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

Info

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
Authority
CN
China
Prior art keywords
deoxy
compound
hepatitis
erythro
hbv
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 - Lifetime
Application number
CNB2004100028639A
Other languages
English (en)
Chinese (zh)
Other versions
CN1606983A (zh
Inventor
吉尔斯·格索林
让-路易斯·伊姆巴克
马丁·L·布兰特
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.)
Novartis AG
Centre National de la Recherche Scientifique CNRS
Universite de Montpellier
Original Assignee
Centre National de la Recherche Scientifique CNRS
Universite de Montpellier
Idenix Cayman Ltd
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=26791121&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN100387237(C) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Centre National de la Recherche Scientifique CNRS, Universite de Montpellier, Idenix Cayman Ltd filed Critical Centre National de la Recherche Scientifique CNRS
Publication of CN1606983A publication Critical patent/CN1606983A/zh
Application granted granted Critical
Publication of CN100387237C publication Critical patent/CN100387237C/zh
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Images

Classifications

    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (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)
  • 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

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
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
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
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

Publications (2)

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

Family

ID=26791121

Family Applications (3)

Application Number Title Priority Date Filing Date
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

Family Applications After (2)

Application Number Title Priority Date Filing Date
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

Country Status (21)

Country Link
US (5) US6395716B1 (enExample)
EP (2) EP2415776B1 (enExample)
JP (2) JP4294870B2 (enExample)
KR (4) KR100702230B1 (enExample)
CN (3) CN100387237C (enExample)
AT (1) ATE313550T1 (enExample)
AU (1) AU5475799A (enExample)
BR (1) BRPI9912896B8 (enExample)
CA (1) CA2340156C (enExample)
CY (2) CY2007017I2 (enExample)
DE (2) DE69929060T2 (enExample)
DK (3) DK1431304T3 (enExample)
ES (3) ES2531928T3 (enExample)
FR (1) FR07C0046I2 (enExample)
LU (1) LU91348I2 (enExample)
MX (1) MXPA01001507A (enExample)
NL (1) NL300286I2 (enExample)
PT (2) PT2415776T (enExample)
RU (1) RU2424016C2 (enExample)
SG (1) SG132498A1 (enExample)
WO (1) WO2000009531A2 (enExample)

