948571-47-9Relevant articles and documents
FUSED PYRIMIDINE COMPOUNDS, COMPOSITIONS AND MEDICINAL APPLICATIONS THEREOF
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Paragraph 0236, (2021/04/02)
The present disclosure relates to a class of fused pyrimidine compounds of Formula I, their stereoisomers, tautomers, pharmaceutically acceptable salts, polymorphs, solvates, and hydrates thereof. The present disclosure also relates to a process of preparation of these fused pyrimidine compounds, and to pharmaceutical compositions containing them.
Preparation method and application of novel 6-amino-1H-pyrazolo[3,4-d]pyrimidine JAK kinase inhibitors
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Paragraph 0240; 0283-0287; 0293-0297, (2020/03/29)
The present invention provides drugs used for preventing, treating and/or ameliorating autoimmune diseases (such as psoriasis, rheumatoid arthritis, inflammatory enteritis diseases, Sjogren's syndrome, Behcet's disease, multiple sclerosis and systemic lupus erythematosus). The drugs have excellent JAK kinase inhibitory activity. The present invention also provides pharmaceutically acceptable compositions including the above compounds, and methods for preparing the compounds.
Design, synthesis, and biological evaluation of some novel 4-aminoquinazolines as Pan-PI3K inhibitors
Ding, Huai-Wei,Wang, Shu,Qin, Xiao-Chun,Wang, Jian,Song, Hong-Rui,Zhao, Qing-Chun,Song, Shao-Jiang
, p. 2729 - 2740 (2019/05/17)
A series of 4-aminoquinazolines derivatives containing hydrophilic group were designed and identified as potent Pan-PI3K inhibitors in this study. The results of antiproliferative assays in vitro showed that this series of compounds had strong inhibition of tumor growth, especially compound 7b for MCF-7 cells but weak inhibition to normal cells. PI3K kinase assay showed that 7b had high activity for three PI3K isoforms with the IC50 values of picomole. The western blot assay indicated that 7b could decrease the phospho-Akt (S473) in a dose-dependent manner. Further experiments showed that 7b could induce apoptosis in MCF-7 cells. Four key hydrogen bonding interactions were found in the docking of 7b with PI3K kinase. All these results suggested that 7b is a potent PI3K inhibitor and could be considered as a potential candidate for the development of anticancer agents.