Title:
NEW COMPOUNDS, COMPOSITIONS AND METHODS FOR TREATMENT OF INFLAMMATORY DISEASES AND CONDITIONS
Document Type and Number:
WIPO Patent Application WO2004005310
Kind Code:
A3
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-alpha. Importantly, anti-inflammatory steroids exert a direct anti-inflammatory effect through binding to the glucocorticosteroid receptor.
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Inventors:
MERCEP MLADEN (HR)
MESIC MILAN (HR)
TOMASKOVIC LINDA (HR)
MARKOVIC STRIBOR (HR)
MAKARUHA ORESTA (HR)
POLJAK VISNJA (HR)
MESIC MILAN (HR)
TOMASKOVIC LINDA (HR)
MARKOVIC STRIBOR (HR)
MAKARUHA ORESTA (HR)
POLJAK VISNJA (HR)
Application Number:
PCT/HR2003/000037
Publication Date:
April 22, 2004
Filing Date:
July 08, 2003
Export Citation:
Assignee:
PLIVA D D (HR)
MERCEP MLADEN (HR)
MESIC MILAN (HR)
TOMASKOVIC LINDA (HR)
MARKOVIC STRIBOR (HR)
MAKARUHA ORESTA (HR)
POLJAK VISNJA (HR)
MERCEP MLADEN (HR)
MESIC MILAN (HR)
TOMASKOVIC LINDA (HR)
MARKOVIC STRIBOR (HR)
MAKARUHA ORESTA (HR)
POLJAK VISNJA (HR)
International Classes:
A61K31/7048; A61K31/58; A61P1/04; A61P5/44; A61P9/00; A61P9/10; A61P11/00; A61P11/06; A61P17/00; A61P17/06; A61P19/02; A61P19/06; A61P27/02; A61P29/00; A61P37/00; C07H17/00; C07H17/08; C07J21/00; C07J43/00; (IPC1-7): C07J43/00; A61K31/58; A61P5/44; C07H17/00; C07H17/08
Domestic Patent References:
| WO1997041255A1 | 1997-11-06 | |||
| WO1999064040A1 | 1999-12-16 | |||
| WO2000064882A2 | 2000-11-02 | |||
| WO2002055531A1 | 2002-07-18 |
Foreign References:
| EP0283055A2 | 1988-09-21 |
Other References:
ROMO D ET AL: "Total Synthesis and Immunosuppressive Activity of (-)-Pateamine A and Related Compounds: Implementation of beta-Lactam Based MacroCYCLIZATION", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, AMERICAN CHEMICAL SOCIETY, WASHINGTON, DC, US, vol. 120, no. 47, 1998, pages 12237 - 12254, XP002200620, ISSN: 0002-7863
BRANDT-RAUF P ET AL: "FLUORESCENT ASSAY FOR ESTIMATING THE BINDING OF ERYTHROMYCIN DERIVATIVES TO RIBOSOMES", ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, AMERICAN SOCIETY FOR MICROBIOLOGY, WASHINGTON, DC, US, vol. 14, no. 1, July 1978 (1978-07-01), pages 88 - 94, XP000923144, ISSN: 0066-4804
See also references of EP 1521764A2
BRANDT-RAUF P ET AL: "FLUORESCENT ASSAY FOR ESTIMATING THE BINDING OF ERYTHROMYCIN DERIVATIVES TO RIBOSOMES", ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, AMERICAN SOCIETY FOR MICROBIOLOGY, WASHINGTON, DC, US, vol. 14, no. 1, July 1978 (1978-07-01), pages 88 - 94, XP000923144, ISSN: 0066-4804
See also references of EP 1521764A2
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