发明名称 Enhanced scintigraphic imaging agents for imaging of infection and inflammation
摘要 A reagent (R) comprises a polybasic compound comprising a peptide, where the peptide comprises at least four arginine residues, and a radiolabel-binding moiety covalently linked to the polybasic compound, where the reagent is capable of accumulating at sites of pathology in the body. Independent claims are also included for the following: (1) a multimeric reagent (MR) comprising at least two polybasic compounds of (R), which may be the same or different, at least one radiolabel-binding moiety covalently linked to one of the polybasic compounds, and a polyvalent linker moiety covalently linked to the polybasic compounds, the radiolabel-binding moieties or both, where the molecular weight of the multimeric polyvalent reagent is less than 20000 Da; (2) complex (CO) formed by either, reacting (R) with technetium-99m in the presence of a reducing agent, preferably a reducing agent chosen from dithionite ion, stannous ion, and ferrous ion, or labeling (R) with technetium-99m by ligand exchange of a prereduced technetium-99 m complex; (3) a composition (C) comprising (R), a polysulfated glycan having a molecular weight of 1000 Da, where the composition is capable of accumulating at sites of pathology in the mammalian body; (4) a scintigraphic imaging agent (IA) comprising (C) and a radioisotope, where the radioisotope is complexed to the reagent within the composition by its radiolabel-binding moiety; (5) a pharmaceutical composition (PC) comprising (R), (CO), (C), or (IA), and further comprising a carrier; (6) a kit (K) for preparing a radiopharmaceutical preparation, the kit comprising a first sealed vial containing a predetermined quantity of (R), and a sufficient amount of a reducing agent to label the reagent with a radioisotope, and a second sealed vial containing a predetermined quantity of a polysulfated glycan of (C); and (7) preparing (M1), (R) by in vitro chemical synthesis.
申请公布号 EP1437145(A1) 申请公布日期 2004.07.14
申请号 EP20030000204 申请日期 2003.01.07
申请人 SCHERING AG 发明人 MANCHANDA, RAJESH;KRAUSE, SABINE
分类号 A61K31/70;A61K51/08 主分类号 A61K31/70
代理机构 代理人
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