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US 8,008,355 B2Granted
Endosomolytic poly(vinyl ether) polymers
AssigneeRoche Madison Inc.
InventorsDavid B. Rozema, Darren H. Wakefield, Sean D. Monahan, Lori Higgs, Jon A. Wolff, James E. Hagstrom
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Abstract
The present invention is directed to membrane active polymers useful for cellular delivery of compounds. Described are polyconjugates systems that incorporate targeting, anti-opsonization, anti-aggregation, and transfection activities into small biocompatible in vivo delivery conjugates. The use of reversible modification provides for physiologically responsive activity modulation.
Claims14
A membrane active random poly(vinyl ether) comprising:
- a plurality of amine-containing monomers, a plurality of lower hydrophobic monomers, and a plurality of higher hydrophobic monomers wherein said first and second hydrophobic monomers are different, wherein the ratio of amine-containing monomers to lower hydrophobic monomers to higher hydrophobic monomer is 4-8:3-5:1.
A reversibly masked membrane active random poly(vinyl ether) comprising:
- membrane active poly(vinyl ether) having a plurality of amine-containing monomers, a plurality of lower hydrophobic monomers, and a plurality of higher hydrophobic monomers in a ratio of 4-8:3-5:1 wherein one or more amines of the amine-containing monomers are linked to targeting groups via physiologically labile bonds thereby inhibiting membrane activity of the membrane active random poly(vinyl ether).
Dependencies are inferred from the claim text.