公开(公告)号：WO2012109611A3

公开(公告)日：2012-11-08

申请号：PCT/US2012024752

申请日：2012-02-10

Applicant: UNIV WASHINGTON ,  SHARMA VIJAY ,  SIVAPACKIAM JOTHILINGAM ,  PIWNICA-WORMS DAVID

Inventor： SHARMA VIJAY ,  SIVAPACKIAM JOTHILINGAM ,  PIWNICA-WORMS DAVID

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

CPC classification number: A61K51/0478 ,  C05D9/02 ,  C07B59/001 ,  C07B59/002 ,  C07C251/24 ,  C07F5/003

Abstract: 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.

Abstract translation: 公开了可用于Pgp分布的PET或SPECT成像的示踪剂。 示踪剂是可以包含诸如67Ga或68Ga的放射性金属离子的金属杂酚。 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表现出：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的心肌存活力检测，d） 与目前可用的探针相比，以及e）与目前可用的探针相比，从非心脏和邻近组织更有效的清除。

公开(公告)号：WO2012109611A2

公开(公告)日：2012-08-16

申请号：PCT/US2012/024752

申请日：2012-02-10

Applicant: WASHINGTON UNIVERSITY ,  SHARMA, Vijay ,  SIVAPACKIAM, Jothilingam ,  PIWNICA-WORMS, David

Inventor： SHARMA, Vijay ,  SIVAPACKIAM, Jothilingam ,  PIWNICA-WORMS, David

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

CPC classification number: A61K51/0478 ,  C05D9/02 ,  C07B59/001 ,  C07B59/002 ,  C07C251/24 ,  C07F5/003

Abstract: 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 67 Ga or 68 Ga. 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.

Abstract translation: 可以用于Pgp分布的PET或SPECT成像的示踪剂被公开。 示踪剂是金属探针，其可以包含放射性金属离子如67 Ga或68 Ga。 还公开了合成示踪物的方法以及使心脏和其他组织成像的方法。 示踪剂可用于获得用于体内成像组织（例如心脏或肿瘤组织）的高信号背景比。 在各种实施方案中，公开的示踪剂可以表现出a）与当前可用的探针相比提高到心脏组织中的首过提取，b）与真实血流的线性，c）与目前可用的探针相比，增强的心肌活力检测，d） 与目前可用的探针相比，e）与目前可用的探针相比，非心脏和邻近组织更有效的清除。