1025721-01-0Relevant articles and documents
PHOSPHONATE CONJUGATES AND USES THEREOF
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Paragraph 0089; 0094-0095, (2020/07/31)
Phosphonate conjugates, preferably, bisphosphonate conjugates; methods of inhibiting Ron receptor tyrosine kinase and methods of treatment of bone destruction due to cancer or other conditions utilizing the provided phosphonate conjugates.
URACIL COMPOUND AS C-MET/AXL INHIBITOR
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Paragraph 0187; 0189, (2020/11/22)
Provided are a uracil compound represented by Formula (IV) or a pharmaceutically acceptable salt thereof and a pharmaceutical composition of the same. Also provided is a use thereof as a c-MET/AXL inhibitor in preparing a c-MET/AXL-inhibiting drug or a dr
Antitumor compound used as AXL inhibitor and application of antitumor compound
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Paragraph 0237; 0238; 0241, (2019/10/23)
The invention discloses a compound shown in a general formula (I) or pharmaceutically acceptable salt of the compound and preparation methods of the compound and the salt, and further discloses pharmaceutical composition containing the compound and an application of the compound and the pharmaceutical composition in preparation of an AXL inhibitory drug. The AXL inhibitory drug is used for treating tumor, nephropathy, immune system disease or circulatory system disease.
Double-[...] compound and its method and use thereof
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Paragraph 0613; 0614, (2018/10/11)
The invention provides a type of substituted bicyclic pyrazolone compounds which can be used for inhibiting the activities of receptor tyrosine kinases especially the activities of Axl, Mer, c-Met and Ron kinases. The invention also provides medicine compositions comprising the type of compounds, and applications of the compound and the medicine compositions in drug preparation. The medicines can be used for preventing and treating proliferative diseases or reducing the severity of the diseases.
PHARMACEUTICAL COMPOSITION AND APPLICATION REPLACING QUINOLONE DERIVATIVE, PHARMACEUTICAL ACCEPTABLE SALT, OR STEREOISOMER
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Paragraph 0218; 0220, (2018/07/06)
Provided are a substituted quinolone derivative as shown by formula (I), or a pharmaceutically acceptable salt and a prodrug molecule thereof, and a pharmaceutical composition thereof, as well as the use of same in preparing drugs for the prevention and treatment of a tumor. The quinolone derivative, salt, prodrug molecule, and pharmaceutical composition thereof can be used as a protein kinase inhibitor, which is effective in inhibiting the activity of AXL protein kinase, and is capable of inhibiting the proliferation, migration and invasion of various tumor cells; and can be used in the preparation of anti-tumor drugs, especially drugs for treating hyperproliferative diseases such as a tumor in human beings and other mammals.
Polysubstituted quinolone compounds, and preparation method and use thereof
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Paragraph 0137; 0138; 0139, (2017/09/19)
The invention provides polysubstituted quinolone compounds, and a preparation method and a use thereof, and concretely provides a polysubstituted quinolone compound represented by formula I, and optical isomers, pharmaceutically acceptable salts or solvates thereof. All groups in the formula I are defined in the description. The quinolone compound has excellent c-Met inhibition activity, and can be used for treating c-Met activity or expression level corrected diseases.
Synthesis and evaluation of a series of pyridine and pyrimidine derivatives as type II c-Met inhibitors
Zhao, Yanmei,Zhang, Jiankang,Zhuang, Rangxiao,He, Ruoyu,Xi, Jianjun,Pan, Xuwang,Shao, Yidan,Pan, Jinming,Sun, Jingjing,Cai, Zhaobin,Liu, Shourong,Huang, Weiwei,Lv, Xiaoqing
, p. 3195 - 3205 (2017/05/25)
In this study, a series of novel pyridine and pyrimidine-containing derivatives were designed, synthesized and biologically evaluated for their c-Met inhibitory activities. In the biological evaluation, half of the target compounds exhibited moderate to p
4-Oxo-1,4-dihydroquinoline-3-carboxamide Derivatives as New Axl Kinase Inhibitors
Tan, Li,Zhang, Zhang,Gao, Donglin,Luo, Jinfeng,Tu, Zheng-Chao,Li, Zhengqiu,Peng, Lijie,Ren, Xiaomei,Ding, Ke
supporting information, p. 6807 - 6825 (2016/08/05)
Axl is a new potential target for anticancer drug discovery. A series of 4-oxo-1,4-dihydroquinoline-3-carboxamides were designed and synthesized as highly potent Axl kinase inhibitors. One of the most promising compounds, 9im, tightly bound with Axl prote
BICYLCIC PYRAZOLONE COMPOUNDS AND METHODS OF USE
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Paragraph 0296, (2015/11/16)
The present invention provides substituted bicyclic pyrazolone compounds, which are used to inhibit or modulate the activity of receptor tyrosine kinases, especially Axl, Mer, c-Met and Ron. The invention also provides pharmaceutical compositions comprising the compound disclosed herein, and a method of preventing, treating or lessening the severity of a proliferative disorder in a patient with the compounds or the pharmaceutical compositions disclosed herein.
SUBSTITUTED PYRAZOLONE COMPOUNDS AND METHODS OF USE
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Paragraph 0294-0296, (2015/02/19)
The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
