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US 6,242,589 B1Granted
Phosphorothioate oligonucleotides having modified internucleoside linkages
AssigneeIsis Pharmaceuticals, Inc.
InventorsPhillip Dan Cook, Muthiah Manoharan
Life of this patent
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Abstract
Novel compounds that mimic and/or modulate the activity of wild-type nucleic acids. In general, the compounds are phosphorothioate oligonucleotides wherein the 5′-terminal internucleoside linkage or the 5′- and 3′-terminal linkages are modified.
Claims16
A compound comprising a plurality of covalently-bound nucleosides, said compound having the formula:
- (5′)NU-L1-[NU-LS]n-NU-L2-NU(3′)
- wherein:
- each NU is, independently, a nucleoside that includes a ribose or deoxyribose sugar portion and a base portion;
- LS is a racemic phosphorothioate internucleoside linkage;
- n is 1-200;
- and
- L1 and L2 are independently selected such that:
- L1 is a Sp phosphorothioate internucleoside linkage, L2 is a racemic phosphorothioate internucleoside linkage, and said compound has greater than about 60% stereoisomeric purity;
- or
- L1 and L2 both are Sp phosphorothioate internucleoside linkages and said compound has greater than about 60% stereoisomeric purity;
- or
- L1 is a Rp phosphorothioate internucleoside linkage, L2 is a racemic phosphorothioate internucleoside linkage, and said compound has greater than about 60% stereoisomeric purity;
- or
- L1 and L2 both are Rp phosphorothioate internucleoside linkages and said compound has greater than about 60% stereoisomeric purity;
- or
- L1 and L2, independently, have the formula CH2—O—NR or CH2—NR—O wherein R is H, alkyl having 1 to about 10 carbon atoms, alkenyl having 2 to about 10 carbon atoms, alkynyl having 2 to about 10 carbon atoms;
- alkaryl having 7 to about 14 carbon atoms, aralkyl having 7 to about 14 carbon atoms.
14 more elements
Dependencies are inferred from the claim text.