公开(公告)号：US09913921B2

公开(公告)日：2018-03-13

申请号：US14115455

申请日：2012-05-07

申请人： Marc Stefan Robillard ,  Johan Lub ,  Raffaella Rossin ,  Sandra Martina Van Ben Bosch ,  Ronny Mathieu Versteegen

发明人： Marc Stefan Robillard ,  Johan Lub ,  Raffaella Rossin ,  Sandra Martina Van Ben Bosch ,  Ronny Mathieu Versteegen

IPC分类号： A61K51/10 ,  A61K51/04 ,  B82Y5/00 ,  C07D207/46 ,  C07D235/02 ,  C07D245/02 ,  C07D249/16 ,  A61K47/68 ,  A61K49/10

CPC分类号： A61K51/1093 ,  A61K47/6897 ,  A61K49/106 ,  A61K51/041 ,  A61K51/0495 ,  A61K51/0497 ,  B82Y5/00 ,  C07D207/46 ,  C07D235/02 ,  C07D245/02 ,  C07D249/16

摘要： Described is a pretargeting method, and related kits, for targeted medical imaging and/or therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention involves the use of [4+2] inverse electron demand (retro) Diels-Alder chemistry in providing the coupling between a Pre-targeting Probe and an Effector Probe. To this end one of these probes comprises an electron-deficient tetrazine or other suitable diene, and the other an E-cyclooctene which has a flattened structure as a result of the position of at least two exocyclic bonds.

公开(公告)号：US20140093450A1

公开(公告)日：2014-04-03

申请号：US14115455

申请日：2012-05-07

申请人： Marc Stefan Robillard ,  Johan Lub ,  Raffaella Rossin ,  Sandra Martina Van Ben Bosch ,  Ronny Mathieu Versteegen

发明人： Marc Stefan Robillard ,  Johan Lub ,  Raffaella Rossin ,  Sandra Martina Van Ben Bosch ,  Ronny Mathieu Versteegen

IPC分类号： A61K51/04 ,  A61K51/10 ,  C07D245/02 ,  C07D235/02 ,  C07D207/46 ,  C07D249/16

CPC分类号： A61K51/1093 ,  A61K47/6897 ,  A61K49/106 ,  A61K51/041 ,  A61K51/0495 ,  A61K51/0497 ,  B82Y5/00 ,  C07D207/46 ,  C07D235/02 ,  C07D245/02 ,  C07D249/16

摘要： Described is a pretargeting method, and related kits, for targeted medical imaging and/or therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention involves the use of [4+2] inverse electron demand (retro) Diels-Alder chemistry in providing the coupling between a Pre-targeting Probe and an Effector Probe. To this end one of these probes comprises an electron-deficient tetrazine or other suitable diene, and the other an E-cyclooctene which has a flattened structure as a result of the position of at least two exocyclic bonds.

摘要翻译： 描述了用于靶向医学成像和/或治疗剂的预靶向方法和相关试剂盒，其中使用对彼此显示出生物正交反应性的非生物反应性化学基团。 本发明涉及使用[4 + 2]反电子需求（复古）Diels-Alder化学来提供预瞄准探针和效应探针之间的耦合。 为此目的，这些探针中的一个包括电子缺乏四嗪或其它合适的二烯，另一个是由于至少两个环外键的位置而具有扁平结构的E-环辛烯。