摘要 |
The present invention relates (a) to new compounds represented by Formula (I ): wherein M represents a macrolide subunit (macrolide moiety) derived from macrolide possessing the property of accumulation in inflammatory cells, S represents a steroid subunit (steroid moiety) derived from steroid drug with anti-inflammatory activity and L represents a linker molecule linking M and S, (b) to their pharmacologically acceptable salts, prodrugs and solvates, (c) to processes and intermediates for their preparation, and (d) to their use in t he treatment of inflammatory diseases and conditions in humans and animals. Suc h compounds inhibit many cytokines and immune mediators involved in immune responses which cause inflammation, allergy, or alloimmunity, including without limitation IL-1, 2, 4, 5, 6, 10, 12, GMCSF, ICAM, and TNF-.alpha.. Importantly, anti-inflammatory steroids exert a direct anti-inflammatory effect through binding to the glucocorticosteroid receptor.
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申请人 |
PLIVA-ISTRAZIVACKI INSTITUT D.O.O. |
发明人 |
MARKOVIC, STRIBOR;TOMASKOVIC, LINDA;POLJAK, VISNJA;MERCEP, MLADEN;MESIC, MILAN;MAKARUHA, ORESTA |