Families Citing this family (68)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69636734T2 (de) * 1995-06-07 2007-10-18 Emory University Nucleoside mit anti-hepatitis b virus wirksamkeit
US6444652B1 (en) * 1998-08-10 2002-09-03 Novirio Pharmaceuticals Limited β-L-2'-deoxy-nucleosides for the treatment of hepatitis B
JP4294870B2 (ja) * 1998-08-10 2009-07-15 インデニックス ファーマシューティカルズ リミティド Ｂ型肝炎の治療のためのβ−Ｌ−２’−デオキシ−ヌクレオシド
WO2001034618A2 (en) * 1999-11-12 2001-05-17 Pharmasset Limited Synthesis of 2'-deoxy-l-nucleosides
EP1600451A3 (en) 1999-11-12 2008-09-10 Pharmasset, Inc. Synthesis of 2'-deoxy-l-nucleosides
ATE312613T1 (de) * 2000-02-29 2005-12-15 Bristol Myers Squibb Co Niedrig dosierte entecavir formulierung und deren verwendung
WO2001067772A2 (en) * 2000-03-09 2001-09-13 Videoshare, Inc. Sharing a streaming video
US6822089B1 (en) * 2000-03-29 2004-11-23 Isis Pharmaceuticals, Inc. Preparation of deoxynucleosides
BR0110023A (pt) 2000-04-13 2003-12-30 Pharmasset Ltd Derivados de nucleosìdeo 3'-ou-2' substituìdos para tratamento de infecções por vìrus da hepatite
MY164523A (en) 2000-05-23 2017-12-29 Univ Degli Studi Cagliari Methods and compositions for treating hepatitis c virus
IL153020A0 (en) 2000-05-26 2003-06-24 Idenix Cayman Ltd 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
TR200402565T4 (tr) * 2000-05-26 2004-12-21 Idenix (Cayman) Limited Hepatit delta virüsü enfeksiyonunun tedavi edilmesinde ß-L-2'-deoksi-nükleosidlerin kullanımı
US6875751B2 (en) 2000-06-15 2005-04-05 Idenix Pharmaceuticals, Inc. 3′-prodrugs of 2′-deoxy-β-L-nucleosides
MY141594A (en) * 2000-06-15 2010-05-14 Novirio Pharmaceuticals Ltd 3'-PRODRUGS OF 2'-DEOXY-ß-L-NUCLEOSIDES
CN101250208B (zh) * 2000-11-29 2012-06-20 三井化学株式会社 L-核酸衍生物及其合成方法
CN100368422C (zh) 2000-11-29 2008-02-13 三井化学株式会社 L-核酸衍生物及其合成方法
AU2002360697B2 (en) 2001-12-20 2009-04-23 Beth Israel Deaconess Medical Center Treatment of EBV and KHSV infection and associated abnormal cellular proliferation
AU2002364216A1 (en) * 2001-12-21 2003-07-15 Micrologix Biotech Inc. Anti-viral 7-deaza l-nucleosides
AU2003217863B9 (en) * 2002-02-28 2009-10-29 Biota Scientific Management Pty Ltd Nucleotide mimics and their prodrugs
KR20050013628A (ko) * 2002-06-27 2005-02-04 메디비르 아베 아바카비르와 알로부딘의 공동상승 상호작용
EP2799442A1 (en) 2002-06-28 2014-11-05 IDENIX Pharmaceuticals, Inc. Modified 2' and 3' -nucleoside prodrugs for treating flaviridae 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
MXPA04012779A (es) 2002-06-28 2005-08-19 Idenix Cayman Ltd Profarmacos de 2'- y 3'-nucleosido para tratar infecciones por flaviviridae.
KR20050035194A (ko) * 2002-06-28 2005-04-15 이데닉스 (케이만) 리미티드 플라비비리다에 감염 치료용 2'-ｃ-메틸-3'-ｏ-ｌ-발린에스테르 리보푸라노실 사이티딘
US7608600B2 (en) 2002-06-28 2009-10-27 Idenix Pharmaceuticals, Inc. Modified 2′ and 3′-nucleoside prodrugs for treating Flaviviridae infections
TWI244393B (en) * 2002-08-06 2005-12-01 Idenix Pharmaceuticals Inc Crystalline and amorphous forms of beta-L-2'-deoxythymidine
JP4173861B2 (ja) * 2002-09-13 2008-10-29 イデニクス（ケイマン）リミテツド 耐性ＨＢＶ菌株の治療のためのβ−Ｌ−２’−デオキシヌクレオシド及び併用療法
CA2503730C (en) * 2002-10-31 2011-10-18 Metabasis Therapeutics, Inc. Cytarabine monophosphate prodrugs
ES2624353T3 (es) * 2002-11-15 2017-07-13 Idenix Pharmaceuticals Llc 2'-Metil nucleósidos en combinación con interferón y mutación de Flaviviridae
AU2003300901A1 (en) * 2002-12-12 2004-06-30 Idenix (Cayman) Limited Process for the production of 2'-branched nucleosides
CN101415719A (zh) 2003-03-20 2009-04-22 微生物化学及药品有限公司 生产2’-脱氧-β-L-核苷的方法
CN1812995A (zh) * 2003-04-28 2006-08-02 艾登尼科斯（开曼）有限公司 工业化规模的核苷合成
WO2004096197A2 (en) * 2003-05-02 2004-11-11 Universita Degli Studi Di Cagliari 5-aza-7-deazapurine nucleosides for treating flaviviridae
FI2604620T4 (fi) 2003-05-30 2024-09-11 Gilead Pharmasset Llc Modifioituja fluorinoituja nukleosidianalogeja
WO2005003374A2 (en) 2003-06-30 2005-01-13 Idenix (Cayman) Limited SYNTHESIS OF β-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
BRPI0515279A (pt) 2004-09-14 2008-07-15 Pharmasset Inc preparação de ribofuranosil pirimidinas e purinas 2'fluoro-2'-alquil- substituìdas ou outras opcionalmente substituìdas e seus 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
EP1976382B1 (en) * 2005-12-23 2013-04-24 IDENIX Pharmaceuticals, Inc. Process for preparing a synthetic intermediate for preparation of branched nucleosides
EP2007789B1 (en) 2006-04-11 2015-05-20 Novartis AG Spirocyclic 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
US8716262B2 (en) 2008-12-23 2014-05-06 Gilead Pharmasset Llc Nucleoside phosphoramidates
