CN1216893C - 具有抗乙型肝炎病毒活性的核苷 - Google Patents

具有抗乙型肝炎病毒活性的核苷 Download PDF

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Publication number
CN1216893C
CN1216893C CN998141895A CN99814189A CN1216893C CN 1216893 C CN1216893 C CN 1216893C CN 998141895 A CN998141895 A CN 998141895A CN 99814189 A CN99814189 A CN 99814189A CN 1216893 C CN1216893 C CN 1216893C
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CN
China
Prior art keywords
acyl group
alkyl
benzyl
phenyl
compound
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 - Fee Related
Application number
CN998141895A
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English (en)
Chinese (zh)
Other versions
CN1329618A (zh
Inventor
吉勒·戈瑟兰
让－路易斯·因巴赫
让-皮埃尔·索马多西
雷蒙德·F·斯基纳齐
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Centre National de la Recherche Scientifique CNRS
Emory University
UAB Research Foundation
Original Assignee
Centre National de la Recherche Scientifique CNRS
Emory University
UAB Research Foundation
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Publication of CN1329618A publication Critical patent/CN1329618A/zh
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Publication of CN1216893C publication Critical patent/CN1216893C/zh
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Expired - Fee Related legal-status Critical Current

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    • 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
    • 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
    • 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
    • A61P31/20—Antivirals for DNA viruses
    • 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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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
CN998141895A 1998-11-05 1999-11-05 具有抗乙型肝炎病毒活性的核苷 Expired - Fee Related CN1216893C (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US10711698P 1998-11-05 1998-11-05
US60/107,116 1998-11-05
US11565399P 1999-01-13 1999-01-13
US60/115,653 1999-01-13

Publications (2)

Publication Number Publication Date
CN1329618A CN1329618A (zh) 2002-01-02
CN1216893C true CN1216893C (zh) 2005-08-31

Family

ID=26804401

Family Applications (1)

Application Number Title Priority Date Filing Date
CN998141895A Expired - Fee Related CN1216893C (zh) 1998-11-05 1999-11-05 具有抗乙型肝炎病毒活性的核苷

Country Status (13)

Country Link
US (1) US6458773B1 (OSRAM)
EP (1) EP1124839B1 (OSRAM)
JP (2) JP2002528554A (OSRAM)
KR (1) KR100618028B1 (OSRAM)
CN (1) CN1216893C (OSRAM)
AT (1) ATE315574T1 (OSRAM)
AU (1) AU774720B2 (OSRAM)
BR (1) BR9915555A (OSRAM)
CA (1) CA2348470C (OSRAM)
DE (1) DE69929460D1 (OSRAM)
IL (2) IL142983A0 (OSRAM)
MX (1) MXPA01004504A (OSRAM)
WO (1) WO2000026225A2 (OSRAM)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT1058686E (pt) * 1998-02-25 2007-01-31 Raymond F Schinazi 2'-fluoronucleósidos
MY164523A (en) 2000-05-23 2017-12-29 Univ Degli Studi Cagliari Methods and compositions for treating hepatitis c virus
CA2410579C (en) 2000-05-26 2010-04-20 Jean-Pierre Sommadossi Methods and compositions for treating flaviviruses and pestiviruses
AU2002257446A1 (en) 2001-05-18 2002-12-03 Rakesh Kumar Antiviral nucleosides
CN1678326A (zh) 2002-06-28 2005-10-05 埃迪尼克斯(开曼)有限公司 用于治疗黄病毒感染的2'－c－甲基－3'－o－l－缬氨酸酯核糖呋喃基胞苷
US7608600B2 (en) * 2002-06-28 2009-10-27 Idenix Pharmaceuticals, Inc. Modified 2′ and 3′-nucleoside prodrugs for treating Flaviviridae infections
CN101172993A (zh) 2002-06-28 2008-05-07 埃迪尼克斯(开曼)有限公司 用于治疗黄病毒感染的2′－c－甲基－3′－o－l－缬氨酸酯核糖呋喃基胞苷
US20040067877A1 (en) 2002-08-01 2004-04-08 Schinazi Raymond F. 2', 3'-Dideoxynucleoside analogues for the treatment or prevention of Flaviviridae infections
CA2503730C (en) * 2002-10-31 2011-10-18 Metabasis Therapeutics, Inc. Cytarabine monophosphate prodrugs
JP2006519753A (ja) 2002-11-15 2006-08-31 イデニクス（ケイマン）リミテツド ２’−分枝ヌクレオシドおよびフラビウイルス科ウイルス突然変異
MXPA05006230A (es) 2002-12-12 2005-09-20 Idenix Cayman Ltd Proceso para la produccion de nucleosidos ramificados-2'.
EP1976382B1 (en) 2005-12-23 2013-04-24 IDENIX Pharmaceuticals, Inc. Process for preparing a synthetic intermediate for preparation of branched nucleosides
WO2015123352A1 (en) 2014-02-13 2015-08-20 Ligand Pharmaceuticals, Inc. Prodrug compounds and their uses
CN106687118A (zh) 2014-07-02 2017-05-17 配体药物公司 前药化合物及其用途
WO2019139919A1 (en) 2018-01-09 2019-07-18 Ligand Pharmaceuticals, Inc. Acetal compounds and therapeutic uses thereof

