CATIONIC OLIGONUCLEOTIDES, AUTOMATED METHODS FOR PREPARING SAME AND THEIR USES

摘要

The invention relates to oligonucleotide-oligocation molecules AiBjH that ca n be synthetized via automated phosphoramidite chemistry having oligonucleotid es moieties Ai and oligocations moieties Bj, wherein . Ai is an i-mer oligonucleotide residue, with i = 5 to 50, where nucleotide A is an oligomer with naturally or non naturally occurring nucleobases and/or pentafuranosyl groups and/or native phosphodiester bonds, for example selected from the gro up comprising deoxyribo, ribo, locked (LNA) nucleotides as well as their chemic al modifications or substitutions such as phosphorothioate, 2'-fluoro, 2'-O- alkyl, or a marker group such as a fluorescent agent, . Bj is a j-mer organi c oligocation moiety, with j = 1 to 50, where B is selected from the group comprising ~ - HPO3-R1 -(X-R2 n)n1-X-R3-O-, where R1, R2n and R3, identical or different, are lower alkylene, X is NH or NC(NH2)2, n varies from 1 to 5 and n1 = 2 to 20, ~ - HPO3-R4-CH(R5X1)-R6-O-, where R4 is lower alkylene, R5 and R6, identical or different, are lower alkylene and X1 is putrescine, spermidine or spermine residue, ~ - HPO3-R7-(aa)n2-R8-O-, where R7 is lower alkylene and R8 is lower alkylene, serine, a natural aminoalcohol, (aa)n2 is a peptide containing natural aminoacids with cationic side chains, such as Arginine, Lysine, Ornithine, - Histidine, Diaminopropionic acid and n2= 2 to 20.