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1. 发明申请

WO2009140743A3 BLOOD IMAGING 审中-公开
标题翻译：血液成像
公开(公告)号：WO2009140743A3
公开(公告)日：2010-06-24
申请号：PCT/BE2009000027
申请日：2009-05-25
申请人： UNIV LEUVEN KATH , BORMANS GUY , VERBRUGGEN ALFONS
发明人： BORMANS GUY , VERBRUGGEN ALFONS
IPC分类号： A61K51/04 , C07C311/37 , C07F1/08 , C07F5/00 , C07F13/00
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。

2. 发明申请

WO2012062752A1 RADIOLABELLED mGLuR2 PET LIGANDS 审中-公开
标题翻译： RADIOLABELLED mGLuR2 PET配方
公开(公告)号：WO2012062752A1
公开(公告)日：2012-05-18
申请号：PCT/EP2011/069643
申请日：2011-11-08
申请人： JANSSEN PHARMACEUTICALS, INC. , ANDRÉS-GIL, José, Ignacio , ALCÁZAR-VACA, Manuel, Jesús , CID-NÚÑEZ, José, Maria , TRABANCO-SUÁREZ, Andrés, Avelino , BORMANS, Guy, Maurits R. , CELEN, Sofie, Jeanne, Leopoldine , KOOLE, Michel
发明人： ANDRÉS-GIL, José, Ignacio , ALCÁZAR-VACA, Manuel, Jesús , CID-NÚÑEZ, José, Maria , TRABANCO-SUÁREZ, Andrés, Avelino , BORMANS, Guy, Maurits R. , CELEN, Sofie, Jeanne, Leopoldine , KOOLE, Michel
IPC分类号： C07D471/04
CPC分类号： A61K51/0455 , C07B59/002 , C07D471/04 , G01N33/60
摘要： The present invention relates to novel, selective, radiolabelled mGluR2 ligands which are useful for imaging and quantifying the metabotropic glutamate receptor mGluR2 in tissues, using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging a tissue, cells or a host, in vitro or in vivo and to precursors of said compounds.
摘要翻译：本发明涉及可用于使用正电子发射断层扫描（PET）在组织中成像和定量代谢型谷氨酸受体mGluR2的新型选择性放射性标记的mGluR2配体。本发明还涉及包含这些化合物的组合物，用于制备此类化合物和组合物的方法，以使用这些化合物和组合物用于在体外或体内成像组织，细胞或宿主以及所述化合物的前体。

3. 发明申请

WO2013000924A1 1-ARYL-4-METHYL-[1,2,4]TRIAZOLO[4,3-a]QUINOXALINE DERIVATIVES 审中-公开
标题翻译： 1-芳基-4-甲基 - [1,2,4]三唑并[4,3-a]喹啉衍生物
公开(公告)号：WO2013000924A1
公开(公告)日：2013-01-03
申请号：PCT/EP2012/062381
申请日：2012-06-26
申请人： JANSSEN PHARMACEUTICA NV , ANDRÉS-GIL, José, Ignacio , ROMBOUTS, Frederik, Jan, Rita , TRABANCO-SUÁREZ, Andrés, Avelino , VANHOOF, Greta, Constantia, Peter , DE ANGELIS, Meri , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , GUILLEMONT, Jerôme, Emile, Georges , BORMANS, Guy, Maurits R. , CELEN, Sofie, Jeanne, Leopoldine , VLIEGEN, Maarten
发明人： ANDRÉS-GIL, José, Ignacio , ROMBOUTS, Frederik, Jan, Rita , TRABANCO-SUÁREZ, Andrés, Avelino , VANHOOF, Greta, Constantia, Peter , DE ANGELIS, Meri , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , GUILLEMONT, Jerôme, Emile, Georges , BORMANS, Guy, Maurits R. , CELEN, Sofie, Jeanne, Leopoldine , VLIEGEN, Maarten
IPC分类号： C07D487/04 , A61K31/4985 , A61P25/00
CPC分类号： C07D487/04 , A61K31/4985 , A61K45/06 , A61K51/0463 , G01N33/60
摘要： The present invention relates to novel l-aryl-4-methyl-[l,2,4]triazolo[4,3-a]- quinoxaline derivatives as inhibitors of phosphodiesterase 2 (PDE2) and to a lesser extent of phosphodiesterase 10 (PDE10) or as inhibitors of both, phosphodiesterases 2 and 10. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which PDE2 is involved, or disorders in which both PDE2 and PDE10 are involved, such as neurological and psychiatric disorders, and endocrinological or metabolic diseases. The present invention also relates to radiolabeled compounds which may be useful for imaging and quantifying the PDE2 enzyme in tissues, using positron- emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging a tissue, cells or a host, in vitro or in vivo and to precursors of said compounds.
摘要翻译：本发明涉及新的1-芳基-4-甲基 - [1,2,4]三唑并[4,3-a] - 喹喔啉衍生物作为磷酸二酯酶2（PDE2）的抑制剂，而较少程度的磷酸二酯酶10（PDE10 ）或作为磷酸二酯酶2和10两者的抑制剂。本发明还涉及包含这些化合物的药物组合物，制备此类化合物和组合物的方法，以及用于预防和治疗疾病的化合物和组合物其中涉及PDE2，或PDE2和PDE10都涉及的疾病，如神经和精神疾病，以及内分泌或代谢疾病。本发明还涉及放射性标记的化合物，其可用于使用正电子发射断层摄影（PET）在组织中成像和定量PDE2酶。本发明还涉及包含这些化合物的组合物，用于制备此类化合物和组合物的方法，以使用这些化合物和组合物用于在体外或体内成像组织，细胞或宿主以及所述化合物的前体。

