CN100387237C - 用于治疗乙型肝炎的β-L-2'-脱氧-核苷 - Google Patents

用于治疗乙型肝炎的β-L-2'-脱氧-核苷 Download PDF

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Publication number
CN100387237C
CN100387237C CNB2004100028639A CN200410002863A CN100387237C CN 100387237 C CN100387237 C CN 100387237C CN B2004100028639 A CNB2004100028639 A CN B2004100028639A CN 200410002863 A CN200410002863 A CN 200410002863A CN 100387237 C CN100387237 C CN 100387237C
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deoxy
compound
hepatitis
erythro
hbv
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Chinese (zh)
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CN1606983A (zh
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吉尔斯·格索林
让-路易斯·伊姆巴克
马丁·L·布兰特
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Novartis AG
Centre National de la Recherche Scientifique
University of Montpellier
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Centre National de la Recherche Scientifique
University of Montpellier
Idenix Cayman Ltd
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    • 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
    • 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
    • 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
    • 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
    • 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
    • A61K31/7072—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 having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
    • 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
    • A61K31/7076—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 containing purines, e.g. adenosine, adenylic 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
    • 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
    • A61K31/7076—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 containing purines, e.g. adenosine, adenylic acid
    • A61K31/708—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 containing purines, e.g. adenosine, adenylic acid having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic acid
    • 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
    • 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
    • C07H19/16—Purine radicals

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  • General Chemical & Material Sciences (AREA)
  • Virology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicinal Preparation (AREA)
CNB2004100028639A 1998-08-10 1999-08-10 用于治疗乙型肝炎的β-L-2'-脱氧-核苷 Expired - Lifetime CN100387237C (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US9611098P 1998-08-10 1998-08-10
US60/096,110 1998-08-10
US13135299P 1999-04-28 1999-04-28
US60/131,352 1999-04-28

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CNB998095532A Division CN1257912C (zh) 1998-08-10 1999-08-10 用于治疗乙型肝炎的β－L－2′－脱氧－核苷

Related Child Applications (2)

Application Number Title Priority Date Filing Date
CN2006101007520A Division CN101120947B (zh) 1998-08-10 1999-08-10 用于治疗乙型肝炎的β-L-2′-脱氧-核苷
CN2006100997025A Division CN1911237B (zh) 1998-08-10 1999-08-10 用于治疗乙型肝炎的β-L-2＇-脱氧-核苷

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CN1606983A CN1606983A (zh) 2005-04-20
CN100387237C true CN100387237C (zh) 2008-05-14

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CNB2004100028639A Expired - Lifetime CN100387237C (zh) 1998-08-10 1999-08-10 用于治疗乙型肝炎的β-L-2'-脱氧-核苷
CNB998095532A Expired - Lifetime CN1257912C (zh) 1998-08-10 1999-08-10 用于治疗乙型肝炎的β－L－2′－脱氧－核苷
CNB021265739A Expired - Lifetime CN100482236C (zh) 1998-08-10 1999-08-10 用于治疗乙型肝炎的β-L-2’-脱氧-核苷

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CNB998095532A Expired - Lifetime CN1257912C (zh) 1998-08-10 1999-08-10 用于治疗乙型肝炎的β－L－2′－脱氧－核苷
CNB021265739A Expired - Lifetime CN100482236C (zh) 1998-08-10 1999-08-10 用于治疗乙型肝炎的β-L-2’-脱氧-核苷

