DE2965318D1 - 5-substituted 1-(2'-deoxy-2'-substituted-beta-d-arabinofuranosyl) pyrimidine nucleosides and pharmaceutical compositions containing them - Google Patents

5-substituted 1-(2'-deoxy-2'-substituted-beta-d-arabinofuranosyl) pyrimidine nucleosides and pharmaceutical compositions containing them

Info

Publication number
DE2965318D1
DE2965318D1 DE7979103673T DE2965318T DE2965318D1 DE 2965318 D1 DE2965318 D1 DE 2965318D1 DE 7979103673 T DE7979103673 T DE 7979103673T DE 2965318 T DE2965318 T DE 2965318T DE 2965318 D1 DE2965318 D1 DE 2965318D1
Authority
DE
Germany
Prior art keywords
substituted
arabinofuranosyl
deoxy
beta
pharmaceutical compositions
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.)
Expired
Application number
DE7979103673T
Other languages
German (de)
English (en)
Inventor
Carlos Lopez
Kyoichi A Watanabe
Uri Reichman
Jack J Fox
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.)
Memorial Sloan Kettering Cancer Center
Original Assignee
Memorial Sloan Kettering Cancer Center
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 Memorial Sloan Kettering Cancer Center filed Critical Memorial Sloan Kettering Cancer Center
Application granted granted Critical
Publication of DE2965318D1 publication Critical patent/DE2965318D1/de
Expired legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06Pyrimidine radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/12Triazine radicals

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
DE7979103673T 1978-10-02 1979-09-27 5-substituted 1-(2'-deoxy-2'-substituted-beta-d-arabinofuranosyl) pyrimidine nucleosides and pharmaceutical compositions containing them Expired DE2965318D1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US05/948,189 US4211773A (en) 1978-10-02 1978-10-02 5-Substituted 1-(2'-Deoxy-2'-substituted-β-D-arabinofuranosyl)pyrimidine nucleosides

Publications (1)

Publication Number Publication Date
DE2965318D1 true DE2965318D1 (en) 1983-06-09

Family

ID=25487441

Family Applications (1)

Application Number Title Priority Date Filing Date
DE7979103673T Expired DE2965318D1 (en) 1978-10-02 1979-09-27 5-substituted 1-(2'-deoxy-2'-substituted-beta-d-arabinofuranosyl) pyrimidine nucleosides and pharmaceutical compositions containing them

Country Status (8)

Country Link
US (1) US4211773A (enExample)
EP (1) EP0010205B1 (enExample)
JP (1) JPS5549395A (enExample)
AU (1) AU533135B2 (enExample)
CA (1) CA1131626A (enExample)
DE (1) DE2965318D1 (enExample)
ES (1) ES484626A1 (enExample)
HU (1) HU182597B (enExample)

