1072833-69-2Relevant academic research and scientific papers
Borate compound and pharmaceutically acceptable salt thereof, and preparation method and application of boric acid ester compound and pharmaceutically acceptable salt thereof
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Paragraph 0053; 0079; 0084-0087, (2021/07/14)
The invention relates to a borate compound as shown in a formula (1), a pharmaceutically acceptable salt thereof, a preparation method and application thereof. The borate compound is novel in structure and has a proteasome inhibition function. The stability of the borate compound disclosed by the invention in a solution is far higher than that of Ixazomib. Especially when the pH is 1.2 and the pH is 6.8, the stability of the compound provided by the invention is more advantageous. Besides, microsome stability results show that the compound has good stability in five different liver microsomes, the half-life period of the microsomes of Ixazomib in cynomolgus monkeys is too long, the medicine is basically not metabolized, and serious toxicity can be caused. The compound can be used for preparing medicines for treating inflammation, immune-related diseases, cancers or hyperproliferative diseases and changing antigen peptides generated by proteasomes in organisms.
Borate drug and uses thereof
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Paragraph 0257; 0262-0264, (2020/04/02)
The invention provides a borate compound as a proteasome inhibitor, a preparation method and applications thereof, wherein the compound has the following structural formula (I), R1 and R2 substituentsare para-position asymmetric substituents, R1 and R2 are respectively selected from halogen, R2 is not Cl when R1 is F, R2 is not Br or F when R1 is Cl, R2 is not Cl when R1 is Br, X1 and X2 are selected from hydroxyl, or X1 and X2 jointly form a substituted or unsubstituted 4-10-membered ring, and the 4-10-membered ring contains 1-4 heteroatoms optionally selected from O, N and S. The borate compound of the present invention has high activity compared with the existing borate compounds as proteasome inhibitors.
PROTEASOME INHIBITORS
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Page/Page column 26-27, (2009/04/25)
The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
Proteasome inhibitors
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Page/Page column 25, (2008/12/04)
The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
