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FI117475B - L-nukleosider för behandling av hepatit-B-virus och Epstein-Barr-virus - Google Patents

L-nukleosider för behandling av hepatit-B-virus och Epstein-Barr-virus Download PDF

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Publication number
FI117475B
FI117475B FI962986A FI962986A FI117475B FI 117475 B FI117475 B FI 117475B FI 962986 A FI962986 A FI 962986A FI 962986 A FI962986 A FI 962986A FI 117475 B FI117475 B FI 117475B
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FI
Finland
Prior art keywords
compound
pharmaceutically acceptable
solution
nucleoside
hbv
Prior art date
Application number
FI962986A
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English (en)
Finnish (fi)
Other versions
FI962986A0 (sv
FI962986A (sv
Inventor
Chung K Chu
Yung-Chi Cheng
Balakrishna S Pai
Gang-Qing Yao
Original Assignee
Univ Georgia
Univ Yale
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=22695792&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=FI117475(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Univ Georgia, Univ Yale filed Critical Univ Georgia
Publication of FI962986A0 publication Critical patent/FI962986A0/sv
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Publication of FI117475B publication Critical patent/FI117475B/sv

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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
    • C07H19/06—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
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H21/00—Compounds 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)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Saccharide Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)

Claims (25)

1. L-nukleosidförening, sora har formeln: OH ________ R*0J F M 5 där R är en bas, som är vald bland tyrnin, adenin och cytosin; och R" är vate; -C(0)R' , där R' är en rakkedjad, för-grenad eller cyklisk Ci-C10-alkyl, Ci-Cio-alkoxi-Ci-C10-10 alkyl, bensyl, fenoxi-Ci-Ci0-alkyl, fenyl, som eventuellt ' \ är substituerad med Ci-C4-alkyl eller Ci~C4-alkoxi, en sul-fonatester, en mono-, di- eller trifosfatester, trityl eller monometoxitrityl, substituerad bensyl, trialkylsilyl eller difenylmetylsilyl; lauryl; myristyl; palmityl; stea-15 ryi; oleyl; monofosfat; difosfat eller trifosfat; eller ett farmaceutiskt godtagbart sait därav.
2. L-nukleosidförening enligt patentkrav 1, där R » ... -$ är tyrnin. I :Y:
3. L-nukleosidförening enligt patentkrav 1, där R i 20 är adenin eller cytosin. • .‘•tJ
4. L-nukleosidförening enligt patentkrav 1, där R' . ,·. är en sulfonatester, som är Ci-Ci0-alkylsulfonyl eller fe- • · · nyl-Ci-Cio-alkylsulfonyl eller bensyl-Ci-Ci0-alkylsulfonyl. • * *
5. L-nukleosidförening enligt patentkrav 1, där R' t t 25 är metansulfonyl.
• · · ♦ 6. L-nukleosidförening enligt patentkrav 1, där R' • · *...* är dimetyl-t-butylsilyl.
·***· 7. L-nukleosidförening enligt patentkrav 1, där R' ··· är Ci-C10-alkyl. • * 30
8. L-nukleosidförening enligt patentkrav 1, där R" ··· · ···! är en mono-, di- eller trifosfatester. . . f • ·'' * · 56 ' 1 1 7475
9. L-nukleosidförening enligt patentkrav 1, där R" | är väte.
10 EBV-infektion. |
10 D-enantiomer.
10. L-nukleosidförening enligt patentkrav 1, där R" är acetyl, propionyl eller butyryl. 5
11. L-nukleosidförening enligt patentkrav 1, som är 2' -fluor-5-metyl-p-L-arabinofuranosyluridin eller ett farmaceutiskt godtagbart sait därav.
12. L-nukleosidförening enligt nägot av de före-gäende patentkraven, som är ätminstone 95-%:igt ren frän >·
13. L-nukleosidförening enligt patentkrav 12, som är ätminstone 98-%-igt ren frän D-enantiomer. '
14. Modifierad oligonukleotid, där en eller flera J av nukleosiderna i den omodifierade oligonukleotiden har g 15 ersatts med en eller flera L-nukleosidföreningar enligt nägot av patentkraven 1-13.
15. Modifierad oligonukleotid enligt patentkrav a 14, där L-nukleosiden har placerats i nägondera ändan av oligonukleotiden.
16. Exonukleasresistent antisense-oligonukleotid, . | som innehäller ätminstone en L-nukleosidförening enligt , .·, ; nägot av patentkraven 1-13. , * · ·
17. Farmaceutisk composition, som innehäller en L-• · · ' £ M nukleosidförening enligt nägot av patentkraven 1 - 13 i en I * · · v'ij. | t 25 f armaceutiskt godtagbar bärare. ' f
® * *· *· 18. Farmaceutisk composition enligt patentkrav 17, " • · * · ' i M.* där den farmaceutiskt godtagbara bäraren är lämplig för m · · ί · oral administrering.
19. Farmaceutisk composition enligt patentkrav 17, : 30 där den farmaceutiskt godtagbara bäraren är en liposomsus- ··· · pension. _
• · .*, 20. Farmaceutisk composition enligt patentkrav 17, .? • · ·' ***·] där den farmaceutiskt godtagbara bäraren är en kontrolle- ? rat frigöringsbar komposition. ·*· 35
21. Farmaceutisk komposition, som innehäller 2'- i • · # * ·;··· f luor-5-metyl-p-L-arabinofuranosyluridin i en effektiv . ' 57 117475 mängd för behandling av HBV eller EBV i en farmaceutiskt godtagbar bärare.
22. Användning av en förening enligt nägot av pa-tentkraven 1-13 eller ett farmaceutiskt godtagbart sait 5 därav för framställning av ett läkemedel för behandling av HBV-infektion.
23. Användning av en förening enligt nägot av patent kraven 1-13 eller ett farmaceutiskt godtagbart sait därav för framställning av ett läkemedel för behandling av
24. Användning av 2’-fluor-S-metyl-p-L-arabino- ; A furanosyluridin eller ett farmaceutiskt godtagbart salt J därav för f ramställning av ett läkemedel för behandling av -r HBV-infektion.
25. Användning av 2'-fluor-5-metyl-0~L-arabino- V furanosyluridin eller ett farmaceutiskt godtagbart sait därav för framställning av ett läkemedel för behandling av EBV-infektion. 11 * ♦ · · • · · * · · · V| *\\ ' :' il • 1 2 3 4 1 ">i • · . --1-1 • a 1 ···". • · • · · • 1 · il • 1 - • · » • · · • · · • · • · · • · · * · 1 · • · · * · • · • · · • · · · · • · · · • · • · 2 ·♦· • · · · · 3 • , • ; > 4
FI962986A 1994-01-28 1996-07-26 L-nukleosider för behandling av hepatit-B-virus och Epstein-Barr-virus FI117475B (sv)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US18907094 1994-01-28
US08/189,070 US5587362A (en) 1994-01-28 1994-01-28 L-nucleosides
US9501253 1995-01-30
PCT/US1995/001253 WO1995020595A1 (en) 1994-01-28 1995-01-30 L-nucleosides for the treatment of hepatitis b-virus and epstein-bar virus

