes, Filipa,Preece, Natasha P.U.,Moreno-Farre, Javier,Raynaud, Florence I.,Kirk, Ruth,Whittaker, Steven,Marais, Richard,Springer, Caroline J.
supporting information; experimental part, p. 2741 - 2756 (2010/09/04)
We describe the design, synthesis, and optimization of a series of new inhibitors of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF), a kinase whose mutant form (V600E) is implicated in several types of cancer, with a particularly high frequency in melanoma. Our previously described inhibitors with a tripartite A-B-C system (where A is a hinge binding pyrido[4,5-b] imidazolone system, B is an aryl spacer group, and C is a heteroaromatic group) were potent against purified V600EBRAF in vitro but were less potent in accompanying cellular assays. Substitution of different aromatic heterocycles for the phenyl based C-ring is evaluated herein as a potential means of improving the cellular potencies of these inhibitors. Substituted pyrazoles, particularly 3-tert-butyl-1-aryl-1H-pyrazoles, increase the cellular potencies without detrimental effects on the potency on isolated V600EBRAF. Thus, compounds have been synthesized that inhibit, with low nanomolar concentrations, V600EBRAF, its downstream signaling in cells [as measured by the reduction of the phosphorylation of extracellular regulated kinase (ERK)], and the proliferation of mutant BRAF-dependent cells. Concomitant benefits are good oral bioavailability and high plasma concentrations in vivo.
KINASE INHIBITORS AND METHODS OF USE THEREOF
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Page/Page column 56-57, (2008/06/13)
The compound of Formula (I) and pharmaceutically acceptable salts and prodrugs thereof are useful in the treatment and prevention of various disorders mediated by kinases.