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4681933A (en) 1986-05-01 1987-07-21 University Of Georgia Research Foundation, Inc. 2',3'-dideoxy-5-substituted uridines and related compounds as antiviral agents
US4916122A (en) 1987-01-28 1990-04-10 University Of Georgia Research Foundation, Inc. 3'-Azido-2',3'-dideoxyuridine anti-retroviral composition
US4841039A (en) 1986-05-01 1989-06-20 Emory University 2',3'-dideoxy-5-substituted uridines and related compounds as antiviral agents
US5077279A (en) 1986-05-01 1991-12-31 University Of Georgia Research Foundation, Inc. 3'-azido-2',3'-dideoxy-5-methylcytidine anti-viral composition
US5084445A (en) 1986-05-01 1992-01-28 University Of Georgia Research Foundation, Inc. 3'-azido-2',3'-dideoxy-5-methylcytidine
US5190926A (en) 1987-01-28 1993-03-02 University Of Georgia Research Foundation, Inc. 3'-azido-2',3'-dideoxypyrimidines and related compounds as antiviral agents
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
US5047407A (en) 1989-02-08 1991-09-10 Iaf Biochem International, Inc. 2-substituted-5-substituted-1,3-oxathiolanes with antiviral properties
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
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
US5204466A (en) 1990-02-01 1993-04-20 Emory University Method and compositions for the synthesis of bch-189 and related compounds
DE4224737A1 (de) 1992-07-27 1994-02-03 Herbert Prof Dr Schott Neue Cytosinnucleosidanaloga, Verfahren zu ihrer Herstellung und ihre Verwendung
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.
CA2637774C (en) * 1993-09-10 2011-07-19 Emory University Nucleosides with anti-hepatitis b virus activity
DE4418690A1 (de) 1994-05-28 1996-01-11 Boehringer Mannheim Gmbh Neue Lipidester von Nucleosid-Monophosphaten und deren Verwendung als immunsuppressive Arzneimittel
US5559101A (en) 1994-10-24 1996-09-24 Genencor International, Inc. L-ribofuranosyl 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
EP0831852B1 (en) 1995-06-07 2006-11-29 Emory University Nucleosides with anti-hepatitis b virus activity
ATE459361T1 (de) 1995-09-07 2010-03-15 Univ Georgia Therapeutische azidverbindungen
ES2195970T3 (es) 1996-10-16 2003-12-16 Ribapharm Inc L-ribavirina y usos de la misma.

Also Published As

Publication number Publication date
ATE315574T1 (de) 2006-02-15
IL142983A (en) 2006-07-05
HK1036069A1 (en) 2001-12-21
JP2002528554A (ja) 2002-09-03
WO2000026225A3 (en) 2000-10-05
DE69929460D1 (de) 2006-04-06
CA2348470C (en) 2007-06-05
CA2348470A1 (en) 2000-05-11
WO2000026225A2 (en) 2000-05-11
EP1124839B1 (en) 2006-01-11
AU774720B2 (en) 2004-07-08
KR100618028B1 (ko) 2006-08-30
CN1329618A (zh) 2002-01-02
EP1124839A2 (en) 2001-08-22
JP2011246469A (ja) 2011-12-08
BR9915555A (pt) 2002-01-15
IL142983A0 (en) 2002-04-21
KR20020013474A (ko) 2002-02-20
MXPA01004504A (es) 2005-04-19
AU1608500A (en) 2000-05-22
US6458773B1 (en) 2002-10-01

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Granted publication date: 20050831

Termination date: 20131105