DK2666859T3 - FARMACEUTISK SAMMENSÆTNING, DER OMFATTER ANTI-miRNA-ANTISENSE-OLIGONUKLEOTIDER - Google Patents
FARMACEUTISK SAMMENSÆTNING, DER OMFATTER ANTI-miRNA-ANTISENSE-OLIGONUKLEOTIDER Download PDFInfo
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Claims (31)
1. Enkeltstrenget oligonukleotid, der er 8-17 nukleotider langt og i stand til at reducere den effektive mængde af et modent humant mikroRNA i en celle, hvor mindst én af nukleobaseenhederne i oligonukleotidet er en LNA-nukleotidenhed, og hvor alle internukleosidbindingerne er phosphorothioatbindinger, hvor oligonukleotidet er komplementært til den modne humane mikroRNA-sekvens, hvor det enkeltstrengede oligonukleotid omfatter en region af sammenhængende nukleobasesekvens, der er 100 % komplementær til den humane mikroRNA-poderegion (seed region), og hvor oligonukleotidet omfatter mindst én LNA-nukleotidenhed i en position, der ligger inden for regionen, der er komplementær til miRNA-poderegionen, hvor yderligere: (a) nukleobaseenhederne 1 til 6 (inklusive) af det enkeltstrengede oligonukleotid målt fra 3'-enden af det enkeltstrengede oligonukleotid er komplementære til mikroRNA-poderegionsekvensen; eller (b) nukleobaseenhederne 1 til 7 (inklusive) af det enkeltstrengede oligonukleotid målt fra 3'-enden af det enkeltstrengede oligonukleotid er komplementære til mikroRNA-poderegionsekvensen; eller (c) nukleobaseenhederne 2 til 7 (inklusive) af det enkeltstrengede oligonukleotid målt fra 3'-enden af det enkeltstrengede oligonukleotid er komplementære til mikroRNA-poderegionsekvensen.
2. Enkeltstrenget oligonukleotid, der er 8-17 nukleotider langt og i stand til at reducere den effektive mængde af et modent humant mikroRNA i en celle, hvor mindst én af nukleobaseenhederne i oligonukleotidet er en LNA-nukleotidenhed, og hvor alle internukleosidbindingerne er phosphorothioatbindinger, hvor oligonukleotidet er komplementært til den modne humane mikroRNA-sekvens, hvor det enkeltstrengede oligonukleotid omfatter en region af sammenhængende nukleobasesekvens, der er 100 % komplementær til den humane mikroRNA-poderegion, og hvor oligonukleotidet omfatter mindst én LNA-nukleotidenhed i en position, der ligger inden for regionen, der er komplementær til miRNA-poderegionen, hvor oligonukleotidet er til anvendelse som et medikament, hvor yderligere: (a) nukleobaseenhederne 1 til 6 (inklusive) af det enkeltstrengede oligonukleotid målt fra 3'-enden af det enkeltstrengede oligonukleotid er komplementære til mikroRNA-poderegionsekvensen; eller (b) nukleobaseenhederne 1 til 7 (inklusive) af det enkeltstrengede oligonukleotid målt fra 3'-enden af det enkeltstrengede oligonukleotid er komplementære til mikroRNA-poderegionsekvensen; eller (c) nukleobaseenhederne 2 til 7 (inklusive) af det enkeltstrengede oligonukleotid målt fra 3'-enden af det enkeltstrengede oligonukleotid er komplementære til mikroRNA-poderegionsekvensen.
3. Oligonukleotid ifølge krav 1 eller oligonukleotid til anvendelse ifølge krav 2, hvor den første eller anden 3'-nukleobase af det enkeltstrengede oligonukleotid svarer til det andet 5'-nukleotid af mikroRNA-sekvensen.
4. Oligonukleotid ifølge krav 1 eller krav 3 eller oligonukleotid til anvendelse ifølge krav 2, hvor oligonukleotidet er i stand til at danne en dupleks med et komplementært enkeltstrenget RNA-nukleinsyremolekyle med phosphodiester-internukleosidbindinger, hvor dupleksen har en Tm på mindst ca. 60 °C.
5. Oligonukleotid ifølge et hvilket som helst af kravene 1, 3 eller 4 eller oligonukleotid til anvendelse ifølge et hvilket som helst af kravene 2-4, hvor oligonukleotidet er i stand til at danne en dupleks med et komplementært enkeltstrenget DNA-nukleinsyremolekyle med phosphodiester-internukleosidbindinger, hvor dupleksen har en Tm på 60-90 °C.
