ES2036196T3 - Procedimiento para la obtencion de nucleosidos fluorados. - Google Patents
Procedimiento para la obtencion de nucleosidos fluorados.Info
- Publication number
- ES2036196T3 ES2036196T3 ES198787110542T ES87110542T ES2036196T3 ES 2036196 T3 ES2036196 T3 ES 2036196T3 ES 198787110542 T ES198787110542 T ES 198787110542T ES 87110542 T ES87110542 T ES 87110542T ES 2036196 T3 ES2036196 T3 ES 2036196T3
- Authority
- ES
- Spain
- Prior art keywords
- uracil
- united
- rest
- derived
- substituted
- 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
Links
Classifications
-
- 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
- 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
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Biochemistry (AREA)
- Engineering & Computer Science (AREA)
- Virology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
Abstract
LA INVENCION SE REFIERE A NUEVOS NUCLEOSIDOS 3'' FLUORADOS ACTIVOS CONTRA INFECCIONES HIV (SIDA), DE FORMULA (I) EN LA QUE R1 ES UN RESTO UNIDO CON ENLACE N-1-GLUCOSIDICO QUE SE DERIVA DE TIMINA, URACILO, URACILO 5-SUSTITUIDO, CITOSINA O UN DERIVADO 5-SUSTITUIDO DE CITOSINA, O BIEN, UN RESTO UNIDO CON ENLACE N-9-GLUCOSIDICO QUE SE DERIVA DE 2-FLUORADENINA, 2,6-DIAMINOPURINA, 2-AMINOPURINA, 6-TIOGUANINA O 7-DEAZAADENINA; R2 ES H U OH; Y R3 ES OH, O-ACETILO, O-PALMITOILO, TRIFOSFATO COMO ACIDO LIBRE O BAJO LA FORMA DE LAS CORRESPONDIENTES SALES ALCALINAS AMONICAS O ALQUILAMONICAS, O UN GRUPO PRECURSOR DEL GRUPO HIDROXI. LA INVENCION SE REFIERE TAMBIEN A LOS AGENTES FARMACEUTICOS CORRESPONDIENTES Y A SU OBTENCION Y UTILIZACION. UN PRINCIPIO ACTIVO ESPECIALMENTE ADECUADO ES LA 2'',2''-DIDESOXI-3''-FLUORTIMINA.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DD86292826A DD279407A1 (de) | 1986-07-24 | 1986-07-24 | Verfahren zur herstellung eines mittels gegen aids |
DD30257387 | 1987-05-08 | ||
DD87303489A DD281346A5 (de) | 1986-07-24 | 1987-06-03 | Verfahren zur herstellung eines mittels gegen hiv-infektionen beim menschen |
CA000571404A CA1333390C (en) | 1986-07-24 | 1988-07-07 | Fluorinated nucleosides and process for treating retrovirus infections therewith |
Publications (2)
Publication Number | Publication Date |
---|---|
ES2036196T3 true ES2036196T3 (es) | 1993-05-16 |
ES2036196T5 ES2036196T5 (es) | 1995-08-16 |
Family
ID=27426554
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ES87110542T Expired - Lifetime ES2036196T5 (es) | 1986-07-24 | 1987-07-21 | Nucleosidos fluorados, su preparacion y su empleo farmaceutico contra el sida. |
Country Status (11)
Country | Link |
---|---|
US (1) | US4963662A (es) |
EP (1) | EP0254268B2 (es) |
JP (1) | JP2525418B2 (es) |
AU (1) | AU615431B2 (es) |
CA (2) | CA1333390C (es) |
DD (2) | DD279407A1 (es) |
DE (1) | DE3765045D1 (es) |
DK (1) | DK378687A (es) |
ES (1) | ES2036196T5 (es) |
GR (1) | GR3001214T3 (es) |
NZ (1) | NZ223836A (es) |
