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WO1992014743A3 - Activite antivirale et resolution de 2-hydroxymethyl-5-5-fluorocytosine-1-yl-1,3-oxathiolane - Google Patents

Activite antivirale et resolution de 2-hydroxymethyl-5-5-fluorocytosine-1-yl-1,3-oxathiolane Download PDF

Info

Publication number
WO1992014743A3
WO1992014743A3 PCT/US1992/001339 US9201339W WO9214743A3 WO 1992014743 A3 WO1992014743 A3 WO 1992014743A3 US 9201339 W US9201339 W US 9201339W WO 9214743 A3 WO9214743 A3 WO 9214743A3
Authority
WO
WIPO (PCT)
Prior art keywords
fluorocytosin
oxathiolane
hydroxymethyl
resolution
pharmaceutically acceptable
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/US1992/001339
Other languages
English (en)
Other versions
WO1992014743A2 (fr
Inventor
Dennis C Liotta
Raymond F Schinazi
Woo-Baeg Choi
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Emory University
Original Assignee
Emory University
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=35276919&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=WO1992014743(A3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from US07/659,760 external-priority patent/US5210085A/en
Priority to KR1019930702516A priority Critical patent/KR0172590B1/ko
Priority to CA002104399A priority patent/CA2104399C/fr
Priority to AU15617/92A priority patent/AU665187C/en
Priority to JP4507549A priority patent/JP2901160B2/ja
Priority to RO93-01137A priority patent/RO119365B1/ro
Priority to PL92300471A priority patent/PL169842B1/pl
Priority to HU9302377A priority patent/HU227823B1/hu
Application filed by Emory University filed Critical Emory University
Priority to PL92310211A priority patent/PL171150B1/pl
Priority to BR9205661A priority patent/BR9205661A/pt
Publication of WO1992014743A2 publication Critical patent/WO1992014743A2/fr
Publication of WO1992014743A3 publication Critical patent/WO1992014743A3/fr
Priority to FI933684A priority patent/FI114915B/fi
Priority to NO19932980A priority patent/NO312399B1/no
Priority to BG98062A priority patent/BG62053B1/bg
Anticipated expiration legal-status Critical
Priority to FI20030932A priority patent/FI20030932A7/fi
Priority to NO2005015C priority patent/NO2005015I2/no
Priority to NO2008010C priority patent/NO2008010I1/no
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—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
    • C07D405/02—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 containing two hetero rings
    • C07D405/04—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 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D411/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D411/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D411/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06—Pyrimidine radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06—Pyrimidine radicals
    • C07H19/10—Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Virology (AREA)
  • Biochemistry (AREA)
  • Communicable Diseases (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • AIDS & HIV (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Medicinal Preparation (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

L'invention décrit un procédé et une composition servant au traitement d'infections dues au VIH et au virus de l'hépatite B chez l'homme et comprenant l'administration d'une dose efficace de 2-hydroxyméthyl-5-(5-fluorocytosine-1-yl)-1,3-oxathiolane, d'un de ses dérivés acceptable pharmaceutiquement, y compris d'un dérivé alkylé ou acylé en 5' ou N4, ou d'un de ses sels acceptable pharmaceutiquement, contenus dans un vecteur acceptable pharmaceutiquement. L'invention décrit également un procédé de résolution d'un mélange racémique d'énantiomères de nucléosides, comprenant l'étape d'exposition dudit mélange racémique à une enzyme qui, de préférence, catalyse une réaction dans l'un des énantiomères.
PCT/US1992/001339 1991-02-22 1992-02-20 Activite antivirale et resolution de 2-hydroxymethyl-5-5-fluorocytosine-1-yl-1,3-oxathiolane Ceased WO1992014743A2 (fr)

Priority Applications (15)

Application Number Priority Date Filing Date Title
BR9205661A BR9205661A (pt) 1991-02-22 1992-02-20 Resoluçoes de (+) - - D-L, (-) -1, (+) - B -D, - 2 - hidroximetil - 5 - (5-fluorocitosin - 1IL-) -1,3 - oxatiolana, composto, composiçao, farmaceutica, processo para tratar infecçao por HIV em seres humanos, processo para tratar infecçao HBV em um ser humano ou outro animal hospedeiro, processo para preparaçao de 2 hodroximetil -5- (5-fluorocitosin-1-IL) -1,3- oxatiolana e processo para resoluçao de mistura racemica de enantiomeros de nucleosideo
PL92310211A PL171150B1 (pl) 1991-07-26 1992-02-20 Sposób rozdzielania racemicznej mieszaniny enancjomerów nukleozydu PL PL
CA002104399A CA2104399C (fr) 1991-02-22 1992-02-20 Activite et resolution antivirale du 2-hydroxymethyl-5-(5-fluorocytosine-1-yl)-1,3-oxathiolane
AU15617/92A AU665187C (en) 1991-02-22 1992-02-20 Antiviral activity and resolution of 2-hydroxymethyl-5-(5-fluorocytosin-1-YL)-1,3-oxathiolane
JP4507549A JP2901160B2 (ja) 1991-02-22 1992-02-20 ２−ヒドロキシメチル−５−（５−フルオロシトシン−１−イル）−１，３−オキサチオランの抗ウィルス活性および分割
KR1019930702516A KR0172590B1 (ko) 1991-02-22 1992-02-20 2-히드록시메틸-5-(5-플루오로시토신-1-일)-1,3-옥사티올란의 항비루스 활성 및 그것의 분해방법
RO93-01137A RO119365B1 (ro) 1991-02-22 1992-02-20 Derivaţi de 1,3-oxatiolan, compoziţie farmaceutică şi metodă pentru tratarea infecţiei hiv
PL92300471A PL169842B1 (pl) 1991-02-22 1992-02-20 Sposób wytwarzania 2-hydroksymetylo-5-(5-fluorocytozynylo-1)-1,3-oksatiolanu PL PL
HU9302377A HU227823B1 (en) 1991-02-22 1992-02-20 Pharmaceutical compositions comprising 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane and further antiviral agent
FI933684A FI114915B (fi) 1991-02-22 1993-08-20 Menetelmä terapeuttisesti käyttökelpoisten beta-2-hydroksimetyyli-5-(5-fluorisytosin-1-yyli)-1,3-oksatiolaanin enantiomeerien valmistamiseksi
BG98062A BG62053B1 (bg) 1991-02-22 1993-08-20 (-)-бета-l-2-хидроксиметил-5-(5-флуороцитозин-1-ил)-1,3-оксатиолан, методиза получаването му, фармацевтичен състав на негова база иприложението му като антивирусно средство
NO19932980A NO312399B1 (no) 1991-02-22 1993-08-20 Terapeutisk aktiv forbindelse, preparat inneholdende forbindelsen samt dens anvendelse
FI20030932A FI20030932A7 (fi) 1991-02-22 2003-06-24 Menetelmä cis-FTC:n enantiomeerien erottamiseksi
NO2005015C NO2005015I2 (no) 1991-02-22 2005-07-01 Terapeutisk aktiv forbindelse preparat inneholdende forbindelsen samt den anvendelse
NO2008010C NO2008010I1 (no) 1991-02-22 2008-06-13 Kombinasjon av efavirenz, emtricitabin og tenofovirdisoproks: 1 eller salter derav