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EP (2) EP1104436B1 (enExample)
JP (2) JP4294870B2 (enExample)
KR (4) KR100702230B1 (enExample)
CN (3) CN100387237C (enExample)
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AU (1) AU5475799A (enExample)
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CA (1) CA2340156C (enExample)
CY (2) CY2007017I1 (enExample)
DE (2) DE122007000062I1 (enExample)
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Families Citing this family (68)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2276404T3 (es) * 1995-06-07 2007-06-16 Emory University Nucleosidos con actividad antivirus de la hepatitis-b.
US6395716B1 (en) * 1998-08-10 2002-05-28 Novirio Pharmaceuticals Limited β-L-2′-deoxy-nucleosides for the treatment of hepatitis B
US6444652B1 (en) * 1998-08-10 2002-09-03 Novirio Pharmaceuticals Limited β-L-2'-deoxy-nucleosides for the treatment of hepatitis B
EP1600452A3 (en) 1999-11-12 2008-09-10 Pharmasset, Inc. Synthesis of 2'-deoxy-L-nucleosides
TR200601782T2 (tr) * 1999-11-12 2006-09-21 Pharmasset Ltd. 2'-Deoksi-L-Nükleositlerin sentezi.
AU2001229775A1 (en) * 2000-02-29 2001-09-12 Bristol-Myers Squibb Company Low dose entecavir formulation and use
AU2001245575A1 (en) * 2000-03-09 2001-09-17 Videoshare, Inc. Sharing a streaming video
US6822089B1 (en) * 2000-03-29 2004-11-23 Isis Pharmaceuticals, Inc. Preparation of deoxynucleosides
JP2003532643A (ja) 2000-04-13 2003-11-05 フアーマセツト・リミテツド 肝炎ウイルス感染症を治療するための３’−または２’−ヒドロキシメチル置換ヌクレオシド誘導体
MY164523A (en) 2000-05-23 2017-12-29 Univ Degli Studi Cagliari Methods and compositions for treating hepatitis c virus
US6787526B1 (en) * 2000-05-26 2004-09-07 Idenix Pharmaceuticals, Inc. Methods of treating hepatitis delta virus infection with β-L-2′-deoxy-nucleosides
DE60105424T2 (de) * 2000-05-26 2005-09-22 Idenix (Cayman) Ltd. Methoden zur behandlung von delta hepatitis virus infektionen mit beta-l-2' deoxy-nucleosiden
PL359169A1 (en) * 2000-05-26 2004-08-23 Idenix (Cayman) Limited Methods and compositions for treating flaviviruses and pestiviruses
MY141594A (en) * 2000-06-15 2010-05-14 Novirio Pharmaceuticals Ltd 3'-PRODRUGS OF 2'-DEOXY-ß-L-NUCLEOSIDES
US6875751B2 (en) * 2000-06-15 2005-04-05 Idenix Pharmaceuticals, Inc. 3′-prodrugs of 2′-deoxy-β-L-nucleosides
CN101250194B (zh) * 2000-11-29 2011-05-04 三井化学株式会社 L-核酸衍生物及其合成方法
CN102241720B (zh) 2000-11-29 2014-01-29 三井化学株式会社 L-核酸衍生物及其合成方法
EP1569658A4 (en) 2001-12-20 2007-05-30 Pharmassett Ltd TREATMENT OF EBV AND KHSV INFECTION AND AN ASSOCIATED ABNORMAL CELL PROLIFERATION
AU2002364216A1 (en) * 2001-12-21 2003-07-15 Micrologix Biotech Inc. Anti-viral 7-deaza l-nucleosides
RU2004128943A (ru) * 2002-02-28 2005-04-20 Байота, Инк. (Us) Средства, имитирующие нуклеотиды, и их пролекарственные формы
BR0311141A (pt) * 2002-06-27 2005-06-07 Medivir Ab Interação sinergìstica de abacavir e alovudine
KR20050055630A (ko) 2002-06-28 2005-06-13 이데닉스 (케이만) 리미티드 플라비비리다에 감염 치료를 위한 1'-, 2'- 및 3'-변형된뉴클레오시드 유도체
KR20050035194A (ko) * 2002-06-28 2005-04-15 이데닉스 (케이만) 리미티드 플라비비리다에 감염 치료용 2'-ｃ-메틸-3'-ｏ-ｌ-발린에스테르 리보푸라노실 사이티딘
AU2003247084B9 (en) 2002-06-28 2018-07-26 Centre National De La Recherche Scientifique Modified 2' and 3'-nucleoside prodrugs for treating flaviridae infections
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
TWI244393B (en) * 2002-08-06 2005-12-01 Idenix Pharmaceuticals Inc Crystalline and amorphous forms of beta-L-2'-deoxythymidine
SI1572095T1 (sl) 2002-09-13 2015-12-31 Novartis Ag Beta-l-2'-deoksinukleozidi za uporabo pri zdravljenju odpornih sevov hbv
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
AU2003298658A1 (en) 2002-11-15 2004-06-15 Idenix (Cayman) Limited 2'-branched nucleosides and flaviviridae mutation
