ATE314077T1 - 5-fluoro-2',3'-ungesättigte pyrimidinnucleoside - Google Patents

5-fluoro-2',3'-ungesättigte pyrimidinnucleoside

Info

Publication number
ATE314077T1
ATE314077T1 AT96902772T AT96902772T ATE314077T1 AT E314077 T1 ATE314077 T1 AT E314077T1 AT 96902772 T AT96902772 T AT 96902772T AT 96902772 T AT96902772 T AT 96902772T AT E314077 T1 ATE314077 T1 AT E314077T1
Authority
AT
Austria
Prior art keywords
pharmaceutically acceptable
fluoro
pyrimidine nucleosides
fluoroü
carboxamido
Prior art date
Application number
AT96902772T
Other languages
English (en)
Inventor
Raymond F Schinazi
Dennis C Liotta
Original Assignee
Univ Emory
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
Application filed by Univ Emory filed Critical Univ Emory
Application granted granted Critical
Publication of ATE314077T1 publication Critical patent/ATE314077T1/de

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Organic Chemistry (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Immunology (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
AT96902772T 1995-01-27 1996-01-29 5-fluoro-2',3'-ungesättigte pyrimidinnucleoside ATE314077T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US08/379,276 US5703058A (en) 1995-01-27 1995-01-27 Compositions containing 5-fluoro-2',3'-didehydro-2',3'-dideoxycytidine or a mono-, di-, or triphosphate thereof and a second antiviral agent
PCT/US1996/000965 WO1996022778A1 (en) 1995-01-27 1996-01-29 Derivatives of succinamide and their use as metalloproteinase inhibitor

Publications (1)

Publication Number Publication Date
ATE314077T1 true ATE314077T1 (de) 2006-01-15

Family

ID=23496579

Family Applications (1)

Application Number Title Priority Date Filing Date
AT96902772T ATE314077T1 (de) 1995-01-27 1996-01-29 5-fluoro-2',3'-ungesättigte pyrimidinnucleoside

Country Status (10)

Country Link
US (6) US5703058A (de)
EP (2) EP0805683B1 (de)
JP (3) JPH10512887A (de)
AT (1) ATE314077T1 (de)
AU (1) AU717580B2 (de)
CA (1) CA2211612C (de)
DE (1) DE69635656T2 (de)
DK (1) DK0805683T3 (de)
ES (1) ES2255710T3 (de)
WO (1) WO1996022778A1 (de)

