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1. WO2000039139 - ANTI-(RETRO)VIRAL CONJUGATES OF SACCHARIDES AND ACETAMIDINO OR GUANIDINO COMPOUNDS

Publication Number WO/2000/039139
Publication Date 06.07.2000
International Application No. PCT/IL1999/000704
International Filing Date 28.12.1999
Chapter 2 Demand Filed 13.07.2000
IPC
C07H 3/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
3Compounds containing only hydrogen atoms and saccharide radicals having only carbon, hydrogen, and oxygen atoms
04Disaccharides
C07H 3/06 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
3Compounds containing only hydrogen atoms and saccharide radicals having only carbon, hydrogen, and oxygen atoms
06Oligosaccharides, i.e. having three to five saccharide radicals attached to each other by glycosidic linkages
C07H 7/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
7Compounds containing non-saccharide radicals linked to saccharide radicals by a carbon-to-carbon bond
C07H 15/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
15Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
02Acyclic radicals, not substituted by cyclic structures
04attached to an oxygen atom of a saccharide radical
CPC
A61P 31/12
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12Antivirals
A61P 31/14
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12Antivirals
14for RNA viruses
A61P 31/18
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12Antivirals
14for RNA viruses
18for HIV
C07H 15/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
15Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
02Acyclic radicals, not substituted by cyclic structures
04attached to an oxygen atom of the saccharide radical
C07H 3/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
3Compounds containing only hydrogen atoms and saccharide radicals having only carbon, hydrogen, and oxygen atoms
04Disaccharides
C07H 3/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
3Compounds containing only hydrogen atoms and saccharide radicals having only carbon, hydrogen, and oxygen atoms
06Oligosaccharides, i.e. having three to five saccharide radicals attached to each other by glycosidic linkages
Applicants
  • YEDA RESEARCH AND DEVELOPMENT CO. LTD. [IL/IL]; Weizmann Institute of Science P.O. Box 95 76100 Rehovot, IL (AllExceptUS)
  • LAPIDOT, Aviva [IL/IL]; IL (UsOnly)
  • LITOVCHICK, Alexander [IL/IL]; IL (UsOnly)
  • EVDOKIMOV, Artem [UA/US]; IL (UsOnly)
Inventors
  • LAPIDOT, Aviva; IL
  • LITOVCHICK, Alexander; IL
  • EVDOKIMOV, Artem; IL
Agents
  • BEN-AMI, Paulina; Yeda Research and Development Co. Ltd. Weizmann Institute of Science P.O. Box 95 76100 Rehovot, IL
Priority Data
12777328.12.1998IL
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) ANTI-(RETRO)VIRAL CONJUGATES OF SACCHARIDES AND ACETAMIDINO OR GUANIDINO COMPOUNDS
(FR) CONJUGUES ANTI-RETROVIRAUX DE SACCHARIDES ET DE COMPOSES ACETAMIDINO OU GUANIDINO
Abstract
(EN)
Conjugates of saccharide and an acetamidino- or guanidino- compounds of formula (I), wherein A is CH3 or NH2; X is a linear or branched C1-C8 alkyl chain optionally containing hydroxy, amino and/or oxo groups; n is an integer from 1 to 6, and Sac is the residue of a mono- or oligo-saccharide are useful as antiviral, particularly as antiretroviral, agents, and can be used either alone or together with other compounds used in AIDS treatment such as AZT and/or protease inhibitors, for the treatment of HIV-infection, AIDS and manifestations of AIDS such as Kaposi sarcoma. Particularly preferred compounds are aminoglycoside-arginine conjugates in which the saccharide is a natural aminoglycoside antibiotic such as kanamycin, gentamycin and neomycin that is conjugated to arginine residues.
(FR)
Conjugués de saccharides et de composés acétamidino ou guanidino représentés par la formule (I), dans laquelle A représente CH3 ou NH2; X représente une chaîne alkyle C1-C8 linéaire ou ramifiée contenant éventuellement des groupes hydroxy, amino et/ou oxo ; n est un entier de 1 à 6 et Sac est le résidu d'un mono-ou oligosaccharide. Ces conjugués sont utiles en tant qu'agents antiviraux, particulièrement, en tant qu'agent antirétroviraux, et on peut les utiliser soit seuls, soit avec d'autres composés faisant partie du traitement du SIDA, tels qu'AZT et/ou des inhibiteurs de protéase, pour le traitement de l'infection par VIH, du SIDA et des manifestations du SIDA, telles que le sarcome de Kaposi. Des composés particulièrement préférés consistent en des conjugués d'aminoglycoside-arginine dans lesquels le saccharide est un antibiotique naturel d'aminoglycoside, tel que kanamycine, gentamycine et néomycine, conjugué à des résidus d'arginine.
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