Compounds and methods for reversible modification of biologically active molecules
View Patent ↗The present invention is directed compounds for reversibly modification of biologically active molecules. 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.
1. An amine-reactive modifying agent represented by the structure consisting of:
wherein R 2 is a methyl group or ethyl group and R 1 is or contains a group selected from the group consisting of: aldehyde, maleic anhydride, galactose, vitamin, biotin, and polyethylene glycol.
2. The amine modifying agent of claim 1 wherein said poly(ethylene glycol) contains 1-500 ethylene glycol units.
3. The amine-reactive modifying agent of claim 2 wherein the modifying agent is represented by the structure selected from the group consisting of:
wherein n is an integer greater from 1 to 500, and R is selected from the group consisting of: hydrogen, alkyl group, targeting group, and reactive group.
4. The amine-reactive modifying agent of claim 1 wherein the modifying agent is represented by the structure consisting of:
5. The amine modifying agent of claim 1 wherein the galactose comprises a galactosamine.
6. The amine-reactive modifying agent of claim 1 wherein the modifying agent is represented by the structure selected from the group consisting of:
7. The amine modifying agent of claim 1 wherein the vitamin comprises folate.
8. The amine-reactive modifying agent of claim 7 wherein the modifying agent is represented by the structure consisting of:
9. The amine-reactive modifying agent of claim 1 wherein the modifying agent is represented by the structure consisting of:
10. A pH labile compound represented by the structure consisting of:
wherein
R 1 is or contains a group selected from the group consisting of: aldehyde, maleic anhydride, galactose, vitamin, biotin and polyethylene glycol;
R 2 is a methyl or ethyl group; and,
R 3 is any group.