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1. WO2006087644 - MACROLIDES WITH ANTI-INFLAMMATORY ACTIVITY

Publication Number WO/2006/087644
Publication Date 24.08.2006
International Application No. PCT/IB2006/001238
International Filing Date 13.01.2006
IPC
C07H 17/00 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
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
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 31/7048 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
A61P 29/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29Non-central analgesic, antipyretic or antiinflammatory agents, e.g antirheumatic agents; Non-steroidal antiinflammatory drugs (NSAIDs)
CPC
A61K 31/7048
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 ; digitoxin or digoxin
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
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 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
A61P 11/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
02Nasal agents, e.g. decongestants
A61P 11/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
06Antiasthmatics
Applicants
  • GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O. [HR]/[HR] (AE, AG, AL, AM, AT, AU, AZ, BA, BB, BE, BF, BG, BJ, BR, BW, BY, BZ, CA, CF, CG, CH, CI, CM, CN, CO, CR, CU, CY, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, FR, GA, GB, GD, GE, GH, GM, GN, GQ, GR, GW, HR, HU, ID, IE, IL, IN, IS, IT, JP, KE, KG, KM, KN, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, LY, MA, MC, MD, MG, MK, ML, MN, MR, MW, MX, MZ, NA, NE, NG, NI, NL, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SI, SK, SL, SM, SN, SY, SZ, TD, TG, TJ, TM, TN, TR, TT, TZ, UA, UG, UZ, VC, VN, YU, ZA, ZM, ZW)
  • CULIC, Ognjen [HR]/[HR] (UsOnly)
  • BOSNAR, Martina [HR]/[HR] (UsOnly)
  • MARJANOVIC, Nikola [HR]/[HR] (UsOnly)
  • JELIC, Dubravko [HR]/[HR] (UsOnly)
  • ALIHODZIC, Sulejman [HR]/[HR] (UsOnly)
  • VELA, Vanja [HR]/[HR] (UsOnly)
  • MARUSIC-ISTUK, Zorica [HR]/[HR] (UsOnly)
  • ERAKOVIC, Vesna [HR]/[HR] (UsOnly)
  • BOSNJAK, Berislav [HR]/[HR] (UsOnly)
  • HRVACIC, Boska [HR]/[HR] (UsOnly)
  • TOMASKOVIC, Marija [HR]/[HR] (UsOnly)
  • MUNIC, Vesna [HR]/[HR] (UsOnly)
  • IVETIC, Vanesa [HR]/[HR] (UsOnly)
  • HUTINEC, Antun [HR]/[HR] (UsOnly)
  • KRAGOL, Goran [HR]/[HR] (UsOnly)
  • LELJAK, Marija [HR]/[HR] (UsOnly)
Inventors
  • CULIC, Ognjen
  • BOSNAR, Martina
  • MARJANOVIC, Nikola
  • JELIC, Dubravko
  • ALIHODZIC, Sulejman
  • VELA, Vanja
  • MARUSIC-ISTUK, Zorica
  • ERAKOVIC, Vesna
  • BOSNJAK, Berislav
  • HRVACIC, Boska
  • TOMASKOVIC, Marija
  • MUNIC, Vesna
  • IVETIC, Vanesa
  • HUTINEC, Antun
  • KRAGOL, Goran
  • LELJAK, Marija
Priority Data
60/643,84113.01.2005US
60/715,82809.09.2005US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) MACROLIDES WITH ANTI-INFLAMMATORY ACTIVITY
(FR) MACROLIDES PRESENTANT UNE ACTIVITE ANTI-INFLAMMATOIRE
Abstract
(EN) The present invention relates to novel semi-synthetic macrolides having anti-inflammatory activity. More particularly, the invention relates to 14- and 15-membered macrolides substituted at the 4' position, to their pharmaceutically acceptable derivatives, to processes and intermediates for their preparation, to pharmaceutical compositions containing them and to their activity and use in the treatment of inflammatory diseases and conditions in humans and animals, especially those diseases associated with excessive secretion of TNF-&agr;, IL-1, IL-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation.
(FR) L'invention concerne de nouveaux macrolides semi-synthétiques qui présentent une activité anti-inflammatoire. D'une manière plus spécifique, l'invention concerne des macrolides à 14 ou 15 éléments substitués en position 4', leurs dérivés pharmaceutiquement acceptables, des processus et des intermédiaires pour leur préparation, des compositions pharmaceutiques contenant ces macrolides ainsi que leur activité et leur utilisation dans le traitement de maladies et d'états inflammatoires sur des humains et des animaux, notamment des maladies associées à une sécrétion excessive de TNF-a, IL-1, IL-8, IL-2 ou IL-5 ; et/ou à l'inhibition d'une prolifération lymphocytaire excessive ; et/ou à une dégranulation excessive des granulocytes.
Latest bibliographic data on file with the International Bureau