AR074977A1 (es) 2008-12-23 2011-03-02 Pharmasset Inc Sintesis de nucleosidos de purina
CN102753563A (zh) 2008-12-23 2012-10-24 吉利德制药有限责任公司 核苷类似物
US20110182850A1 (en) 2009-04-10 2011-07-28 Trixi Brandl Organic compounds and their uses
US8512690B2 (en) 2009-04-10 2013-08-20 Novartis Ag Derivatised proline containing peptide compounds as protease inhibitors
US8618076B2 (en) 2009-05-20 2013-12-31 Gilead Pharmasset Llc Nucleoside phosphoramidates
TWI583692B (zh) 2009-05-20 2017-05-21 基利法瑪席特有限責任公司 核苷磷醯胺
WO2011060408A2 (en) * 2009-11-16 2011-05-19 University Of Georgia Research Foundation, Inc. 2'-fluoro-6'-methylene carbocyclic nucleosides and methods of treating viral infections
PT3290428T (pt) 2010-03-31 2021-12-27 Gilead Pharmasset Llc Comprimido compreendendo 2-(((s)-(((2r,3r,4r,5r)-5-(2,4-dioxo-3,4-dihidropirimidin-1-(2h)-il)¿4¿fluoro¿3¿hidroxi¿4¿metiltetrahidrofuran¿2¿il)metoxi) (fenoxi)fosforil)amino)propanoato de (s)- isopropil cristalino
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
US8841275B2 (en) 2010-11-30 2014-09-23 Gilead Pharmasset Llc 2′-spiro-nucleosides and derivatives thereof useful for treating hepatitis C virus and dengue virus infections
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
KR101991298B1 (ko) 2011-09-16 2019-06-21 길리애드 파마셋 엘엘씨 Hcv 치료 방법
US8889159B2 (en) 2011-11-29 2014-11-18 Gilead Pharmasset Llc Compositions and methods for treating hepatitis C virus
HUE047777T2 (hu) 2013-01-31 2020-05-28 Gilead Pharmasset Llc Két vírusellenes vegyület kombinációs készítménye
EP4005560A1 (en) 2013-08-27 2022-06-01 Gilead Pharmasset LLC Combination formulation of two antiviral compounds
EP3105238A4 (en) 2014-02-13 2017-11-08 Ligand Pharmaceuticals, Inc. Prodrug compounds and their uses
JP2017520545A (ja) 2014-07-02 2017-07-27 リガンド・ファーマシューティカルズ・インコーポレイテッド プロドラッグ化合物およびそれらの使用
JP2021509907A (ja) 2018-01-09 2021-04-08 リガンド・ファーマシューティカルズ・インコーポレイテッド アセタール化合物およびその治療的使用
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
WO1989002733A1 (en) 1987-09-22 1989-04-06 The Regents Of The University Of California Liposomal nucleoside analogues for treating aids
US6020322A (en) 1993-11-09 2000-02-01 Pro-Neuron, Inc. Acyl deoxyribonucleoside derivatives and uses thereof
ZA888083B (en) 1987-10-28 1990-06-27 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
WO1991016920A1 (en) 1990-05-07 1991-11-14 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
DE69115694T2 (de) 1990-06-13 1996-10-17 Arnold Newton Mass. Glazier Phosphorylierte prodrugs
WO1992001138A1 (en) 1990-07-12 1992-01-23 G-Drill Ab Hydraulic down-the-hole rock drill
DE69129650T2 (de) * 1990-09-14 1999-03-25 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic, Prag/Praha Wirkstoffvorläufer von Phosphonaten
US5206244A (en) * 1990-10-18 1993-04-27 E. R. Squibb & Sons, Inc. Hydroxymethyl (methylenecyclopentyl) purines and pyrimidines
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
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
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
JPH07500573A (ja) 1991-07-12 1995-01-19 ネクススター・ファーマシューティカルズ・インコーポレイテッド 抗ウィルス性リポヌクレオシド：ｂ型肝炎の治療
US5554728A (en) 1991-07-23 1996-09-10 Nexstar Pharmaceuticals, Inc. Lipid conjugates of therapeutic peptides and protease inhibitors
AU6402594A (en) * 1993-03-10 1994-09-26 Wellcome Foundation Limited, The 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
WO1995007086A1 (en) * 1993-09-10 1995-03-16 Emory University 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
DE69636734T2 (de) 1995-06-07 2007-10-18 Emory University Nucleoside mit anti-hepatitis b virus wirksamkeit
WO1999045935A1 (en) 1998-03-11 1999-09-16 Lipitek International, Inc. Novel nucleoside analogs and uses in treating disease
JP2002518452A (ja) 1998-06-24 2002-06-25 エモリ ユニバーシティ Ｈｉｖの治療薬物の製造のための他の抗ｈｉｖ薬と組み合わせた３’−アジド−２’，３’−ジデオキシウリジンの使用
US6444652B1 (en) * 1998-08-10 2002-09-03 Novirio Pharmaceuticals Limited β-L-2'-deoxy-nucleosides for the treatment of hepatitis B
JP4294870B2 (ja) * 1998-08-10 2009-07-15 インデニックス ファーマシューティカルズ リミティド Ｂ型肝炎の治療のためのβ−Ｌ−２’−デオキシ−ヌクレオシド
MY164523A (en) * 2000-05-23 2017-12-29 Univ Degli Studi Cagliari Methods and compositions for treating hepatitis c virus
IL153020A0 (en) * 2000-05-26 2003-06-24 Idenix Cayman Ltd Methods and compositions for treating flaviviruses and pestiviruses
TR200402565T4 (tr) * 2000-05-26 2004-12-21 Idenix (Cayman) Limited Hepatit delta virüsü enfeksiyonunun tedavi edilmesinde ß-L-2'-deoksi-nükleosidlerin kullanımı
US6787526B1 (en) * 2000-05-26 2004-09-07 Idenix Pharmaceuticals, Inc. Methods of treating hepatitis delta virus infection with β-L-2′-deoxy-nucleosides