Families Citing this family (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6228860B1 (en) * 1990-11-13 2001-05-08 Biochem Pharma Inc. Substituted 1,3-oxathiolanes with antiviral properties
US6369066B1 (en) 1990-11-13 2002-04-09 Biochem Pharma, Inc. Substituted 1,3-oxathiolanes with antiviral properties
US5703058A (en) 1995-01-27 1997-12-30 Emory University Compositions containing 5-fluoro-2',3'-didehydro-2',3'-dideoxycytidine or a mono-, di-, or triphosphate thereof and a second antiviral agent
US6391859B1 (en) * 1995-01-27 2002-05-21 Emory University [5-Carboxamido or 5-fluoro]-[2′,3′-unsaturated or 3′-modified]-pyrimidine nucleosides
US20030100532A1 (en) * 1997-02-14 2003-05-29 Gary S. Jacob Use of n-substituted-1,5-dideoxy-1,5-imino-d-glucitol compounds in combination therapy for treating hepatitis virus infections
US6689759B1 (en) * 1998-02-12 2004-02-10 G. D. Searle & Co. Methods of Treating hepatitis virus infections with N-substituted-1,5-dideoxy-1,5-imino-d-glucitol compounds in combination therapy
DE69932154T2 (de) * 1998-02-12 2007-05-31 G.D. Searle Llc, Chicago Verwendung von n-substituirten-1,5-dideoxy-1,5-imino-d-glucitolen zur behandlung von hepatitis infektionen
EP1754710A3 (de) * 1998-02-25 2007-12-19 Emory University 2'-Fluoronukleoside
WO1999043691A1 (en) * 1998-02-25 1999-09-02 Emory University 2'-fluoronucleosides
KR100886653B1 (ko) 1998-02-25 2009-03-04 에모리 유니버시티 2'-플루오로뉴클레오사이드
AU4219799A (en) * 1998-05-29 1999-12-13 University Of Florida Combination therapy for treatment of fiv infection
US6875773B1 (en) 1998-05-29 2005-04-05 Ben M. Dunn Combination therapy for treatment of FIV infection
CA2335617C (en) * 1998-06-24 2009-12-15 Novirio Pharmaceuticals Limited Use of 3'-azido-2',3'-dideoxyuridine in combination with further anti-hiv drugs for the manufacture of a medicament for the treatment of hiv
DE69939604D1 (de) * 1998-11-02 2008-10-30 Gilead Sciences Inc Kombinationstherapie zur Behandlung von Hepatitis B Infektionen
WO2000026225A2 (en) 1998-11-05 2000-05-11 Centre National De La Recherche Scientifique Nucleosides with anti-hepatitis b virus activity
US6407077B1 (en) 1998-11-05 2002-06-18 Emory University β-L nucleosides for the treatment of HIV infection
US7635690B2 (en) 1999-01-22 2009-12-22 Emory University HIV-1 mutations selected for by β-2′,3′-didehydro-2′,3′-dideoxy-5-fluorocytidine
US7115584B2 (en) * 1999-01-22 2006-10-03 Emory University HIV-1 mutations selected for by β-2′,3′-didehydro-2′,3′-dideoxy-5-fluorocytidine
EP1731155A3 (de) * 1999-01-22 2007-02-21 Emory University Beta-d-2', 3' -didehydro-2', 3' -dideoxy-5-fluorocytidine für die verwendung in der behandlung von hiv infektionen
CN101219148A (zh) * 1999-01-22 2008-07-16 爱莫里大学 由β-2’,3’-二脱氢-2’,3’-二脱氧-5-氟胞苷选择的HIV-1突变
JP2003505501A (ja) 1999-02-12 2003-02-12 ジー・ディー・サール・アンド・カンパニー 肝炎ウィルス感染の処置のためのグルカミン化合物
ATE402701T1 (de) * 1999-02-12 2008-08-15 United Therapeutics Corp N-(8,8,8-trifluorooctyl)-1,5-dideoxy-1,5-imino- - glucitol zur behandlung von hepatitis-virus- infektionen
AU6792700A (en) * 1999-08-20 2001-03-19 Research Foundation Of The State University Of New York, The 5-propynylpyrimidine derivatives as cytotoxic enzyme inhibitors
KR100325682B1 (ko) * 1999-10-25 2002-02-25 김태성 2',3'-디디하이드로-2',3'-디데옥시시티딘 유도체의 제조방법
JP2003522791A (ja) * 2000-02-14 2003-07-29 ファルマシア コーポレイション 肝炎ウイルス感染症治療用ｎ‐置換‐１，５‐ジデオキシ‐１，５‐イミノ‐ｄ‐グルシトール化合物の使用
EP1964569A3 (de) 2000-04-13 2009-07-22 Pharmasset, Inc. 3'- oder 2'-Hydroxymethyl-substituierte Nukleosidderivate zur Behandlung von Virusinfektionen
US6787526B1 (en) 2000-05-26 2004-09-07 Idenix Pharmaceuticals, Inc. Methods of treating hepatitis delta virus infection with β-L-2′-deoxy-nucleosides
US6875751B2 (en) * 2000-06-15 2005-04-05 Idenix Pharmaceuticals, Inc. 3′-prodrugs of 2′-deoxy-β-L-nucleosides
WO2002032920A2 (en) 2000-10-18 2002-04-25 Pharmasset Limited Modified nucleosides for treatment of viral infections and abnormal cellular proliferation
CA2439836A1 (en) * 2001-03-01 2002-09-12 Pharmasset, Inc. Method for the synthesis of 2',3'-dideoxy-2',3'-didehydronucleosides
