Methods of MRI enhancement using compounds having improved functionalization

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United States of America Patent

PATENT NO 5601802
SERIAL NO

08486886

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Abstract

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Texaphyrin metal complexes having improved functionalization include the addition of electron-donating groups to positions 2, 7, 12, 15, 18 and/or 21 and/or the addition of electron-withdrawing groups to positions 15 and/or 18 of the macrocycle. Electron-donating groups at positions 2, 7, 12, 15, 18 and/or 21 contribute electrons to the aromatic .pi. system of the macrocycle which stabilizes the metal complex to demetallation and the imine bonds to hydrolysis. These texaphyrin metal complexes having enhanced stability are useful for localization, magnetic resonance imaging, radiosensitization, radiation therapy, fluorescence imaging, photodynamic therapy, RNA hydrolysis, DNA photocleavage, and applications requiring singlet oxygen production for cytotoxicity. Electron-withdrawing groups at positions 15 and/or 18 render the macrocycle more readily reduced, i.e. the redox potential is lower and the macrocycle more readily gains an electron to form a radical. Such texaphyrins having a low redox potential are useful for radiation sensitization applications.

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Patent Owner(s)

Patent OwnerAddress
PHARMACYCLICS INCCALIFORNIA USA CALIFORNIA

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Hemmi, Gregory W Sunnyvale, CA 34 1650
Mody, Tarak D Sunnyvale, CA 73 3051
Sessler, Jonathan L Austin, TX 94 2801

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