821791-59-7Relevant academic research and scientific papers
Compound with cell proliferative resistance activity, preparation method and application
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Paragraph 0074; 0075; 0111; 0113; 0193; 0194; 0195; 0196, (2018/08/03)
The invention relates to a compound with cell proliferative resistance activity, a preparation method and application. The invention discloses a compound with cell proliferative resistance activity, as shown in formula I, pharmaceutically acceptable salt
NOVEL ANTIFUNGAL OXODIHYDROPYRIDINECARBOHYDRAZIDE DERIVATIVE
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Paragraph 353; 354, (2015/05/06)
The present invention relates to novel oxodihydropyridinecarbohydrazide derivatives with excellent antifungal activities, an antifungal composition containing the same, and its use for the prevention and treatment of fungal infectious diseases. The oxodihydropyridinecarbohydrazide derivatives of the present invention have excellent antifungal and fungicidal activities, and thus will be useful for the prevention and treatment of various fungal infections by Candida spp., Aspergillus spp., Cryptococcus neoformans and Trichophyton spp., etc. Additionally, the oxodihydropyridinecarbohydrazide derivatives of the present invention, unlike other fungicidal preparations, can be orally administered.
4-Anilino-5-carboxamido-2-pyridone derivatives as noncompetitive inhibitors of mitogen-activated protein kinase kinase
Spicer, Julie A.,Rewcastle, Gordon W.,Kaufman, Michael D.,Black, Shannon L.,Plummer, Mark S.,Denny, William A.,Quin III, John,Shahripour, Aurash B.,Barrett, Stephen D.,Whitehead, Christopher E.,Milbank, Jared B. J.,Ohren, Jeffrey F.,Gowan, Richard C.,Omer, Charles,Camp, Heidi S.,Esmaeil, Nadia,Moore, Kelley,Sebolt-Leopold, Judith S.,Pryzbranowski, Sally,Merriman, Ronald L.,Ortwine, Daniel F.,Warmus, Joseph S.,Flamme, Cathlin M.,Pavlovsky, Alexander G.,Tecle, Haile
, p. 5090 - 5102 (2008/03/13)
A new series of MEK1 inhibitors, the 4-anilino-5-carboxamido-2-pyridones, were designed and synthesized using a combination of medicinal chemistry, computational chemistry, and structural elucidation. The effect of variation in the carboxamide side chain,
Potent and selective mitogen-activated protein kinase kinase (MEK) 1,2 inhibitors. 1. 4-(4-bromo-2-fluorophenylamino)-1-methylpyridin-2(1h)-ones
Wallace, Eli M.,Lyssikatos, Joseph,Blake, James F.,Seo, Jeongbeob,Yang, Hong Woon,Yeh, Tammie C.,Perrier, Michele,Jarski, Heidi,Marsh, Vivienne,Poch, Gregory,Livingston, Michelle Goyette,Otten, Jennifer,Hingorani, Gary,Woessner, Rich,Lee, Patrice,Winkler, James,Koch, Kevin
, p. 441 - 444 (2007/10/03)
The role of MEK 1,2 in cancer tumorgenesis has been clearly demonstrated preclinically, and two selective inhibitors are currently undergoing clinical evaluation to determine their role in the human disease. We have discovered 4-(4-bromo-2-fluorophenylamino)-1-methylpyridin-2(1H)-ones as a new class of ATP noncompetitive MEK inhibitors. These inhibitors exhibit excellent cellular potency and good pharmacokinetic properties and have demonstrated the ability to inhibit ERK phosphorylation in HT-29 tumors from mouse xenograft studies.
5-SUBSTITUTED-4-`(SUBSTITUTED PHENYL)!AMINO!-2-PYRIDONE DEVIATIVES FOR USE AS MEK INHIBITORS
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Page 92, (2010/02/10)
The present invention relates to 5-substituted-4-(substituted) phenylamino-2-pyridone derivatives of formula (I), pharmaceutical compositions and methods of use thereof as MEK inhibitors. Formula (I) wherein W is formula (II), formula (III), formula (IV),
Heterocyclic inhibitors of MEK and methods of use thereof
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, (2008/06/13)
Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, W, X and Y are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.
