申请人:Cappelletti Enrico
公开号:US20060018830A1
公开(公告)日:2006-01-26
New and improved compounds for use in diagnostic imaging or therapy having the formula M-N—O—P-G, wherein M is a metal chelator having the structure:
wherein R1-R5 and FG are as defined herein (in the form complexed with a metal radionuclide or not), N—O—P is the linker containing at least one non-alpha amino acid with a cyclic group, at least one substituted bile acid or at least one non-alpha amino acid, and G is the GRP receptor targeting peptide. In the preferred embodiment, M is an Aazta metal chelator or a derivative thereof. Methods for imaging a patient and/or providing radiotherapy or phototherapy to a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound is further provided. Methods and kits for preparing a radiotherapeutic agent are further provided.
新的改进化合物用于诊断影像或治疗,其化学式为M-N—O—P-G,其中M是具有以下结构的金属螯合剂:
其中R1-R5和FG的定义如本文所述(以金属放射性核素或未配合的形式),N—O—P是含有至少一个非α氨基酸的连接剂,其中该氨基酸具有一个环形基团,至少一个取代的胆汁酸或至少一个非α氨基酸,而G是GRP受体靶向肽。在首选实施例中,M是Aazta金属螯合剂或其衍生物。还提供了使用该发明的化合物对患者进行成像和/或提供放射治疗或光疗的方法。还提供了制备诊断成像剂的方法和试剂盒。还提供了制备放射治疗剂的方法和试剂盒。