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US 5,629,184 AGranted
Cationic copolymers of vinylamine and vinyl alcohol for the delivery of oligonucleotides
AssigneeAmgen Inc.
InventorsMerrill S. Goldenberg, Alice C. Beekman
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Abstract
The present invention relates to an improved method for the cytoplasmic delivery of oligonucleotides using cationic copolymers based on vinyl alcohol with low levels of vinyl amine (PVAVAMs). Improved compositions for use in such method are also provided.
Claims13
A composition comprising a copolymer of the general formula I,
- --(CH.sub.2 --HCOH--)x--(CH.sub.2 --HCNR1R2R3--)y--(A)z-- I.
- where
- R1, R2 and R3 are independently hydrogen, lower alkyl or 2-hydroxyalkyl;
- or R1=R2=hydrogen, lower alkyl or 2-hydroxyalkyl and R3 is a lone pair electron
- A is a residual unit of a vinylic monomer
- x, y, and z are integers, representing the number of incorporated monomer and where x+y+z=100
- wherein x=25-99.5 mole %, y=0.5-75 mole %, and z<50 mole %, combined with a polynucleotide, wherein the molar ratio of y to anion units is 0.1-100, optionally in a pharmaceutically acceptable carrier, and wherein said composition allows for the cellular uptake of the polynucleotide.
4 more elements
Dependencies are inferred from the claim text.