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Psoralen derivatives as non-peptidic inhibitors of chymotrypsin-like activity of the immunoproteasome : European patent specification EP 3256120 (B1), 2018-11-14
Sosič, Izidor ...
The present invention belongs to the field of pharmaceutical industry and relates to novel inhibitors of chymotrypsin- like activity of the immunoproteasome (inhibitors of %5i or LMP7 subunit) with a ...psoralen-based structure in the form of pure diastereoisomers, mixture of diastereomers, in the form of pure enantiomers, mixture of enantiomers, or pharmaceutically acceptable salts, hydrates or solvates thereof. Such compounds are particularly useful for the treatment of diseases that are related with increased activity of the immunoproteasome. The present invention also relates to the preparation of these compounds, use of these compounds, and to the pharmaceutical products that contain these compounds. The characteristic of these compounds is that they bind into the active site of the 5i subunit through specific noncovalent (polar and hydrophobic interactions) or concurrent noncovalent (polar and hydrophobic interactions) and covalent interactions.
Type of material - patent
; adult, serious
Publication and manufacture - München : European Patent and Trademark Office, 2018
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