895244-45-8Relevant articles and documents
4-Quinazolinyloxy-diaryl ureas as novel BRAFV600E inhibitors
Holladay, Mark W.,Campbell, Brian T.,Rowbottom, Martin W.,Chao, Qi,Sprankle, Kelly G.,Lai, Andiliy G.,Abraham, Sunny,Setti, Eduardo,Faraoni, Raffaella,Tran, Lan,Armstrong, Robert C.,Gunawardane, Ruwanthi N.,Gardner, Michael F.,Cramer, Merryl D.,Gitnick, Dana,Ator, Mark A.,Dorsey, Bruce D.,Ruggeri, Bruce R.,Williams, Michael,Bhagwat, Shripad S.,James, Joyce
, p. 5342 - 5346 (2011)
Aryl phenyl ureas with a 4-quinazolinoxy substituent at the meta-position of the phenyl ring are potent inhibitors of mutant and wild type BRAF kinase. Compound 7 (1-(5-tert-butylisoxazol-3-yl)-3-(3-(6,7-dimethoxyquinazolin-4-yloxy) phenyl)urea hydrochloride) exhibits good pharmacokinetic properties in rat and mouse and is efficacious in a mouse tumor xenograft model following oral dosing.
QUINAZOLINE DERIVATIVES AS RAF KINASE MODULATORS AND METHODS OF USE THEREOF
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Page/Page column 181, (2009/10/22)
Compounds according to formula (I), compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases. Formula (I): or a pharmaceutically acceptable salt, solvate, clathrate of hydrate thereof, wherein X is O or S(O)t; Ra is O or S.