WO2000009531A3 - β-L-2'-DEOXY-NUCLEOSIDES FOR THE TREATMENT OF HEPATITIS B - Google Patents

β-L-2'-DEOXY-NUCLEOSIDES FOR THE TREATMENT OF HEPATITIS B Download PDF

Info

Publication number
WO2000009531A3
WO2000009531A3 PCT/US1999/018149 US9918149W WO0009531A3 WO 2000009531 A3 WO2000009531 A3 WO 2000009531A3 US 9918149 W US9918149 W US 9918149W WO 0009531 A3 WO0009531 A3 WO 0009531A3
Authority
WO
WIPO (PCT)
Prior art keywords
deoxy
pentofuranonucleoside
erythro
hepatitis
prodrug
Prior art date
Application number
PCT/US1999/018149
Other languages
French (fr)
Other versions
WO2000009531A2 (en
Inventor
Gilles Gosselin
Jean-Louis Imbach
Martin L Bryant
Original Assignee
Norivio Pharmaceuticals Ltd
Centre Nat Rech Scient
Gilles Gosselin
Imbach Jean Louis
Martin L Bryant
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=WO2000009531(A3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority to EP99941027A priority Critical patent/EP1104436B1/en
Priority to DE69929060T priority patent/DE69929060T2/en
Priority to BRPI9912896A priority patent/BRPI9912896B8/en
Priority to MXPA01001507A priority patent/MXPA01001507A/en
Priority to CA002340156A priority patent/CA2340156C/en
Priority to JP2000564981A priority patent/JP4294870B2/en
Priority to AU54757/99A priority patent/AU5475799A/en
Application filed by Norivio Pharmaceuticals Ltd, Centre Nat Rech Scient, Gilles Gosselin, Imbach Jean Louis, Martin L Bryant filed Critical Norivio Pharmaceuticals Ltd
Priority to AT99941027T priority patent/ATE313550T1/en
Priority to DE200712000062 priority patent/DE122007000062I1/en
Publication of WO2000009531A2 publication Critical patent/WO2000009531A2/en
Publication of WO2000009531A3 publication Critical patent/WO2000009531A3/en
Priority to HK01104418A priority patent/HK1034083A1/en
Priority to LU91348C priority patent/LU91348I2/en
Priority to CY200700017C priority patent/CY2007017I1/en
Priority to NL300286C priority patent/NL300286I2/en
Priority to FR07C0046C priority patent/FR07C0046I2/en

Links

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

Abstract

This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2'-deoxy-β-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2'-deoxy-β-L-erythro-pentofuranonucleoside has formula (I) wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted. The 2'-deoxy-β-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2'-deoxy-β-L-erythro-pentofuranonucleoside or in combination with another anti-hepatitis B agent.
PCT/US1999/018149 1998-08-10 1999-08-10 β-L-2'-DEOXY-NUCLEOSIDES FOR THE TREATMENT OF HEPATITIS B WO2000009531A2 (en)

Priority Applications (14)

Application Number Priority Date Filing Date Title
CA002340156A CA2340156C (en) 1998-08-10 1999-08-10 .beta.-l-2'-deoxy-nucleosides for the treatment of hepatitis b
DE200712000062 DE122007000062I1 (en) 1998-08-10 1999-08-10 Beta-L-2'-deoxynucleosides for the treatment of hepatitis B virus
AT99941027T ATE313550T1 (en) 1998-08-10 1999-08-10 BETA-L-2'-DEOXYNUCLEOSIDES FOR THE TREATMENT OF HEPATITIS B VIRUS
MXPA01001507A MXPA01001507A (en) 1998-08-10 1999-08-10 beta-L-2'-DEOXY-NUCLEOSIDES FOR THE TREATMENT OF HEPATITIS B.
DE69929060T DE69929060T2 (en) 1998-08-10 1999-08-10 BETA-L-2'-DEOXYNUCLEOSIDE FOR THE TREATMENT OF HEPATITIS B VIRUS
JP2000564981A JP4294870B2 (en) 1998-08-10 1999-08-10 Β-L-2'-deoxy-nucleoside for the treatment of hepatitis B
AU54757/99A AU5475799A (en) 1998-08-10 1999-08-10 Beta-l-2'-deoxy-nucleosides for the treatment of hepatitis
EP99941027A EP1104436B1 (en) 1998-08-10 1999-08-10 Beta-l-2'-deoxy-nucleosides for the treatment of hepatitis b virus
BRPI9912896A BRPI9912896B8 (en) 1998-08-10 1999-08-10 ß-1-2'-deoxynucleosides for treating hepatitis b
HK01104418A HK1034083A1 (en) 1998-08-10 2001-06-26 Beta-L-2'-deoxy-nucleosides for the treatment of hepatitis b virus
LU91348C LU91348I2 (en) 1998-08-10 2007-07-18 Telbivudine and its pharmaceutically acceptable salts
CY200700017C CY2007017I1 (en) 1998-08-10 2007-08-06 B-L-2'-DEOXY-NUCLEOSIDES FOR THE TREATMENT OF HEPATITIS B
NL300286C NL300286I2 (en) 1998-08-10 2007-08-09 Beta-L-2'-deoxynucleosides for the treatment of Heparitis B virus.
FR07C0046C FR07C0046I2 (en) 1998-08-10 2007-09-21 BETA-L-2'-DESOXY-NUCLEOSIDES FOR THE TREATMENT OF HEPATITIS B

