Oligomeric compounds for the modulation of bcl-2

Details Oligomeric compounds for the modulation of bcl-2 Oligomeric compounds for the modulation of bcl-2

C - Chemistry, Metallurgy

12

N

C12N 15/11 (2006.01) A61K 31/7088 (2006.01)

Patent

CA 2550258

The present invention provides improved oligomeric compound, in particular oligonucleotide compounds, and methods for modulating the expression of the Bcl-2 gene in humans. In particular, this invention relates to oligomeric compounds of 10-30 nucleobases in length which comprise a target binding domain that is specifically hybridizable to a region ranging from base position N~1459 (5~) to N~1476 (3~) of the human Bcl-2 mRNA, said target binding domain having the formula: 5~-[DNA/RNA)0-1-(LNA/LNA*)2-7- (DNA/RNA/LNA*)4-14-(LNA/LNA*)2-7-(DNA/RNA)0-1]-3~ and said target binding domain comprising at least two LNA nucleotides or LNA analogue nucleotides linked by a phosphorothioate group (-O-P(O,S)-O). In particular the oligo is predominantly or fully thiolated. The invention also provides the use of such oligomers or conjugates or chimera for the treatment of various diseases associated with the expression of the Bcl-2 gene, such as cancer.

La présente invention se rapporte à des composés oligomères améliorés, en particulier à des composés oligonucléotidiques, et à des procédés permettant de moduler l'expression du gène Bcl-2 chez les êtres humains. En particulier, l'invention a trait à des composés oligomères d'une longueur de 10-30 nucléobases, qui contiennent un domaine de liaison cible pouvant s'hybrider spécifiquement à une région allant de la position de base n· 1459 (5') à n· 1476 (3') de l'ARNm de Bcl-2 humain. Ledit domaine de liaison cible est représenté par la formule : 5'-[ADN/ARN)¿0-1?-(LNA/LNA*)¿2-7?-(ADN/ARN/LNA*)¿4-14?-(LNA/LNA*)¿2-7?-(ADN/ARN)¿0-1?]-3', et il contient au moins deux nucléotides LNA ou nucléotides analogues de LNA liés par un groupe phosphorothioate (-O-P(O,S)-O-). En particulier, l'oligomère selon l'invention est en majeure partie ou totalement thiolé. L'invention concerne également l'utilisation de tels oligomères, conjugués ou chimères pour traiter diverses maladies associées à l'expression du gène Bcl-2, telles que le cancer.

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