US7598373B2 (en) 2002-12-12 2009-10-06 Idenix Pharmaceuticals, Inc. Process for the production of 2-C-methyl-D-ribonolactone
US7582748B2 (en) * 2003-03-20 2009-09-01 Microbiologica Quimica E Farmaceutical Ltd. Methods of manufacture of 2′-deoxy-β-L-nucleosides
KR20060015542A (ko) * 2003-04-28 2006-02-17 이데닉스 (케이만) 리미티드 산업 규모의 뉴클레오시드 합성
WO2004096197A2 (en) * 2003-05-02 2004-11-11 Universita Degli Studi Di Cagliari 5-aza-7-deazapurine nucleosides for treating flaviviridae
RU2358979C2 (ru) 2003-05-30 2009-06-20 Фармассет, Инк. Модифицированные фторированные аналоги нуклеозида
US20050059632A1 (en) 2003-06-30 2005-03-17 Richard Storer Synthesis of beta-L-2'-deoxy nucleosides
CN1315863C (zh) * 2003-12-12 2007-05-16 河南省科学院质量检验与分析测试研究中心 β－L－2'－脱氧－核苷衍生物、其合成方法及其药物用途
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
ES2725457T3 (es) 2004-09-14 2019-09-24 Gilead Pharmasset Llc Preparación de ribofuranosil pirimidinas y purinas 2'fluoro-2'-alquil-sustituidas u otras opcionalmente sustituidas y sus derivados
JP4516863B2 (ja) * 2005-03-11 2010-08-04 株式会社ケンウッド 音声合成装置、音声合成方法及びプログラム
US8076303B2 (en) 2005-12-13 2011-12-13 Spring Bank Pharmaceuticals, Inc. Nucleotide and oligonucleotide prodrugs
US7781576B2 (en) * 2005-12-23 2010-08-24 Idenix Pharmaceuticals, Inc. Process for preparing a synthetic intermediate for preparation of branched nucleosides
EP2518079A3 (en) 2006-04-11 2012-12-12 Novartis AG HCV/HIV inhibitors and their uses
US7964580B2 (en) 2007-03-30 2011-06-21 Pharmasset, Inc. Nucleoside phosphoramidate prodrugs
US20090082306A1 (en) * 2007-09-26 2009-03-26 Protia, Llc Deuterium-enriched telbivudine
TW200946541A (en) 2008-03-27 2009-11-16 Idenix Pharmaceuticals Inc Solid forms of an anti-HIV phosphoindole compound
MX2011006890A (es) 2008-12-23 2011-07-20 Pharmasset Inc Analogos de nucleosidos.
AR074897A1 (es) 2008-12-23 2011-02-23 Pharmasset Inc Fosforamidatos de nucleosidos
CL2009002206A1 (es) 2008-12-23 2011-08-26 Gilead Pharmasset Llc Compuestos derivados de pirrolo -(2-3-d]-pirimidin-7(6h)-tetrahidrofuran-2-il fosfonamidato, composicion farmaceutica; y su uso en el tratamiento de enfermedades virales.
US8512690B2 (en) 2009-04-10 2013-08-20 Novartis Ag Derivatised proline containing peptide compounds as protease inhibitors
US20110182850A1 (en) 2009-04-10 2011-07-28 Trixi Brandl Organic compounds and their uses
TWI576352B (zh) 2009-05-20 2017-04-01 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
KR101840479B1 (ko) * 2009-11-16 2018-03-20 유니버시티 오브 조지아 리서치 파운데이션, 인코포레이티드 바이러스 감염 치료를 위한 ２＇―플루오로―６＇―메틸렌 카보사이클릭 뉴클레오사이드 및 방법
AP2012006535A0 (en) 2010-03-31 2012-10-31 Gilead Pharmasset Llc Stereoselective synthesis of phosphorous containing actives
CN103179966B (zh) 2010-10-08 2017-03-15 诺瓦提斯公司 磺酰胺ns3抑制剂的维生素e制剂
ES2716158T3 (es) 2010-11-30 2019-06-10 Gilead Pharmasset Llc 2'-spiro-nucleótidos para el tratamiento de hepatitis C
CN102649788B (zh) * 2011-02-28 2015-03-25 四川大学 β-L-2’-脱氧-胸腺嘧啶核苷衍生物及其制备方法和用途
HRP20180237T4 (hr) 2011-09-16 2020-12-11 Gilead Pharmasset Llc Metode za liječenje hcv-a
US8889159B2 (en) 2011-11-29 2014-11-18 Gilead Pharmasset Llc Compositions and methods for treating hepatitis C virus
EP2950786B1 (en) 2013-01-31 2019-11-27 Gilead Pharmasset LLC Combination formulation of two antiviral compounds
EA201690473A1 (ru) 2013-08-27 2017-03-31 ГАЙЛИД ФАРМАССЕТ ЭлЭлСи Комбинированный состав двух противовирусных соединений
EP3623364A1 (en) 2014-02-13 2020-03-18 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
CN110680806A (zh) * 2018-07-04 2020-01-14 郑州泰丰制药有限公司 一种替比夫定颗粒的制备方法
CN108570078A (zh) * 2018-07-18 2018-09-25 荆门医药工业技术研究院 一种制备1-O-乙酰基-2,3,5-三-O-苯甲酰基-β-D-呋喃核糖的方法
CN114133398B (zh) * 2021-12-31 2022-11-22 中南民族大学 氨基酸取代的阿昔洛韦类三环核苷衍生物及其合成方法和应用