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

Publications (2)

Publication Number Publication Date
WO2000009531A2 WO2000009531A2 (en) 2000-02-24
WO2000009531A3 true WO2000009531A3 (en) 2000-06-15

Family

ID=26791121

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1999/018149 WO2000009531A2 (en) 1998-08-10 1999-08-10 β-L-2'-DEOXY-NUCLEOSIDES FOR THE TREATMENT OF HEPATITIS B

Country Status (22)

Country Link
US (5) US6395716B1 (en)
EP (2) EP1104436B1 (en)
JP (2) JP4294870B2 (en)
KR (4) KR100691737B1 (en)
CN (3) CN1257912C (en)
AT (1) ATE313550T1 (en)
AU (1) AU5475799A (en)
BR (1) BRPI9912896B8 (en)
CA (1) CA2340156C (en)
CY (2) CY2007017I1 (en)
DE (2) DE122007000062I1 (en)
DK (3) DK1431304T3 (en)
ES (3) ES2531928T3 (en)
FR (1) FR07C0046I2 (en)
HK (3) HK1034083A1 (en)
LU (1) LU91348I2 (en)
MX (1) MXPA01001507A (en)
NL (1) NL300286I2 (en)
PT (2) PT1431304E (en)
RU (1) RU2424016C2 (en)
SG (1) SG132498A1 (en)
WO (1) WO2000009531A2 (en)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US8957046B2 (en) 2007-03-30 2015-02-17 Gilead Pharmasset Llc Nucleoside phosphoramidate prodrugs
US9045520B2 (en) 2008-12-23 2015-06-02 Gilead Pharmasset Llc Synthesis of purine nucleosides
US9393256B2 (en) 2011-09-16 2016-07-19 Gilead Pharmasset Llc Methods for treating HCV
US9549941B2 (en) 2011-11-29 2017-01-24 Gilead Pharmasset Llc Compositions and methods for treating hepatitis C virus