AU2002255707A1 (en) 2001-03-15 2002-10-03 Trustees Of Boston College, The Selective anti-viral nucleoside chain terminators
EP1478322A4 (de) * 2001-06-22 2007-08-08 Pharmasset Ltd Beta-2'-OR 3'-HALONUCLEOSIDE
US7462733B2 (en) 2001-07-30 2008-12-09 University Of Southern California Preparation and use of α-keto phosphonates
AU2002365234B2 (en) * 2001-12-14 2009-01-29 Pharmasset Inc N4-acylcytosine nucleosides for treatment of viral infections
MXPA04009986A (es) * 2002-04-12 2005-08-16 Achillion Pharmaceuticals Inc Metodo para sintetizar beta-l-5-fluoro-2¦,3¦-didesoxi-2¦,3¦-dideshidrocitidina (¦-l-fd4c).
AU2003253888A1 (en) * 2002-07-15 2004-02-02 Gilead Sciences, Inc. Combination therapies with l-fmau for the treatment of hepatitis b virus infection
US20040157793A1 (en) * 2002-11-12 2004-08-12 Stuyver Lieven J. Modified nucleosides as antiviral agents
HUE029877T2 (en) * 2003-05-30 2017-04-28 Gilead Pharmasset Llc Modified fluorinated nucleoside analogues
AU2004296877A1 (en) * 2003-12-09 2005-06-23 Incyte Corporation Dosing methods for ss-D-2',3'-dideoxy-2',3'-didehydro-5-fluorocytidine antiviral therapy
US7741334B2 (en) * 2004-04-01 2010-06-22 Achillion Pharmaceuticals, Inc. Low dose therapy for treating viral infections
CN101023094B (zh) * 2004-07-21 2011-05-18 法莫赛特股份有限公司 烷基取代的2-脱氧-2-氟代-d-呋喃核糖基嘧啶和嘌呤及其衍生物的制备
US8492539B2 (en) 2004-09-14 2013-07-23 Gilead Pharmasset Llc Preparation of 2′-fluoro-2′-alkyl-substituted or other optionally substituted ribofuranosyl pyrimidines and purines and their derivatives
CA2584670A1 (en) * 2004-10-19 2006-04-27 Achillion Pharmaceuticals, Inc. Combination therapy for treating viral infections
WO2006055754A1 (en) * 2004-11-19 2006-05-26 Boehringer Ingelheim International Gmbh Method for treating hiv infection through co-administration of tipranavir and reverset
US7645752B2 (en) * 2006-01-13 2010-01-12 Wyeth Llc Sulfonyl substituted 1H-indoles as ligands for the 5-hydroxytryptamine receptors
FR2907786B1 (fr) * 2006-10-27 2009-09-18 Univ Grenoble 1 Thionucleosides et applications pharmaceutiques
US7964580B2 (en) 2007-03-30 2011-06-21 Pharmasset, Inc. Nucleoside phosphoramidate prodrugs
CA2684061A1 (en) * 2007-04-10 2008-10-16 Emory University Novel hiv-1 reverse transcriptase codon deletion and its use in the management and treatment of hiv infections
RU2373218C2 (ru) * 2007-08-10 2009-11-20 Роберт Шалвович Бибилашвили 5'-фосфорсодержащие производные 2',3'-дидезокси-3'-тиацитидина новые противовирусные агенты
BRPI0816498A2 (pt) * 2007-10-02 2019-02-26 Emory University combinações potentes de zidovudina e drogas que selecionam para a mutuação k65r na polimerase do hiv
US8173621B2 (en) 2008-06-11 2012-05-08 Gilead Pharmasset Llc Nucleoside cyclicphosphates
PA8855601A1 (es) 2008-12-23 2010-07-27 Forformidatos de nucleósidos
AU2009329872B2 (en) 2008-12-23 2016-07-07 Gilead Pharmasset Llc Synthesis of purine nucleosides
NZ593649A (en) * 2008-12-23 2013-11-29 Gilead Pharmasset Llc Nucleoside analogs
TWI583692B (zh) * 2009-05-20 2017-05-21 基利法瑪席特有限責任公司 核苷磷醯胺
US8618076B2 (en) 2009-05-20 2013-12-31 Gilead Pharmasset Llc Nucleoside phosphoramidates
WO2011035120A2 (en) * 2009-09-17 2011-03-24 Gk Ventures, L.L.C. Therapeutic composition to treat lesions caused by herpes simplex virus
US8563530B2 (en) 2010-03-31 2013-10-22 Gilead Pharmassel LLC Purine nucleoside phosphoramidate
SG184324A1 (en) 2010-03-31 2012-11-29 Gilead Pharmasset Llc Nucleoside phosphoramidates
CA2818853A1 (en) 2010-11-30 2012-06-07 Gilead Pharmasset Llc 2'-spirocyclo-nucleosides for use in therapy of hcv or dengue virus
EP2709613B2 (de) 2011-09-16 2020-08-12 Gilead Pharmasset LLC Verfahren zur behandlung von hcv
US8889159B2 (en) 2011-11-29 2014-11-18 Gilead Pharmasset Llc Compositions and methods for treating hepatitis C virus
EP2950786B1 (de) 2013-01-31 2019-11-27 Gilead Pharmasset LLC Kombinationsformulierung zweier antiviraler verbindungen
PT3038601T (pt) 2013-08-27 2020-06-30 Gilead Pharmasset Llc Formulação combinada de dois compostos antivirais

