Synthesis of sulfide-linked di-or oligonucleotide analogs...

C - Chemistry – Metallurgy – 07 – H

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C07H 21/00 (2006.01) C07D 409/00 (2006.01) C07D 473/00 (2006.01) C07H 19/04 (2006.01) C07H 23/00 (2006.01)

Patent

CA 2078256

ABSTRACT OF THE DISCLOSURE An oligonucleotide analog of formula I in which one or more of the internucleoside phosphodiester groups are replaced by non- hydrolysable dialkyl sulfide, sulfoxide or sulfone linkages, such as in: Image in which R and R' are independently selected from H, DNA, RNA unsubstituted or substituted by I, nucleoside, nucleotides and analogs thereof; B is a base having a heterocyclic ring, X is independently O, CH2 or S; Y is independently H, OH or O-alkyl; Y' is H or O-alkyl; n is 0, 1 or 2; and m is 0 or an integer. These compounds are useful for binding selectively to complementary DNA or RNA strands (particularly mRNA strands) for use in regulating gene expression and as biological probes.

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