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1. WO2000066603 - HALO DERIVATIVES OF 9-DEOXO-9A-AZA-9A-HOMERYTHROMYCIN A

Publication Number WO/2000/066603
Publication Date 09.11.2000
International Application No. PCT/HR2000/000013
International Filing Date 02.05.2000
Chapter 2 Demand Filed 30.11.2000
IPC
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
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 31/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
04Antibacterial agents
C07H 1/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
1Processes for the preparation of sugar derivatives
C07H 17/08
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
Applicants
  • PLIVA, FARMACEUTSKA INDUSTRIJA, DIONICKO DRUSTVO [HR]/[HR] (AllExceptUS)
  • MARUŠIĆ-IŠTUK, Zorica [HR]/[HR] (UsOnly)
  • KUJUNDŽIĆ, Nedjelko [HR]/[HR] (UsOnly)
  • KOBREHEL, Gabrijela [HR]/[HR] (UsOnly)
  • MUTAK, Stjepan [HR]/[HR] (UsOnly)
  • MARŠIĆ, Nataša [HR]/[HR] (UsOnly)
Inventors
  • MARUŠIĆ-IŠTUK, Zorica
  • KUJUNDŽIĆ, Nedjelko
  • KOBREHEL, Gabrijela
  • MUTAK, Stjepan
  • MARŠIĆ, Nataša
Agents
  • PLIVA, FARMACEUTSKA INDUSTRIJA, DIONICKO DRUSTVO
  • PLIVA D.D.
Common Representative
  • PLIVA, FARMACEUTSKA INDUSTRIJA, DIONICKO DRUSTVO
Priority Data
P990130A03.05.1999HR
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) HALO DERIVATIVES OF 9-DEOXO-9A-AZA-9A-HOMERYTHROMYCIN A
(FR) DERIVES HALO DE 9-DESOXO-9A-AZA-9A-HOMOERYTHROMYCINE A
Abstract
(EN) The invention relates to halo derivatives of 9a-$i(N)-($i(N')-arylcarbamoyl)- and 9a-$i(N)-($i(N')- arylthiocarbamoyl) -9- deoxo-9a-aza-9a-homoerythromycin A of general formula (I) wherein R has the meaning of a substituted aryl group of formula (II) wherein substituents a, b, c, d and e are the same or different and at least one of them has the meaning of halo, a(C1-C6)haloalkyl or a (C1-C6)haloalkoxy group, whereas the remaining ones have the meaning of hydrogen, halo, a (C1-C6)alkyl or a (C1-C6)alkoxy group, and X has the meaning of oxygen or sulfur, and pharmaceutically acceptable addition salts thereof with inorganic or organic acids, to a process for the preparation, of pharmaceutical compositions comprising them and to the use of these pharmaceutical compositions for the treatment or prevention of bacterial infections.
(FR) L'invention se rapporte à des dérivés halo de 9a-$i(N)-($i(N')-arylcarbamoyl)- and 9a-$i(N)-($i(N')-arylthiocarbamoyl)-9-désoxo-9a-aza-9a-homoérythromycine A, représentés par la formule (I) dans laquelle R représente un groupe aryle substitué de formule (II) où les substituants a, b, c, d et e sont identiques ou différents et représentent, au moins pour l'un d'entre eux, un groupe halo, un groupe haloalkyle (C1-C6) ou haloalcoxy (C1-C6), tandis que les autres substituants représentent hydrogène, halo, un groupe alkyle (C1-C6) ou alcoxy (C1-C6), et X représente oxygène ou soufre. L'invention se rapporte également à des sels d'addition pharmaceutiquement acceptables de ces composés obtenus avec des acides inorganiques ou organiques. Elle se rapporte également à un procédé de préparation de compositions pharmaceutiques contenant ces composés ainsi qu'à l'utilisation de ces compositions pharmaceutiques pour le traitement ou la prévention d'infections bactériennes.
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