Family Cites Families (97)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US521161A (en) * 1894-06-12 Broom-head
US400137A (en) * 1889-03-26 Louis steinberger
US2248776A (en) * 1938-07-28 1941-07-08 Bell Telephone Labor Inc Wave filter
US3116282A (en) * 1960-04-27 1963-12-31 Upjohn Co Pyrimidine nucleosides and process
US3346561A (en) * 1965-10-24 1967-10-10 Merck & Co Inc Pyrimidine 3-deoxynucleosides
US3553192A (en) * 1968-07-15 1971-01-05 Robugen Gmbh Substituted (2'-deoxyribosyl) uracil compounds, compositions containing same and process of making and using same
US3817982A (en) 1971-12-29 1974-06-18 Syntex Inc 2{40 ,3{40 -unsaturated nucleosides and method of making
US4000137A (en) * 1975-06-10 1976-12-28 American Home Products Corporation Antitumor derivatives of periodate-oxidized nucleosides
JPS5668674A (en) * 1979-11-08 1981-06-09 Shionogi & Co Ltd 5-fluorouracil derivative
ES8801303A1 (es) * 1985-05-15 1987-12-16 Wellcome Found Un procedimiento para preparar una formulacion farmaceutica que contiene un 2'3'-didesoxi-nucleosido.
AU570853B2 (en) * 1985-08-26 1988-03-24 United States of America, as represented by the Secretary, U.S. Department of Commerce, The Inhibition of infectivity and cytopathic effect of htlv-111/ lav by purine bases
US4879277A (en) * 1985-08-26 1989-11-07 The United States Of America As Represented By The Department Of Health And Human Services Antiviral compositions and methods
DE3650741T2 (de) * 1985-09-17 2000-10-12 The Wellcome Foundation Ltd., Greenford Kombination therapeutische Nukleoside mit weiteren therapeutisch wirksamen Komponenten.
IN164556B (de) * 1986-03-06 1989-04-08 Takeda Chemical Industries Ltd
JPS62242624A (ja) * 1986-04-15 1987-10-23 Asahi Glass Co Ltd 抗腫瘍剤
US4916122A (en) * 1987-01-28 1990-04-10 University Of Georgia Research Foundation, Inc. 3'-Azido-2',3'-dideoxyuridine anti-retroviral composition
US5446029A (en) * 1986-07-04 1995-08-29 Medivir Ab Anti-retroviral activity of 2',3'-dideoxy-3'-fluoronucleosides
DD279407A1 (de) * 1986-07-24 1990-06-06 Akad Wissenschaften Ddr Verfahren zur herstellung eines mittels gegen aids
US4788181A (en) * 1986-09-29 1988-11-29 The United States Of America As Represented By The Department Of Health And Human Services 5-substituted-2',3'-dideoxycytidine compounds with anti-HTLV-III activity
US4963533A (en) * 1986-10-24 1990-10-16 Stichting Rega Vzw (Rega) Therapeutic application of dideoxycytidinene
US5215971A (en) * 1986-12-19 1993-06-01 Medivir Ab Antiviral pharmaceutical composition comprising 5-substituted pyrimidine nucleosides
SE469823B (sv) 1987-02-23 1993-09-27 Univ Western Australia Ledmekanism för robotarmar
IL85778A0 (en) * 1987-03-20 1988-09-30 Bristol Myers Co Production of 2',3'-dideoxynucleosides and certain such novel compounds
AU613026B2 (en) * 1987-03-24 1991-07-25 Nycomed As 2',3' dideoxyribofuranoxide derivatives
US5185437A (en) * 1987-04-09 1993-02-09 Burroughs Wellcome Co. Therapeutic nucleosides
SE8701605D0 (sv) * 1987-04-16 1987-04-16 Astra Ab Novel medicinal compounds
