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1. WO2006075255 - ANTI-INFLAMATORY MACROLIDE CONJUGATES

Publication Number WO/2006/075255
Publication Date 20.07.2006
International Application No. PCT/IB2006/001079
International Filing Date 13.01.2006
IPC
C07D 495/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
495Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07H 17/08 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
17Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
04Heterocyclic radicals containing only oxygen as ring hetero atoms
08Hetero rings containing eight or more ring members, e.g. erythromycins
C07D 498/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
498Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61K 31/7048 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7042Compounds having saccharide radicals and heterocyclic rings
7048having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 31/7052 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7042Compounds having saccharide radicals and heterocyclic rings
7052having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
A61K 31/55 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
55having seven-membered rings, e.g. azelastine, pentylenetetrazole
CPC
A61P 1/04
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
04for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 1/08
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
08for nausea, cinetosis or vertigo; Antiemetics
A61P 1/10
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
10Laxatives
A61P 1/12
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
12Antidiarrhoeals
A61P 1/16
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
16for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 11/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
Applicants
  • GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O. [HR]/[HR] (AllExceptUS)
  • MERCEP, Mladen [HR]/[HR] (UsOnly)
  • MESIC, Milan [HR]/[HR] (UsOnly)
  • MARKOVIC, Stribor [HR]/[HR] (UsOnly)
  • PESIC, Dijana [HR]/[HR] (UsOnly)
  • OZIMEC LANDEK, Ivana [HR]/[HR] (UsOnly)
  • KOMAC, Marijana [HR]/[HR] (UsOnly)
  • MAKARUHA STEGIC, Oresta [HR]/[HR] (UsOnly)
  • SELMANI, Selvira [HR]/[HR] (UsOnly)
  • TOMASKOVIC, Linda [HR]/[HR] (UsOnly)
  • BANJANAC, Mihailo [HR]/[HR] (UsOnly)
Inventors
  • MERCEP, Mladen
  • MESIC, Milan
  • MARKOVIC, Stribor
  • PESIC, Dijana
  • OZIMEC LANDEK, Ivana
  • KOMAC, Marijana
  • MAKARUHA STEGIC, Oresta
  • SELMANI, Selvira
  • TOMASKOVIC, Linda
  • BANJANAC, Mihailo
Agents
  • LUDWIG, Peter, S.
Priority Data
60/643,93113.01.2005US
Publication Language English (en)
Filing Language English (EN)
Designated States
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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