CHITOSAN COVALENTLY LINKED WITH SMALL MOLECULE INTEGRIN ANTAGONIST FOR TARGETED DELIVERY

摘要

The invention relates to the chitosan polymer derivatives of formula I: and pharmaceutically acceptable salts and esters thereof, wherein Y, X1, X4, R1, R2, and n are defined in the detailed description and claims. The chitosan polymer derivatives of formula I bind to or associate with alpha-4-beta-1 (α4β1) and alpha-V-beta-3 (αVβ3) integrin dimers and can be used in delivery formulations to deliver drugs, nucleic acids, or other therapeutic compounds to tissues or cells expressing such integrins.;

主权项

1. A chitosan polymer derivative of formula I: wherein the monomers of formula I are covalently linked to each other by a single oxygen atom at positions X1 and X4 which represent beta-1-4 linkages, except at the terminal ends of the polymer wherein X1 and X4 represent hydroxy of any stereochemistry; and wherein: Y is selected from the group consisting of:
(1) a moiety of the formula: and(2) a moiety of the formula: R1 is selected from the group consisting of:
(1) a moiety of the formula: wherein m is 0 or 1; and(2) a moiety of the formula: wherein is: R2 is hydrogen or methyl, and n is 8-25.