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    • 9. 发明申请
    • UPAR SELECTIVE CONTRAST AGENT FOR MAGNETIC RESONANCE IMAGING
    • 用于磁共振成像的最新选择性对比剂
    • WO2008037666A1
    • 2008-04-03
    • PCT/EP2007/060051
    • 2007-09-21
    • DKFZ DEUTSCHES KREBSFORSCHUNGSZENTRUM, STIFTUNG DES ÖFFENTLICHEN RECHTSJUGOLD, ManfredKIESSLING, FabianZHANG, ChunfuWÄNGLER, BjörnPIPKORN, RüdigerSEMMLER, Wolfhard
    • JUGOLD, ManfredKIESSLING, FabianZHANG, ChunfuWÄNGLER, BjörnPIPKORN, RüdigerSEMMLER, Wolfhard
    • A61K47/48A61K38/04
    • A61K38/04A61K49/14A61K49/186A61K49/1863A61K49/1866B82Y5/00
    • The present invention relates to a contrast agent for magnetic resonance imaging comprising a compound of the formula Pep-L-Im, wherein Pep is a polypeptide molecule selected from the group consisting of (i) polypept ide having an amino acid sequence of NO:1; SEQ ID NO:2; SEQ ID NO:3; SEQ ID NO: 7; SEQ ID NO: 8; SEQ ID NO: 9; or SEQ ID NO: 13; (ii) polypept ide having an amino acid sequence which is at least 80 % identical with one of the amino acid sequences of NO:1; SEQ ID NO:2; SEQ ID NO:3; SEQ ID NO: 7; SEQ ID NO: 8; SEQ ID NO: 9; or SEQ ID NO: 13; and (iii) polypept ide derivative obtained through substitution, addition, inversion and/or deletion of one or two amino acids of the amino acid sequences of NO:1; SEQ ID NO:2; SEQ ID NO:3; SEQ ID NO: 7; SEQ ID NO: 8; SEQ ID NO: 9; or SEQ ID NO: 13, which binds to uPAR; L is a covalent single bond or a spacer; and Im is at least one superparamagnetic iron oxide particle having a coating of an anorganic or organic or anorganic and organic polymer, wherein the coating is covalently attached to L or to Pep, when L is a bond. Another aspect of the present invention is an in-vivo diagnostic method based on magnetic resonance imaging using said contrast agent.
    • 本发明涉及一种用于磁共振成像的造影剂,其包含式Pep-L-Im的化合物,其中Pep是选自(i)具有NO:1氨基酸序列的多肽的多肽分子 ; SEQ ID NO:2; SEQ ID NO:3; SEQ ID NO:7; SEQ ID NO:8; SEQ ID NO:9; 或SEQ ID NO:13; (ii)具有与NO:1的氨基酸序列之一至少80%相同的氨基酸序列的多肽; SEQ ID NO:2; SEQ ID NO:3; SEQ ID NO:7; SEQ ID NO:8; SEQ ID NO:9; 或SEQ ID NO:13; 和(iii)通过取代,添加,倒位和/或缺失NO:1的氨基酸序列的一个或两个氨基酸获得的多肽衍生物; SEQ ID NO:2; SEQ ID NO:3; SEQ ID NO:7; SEQ ID NO:8; SEQ ID NO:9; 或SEQ ID NO:13,其结合uPAR; L是共价单键或间隔基; 并且Im是至少一种具有无机或有机或有机和有机聚合物涂层的超顺磁性氧化铁颗粒,其中当L是键时,涂层共价连接到L或Pep。 本发明的另一方面是使用所述造影剂的基于磁共振成像的体内诊断方法。