1065100-83-5Relevant academic research and scientific papers
Discovery of Potent, Selective, and Brain-Penetrant 1 H-Pyrazol-5-yl-1 H-pyrrolo[2,3- b]pyridines as Anaplastic Lymphoma Kinase (ALK) Inhibitors
Fushimi, Makoto,Fujimori, Ikuo,Wakabayashi, Takeshi,Hasui, Tomoaki,Kawakita, Youichi,Imamura, Keisuke,Kato, Tomoko,Murakami, Morio,Ishii, Tsuyoshi,Kikko, Yorifumi,Kasahara, Maki,Nakatani, Atsushi,Hiura, Yuto,Miyamoto, Maki,Saikatendu, Kumar,Zou, Hua,Lane, Scott Weston,Lawson, J. David,Imoto, Hiroshi
, p. 4915 - 4935 (2019/05/22)
Anaplastic lymphoma kinase (ALK), a member of the receptor tyrosine kinase family, is predominantly expressed in the brain and implicated in neuronal development and cognition. However, the detailed function of ALK in the central nervous system (CNS) is s
Synthesis method of 7-azaindole-3-carboxylic acid
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Paragraph 0020; 0027; 0034; 0041; 0048; 0055, (2018/05/01)
The invention discloses a synthesis method of 7-azaindole-3-carboxylic acid. The synthesis method of the 7-azaindole-3-carboxylic acid comprises the following steps of adding 7-azaindole and water into a reaction kettle, stirring for 20 to 45min, then adding tetramethyl guanidine and zeolite, heating to 50 to 70 DEG C, adding formaldehyde after uniformly stirring and mixing, carrying out microwaveirradiation for 1 to 2h after uniformly stirring, then continuously stirring for reacting for 6 to 8h, filtering, dissolving a precipitate into dichloromethane, filtering again, carrying out vacuum distillation on a filter liquor, and recrystallizing to obtain 7-azaindole-3-methyl alcohol; oxidizing the 7-azaindole-3-methyl alcohol to obtain the 7-azaindole-3-carboxylic acid. The synthesis methodprovided by the invention is simple to operate, mild in conditions, less in byproducts, high in product purity, and higher in product yield.
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
, 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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, (2012/10/08)
Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.
CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR
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Page/Page column 23, (2011/07/30)
Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.
