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1. (WO2006075255) ANTI-INFLAMATORY MACROLIDE CONJUGATES
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2006/075255 International Application No.: PCT/IB2006/001079
Publication Date: 20.07.2006 International Filing Date: 13.01.2006
IPC:
C07D 495/04 (2006.01) ,C07H 17/08 (2006.01) ,C07D 498/04 (2006.01) ,A61K 31/7048 (2006.01) ,A61K 31/7052 (2006.01) ,A61K 31/55 (2006.01) ,A61P 29/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
495
Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
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
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
498
Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
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
7048
having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
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
55
having seven-membered rings, e.g. azelastine, pentylenetetrazole
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)
Applicants:
MERCEP, Mladen [HR/HR]; HR (UsOnly)
MESIC, Milan [HR/HR]; HR (UsOnly)
MARKOVIC, Stribor [HR/HR]; HR (UsOnly)
PESIC, Dijana [HR/HR]; HR (UsOnly)
OZIMEC LANDEK, Ivana [HR/HR]; HR (UsOnly)
KOMAC, Marijana [HR/HR]; HR (UsOnly)
MAKARUHA STEGIC, Oresta [HR/HR]; HR (UsOnly)
SELMANI, Selvira [HR/HR]; HR (UsOnly)
TOMASKOVIC, Linda [HR/HR]; HR (UsOnly)
BANJANAC, Mihailo [HR/HR]; HR (UsOnly)
GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O. [HR/HR]; Prilaz Baruna Fillipovica 29 10000 Zagreb, HR (AllExceptUS)
Inventors:
MERCEP, Mladen; HR
MESIC, Milan; HR
MARKOVIC, Stribor; HR
PESIC, Dijana; HR
OZIMEC LANDEK, Ivana; HR
KOMAC, Marijana; HR
MAKARUHA STEGIC, Oresta; HR
SELMANI, Selvira; HR
TOMASKOVIC, Linda; HR
BANJANAC, Mihailo; HR
Agent:
LUDWIG, Peter, S.; Darby & Darby P.C. P.O. Box 5257 New York, NY 10150-5257, US
Priority Data:
60/643,93113.01.2005US
Title (EN) ANTI-INFLAMATORY MACROLIDE CONJUGATES
(FR) CONJUGUES DE MACROLIDES ANTI-INFLAMATOIRES
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, D represents a dibenzo[e,/z]azulene subunit with anti-inflammatory, analgesic and/or antipyretic 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) L'invention concerne : (a) des composés représentés par la formule I: dans laquelle M représente un sous-motif de macrolide (fraction de macrolide) dérivé d'un macrolide possédant la propriété d'accumulation dans des cellules inflammatoires, D représente un sous-motif de dibenzo[e,/z]azulène à activité anti-inflammatoire, analgésique et/ou antipyrétique et L représente un groupe de liaison liant par covalence M et D; (b) des sels, des promédicaments et des solvates acceptables sur le plan pharmacologique de ceux-ci, (c) des procédés et des intermédiaires destinés à la préparation de ceux-ci et (d) l'utilisation de ceux-ci dans le traitement de maladies et d'états inflammatoires chez des êtres humains et des 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)