1800465-47-7Relevant academic research and scientific papers
Novel 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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, (2016/09/26)
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.
Novel 8-oxoprotoberberine derivatives or pharmaceutically acceptable salts thereof, preparation method thereof and pharmaceutical composition for prevention or treatment of diseases induced by activation of NFAT5 containing the same as an active ingredient
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, (2016/10/27)
The present invention relates to: novel 8-oxoprotoberberine derivatives or pharmaceutically acceptable salts thereof; a method for preparing same; and a pharmaceutical composition containing the same as active ingredient for preventing or treating diseases related to NFAT5 activity. According to the present invention, the novel 8-oxoprotoberberine derivatives or the pharmaceutically acceptable salts thereof is proven to: have an oral absorption rate which is significantly higher thatn than of the prior protoberberine; inhibit NFAT5 activity and secretion of inflammatory cyotokine by directly inhibiting transcription of NFAT5; and reduce expression of NFAT5 in a mouse with rheumarthritis. Therefore, the novel 8-oxoprotoberberine derivatives or the pharmaceutically acceptable salts thereof can be advantageously used as a pharmaceutical composition for preventing or treating NFTA5 activity-related diseases, particularly rheumarthritis or inflammation disease.(AA) Days after immune response induction(BB) Control group(CC) Example 1COPYRIGHT KIPO 2015
