公开(公告)号：US10927132B2

公开(公告)日：2021-02-23

申请号：US15055203

申请日：2016-02-26

申请人： Hans F. Schmitthenner ,  Anne M. Sweeney-Jones ,  Scott Williams

发明人： Hans F. Schmitthenner ,  Anne M. Sweeney-Jones ,  Scott Williams

IPC分类号： A61K51/00 ,  A61M36/14 ,  C07F5/00 ,  C07F1/00 ,  A61K51/08 ,  B01D15/38 ,  B01D15/42 ,  C07F1/08 ,  B01D15/32

摘要： A process for the preparation of a radionuclide imaging agent includes providing an imaging agent including a chelated place-holder metal; loading the imaging agent onto an acid stable stationary phase; replacing the chelated place-holder metal of the imaging agent loaded on the stationary phase with a replacement radioactive metal under mild reaction conditions; and eluting the imaging agent including the chelated replacement radioactive metal from the stationary phase to provide a radionuclide imaging agent suitable for positron emission tomography (PET) or single-photon emission computed tomography (SPECT). The imaging agent can include a targeting agent that is directly conjugated to the imaging agent or by means of a linker. The process may also apply to other metals that are non-radioactive but used as diluent metals or other metals that are strongly bound to DOTA.

公开(公告)号：US20160251378A1

公开(公告)日：2016-09-01

申请号：US15055203

申请日：2016-02-26

申请人： Hans F. Schmitthenner ,  Anne M. Sweeney-Jones ,  Scott Williams

发明人： Hans F. Schmitthenner ,  Anne M. Sweeney-Jones ,  Scott Williams

IPC分类号： C07F5/00 ,  B01D15/38 ,  B01D15/42 ,  C07F1/08

CPC分类号： C07F5/00 ,  A61K51/082 ,  A61K51/088 ,  B01D15/325 ,  B01D15/3857 ,  B01D15/426 ,  C07F1/005 ,  C07F1/08 ,  C07F5/003

摘要： A process for the preparation of a radionuclide imaging agent includes providing an imaging agent including a chelated place-holder metal; loading the imaging agent onto an acid stable stationary phase; replacing the chelated place-holder metal of the imaging agent loaded on the stationary phase with a replacement radioactive metal under mild reaction conditions; and eluting the imaging agent including the chelated replacement radioactive metal from the stationary phase to provide a radionuclide imaging agent suitable for positron emission tomography (PET) or single-photon emission computed tomography (SPECT). The imaging agent can include a targeting agent that is directly conjugated to the imaging agent or by means of a linker. The process may also apply to other metals that are non-radioactive but used as diluent metals or other metals that are strongly bound to DOTA.

摘要翻译： 一种制备放射性核素成像剂的方法包括提供包含螯合位置保持金属的成像剂; 将成像剂加载到酸稳定的固定相上; 在温和的反应条件下用置换的放射性金属代替负载在固定相上的成像剂的螯合的载体金属; 并从固定相中洗脱包含螯合置换放射性金属的成像剂，以提供适用于正电子发射断层摄影（PET）或单光子发射计算机断层摄影（SPECT）的放射性核素显像剂。 成像剂可以包括直接与成像剂结合的靶向剂或借助于接头。 该方法也可以应用于其它非放射性但用作稀释金属或与DOTA强烈结合的其它金属的金属。