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DE98905804T1 - Bicyclonukleosid- und oligonukleotid-analoga - Google Patents

Bicyclonukleosid- und oligonukleotid-analoga Download PDF

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Publication number
DE98905804T1
DE98905804T1 DE98905804T DE98905804T DE98905804T1 DE 98905804 T1 DE98905804 T1 DE 98905804T1 DE 98905804 T DE98905804 T DE 98905804T DE 98905804 T DE98905804 T DE 98905804T DE 98905804 T1 DE98905804 T1 DE 98905804T1
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group
analog
nucleoside
hydrogen atom
oligonucleotide
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Takeshi Nara-shi IMANISHI
Satoshi Takatsuki-shi OBIKA
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Exiqon AS
Roche Innovation Center Copenhagen AS
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Exiqon AS
Santaris Pharma AS
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Application filed by Exiqon AS, Santaris Pharma AS filed Critical Exiqon AS
Publication of DE98905804T1 publication Critical patent/DE98905804T1/de
Pending legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds 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
    • A61K31/7064Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06Pyrimidine radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16Purine radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H21/00Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
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  • Veterinary Medicine (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Nukleosidanalogon der folgenden allgemeinen Formel (I)
Figure 00000001
wobei B eine Pyrimidin- oder Purin-Nukleinsäurebase oder ein Analogon davon ist und X und Y identisch oder verschieden sind und jeweils ein Wasserstoffatom, eine Alkylgruppe, eine Alkenylgruppe, eine Alkinylgruppe, eine Cycloalkylgruppe, eine Aralkylgruppe, eine Arylgruppe, eine Acylgruppe oder eine Silylgruppe repräsentieren,
oder ein Amiditderivat davon.

Claims (5)

  1. Nukleosidanalogon der folgenden allgemeinen Formel (I)
    Figure 00010001
    wobei B eine Pyrimidin- oder Purin-Nukleinsäurebase oder ein Analogon davon ist und X und Y identisch oder verschieden sind und jeweils ein Wasserstoffatom, eine Alkylgruppe, eine Alkenylgruppe, eine Alkinylgruppe, eine Cycloalkylgruppe, eine Aralkylgruppe, eine Arylgruppe, eine Acylgruppe oder eine Silylgruppe repräsentieren, oder ein Amiditderivat davon.
  2. Nukleosidanalogon nach Anspruch 1, wobei X und Y jeweils ein Wasserstoffatom repräsentieren.
  3. Mononukleosidamiditderivat nach Anspruch 1, wobei X 4,4-Dimethoxytrityl (DMTr) ist und Y eine 2-Cyanoethoxy(diisopropylamino)phosphinogruppe (Amiditgruppe) ist.
  4. Oligonukleotid- oder Polynukleotidanalogon mit einer oder mehreren Strukturen der allgemeinen Formel (Ia)
    Figure 00020001
    wobei B eine Pyrimidin- oder Purin-Nukleinsäurebase oder ein Analogon davon ist.
  5. Oligonukleotid- oder Polynukleotidanalogon der allgemeinen Formel (II)
    Figure 00020002
    wobei B1 und B identisch oder verschieden sind und jeweils eine Pyrimidin- oder Purin-Nukleinsäurebase oder ein Analogon davon repräsentieren, R ein Wasserstoffatom, eine Hydroxylgruppe, ein Halogenatom oder eine Alkoxygruppe ist, W1 und W2 identisch oder verschieden sind und jeweils ein Wasserstoffatom, eine Alkylgruppe, eine Alkenylgruppe, eine Alkinylgruppe, eine Cycloalkylgruppe, eine Aralkylgruppe, eine Arylgruppe, eine Acylgruppe, eine Silylgruppe, einen Phosphorsäurerest, ein natürlich vorkommendes Nukleosid oder ein synthetisches Nukleosid, gebunden über eine Phosphodiesterbindung, oder ein Oligonukleotid oder Polynukleotid, welches das Nukleosid enthält, repräsentieren, n1 oder n2 identisch oder verschieden sind und jeweils eine ganze Zahl von 0 bis 50 bezeichnen, mit der Maßgabe, dass n1 oder n2 nicht gleichzeitig Null sind und dass nicht alle n2 gleichzeitig Null sind, n3 eine ganze Zahl von 1 bis 50 bezeichnet, mit der Maßga be, dass, wenn n1 und/oder n2 2 oder mehr ist oder sind, B1 und B nicht identisch sein müssen und R nicht identisch sein müssen.
DE98905804T 1997-03-07 1998-03-09 Bicyclonukleosid- und oligonukleotid-analoga Pending DE98905804T1 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP5340997 1997-03-07
JP5340997 1997-03-07
PCT/JP1998/000945 WO1998039352A1 (fr) 1997-03-07 1998-03-09 Nouveaux analogues de bicyclonucleoside et d'oligonucleotide

Publications (1)

Publication Number Publication Date
DE98905804T1 true DE98905804T1 (de) 2010-08-26

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ID=12942037

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US (1) US6268490B1 (de)
EP (3) EP1013661B2 (de)
JP (1) JP3756313B2 (de)
AT (1) ATE541576T2 (de)
AU (1) AU720472B2 (de)
CA (1) CA2283509C (de)
DE (1) DE98905804T1 (de)
DK (3) DK2361921T3 (de)
ES (3) ES2545211T3 (de)
PT (2) PT1013661E (de)
WO (1) WO1998039352A1 (de)

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