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1. 发明申请

WO2009067767A2 TARGETED RADIOTHERAPY 审中-公开
标题翻译：目标放射治疗
公开(公告)号：WO2009067767A2
公开(公告)日：2009-06-04
申请号：PCT/BE2008/000099
申请日：2008-11-26
申请人： KATHOLIEKE UNIVERSITEIT LEUVEN , NI, Yicheng , VAN DE PUTTE, Marie , DE WITTE, Peter , VERBRUGGEN, Alfons , MARCHAL, Guy
发明人： NI, Yicheng , VAN DE PUTTE, Marie , DE WITTE, Peter , VERBRUGGEN, Alfons , MARCHAL, Guy
IPC分类号： A61K51/04 , A61P35/00
CPC分类号： A61K51/04
摘要： The present invention concerns a therapeutically labeled napthodianthrone or phenanthro[1,10,9,8-opqra]perylene-7,14-dione compound, which comprises a chemical element or an isotope that has an unstable nucleus and emits radiation during its decay to a stable form sufficient to destroy neighboring cells or tissues for use in a targeted radiotherapy to enhance curability of a warm-blooded animal that has been subjected to a necrosis-inducing antitumor therapy. A particular advantage of present invention is that viable rim resistant to a necrosis-inducing antitumor therapy such as vascular targeting agent (VTA) can be supplemented by one single or repeated doses of a therapeutically radiolabeled small molecule necrosis-avid chemical compound treatment to enhance the curability. Examples of necrosis inducing therapies are for instance minimally invasive tumor ablations applied chemically by percutaneous injection of ethanol or acetic acid, or physically by cryotherapy, microwave, focused ultrasound, interstitial laser therapy and radio- frequency ablation (RFA); by chemotherapies using cytotoxic agents or vascular targeting agents (VTA); and by external or internal radiotherapies.
摘要翻译：本发明涉及一种治疗上标记的阴蒂龙酮或菲咯啉[1,10,9,8-吖庚因]二萘嵌苯-7,14-二酮化合物，其包含具有不稳定核的化学元素或同位素，并在其衰变期间发射辐射足以破坏用于靶向放射治疗的相邻细胞或组织的稳定形式，以增强已经进行坏死诱导的抗肿瘤治疗的温血动物的固化性。本发明的一个特别优点是可以通过一种单独或重复剂量的治疗性放射性标记的小分子坏死化学化合物治疗来补充对坏死诱导的抗肿瘤治疗如血管靶向剂（VTA）有抗性的活性边缘，以增强固化性。坏死诱导疗法的实例是例如通过经皮注射乙醇或乙酸而化学施用的微创肿瘤消融，或通过冷冻治疗，微波，聚焦超声，间质激光治疗和射频消融（RFA）物理化的微创肿瘤消融。通过使用细胞毒剂或血管靶向剂（VTA）的化疗; 以及外部或内部放射治疗。

2. 发明申请

WO2005009423A1 NECROSIS AVID TRACER AGENT 审中-公开
标题翻译： NECROSIS AVID追踪器代理
公开(公告)号：WO2005009423A1
公开(公告)日：2005-02-03
申请号：PCT/BE2004/000107
申请日：2004-07-23
申请人： K.U.LEUVEN RESEARCH AND DEVELOPMENT , NI, Yicheng , BORMANS, Guy , MARCHAL, Guy , VERBRUGGEN, Alfons
发明人： NI, Yicheng , BORMANS, Guy , MARCHAL, Guy , VERBRUGGEN, Alfons
IPC分类号： A61K31/122
CPC分类号： A61K31/122 , A61K51/0406
摘要： The present invention concerns to the use of phenanthro[1,10,9,8-opqra]perylene-7,14-dione derivatives, and more specifically hypericin or its derivatives, as necrosis or infarct specific agents. The phenanthro[1,10,9,8-opqra]perylene-7,14-dione derivatives can be labeled with a radionuclide, a radiopaque material or a material enhancing the effects magnetic resonance imaging.
摘要翻译：本发明涉及菲咯啉[1,10,9,8-opqra]苝-7,14-二酮衍生物，更具体地涉及金丝桃素或其衍生物作为坏死或梗死特异性试剂的用途。菲咯啉[1,10,9,8-opqra]苝-7,14-二酮衍生物可用放射性核素，不透射线材料或增强磁共振成像效果的材料进行标记。