US5215970A (en) * 1987-04-16 1993-06-01 Medivir Ab Nucleosides and nucleotide analogues, pharmaceutical composition and processes for the preparation of the compounds
US5011774A (en) * 1987-07-17 1991-04-30 Bristol-Myers Squibb Co. Dideoxyinosine by enzymatic deamination of dideoxyadenosine
US5246924A (en) * 1987-09-03 1993-09-21 Sloan-Kettering Institute For Cancer Research Method for treating hepatitis B virus infections using 1-(2'-deoxy-2'-fluoro-beta-D-arabinofuranosyl)-5-ethyluracil
US5466806A (en) * 1989-02-08 1995-11-14 Biochem Pharma Inc. Processes for preparing substituted 1,3-oxathiolanes with antiviral properties
US5041449A (en) * 1988-04-11 1991-08-20 Iaf Biochem International, Inc. 4-(nucleoside base)-substituted-1,3-dioxolanes useful for treatment of retroviral infections
NZ228645A (en) * 1988-04-11 1991-09-25 Iaf Biochem Int 1,3-dioxolane derivatives substituted in the 5th position by a purine or pyrimidine radical; treatment of viral infections
US5270315A (en) * 1988-04-11 1993-12-14 Biochem Pharma Inc. 4-(purinyl bases)-substituted-1,3-dioxlanes
US5047407A (en) * 1989-02-08 1991-09-10 Iaf Biochem International, Inc. 2-substituted-5-substituted-1,3-oxathiolanes with antiviral properties
JPH02152976A (ja) * 1988-05-06 1990-06-12 Bristol Myers Co ２´，３´―ジデヒドロ―２´，３´―ジデオキシヌクレオシドのプロドラッグ
US4900828A (en) * 1988-05-12 1990-02-13 Hoffmann-Laroche Inc. Intermediate compounds and an improved procedure for the synthesis of 2',3'-dideoxycytidine
GB8815265D0 (en) * 1988-06-27 1988-08-03 Wellcome Found Therapeutic nucleosides
SE8802687D0 (sv) * 1988-07-20 1988-07-20 Astra Ab Nucleoside derivatives
EP0355031A3 (de) 1988-08-17 1990-12-27 MATTHES, Eckart, Dr. Substituierte Pyrimidinnucleoside, Verfahren zu ihrer Herstellung und sie enthaltende pharmazeutische Mittel
DE68922903T2 (de) * 1988-12-19 1995-11-23 Wellcome Found Antivirale Pyrimidin- und Purinverbindungen, Verfahren zu ihrer Herstellung und sie enthaltende pharmazeutische Präparate.
DK0674634T3 (da) * 1989-02-08 2003-08-04 Iaf Biochem Int Fremgangsmåde til fremstilling af substituerede 1,3-oxathiolaner med antivirale egenskaber
UA45942A (uk) * 1989-02-08 2002-05-15 Біокем Фарма, Інк. 1,3-оксатіолан, його похідні, спосіб (варіанти) його одержання та фармацевтична композиція
NZ233197A (en) * 1989-04-13 1991-11-26 Richard Thomas Walker Aromatically substituted nucleotide derivatives, intermediates therefor and pharmaceutical compositions
US5059690A (en) * 1990-03-01 1991-10-22 E. R. Squibb & Sons, Inc. Purinyl tetrahydrofurans
NL8901258A (nl) * 1989-05-19 1990-12-17 Stichting Rega V Z W 5-halogeno-2',3'-dideoxycytidinederivaten in geneesmiddelen voor het behandelen van retrovirus-infecties.
DD293498A5 (de) * 1989-07-20 1991-09-05 Zi Fuer Molekularbiologie Der Adw,De Verfahren zur herstellung eines mittels fuer die behandlung oder prophylaxe von hepatits-infektionen bei mensch und tier
US5071983A (en) * 1989-10-06 1991-12-10 Burroughs Wellcome Co. Therapeutic nucleosides
CA2073063A1 (en) 1989-11-06 1991-05-07 Jo Klaveness Nucleoside derivatives