Families Citing this family (61)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2276404T3 (en) * 1995-06-07 2007-06-16 Emory University NUCLEOSIDS WITH ANTIVIRUS ACTIVITY OF HEPATITIS-B.
AU5475799A (en) * 1998-08-10 2000-03-06 Centre National De La Recherche Scientifique Beta-l-2'-deoxy-nucleosides for the treatment of hepatitis
US6444652B1 (en) * 1998-08-10 2002-09-03 Novirio Pharmaceuticals Limited β-L-2'-deoxy-nucleosides for the treatment of hepatitis B
EP1634888A3 (en) 1999-11-12 2007-11-21 Pharmasset, Inc. Synthesis of 2'-deoxy-L-nucleosides
CN1919860A (en) * 1999-11-12 2007-02-28 法玛赛特有限公司 Synthesis of 2'-deoxy-l-nucleosides
EP1642582A1 (en) * 2000-02-29 2006-04-05 Bristol-Myers Squibb Company Low dose entecavir formulation and use
US20020056123A1 (en) * 2000-03-09 2002-05-09 Gad Liwerant Sharing a streaming video
US6822089B1 (en) * 2000-03-29 2004-11-23 Isis Pharmaceuticals, Inc. Preparation of deoxynucleosides
US7094770B2 (en) * 2000-04-13 2006-08-22 Pharmasset, Ltd. 3′-or 2′-hydroxymethyl substituted nucleoside derivatives for treatment of hepatitis virus infections
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
JP2004513070A (en) 2000-05-26 2004-04-30 イデニクス（ケイマン）リミテツド Method for treating hepatitis delta virus infection using β-L-2′-deoxynucleoside
CN1315862C (en) 2000-05-26 2007-05-16 艾登尼科斯（开曼）有限公司 Methods and compositions for treating flaviviruses and pestiviruses
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
JP3942414B2 (en) 2000-11-29 2007-07-11 三井化学株式会社 L-type nucleic acid derivative and synthesis method thereof
CN101250194B (en) * 2000-11-29 2011-05-04 三井化学株式会社 L-nucleic acid derivative and processes for the synthesis thereof
JP4651942B2 (en) 2001-12-20 2011-03-16 フアーマセツト・インコーポレイテッド Treatment of EBV and KHSV infection and associated abnormal cell proliferation
US20030153744A1 (en) * 2001-12-21 2003-08-14 Micrologix Biotech Inc. Anti-viral 7-deaza L-nucleosides
WO2003072757A2 (en) * 2002-02-28 2003-09-04 Biota, Inc. Nucleotide mimics and their prodrugs
DE60303131T2 (en) * 2002-06-27 2006-07-20 Medivir Ab SYNERGISTIC INTERACTION OF ABACAVIR AND ALOVUDIN
NZ537662A (en) * 2002-06-28 2007-10-26 Idenix Cayman Ltd 2'-C-methyl-3'-O-L-valine ester ribofuranosyl cytidine for treatment of flaviviridae infections
US7608600B2 (en) * 2002-06-28 2009-10-27 Idenix Pharmaceuticals, Inc. Modified 2′ and 3′-nucleoside prodrugs for treating Flaviviridae infections
AP2005003211A0 (en) 2002-06-28 2005-03-31 Idenix Cayman Ltd 1'-,2'-and 3'-modified nucleoside derivatives for treating flaviviridae infections.
CN103319554A (en) 2002-06-28 2013-09-25 埃迪尼克斯医药公司 Modified 2' and 3' -nucleoside produgs for treating flaviridae infections
US7456155B2 (en) * 2002-06-28 2008-11-25 Idenix Pharmaceuticals, Inc. 2′-C-methyl-3′-O-L-valine ester ribofuranosyl cytidine for treatment of flaviviridae infections
TWI244393B (en) * 2002-08-06 2005-12-01 Idenix Pharmaceuticals Inc Crystalline and amorphous forms of beta-L-2'-deoxythymidine
PT1572095E (en) 2002-09-13 2015-10-13 Novartis Ag Beta-l-2'-deoxynucleosides for use in the treatment of resistant hbv strains
ATE442375T1 (en) * 2002-10-31 2009-09-15 Metabasis Therapeutics Inc CYTARABINE MONOPHOSPHATE PRODRUGS