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。

5. 发明申请

WO2011051324A1 RADIOLABELLED PDE10 LIGANDS 审中-公开
标题翻译： RADIOLABELLED PDE10配对
公开(公告)号：WO2011051324A1
公开(公告)日：2011-05-05
申请号：PCT/EP2010/066237
申请日：2010-10-27
申请人： JANSSEN PHARMACEUTICA NV , ANDRÉS-GIL, José, Ignacio , DE ANGELIS, Meri , BORMANS, Guy, Maurits, R. , CELEN, Sofie, Jeanne, Leopoldine
发明人： ANDRÉS-GIL, José, Ignacio , DE ANGELIS, Meri , BORMANS, Guy, Maurits, R. , CELEN, Sofie, Jeanne, Leopoldine
IPC分类号： A61K51/04 , C07D401/14
CPC分类号： C07D401/14 , A61K51/0455
摘要： The present invention relates to novel, selective, radio labelled PDE10 ligands which are useful for imaging and quantifying the PDE10A enzyme in tissues, using positron- emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for imaging a tissue, cells or a host, in vitro or in vivo.
摘要翻译：本发明涉及可用于使用正电子发射断层摄影（PET）在组织中成像和定量PDE10A酶的新型选择性放射性标记的PDE10配体。本发明还涉及包含这些化合物的组合物，制备此类化合物和组合物的方法，以及用于在体外或体内成像组织，细胞或宿主的这些化合物和组合物的用途。

6. 发明申请

WO2010105315A3 REPORTER GENE CONSTRUCTS FOR PET 审中-公开
标题翻译：报告基因构建PET
公开(公告)号：WO2010105315A3
公开(公告)日：2010-11-18
申请号：PCT/BE2010000022
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： C07K14/705 , 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，更具体地说，涉及通过正电子发射断层摄影（PET）的报告基因成像方法，其可应用于神经系统（脑，大脑，小脑，髓质，脑脊髓，脊髓）绳，坐骨神经），特别是在脑中。本发明还涉及基于2型大麻素受体（CB2）的报告基因构建体和用于例如PET的分子成像治疗的报道探针或示踪剂（报道系统）。报告基因编码报告基因探针结合的报道蛋白。

7. 发明申请

WO2010097367A1 RADIOLABELLED PDE10 LIGANDS 审中-公开
标题翻译： RADIOLABELLED PDE10配对
公开(公告)号：WO2010097367A1
公开(公告)日：2010-09-02
申请号：PCT/EP2010/052214
申请日：2010-02-22
申请人： JANSSEN PHARMACEUTICA NV , ANDRÉS-GIL, José, Ignacio , BORMANS, Guy, Maurits R. , DE ANGELIS, Meri , CELEN, Sofie, Jeanne, Leopoldine
发明人： ANDRÉS-GIL, José, Ignacio , BORMANS, Guy, Maurits R. , DE ANGELIS, Meri , CELEN, Sofie, Jeanne, Leopoldine
IPC分类号： A61K51/04 , C07D401/14 , G01N33/60 , A61K101/02
CPC分类号： C07D401/14 , A61K51/0455 , G01N2333/916
摘要： The present invention relates to novel, selective, radiolabeled PDE10 ligands which are useful for imaging and quantifying the PDE10A enzyme in tissues using positron- emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for imaging a tissue, cells or a host, in vitro or in vivo.
摘要翻译：本发明涉及可用于使用正电子发射断层扫描（PET）在组织中成像和定量PDE10A酶的新型选择性放射性标记的PDE10配体。本发明还涉及包含这些化合物的组合物，制备此类化合物和组合物的方法，以及用于在体外或体内成像组织，细胞或宿主的这些化合物和组合物的用途。

8. 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。

9. 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。

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