Families Citing this family (45)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6458772B1 (en) * | 1909-10-07 | 2002-10-01 | Medivir Ab | Prodrugs |
US6448392B1 (en) | 1985-03-06 | 2002-09-10 | Chimerix, Inc. | Lipid derivatives of antiviral nucleosides: liposomal incorporation and method of use |
US5223263A (en) * | 1988-07-07 | 1993-06-29 | Vical, Inc. | Liponucleotide-containing liposomes |
US5446029A (en) * | 1986-07-04 | 1995-08-29 | Medivir Ab | Anti-retroviral activity of 2',3'-dideoxy-3'-fluoronucleosides |
US5153180A (en) * | 1986-07-24 | 1992-10-06 | Eckart Matthes | Fluorinated nucleosides and process for treating retrovirus infections therewith |
WO1988003804A2 (en) * | 1986-11-21 | 1988-06-02 | Max-Planck-Gesellschaft Zur Förderung Der Wissensc | Method of treating viral infections in humans and compositions therefor |
US5459256A (en) * | 1987-04-17 | 1995-10-17 | The Government Of The United States Of America As Represented By The Department Of Health And Human Services | Lipophilic, aminohydrolase-activated prodrugs |
US5495010A (en) * | 1987-04-17 | 1996-02-27 | The United States Of America As Represented By The Department Of Health And Human Services | Acid stable purine dideoxynucleosides |
GB8719877D0 (en) * | 1987-08-22 | 1987-09-30 | Wellcome Found | Antiviral compounds |
JPS6468395A (en) * | 1987-09-08 | 1989-03-14 | Yamasa Shoyu Kk | 3'-deoxyarbinofuranosylpyrimidine nucleoside derivative |
JPH01265099A (ja) * | 1987-10-08 | 1989-10-23 | Stichting Rega Vzw | 抗hiv活性をもつ3’,−フルオロプリン−2’,3’−ジデオキシリボシド類 |
SE8704298D0 (sv) * | 1987-11-03 | 1987-11-03 | Astra Ab | Compounds for use in therapy |
US5506215A (en) * | 1987-11-03 | 1996-04-09 | Medivir Ab | 1-(3'-fluoro-2',3'-dideoxy-β-D-ribofuranosyl)-5-substituted pyrimidine nucleosides |
GB8726136D0 (en) * | 1987-11-07 | 1987-12-09 | Wellcome Found | Therapeutic nucleosides |
EP0316592A3 (en) * | 1987-11-13 | 1990-09-19 | Stichting REGA V.Z.W. | 3'-fluoro-2',3'-dideoxyuridine, and its therapeutic application |
US4997926A (en) * | 1987-11-18 | 1991-03-05 | Scripps Clinic And Research Foundation | Deaminase-stable anti-retroviral 2-halo-2',3'-dideoxy |
US5817638A (en) * | 1988-07-07 | 1998-10-06 | Nexstar Pharmaceuticals, Inc. | Antiviral liponucleosides: treatment of hepatitis B |
US6599887B2 (en) | 1988-07-07 | 2003-07-29 | Chimerix, Inc. | Methods of treating viral infections using antiviral liponucleotides |
US6252060B1 (en) | 1988-07-07 | 2001-06-26 | Nexstar Pharmaceuticals, Inc. | Antiviral liponucleosides: treatment of hepatitis B |
EP0355031A3 (de) * | 1988-08-17 | 1990-12-27 | MATTHES, Eckart, Dr. | Substituierte Pyrimidinnucleoside, Verfahren zu ihrer Herstellung und sie enthaltende pharmazeutische Mittel |
US5157114A (en) * | 1988-08-19 | 1992-10-20 | Burroughs Wellcome Co. | 2',3'-dideoxy-3'-fluoro-5-ethyngluridine |
WO1990003978A1 (en) * | 1988-10-03 | 1990-04-19 | Stichting Rega Vzw | 5-halogeno-3'-fluoro-2',3'-dideoxyuridine compounds and their therapeutic application |
