Oligonucleotides having aminohydrocarbon phosphonate moieties

C - Chemistry – Metallurgy – 12 – Q

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C12Q 1/68 (2006.01) A61K 31/70 (2006.01) A61K 47/48 (2006.01) A61K 48/00 (2006.01) A61K 49/00 (2006.01) C07H 21/00 (2006.01)

Patent

CA 2122470

2122470 9311148 PCTABS00022 An oligonucleotide wherein at least one nucleotide unit includes a phosphonate moiety having the structural formula (I) , wherein X is (a), R1 is a hydrocarbon, preferably methylene, and each of R2, R3, and R4 is hydrogen or a hydrocarbon, and each of R2, R3, and R4 may be the same or different. Preferably, X is an aminomethyl moiety. Such oligonucleotides having improved binding capabilities and improved resistance to nucleases. Alternatively, X may be (b) or (c), wherein R1, R2, and R3 are as hereinabove described, and R5 is a detectable marker, thus making such oligonucleotides useful as diagnostic probes.

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