发明申请
US20140093450A1 PRETARGETING KIT FOR IMAGING OR THERAPY COMPRISING A TRANS-CYCLOOCTENE DIENOPHILE AND A DIENE
有权
用于成像或治疗包含转运环形胆固醇和二苯胺的预备套件
- 专利标题： PRETARGETING KIT FOR IMAGING OR THERAPY COMPRISING A TRANS-CYCLOOCTENE DIENOPHILE AND A DIENE
- 专利标题（中）： 用于成像或治疗包含转运环形胆固醇和二苯胺的预备套件
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申请号： US14115455申请日： 2012-05-07
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公开(公告)号： US20140093450A1公开(公告)日： 2014-04-03
- 发明人: Marc Stefan Robillard , Johan Lub , Raffaella Rossin , Sandra Martina Van Ben Bosch , Ronny Mathieu Versteegen
- 申请人： Marc Stefan Robillard , Johan Lub , Raffaella Rossin , Sandra Martina Van Ben Bosch , Ronny Mathieu Versteegen
- 申请人地址： NL EINDHOVEN
- 专利权人： KONINKLIJKE PHILIPS N.V.
- 当前专利权人： KONINKLIJKE PHILIPS N.V.
- 当前专利权人地址： NL EINDHOVEN
- 优先权： EP11165267.3 20110509
- 国际申请： PCT/IB2012/052260 WO 20120507
- 主分类号： A61K51/04
- IPC分类号： A61K51/04 ; A61K51/10 ; C07D245/02 ; C07D235/02 ; C07D207/46 ; 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.