Publications (3)

Publication Number Publication Date
FI962986A0 FI962986A0 (sv) 1996-07-26
FI962986A FI962986A (sv) 1996-07-26
FI117475B true FI117475B (sv) 2006-10-31

Family

ID=22695792

Family Applications (4)

Application Number Title Priority Date Filing Date
FI962986A FI117475B (sv) 1994-01-28 1996-07-26 L-nukleosider för behandling av hepatit-B-virus och Epstein-Barr-virus
FI20051033A FI119416B (sv) 1994-01-28 2005-10-13 L-nukleosider för behandling av hepatit-B-virus och Epstein-Barr-virus
FI20070005A FI118954B (sv) 1994-01-28 2007-01-03 L-nukleosider för behandling av hepatit-B-virus och Epstein-Barr-virus
FI20080432A FI121846B (sv) 1994-01-28 2008-07-08 L-nukleosider för behandling av hepatit-B-virus och Epstein-Barr-virus

Family Applications After (3)

Application Number Title Priority Date Filing Date
FI20051033A FI119416B (sv) 1994-01-28 2005-10-13 L-nukleosider för behandling av hepatit-B-virus och Epstein-Barr-virus
FI20070005A FI118954B (sv) 1994-01-28 2007-01-03 L-nukleosider för behandling av hepatit-B-virus och Epstein-Barr-virus
FI20080432A FI121846B (sv) 1994-01-28 2008-07-08 L-nukleosider för behandling av hepatit-B-virus och Epstein-Barr-virus

Country Status (23)

Country Link
US (3) US5587362A (sv)
EP (2) EP0748330B1 (sv)
JP (1) JP3899440B2 (sv)
KR (1) KR100321209B1 (sv)
CN (1) CN1043769C (sv)
AT (2) ATE328889T1 (sv)
AU (1) AU710262B2 (sv)
BG (1) BG62571B1 (sv)
BR (1) BRPI9506596B8 (sv)
CA (1) CA2182273C (sv)
CZ (1) CZ292574B6 (sv)
DE (2) DE69530192T2 (sv)
DK (2) DK1283211T3 (sv)
ES (2) ES2194902T3 (sv)
FI (4) FI117475B (sv)
HK (1) HK1014716A1 (sv)
HU (1) HU228135B1 (sv)
NO (1) NO306408B1 (sv)
NZ (2) NZ330137A (sv)
PT (2) PT748330E (sv)
RO (1) RO116623B1 (sv)
SK (1) SK285191B6 (sv)
WO (1) WO1995020595A1 (sv)

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