EP1576138B1 (en) * 2002-11-15 2017-02-01 Idenix Pharmaceuticals LLC. 2'-methyl nucleosides in combination with interferon and flaviviridae mutation
KR20050109918A (en) * 2002-12-12 2005-11-22 이데닉스 (케이만) 리미티드 Process for the production of 2'-branched nucleosides
WO2004084453A2 (en) 2003-03-20 2004-09-30 Microbiologica Quimica E Farmaceutica Ltd. METHODS OF MANUFACTURE OF 2'-DEOXY-β-L-NUCLEOSIDES
US7595390B2 (en) * 2003-04-28 2009-09-29 Novartis Ag Industrially scalable nucleoside synthesis
WO2004096197A2 (en) * 2003-05-02 2004-11-11 Universita Degli Studi Di Cagliari 5-aza-7-deazapurine nucleosides for treating flaviviridae
ES2726998T3 (en) 2003-05-30 2019-10-11 Gilead Pharmasset Llc Modified fluorinated nucleoside analogs
NZ544634A (en) 2003-06-30 2009-10-30 Idenix Cayman Ltd Synthesis of beta-l-2-deoxy nucleosides
CN1315863C (en) * 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 Beta-2'-deoxygenation-ramification of nucleotide, synthetic method and application of medication
NZ554442A (en) 2004-09-14 2011-05-27 Pharmasset Inc Preparation of 2'fluoro-2'-alkyl-substituted or other optionally substituted ribofuranosyl pyrimidines and purines and their derivatives
JP4516863B2 (en) * 2005-03-11 2010-08-04 株式会社ケンウッド Speech synthesis apparatus, speech synthesis method and program
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
MX2008013119A (en) 2006-04-11 2008-10-21 Novartis Ag Hcv/hiv inhibitors an their uses.
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
CA2748034A1 (en) 2008-12-23 2010-07-01 Pharmasset, Inc. Purified 2'-deoxy'2'-fluoro-2'-c-methyl-nucleoside-phosphoramidate prodrugs for the treatment of viral infections
PA8855601A1 (en) 2008-12-23 2010-07-27 NUCLEOSID FORFORMIDATES
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
US8618076B2 (en) 2009-05-20 2013-12-31 Gilead Pharmasset Llc Nucleoside phosphoramidates
TWI576352B (en) 2009-05-20 2017-04-01 基利法瑪席特有限責任公司 Nucleoside phosphoramidates
MX2012005601A (en) * 2009-11-16 2012-08-01 Univ Georgia 2'-fluoro-6'-methylene carbocyclic nucleosides and methods of treating viral infections.
SG184323A1 (en) 2010-03-31 2012-11-29 Gilead Pharmasett Llc Stereoselective synthesis of phosphorus containing actives
US9011833B2 (en) 2010-10-08 2015-04-21 Novartis Ag Vitamin E formulations of sulfamide NS3 inhibitors
CN102649788B (en) * 2011-02-28 2015-03-25 四川大学 Beta-L-2'-desoxy-thymin-nucleoside derivative, preparation method and purposes thereof
PL2950786T3 (en) 2013-01-31 2020-05-18 Gilead Pharmasset Llc Combination formulation of two antiviral compounds
PL3038601T3 (en) 2013-08-27 2020-08-24 Gilead Pharmasset Llc Combination formulation of two antiviral compounds
CN106061984A (en) 2014-02-13 2016-10-26 配体药物公司 Prodrug compounds and their uses
EP3164136A4 (en) 2014-07-02 2018-04-04 Ligand Pharmaceuticals, Inc. Prodrug compounds and uses therof
CN110680806A (en) * 2018-07-04 2020-01-14 郑州泰丰制药有限公司 Preparation method of telbivudine particles
CN108570078A (en) * 2018-07-18 2018-09-25 荆门医药工业技术研究院 A method of preparing three-O- benzoyls-β of 1-O- acetyl group -2,3,5--D-RIBOSE
CN114133398B (en) * 2021-12-31 2022-11-22 中南民族大学 Amino acid substituted acyclovir tricyclic nucleoside derivative and synthesis method and application thereof

