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1.发明授权Small technetium-99m and rhenium labeled agents and methods for imaging tumors 失效小锝-99m和铼标记的药剂和肿瘤成像方法公开(公告)号：US07321027B2
公开(公告)日：2008-01-22
申请号：US10279214
申请日：2002-10-23
IPC分类号： C07F13/00
CPC分类号： C07D295/13 , A61K51/0478 , C07C323/41 , C07F13/005 , C07K5/06026
摘要： The present invention relates to compounds and related technetium and rhenium complexes thereof which are suitable for imaging or therapeutic treatment of tumors, e.g., carcinomas, melanomas and other tumors. In another embodiment, the invention relates to methods of imaging tumors using radiolabeled metal complexes. Preferred radiolabeled complexes for imaging tumors include technetium and rhenium complexes. The high tumor uptake and significant tumor/nontumor ratios of the technetium complexes of the invention indicate that such small technetium-99m-based molecular probes can be developed as in-vivo diagnostic agents for melanoma and its metastases. In yet another embodiment, the invention relates to methods of treatment of tumors using a radiolabeled metal complex as a radiopharmaceutical agent to treat the tumor.
摘要翻译： 本发明涉及适用于肿瘤例如癌，黑素瘤和其他肿瘤的成像或治疗性治疗的化合物及其相关的锝和铼络合物。 在另一个实施方案中，本发明涉及使用放射性标记的金属络合物成像肿瘤的方法。 用于成像肿瘤的优选放射性标记复合物包括锝和铼络合物。 本发明的锝络合物的高肿瘤摄取和显着的肿瘤/非肿瘤比率表明，这种基于锝-99m的小分子探针可以作为黑色素瘤及其转移的体内诊断剂开发。 在另一个实施方案中，本发明涉及使用放射性标记的金属络合物作为放射性药物治疗肿瘤的方法治疗肿瘤。
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2.发明申请SMALL TECHNETIUM-99M AND RHENIUM LABELED AGENTS AND METHODS FOR IMAGING TUMORS 审中-公开小技术-99M和氙标签代理和成像肿瘤的方法公开(公告)号：US20080226550A1
公开(公告)日：2008-09-18
申请号：US12017328
申请日：2008-01-21
IPC分类号： A61K51/04 , C07F5/00 , C07D211/00 , A61P35/00 , C07D295/00
CPC分类号： C07D295/13 , A61K51/0478 , C07C323/41 , C07F13/005 , C07K5/06026
摘要： The present invention relates to compounds and related technetium and rhenium complexes thereof which are suitable for imaging or therapeutic treatment of tumors, e.g., carcinomas, melanomas and other tumors. In another embodiment, the invention relates to methods of imaging tumors using radiolabeled metal complexes. Preferred radiolabeled complexes for imaging tumors include technetium and rhenium complexes. The high tumor uptake and significant tumor/nontumor ratios of the technetium complexes of the invention indicate that such small technetium-99m-based molecular probes can be developed as in-vivo diagnostic agents for melanoma and its metastases. In yet another embodiment, the invention relates to methods of treatment of tumors using a radiolabeled metal complex as a radiopharmaceutical agent to treat the tumor.
摘要翻译： 本发明涉及适用于肿瘤例如癌，黑素瘤和其他肿瘤的成像或治疗性治疗的化合物及其相关的锝和铼络合物。 在另一个实施方案中，本发明涉及使用放射性标记的金属络合物成像肿瘤的方法。 用于成像肿瘤的优选放射性标记复合物包括锝和铼络合物。 本发明的锝络合物的高肿瘤摄取和显着的肿瘤/非肿瘤比率表明，这种基于锝-99m的小分子探针可以作为黑色素瘤及其转移的体内诊断剂开发。 在另一个实施方案中，本发明涉及使用放射性标记的金属络合物作为放射性药物治疗肿瘤的方法治疗肿瘤。
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公开(公告)号：US06171576B2
公开(公告)日：2001-01-09
申请号：US08552584
申请日：1995-11-03
申请人： Peter C. Meltzer , Bertha K. Madras , Alan Davison , Paul Blundell , Ashfaq Mahmood , Alun G. Jones
发明人： Peter C. Meltzer , Bertha K. Madras , Alan Davison , Paul Blundell , Ashfaq Mahmood , Alun G. Jones
IPC分类号： A61K5100
CPC分类号： A61K51/0448 , A61K2123/00 , C07C69/753 , C07C2602/44 , C07D451/02
摘要： Radiopharmaceutical compounds are disclosed. A tropane compound is linked through the N atom at the 8-position to a chelating ligand capable of complexing technetium or rhenium to produce a neutral labeled complex that selectively binds to the dopamine transporter. These compounds can be prepared as separate diastereoisomers as well as a mixture of diastereoisomers. Also disclosed are radiopharmaceutical kits for preparing the labeled radiopharmaceutical compounds.
