913376-52-0Relevant 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
scheme or table, 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
Selective β-hydroxyethylation at the N-1 position of a pyrazolone: Synthesis of benzyl 1-(β-hydroxyethyl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro- 1H-pyrazole-4-carboxylate
Siegmund, Aaron,Retz, Daniel,Xi, Ning,Dominguez, Celia,Bürli, Roland,Liu, Longbin
experimental part, p. 1005 - 1008 (2009/04/06)
Selective 2-hydroxyethylation at the N-1 position of benzyl 5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxylate with epoxides was achieved using either AlMe3 or Mg(ClO4)2 under mild conditions. The epoxide ring opening was both regioselective and stereospecific. Moderate to excellent yields were obtained from mono- and disubstituted epoxides with the exception of cis-dimethyl-2-butene oxide that gave only a trace amount of the product. Georg Thieme Verlag Stuttgart.
BIS-ARYL AMIDE DERIVATIVES AND METHODS OF USE
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Page/Page column 56, (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.
