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1. (WO2004005310) NEW COMPOUNDS, COMPOSITIONS AND METHODS FOR TREATMENT OF INFLAMMATORY DISEASES AND CONDITIONS

Pub. No.:    WO/2004/005310    International Application No.:    PCT/HR2003/000037
Publication Date: Fri Jan 16 00:59:59 CET 2004 International Filing Date: Wed Jul 09 01:59:59 CEST 2003
IPC: C07H 17/00
Applicants: PLIVA-ISTRAZIVACKI INSTITUT D.O.O.
MERCEP, Mladen
MESIC, Milan
TOMASKOVIC, Linda
MARKOVIC, Stribor
MAKARUHA, Oresta
POLJAK, Visnja
Inventors: MERCEP, Mladen
MESIC, Milan
TOMASKOVIC, Linda
MARKOVIC, Stribor
MAKARUHA, Oresta
POLJAK, Visnja
Title: NEW COMPOUNDS, COMPOSITIONS AND METHODS FOR TREATMENT OF INFLAMMATORY DISEASES AND CONDITIONS
Abstract:
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 the treatment of inflammatory diseases and conditions in humans and animals. Such 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-α. Importantly, anti-inflammatory steroids exert a direct anti-inflammatory effect through binding to the glucocorticosteroid receptor.