Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3- d ]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells
The RAS-RAF-MEK-MAPK cascade is an essential signaling pathway, with activation typically mediated through cell surface receptors. The kinase inhibitors vemurafenib and dabrafenib, which target oncogenic BRAF V600E, have shown significant clinical efficac
Henry, James R.,Kaufman, Michael D.,Peng, Sheng-Bin,Ahn, Yu Mi,Caldwell, Timothy M.,Vogeti, Lakshminarayana,Telikepalli, Hanumaiah,Lu, Wei-Ping,Hood, Molly M.,Rutkoski, Thomas J.,Smith, Bryan D.,Vogeti, Subha,Miller, David,Wise, Scott C.,Chun, Lawrence,Zhang, Xiaoyi,Zhang, Youyan,Kays, Lisa,Hipskind, Philip A.,Wrobleski, Aaron D.,Lobb, Karen L.,Clay, Julia M.,Cohen, Jeffrey D.,Walgren, Jennie L.,McCann, Denis,Patel, Phenil,Clawson, David K.,Guo, Sherry,Manglicmot, Danalyn,Groshong, Chris,Logan, Cheyenne,Starling, James J.,Flynn, Daniel L.
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(2015/06/08)
RAF INHIBITOR COMPOUNDS
This invention provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula (I); and use of a compound of Formula (I) for treating specified cancers.
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(2013/09/26)
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