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 *

Also Published As

Publication number Publication date
FR07C0046I2 (fr) 2008-05-09
US20080064655A1 (en) 2008-03-13
DE69929060T2 (de) 2006-08-31
US20030225028A1 (en) 2003-12-04
CY1116988T1 (el) 2017-04-05
FR07C0046I1 (enExample) 2007-10-26
EP2415776A1 (en) 2012-02-08
US7304043B2 (en) 2007-12-04
EP2415776B1 (en) 2016-05-25
HK1097776A1 (en) 2007-07-06
KR20050062664A (ko) 2005-06-23
LU91348I9 (enExample) 2018-12-31
KR100702230B1 (ko) 2007-04-03
ATE313550T1 (de) 2006-01-15
PT1431304E (pt) 2015-03-09
PT2415776T (pt) 2016-07-07
SG132498A1 (en) 2007-06-28
DK2415776T3 (en) 2016-07-04
EP1104436A2 (en) 2001-06-06
CA2340156C (en) 2007-10-23
JP2002522552A (ja) 2002-07-23
JP2007269798A (ja) 2007-10-18
RU2424016C2 (ru) 2011-07-20
KR100568035B1 (ko) 2006-04-07
HK1034083A1 (en) 2001-10-12
CN1320128A (zh) 2001-10-31
KR20010072392A (ko) 2001-07-31
CY2007017I1 (el) 2009-11-04
CN1478483A (zh) 2004-03-03
HK1111913A1 (en) 2008-08-22
CY2007017I2 (el) 2009-11-04
ES2579903T3 (es) 2016-08-17
US6569837B1 (en) 2003-05-27
KR20060035817A (ko) 2006-04-26
US6395716B1 (en) 2002-05-28
JP4294870B2 (ja) 2009-07-15
CN100482236C (zh) 2009-04-29
KR20060038483A (ko) 2006-05-03
NL300286I2 (nl) 2008-01-02
RU2006147216A (ru) 2008-07-10
KR100634342B1 (ko) 2006-10-16
DE122007000062I1 (de) 2007-12-20
BRPI9912896B8 (pt) 2021-05-25
CN1257912C (zh) 2006-05-31
EP1104436B1 (en) 2005-12-21
WO2000009531A2 (en) 2000-02-24
DK1104436T3 (da) 2006-04-03
DK1431304T3 (en) 2015-03-02
ES2255295T3 (es) 2006-06-16
BRPI9912896B1 (pt) 2016-08-09
CN1606983A (zh) 2005-04-20
AU5475799A (en) 2000-03-06
MXPA01001507A (es) 2003-09-10
KR100691737B1 (ko) 2007-03-12
BR9912896A (pt) 2002-02-13
WO2000009531A3 (en) 2000-06-15
NL300286I1 (nl) 2007-10-01
ES2531928T3 (es) 2015-03-20
LU91348I2 (fr) 2007-09-18
US20060084624A1 (en) 2006-04-20
CA2340156A1 (en) 2000-02-24
DE69929060D1 (de) 2006-01-26

