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US 2012/0238735 A1Published application
Monoconjugated Chitosans as Delivery Agents for Small Interfering Nucleic Acids
AssigneeNektar Therapeutics
InventorsSamuel P. McManus, Antoni Kozlowski, Patrick D. Youso
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Abstract
Conjugates are provided, an exemplary conjugating having a single water-soluble, non-peptidic polymer, such as a poly(ethylene oxide), attached to a chitosan. Complexes of small interfering nucleic acids formed with such conjugates as well as small interfering nucleic acids attached to such conjugates are also provided. Related methods, intermediates, and compositions are also provided.
Claims17
A conjugate having a single water-soluble, non-peptidic polymer attached to a chitosan.
A chitosan having the following structure:
- G1-L2-X—N═CH-(Chitosan) (Formula IVa)
- wherein:
- G1 is a functional group, in protected or unprotected form;
- L2 is a linker group;
- X is oxygen or NR2, wherein R2 is selected from the group consisting of hydrogen, methyl, lower alkyl, cycloalkyl, and aryl;
- and
- Chitosan is a residue of a chitosan.
4 more elements
A chitosan having the following structure:
- G1-L2-X—NH—CH2-(Chitosan) (Formula IVb)
- wherein:
- G1 is a functional group, in protected or unprotected form;
- L2 is a linker group;
- X is oxygen or NR2, wherein R2 is selected from the group consisting of hydrogen, methyl, lower alkyl, cycloalkyl, and aryl;
- and
- Chitosan is a residue of a chitosan.
4 more elements
An siNA conjugate of:
- (a) an siNA;
- and (b) a single-water-soluble, non-peptidic polymer attached to a chitosan.
Dependencies are inferred from the claim text.