Disulfide-Containing Alkyne Linking Agents
AssigneeArrowhead Pharmaceuticals, Inc.
InventorsAaron Almeida, Andrei V. Blokhin, Darren H. Wakefield, Jonathan D. Benson, David B. Rozema
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Abstract
Described are improved disulfide-containing alkyne linking agents having have branched disulfides. The improved linking agents exhibit improved stability. The linking agents are useful for attachment of oligonucleotides to targeting groups or delivery agents.
Claims12
An RNAi agent-containing composition for inhibiting the expression of a target gene in a cell in vitro or in vivo, the RNAi agent-containing composition comprising an RNAi agent covalently linked to an cyclooctyne-alkyl disulfide compound having the structure represented by:
- wherein
- R1 is an alkyl group and R2 is hydrogen, or R1 is hydrogen and R2 is an alkyl group,
- L1 and L2 are linkers,
- X comprises a cyclooctyne, and
- Y comprises a reactive group.
An RNAi agent-containing composition for inhibiting the expression of a target gene in a cell in vitro or in vivo, the RNAi agent-containing composition comprising an RNAi agent covalently linked to an cyclooctyne-alkyl disulfide compound having the structure represented by:
- wherein
- R1 and R1′ are each alkyl groups and R2 and R2′ are each hydrogen, or R1 and R1′ are each hydrogen and R2 and R2′ are each alkyl groups,
- L1 and L2 are linkers,
- X comprises a cyclooctyne, and
- Y comprises a reactive group.
Dependencies are inferred from the claim text.