756520-82-8Relevant academic research and scientific papers
SELECTIVE JAK2 INHIBITOR AND APPLICATION THEREOF
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, (2021/02/25)
Provided is a selective JAK2 inhibitor and application thereof. In particular, it relates to the compound of the following Formula (I), and the use of the compound in the treatment of JAK2-mediated related diseases and in the preparation of the medicament for treating JAK2-mediated related diseases.
Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2
Wang, Wanqi,Diao, Yanyan,Li, Wenjie,Luo, Yating,Yang, Tingyuan,Zhao, Yuyu,Qi, TianTian,Xu, Fangling,Ma, Xiangyu,Ge, Huan,Liang, Yingfan,Zhao, Zhenjiang,Liang, Xin,Wang, Rui,Zhu, Lili,Li, Honglin,Xu, Yufang
, p. 1507 - 1513 (2019/04/17)
Janus Kinase 2 (JAK2) is a kind of intracellular non-receptor protein tyrosine kinase and has been certified as an important target for the treatment of myeloproliferative neoplasms and rheumatoid arthritis. However, the low selectivity and potential safety issues restrict the clinical applications of JAK2 inhibitors. Here we found that crizotinib showed good inhibitory activity against JAK2 by enzymatic assays (IC50 = 27 nM). Then we carried out structure-based drug design and synthesized a series of compounds with an aminopyridine scaffold. Finally, compound 12k and 12l were identified as the promising inhibitors of JAK2, which exhibited high inhibitory activity (IC50 = 6 nM and 3 nM, respectively) and selectivity for JAK2 over JAK1 and JAK3, and showed potent antiproliferative activities toward HEL human erythroleukemia cells. Moreover, 12k suppressed symptoms of the collagen-induced arthritis (CIA) model in rats.
Substituted pyridine compound and its method and use thereof
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, (2018/06/21)
The invention relates to a novel substitutive pyridine compound, and a pharmaceutically acceptable salt and a pharmaceutical preparation of the substitutive pyridine compound for regulating the activity of protein kinases and regulating signal responses between cells or in the cells. Meanwhile, the invention further relates to a pharmaceutical composition containing the compound provided by the invention, and a method for treating high proliferative diseases of mammals, especially human with the pharmaceutical composition.
Substituted ring compound and its method and use thereof
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, (2017/08/25)
The invention provides a substituted cyclic compound as well as a use method and application thereof. The compound is a compound as shown in a formula (I) or stereoisomers, stereomers, tautomers, nitric oxides, solvates, metabolites and pharmaceutically acceptable salts or prodrugs of the compound as shown in the formula (I). The invention further provides a medicament composition containing the compound. The compound and the medicament composition are capable of regulating the activity of protein kinase in a biological sample body and are used for protecting, treating or relieving proliferative diseases of patients. The formula (I) is as shown in the specification.
SUBSTITUTED CYCLIC COMPOUNDS AND METHODS OF USE
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, (2014/06/24)
The present invention provides novel substituted alkynyl 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.
