C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
C07H 21/00 (2006.01) C12N 15/11 (2006.01)
Patent
CA 2369976
The present invention relates to novel antisense (AS) oligos containing one or more antisense sequence to mRNA region with a less secondary structure. Particularly, the present invention relates to a covalently-closed multiple antisense (CMAS)-oligo, which is constructed to form a closed type by ligation using complementary primer, and a ribbon-type antisense (RiAS)-oligo, which is composed of two loops containing multiple antisense sequences and a stem connecting the two loops that is constructed to by ligation using complementary sequences at both 5 prime ends. Since the novel AS-oligos of this invention are extremely stable to exonuclease activities, and show a significant growth inhibition of tumor cells, pharmaceutical compositions containing the novel types of AS-oligos of the invention are effective for treatment cancer, immune diseases, infectious diseases, and other human diseases caused by aberrant gene expression.
L'invention concerne de nouveaux oligonucléotides antisens (AS) contenant une ou plusieurs séquences antisens d'une région d'ARNm avec une structure secondaire moindre. L'invention concerne plus particulièrement un oligonucléotide antisens (CMAS) multiple fermé par covalence construit pour former un type fermé par liaison utilisant une amorce complémentaire et un oligonucléotide antisens (RiAS) de type bande se composant de deux boucles contenant de multiples séquences antisens et une tige reliant les deux boucles construite à l'aide des séquences complémentaires aux deux extrémités des amorces 5. Les nouveaux oligonucléotides AS sont extrêmement stables aux activités de l'exonucléase et font preuve d'une inhibition importante à la croissance de cellules tumorales. Les compositions pharmaceutiques contenant ces nouveaux types d'oligonucléotides AS sont efficaces pour le traitement du cancer, de maladies immunes, de maladies infectieuses et d'autres maladies affectant l'homme provoquées par l'expression génique aberrante.
Park Jong-Gu
Sim & Mcburney
LandOfFree
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