WO2000009531A2 - 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 PDFInfo
- Publication number
- WO2000009531A2 WO2000009531A2 PCT/US1999/018149 US9918149W WO0009531A2 WO 2000009531 A2 WO2000009531 A2 WO 2000009531A2 US 9918149 W US9918149 W US 9918149W WO 0009531 A2 WO0009531 A2 WO 0009531A2
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- deoxy
- prodrug
- erythro
- pentofuranonucleoside
- alkyl
- Prior art date
Links
- 0 *OCC(CO[C@@](C1)N(C=CC(N2)=O)C2=O)C1O Chemical compound *OCC(CO[C@@](C1)N(C=CC(N2)=O)C2=O)C1O 0.000 description 2
- OIRDTQYFTABQOQ-TVOLHPCASA-N Nc1c2nc[n]([C@H](C3O)OC(CO)C3O)c2ncn1 Chemical compound Nc1c2nc[n]([C@H](C3O)OC(CO)C3O)c2ncn1 OIRDTQYFTABQOQ-TVOLHPCASA-N 0.000 description 1
Classifications
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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
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/16—Purine radicals
Abstract
Description
Claims
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 |
MXPA01001507A MXPA01001507A (en) | 1998-08-10 | 1999-08-10 | beta-L-2'-DEOXY-NUCLEOSIDES FOR THE TREATMENT OF HEPATITIS B. |
EP99941027A EP1104436B1 (en) | 1998-08-10 | 1999-08-10 | Beta-l-2'-deoxy-nucleosides for the treatment of hepatitis b virus |
AU54757/99A AU5475799A (en) | 1998-08-10 | 1999-08-10 | Beta-l-2'-deoxy-nucleosides for the treatment of hepatitis |
AT99941027T ATE313550T1 (en) | 1998-08-10 | 1999-08-10 | BETA-L-2'-DEOXYNUCLEOSIDES FOR THE TREATMENT OF HEPATITIS B VIRUS |
DE69929060T DE69929060T2 (en) | 1998-08-10 | 1999-08-10 | BETA-L-2'-DEOXYNUCLEOSIDE FOR THE TREATMENT OF HEPATITIS B VIRUS |
BRPI9912896A BRPI9912896B8 (en) | 1998-08-10 | 1999-08-10 | ß-1-2'-deoxynucleosides for treating hepatitis b |
JP2000564981A JP4294870B2 (en) | 1998-08-10 | 1999-08-10 | Β-L-2'-deoxy-nucleoside for the treatment of 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 true WO2000009531A2 (en) | 2000-02-24 |
WO2000009531A3 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) | EP2415776B1 (en) |
JP (2) | JP4294870B2 (en) |
KR (4) | KR100634342B1 (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) | DE69929060T2 (en) |
DK (3) | DK2415776T3 (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) | PT2415776T (en) |
RU (1) | RU2424016C2 (en) |
SG (1) | SG132498A1 (en) |
WO (1) | WO2000009531A2 (en) |
Cited By (43)
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WO2001091737A2 (en) * | 2000-05-26 | 2001-12-06 | Idenix (Cayman) Limited | Methods for treating hepatitis delta virus infection with beta-l-2' deoxy-nucleosides |
WO2001096353A2 (en) * | 2000-06-15 | 2001-12-20 | Idenix (Cayman) Limited | 3'-PRODRUGS OF 2'-DEOXY-β-L-NUCLEOSIDES |
WO2002044194A1 (en) * | 2000-11-29 | 2002-06-06 | Mitsui Chemicals, Inc. | L-nucleic acid derivatives and processes for the synthesis thereof |
WO2003055896A2 (en) * | 2001-12-21 | 2003-07-10 | Micrologix Biotech Inc. | Anti-viral 7-deaza l-nucleosides |
WO2004003000A2 (en) | 2002-06-28 | 2004-01-08 | Idenix (Cayman) Limited | 1’-, 2'- and 3'- modified nucleoside derivatives for treating flaviviridae infections |