CA2032259A1 (en) * 1989-12-18 1991-06-19 Wayne J. Thompson Hiv protease inhibitors useful for the treatment of aids
DE69031271T2 (de) * 1989-12-20 1998-02-26 Biotech Australia Pty Ltd Varianten von pai-2
IE904378A1 (en) * 1989-12-20 1991-07-03 Abbott Lab Analogs of oxetanyl purines and pyrimidines
US5276151A (en) * 1990-02-01 1994-01-04 Emory University Method of synthesis of 1,3-dioxolane nucleosides
US5204466A (en) * 1990-02-01 1993-04-20 Emory University Method and compositions for the synthesis of bch-189 and related compounds
US5527782A (en) * 1990-03-13 1996-06-18 Acic (Canada) Inc. 5-halo-2,3'-O-cyclocytidines
US5241069A (en) * 1990-04-06 1993-08-31 Glaxo Inc. Carbonate intermediates for the synthesis of purine substituted cyclopentene derivatives
US5128458A (en) * 1990-04-20 1992-07-07 Southern Research Institute 2',3'-dideoxy-4'-thioribonucleosides as antiviral agents
GB9009861D0 (en) * 1990-05-02 1990-06-27 Glaxo Group Ltd Chemical compounds
AU8239891A (en) * 1990-06-19 1992-01-07 Sloan-Kettering Institute For Cancer Research 5'-hydrogenphosphonates and 5'-methylphosphonates of sugar modified nucleosides, compositions and uses thereof
EP0465297B1 (de) * 1990-07-04 1996-01-31 Merrell Dow Pharmaceuticals Inc. 9-Purinyl-Phosphonsäurederivate
SE9003151D0 (sv) * 1990-10-02 1990-10-02 Medivir Ab Nucleoside derivatives
IT1246983B (it) * 1990-11-13 1994-12-12 Consiglio Nazionale Ricerche L-2'-desossiuridine e composizioni farmaceutiche che le contengono.
US5179104A (en) * 1990-12-05 1993-01-12 University Of Georgia Research Foundation, Inc. Process for the preparation of enantiomerically pure β-D-(-)-dioxolane-nucleosides
WO1992010496A1 (en) * 1990-12-05 1992-06-25 University Of Georgia Research Foundation, Inc. ENANTIOMERICALLY PURE β-L-(-)-1,3-OXATHIOLANE NUCLEOSIDES
US5248776A (en) * 1990-12-05 1993-09-28 University Of Georgia Research Foundation, Inc. Process for enantiomerically pure β-L-1,3-oxathiolane nucleosides
US5444063A (en) * 1990-12-05 1995-08-22 Emory University Enantiomerically pure β-D-dioxolane nucleosides with selective anti-Hepatitis B virus activity
IL100502A (en) * 1991-01-03 1995-12-08 Iaf Biochem Int PHARMACEUTICAL PREPARATIONS CONTAINING CIS-4-AMINO-1-) 2-HYDROXIMETHIL-1,3-OXETYOLEN-5-IL (-
IL100965A (en) * 1991-02-22 1999-12-31 Univ Emory 2-Hydroxymethyl-5-(5-fluorocytosin-l-yl)-1,3-oxathiolane its resolution and pharmaceutical compositions containing it
KR100270806B1 (ko) * 1991-03-06 2000-11-01 템블 존 엘 5-플루오로-2`-데옥시-3`-티아시티딘을 함유하는 b형 간염 치료를 위한 약제
GB9104740D0 (en) * 1991-03-06 1991-04-17 Wellcome Found Antiviral nucleoside combination
WO1992018517A1 (en) * 1991-04-17 1992-10-29 Yale University Method of treating or preventing hepatitis b virus
GB9110874D0 (en) * 1991-05-20 1991-07-10 Iaf Biochem Int Medicaments
ZA923640B (en) * 1991-05-21 1993-02-24 Iaf Biochem Int Processes for the diastereoselective synthesis of nucleosides
GB9111902D0 (en) * 1991-06-03 1991-07-24 Glaxo Group Ltd Chemical compounds
JP3042073B2 (ja) 1991-06-19 2000-05-15 味の素株式会社 ヌクレオシド誘導体とその製造方法
