DK2604620T3 - Modificerede fluorerede nucleosidanaloger - Google Patents

Modificerede fluorerede nucleosidanaloger Download PDF

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Publication number
DK2604620T3
DK2604620T3 DK13152340.9T DK13152340T DK2604620T3 DK 2604620 T3 DK2604620 T3 DK 2604620T3 DK 13152340 T DK13152340 T DK 13152340T DK 2604620 T3 DK2604620 T3 DK 2604620T3
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hcv
nucleoside
pharmaceutically acceptable
virus
fluoro
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DK13152340.9T
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Jeremy Clark
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Gilead Pharmasset Llc
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    • 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
    • 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
    • A61K31/7068Compounds 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
    • 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
    • A61K31/7068Compounds 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
    • A61K31/7072Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • 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
    • A61P31/14Antivirals for RNA viruses
    • A61P31/16Antivirals for RNA viruses for influenza or rhinoviruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • C07H19/048Pyridine 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
    • C07H19/06Pyrimidine radicals
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    • 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
    • C07H19/14Pyrrolo-pyrimidine 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

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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)
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  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
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  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Virology (AREA)
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  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Saccharide Compounds (AREA)
  • Medicinal Preparation (AREA)

Claims (6)

  1. MODIFICEREDE FLUOREREDE NUCLEOSID AN ALOGER 1. (27?)-2'-deoxy-2'-fluor-2'-C-methylnucleosid (β-D eller β-L) eller et farmaceutisk acceptabelt salt deraf med strukturen:
    hvor basen er en pyrimidinbase, der er repræsenteret ved følgende formel XerO;
    R1 og R7 uafhængigt er H, et monophosphat, et diphosphat eller et triphosphat; R3 er H; og R4 er NH2 eller OH. 2. (2'Æ)-2'-deoxy-2'-fluor-2'-C-methylnucleosid (β-D eller β-L) ifølge krav 1 eller et farmaceutisk acceptabelt salt deraf, hvor R7 er H, og R1 er et monophosphat, et diphosphat eller et triphosphat. 3. (2'Æ)-2'-deoxy-2'-fluor-2'-C-methylnucleosid (β-D eller β-L) ifølge krav 1 eller et farmaceutisk acceptabelt salt deraf, hvor R7 er H, og R1 er et triphosphat. 4. (27i)-2'-dcoxy-2'-fluor-2'-C-methylnucleosid (β-D eller β-L) ifølge krav 1 eller et farmaceutisk acceptabelt salt deraf, hvor R1 og R7 er H. 5. (27?)-2'-deoxy-2'-fluor-2'-C-methylnucleosid (β-D) ifølge krav 1 eller et farmaceutisk acceptabelt salt deraf med formlen:
    6. (2'/?)-2'-deoxy-2'-fluor-2'-C-methylnucleosid (β-D) ifølge krav 1 eller et farmaceutisk acceptabelt salt deraf med formlen:
  2. 7. Farmaceutisk sammensætning, der omfatter et nucleosid ifølge et hvilket som helst af kravene 1 til 6, eller et farmaceutisk acceptabelt salt deraf, og en farmaceutisk acceptabel bærer.
  3. 8. Farmaceutisk sammensætning ifølge krav 7, hvor sammensætningen omfatter et nucleosid ifølge krav 1 eller et farmaceutisk acceptabelt salt deraf, og en farmaceutisk acceptabel bærer.
  4. 9. Farmaceutisk sammensætning ifølge krav 7, hvor sammensætningen omfatter et nucleosid ifølge krav 2 eller et farmaceutisk acceptabelt salt deraf, og en farmaceutisk acceptabel bærer.
  5. 10. Farmaceutisk sammensætning ifølge krav 7, hvor sammensætningen omfatter et nucleosid ifølge krav 3 eller et farmaceutisk acceptabelt salt deraf, og en farmaceutisk acceptabel bærer.
  6. 11. Farmaceutisk sammensætning ifølge krav 7, hvor sammensætningen omfatter et nucleosid ifølge et hvilket som helst af kravene 4, 5 og 6 eller et farmaceutisk acceptabelt salt deraf, og en farmaceutisk acceptabel bærer.
DK13152340.9T 2003-05-30 2004-04-21 Modificerede fluorerede nucleosidanaloger DK2604620T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US47436803P 2003-05-30 2003-05-30
EP04775900.6A EP1633766B1 (en) 2003-05-30 2004-04-21 Modified fluorinated nucleoside analogues

Publications (1)

Publication Number Publication Date
DK2604620T3 true DK2604620T3 (da) 2016-10-03

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ID=33563735

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DK13152340.9T DK2604620T3 (da) 2003-05-30 2004-04-21 Modificerede fluorerede nucleosidanaloger

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US (8) US7429572B2 (da)
EP (8) EP2345657A1 (da)
JP (5) JP4958158B2 (da)
KR (1) KR100883703B1 (da)
CN (1) CN100503628C (da)
AR (6) AR044566A1 (da)
AU (1) AU2004253860B2 (da)
BR (3) BRPI0410846B8 (da)
CA (5) CA2733842A1 (da)
CO (1) CO5660270A2 (da)
CY (2) CY1118020T1 (da)
DK (1) DK2604620T3 (da)
ES (3) ES2726998T3 (da)
HR (1) HRP20160873T1 (da)
HU (2) HUE029877T2 (da)
IL (2) IL172259A (da)
LT (2) LT2604620T (da)
MX (1) MXPA05012788A (da)
MY (1) MY138477A (da)
NO (5) NO333700B1 (da)
NZ (1) NZ543867A (da)
PL (3) PL3521297T3 (da)
PT (3) PT1633766T (da)
RU (1) RU2358979C2 (da)
SI (3) SI1633766T1 (da)
TR (1) TR201906767T4 (da)
TW (1) TWI333956B (da)
WO (1) WO2005003147A2 (da)
ZA (1) ZA200509521B (da)

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