Polylysine dendrimer contrast agent

摘要

The present invention relates generally to branched macromolecules and their use as imaging or contrast agents. In particular, the invention relates to dendrimers, derived from lysine or lysine analogs, bearing a plurality of functional moieties and their application to imaging techniques in which a disease state may be imaged with a targeted contrast agent.

主权项

1. A macromolecule comprising:
a dendrimer comprising (i) a core moiety having a first amino nitrogen atom for attachment to a first functional moiety and at least two further amino nitrogen atoms for attachment to lysine or lysine analogue building units; wherein the core is selected from the group consisting of a tri-amino compound, a tetra-amino compound, and a penta-amino compound; and (ii) at least one layer of lysine or lysine analogue building units, wherein each building unit in a first of the layers is attached to the core moiety by an amide bond, through the at least two further amino nitrogen atoms of the core moiety, and any building units in subsequent layers are attached to a previous layer through an amide bond, wherein an outermost layer of the at least one layer of lysine or lysine analogue building units has at least one surface amine for attachment to the one or more second functional moieties; and a first functional moiety attached to the core moiety through the first amino nitrogen atom; one or more second functional moieties attached to the surface amino nitrogen atoms of the outermost layer of lysine or lysine analogue building units; wherein the first functional moiety is a targeting molecule, which retains the ability in said macromolecule to specifically bind to another molecule, and the second functional moiety is a signalling entity.