GB9116601D0 (en) * 1991-08-01 1991-09-18 Iaf Biochem Int 1,3-oxathiolane nucleoside analogues
US5233041A (en) * 1991-10-07 1993-08-03 Glaxo Group Limited Synthesis of a 3,4-dihydroxy-1-cyclopentanylpurinone from a 2,3-unsaturated-1-cyclopentanylpurinone
US5232300A (en) * 1992-01-17 1993-08-03 Paco Pharmaceutical Services, Inc. Brush decontamination kit
US5432165A (en) * 1992-04-06 1995-07-11 Oclassen Pharmaceuticals, Inc. Methods for the treatment of infection caused by Hepatitis B virus (HBV)
US5271186A (en) * 1992-05-13 1993-12-21 Perneczky George C Tandem pneumatic/hydraulic reciprocating cylinder with integral oil reservoir
AU4079593A (en) * 1992-05-13 1993-12-13 Wellcome Foundation Limited, The Therapeutic combinations
GB9307013D0 (en) * 1993-04-02 1993-05-26 Wellcome Found Therapeutic combinations
EP0626970A1 (de) * 1992-12-18 1994-12-07 The University Of Alberta Dihydropyrimidin nucleoside mit antivirale aktivität
GB9226927D0 (en) * 1992-12-24 1993-02-17 Iaf Biochem Int Dideoxy nucleoside analogues
US5329008A (en) * 1993-04-07 1994-07-12 Glaxo Inc. Synthesis of a 3,4-dihydroxy-1-cyclopentanylpurinone
AU685128B2 (en) * 1993-05-21 1998-01-15 Government Of The United States Of America, As Represented By The Secretary Of The Department Of Health And Human Services, The New procedure to block the replication of reverse transcriptase dependent viruses by the use of inhibitors of deoxynucleotides synthesis
TW374087B (en) 1993-05-25 1999-11-11 Univ Yale L-2',3'-dideoxy nucleotide analogs as anti-hepatitis B(HBV) and anti-HIV agents
US5627160A (en) * 1993-05-25 1997-05-06 Yale University L-2',3'-dideoxy nucleoside analogs as anti-hepatitis B (HBV) and anti-HIV agents
EP0631783A1 (de) 1993-06-03 1995-01-04 Mitsubishi Chemical Corporation Antivirale Kombinationen von 2',3-Di-deoxyribonukleosiden mit 6-benzyl-1-ethoxy-methyl-5-substituierten Uracil-Derivaten
CA2171550C (en) * 1993-09-10 2008-08-26 Raymond F. Schinazi Nucleosides with anti-hepatitis b virus activity
FR2709754B1 (fr) * 1993-09-10 1995-12-01 Centre Nat Rech Scient Composés 2' ou 3'-déoxy- et 2', 3'-didéoxy-beta-L-pentofuranonucléosides, procédé de préparation et application thérapeutique, notamment anti-virale.
US5521161A (en) * 1993-12-20 1996-05-28 Compagnie De Developpment Aguettant S.A. Method of treating HIV in humans by administration of ddI and hydroxycarbamide
US5811538A (en) * 1993-12-30 1998-09-22 Genta, Incorporated Process for the purification of oligomers
US5587362A (en) * 1994-01-28 1996-12-24 Univ. Of Ga Research Foundation L-nucleosides
US6391859B1 (en) 1995-01-27 2002-05-21 Emory University [5-Carboxamido or 5-fluoro]-[2′,3′-unsaturated or 3′-modified]-pyrimidine nucleosides
US5703058A (en) * 1995-01-27 1997-12-30 Emory University Compositions containing 5-fluoro-2',3'-didehydro-2',3'-dideoxycytidine or a mono-, di-, or triphosphate thereof and a second antiviral agent
US5869461A (en) * 1995-03-16 1999-02-09 Yale University Reducing toxicity of L-nucleosides with D-nucleosides
WO1999043691A1 (en) 1998-02-25 1999-09-02 Emory University 2'-fluoronucleosides

