6127-11-3Relevant academic research and scientific papers
Discovery of GNF-5837, a selective TRK inhibitor with efficacy in rodent cancer tumor models
Albaugh, Pam,Fan, Yi,Mi, Yuan,Sun, Fangxian,Adrian, Francisco,Li, Nanxin,Jia, Yong,Sarkisova, Yelena,Kreusch, Andreas,Hood, Tami,Lu, Min,Liu, Guoxun,Huang, Shenlin,Liu, Zuosheng,Loren, Jon,Tuntland, Tove,Karanewsky, Donald S.,Seidel, H. Martin,Molteni, Valentina
supporting information; experimental part, p. 140 - 145 (2012/04/10)
Neurotrophins and their receptors (TRKs) play key roles in the development of the nervous system and the maintenance of the neural network. Accumulating evidence points to their role in malignant transformations, chemotaxis, metastasis, and survival signaling and may contribute to the pathogenesis of a variety of tumors of both neural and non-neural origin. By screening the GNF kinase collection, a series of novel oxindole inhibitors of TRKs were identified. Optimization led to the identification of GNF-5837 (22), a potent, selective, and orally bioavailable pan-TRK inhibitor that inhibited tumor growth in a mouse xenograft model derived from RIE cells expressing both TRKA and NGF. The properties of 22 make it a good tool for the elucidation of TRK biology in cancer and other nononcology indications.
Indolin-2-one p38α inhibitors I: Design, profiling and crystallographic binding mode
Eastwood, Paul,González, Jacob,Gómez, Elena,Vidal, Bernat,Caturla, Francisco,Roca, Ramón,Balagué, Cristina,Orellana, Adelina,Domínguez, María
, p. 4130 - 4133 (2011/08/10)
The use of structure-based design and molecular modeling led to the discovery of indolin-2-one derivatives as potent and selective p38α inhibitors. The predicted binding mode was confirmed by X-ray crystallography.
New substituted spiro[cycloalkyl-1,3'-indo]-2'(1'H)-one derivatives and their use as p38 mitogen-activated kinase inhibitors
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Page/Page column 29, (2009/10/21)
This invention is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I) to processes for their preparation; to pharmaceutical compositions comprising them; and to their use in therapy.
New substituted indolin-2-one derivatives and their use as p39 mitogen-activated kinase inhibitors
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Page/Page column 21, (2009/12/04)
This invention is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I) to processes for their preparation; to pharmaceutical compositions comprising them; and to their use in therapy.
Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, pyrazolopyridines, isothiazolopyridines, and preparation and uses thereof
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Page/Page column 72, (2010/11/26)
The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the α7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS
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Page/Page column 48, (2010/11/30)
The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly di
Synthesis and biological evaluation of 3-ethylidene-1,3-dihydro-indol-2- ones as novel checkpoint 1 inhibitors
Lin, Nan-Horng,Xia, Ping,Kovar, Peter,Park, Chang,Chen, Zehan,Zhang, Haiying,Rosenberg, Saul H.,Sham, Hing L.
, p. 421 - 426 (2007/10/03)
Chk1 inhibitors have emerged as a novel class of neoplastic agents for abrogating the G2 DNA damage checkpoint arrest. Analogs of the Chk1 inhibitor, 3-ethylidene-1,3-dihydro-indol-2-one, were synthesized and tested in vitro for their inhibitory activitie
INDOLES, 1H-INDAZOLES, 1,2-BENZISOXAZOLES, AND 1,2-BENZISOTHIAZOLES, AND PREPARATION AND USES THEREOF
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Page/Page column 44, (2008/06/13)
The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds for example, indoles, 1H-indazoles, 1,2-benzisoxazoles, and 1,2-benzisothiazoles, which act as ligands for the α7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
