DK2284269T3 - Antisense-design - Google Patents

Antisense-design Download PDF

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DK2284269T3
DK2284269T3 DK10182316.9T DK10182316T DK2284269T3 DK 2284269 T3 DK2284269 T3 DK 2284269T3 DK 10182316 T DK10182316 T DK 10182316T DK 2284269 T3 DK2284269 T3 DK 2284269T3
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lna
oxy
alpha
nucleotide units
beta
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DK10182316.9T
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Signe Christensen
Nikolaj Mikkelsen
Miriam Frieden
Henrik Hansen
Troels Koch
Daniel Pedersen
Majken Westergaard
Christoph Rosenbohm
Charlotte Thrue
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Roche Innovation Ct Copenhagen As
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    • C12N15/09—Recombinant DNA-technology
    • C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • C12N15/113—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing
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    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
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    • C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • C12N15/113—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing
    • C12N15/1137—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing against enzymes
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    • C12N2310/32—Chemical structure of the sugar
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Claims (14)

1. Antisense-oligonukleotid-konstrukt til anvendelse i en farmaceutisk sammensætning, omfattende mindst et alfa-L-oxy-LNA; hvor mindst en af bindingerne mellem nukleosidenhederne af antisense-oligonukleotid-konstruktet er en phosphorthioatbinding.
2. Antisense-oligonukleotid-konstrukt ifølge krav 1, der omfatter mindst to låste nukleotidenheder placeretefter hinanden, hvoraf mindst en er alfa-L-oxy-LNA.
3. Antisense-oligonukleotid-konstrukt ifølge krav 1, hvor antisense- oligonukleotid-konstruktet er i stand til at rekruttere RNaseH-aktivitet.
4. Antisense-oligonukleotid-konstrukt ifølge krav 2, hvor antisense- oligonukleotid-konstruktet omfatter to nukleotidsekvenser A og B placeret ved siden af hinanden, hvor: A betegner en sekvens af nukleotidenheder, der omfatter mindst to låste nukleotidenheder placeret efter hinanden, hvoraf mindst en er en alfa-L-oxy-LNA-enhed; og B betegner en nukleotidenhed eller en sekvens af nukleotidenheder med det forbehold, at mindst en nukleotidenhed i B har en 2'-deoxy-erythro-pentofuranosyl-sukkergruppe.
5. Antisense-oligonukleotid-konstrukt ifølge krav 4, hvor sekvens A omfatter 2, 3, 4 eller 5 LNA-enheder.
6. Antisense-oligonukleotid-konstrukt ifølge krav 3, hvor oligonukleotid-konstruktet indeholder tre nukleotidsekvenser A, B og C placeret ved siden af hinanden i følgende rækkefølge (5' til 3'): A-B-C eller C-B-A, hvor A betegner en sekvens, der omfatter mindst to låste nukleotidenheder placeret efter hinanden, hvoraf mindst en er en alfa-L-oxy-LNA-enhed, B betegner en nukleotidenhed eller en sekvens af nukleotidenheder med det forbehold, at mindst en nukleotidenhed i B har en 2'-deoxy-erythro-pentofuranosyl-sukkergruppe; og C betegner en sekvens, der omfatter mindst to låste nukleotidenheder placeret efter hinanden, hvoraf mindst en er en alfa-L-oxy-LNA-enhed.
7. Antisense-oligonukleotid-konstrukt ifølge et hvilket som helst af kravene 4-6, hvor B betegner en sekvens af nukleotidenheder, der gør konstruktet i stand til at rekruttere RNaseH, når det er hybridiseret til en mål-nukleinsyre.
8. Antisense-oligonukleotid-konstrukt ifølge krav 6 eller 7, hvor A har en længde på 2-8 nukleotidenheder, B haren længde på 5-10 nukleotidenheder, og C har en længde på 2-8 nukleotidenheder.
9. Antisense-oligonukleotid-konstrukt ifølge krav 8, hvor den samlede længde af konstruktet er 10-20 nukleotidenheder.
10. Antisense-oligonukleotid-konstrukt ifølge et hvilket som helst af kravene 6-9, hvor A betegner en sekvens af nukleotidenheder, der omfatter mindst tre låste nukleotidenheder placeret efter hinanden, idet mindst en af de låste nukleotidenheder er alfa-L-oxy-LNA.
11. Antisense-oligonukleotid-konstrukt ifølge et hvilket som helst af kravene 6-10, hvor C betegner en sekvens af nukleotidenheder, der omfatter mindst tre låste nukleotidenheder placeret efter hinanden, idet mindst en af de låste nukleotidenheder er alfa-L-oxy-LNA.
12. Antisense-oligonukleotid-konstrukt ifølge et hvilket som helst af kravene 6-11, hvor B betegner en sekvens af 5, 6, 7, 8, 9 eller 10 nukleotidenheder, der er valgt fra gruppen bestående af 2'-deoxy-erythro-pentofuranosyl-sukkergruppe(r)-nukleotidenheder og alfa-L-oxy-LNA-nukleotidenheder.
13. Antisense-oligonukleotid-konstrukt ifølge et hvilket som helst af kravene 6-12, hvor A og C omfatter mindst en alfa-L-oxy-LNA-enhed placeret ved siden af B.
14. Antisense-oligonukleotid-konstrukt ifølge et hvilket som helst af kravene 1-13 til anvendelse ved antisense-terapi.
DK10182316.9T 2002-11-18 2003-11-18 Antisense-design DK2284269T3 (da)

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DKPA200201774 2002-11-18
DKPA200301540 2003-10-20
EP09169370.5A EP2141233B1 (en) 2002-11-18 2003-11-18 Antisense design

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DK09169370.5T DK2141233T3 (da) 2002-11-18 2003-11-18 Antisense design
DK17170205.3T DK3222722T3 (da) 2002-11-18 2003-11-18 Antisense-design
DK14163184.6T DK2752488T3 (da) 2002-11-18 2003-11-18 Antisense-design
DK03773575T DK1569661T3 (da) 2002-11-18 2003-11-18 Antisense design
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DK17170205.3T DK3222722T3 (da) 2002-11-18 2003-11-18 Antisense-design
DK14163184.6T DK2752488T3 (da) 2002-11-18 2003-11-18 Antisense-design
DK03773575T DK1569661T3 (da) 2002-11-18 2003-11-18 Antisense design

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US (15) US7687617B2 (da)
EP (5) EP2752488B1 (da)
AT (1) ATE442152T1 (da)
AU (2) AU2003281969B2 (da)
CA (2) CA2506576C (da)
DE (1) DE60329220D1 (da)
DK (5) DK2141233T3 (da)
ES (1) ES2607471T3 (da)
HK (1) HK1244504A1 (da)
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