ATE486882T1 - Nukleotidanaloge - Google Patents

Nukleotidanaloge

Info

Publication number
ATE486882T1
ATE486882T1 AT94929832T AT94929832T ATE486882T1 AT E486882 T1 ATE486882 T1 AT E486882T1 AT 94929832 T AT94929832 T AT 94929832T AT 94929832 T AT94929832 T AT 94929832T AT E486882 T1 ATE486882 T1 AT E486882T1
Authority
AT
Austria
Prior art keywords
nucleotide analogues
analogs
ester
nucleotide analogs
nucleotide
Prior art date
Application number
AT94929832T
Other languages
English (en)
Inventor
Norbert Bischofberger
Robert Jones
Murty Arimilli
Kuei-Ying Lin
Michael Louie
Lawwrence Mcgee
Ernest PRISBE
William Lee
Kenneth Cundy
Original Assignee
Gilead Sciences Inc
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
Priority claimed from US08/123,483 external-priority patent/US5656745A/en
Application filed by Gilead Sciences Inc filed Critical Gilead Sciences Inc
Application granted granted Critical
Publication of ATE486882T1 publication Critical patent/ATE486882T1/de

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
    • C07H19/16—Purine radicals
    • C07H19/20—Purine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic 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
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • 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
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6509—Six-membered rings
    • C07F9/6512—Six-membered rings having the nitrogen atoms in positions 1 and 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C07F9/65616—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing the ring system having three or more than three double bonds between ring members or between ring members and non-ring members, e.g. purine or analogs
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6571—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
    • C07F9/657163—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms the ring phosphorus atom being bound to at least one carbon atom
    • C07F9/657181—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms the ring phosphorus atom being bound to at least one carbon atom the ring phosphorus atom and, at least, one ring oxygen atom being part of a (thio)phosphonic acid derivative
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6571—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
    • C07F9/6574—Esters of oxyacids of phosphorus
    • C07F9/65742—Esters of oxyacids of phosphorus non-condensed with carbocyclic rings or heterocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6571—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
    • C07F9/6574—Esters of oxyacids of phosphorus
    • C07F9/65744—Esters of oxyacids of phosphorus condensed with carbocyclic or heterocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6578—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and sulfur atoms with or without oxygen atoms, as ring hetero atoms
    • C07F9/65785—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and sulfur atoms with or without oxygen atoms, as ring hetero atoms the ring phosphorus atom and, at least, one ring sulfur atom being part of a thiophosphonic acid derivative
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H11/00—Compounds containing saccharide radicals esterified by inorganic acids; Metal salts thereof
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Oscillators With Electromechanical Resonators (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Steroid Compounds (AREA)
  • Peptides Or Proteins (AREA)
AT94929832T 1993-09-17 1994-09-16 Nukleotidanaloge ATE486882T1 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US08/123,483 US5656745A (en) 1993-09-17 1993-09-17 Nucleotide analogs
US19334194A 1994-02-08 1994-02-08
PCT/US1994/010539 WO1995007920A1 (en) 1993-09-17 1994-09-16 Nucleotide analogs

Publications (1)

Publication Number Publication Date
ATE486882T1 true ATE486882T1 (de) 2010-11-15

Family

ID=42066188

Family Applications (1)

Application Number Title Priority Date Filing Date
AT94929832T ATE486882T1 (de) 1993-09-17 1994-09-16 Nukleotidanaloge

Country Status (8)

Country Link
EP (1) EP0719273B1 (de)
JP (1) JP4086314B2 (de)
AT (1) ATE486882T1 (de)
AU (1) AU691527B2 (de)
BR (1) BR9407510A (de)
CA (1) CA2171743C (de)
DE (1) DE69435319D1 (de)
WO (1) WO1995007920A1 (de)

Families Citing this family (52)