6. Oligonukleotid ifølge et hvilket som helst af kravene 1 eller 3-5 eller oligonukleotid til anvendelse ifølge et hvilket som helst af kravene 2-5, som omfatter mindst én 3'-terminal LNA-nukleotidenhed.
7. Oligonukleotid ifølge et hvilket som helst af kravene 1 eller 3-6 eller oligonukleotid til anvendelse ifølge et hvilket som helst af kravene 2-6, som omfatter mindst én 5'-terminal LNA-nukleotidenhed.
8. Oligonukleotid ifølge et hvilket som helst af kravene 1 eller 3-7 eller oligonukleotid til anvendelse ifølge et hvilket som helst af kravene 2-7, hvor mindst 30 % af nukleobaserne er LNA-enheder.
9. Oligonukleotid ifølge et hvilket som helst af kravene 1 eller 3-8 eller oligonukleotid til anvendelse ifølge et hvilket som helst af kravene 2-8, hvor oligonukleotidet omfatter mindst én region af mindst to på hinanden følgende LNA-nukleotidenheder.
10. Oligonukleotid ifølge et hvilket som helst af kravene 1 eller 3-9 eller oligonukleotid til anvendelse ifølge et hvilket som helst af kravene 2-9, hvor oligonukleotidet ikke omfatter en region på mere end 7 på hinanden følgende LNA-nukleotidenheder .
11. Oligonukleotid ifølge et hvilket som helst af kravene 1 eller 3-10 eller oligonukleotid til anvendelse ifølge et hvilket som helst af kravene 2-10, hvor oligonukleotidet ikke omfatter en region på mere end 6 eller mere end 5 eller mere end 4 eller mere end 3 eller mere end 2 på hinanden følgende LNA-nukleotidenheder.
12. Oligonukleotid ifølge et hvilket som helst af kravene 1 eller 3-11 eller oligonukleotid til anvendelse ifølge et hvilket som helst af kravene 2-11, som ikke omfatter en region på mere end 5 på hinanden følgende DNA-nukleotidenheder.
13. Oligonukleotid ifølge et hvilket som helst af kravene 1 eller 3-12 eller oligonukleotid til anvendelse ifølge et hvilket som helst af kravene 2-12, hvor oligonukleotidet ikke medierer RNAseH-baseret spaltning af et komplementært enkeltstrenget RNA-molekyle.
14. Oligonukleotid ifølge et hvilket som helst af kravene 1 eller 3-13 eller oligonukleotid til anvendelse ifølge et hvilket som helst af kravene 2-13, hvor oligonukleotidet har en længde på mellem 8 og 16 nukleobaser.
15. Oligonukleotid ifølge et hvilket som helst af kravene 1 eller 3-13 eller oligonukleotid til anvendelse ifølge et hvilket som helst af kravene 2-13, hvor oligonukleotidet har en længde på mellem 12 og 17 nukleobaser.
16. Oligonukleotid ifølge et hvilket som helst af kravene 1 eller 3-13 eller oligonukleotid til anvendelse ifølge et hvilket som helst af kravene 2-13, hvor oligonukleotidet har en længde på mellem 14 og 17 nukleobaser.
17. Oligonukleotid ifølge et hvilket som helst af kravene 1 eller 3-14 eller oligonukleotid til anvendelse ifølge et hvilket som helst af kravene 2-14, hvor oligonukleotidet har en længde på 10, 11, 12, 13, 14 eller 15 nukleobaser.
18. Oligonukleotid ifølge et hvilket som helst af kravene 1 eller 3-15 eller oligonukleotid til anvendelse ifølge et hvilket som helst af kravene 2-15, hvor oligonukleotidet har en længde på 14 nukleobaser.
19. Oligonukleotid ifølge et hvilket som helst af kravene 1 eller 3-15 eller oligonukleotid til anvendelse ifølge et hvilket som helst af kravene 2-15, hvor oligonukleotidet har en længde på 15 nukleobaser.
20. Oligonukleotid ifølge et hvilket som helst af kravene 1 eller 3-15 eller oligonukleotid til anvendelse ifølge et hvilket som helst af kravene 2-15, hvor oligonukleotidet har en længde på 16 nukleobaser.
21. Oligonukleotid ifølge et hvilket som helst af kravene 1 eller 3-15 eller oligonukleotid til anvendelse ifølge et hvilket som helst af kravene 2-15, hvor oligonukleotidet har en længde på 17 nukleobaser.
22. Oligonukleotid ifølge et hvilket som helst af kravene 1 eller 3-14 eller oligonukleotid til anvendelse ifølge et hvilket som helst af kravene 2-14, hvor oligonukleotidet har en længde på mellem 8 og 16 nukleobaser, og hvor oligonukleotidet ikke omfatter en region på mere end 7 på hinanden følgende LNA-nukleotidenheder.
