8-oxoprotoberberine derivative or pharmaceutically acceptable salt thereof, preparation method therefor and pharmaceutical composition for preventing or treating diseases associated with activity of NFAT5, containing same as active ingredient
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United States of America Patent
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May 16, 2017
Grant Date -
Sep 1, 2016
app pub date -
Dec 30, 2014
filing date -
Dec 31, 2013
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Abstract
The preset invention relates to a novel 8-oxoprotoberberine derivative or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition for preventing or treating diseases associated with the activity of NFAT5 containing the same as an active ingredient. The novel 8-oxoproteoberberine derivative or the pharmaceutically acceptable salt thereof according to the present invention can be useful in a pharmaceutical composition for preventing or treating diseases associated with the activity of NFAT5, particularly rheumatoid arthritis or inflammatory diseases, since it is ascertained that the derivative or a pharmaceutically acceptable salt thereof has remarkably increased oral absorption compared with known protoberberine due to an improvement in the properties thereof, and inhibits the activity of NFAT5 and the secretion of inflammatory cytokines and reduces the expression of NAFT5 in mice with rheumatoid arthritis by directly inhibiting the transcription of NFT5.
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