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1. (WO2007093840) USE OF CELL-SPECIFIC CONJUGATES FOR TREATMENT OF INFLAMMATORY DISEASES OF THE GASTROINTESTINAL TRACT

Pub. No.:    WO/2007/093840    International Application No.:    PCT/IB2006/001488
Publication Date: Fri Aug 24 01:59:59 CEST 2007 International Filing Date: Thu Feb 16 00:59:59 CET 2006
IPC: A61K 47/48
Applicants: GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O.
MERCEP, Mladen
MESIC, Milan
TOMASKOVIC, Linda
MARKOVIC, Stribor
Inventors: MERCEP, Mladen
MESIC, Milan
TOMASKOVIC, Linda
MARKOVIC, Stribor
Title: USE OF CELL-SPECIFIC CONJUGATES FOR TREATMENT OF INFLAMMATORY DISEASES OF THE GASTROINTESTINAL TRACT
Abstract:
The present invention is directed to methods for the prevention and treatment of inflammatory diseases, disorders, and conditions of gastrointestinal tract by administering to a patient in need of such treatment, conjugate compounds of Formula (VII) having low oral- bioavailability, or pharmaceutically acceptable salts, prodrugs, or solvate thereof wherein M represents a macrolide subunit possessing the property of accumulation in inflammatory cells, T represents an anti-inflammatory subunit that can be a steroid or nonsteroid (nonsteroidal moiety) derived from a non-steroid drug with anti- inflammatory, analgesic and/or antipyretic activity (NSAID) and L represents a linker covalently linking M and T. The present disclosure is also directed to pharmaceutical compositions containing conjugate compounds of Formula (VII) having low oral-bioavailability.