Compositions for inhibiting RNA activity
AssigneeIsis Pharmaceuticals, Inc.
InventorsPhillip D. Cook, Thomas Bruice, Charles J. Guinosso, Andrew M. Kawasaki
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Abstract
Compositions and methods for modulating the activity of RNA are disclosed. In accordance with preferred embodiments, antisense compositions are prepared comprising targeting and reactive portions. The reactive portions preferably comprise one or two imidazole functionalities conjugated to the targeting oligonucleotide via linkers with or without intervening intercalating moieties. Therapeutics, diagnostics and research methods also are disclosed, as are synthetic nucleosides and nucleoside fragments that can be elaborated into oligonucleotides.
Claims21
A compound of the structure:
- G.sub.0 --G.sub.1 --G.sub.2 --G.sub.3
- wherein:
- G.sub.0 is a nucleoside, a nucleotide or an oligonucleotide;
- G.sub.1 is O--alkyl, O--alkenyl, or O--alkynyl;
- G.sub.2 is an aryl moiety;
- and
- G.sub.3 includes at least one imidazole moiety.
A compound of the structure:
- ##STR10## T.sub.5 is H, a hydroxyl protecting group, a phosphate group, a nucleotide or an oligonucleotide;
- T.sub.3 is H, a hydroxyl protecting group, a nucleotide, an oligonucleotide, a phosphate group, an activated phosphate group or solid phase support;
- G.sub.1' is O;
- G.sub.1" is alkyl, alkenyl, or alkynyl;
- G.sub.2 is an aryl moiety;
- G.sub.3 includes at least one imidazole moiety;
- and
- Bx is a heterocyclic base moiety.
A compound of the structure:
- ##STR11## T.sub.5 is H, a hydroxyl protecting group, a phosphate group, a nucleotide or an oligonucleotide;
- T.sub.3 is H, a hydroxyl protecting group, a nucleotide, an oligonucleotide, a phosphate group, an activated phosphate group or a solid phase support;
- G.sub.1' is O;
- G.sub.1" is alkynyl;
- and
- Bx is a heterocyclic base moiety, provided that when Bx is uracil then T.sub.3 and T.sub.5 are not H or acetyl.
Dependencies are inferred from the claim text.