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0352248A1 (en) * 1988-07-20 1990-01-24 Medivir Aktiebolag Nucleoside derivatives
WO1992008727A1 (en) * 1990-11-13 1992-05-29 Consiglio Nazionale Delle Ricerche L-2'-desoxyuridines and pharmaceutical compositions containing them
WO1996013512A2 (en) * 1994-10-24 1996-05-09 Genencor International, Inc. L-ribofuranosyl nucleosides
CA2206878A1 (en) * 1995-09-21 1997-03-27 Lipitek International, Inc. L-nucleoside dimer compounds and therapeutic uses
WO1999045935A1 (en) * 1998-03-11 1999-09-16 Lipitek International, Inc. Novel nucleoside analogs and uses in treating disease

Family Cites Families (46)

* 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
AU2526188A (en) 1987-09-22 1989-04-18 Regents Of The University Of California, The Liposomal nucleoside analogues for treating aids
US6020322A (en) 1993-11-09 2000-02-01 Pro-Neuron, Inc. Acyl deoxyribonucleoside derivatives and uses thereof
WO1989003838A1 (en) 1987-10-28 1989-05-05 Pro-Neuron, Inc. Acyl deoxyribonucleoside derivatives and uses thereof
JP2675864B2 (en) 1988-07-05 1997-11-12 キヤノン株式会社 Recording material and inkjet recording method using the same
US5194654A (en) 1989-11-22 1993-03-16 Vical, Inc. Lipid derivatives of phosphonoacids for liposomal incorporation and method of use
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
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
CA2083386C (en) 1990-06-13 1999-02-16 Arnold Glazier Phosphorous prodrugs
EP0543806B1 (en) 1990-07-12 1996-01-17 G-Drill Ab Hydraulic down-the-hole rock drill
DE69129650T2 (en) * 1990-09-14 1999-03-25 Acad Of Science Czech Republic Precursor of phosphonates
US5206244A (en) * 1990-10-18 1993-04-27 E. R. Squibb & Sons, Inc. Hydroxymethyl (methylenecyclopentyl) purines and pyrimidines
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
US5256641A (en) 1990-11-01 1993-10-26 State Of Oregon Covalent polar lipid-peptide conjugates for immunological targeting
IL100502A (en) 1991-01-03 1995-12-08 Iaf Biochem Int Pharmaceutical compositions containing cis-4-amino-1(hydroxymethyl-1,3-oxathiolan-5-yl)-1H-pyrimid-2-one nucleoside or its derivatives
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
JPH08512019A (en) * 1993-03-10 1996-12-17 ザ・ウエルカム・ファウンデーション・リミテッド Tumor targeting using L-enantiomeric oligonucleotide conjugates consisting of immunoreactive agent and chelated radionuclide
JP3693357B2 (en) 1993-04-09 2005-09-07 峯郎 実吉 Reverse transcriptase inhibitor
WO1994026273A1 (en) 1993-05-12 1994-11-24 Hostetler Karl Y Acyclovir derivatives for topical use
US5627160A (en) * 1993-05-25 1997-05-06 Yale University L-2',3'-dideoxy nucleoside analogs as anti-hepatitis B (HBV) and anti-HIV agents
JPH09504785A (en) * 1993-09-10 1997-05-13 エモリー、ユニバーシティー Nucleosides with anti-hepatitis B virus activity
US5587362A (en) 1994-01-28 1996-12-24 Univ. Of Ga Research Foundation L-nucleosides
WO1996011204A1 (en) * 1994-10-07 1996-04-18 Max-Delbrück-Centrum für Molekulare Medizin NOVEL β-L-NUCLEOSIDES AND THEIR USE
US5696277A (en) 1994-11-15 1997-12-09 Karl Y. Hostetler Antiviral prodrugs
ES2276404T3 (en) 1995-06-07 2007-06-16 Emory University NUCLEOSIDS WITH ANTIVIRUS ACTIVITY OF HEPATITIS-B.
AU4716299A (en) 1998-06-24 2000-01-10 Emory University Use of 3'-azido-2',3'-dideoxyuridine in combination with further anti-hiv drugs for the manufacture of a medicament for the treatment of hiv
US6444652B1 (en) * 1998-08-10 2002-09-03 Novirio Pharmaceuticals Limited β-L-2'-deoxy-nucleosides for the treatment of hepatitis B
AU5475799A (en) * 1998-08-10 2000-03-06 Centre National De La Recherche Scientifique Beta-l-2'-deoxy-nucleosides for the treatment of hepatitis
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
JP2004513070A (en) * 2000-05-26 2004-04-30 イデニクス（ケイマン）リミテツド Method for treating hepatitis delta virus infection using β-L-2′-deoxynucleoside
CN1315862C (en) * 2000-05-26 2007-05-16 艾登尼科斯（开曼）有限公司 Methods and compositions for treating flaviviruses and pestiviruses

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0352248A1 (en) * 1988-07-20 1990-01-24 Medivir Aktiebolag Nucleoside derivatives
WO1992008727A1 (en) * 1990-11-13 1992-05-29 Consiglio Nazionale Delle Ricerche L-2'-desoxyuridines and pharmaceutical compositions containing them
WO1996013512A2 (en) * 1994-10-24 1996-05-09 Genencor International, Inc. L-ribofuranosyl nucleosides
CA2206878A1 (en) * 1995-09-21 1997-03-27 Lipitek International, Inc. L-nucleoside dimer compounds and therapeutic uses
WO1999045935A1 (en) * 1998-03-11 1999-09-16 Lipitek International, Inc. Novel nucleoside analogs and uses in treating disease

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
CHEMICAL ABSTRACTS, vol. 98, no. 13, 28 March 1983, Columbus, Ohio, US; abstract no. 107670, ROBINS, MORRIS J.: "Selective deoxygenation and modification at C2' of nucleosides" XP002134809 *
LIN T -S ET AL: "Synthesis of Several Pyrimidine l-Nucleoside Analogues as Potential Antiviral Agents", TETRAHEDRON,NL,ELSEVIER SCIENCE PUBLISHERS, AMSTERDAM, vol. 51, no. 4, 23 January 1995 (1995-01-23), pages 1055 - 1068, XP004104973, ISSN: 0040-4020 *
NUCLEIC ACIDS SYMP. SER. (1982), 11(SYMP. NUCLEIC ACIDS CHEM., 10TH, 1982), 1-4 *
ZHU, YONG-LIAN ET AL: "Anti-hepatitis B virus activity and metabolism of 2',3'-dideoxy-2',3'- didehydro-.beta.-L(-)-5-fluorocytidine", ANTIMICROB. AGENTS CHEMOTHER. (1998), 42(7), 1805-1810, XP002134808 *