Similar Documents

Publication Publication Date Title
CN100387237C (zh) 用于治疗乙型肝炎的β-L-2'-脱氧-核苷
CN100490818C (zh) β-L-2′-脱氧核苷在制备用于治疗丁型肝炎病毒感染的药物中的用途
US7795238B2 (en) β-L-2′-deoxy-nucleosides for the treatment of hepatitis B
CN1911237B (zh) 用于治疗乙型肝炎的β-L-2＇-脱氧-核苷
AU2013203196B2 (en) Beta-L-2'-Deoxy Nucleosides for the Treatment of Hepatitis B
EP1431304B1 (en) Beta - L-2'-Deoxy-Nucleosides for the treatment of Hepatitis B
AU2007216721B2 (en) Beta-L-2'-Deoxy Nucleosides for the Treatment of Hepatitis B
CA2599597A1 (en) .beta.-l-2'-deoxy-nucleosides for the treatment of hepatitis b
HK1111913B (en) ß-L-2'-DEOXY-NUCLEOSIDES FOR THE TREATMENT OF HEPATITIS B
HK1097776B (en) ß-L-2'-DEOXY-NUCLEOSIDES FOR THE TREATMENT OF HEPATITIS B

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
ASS Succession or assignment of patent right

Owner name: FRANCE SCIENTIFIC RESEARCH NATIONAL CENTER; MONTP

Free format text: FORMER OWNER: FRANCE SCIENTIFIC RESEARCH NATIONAL CENTER

Effective date: 20050520

C10 Entry into substantive examination
C41 Transfer of patent application or patent right or utility model
SE01 Entry into force of request for substantive examination
TA01 Transfer of patent application right

Effective date of registration: 20050520

Address after: Cayman Islands (Great Britain) Grand Cayman

Applicant after: Idenix Cayman Ltd.

Co-applicant after: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE

Co-applicant after: UNIVERSITE MONTPELLIER 2

Address before: Cayman Islands (Great Britain) Grand Cayman

Applicant before: Idenix Cayman Ltd.

Co-applicant before: Centre National De La Recherche Scientifique

REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1072382

Country of ref document: HK

C14 Grant of patent or utility model
GR01 Patent grant
REG Reference to a national code

Ref country code: HK

Ref legal event code: WD

Ref document number: 1072382

Country of ref document: HK

ASS Succession or assignment of patent right

Owner name: IDENIX PHARMACEUTICALS, INC.

Free format text: FORMER OWNER: IDENIX (CAYMAN) LIMITED

Effective date: 20120710

C41 Transfer of patent application or patent right or utility model
TR01 Transfer of patent right

Effective date of registration: 20120710

Address after: Massachusetts, USA

Co-patentee after: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE

Patentee after: Aidan Nicks pharmaceuticals Ltd.

Co-patentee after: UNIVERSITE MONTPELLIER 2

Address before: The Cayman Islands (British) Grand Cayman

Co-patentee before: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE

Patentee before: Idenix Cayman Ltd.

Co-patentee before: UNIVERSITE MONTPELLIER 2

ASS Succession or assignment of patent right

Owner name: NOVARTIS CO., LTD.

Free format text: FORMER OWNER: IDENIX PHARMACEUTICALS, INC.

Effective date: 20130517

C41 Transfer of patent application or patent right or utility model
TR01 Transfer of patent right

Effective date of registration: 20130517

Address after: Basel, Switzerland

Patentee after: NOVARTIS AG

Patentee after: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE

Patentee after: UNIVERSITE MONTPELLIER 2

Address before: Massachusetts, USA

Patentee before: Aidan Nicks pharmaceuticals Ltd.

Patentee before: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE

Patentee before: UNIVERSITE MONTPELLIER 2

CX01 Expiry of patent term

Granted publication date: 20080514

CX01 Expiry of patent term