DD293498A5 (de) * | 1989-07-20 | 1991-09-05 | Zi Fuer Molekularbiologie Der Adw,De | Verfahren zur herstellung eines mittels fuer die behandlung oder prophylaxe von hepatits-infektionen bei mensch und tier |
CA2073063A1 (en) * | 1989-11-06 | 1991-05-07 | Jo Klaveness | Nucleoside derivatives |
GB9003543D0 (en) * | 1990-02-16 | 1990-04-11 | Wellcome Found | Therapeutic nucleosides |
FR2668153B1 (fr) * | 1990-10-22 | 1995-03-31 | Pasteur Merieux Serums Vacc | Nouveaux composes ribonucleosides, leur procede de preparation et les medicaments les contenant. |
AU648851B2 (en) * | 1990-10-23 | 1994-05-05 | City Of Hope | Mechanism based inhibitors of DNA methyltransferase |
IT1246983B (it) * | 1990-11-13 | 1994-12-12 | Consiglio Nazionale Ricerche | L-2'-desossiuridine e composizioni farmaceutiche che le contengono. |
US5180824A (en) * | 1990-11-29 | 1993-01-19 | Berlex Biosciences Inc. | 6-azido-2-fluoropurine, useful in the synthesis of nucleosides |
US5283331A (en) * | 1990-12-20 | 1994-02-01 | Nippon Kayaku Kabushiki Kaisha | 2-halogeno-oxetanocin A and phosphoric ester thereof |
ES2130246T3 (es) * | 1992-01-06 | 1999-07-01 | Wellcome Found | Nucleosidos terapeuticos de la serie 2',3'-didesoxi-3'-fluoro-purina. |
WO1996011204A1 (de) * | 1994-10-07 | 1996-04-18 | Max-Delbrück-Centrum für Molekulare Medizin | NEUE β-L-NUCLEOSIDE UND IHRE VERWENDUNG |
US5703058A (en) * | 1995-01-27 | 1997-12-30 | Emory University | Compositions containing 5-fluoro-2',3'-didehydro-2',3'-dideoxycytidine or a mono-, di-, or triphosphate thereof and a second antiviral agent |
US6391859B1 (en) | 1995-01-27 | 2002-05-21 | Emory University | [5-Carboxamido or 5-fluoro]-[2′,3′-unsaturated or 3′-modified]-pyrimidine nucleosides |
US5728560A (en) * | 1996-06-14 | 1998-03-17 | Enzon, Inc. | Method of treating CD4+ T cell lymphopenia in immuno-compromised patients |
US6013790A (en) * | 1996-09-25 | 2000-01-11 | Board Of Regents University Of Nebraska-Lincoln | Heavily fluorinated sugar analogs |
DE19720151A1 (de) * | 1997-05-02 | 1998-11-05 | Max Delbrueck Centrum | Chimäre Oligonucleotide und ihre Verwendung |
US20020128301A1 (en) * | 1998-02-13 | 2002-09-12 | Medivir AB | Non-nucleoside reverse transcriptase inhibitors |
US7635690B2 (en) | 1999-01-22 | 2009-12-22 | Emory University | HIV-1 mutations selected for by β-2′,3′-didehydro-2′,3′-dideoxy-5-fluorocytidine |
US7115584B2 (en) * | 1999-01-22 | 2006-10-03 | Emory University | HIV-1 mutations selected for by β-2′,3′-didehydro-2′,3′-dideoxy-5-fluorocytidine |
WO2001060315A2 (en) * | 2000-02-18 | 2001-08-23 | Shire Biochem Inc. | Method for the treatment or prevention of flavivirus infections using nucleoside analogues |
US6949522B2 (en) * | 2001-06-22 | 2005-09-27 | Pharmasset, Inc. | β-2′- or 3′-halonucleosides |
EP1425022A4 (en) * | 2001-08-24 | 2009-04-29 | Koronis Pharmaceuticals Inc | MUTAGENIC NUCLEOSIDE ANALOGUES FOR THE TREATMENT OF VIRAL DISEASE |