Also Published As

Publication number Publication date
DE69635656T2 (de) 2006-09-21
EP0805683A4 (de) 1999-09-01
AU4705696A (en) 1996-08-14
US20020198173A1 (en) 2002-12-26
ES2255710T3 (es) 2006-07-01
WO1996022778A1 (en) 1996-08-01
US7419966B2 (en) 2008-09-02
CA2211612A1 (en) 1996-08-01
JPH10512887A (ja) 1998-12-08
EP1361227A2 (de) 2003-11-12
EP0805683B1 (de) 2005-12-28
EP1361227A3 (de) 2004-03-03
EP0805683A1 (de) 1997-11-12
US5703058A (en) 1997-12-30
US6232300B1 (en) 2001-05-15
US20040167140A1 (en) 2004-08-26
JP2007246540A (ja) 2007-09-27
JP2005325128A (ja) 2005-11-24
US20080293668A1 (en) 2008-11-27
DK0805683T3 (da) 2006-05-22
AU717580B2 (en) 2000-03-30
DE69635656D1 (de) 2006-02-02
US6680303B2 (en) 2004-01-20
US5905070A (en) 1999-05-18
CA2211612C (en) 2006-08-15

Similar Documents

Publication Publication Date Title
ATE314077T1 (de) 5-fluoro-2',3'-ungesättigte pyrimidinnucleoside
ATE165004T1 (de) Ematiomerenreine beta-d-dioxolane nucleoside mit selektiver antihepatitis b-virus wirkung
IE860676L (en) Therapeutic nucleosides
NO963138D0 (no) L-Nukleosider for behandling av hepatit-B-virus og Epstein-bar-virus
EP1808434A3 (de) Verwendung von 5-Fluoro-2'-deoxy-3'-thiacytidin zur Behandlung von Hepatitis B
WO1992014743A3 (en) Antiviral activity and resolution of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane
DK224286A (da) 2',3'-dideoxy-nucleosider
MY102693A (en) Antiviral nucleosides
AU4461189A (en) Novel 2'-halomethylidene, 2'-ethenylidene and 2'-ethynyl cytidine, uridine and guanosine derivatives
NO904901L (no) N-substituerte derivater av 3r,4r-etyl-((1-metyl-1h-imidazol-5-yl)metyl) -2-pyrrolidinon.
ATE267198T1 (de) Synthese und anti-hiv und anti-hepatitis virus aktivität von 1,3-oxaselenolan nucleosiden
DK630589A (da) 2',3'-dideoxypurinnucleosid/purinnucleosid-phosphorylase-inhibitor-sammensaetning
DE68918215D1 (de) 2'-Halomethyliden, 2'-Ethenyliden und 2'-Ethynyl-Adenosinderivate.
DK291390D0 (da) Terapeutiske anvendelser af 2',5'-oligoadenylatderivater
NO891835D0 (no) Prodrug-former av 2',3'-didehydro-2',3'-dideoksy-nukleosider.
AU2487688A (en) Composition and method for treating hepatitis virus infections using 1-(2'-deoxy-2'-fluoro-beta-d-arabinofuranosyl)-5- ethyluracil
AU4544289A (en) Antiviral 5-propynyl pyrimidine nucleosides
WO1988003804A3 (en) Method of treating viral infections in humans and compositions therefor
FI96607C (fi) Menetelmä uusien terapeuttisesti käyttökelpoisten 2'-etenylideenisytidiini-, uridiini- ja guanosiinijohdannaisten valmistamiseksi
MY113560A (en) Use of 5-fluoro-2'-deoxy-3'-thiacytidine for the treatment of hepatitis b

Legal Events

Date Code Title Description
UEP Publication of translation of european patent specification

Ref document number: 0805683

Country of ref document: EP

REN Ceased due to non-payment of the annual fee