Search International and National Patent Collections
Some content of this application is unavailable at the moment.
If this situation persists, please contact us atFeedback&Contact
1. (WO1992010497) ENANTIOMERICALLY PURE $g(b)-D-(-)-DIOXOLANE-NUCLEOSIDES
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1992/010497 International Application No.: PCT/US1991/009124
Publication Date: 25.06.1992 International Filing Date: 05.12.1991
Chapter 2 Demand Filed: 29.06.1992
IPC:
A61K 31/506 (2006.01) ,A61K 31/675 (2006.01) ,A61K 31/7076 (2006.01) ,C07D 327/04 (2006.01) ,C07D 405/04 (2006.01) ,C07D 411/04 (2006.01) ,C07D 473/00 (2006.01) ,C07D 497/08 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506
not condensed and containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
66
Phosphorus compounds
675
having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
70
Carbohydrates; Sugars; Derivatives thereof
7042
Compounds having saccharide radicals and heterocyclic rings
7052
having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
706
containing six-membered rings with nitrogen as a ring hetero atom
7064
containing condensed or non-condensed pyrimidines
7076
containing purines, e.g. adenosine, adenylic acid
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
327
Heterocyclic compounds containing rings having oxygen and sulfur atoms as the only ring hetero atoms
02
one oxygen atom and one sulfur atom
04
Five-membered rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
411
Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
473
Heterocyclic compounds containing purine ring systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
497
Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms
02
in which the condensed system contains two hetero rings
08
Bridged systems
Applicants:
UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC. [US/US]; Boyd Graduate Studies Research Center Athens, GA 30602, US
EMORY UNIVERSITY [US/US]; 1380 S. Oxford Road Atlanta, GA 30322, US
Inventors:
CHUNG, K., Chu; US
RAYMOND, F., Schinazi; US
Agent:
PRATT, John, S. ; Kilpatrick & Cody 1100 Peachtree Street Suite 2800 Atlanta, GA 30309-6555, US
ZALESKY, Cheryl, K. ; Kilpatrick & Cody 1100 Peachtree Street Suite 2800 Atlanta, GA 30309-4530, US
Priority Data:
622,76205.12.1990US
Title (EN) ENANTIOMERICALLY PURE $g(b)-D-(-)-DIOXOLANE-NUCLEOSIDES
(FR) NUCLEOSIDES DE $g(b)-D-(-)-DIOXOLANE ENANTIOMERIQUEMENT PURS
Abstract:
(EN) An asymmetric process for the preparation of enantiomerically pure $g(b)-D-(-)-dioxolane-nucleosides. The enantiomerically pure dioxolane nucleosides are active HIV agents, that are significantly more effective than the prior prepared racemic mixtures of the nucleosides. The anti-viral activity of the compounds is surprising in light of the generally accepted theory that moieties in the endo conformation, including these dioxolanes, are not effective antiviral agents. The toxicity of the enantiomerically pure dioxolane nucleosides is lower than that of the racemic mixture of the nucleosides, because the nonnaturally occurring $g(a)-isomer is not included. The product can be used as a research tool to study the inhibition of HIV $i(in vitro) or can be administered in a pharmaceutical composition to inhibit the growth of HIV $i(in vivo).
(FR) Est décrit un procédé asymétrique pour la préparation de nucléosides de $g(b)-D-(-)-dioxolane énantiomériquement purs. Ces nucléosides de dioxolane énantiomériquement purs sont des agents actifs contre le VIH, qui sont considérablement plus efficaces que les mélanges racémiques des nucléosides préparés antérieurement. L'activité antivirale des composés est étonnante à la lumière de la théorie généralement admise que des fractions dans la conformation endo, y compris ces dioxolanes, ne sont pas des agents antiviraux efficaces. La toxicité des nucléosides de dioxolane énantiomériquement purs est inférieure à celle du mélange racémique des nucléosides, car l'$g(a)-isomère qui ne se rencontre pas à l'état naturel n'est pas inclus. Ce produit peut s'utiliser comme outil de recherche pour étudier l'inhibition du VIH $i(in vitro) ou peut être administré dans une composition pharmaceutique pour inhiber la croissance du VIH $i(in vivo).
Designated States: AU, CA, JP
European Patent Office (AT, BE, CH, DE, DK, ES, FR, GB, GR, IT, LU, MC, NL, SE)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
ES2291268EP0562009JP2007008959US5925643JP3421335JPH07502973
JP2001097973 CA2099589CA2590125AU1991091259AU1991091475AU1997016640