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8957046B2 (en) 2007-03-30 2015-02-17 Gilead Pharmasset Llc Nucleoside phosphoramidate prodrugs
US9045520B2 (en) 2008-12-23 2015-06-02 Gilead Pharmasset Llc Synthesis of purine nucleosides
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
US9394331B2 (en) 2010-11-30 2016-07-19 Gilead Pharmasset Llc 2′-spiro-nucleosides and derivatives thereof useful for treating hepatitis C virus and dengue virus infections
US9393256B2 (en) 2011-09-16 2016-07-19 Gilead Pharmasset Llc Methods for treating HCV
US9549941B2 (en) 2011-11-29 2017-01-24 Gilead Pharmasset Llc Compositions and methods for treating hepatitis C virus

Also Published As

Publication number Publication date
CY2007017I2 (en) 2009-11-04
HK1097776A1 (en) 2007-07-06
CN1606983A (en) 2005-04-20
DE69929060T2 (en) 2006-08-31
LU91348I2 (en) 2007-09-18
EP1104436A2 (en) 2001-06-06
CA2340156A1 (en) 2000-02-24
NL300286I2 (en) 2008-01-02
HK1111913A1 (en) 2008-08-22
KR100702230B1 (en) 2007-04-03
RU2424016C2 (en) 2011-07-20
DE69929060D1 (en) 2006-01-26
RU2006147216A (en) 2008-07-10
AU5475799A (en) 2000-03-06
ES2531928T3 (en) 2015-03-20
CN1478483A (en) 2004-03-03
CY2007017I1 (en) 2009-11-04
US6569837B1 (en) 2003-05-27
WO2000009531A2 (en) 2000-02-24
CN1257912C (en) 2006-05-31
FR07C0046I1 (en) 2007-10-26
DK2415776T3 (en) 2016-07-04
KR20050062664A (en) 2005-06-23
HK1034083A1 (en) 2001-10-12
MXPA01001507A (en) 2003-09-10
BR9912896A (en) 2002-02-13
JP2002522552A (en) 2002-07-23
KR100634342B1 (en) 2006-10-16
FR07C0046I2 (en) 2008-05-09
ATE313550T1 (en) 2006-01-15
SG132498A1 (en) 2007-06-28
US7304043B2 (en) 2007-12-04
LU91348I9 (en) 2018-12-31
US20080064655A1 (en) 2008-03-13
EP1104436B1 (en) 2005-12-21
CA2340156C (en) 2007-10-23
DK1431304T3 (en) 2015-03-02
KR100691737B1 (en) 2007-03-12
ES2579903T3 (en) 2016-08-17
DE122007000062I1 (en) 2007-12-20
CN100482236C (en) 2009-04-29
BRPI9912896B1 (en) 2016-08-09
CY1116988T1 (en) 2017-04-05
KR20060035817A (en) 2006-04-26
EP2415776B1 (en) 2016-05-25
JP2007269798A (en) 2007-10-18
PT1431304E (en) 2015-03-09
PT2415776T (en) 2016-07-07
KR100568035B1 (en) 2006-04-07
KR20060038483A (en) 2006-05-03
JP4294870B2 (en) 2009-07-15
KR20010072392A (en) 2001-07-31
ES2255295T3 (en) 2006-06-16
EP2415776A1 (en) 2012-02-08
BRPI9912896B8 (en) 2021-05-25
CN100387237C (en) 2008-05-14
US20030225028A1 (en) 2003-12-04
US6395716B1 (en) 2002-05-28
US20060084624A1 (en) 2006-04-20
NL300286I1 (en) 2007-10-01
DK1104436T3 (en) 2006-04-03
CN1320128A (en) 2001-10-31

