公开(公告)号：EP2673257A4

公开(公告)日：2014-11-12

申请号：EP12744282

申请日：2012-02-10

申请人： UNIV WASHINGTON

发明人： SHARMA VIJAY ,  SIVAPACKIAM JOTHILINGAM ,  PIWNICA-WORMS DAVID

IPC分类号： C07C211/49 ,  C05D9/00 ,  C07F5/00

CPC分类号： A61K51/0478 ,  C05D9/02 ,  C07B59/001 ,  C07B59/002 ,  C07C251/24 ,  C07F5/003

摘要： Tracers that can be used for PET or SPECT imaging of the distribution of Pgp are disclosed. The tracers are metalloprobes that can comprise a radioactive metal ion such as 67Ga or 68Ga. Methods of synthesizing the tracers, and methods of imaging heart and other tissues are also disclosed. The tracers can be used to obtain high signal-to-background ratios for imaging tissues in vivo such as heart or tumor tissue. In various embodiments, disclosed tracers can exhibit, a) enhanced first pass extraction into heart tissue compared to presently available probes, b) linearity with true blood flow, c) enhanced detection of myocardial viability compared to presently available probes, d) reduced liver retention compared to presently available probes, and e) more efficient clearance from non-cardiac and adjoining tissues compared to presently available probes.

摘要翻译： 公开了可用于Pgp分布的PET或SPECT成像的示踪剂。 示踪剂是可以包含放射性金属离子如67Ga或68Ga的金属杂酚。 还公开了合成示踪剂的方法，以及心脏和其他组织成像方法。 示踪剂可用于获得体内成像组织（例如心脏或肿瘤组织）的高信噪比。 在各种实施方案中，所公开的示踪剂可以显示a）与目前可用的探针相比，增强的第一次通过提取到心脏组织中，b）具有真实血流的线性，c）与目前可用的探针相比增强了心肌存活力的检测，d） 与目前可用的探针相比，和e）与目前可用的探针相比，非心脏和邻近组织的更有效的清除。