US6812219B2 (en) | 2000-05-26 | 2004-11-02 | Idenix Pharmaceuticals, Inc. | Methods and compositions for treating flaviviruses and pestiviruses |
WO2004096197A2 (en) * | 2003-05-02 | 2004-11-11 | Universita Degli Studi Di Cagliari | 5-aza-7-deazapurine nucleosides for treating flaviviridae |
WO2005003147A2 (en) | 2003-05-30 | 2005-01-13 | Pharmasset, Inc. | Modified fluorinated nucleoside analogues |
US6875751B2 (en) | 2000-06-15 | 2005-04-05 | Idenix Pharmaceuticals, Inc. | 3′-prodrugs of 2′-deoxy-β-L-nucleosides |
US6914054B2 (en) | 2000-05-23 | 2005-07-05 | Idenix Pharmaceuticals, Inc. | Methods and compositions for treating hepatitis C virus |
JP2005533870A (en) * | 2002-06-27 | 2005-11-10 | メディヴィル・アクチボラグ | Synergistic interaction of abaca beer and alovudine |
EP1600452A2 (en) | 1999-11-12 | 2005-11-30 | Pharmasset Limited | Synthesis of 2'-deoxy-L-nucleosides |
US7094770B2 (en) | 2000-04-13 | 2006-08-22 | Pharmasset, Ltd. | 3′-or 2′-hydroxymethyl substituted nucleoside derivatives for treatment of hepatitis virus infections |
US7148349B2 (en) | 2002-10-31 | 2006-12-12 | Metabasis Therapeutics, Inc. | Cyclic phosphate diesters of 1,3-propane-1-aryl diols and their use in preparing prodrugs |
US7186700B2 (en) | 2002-09-13 | 2007-03-06 | Idenix Pharmaceuticals, Inc. | β-L-2′-deoxynucleosides for the treatment of resistant HBV strains and combination therapies |
US7211570B2 (en) | 2001-12-20 | 2007-05-01 | Pharmasset, Inc. | Treatment of EBV and KHSV infection |
KR100757155B1 (en) * | 2000-02-29 | 2007-09-07 | 브리스톨-마이어스스퀴브컴파니 | Low Dose Entecavir Formulation and Use |
US7304043B2 (en) | 1998-08-10 | 2007-12-04 | Idenix Pharmaceuticals, Inc. | β-L-2′-deoxy-nucleosides for the treatment of hepatitis B |
US7323451B2 (en) | 2002-08-06 | 2008-01-29 | Idenix Pharmaceuticals, Inc. | Crystalline and amorphous forms of beta-L-2′-deoxythymidine |
US7582748B2 (en) | 2003-03-20 | 2009-09-01 | Microbiologica Quimica E Farmaceutical Ltd. | Methods of manufacture of 2′-deoxy-β-L-nucleosides |
US7595390B2 (en) | 2003-04-28 | 2009-09-29 | Novartis Ag | Industrially scalable nucleoside synthesis |
EP2157095A2 (en) | 2003-06-30 | 2010-02-24 | Novartis Ag | Synthesis of beta-L-2-Deoxy nucleosides |
US7795238B2 (en) | 1998-08-10 | 2010-09-14 | Idenix Pharmaceuticals, Inc. | β-L-2′-deoxy-nucleosides for the treatment of hepatitis B |
US7824851B2 (en) | 2002-11-15 | 2010-11-02 | Idenix Pharmaceuticals, Inc. | 2′-branched nucleosides and Flaviviridae mutation |
EP2332952A1 (en) | 2002-06-28 | 2011-06-15 | IDENIX Pharmaceuticals, Inc. | Modified 2' and 3'-nucleoside prodrugs for treating flaviridae infections |
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US8492539B2 (en) | 2004-09-14 | 2013-07-23 | Gilead Pharmasset Llc | Preparation of 2′-fluoro-2′-alkyl-substituted or other optionally substituted ribofuranosyl pyrimidines and purines and their derivatives |
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