913376-56-4Relevant academic research and scientific papers
Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series
Liu, Longbin,Norman, Mark H.,Lee, Matthew,Xi, Ning,Siegmund, Aaron,Boezio, Alessandro A.,Booker, Shon,Choquette, Debbie,D'Angelo, Noel D.,Germain, Julie,Yang, Kevin,Yang, Yajing,Zhang, Yihong,Bellon, Steven F.,Whittington, Douglas A.,Harmange, Jean-Christophe,Dominguez, Celia,Kim, Tae-Seong,Dussault, Isabelle
, p. 1868 - 1897 (2012/05/04)
As part of our effort toward developing an effective therapeutic agent for c-Met-dependent tumors, a pyrazolone-based class II c-Met inhibitor, N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)-3-fluorophenyl)-1,5-dimethyl-3-oxo-2- phenyl-2,3-dihydro-1H-pyrazole-4-c
Discovery of a potent, selective, and orally bioavailable c-met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl) -5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458)
Liu, Longbin,Siegmund, Aaron,Xi, Ning,Kaplan-Lefko, Paula,Rex, Karen,Chen, April,Lin, Jasmine,Moriguchi, Jodi,Berry, Loren,Huang, Liyue,Teffera, Yohannes,Yang, Yajing,Zhang, Yihong,Bellon, Steven F.,Lee, Matthew,Shimanovich, Roman,Bak, Annette,Dominguez, Celia,Norman, Mark H.,Harmange, Jean-Christophe,Dussault, Isabelle,Kim, Tae-Seong
supporting information; experimental part, p. 3688 - 3691 (2009/04/11)
Deregulation of the receptor tyrosine kinase c-Met has been implicated in human cancers. Pyrazolones with N-1 bearing a pendent hydroxyalkyl side chain showed selective inhibition of c-Met over VEGFR2. However, studies revealed the generation of active, n
BIS-ARYL AMIDE DERIVATIVES AND METHODS OF USE
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Page/Page column 56-57, (2008/12/07)
Selected compounds are effective for prophylaxis and treatment of diseases, such as c Met mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
SUBSTITUTED AMIDE DERIVATIVES AS PROTEIN KINASE INHIBITORS
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Page/Page column 116-117, (2008/06/13)
Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