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ZA859008B (en) * 1984-12-04 1987-07-29 Lilly Co Eli The treatment of tumors in mammals
JPS61204193A (ja) * 1985-03-05 1986-09-10 Takeda Chem Ind Ltd シトシンヌクレオシド類の製造法
CA1295998C (en) * 1985-07-29 1992-02-18 Sai P. Sunkara Nucleosides and their use as antineoplastic agents
NO170884C (no) * 1986-08-18 1992-12-23 Hoffmann La Roche Analogifremgangsmaate ved fremstilling av terapeutisk aktive pyrimidinderivater
GB8629892D0 (en) * 1986-12-15 1987-01-28 Wellcome Found Antiviral compounds
CA1340032C (en) * 1987-06-24 1998-09-08 Jim Haralambidis Lucleoside derivatives
DE3871778T2 (de) * 1987-09-22 1993-01-21 Univ Temple Kuenstliche analogen der dns-basenpaare.
US4908440A (en) * 1987-11-12 1990-03-13 Bristol Myers Company 2',3'-dideoxy-2'-fluoroarabinopyrimidine nucleosides
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SE8802173D0 (sv) * 1988-06-10 1988-06-10 Astra Ab Pyrimidine derivatives
GB8827339D0 (en) * 1988-11-23 1988-12-29 Wellcome Found Antiviral compounds
US5006646A (en) * 1989-02-22 1991-04-09 Yuki Gosei Kogyo Co., Ltd. Process for preparing 2'-deoxy-5-trifluoromethyl-beta-uridine
FI95384C (fi) * 1989-04-06 1996-01-25 Squibb Bristol Myers Co Menetelmä 3'-deoksi-3'-substituoitujen metyylinukleosidien valmistamiseksi ja menetelmässä käytettäviä välituotteita
US6258360B1 (en) * 1989-05-04 2001-07-10 Igen International, Inc. Prodrugs activated by targeted catalytic proteins
GB8912972D0 (en) * 1989-06-06 1989-07-26 Wellcome Found Therapeutic nucleosides
IE902574A1 (en) * 1989-07-17 1991-02-27 Univ Birmingham Antiviral pyrimidine nucleosides
US5134066A (en) * 1989-08-29 1992-07-28 Monsanto Company Improved probes using nucleosides containing 3-dezauracil analogs
US5200514A (en) * 1990-01-19 1993-04-06 University Of Georgia Research Foundation, Inc. Synthesis of 2'-deoxypyrimidine nucleosides
US5352584A (en) * 1990-01-22 1994-10-04 E. R. Squibb & Sons, Inc. Monoclonal antibodies which bind (E)-5- (2-bromovinyl)-arabinofuranosyluracil and diagnostic methods based thereon
GB9009861D0 (en) * 1990-05-02 1990-06-27 Glaxo Group Ltd Chemical compounds
US5817799A (en) * 1990-07-23 1998-10-06 The United States Of America As Represented By The Department Of Health And Human Services 2'-Fluorofuranosyl derivatives and methods for preparing 2'-fluoropyrimidine and 2'-fluoropurine nucleosides
DE550714T1 (de) * 1991-06-21 1995-06-14 Acic Canada Inc Antiviralverbindungen und Ihrer Verfahren zur Herstellung.
US5248771A (en) * 1991-06-26 1993-09-28 Triumf Process for preparing no-carrier-added radiohalogenated vinyl nucleosides
RU2085557C1 (ru) * 1991-09-30 1997-07-27 Санкио Компани Лимитед Производные нуклеозидов пиримидина или их фармацевтически приемлемые соли и способ их получения
GB2260319B (en) * 1991-10-07 1995-12-06 Norsk Hydro As Acyl derivatives of nucleosides and nucleoside analogues having anti-viral activity
HU207524B (en) * 1991-11-22 1993-04-28 Mta Koezponti Kemiai Kutato In Industrial process for producing 5-alkyl-2'-deoxy-beta-uridines with stereoselective synthesis
FR2688003B1 (fr) * 1992-02-28 1995-06-30 Univ Limoges Derives de nucleosides, leur preparation et leurs applications biologiques.
US5432165A (en) * 1992-04-06 1995-07-11 Oclassen Pharmaceuticals, Inc. Methods for the treatment of infection caused by Hepatitis B virus (HBV)
US5821357A (en) * 1992-06-22 1998-10-13 Eli Lilly And Company Stereoselective glycosylation process for preparing 2'-deoxy-2',2'-difluoropurine and triazole nucleosides
US5401838A (en) * 1992-06-22 1995-03-28 Eli Lilly And Company Stereoselective fusion glycosylation process for preparing 2'-deoxy-2',2'-difluoronucleosides and 2'-deoxy-2'-fluoronucleosides
US5606048A (en) * 1992-06-22 1997-02-25 Eli Lilly And Company Stereoselective glycosylation process for preparing 2'-Deoxy-2', 2'-difluoronucleosides and 2'-deoxy-2'-fluoronucleosides
IL106078A0 (en) * 1992-06-22 1993-10-20 Lilly Co Eli Stereoselective anion glycosylation process
US5426183A (en) * 1992-06-22 1995-06-20 Eli Lilly And Company Catalytic stereoselective glycosylation process for preparing 2'-deoxy-2',2'-difluoronucleosides and 2'-deoxy-2'-fluoronucleosides
US5594124A (en) * 1992-06-22 1997-01-14 Eli Lilly And Company Stereoselective glycosylation process for preparing 2'-Deoxy-2',2'-difluoropyrimidine nucleosides and 2'-deoxy-2'-fluoropyrimidine nucleosides and intermediates thereof
