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1. (WO2006092739) ANTI-INFLAMMATORY CONJUGATES OF MACROLIDES AND COUMARINS
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2006/092739 International Application No.: PCT/IB2006/001422
Publication Date: 08.09.2006 International Filing Date: 13.01.2006
IPC:
C07H 17/00 (2006.01) ,C07D 413/12 (2006.01) ,A61K 47/48 (2006.01) ,A61P 37/06 (2006.01) ,A61P 29/00 (2006.01) ,A61K 31/7052 (2006.01) ,A61K 31/395 (2006.01) ,C07D 413/14 (2006.01) ,C07H 17/08 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
17
Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
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
37
Drugs for immunological or allergic disorders
02
Immunomodulators
06
Immunosuppressants, e.g. drugs for graft rejection
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
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
70
Carbohydrates; Sugars; Derivatives thereof
7042
Compounds having saccharide radicals and heterocyclic rings
7052
having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
17
Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
04
Heterocyclic radicals containing only oxygen as ring hetero atoms
08
Hetero rings containing eight or more ring members, e.g. erythromycins
Applicants:
MERCEP, Mladen [HR/HR]; HR (UsOnly)
MALNAR, Ivica [HR/HR]; HR (UsOnly)
FILIPOVIC SUCIC, Anita [HR/HR]; HR (UsOnly)
MESIC, Milan [HR/HR]; HR (UsOnly)
GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O. [HR/HR]; Prilaz baruna Filipovica 29 10000 Zagreb, HR (AllExceptUS)
Inventors:
MERCEP, Mladen; HR
MALNAR, Ivica; HR
FILIPOVIC SUCIC, Anita; HR
MESIC, Milan; HR
Agent:
GLAXOSMITHKLINE SERVICES UNLIMITED; 980 Great West Road Brentford5257 Middlesex TW8 9GS, GB
Priority Data:
60/644,35914.01.2005US
60/647,79327.01.2005US
Title (EN) ANTI-INFLAMMATORY CONJUGATES OF MACROLIDES AND COUMARINS
(FR) CONJUGUES ANTI-INFLAMMATOIRES DES MACROLIDES ET DES COUMARINES
Abstract:
(EN) 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, each D represents a coumarin subunit with anti-inflammatory activity and L represents a linking group covalently linking M and D; (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.
(FR) La présente invention concerne (a) de nouveaux composés représentés par la formule (I) où M représente une sous-unité macrolide (fraction macrolide) dérivée d’un macrolide possédant la propriété de s’accumuler dans les cellules inflammatoires, chaque D représente une sous-unité coumarine à activité anti-inflammatoire et L représente un groupe de liaison se liant de manière covalente à M et à D; (b) leurs sels, promédicaments et solvates pharmacologiquement acceptables, (c) des procédés et intermédiaires destinés à leur préparation et (d) leur utilisation dans le traitement de maladies et troubles inflammatoires chez les humains et les animaux.
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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, KN, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, LY, 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 Office (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (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)