Cationic oligonucleotides, automated methods for preparing same and their uses

Abstract

The invention relates to oligonucleotide-oligocation molecules ABH that can be synthetized via automated phosphoramidite chemistry having oligonucleotides moieties Ai and oligocations moieties Bj, wherein •Ais 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 group comprising deoxyribo, ribo, locked (LNA) nucleotides as well as their chemical 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 organic oligocation moiety, with j=1 to 50, where B is selected from the group comprising •—HPO—R—(X—R)—X—R—O—, where R, Rn and R, identical or different, are lower alkylene, X is NH or NC(NH), n varies from 1 to 5 and n1=2 to 20, •—HPO—R—CH(RX)—R—O—, where Ris lower alkylene, Rand R, identical or different, are lower alkylene and Xis putrescine, spermidine or spermine residue, •—HPO—R-(aa)-R—O—, where Ris lower alkylene and Ris lower alkylene, serine, a natural aminoalcohol, (aa)is a peptide containing natural aminoacids with cationic side chains, such as Arginine, Lysine, Ornithine, -Histidine, Diaminopropionic acid and n2=2 to 20.