发明名称 COMPOSITIONS AND METHODS FOR TUMOR IMAGING AND TARGETING BY A CLASS OF ORGANIC HEPTAMETHINE CYANINE DYES THAT POSSESS DUAL NUCLEAR AND NEAR-INFRARED PROPERTIES
摘要 The present invention provides for heptamethine cyanine dyes that possess both nuclear and near-infrared imaging capabilities. These dyes can be used for imaging, targeting and detecting tumors in patients.
申请公布号 US2014248213(A1) 申请公布日期 2014.09.04
申请号 US201214350194 申请日期 2012.10.05
申请人 University of Virginia Patent Foundation ;Cedars- Sinai Medical Center 发明人 Chung Leland W. K.;Pan Dongfeng
分类号 A61K51/04;A61B5/00;A61B6/00;A61K49/04;A61K49/00 主分类号 A61K51/04
代理机构 代理人
主权项 1. A Dual Nuclear/NIR Agent having a structure according to one of the following formulas: wherein R1 and R2 are each independently selected from the group consisting of radioisotopes I-125, I-123, I-131, I-124, F-18, hydrogen, sulfonato, an electron withdrawing group (EWG), an electron donating group (EDG), and are each independently attached at any of the aromatic ring positions; R3 and R4 are independently selected from the group consisting of hydrogen, alkyl, aryl, aralkyl, alkylsulfonato, alkylcarboxylic, alkylamino, ω-alkylaminium, ω-alkynyl, PEGyl, PEGylcarboxylate, ω-PEGylaminium, ω-acyl-NH—CR, ω-acyl-lysine-CR, ω-acyl-triazole-CR, ω-PEGylcarboxyl-NH—CR, ω-PEGylcarboxyl-lysine-CR, and ω-PEGylcarboxyl-triazole-CR; X is selected from the group consisting of a hydrogen, halogen, I-125, I-123, I-131, I-124, F-18, CN, Me, OH, 4-O-Ph-CH2CH2COOH, 4-O-Ph-NH—CR, NH—CR, 4-S-Ph-NH—CR, ω-iminoacyl-NH—CR, ω-aminoacyl-lysine-CR, ω-iminoacyl-triazole-CR, 4-O-Ph-CH2CH2COOCT, 4-O-Ph-O-CT, 4-S-Ph-O-CT, and ω-iminoacyl-O-CT, wherein CR is selected from the group consisting of a metal chelating agent, a radioactive or nonradioactive metal complex, a radioiodine or iodine labeled Bolten-Hunter reagent, and a radioiodine or iodine labeled tyrosine moiety, wherein the metal is selected from the group consisting of Cu-64, In-111, Tc-99m, Ga-68, Y-90, Lu-177, Re-188, At-211, Bi-213, Ac-225 and their nonradioactive counterparts, wherein CT is selected from the group consisting of radiolabeled or non-radiolabeled cytotoxic drugs, antibodies, toxins, aptamers, siRNA, antisense constructs and microRNAs; and counteranion A is selected from the group consisting of iodide, bromide, arylsulfonato, alkylsulfonato, tetrafluoroborate, chloride, and a pharmaceutically acceptable anion.
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