2'-o-alkylnucleotides as well as polymers which contain such...

C - Chemistry – Metallurgy – 07 – H

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C07H 21/00 (2006.01) A61K 31/70 (2006.01) A61K 48/00 (2006.01) C07H 19/04 (2006.01) C07H 19/06 (2006.01) C07H 19/10 (2006.01) C07H 19/16 (2006.01) C07H 19/20 (2006.01)

Patent

CA 2080231

Oligonucleotides having the general formula, Image in which B denotes an arbitrary nucleobase, A equals 0 or CH2; X or Z equals O, S, NH or denotes CH2 whereby X and Z can be the same or different, V and W denote O, S, Se, NH2 or an alkyloxy residue, or OH or SH whereby V and W can be the same or different in a monomer unit and L is a H atom or a partner of a binding pair and C equals -O-R and R is an alkyl group with at least 1 C atom which may be modified if desired, or it denotes an alkenyl or alkinyl group with at least 2 C atoms which may be modified if desired, whereby the modification consists of a substitution by one or several halogen, cyano, carboxy, hydroxy, nitro or/and mercapto residues, and n is an arbitrary whole number, are stable antisense probes which bind specifically. Such oligonucleotides and polynucleotides may be used for the regulation of -2- gene expression and as pharmaceutical agents. They are synthesized from the corresponding 2'-substituted monomers according to well-known methods, preferably on a solid phase.

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