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
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
Sloan Kettering Institute for Cancer Research
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 Sloan Kettering Institute for Cancer Research filed Critical Sloan Kettering Institute for Cancer Research
Application granted granted Critical
Publication of DE2965318D1 publication Critical patent/DE2965318D1/de
Expired legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • A61P31/04—Antibacterial agents
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • C07H19/12—Triazine radicals

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (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 (de)
EP (1) EP0010205B1 (de)
JP (1) JPS5549395A (de)
AU (1) AU533135B2 (de)
CA (1) CA1131626A (de)
DE (1) DE2965318D1 (de)
ES (1) ES484626A1 (de)
HU (1) HU182597B (de)

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ZA859008B (en) * 1984-12-04 1987-07-29 Lilly Co Eli The treatment of tumors in mammals
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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
ATE113059T1 (de) * 1987-06-24 1994-11-15 Florey Howard Inst Nukleosid-derivate.
JPH02501354A (ja) * 1987-09-22 1990-05-17 テンプル・ユニバーシティ 人工ｄｎａ塩基対類似体
US4908440A (en) * 1987-11-12 1990-03-13 Bristol Myers Company 2',3'-dideoxy-2'-fluoroarabinopyrimidine nucleosides
EP0346108A3 (de) * 1988-06-09 1991-04-24 The Wellcome Foundation Limited Anti-infektiöse Nukleoside
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
NZ234534A (en) * 1989-07-17 1994-12-22 Univ Birmingham Pyrimidine 4'-thionucleoside derivatives and their preparation; intermediates therefor
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
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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
HUT63852A (en) * 1991-06-21 1993-10-28 Acic Canada Inc Process for producing antiviral compounds and pharmaceutical compositions comprising same as active ingredient
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FI105556B (fi) * 1991-09-30 2000-09-15 Sankyo Co Menetelmä lääkeaineina käyttökelpoisten pyrimidiiniukleosidijohdannaisten valmistamiseksi, joilla on kasvaimen vastaista vaikutusta
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
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
CN1086519A (zh) * 1992-06-22 1994-05-11 伊莱利利公司 立体有择阴离子糖基化方法
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
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
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
PL186888B1 (pl) * 1997-01-24 2004-03-31 Conpharma As Pochodne gemcytabiny
EP2390257A1 (de) * 1998-02-25 2011-11-30 Emory University 2'-Fluornucleoside
PT1411954E (pt) * 2000-10-18 2011-03-16 Pharmasset Inc Nucleosídeos modificados para o tratamento de infecções virais e proliferação celular anormal
US8481712B2 (en) 2001-01-22 2013-07-09 Merck Sharp & Dohme Corp. Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
KR20050059975A (ko) 2001-06-22 2005-06-21 파마셋 인코포레이티드 β-2'- 또는 3'-할로뉴클레오시드
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
TWI444731B (zh) 2006-05-16 2014-07-11 Semiconductor Energy Lab 液晶顯示裝置和半導體裝置
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
WO2012142075A1 (en) 2011-04-13 2012-10-18 Merck Sharp & Dohme Corp. 2'-azido substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases
CA2832459A1 (en) 2011-04-13 2012-10-18 Merck Sharp & Dohme Corp. 2'-substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases
CA2832449A1 (en) 2011-04-13 2012-10-18 Vinay GIRIJAVALLABHAN 2'-cyano substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases
US9416154B2 (en) 2011-07-13 2016-08-16 Merck Sharp & Dohme Corp. 5′-substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases
EP2731433A4 (de) 2011-07-13 2014-12-31 Merck Sharp & Dohme 5'-substituierte nukleosidanaloga und verfahren zu ihrer verwendung zur behandlung von virenerkrankungen
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KR20160030876A (ko) * 2013-04-29 2016-03-21 플라스미아 바이오텍 에스엘 약제학적 활성 성분들로써 뉴클레오시드 유사체들의 생물촉매적 생산
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TWI787201B (zh) 2016-08-31 2022-12-21 日商富士軟片股份有限公司 抗腫瘤劑、抗腫瘤效果增強劑及抗腫瘤用套組
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US3687931A (en) * 1970-03-19 1972-08-29 Syntex Corp Halogenated purine and pyrimidine nucleosides and process therefor
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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
JPS5549395A (en) 1980-04-09
AU533135B2 (en) 1983-11-03
EP0010205B1 (de) 1983-05-04
ES484626A1 (es) 1980-05-16
CA1131626A (en) 1982-09-14
US4211773A (en) 1980-07-08
AU5075779A (en) 1980-04-17
HU182597B (en) 1984-02-28
JPS6254315B2 (de) 1987-11-13
EP0010205A1 (de) 1980-04-30

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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