23. Oligonukleotid ifølge et hvilket som helst af kravene 1 eller 3-14 eller oligonukleotid til anvendelse ifølge et hvilket som helst af kravene 2-14, hvor oligonukleotidet har en længde på mellem 8 og 16 nukleobaser, og hvor nukleobaseenhederne 1 til 6 (inklusive) af det enkeltstrengede oligonukleotid målt fra 3'-enden af det enkeltstrengede oligonukleotid er komplementære til mikroRNA-poderegionsekvensen.
24. Oligonukleotid ifølge et hvilket som helst af kravene 1 eller 3-14 eller oligonukleotid til anvendelse ifølge et hvilket som helst af kravene 2-14, hvor oligonukleotidet har en længde på mellem 8 og 16 nukleobaser, og hvor oligonukleotidet ikke omfatter en region på mere end 7 på hinanden følgende LNA-nukleotidenheder, hvor yderligere nukleobaseenhederne 1 til 6 (inklusive) af det enkeltstrengede oligonukleotid målt fra 3'-enden af det enkeltstrengede oligonukleotid er komplementære til mikroRNA-poderegionsekvensen.
25. Oligonukleotid ifølge et hvilket som helst af kravene 22-24 eller oligonukleotid til anvendelse ifølge et hvilket som helst af kravene 22-24, hvor oligonukleotidet har en længde på 14 nukleobaser.
26. Oligonukleotid ifølge et hvilket som helst af kravene 22-24 eller oligonukleotid til anvendelse ifølge et hvilket som helst af kravene 22-24, hvor oligonukleotidet har en længde på 15 nukleobaser.
27. Oligonukleotid ifølge et hvilket som helst af kravene 22-24 eller oligonukleotid til anvendelse ifølge et hvilket som helst af kravene 22-24, hvor oligonukleotidet har en længde på 16 nukleobaser.
28. Oligonukleotid ifølge et hvilket som helst af kravene 1 eller 3-27 eller oligonukleotid til anvendelse ifølge et hvilket som helst af kravene 2-27, hvor oligonukleotidet har mindst to LNA-enheder i positioner, der er komplementære til miRNA-poderegionen.
29. Oligonukleotid ifølge et hvilket som helst af kravene 1 eller 3-28 eller oligonukleotid til anvendelse ifølge et hvilket som helst af kravene 2-28, hvor oligonukleotidet har mindst tre LNA-enheder i positioner, der er komplementære til miRNA-poderegionen.
30. Oligonukleotid ifølge et hvilket som helst af kravene 1 eller 3-29 eller oligonukleotid til anvendelse ifølge et hvilket som helst af kravene 2-29, hvor oligonukleotidet har mindst fire LNA-enheder i positioner, der er komplementære til miRNA-poderegionen.
31. Farmaceutisk sammensætning, der omfatter det enkeltstrengede oligonukleotid ifølge et hvilket som helst af kravene 1 eller 3-30 og et farmaceutisk acceptabelt fortyndingsmiddel, bæremateriale eller adjuvans.
Applications Claiming Priority (7)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US78899506P | 2006-04-03 | 2006-04-03 | |
DKPA200600478 | 2006-04-03 | ||
US79681306P | 2006-05-01 | 2006-05-01 | |
DKPA200600615 | 2006-05-01 | ||
US83871006P | 2006-08-18 | 2006-08-18 | |
DKPA200601401 | 2006-10-30 | ||
EP20100158023 EP2194129A3 (en) | 2006-04-03 | 2007-03-30 | Pharmaceutical composition comprising anti-miRNA antisense oligonucleotides |
Publications (1)
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DK2666859T3 true DK2666859T3 (da) | 2019-04-08 |
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Application Number | Title | Priority Date | Filing Date |
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DK13172958.4T DK2666859T3 (da) | 2006-04-03 | 2007-03-30 | FARMACEUTISK SAMMENSÆTNING, DER OMFATTER ANTI-miRNA-ANTISENSE-OLIGONUKLEOTIDER |
Country Status (12)
Country | Link |
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US (8) | US20100004320A1 (da) |
EP (3) | EP2007889A2 (da) |
JP (5) | JP5814505B2 (da) |
KR (1) | KR101407707B1 (da) |
AU (1) | AU2007234191B2 (da) |
CA (4) | CA2649045C (da) |
DK (1) | DK2666859T3 (da) |
EA (1) | EA015570B1 (da) |
ES (1) | ES2715625T3 (da) |
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