373608-48-1Relevant articles and documents
FGFR4 Inhibitor. Compositions and their use in pharmaceutical preparations
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, (2021/10/27)
The invention provides 3 inhibitor which takes 4 - 4 dihydropyrimidine [5 - d,2] pyrimidine - (1H) FGFR4 ketone as a mother nucleus and has a covalent structure. The examples give 9 specific compounds and kinase inhibitory activity testing of these 9 compounds, wherein LX08 for FGFR4 kinase inhibitory activity is only 7 nm, lower than FIIN - 2 of the active control, and potential application prospects. In addition, by subjecting the synthesized compound to MALDI-TOF mass spectrometry, we found that compounds of LX01, LX05, LX06, LX07, LX08 are covalently bound to FGFR4 of Cys552, cannot covalently bind FGFR4 of Cys477, and LX09 are FGFR4 inhibitors which can be covalently bound to the two cysteines Cys552 and Cys477 in FGFR4.
Synthetic route of generic FGFR covalent inhibitor PRN1371
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, (2021/01/11)
The invention relates to a synthetic route of a generic FGFR covalent inhibitor PRN1371, and belongs to the field of medicinal chemistry. The synthetic route steps of the PRN1371 comprise 11 steps, purification of a product can be achieved through simple operation of various intermediates in the aftertreatment process, the problems that the product is difficult to separate, the purification operation yield is low and the like are solved, and industrial production is facilitated. The invention aims to provide a synthetic route of the FGFR irreversible covalent inhibitor PRN1371, and the methodhas the advantages of few synthesis steps, simple operation, high yield, reduction of the production cost, and provision of a new synthesis idea for the industrial production of PRN1371.
ANTIBACTERIAL COMPOUNDS HAVING BROAD SPECTRUM OF ACTIVITY
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Page/Page column 44, (2016/07/05)
The present invention relates to novel antibacterial compounds, pharmaceutical compositions containing them and their use as antimicrobials.