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CA2171868A1 (en) * 1993-09-17 1995-03-23 Petr Alexander Method for dosing therapeutic compounds
US5798340A (en) 1993-09-17 1998-08-25 Gilead Sciences, Inc. Nucleotide analogs
US5659023A (en) * 1995-02-01 1997-08-19 Gilead Sciences, Inc. Nucleotide analogues
GB9505025D0 (en) 1995-03-13 1995-05-03 Medical Res Council Chemical compounds
US5977061A (en) * 1995-04-21 1999-11-02 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic N6 - substituted nucleotide analagues and their use
AU1427097A (en) * 1995-12-29 1997-07-28 Gilead Sciences, Inc. Nucleotide analogs
US5717095A (en) * 1995-12-29 1998-02-10 Gilead Sciences, Inc. Nucleotide analogs
WO1998004569A1 (en) * 1996-07-26 1998-02-05 Gilead Sciences, Inc. Nucleotide analogs
US5922695A (en) * 1996-07-26 1999-07-13 Gilead Sciences, Inc. Antiviral phosphonomethyoxy nucleotide analogs having increased oral bioavarilability
US5935946A (en) * 1997-07-25 1999-08-10 Gilead Sciences, Inc. Nucleotide analog composition and synthesis method
CZ297264B6 (cs) 1998-09-09 2006-10-11 Metabasis Therapeutics, Inc. Nové heteroaromatické inhibitory fruktóza-1,6-bisfosfatázy
GB9821058D0 (en) 1998-09-28 1998-11-18 Univ Cardiff Chemical compound
CN1740182A (zh) * 1999-12-22 2006-03-01 症变治疗公司 新的双氨基化膦酸酯前药
AU2006202624B2 (en) * 1999-12-22 2008-08-14 Metabasis Therapeutics, Inc. Novel bisamidate phosphonate prodrugs
EP1607401A1 (de) 2000-03-08 2005-12-21 Metabasis Therapeutics, Inc. Neue Aryl-Fructose-1,6-Bisphosphatase-Inhibitoren
US7563774B2 (en) 2000-06-29 2009-07-21 Metabasis Therapeutics, Inc. Combination of FBPase inhibitors and antidiabetic agents useful for the treatment of diabetes
HRP20030047B1 (hr) 2000-07-21 2016-02-26 Gilead Sciences, Inc. Prolijekovi koji su fosfonatni analozi nukleotida i metode njihovog odabira te njihova priprava
BRPI0210746B8 (pt) 2001-06-29 2021-05-25 Inst Of Organic Chemistry And Biochemistry Ascr derivados de 6-'2-(fosfonometóxi)alcóxi-pirimidina e seu método de preparação
IL164809A0 (en) 2002-05-13 2005-12-18 Metabasis Therapeutics Inc Novel phosphonic acid basdrugs of pmea and its analogues
PL376474A1 (en) 2002-10-31 2005-12-27 Metabasis Therapeutics, Inc. Novel cyclic phosphate diesters of 1,3-propane-1-aryl diols and their use in preparing prodrugs
PT1583542E (pt) 2003-01-14 2008-09-17 Gilead Sciences Inc Composições e métodos para terapia de combinação antiviral
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NZ543864A (en) 2003-06-16 2009-10-30 Leuven K U Res & Dev Pyrimidine compounds having phosphonate groups as antiviral nucleotide analogs
US20060252729A1 (en) 2003-07-30 2006-11-09 Krawczyk Steven H Nucleobase phosphonate analogs for antiviral treatment
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PT2258376T (pt) 2004-07-27 2019-05-31 Gilead Sciences Inc Análogos fosfonatados de compostos inibidores do vih
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TWI471145B (zh) 2005-06-13 2015-02-01 Bristol Myers Squibb & Gilead Sciences Llc 單一式藥學劑量型
US7893264B2 (en) 2006-07-07 2011-02-22 Gilead Sciences, Inc. Antiviral phosphinate compounds
WO2008005542A2 (en) 2006-07-07 2008-01-10 Gilead Sciences, Inc., Antiviral phosphinate compounds
AU2007342367B2 (en) * 2007-01-05 2012-12-06 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Nucleoside aryl phosphoramidates for the treatment of RNA-dependent RNA viral infection
TWI444384B (zh) 2008-02-20 2014-07-11 Gilead Sciences Inc 核苷酸類似物及其在治療惡性腫瘤上的用途
BRPI0915878A2 (pt) 2008-07-08 2015-11-03 Gilead Sciences Inc sais ou hidratos de compostos inibidores de hiv, seu uso e composição farmacêutica que os compreende
CA2857490C (en) 2011-12-22 2020-03-31 Geron Corporation Guanine analogs as telomerase substrates and telomere length affectors
KR102072041B1 (ko) 2011-12-22 2020-01-31 앨리오스 바이오파마 인크. 치환된 뉴클레오사이드, 뉴클레오타이드 및 그의 유사체
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USRE48171E1 (en) 2012-03-21 2020-08-25 Janssen Biopharma, Inc. Substituted nucleosides, nucleotides and analogs thereof
CN102786549B (zh) * 2012-08-13 2013-07-03 洛阳聚慧投资股份有限公司 一组具有抑制hiv-1病毒复制活性的替诺福韦双酯化合物、制备方法及其药物用途
CN107312039B (zh) 2012-08-30 2019-06-25 江苏豪森药业集团有限公司 一种替诺福韦前药的制备方法
AU2014250762A1 (en) 2013-04-12 2015-10-29 Achillion Pharmaceuticals, Inc. Highly active nucleoside derivative for the treatment of HCV
EP3623364A1 (de) 2014-02-13 2020-03-18 Ligand Pharmaceuticals, Inc. Organische verbindungen und deren verwendungen
CN106687118A (zh) 2014-07-02 2017-05-17 配体药物公司 前药化合物及其用途
WO2016106050A1 (en) 2014-12-26 2016-06-30 Emory University N4-hydroxycytidine and derivatives and anti-viral uses related thereto
WO2017100108A1 (en) * 2015-12-10 2017-06-15 Merck Sharp & Dohme Corp. Antiviral phosphodiamide prodrugs of tenofovir
US10450335B2 (en) 2015-12-15 2019-10-22 Merck Sharp & Dohme Corp. Antiviral oxime phosphoramide compounds
WO2018080903A1 (en) 2016-10-26 2018-05-03 Merck Sharp & Dohme Corp. Antiviral aryl-amide phosphodiamide compounds
EP3558322B1 (de) 2016-12-22 2021-09-29 Merck Sharp & Dohme Corp. Antivirale benzyl-amin-phosphodiamidverbindungen
PT3661937T (pt) 2017-08-01 2021-09-24 Gilead Sciences Inc Formas cristalinas de ((s)-((((2r,5r)-5-(6-amino-9h-purin-9-il)-4-fluoro-2,5-dihidrofurano-2-il)oxi)metil)(fenoxi)fosforil)-l-alaninato de etil (gs-9131) para tratamento de infeções virais
RU2020116571A (ru) 2017-12-07 2021-11-22 Эмори Юниверсити N4-гидроксицитидин и производные и связанные с этим противовирусные применения
WO2019139919A1 (en) 2018-01-09 2019-07-18 Ligand Pharmaceuticals, Inc. Acetal compounds and therapeutic uses thereof
EP3823629B1 (de) 2018-07-19 2024-12-25 Merck Sharp & Dohme LLC Phosphinamid-prodrugs von tenofovir
CN117285566A (zh) * 2022-06-24 2023-12-26 润佳（苏州）医药科技有限公司 一种膦酸酯类化合物及其医药用途

