发明名称 Radioactive transition metal-imido hetero-diphosphine complexes, their preparation and radiopharmaceutical compositions thereof
摘要 The present invention provides radioactive metal heterocomplexes of formula (I): [(Me=N—R)L1L2]+Z− wherein Me, R, L1L2 and Z− have the meanings indicated in the description. The complexes include a trivalent radioactive metal-imido group, typically a technetium-or rhenium-imido group, strongly stabilized by the presence of an ancillary tridentate hetero-diphosphine ligand L1, which allows the formation of substitution-inert [(Me=N—R)L1] moieties. Such moieties are fixed in an intermediate [(Me=N—R)Y2L1)]+ compound which contains two labile, cispositioned, Y ligands, where Y is preferably an halide group. The latter are easily replaced by a bidentate ligand L2 to give the final [(Me=N—R)L1L2]+ Z−heterocomplexes. The complexes of the invention are useful for the preparation of radiopharmaceuticals: in fact, a bioactive fragment which confers biological target-seeking properties can be introduced either on the L2 framework or the imido R group.
申请公布号 US7771704(B2) 申请公布日期 2010.08.10
申请号 US20080144370 申请日期 2008.06.23
申请人 BRACCO IMAGING S.P.A. 发明人 TISATO FRANCESCO;BOLZATI CRISTINA;PORCHIA MARINA;REFOSCO FIORENZO
分类号 A61K51/00;A61K51/04;A61M36/14;C07F9/50;C07F13/00 主分类号 A61K51/00
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