公开(公告)号：US07767796B2

公开(公告)日：2010-08-03

申请号：US11572161

申请日：2005-07-19

申请人： Anthony Eamonn Storey ,  Harry John Wadsworth ,  Nigel Anthony Powell ,  Philip Duncanson

发明人： Anthony Eamonn Storey ,  Harry John Wadsworth ,  Nigel Anthony Powell ,  Philip Duncanson

IPC分类号： C07F13/00

CPC分类号： A61K51/0478 ,  A61K51/0497

摘要： The present invention provides tetra-amine chelator conjugates with biological targeting moieties, linked via a linker group and technetium complexes thereof as radiopharmaceuticals. The linker group is such that the chelator is mono-functionalized at the bridgehead position and provides both flexibility and a lack or aryl groups, to minimize lipophilicity and steric hulk. Protected versions of the chelators are provided which permit conjugation with a wide range of targeting molecules without interfering reactions with the amine nitrogens of the tetra-amine chelator. Syntheses of the functionalised chelators are described, together with bifunctional chelate precursors. Radiopharmaceutical compositions comprising the technetium metal complexes of the invention are described, together with non-radioactive kits for the preparation of such radiopharmaceuticals.

摘要翻译： 本发明提供四胺螯合剂与生物靶向部分，通过连接基团和其锝络合物作为放射性药物连接。 接头基团使得螯合剂在桥头位置被单官能化并且提供柔性和缺乏或芳基，以使亲脂性和空间巨大的最小化。 提供了螯合剂的保护形式，其允许与宽范围的靶向分子缀合，而不与四胺螯合剂的胺氮化物发生干扰反应。 描述了官能化螯合剂的合成以及双官能螯合物前体。 本发明描述了包含本发明的锝金属络合物的放射性药物组合物，以及用于制备这种放射性药物的非放射性试剂盒。

公开(公告)号：US20080131368A1

公开(公告)日：2008-06-05

申请号：US11572161

申请日：2005-07-19

申请人： Anthony Eamonn Storey ,  Harry John Wadsworth ,  Nigel Anthony Powell ,  Philip Duncanson

发明人： Anthony Eamonn Storey ,  Harry John Wadsworth ,  Nigel Anthony Powell ,  Philip Duncanson

IPC分类号： A61K51/08 ,  C07K7/06 ,  C07C271/10 ,  C07D403/08 ,  C07K5/062

CPC分类号： A61K51/0478 ,  A61K51/0497

摘要： The present invention provides tetra-amine chelator conjugates with biological targeting moieties, linked via a linker group and technetium complexes thereof as radiopharmaceuticals. The linker group is such that the chelator is mono-functionalised at the bridgehead position and provides both flexibility and a lack or aryl groups, to minimise lipophilicity and steric hulk. Protected versions of the chelators are provided which permit conjugation with a wide range of targeting molecules without interfering reactions with the amine nitrogens of the tetra-amine chelator. Syntheses of the functionalised chelators are described, together with bifunctional chelate precursors. Radiopharmaceutical compositions comprising the technetium metal complexes of the invention are described, together with non-radioactive kits for the preparation of such radiopharmaceuticals.

摘要翻译： 本发明提供四胺螯合剂与生物靶向部分，通过连接基团和其锝络合物作为放射性药物连接。 接头基团使得螯合剂在桥头位置单官能化并提供柔性和缺乏或芳基，以使亲脂性和空间巨噬最小化。 提供了螯合剂的保护形式，其允许与宽范围的靶向分子缀合，而不与四胺螯合剂的胺氮化物发生干扰反应。 描述了官能化螯合剂的合成以及双官能螯合物前体。 本发明描述了包含本发明的锝金属络合物的放射性药物组合物，以及用于制备这种放射性药物的非放射性试剂盒。