Derivatization and solubilization of fullerenes for use in therapeutic and diagnostic applications
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United States of America Patent
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Oct 12, 2010
Grant Date -
Nov 27, 2003
app pub date -
Apr 9, 2003
filing date -
Oct 1, 2001
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Abstract
The invention provides improved therapeutic and diagnostic fullerenes and endohedral fullerenes. The fullerenes and endohedral fullerenes of the invention are derivatized with at least two charged functional groups (and preferably more than two charged functional groups) to provide for water-solubility and improved in vivo biodistribution. Improved derivatized fullerenes and endohedral fullerenes carry a plurality of functional groups at least two of which are charged. Preferably at least about ⅙ of the possible derivations sites on the fullerene caged carry derivatives and preferably at least about ½ of the functional groups on the fullerene cage are charged groups. The invention also provides water-soluble endohedral metallofullerene with improved biodistribution which are useful as in vivo imaging agents, including MRI contrast agents.
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