发明名称 TEXAPHYRIN METAL COMPLEXES HAVING IMPROVED FUNCTIONALIZATION
摘要 Texaphyrin metal complexes of formula (I) 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 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 tumor therapy and applications requiring singlet oxygen production for cytotoxicity. Electron withdrawing groups at positions 15 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 radiosensitization applications.
申请公布号 WO9521845(A1) 申请公布日期 1995.08.17
申请号 WO1995US01996 申请日期 1995.02.15
申请人 BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM;PHARMACYCLICS, INC.;SESSLER, JONATHAN, L.;MODY, TARAK, D.;HEMMI, GREGORY, W. 发明人 SESSLER, JONATHAN, L.;MODY, TARAK, D.;HEMMI, GREGORY, W.
分类号 A61K31/40;A61K41/00;A61K47/48;A61K49/00;A61K49/06;A61K49/08;A61K51/00;A61K51/04;A61L2/00;A61P35/00;C07D487/22;C07H21/00;(IPC1-7):C07D487/22 主分类号 A61K31/40
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