US5371210A (en) * 1992-06-22 1994-12-06 Eli Lilly And Company Stereoselective fusion glycosylation process for preparing 2'-deoxy-2',2'-difluoronucleosides and 2'-deoxy-2'-fluoronucleosides
US6040298A (en) * 1992-12-23 2000-03-21 Oclassen Pharmaceuticals, Inc. Methods for treatment with compositions effective against acyclovir-resistant strains of herpes viruses
US5424416A (en) * 1993-08-25 1995-06-13 Eli Lilly And Company Process for preparation of 2-deoxy-2,2-difluoro-D-ribofuranosyl-3,5-hydroxy protected-1-alkyl and aryl sulfonates and their use in preparation of 2',2'-difluoro-2'-deoxy nucleosides
US5811073A (en) * 1995-06-19 1998-09-22 President And Fellows Of Harvard College Method for radioisotopic detection and localization of inflammation in a host
US6331287B1 (en) * 1995-08-23 2001-12-18 University Advanced Bio-Imaging Associates 2′-deoxy-2′-fluoro-d-arabinofuranosyl pyrimidine nucleoside
US5756775A (en) * 1995-12-13 1998-05-26 Eli Lilly And Company Process to make α,α-difluoro-β-hydroxyl thiol esters
US6001994A (en) * 1995-12-13 1999-12-14 Eli Lilly And Company Process for making gemcitabine hydrochloride
ATE236188T1 (de) * 1997-01-24 2003-04-15 Conpharma As Gemcitabin-derivate
EA008609B1 (ru) * 1998-02-25 2007-06-29 Эмори Юниверсити 2'-фторнуклеозиды
CA2426187C (en) * 2000-10-18 2011-08-16 Pharmasset Limited Modified nucleosides for the treatment of viral infections and abnormal cellular proliferation
US8481712B2 (en) 2001-01-22 2013-07-09 Merck Sharp & Dohme Corp. Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
US6949522B2 (en) 2001-06-22 2005-09-27 Pharmasset, Inc. β-2′- or 3′-halonucleosides
AU2003278904A1 (en) * 2002-09-24 2004-04-19 Kornis Pharmaceuticals, Incorporated 1, 3, 5-triazines for treatment of viral diseases
US8895531B2 (en) * 2006-03-23 2014-11-25 Rfs Pharma Llc 2′-fluoronucleoside phosphonates as antiviral agents
TWI764143B (zh) 2006-05-16 2022-05-11 日商半導體能源研究所股份有限公司 液晶顯示裝置
US20090274686A1 (en) * 2008-05-02 2009-11-05 Yat Sun Or Nucleoside phosphonate derivatives
US9011817B2 (en) * 2009-09-03 2015-04-21 The Board Of Trustees Of The Leland Stanford Junior University Compounds and methods of making compounds
CN103582420B (zh) 2011-04-13 2016-10-19 默沙东公司 2’-取代的核苷衍生物和使用其治疗病毒病的方法
US9156872B2 (en) 2011-04-13 2015-10-13 Merck Sharp & Dohme Corp. 2′-azido substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases
WO2012142093A2 (en) 2011-04-13 2012-10-18 Merck Sharp & Dohme Corp. 2'-cyano substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases
WO2013009735A1 (en) 2011-07-13 2013-01-17 Merck Sharp & Dohme Corp. 5'-substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases
WO2013009737A1 (en) 2011-07-13 2013-01-17 Merck Sharp & Dohme Corp. 5'-substituted nucleoside analogs and methods of use thereof for the treatment of viral diseases
CA3107640A1 (en) 2011-12-22 2013-06-27 Janssen Biopharma, Inc. Substituted nucleosides, nucleotides and analogs thereof and their use in ameliorating or treating a disease or condition associated with viral infections
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CA2880794C (en) 2012-08-13 2018-08-28 Fujifilm Corporation Synthetic intermediate of 1-(2-deoxy-2-fluoro-4-thio-.beta.-d-arabinofuranosyl)cytosine, synthetic intermediate of thionucleoside, and methods for producing the same
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US3873516A (en) * 1973-05-29 1975-03-25 Miles Lab Process for the preparation of 1-{8 {62 -D-2-substituted-2-deoxyribofuranosyl{9 -pyrimidines
US3870700A (en) * 1973-05-29 1975-03-11 Miles Lab 2-halogeno-2-deoxy-5-(substituted)uridines

Also Published As

Publication number Publication date
HU182597B (en) 1984-02-28
JPS6254315B2 (enExample) 1987-11-13
AU533135B2 (en) 1983-11-03
ES484626A1 (es) 1980-05-16
JPS5549395A (en) 1980-04-09
US4211773A (en) 1980-07-08
EP0010205A1 (en) 1980-04-30
CA1131626A (en) 1982-09-14
AU5075779A (en) 1980-04-17
EP0010205B1 (en) 1983-05-04

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Free format text: VOSSIUS, V., DIPL.-CHEM. DR.RER.NAT. TAUCHNER, P., DIPL.-CHEM. DR.RER.NAT. HEUNEMANN, D., DIPL.-PHYS. DR.RER.NAT. RAUH, P., DIPL.-CHEM. DR.RER.NAT. HERMANN, G., DIPL.-PHYS. DR.RER.NAT., PAT.-ANWAELTE, 8000 MUENCHEN