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US 9,803,201 B2Granted
Disulfide-containing alkyne linking agents
AssigneeArrowhead Pharmaceuticals, Inc.
InventorsAaron Almeida, Andrei V. Blokhin, Darren H. Wakefield, Jonathan D. Benson, David B. Rozema
Life of this patent
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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.
Claims14
A cyclooctyne-alkyl disulfide compound having the structure represented by:
- wherein,
- R3 is C(R5R6), wherein R5 is hydrogen, methyl or ethyl, and R6 is hydrogen, methyl or ethyl;
- R4 is C(R7R8), wherein R7 is hydrogen, methyl or ethyl, and R8 is hydrogen, methyl or ethyl;
- at least one of R5, R6, R7, and R8 is methyl or ethyl;
- L1 is a first linker;
- L2 is a second linker;
- and
- Y comprises a reactive group or a synthetic oligonucleotide.
5 more elements
A cyclooctyne-alkyl disulfide compound having the structure represented by:
- wherein,
- R3 is C(R5R6), wherein R5 is hydrogen, methyl or ethyl, and R6 is hydrogen, methyl or ethyl;
- R4 is C(R7R8), wherein R7 is hydrogen, methyl or ethyl, and R8 is hydrogen, methyl or ethyl;
- at least one of R5, R6, R7, and R8 is methyl or ethyl;
- L1 is a linker;
- and
- Y comprises a reactive group or a synthetic oligonucleotide.
4 more elements
Dependencies are inferred from the claim text.