Similar Documents

Publication Publication Date Title
WO2000009531A3 (en) β-L-2'-DEOXY-NUCLEOSIDES FOR THE TREATMENT OF HEPATITIS B
JP2004513070A5 (en)
AR035711A1 (en) PRODROGAS 3 'DE 2'-DEOXI-BETA-L-NUCLEOSIDOS; YOUR PHARMACEUTICAL COMPOSITIONS; METHOD FOR THE TREATMENT OR PROFILAXIS OF AN INFECTION OF THE HEPATITIS B VIRUS AND ITS USES FOR THE MANUFACTURE OF PHARMACEUTICAL COMPOSITIONS
PL409123A1 (en) Compounds, their use and compositions for the treatment of hepatitis C.
WO2001060315A3 (en) Method for the treatment or prevention of flavivirus infections using nucleoside analogues
IL153078A0 (en) Methods for treating hepatitis delta virus infection with beta-l-2' deoxy nucleosides
ES2115918T3 (en) NUCLEOSIDES OF BETA-D-DIOXOLANE OF ENANTIOMOUS PURITY AND OF ACTIVITY SELECTIVELY DIRECTED AGAINST THE HEPATITIS B VIRUS.
EP0198388A3 (en) Enterally effective biologically active peptide or protein composition, method for the production thereof, and a pharmaceutical composition containing same
DE69031340T2 (en) ANTIVIRAL COMPOSITIONS CONTAINING 3'-AZIDO-2 ', 3'-DIDEOXY-5-METHYLCYTIDINE
HK1036069A1 (en) Nucleosides with anti-hepatitis b virus activity
HU901252D0 (en) Process for manufacturing of pharmaceutical compositions comprising purine derivatives
CY1117836T1 (en) BETA-L-2'-DEOXY-NUCLEOSIDES FOR USE TREATMENT B
IL142982A0 (en) β-L-2'-DEOXY-NUCLEOSIDES FOR THE TREATMENT OF HIV INFECTION
RU2001106651A (en) BETA-L-2 - DESOXY-NUCLEOTIDES FOR THE TREATMENT OF HEPATITIS IN
RU2001115094A (en) NUCLEOSIDES ACTIVATING AGAINST HEPATITIS B VIRUS
MX9704336A (en) Use of aminopurine antiviral agents for the treatment and prophylaxis of latent herpesvirus infections.

Legal Events

Date Code Title Description
WWE Wipo information: entry into national phase

Ref document number: 99809553.2

Country of ref document: CN

AK Designated states

Kind code of ref document: A2

Designated state(s): AE AL AM AT AU AZ BA BB BG BR BY CA CH CN CU CZ DE DK EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MD MG MK MN MW MX NO NZ PL PT RO RU SD SE SG SI SK SL TJ TM TR TT UA UG US UZ VN YU ZA ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): GH GM KE LS MW SD SL SZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE BF BJ CF CG CI CM GA GN GW ML MR NE SN TD TG

DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
121 Ep: the epo has been informed by wipo that ep was designated in this application
AK Designated states

Kind code of ref document: A3

Designated state(s): AE AL AM AT AU AZ BA BB BG BR BY CA CH CN CU CZ DE DK EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MD MG MK MN MW MX NO NZ PL PT RO RU SD SE SG SI SK SL TJ TM TR TT UA UG US UZ VN YU ZA ZW

AL Designated countries for regional patents

Kind code of ref document: A3

Designated state(s): GH GM KE LS MW SD SL SZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE BF BJ CF CG CI CM GA GN GW ML MR NE SN TD TG

ENP Entry into the national phase

Ref document number: 2340156

Country of ref document: CA

Ref document number: 2340156

Country of ref document: CA

Kind code of ref document: A

WWE Wipo information: entry into national phase

Ref document number: PA/a/2001/001507

Country of ref document: MX

Ref document number: 1020017001758

Country of ref document: KR

WWE Wipo information: entry into national phase

Ref document number: 54757/99

Country of ref document: AU

WWE Wipo information: entry into national phase

Ref document number: IN/PCT/2001/00194/DE

Country of ref document: IN

WWE Wipo information: entry into national phase

Ref document number: 1999941027

Country of ref document: EP

WWP Wipo information: published in national office

Ref document number: 1999941027

Country of ref document: EP

REG Reference to national code

Ref country code: DE

Ref legal event code: 8642

WWP Wipo information: published in national office

Ref document number: 1020017001758

Country of ref document: KR

WWG Wipo information: grant in national office

Ref document number: 1999941027

Country of ref document: EP

WWG Wipo information: grant in national office

Ref document number: 1020017001758

Country of ref document: KR