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1. WO1991000867 - 5'-DIPHOSPHOHEXOSE NUCLEOSIDE PHARMACEUTICAL COMPOSITIONS

Publication Number WO/1991/000867
Publication Date 24.01.1991
International Application No. PCT/US1990/003852
International Filing Date 10.07.1990
Chapter 2 Demand Filed 07.02.1991
IPC
C07H 19/10 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro derivatives thereof
02sharing nitrogen
04Heterocyclic radicals containing only nitrogen as ring hetero atom
06Pyrimidine radicals
10with the saccharide radical being esterified by phosphoric or polyphosphoric acids
C07H 19/20 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro derivatives thereof
02sharing nitrogen
04Heterocyclic radicals containing only nitrogen as ring hetero atom
16Purine radicals
20with the saccharide radical being esterified by phosphoric or polyphosphoric acids
CPC
A61K 31/70
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
C07H 19/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides ; Anhydro-derivatives thereof
02sharing nitrogen
04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
06Pyrimidine radicals
C07H 19/10
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides ; Anhydro-derivatives thereof
02sharing nitrogen
04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
06Pyrimidine radicals
10with the saccharide radical esterified by phosphoric or polyphosphoric acids
C07H 19/20
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides ; Anhydro-derivatives thereof
02sharing nitrogen
04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
16Purine radicals
20with the saccharide radical esterified by phosphoric or polyphosphoric acids
Y02A 50/475
YSECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
50in human health protection
30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
46Medical treatment of waterborne diseases characterized by the agent
468The waterborne disease being caused by a bacteria
475of the genus Shigella, i.e. Dysentery
Y02A 50/478
YSECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
50in human health protection
30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
46Medical treatment of waterborne diseases characterized by the agent
468The waterborne disease being caused by a bacteria
478of the genus Legionella, i.e. Legionellosis or Legionnaires' disease
Applicants
  • UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC. [US/US]; Boyd Graduate Studies Research Center Athens, GA 30602, US
  • UAB RESEARCH FOUNDATION [US/US]; 1825 University Boulevard Room 204, Mortimer Jordan Hall Birmingham, AL 35294, US
  • SCHINAZI, Raymond, F. [US/US]; US
  • SHAFER, William, M. [US/US]; US
Inventors
  • SCHINAZI, Raymond, F.; US
  • SHAFER, William, M.; US
  • SOMMADOSSI, Jean-Pierre; US
  • CHU, Chung, K.; US
Agents
  • PRATT, John, S. ; Kilpatrick & Cody 100 Peachtree Street Suite 3100 Atlanta, GA 30303, US
Priority Data
377,61710.07.1989US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) 5'-DIPHOSPHOHEXOSE NUCLEOSIDE PHARMACEUTICAL COMPOSITIONS
(FR) COMPOSITIONS PHARMACEUTIQUES DE NUCLEOSIDE DE 5'-DIPHOSPHOHEXOSE
Abstract
(EN)
This invention provides compounds and pharmaceutical compositions that include compounds of formula (I) in which A, B and C are hydrogen, halogen, or azido; D is hydrogen, halogen, azido, or OH; A and B or C and D can be replaced with a double bond; R is an aldohexose, aldohexosamine, or N-acetyl aldohexosamine, W is O or S; X is O, S, or CH2; Y is a purine or pyrimidine base, Z is C, S, or O, and wherein when Z is S or O, A and C are not present. The compounds of this invention have enhanced pharmaceutical or biological activity or increased intracellular absorption compared to the corresponding parent nucleoside as a function of the 5'-diphosphohexose moiety. Many of these compounds have antiviral, including anti-HIV, activity. Others have antibacterial activity. In one embodiment, the invention is a method to treat HIV infection and opportunistic infections concomitantly.
(FR)
L'invention concerne des composés et des compositions pharmaceutiques qui comprennent les composés de la formule (I) dans laquelle A, B et C représentent un hydrogène, un halogène ou un azido; D représente un hydrogène, un halogène, un azido ou OH; A et B ou C et D peuvent être remplacés par une double liaison; R représente aldohexose, aldohexosamine ou N-acétyle aldohexosamine; W représente O ou S; X représente O, S ou CH2; Y représente une base de purine ou de pyrimidine, Z représente C, S ou O et, lorsque Z représente S ou O, alors A et C ne sont pas présents. Les composés de cette invention ont une activité pharmaceutique ou biolgique intensifiée ou une plus grande absorption intracellulaire par rapport au nucléoside parent correspondant en fonction de la fraction 5'-diphosphohexose. Un grand nombre de ces composés ont une activité antivirale, y compris une activité anti-HIV. D'autres ont une activité antibactérienne. Dans un mode de réalisation, l'invention concerne une méthode pour traiter l'infection par le virus HIV et les infections concomitantes.
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