3. 发明申请

WO2009140743A2 BLOOD IMAGING 审中-公开
标题翻译：血液成像
公开(公告)号：WO2009140743A2
公开(公告)日：2009-11-26
申请号：PCT/BE2009/000027
申请日：2009-05-25
申请人： Katholieke Universiteit Leuven , BORMANS, Guy , VERBRUGGEN, Alfons
发明人： BORMANS, Guy , VERBRUGGEN, Alfons
CPC分类号： A61K51/04 , A61K51/0478 , C07B59/001 , C07B2200/05 , C07C311/29 , C07C311/46 , C07F13/005
摘要： The invention generally relates to the application of imaging techniques, in particular positron emission tomography (PET) or single photon emission tomography (SPECT), in the assessment of physiological parameters in a subject. The compounds of the present invention were shown to be cell membrane permeant and to have a specific binding affinity (or substrate affinity) for the carbonic anhydrases type I and II, and are accordingly useful for the in vivo and in vitro labeling of erythrocytes (RBC). It is accordingly an object of the present invention to provide said novel compounds, in particular the radio labeled variants thereof, and their use in imaging techniques to perform the assessment of physiological parameters, such as blood volume measurements, or blood flow measurements.
摘要翻译：本发明通常涉及成像技术，特别是正电子发射断层摄影（PET）或单光子发射断层摄影（SPECT）在评估受试者生理参数方面的应用。本发明的化合物被证明是细胞膜透膜，并且对于I型和II型碳酸酐酶具有特异性结合亲和力（或底物亲和力），因此可用于红细胞（RBC）的体内和体外标记）。因此，本发明的目的是提供所述新型化合物，特别是其放射性标记的变体，以及它们在成像技术中用于进行诸如血容量测量或血液流量测量的生理参数评估的用途。

4. 发明申请

WO2010105315A2 REPORTER GENE CONSTRUCTS FOR PET 审中-公开
标题翻译：报告基因结构的PET
公开(公告)号：WO2010105315A2
公开(公告)日：2010-09-23
申请号：PCT/BE2010/000022
申请日：2010-03-22
申请人： KATHOLIEKE UNIVERSIFEIT LEUVEN , BAEKELANDT, Veerle , BORMANS, Guy , DEBYSER, Zeger , DEROOSE, Christophe , EVENS, Nele , TOELEN, Jaan , VANDEPUTTE, Caroline , VAN LAERE, Koenraad , VERBRUGGEN, Alfons
发明人： BAEKELANDT, Veerle , BORMANS, Guy , DEBYSER, Zeger , DEROOSE, Christophe , EVENS, Nele , TOELEN, Jaan , VANDEPUTTE, Caroline , VAN LAERE, Koenraad , VERBRUGGEN, Alfons
IPC分类号： C12Q1/68
CPC分类号： C07K14/70571 , A61K51/0455 , A61K51/0463 , C12Q1/6897
摘要： The present invention relates to the field of in vivo molecular imaging and, more particularly to a method for reporter gene imaging via positron emission tomography (PET), which can be applied in nervous system (brain, cerebrum, cerebellum, medulla, pons, spinal cord, sciatic nerve) and particularly in the brain. The present invention also involves type 2 cannabinoid receptor (CB2) based reporter gene constructs and a reporter probe or tracer (reporter system) for use in a molecular imaging therapy for instance by PET. The reporter gene encodes the reporter protein to which the reporter probe binds.
摘要翻译：本发明涉及体内分子成像领域，并且更具体地涉及经由正电子发射断层摄影术（PET）进行报道基因成像的方法，其可以应用于神经系统（脑，大脑），小脑，髓质，脑桥，脊髓，坐骨神经），特别是在大脑中。本发明还涉及基于2型大麻素受体（CB2）的报道基因构建体和报道探针或示踪剂（报道系统），用于例如通过PET的分子成像疗法。报道基因编码报道探针结合的报道蛋白。

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