136117-69-6Relevant articles and documents
Discovery of (S)-1-(1-(Imidazo[1,2- a ]pyridin-6-yl)ethyl)-6-(1-methyl-1 H -pyrazol-4-yl)-1 H -[1,2,3]triazolo[4,5- b ]pyrazine (Volitinib) as a Highly Potent and Selective Mesenchymal-Epithelial Transition Factor (c-Met) Inhibitor in Clinical Development for Treatment of Cancer
Jia, Hong,Dai, Guangxiu,Weng, Jianyang,Zhang, Zhulin,Wang, Qing,Zhou, Feng,Jiao, Longxian,Cui, Yumin,Ren, Yongxin,Fan, Shiming,Zhou, Jinghong,Qing, Weiguo,Gu, Yi,Wang, Jian,Sai, Yang,Su, Weiguo
supporting information, p. 7577 - 7589 (2014/12/11)
HGF/c-Met signaling has been implicated in human cancers. Herein we describe the invention of a series of novel triazolopyrazine c-Met inhibitors. The structure-activity relationship of these compounds was investigated, leading to the identification of compound 28, which demonstrated favorable pharmacokinetic properties in mice and good antitumor activities in the human glioma xenograft model in athymic nude mice.
CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR
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Page/Page column 28, (2012/10/08)
Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.
Fragment based discovery of a novel and selective PI3 kinase inhibitor
Hughes, Samantha J.,Millan, David S.,Kilty, Iain C.,Lewthwaite, Russell A.,Mathias, John P.,Reilly, Mark A.O.,Pannifer, Andrew,Phelan, Anne,Stühmeier, Frank,Baldock, Darren A.,Brown, David G.
scheme or table, p. 6586 - 6590 (2011/12/04)
We report the use of fragment screening and fragment based drug design to develop a PI3c kinase fragment hit into a lead. Initial fragment hits were discovered by high concentration biochemical screening, followed by a round of virtual screening to identify additional ligand efficient fragments. These were developed into potent and ligand efficient lead compounds using structure guided fragment growing and merging strategies. This led to a potent, selective, and cell permeable PI3c kinase inhibitor with good metabolic stability that was useful as a preclinical tool compound.
CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR
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Page/Page column 44-45, (2011/07/30)
Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.
ORGANIC COMPOUNDS
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Page/Page column 122, (2009/05/28)
Compounds of formula (I): in free or salt or solvate form, where R1, R2, R3 and R20 have the meanings as indicated in the specification, are useful for treati ng diseases mediated by the ALK-5 and/or ALK-4 receptor. Pharmaceutical composit ions that contain the compounds and processes for preparing the compounds are also described.
SYNTHESIS OF PYRAZOLES
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Page/Page column 39; 43, (2009/08/16)
The present invention provides methods of making HCl salts, and methods of using them to modulate alpha7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other
NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS
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Page/Page column 40-41, (2008/12/07)
The present invention provides compounds of formula (I) and compositions thereof, methods of making them, and methods of using them to modulate alpha7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other things, neurological, psychiatric and/or inflammatory system.
INHIBITORS OF HISTONE DEACETYLASE
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Page/Page column 247, (2010/02/11)
The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
Retinoid x receptor modulators
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, (2008/06/13)
The present invention is directed to compounds represented by Structural Formula (I) and pharmaceutically acceptable salts, solvates and hydrates thereof: (I). The invention is also directed to pharmaceutical compositions, methods of use and methods of making compounds represented by Structural Formula (I) and pharmaceutically acceptable salts, solvates and hydrates thereof.
Synthesis and biological evaluation of 2-Indolyloxazolines as a new class of tubulin polymerization inhibitors. Discovery of A-289099 as an orally active antitumor agent
Li, Qun,Woods, Keith W.,Claiborne, Akiyo,Gwaltney, Ii, Stephen L.,Barr, Kenneth J.,Liu, Gang,Gehrke, Laura,Credo,Hui, Yu Hua,Lee, Jang,Warner, Robert B.,Kovar, Peter,Nukkala, Michael A.,Zielinski, Nicolette A.,Tahir, Stephen K.,Fitzgerald, Michael,Kim, Ki H.,Marsh, Kennan,Frost, David,Ng, Shi-Chung,Rosenberg, Saul,Sham, Hing L.
, p. 465 - 469 (2007/10/03)
A series of indole containing oxazolines has been discovered as a result of structural modifications of the lead compound A-105972. The compounds exert their anticancer activity through inhibition of tubulin polymerization by binding at the colchicine site. A-289099 was identified as an orally active antimitotic agent active against various cancer cell lines including those that express the MDR phenotype. The anticancer activity, pharmacokinetics, and an efficient and enantioselective synthesis of A-289099 are described.