- 4-Quinazolinyloxy-diaryl ureas as novel BRAFV600E inhibitors
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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.
- 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
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p. 5342 - 5346
(2011/10/09)
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- QUINAZOLINE COMPOUNDS
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Disclosed are compounds having the formula: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein, and methods of making and using the same.
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Page/Page column 40-41
(2011/06/11)
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- QUINAZOLINE DERIVATIVES AS RAF KINASE MODULATORS AND METHODS OF USE THEREOF
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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.
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Page/Page column 173
(2009/10/22)
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