97267-60-2Relevant academic research and scientific papers
HETEROCYCLIC NLRP3 MODULATORS, FOR USE IN THE TREATMENT OF CANCER
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Page/Page column 63-64, (2020/07/31)
The present invention provides compounds of Formula (I): wherein all of the variables are as defined herein. These compounds are modulators of NLRP3, which may be used as medicaments for the treatment of proliferative disorders, such as cancer in a subjec
Aurora Kinase Modulators and Method of Use
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, (2014/11/27)
The present invention relates to chemical compounds having a general formula I wherein A1-8, D′, L1, L2, R1, R6-8 and n are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of such kinases. For example, the compounds are capable of modulating Aurora kinase thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.
Discovery of 7-aryl-substituted (1,5-naphthyridin-4-yl)ureas as Aurora kinase inhibitors
Defaux, Julien,Antoine, Maud,Le Borgne, Marc,Schuster, Tilmann,Seipelt, Irene,Aicher, Babette,Teifel, Michael,Guenther, Eckhard,Gerlach, Matthias,Marchand, Pascal
, p. 217 - 232 (2014/01/17)
As part of our research projects to identify new chemical entities of biological interest, we developed a synthetic approach and the biological evaluation of (7-aryl-1,5-naphthyridin-4-yl)ureas as a novel class of Aurora kinase inhibitors for the treatment of malignant diseases based on pathological cell proliferation. 1,5-Naphthyridine derivatives showed excellent inhibitory activities toward Aurora kinases A and B, and the most active compound, 1-cyclopropyl-3-[7-(1-methyl-1H-pyrazol-4-yl)-1,5-naphthyridin-4-yl]urea (49), displayed IC50 values of 13 and 107 nM against Aurora kinases A and B, respectively. In addition, the selectivity toward a panel of seven cancer-related protein kinases was highlighted. In vitro ADME properties were also determined in order to rationalize the difficulties in correlating antiproliferative activity with Aurora kinase inhibition. Finally, the good safety profile of these compounds imparts promising potential for their further development as anticancer agents. Promising Aurora inhibitors: Herein we report a series of (7-aryl-1,5-naphthyridin-4-yl)ureas as a novel class of nanomolar-range Aurora kinase inhibitors. The described derivatives have good cell-penetration parameters and safety profiles, but their efficiency toward signaling pathways are insufficient to induce cell death. We also highlight their selectivity toward a panel of seven cancer-related protein kinases. Copyright
AURORA KINASE MODULATORS AND METHOD OF USE
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, (2008/12/04)
The present invention relates to chemical compounds having a general formula I {INSERT STRUCTURE HERE} wherein A1-8, D,, L1, L2, R1, R6-8 and n are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of such kinases. For example, the compounds are capable of modulating Aurora kinase thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.
ARYL SUBSTITUTED IMIDAZONAPHTHYRIDINES
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Page/Page column 66, (2008/06/13)
Imidazonaphthyridine ring systems substituted with an aryl substituent, pharmaceutical compositions containing the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of
SUBSTITUTED IMIDAZOQUINOLINES, IMIDAZOPYRIDINES, AND IMIDAZONAPHTHYRIDINES
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Page/Page column 222, (2010/10/20)
Imidazo-quinoline, -pyridine, and -naphthyridine ring systems (particularly quinolines, tetrahydroquinolines, pyridines, [1,5]naphthyridines, [1,5]tetrahydronaphthyridines) substituted at the 1-position with a cyclic substituent, pharmaceutical compositions containing the compounds, methods of making these compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
NITROGEN-CONTAINING HETEROCYCLYL SUBSTITUTED IMIDAZOQUINOLINES AND IMIDAZONAPHTHYRIDINES
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Page/Page column 69, (2010/02/15)
Imidazoquinoline and imidazonaphthyridine compounds having a nitrogen-containing heterocyclyl substituent at the 5-, 6-, 7-, or 8-position, pharmaceutical compositions containing the compounds, intermediates, and methods of making and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
OXIME SUBSTITUTED IMIDAZO-CONTAINING COMPOUNDS
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Page/Page column 197, (2008/06/13)
Imidazo-containing compounds (e.g., imidazoquinolines, imidazonaphthyridines, and imidazopyridines) with an oxime substituent at the 1-position, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
