130112-64-0Relevant articles and documents
PYRIDONE COMPOUNDS AND METHODS OF USE IN THE MODULATION OF A PROTEIN KINASE
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Paragraph 01065, (2021/04/02)
The present disclosure relates generally to compounds and pharmaceutical compositions suitable as modulators of protein kinases, and methods for their use in treating disorders mediated, at least in part by, protein kinases.
Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7- oxo-7,8-dihydro-pyrido[2,3- d ]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5)
Reddy, M. V. Ramana,Akula, Balireddy,Cosenza, Stephen C.,Athuluridivakar, Saikrishna,Mallireddigari, Muralidhar R.,Pallela, Venkat R.,Billa, Vinay K.,Subbaiah, D. R. C. Venkata,Bharathi, E. Vijaya,Vasquez-Del Carpio, Rodrigo,Padgaonkar, Amol,Baker, Stacey J.,Reddy, E. Premkumar
, p. 578 - 599 (2014/03/21)
The success of imatinib, a BCR-ABL inhibitor for the treatment of chronic myelogenous leukemia, has created a great impetus for the development of additional kinase inhibitors as therapeutic agents. However, the complexity of cancer has led to recent interest in polypharmacological approaches for developing multikinase inhibitors with low toxicity profiles. With this goal in mind, we analyzed more than 150 novel cyano pyridopyrimidine compounds and identified structure-activity relationship trends that can be exploited in the design of potent kinase inhibitors. One compound, 8-cyclopentyl-2-[4-(4-methyl- piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6- carbonitrile (7x), was found to be the most active, inducing apoptosis of tumor cells at a concentration of approximately 30-100 nM. In vitro kinase profiling revealed that 7x is a multikinase inhibitor with potent inhibitory activity against the CDK4/CYCLIN D1 and ARK5 kinases. Here, we report the synthesis, structure-activity relationship, kinase inhibitory profile, in vitro cytotoxicity, and in vivo tumor regression studies by this lead compound.
AMIDOPHENOXYINDAZOLES USEFUL AS INHIBITORS OF C-MET
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Page/Page column 15, (2010/02/17)
The present invention provides amidophenoxyindazole compounds useful in the treatment of cancer.
Fluoroquinolones from imidoylketenes and iminopropadienones, RN≤C≤C≤C≤O
Fulloon, Belinda E.,Wentrup, Curt
body text, p. 115 - 120 (2009/08/15)
3-Fluoro-, 4-fluoro-, and 2,3,4-trifluorophenyliminopropadienones have been generated by flash vacuum thermolysis (FVT) of 5-[(fluoroarylamino) methoxymethylene]-2,2-dimethyldioxan-4,6-dione (Meldrum's acid) derivatives. Their reaction with methanol affor
N3-Arylmalonamides: A new series of thieno[3,2-b]pyridine based inhibitors of c-Met and VEGFR2 tyrosine kinases
Saavedra, Oscar,Claridge, Stephen,Zhan, Lijie,Raeppel, Franck,Granger, Marie-Claude,Raeppel, Stéphane,Mannion, Michael,Gaudette, Frédéric,Zhou, Nancy,Isakovic, Ljubomir,Bernstein, Naomy,Déziel, Robert,Nguyen, Hannah,Beaulieu, Normand,Beaulieu, Carole,Dupont, Isabelle,Wang, James,Macleod, A. Robert,Besterman, Jeffrey M.,Vaisburg, Arkadii
scheme or table, p. 6836 - 6839 (2010/06/19)
A family of thieno[3,2-b]pyridine based small molecule inhibitors of c-Met and VEGFR2 were designed based on lead structure 2. These compounds were shown to have IC50 values in the low nanomolar range in vitro and were efficacious in human tumo