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
Application number
ES198787110542T
Other languages
English (en)
Other versions
ES2036196T5 (es
Inventor
Eckart Dr. Matthes
Christine Lehmann
Dieter Dr. Scholz
Dr. Von Janta-Lipinski
Klaus Gaertner
Peter Prof. Dr. Langen
Hans-Alfred Prof. Dr. Rosenthal
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.)
Berlin Brandenburg Academy of Sciences and Humanities
Original Assignee
Berlin Brandenburg Academy of Sciences and Humanities
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=27426554&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ES2036196(T3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Berlin Brandenburg Academy of Sciences and Humanities filed Critical Berlin Brandenburg Academy of Sciences and Humanities
Application granted granted Critical
Publication of ES2036196T3 publication Critical patent/ES2036196T3/es
Publication of ES2036196T5 publication Critical patent/ES2036196T5/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Virology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (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.
ES87110542T 1986-07-24 1987-07-21 Nucleosidos fluorados, su preparacion y su empleo farmaceutico contra el sida. Expired - Lifetime ES2036196T5 (es)

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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6458772B1 (en) 1909-10-07 2002-10-01 Medivir Ab Prodrugs
US5223263A (en) * 1988-07-07 1993-06-29 Vical, Inc. Liponucleotide-containing liposomes
US6448392B1 (en) 1985-03-06 2002-09-10 Chimerix, Inc. Lipid derivatives of antiviral nucleosides: liposomal incorporation and method of use
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
EP0332626A1 (en) * 1986-11-21 1989-09-20 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Compositions for treating viral infections in humans
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
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
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
US6252060B1 (en) 1988-07-07 2001-06-26 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
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.
EP0506944A4 (en) * 1990-10-23 1994-08-17 Hope City 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
DE69324244T2 (de) * 1992-01-06 1999-09-30 The Wellcome Foundation Ltd., Greenford Therapeutische nukleoside der 2',3'-dideoxy-3'-fluor -purin reihe
WO1996011204A1 (de) * 1994-10-07 1996-04-18 Max-Delbrück-Centrum für Molekulare Medizin NEUE β-L-NUCLEOSIDE UND IHRE VERWENDUNG
US6391859B1 (en) 1995-01-27 2002-05-21 Emory University [5-Carboxamido or 5-fluoro]-[2′,3′-unsaturated or 3′-modified]-pyrimidine nucleosides
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
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
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
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
KR20030005197A (ko) * 2000-02-18 2003-01-17 샤이어 바이오켐 인코포레이티드 뉴클레오시드유도체를 이용한 플라비바이러스 감염의 치료또는 예방 방법
EP1478322A4 (en) * 2001-06-22 2007-08-08 Pharmasset Ltd Beta 2'-OR 3'-HALONUCLEOSIDE
WO2003018030A1 (en) * 2001-08-24 2003-03-06 Koronis Pharmaceuticals, Inc. Mutagenic nucleoside analogs 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)

* Cited by examiner, † Cited by third party
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

Also Published As

Publication number Publication date
ES2036196T5 (es) 1995-08-16
CA1336820C (en) 1995-08-29
DD279407A1 (de) 1990-06-06
EP0254268A2 (de) 1988-01-27
JP2525418B2 (ja) 1996-08-21
NZ223836A (en) 1990-12-21
CA1333390C (en) 1994-12-06
GR3001214T3 (en) 1992-07-30
EP0254268A3 (en) 1988-07-13
DK378687D0 (da) 1987-07-21
DE3765045D1 (de) 1990-10-25
EP0254268B2 (de) 1994-01-12
US4963662A (en) 1990-10-16
DK378687A (da) 1988-01-25
JPS63107936A (ja) 1988-05-12
AU615431B2 (en) 1991-10-03
EP0254268B1 (de) 1990-09-19
AU1259288A (en) 1988-11-10
DD281346A5 (de) 1990-08-08

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