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1. (WO2006018698) USE OF CELL-SPECIFIC CONJUGATES FOR TREATMENT OF INFLAMMATORY DISEASES OF THE GASTROINTESTINAL TRACT
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2006/018698 International Application No.: PCT/IB2005/002406
Publication Date: 23.02.2006 International Filing Date: 10.08.2005
IPC:
A61K 47/48 (2006.01) ,A61P 29/00 (2006.01) ,A61P 1/00 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
48
the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29
Non-central analgesic, antipyretic or antiinflammatory agents, e.g antirheumatic agents; Non-steroidal antiinflammatory drugs (NSAIDs)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1
Drugs for disorders of the alimentary tract or the digestive system
Applicants:
GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O. [HR/HR]; Prilaz baruna Filipovica 29 10000 Zagreb, HR (AllExceptUS)
MERCEP, Mladen [HR/HR]; HR (UsOnly)
MESIC, Milan [HR/HR]; HR (UsOnly)
TOMASKOVIC, Linda [HR/HR]; HR (UsOnly)
MARKOVIC, Stribor [HR/HR]; HR (UsOnly)
Inventors:
MERCEP, Mladen; HR
MESIC, Milan; HR
TOMASKOVIC, Linda; HR
MARKOVIC, Stribor; HR
Priority Data:
60/601,08712.08.2004US
60/603,31519.08.2004US
Title (EN) USE OF CELL-SPECIFIC CONJUGATES FOR TREATMENT OF INFLAMMATORY DISEASES OF THE GASTROINTESTINAL TRACT
(FR) UTILISATION DE CONJUGUES SPECIFIQUES DE CELLULE POUR LE TRAITEMENT DE MALADIES INFLAMMATOIRES DU TRACTUS GASTRO-INTESTINAL
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 oral­bioavailability, 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 anti­inflammatory, 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) L'invention concerne des procédés pour la prévention et le traitement de maladies, de troubles, et d'états inflammatoires du tractus gastro-intestinal par administration à un patient nécessitant un tel traitement de composés conjugués de formule (VII) à faible biodisponibilité orale, ou de sels, promédicaments ou solvates de ceux-ci acceptables sur le plan pharmaceutique. Dans la formule, M représente une sous-unité macrolide possédant la propriété de s'accumuler dans des cellules inflammatoires ; T représente une sous-unité anti-inflammatoire pouvant être un stéroïdien ou un non-stéroïdien (fragment non-stéroïdien) dérivé d'un médicament non-stéroïdien à activité anti-inflammatoire, analgésique et/ou antipyrétique (NSAID) ; et L représente un liant qui lie par covalence M et T. L'invention concerne également des compositions pharmaceutiques contenant les composés conjugués de formule (VII) à faible biodisponibilité orale.
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Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IS, IT, LT, LU, LV, MC, NL, PL, PT, RO, SE, SI, SK, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
DZDZP2007000166NO20071244NZ552896MXMX/a/2007/001669KR1020070046917VN14820
IL181240EP1778292ZA2007/00668JP2008509899CN101043907CA2576291
AU2005273592ID047.1655IN1351/DELNP/2007