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

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Publication Number WO/2007/093840
Publication Date 23.08.2007
International Application No. PCT/IB2006/001488
International Filing Date 15.02.2006
IPC
A61K 47/48 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
48the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
CPC
A61K 47/545
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
54the modifying agent being an organic compound
545Heterocyclic compounds
A61K 47/554
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
54the modifying agent being an organic compound
554the modifying agent being a steroid plant sterol, glycyrrhetic acid, enoxolone or bile acid
A61P 1/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
Applicants
  • GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O. [HR]/[HR] (AllExceptUS)
  • MERCEP, Mladen [HR]/[HR] (UsOnly)
  • MESIC, Milan [HR]/[HR] (UsOnly)
  • TOMASKOVIC, Linda [HR]/[HR] (UsOnly)
  • MARKOVIC, Stribor [HR]/[HR] (UsOnly)
Inventors
  • MERCEP, Mladen
  • MESIC, Milan
  • TOMASKOVIC, Linda
  • MARKOVIC, Stribor
Priority Data
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) USE OF CELL-SPECIFIC CONJUGATES FOR TREATMENT OF INFLAMMATORY DISEASES OF THE GASTROINTESTINAL TRACT
(FR) UTILISATION DE CONJUGUÉS SPÉCIFIQUES DE CELLULE POUR TRAITER DES MALADIES INFLAMMATOIRES DES VOIES GASTRO-INTESTINALES
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Abstract
(EN) 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.
(FR) La présente invention concerne des méthodes de prévention et de traitement de maladies, de troubles, et de pathologies inflammatoires des voies gastro-intestinales en administrant à un patient nécessitant un tel traitement, des composés conjugués de Formule VII de faible biodisponibilité orale ou des sels, promédicaments ou solutés de ceux-ci pharmaceutiquement acceptables, M représentant une sous-unité macrolide qui possède une propriété d'accumulation dans des cellules inflammatoires, T représentant une sous-unité anti-inflammatoire qui peut être un stéroïde ou un non stéroïde (groupement non stéroïdien) dérivé d'un médicament non stéroïdien à activité anti-inflammatoire, analgésique et/ou antipyrétique (AINS), et L représentant un lieur covalent entre M et T. La présente invention concerne aussi des compositions pharmaceutiques contenant des composés conjugués de Formule VII à faible biodisponibilité orale.
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