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1100303A (zh) * 1993-05-25 1995-03-22 耶鲁大学 作为抗乙肝(hbv)及抗hiv药物的l-2′，3′，-二去氧核苷类似物
US5559101A (en) * 1994-10-24 1996-09-24 Genencor International, Inc. L-ribofuranosyl nucleosides
CA2206878A1 (en) * 1995-09-21 1997-03-27 Lipitek International, Inc. L-nucleoside dimer compounds and therapeutic uses

Family Cites Families (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB875971A (en) 1959-01-14 1961-08-30 Hoffmann La Roche A process for the manufacture of uridine and thymidine derivatives and novel compounds concerned therein
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
US5223263A (en) 1988-07-07 1993-06-29 Vical, Inc. Liponucleotide-containing liposomes
US4916122A (en) 1987-01-28 1990-04-10 University Of Georgia Research Foundation, Inc. 3'-Azido-2',3'-dideoxyuridine anti-retroviral composition
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
GB8719367D0 (en) 1987-08-15 1987-09-23 Wellcome Found Therapeutic compounds
JPH03501253A (ja) 1987-09-22 1991-03-22 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア エイズ（ａｉｄｓ）治療を目的とするリポソームによるヌクレオシド類似物質
US6020322A (en) 1993-11-09 2000-02-01 Pro-Neuron, Inc. Acyl deoxyribonucleoside derivatives and uses thereof
EP0355131B1 (en) 1987-10-28 1996-09-04 Pro-Neuron, Inc. Acyl deoxyribonucleoside derivatives and uses thereof
JP2675864B2 (ja) 1988-07-05 1997-11-12 キヤノン株式会社 被記録材及びこれを用いたインクジェット記録方法
SE8802687D0 (sv) * 1988-07-20 1988-07-20 Astra Ab Nucleoside derivatives
US5411947A (en) 1989-06-28 1995-05-02 Vestar, Inc. Method of converting a drug to an orally available form by covalently bonding a lipid to the drug
US5194654A (en) 1989-11-22 1993-03-16 Vical, Inc. Lipid derivatives of phosphonoacids for liposomal incorporation and method of use
US5463092A (en) 1989-11-22 1995-10-31 Vestar, Inc. Lipid derivatives of phosphonacids for liposomal incorporation and method of use
US5204466A (en) 1990-02-01 1993-04-20 Emory University Method and compositions for the synthesis of bch-189 and related compounds
AU7872491A (en) 1990-05-07 1991-11-27 Vical, Inc. Lipid prodrugs of salicylate and nonsteroidal anti-inflammatory drugs
EP0531452A4 (en) 1990-05-29 1993-06-09 Vical, Inc. Synthesis of glycerol di- and triphosphate derivatives
ES2083580T3 (es) 1990-06-13 1996-04-16 Arnold Glazier Profarmacos de fosforo.
ATE133233T1 (de) 1990-07-12 1996-02-15 G Drill Ab Gesteinsbohrgerät mit hydraulischem antrieb im bohrloch
DK0481214T3 (da) * 1990-09-14 1999-02-22 Acad Of Science Czech Republic Prolægemidler af phosphonater
US5206244A (en) * 1990-10-18 1993-04-27 E. R. Squibb & Sons, Inc. Hydroxymethyl (methylenecyclopentyl) purines and pyrimidines
US5543390A (en) 1990-11-01 1996-08-06 State Of Oregon, Acting By And Through The Oregon State Board Of Higher Education, Acting For And On Behalf Of The Oregon Health Sciences University Covalent microparticle-drug conjugates for biological targeting
US5543389A (en) 1990-11-01 1996-08-06 State Of Oregon, Acting By And Through The Oregon State Board Of Higher Education On Behalf Of The Oregon Health Sciences University, A Non Profit Organization Covalent polar lipid-peptide conjugates for use in salves
US5256641A (en) 1990-11-01 1993-10-26 State Of Oregon Covalent polar lipid-peptide conjugates for immunological targeting
US5149794A (en) 1990-11-01 1992-09-22 State Of Oregon Covalent lipid-drug conjugates for drug targeting
