Iodine-containing radial-shaped macromolecular compounds, preparation method thereof and contrast media compositions for CT comprising the same

摘要

Disclosed herein is an iodine-containing radial-shaped macromolecule suitable for an active ingredient of the computed tomography (CT) contrast medium, a method to prepare the same, and a contrast medium composition including the same. With respect to the iodine-containing radial-shaped macromolecule according to the present invention, the duration of contrast enhancement has been significantly improved in comparison to that of the current small molecular contrast media compounds containing iodine.

主权项

1. An iodine-containing radial-shaped macromolecule comprising:
a core composed of a circular or spherical symmetric small molecular compound, or a radial-shaped macromolecule; an iodine-containing compound bound to the core directly or through a peptide; and a biocompatible polymer bound to the core directly or through a peptide, or directly bound to the iodine-containing compound bound to the core, wherein the iodine-containing radial-shaped macromolecule has a structure in which the biocompatible polymers form a protective layer to prevent the exposure of the core and the iodine-containing compound in vivo; and the core has one or more surface functional groups selected form the group consisting of amine, hydroxyl, hydroxylamine, carboxyl, carboxyhydrazide, hydrazine, thiol, azide, alkynyl, halogen, aldehyde, ketone, epoxy, 3-carbomethoxypyrrolidinone, and tri-(C1-4 alkoxy)-silyl, which is covalently linked to the iodine-containing compound, the peptide, or the biocompatible polymer.