1374507-25-1Relevant articles and documents
Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors
Chang, Xiayun,Gao, Yong,He, Xiangyi,Lu, Peng,Ren, Jing,Shi, Wei,Wang, Qinglin,Wang, Xiaojin,Xu, Hongjiang,Zhang, Xiquan,Zhang, Yinsheng,Zhao, Damin
, (2019)
Bruton's tyrosine kinase (BTK) and Janus kinase 3 (JAK3) are very promising targets for hematological malignancies and autoimmune diseases. In recent years, a few compounds have been approved as a marketed medicine, and several are undergoing clinical trials. By recombining the dominant backbone of known active compounds, constructing a foused library, and screening a broad panel of kinases, we found a class of compounds with dual activities of anti-BTK and anti-JAK3. Some of the compounds have shown 10-folds more active in the enzyme and cell-based assays than a known active compound. Furthermore, liver microsome stability experiments show that these compounds have better stability than ibrutinib. These explorations offered new clues to discover benzoxaborole fragment and pyrimidine scaffold as more effective BTK and JAK3 dual inhibitors.
A including a spiro ring or bridge of the pyrimidines
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, (2017/08/25)
The invention discloses a spiral ring or bridged ring containing pyrimidine compound. The compound has a structure shown as formula I, and also can be an enantiomer, a diastereomer, a pharmaceutically acceptable salt, a prodrug molecule, a solvate, a taut
2,4-dibasic miazines compound
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, (2017/08/29)
The invention belongs to the field of medical chemistry, relates to a 2,4-dibasic miazines compound and specifically relates to a compound shown as formula (I) or a pharmaceutically acceptable salt thereof, a drug compound thereof and an application thereof in treating EGFR or/and ALK mediated diseases.