PL217132B1 (pl) | 2010-06-30 | 2014-06-30 | Inst Biochemii I Biofizyki Polskiej Akademii Nauk | Modyfikowane 2',3'-dideoksynukleozydy do leczenia zakażeń szczepami ludzkiego wirusa nabytego niedoboru odporności (HIV) wykazującymi oporność wielolekową, sposób ich wytwarzania oraz farmaceutycznie dopuszczalna forma leku |
WO2021188959A1 (en) | 2020-03-20 | 2021-09-23 | Gilead Sciences, Inc. | Prodrugs of 4'-c-substituted-2-halo-2'-deoxyadenosine nucleosides and methods of making and using the same |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE158902C (es) * | ||||
GB1189973A (en) * | 1969-02-14 | 1970-04-29 | Akad Wissenschaften Ddr | Cytostatically-Active 2',3'-Didesoxy-3'-Fluoropyrimidine-Nucleosides |
US3775397A (en) * | 1969-11-12 | 1973-11-27 | Akad Wissenschaften Ddr | Novel cytostatic 2',3'-dideoxy-3'-fluoropyrimidine-nucleosides |
DD158903A1 (de) * | 1981-05-18 | 1983-02-09 | Gotthard Kowollik | Verfahren zur herstellung von 3'-fluor-2',3'-didesoxyadenosin |
DD209197A1 (de) * | 1981-07-21 | 1984-04-25 | Akad Wissenschaften Ddr | Verfahren zur herstellung von 3'-fluor-2',3'-didesoxyguanosin |
JPH02240622A (ja) * | 1989-03-14 | 1990-09-25 | Canon Inc | 防振光学系 |
-
1986
- 1986-07-24 DD DD86292826A patent/DD279407A1/de unknown
-
1987
- 1987-06-03 DD DD87303489A patent/DD281346A5/de unknown
- 1987-07-21 DE DE8787110542T patent/DE3765045D1/de not_active Expired - Lifetime
- 1987-07-21 DK DK378687A patent/DK378687A/da not_active Application Discontinuation
- 1987-07-21 EP EP87110542A patent/EP0254268B2/de not_active Expired - Lifetime
- 1987-07-21 ES ES87110542T patent/ES2036196T5/es not_active Expired - Lifetime
- 1987-07-23 JP JP62182423A patent/JP2525418B2/ja not_active Expired - Lifetime
-
1988
- 1988-03-03 AU AU12592/88A patent/AU615431B2/en not_active Expired
- 1988-03-10 NZ NZ223836A patent/NZ223836A/en unknown
- 1988-07-07 CA CA000571404A patent/CA1333390C/en not_active Expired - Lifetime
- 1988-07-15 US US07/223,677 patent/US4963662A/en not_active Expired - Fee Related
-
1990
- 1990-12-19 GR GR90401088T patent/GR3001214T3/el unknown
-
1994
- 1994-05-31 CA CA000616868A patent/CA1336820C/en not_active Expired - Lifetime
Also Published As
Publication number | Publication date |
---|---|
CA1333390C (en) | 1994-12-06 |
US4963662A (en) | 1990-10-16 |
JPS63107936A (ja) | 1988-05-12 |
DK378687A (da) | 1988-01-25 |
EP0254268B2 (de) | 1994-01-12 |
ES2036196T5 (es) | 1995-08-16 |
DD281346A5 (de) | 1990-08-08 |
NZ223836A (en) | 1990-12-21 |
AU615431B2 (en) | 1991-10-03 |
GR3001214T3 (en) | 1992-07-30 |
EP0254268B1 (de) | 1990-09-19 |
CA1336820C (en) | 1995-08-29 |
JP2525418B2 (ja) | 1996-08-21 |
DE3765045D1 (de) | 1990-10-25 |
AU1259288A (en) | 1988-11-10 |
EP0254268A2 (de) | 1988-01-27 |
EP0254268A3 (en) | 1988-07-13 |
DD279407A1 (de) | 1990-06-06 |
DK378687D0 (da) | 1987-07-21 |
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