IT1246983B (it) 1990-11-13 1994-12-12 Consiglio Nazionale Ricerche L-2'-desossiuridine e composizioni farmaceutiche che le contengono.
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 (-
CA2105486C (en) 1991-03-06 2003-10-28 George Robert Painter Iii Therapeutic nucleosides
US5220003A (en) * 1991-03-29 1993-06-15 The Regents Of The University Of California Process for the synthesis of 2',3'-dideoxynucleosides
WO1992018517A1 (en) 1991-04-17 1992-10-29 Yale University Method of treating or preventing hepatitis b virus
CA2112803A1 (en) 1991-07-12 1993-01-21 Karl Y. Hostetler Antiviral liponucleosides: treatment of hepatitis b
US5554728A (en) 1991-07-23 1996-09-10 Nexstar Pharmaceuticals, Inc. Lipid conjugates of therapeutic peptides and protease inhibitors
EP0691981A1 (en) * 1993-03-10 1996-01-17 The Wellcome Foundation Limited Tumor targeting with l-enantiomeric oligonucleotide conjugates of immunoreagents and of chelated radionuclides
GB9307043D0 (en) * 1993-04-05 1993-05-26 Norsk Hydro As Chemical compounds
JP3693357B2 (ja) 1993-04-09 2005-09-07 峯郎 実吉 逆転写酵素阻害剤
JPH08510236A (ja) 1993-05-12 1996-10-29 カール ワイ． ホステトラー 局所使用のためのアシクロビル誘導体
AU7954694A (en) * 1993-09-10 1995-03-27 Centre National De La Recherche Scientifique (Cnrs) Nucleosides with anti-hepatitis b virus activity
US5587362A (en) 1994-01-28 1996-12-24 Univ. Of Ga Research Foundation L-nucleosides
WO1996011204A1 (de) * 1994-10-07 1996-04-18 Max-Delbrück-Centrum für Molekulare Medizin NEUE β-L-NUCLEOSIDE UND IHRE VERWENDUNG
US5696277A (en) 1994-11-15 1997-12-09 Karl Y. Hostetler Antiviral prodrugs
ES2276404T3 (es) 1995-06-07 2007-06-16 Emory University Nucleosidos con actividad antivirus de la hepatitis-b.
AU3080899A (en) 1998-03-11 1999-09-27 Lipitek International, Inc. Novel nucleoside analogs and uses in treating disease
US6194391B1 (en) 1998-06-24 2001-02-27 Emory University 3′-azido-2′,3′-dideoxyuridine administration to treat HIV and related test protocol
US6395716B1 (en) 1998-08-10 2002-05-28 Novirio Pharmaceuticals Limited β-L-2′-deoxy-nucleosides for the treatment of hepatitis B
US6444652B1 (en) * 1998-08-10 2002-09-03 Novirio Pharmaceuticals Limited β-L-2'-deoxy-nucleosides for the treatment of hepatitis B
MY164523A (en) * 2000-05-23 2017-12-29 Univ Degli Studi Cagliari Methods and compositions for treating hepatitis c virus
PL359169A1 (en) * 2000-05-26 2004-08-23 Idenix (Cayman) Limited Methods and compositions for treating flaviviruses and pestiviruses
US6787526B1 (en) * 2000-05-26 2004-09-07 Idenix Pharmaceuticals, Inc. Methods of treating hepatitis delta virus infection with β-L-2′-deoxy-nucleosides
DE60105424T2 (de) * 2000-05-26 2005-09-22 Idenix (Cayman) Ltd. Methoden zur behandlung von delta hepatitis virus infektionen mit beta-l-2' deoxy-nucleosiden

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1100303A (zh) * 1993-05-25 1995-03-22 耶鲁大学 作为抗乙肝(hbv)及抗hiv药物的l-2′，3′，-二去氧核苷类似物
US5559101A (en) * 1994-10-24 1996-09-24 Genencor International, Inc. L-ribofuranosyl nucleosides
CA2206878A1 (en) * 1995-09-21 1997-03-27 Lipitek International, Inc. L-nucleoside dimer compounds and therapeutic uses

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Newly Synthesized L-Enantiomers of 3'-Fluoro-Modifiedβ-2'Deoxyribonucleoside 5'-Triphosphates Inhibit Hepatitis BDNA Polymerases But Not the five Cellular DNA Polymerasesα,β,γ,δ,and ε Nor HIV -1Reverse Transcriptase. Martin von.Journal of Medicinal Chemistry,Vol.41 No.12. 1998 *

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