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CA931561A (en) * 1969-03-10 1973-08-07 Syntex Corporation Nucleoside phosphonates, phosphonic acids, phosphonic acid salts, and process for producing same
CA2001715C (en) * 1988-11-14 1999-12-28 Muzammil M. Mansuri Carbocyclic nucleosides and nucleotides
CA2297294C (en) * 1989-05-15 2005-11-08 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Phosphonomethoxymethylpurine/pyrimidine derivatives
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US5672697A (en) * 1991-02-08 1997-09-30 Gilead Sciences, Inc. Nucleoside 5'-methylene phosphonates
DE4138584A1 (de) * 1991-11-23 1993-05-27 Hoechst Ag Carbocyclische phosphonat-nucleotidanaloge, deren herstellung und verwendung

Also Published As

Publication number Publication date
CA2171743C (en) 2007-11-20
EP0719273B1 (de) 2010-11-03
AU7875294A (en) 1995-04-03
AU691527B2 (en) 1998-05-21
DE69435319D1 (de) 2010-12-16
JPH09506334A (ja) 1997-06-24
JP4086314B2 (ja) 2008-05-14
WO1995007920A1 (en) 1995-03-23
BR9407510A (pt) 1997-01-07
CA2171743A1 (en) 1995-03-23
EP0719273A1 (de) 1996-07-03

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