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US659,760 1991-02-22
US07/659,760 US5210085A (en) 1990-02-01 1991-02-22 Method for the synthesis, compositions and use of 2'-deoxy-5-fluoro-3'-thiacytidine and related compounds
US73608991A 1991-07-26 1991-07-26
US736,089 1991-07-26
US83115392A 1992-02-12 1992-02-12
US831,153 1992-02-12

Publications (2)

Publication Number Publication Date
WO1992014743A2 WO1992014743A2 (fr) 1992-09-03
WO1992014743A3 true WO1992014743A3 (fr) 1992-10-29

Family

ID=35276919

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1992/001339 Ceased WO1992014743A2 (fr) 1991-02-22 1992-02-20 Activite antivirale et resolution de 2-hydroxymethyl-5-5-fluorocytosine-1-yl-1,3-oxathiolane

Country Status (24)

Country Link
EP (3) EP0575482A1 (fr)
JP (2) JP2901160B2 (fr)
KR (1) KR0172590B1 (fr)
CN (4) CN1037682C (fr)
AT (2) ATE270291T1 (fr)
AU (2) AU679649B2 (fr)
BG (1) BG62053B1 (fr)
BR (1) BR9205661A (fr)
CA (2) CA2513440C (fr)
CZ (1) CZ295074B6 (fr)
DE (2) DE69233786D1 (fr)
DK (2) DK0984013T3 (fr)
ES (2) ES2345102T3 (fr)
FI (2) FI114915B (fr)
HU (2) HU227823B1 (fr)
IE (1) IE920545A1 (fr)
IL (1) IL100965A (fr)
MX (1) MX9200747A (fr)
MY (1) MY114350A (fr)
NO (3) NO312399B1 (fr)
NZ (2) NZ250842A (fr)
PT (1) PT100151B (fr)
RO (2) RO122814B1 (fr)
WO (1) WO1992014743A2 (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9045520B2 (en) 2008-12-23 2015-06-02 Gilead Pharmasset Llc Synthesis of purine nucleosides
US9545414B2 (en) 2005-06-13 2017-01-17 Bristol-Myers Squibb & Gilead Sciences, Llc Unitary pharmaceutical dosage form

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WO2021209563A1 (fr) 2020-04-16 2021-10-21 Som Innovation Biotech, S.A. Composés destinés à être utilisés dans le traitement d'infections virales par un coronavirus associé au syndrome respiratoire
WO2022011554A1 (fr) * 2020-07-14 2022-01-20 四川大学 Dérivé contenant de l'azote d'acide 3-désoxy-2-cétonique, son procédé de préparation et son utilisation

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US9045520B2 (en) 2008-12-23 2015-06-02 Gilead Pharmasset Llc Synthesis of purine nucleosides

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MX9200747A (es) 1992-09-01
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CN1084745C (zh) 2002-05-15
CN1109108C (zh) 2003-05-21
CZ49792A3 (en) 1993-03-17
EP1439177B1 (fr) 2010-05-26
CA2513440A1 (fr) 1992-09-03
FI933684A0 (fi) 1993-08-20
NO2008010I1 (no) 2008-07-07
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HUT65548A (en) 1994-06-28
HU211344A9 (en) 1995-11-28
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BG98062A (bg) 1994-04-29
JP2901160B2 (ja) 1999-06-07
JP3292830B2 (ja) 2002-06-17
AU8077398A (en) 1998-10-15
WO1992014743A2 (fr) 1992-09-03
IE920545A1 (en) 1992-08-26
ATE469147T1 (de) 2010-06-15
JPH10147586A (ja) 1998-06-02
CA2104399C (fr) 2005-10-18
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PT100151A (pt) 1993-05-31
KR0172590B1 (ko) 1999-02-01
DE69233379T2 (de) 2005-07-14
EP0984013B1 (fr) 2004-06-30
HK1026419A1 (en) 2000-12-15
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