摘要翻译： 公开了放射性药物化合物。 托烷化合物通过8位的N原子连接到能够络合锝或铼的螯合配体以产生选择性结合多巴胺转运蛋白的中性标记复合物。 这些化合物可以制备成单独的非对映异构体以及非对映异构体的混合物。 还公开了用于制备标记的放射性药物化合物的放射性药物试剂盒。
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公开(公告)号：US08747810B2
公开(公告)日：2014-06-10
申请号：US13325051
申请日：2011-12-13
CPC分类号： A61K49/0002 , A61K51/02 , A61K51/04 , A61K51/0478 , A61K2123/00 , C07C323/41 , C07C2602/10 , C07D211/14 , C07D211/22 , C07D213/36 , C07D333/20 , C07D401/12 , C07F13/005
摘要： The present invention relates to compounds and related technetium and rhenium complexes thereof which are suitable for imaging or therapeutic treatment of tissues, organs, or tumors. In another embodiment, the invention relates to methods of imaging tissues, organs, or tumors using radiolabeled metal complexes, particularly tissues, organs, or tumors which express certain receptors to which the compounds or complexes of the invention have an affinity. The present invention also relates to methods of treating cancer, particularly those cancer lines which express certain receptors to which the compounds or complexes of the invention have an affinity. In yet another embodiment, the present invention provides methods of imaging and/or inhibiting receptors or neuroreceptors using compounds or complexes of the invention which have an affinity for the receptor or neuroreceptor to be imaged and/or inhibited.
摘要翻译： 本发明涉及适用于组织，器官或肿瘤的成像或治疗性治疗的化合物及其相关锝和铼络合物。 在另一个实施方案中，本发明涉及使用放射性标记的金属络合物，特别是表达本发明的化合物或复合物具有亲和力的某些受体的组织，器官或肿瘤来成像组织，器官或肿瘤的方法。 本发明还涉及治疗癌症的方法，特别是那些表达本发明化合物或复合物具有亲和力的某些受体的那些癌症系。 在另一个实施方案中，本发明提供使用对受体或神经受体成像和/或抑制的亲和力的本发明化合物或复合物成像和/或抑制受体或神经受体的方法。
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公开(公告)号：US20120269724A1
公开(公告)日：2012-10-25
申请号：US13325051
申请日：2011-12-13
IPC分类号： A61K51/04 , C07D213/36 , C07D401/12 , C07C215/50 , C07D295/13 , C07D211/14 , C07F13/00 , C07D333/20 , C07D409/12 , C07C323/60 , G01N33/60 , C07D211/22
CPC分类号： A61K49/0002 , A61K51/02 , A61K51/04 , A61K51/0478 , A61K2123/00 , C07C323/41 , C07C2602/10 , C07D211/14 , C07D211/22 , C07D213/36 , C07D333/20 , C07D401/12 , C07F13/005
摘要： The present invention relates to compounds and related technetium and rhenium complexes thereof which are suitable for imaging or therapeutic treatment of tissues, organs, or tumors. In another embodiment, the invention relates to methods of imaging tissues, organs, or tumors using radiolabeled metal complexes, particularly tissues, organs, or tumors which express certain receptors to which the compounds or complexes of the invention have an affinity. The present invention also relates to methods of treating cancer, particularly those cancer lines which express certain receptors to which the compounds or complexes of the invention have an affinity. In yet another embodiment, the present invention provides methods of imaging and/or inhibiting receptors or neuroreceptors using compounds or complexes of the invention which have an affinity for the receptor or neuroreceptor to be imaged and/or inhibited.
摘要翻译： 本发明涉及适用于组织，器官或肿瘤的成像或治疗性治疗的化合物及其相关锝和铼络合物。 在另一个实施方案中，本发明涉及使用放射性标记的金属络合物，特别是表达本发明的化合物或复合物具有亲和力的某些受体的组织，器官或肿瘤来成像组织，器官或肿瘤的方法。 本发明还涉及治疗癌症的方法，特别是那些表达本发明化合物或复合物具有亲和力的某些受体的那些癌症系。 在另一个实施方案中，本发明提供使用对受体或神经受体成像和/或抑制的亲和力的本发明化合物或复合物成像和/或抑制受体或神经受体的方法。
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公开(公告)号：US06548041B1
公开(公告)日：2003-04-15
申请号：US09568106
申请日：2000-05-10
申请人： Peter C. Meltzer , Paul Blundell , Bertha K. Madras , Alan J. Fischman , Alun G. Jones , Ashfaq Mahmood
发明人： Peter C. Meltzer , Paul Blundell , Bertha K. Madras , Alan J. Fischman , Alun G. Jones , Ashfaq Mahmood
IPC分类号： A61K5100
CPC分类号： A61K31/46 , A61B6/506 , A61K51/0448 , A61K51/0478 , A61K51/0497 , C07D451/02 , C07F13/005
摘要： Radiopharmaceutical compounds are disclosed. A tropane compound is linked through the N atom at the 8-position to a chelating ligand capable of complexing technetium or rhenium to produce a neutral labeled complex that selectively binds to the dopamine transporter over the serotonin transporter with a ratio of 10 or more. These compounds can be prepared as separate diastereoisomers as well as a mixture of diastereoisomers. Also disclosed are radiopharmaceutical kits for preparing the labeled radiopharmaceutical compounds.
摘要翻译： 公开了放射性药物化合物。 托烷化合物通过8-位的N原子连接到能够络合锝或铼的螯合配体，以产生中性标记的复合物，其以比例为10或更高的比例选择性地结合血清素转运蛋白上的多巴胺转运蛋白。 这些化合物可以制备成单独的非对映异构体以及非对映异构体的混合物。 还公开了用于制备标记的放射性药物化合物的放射性药物试剂盒。
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7.发明申请Small technetium-99m and rhenium labeled agents and methods for imaging tissues, organs and tumors 审中-公开小锝-99m和铼标记的试剂和成像组织，器官和肿瘤的方法公开(公告)号：US20060159617A1
公开(公告)日：2006-07-20
申请号：US10534225
申请日：2003-11-08
申请人： Ashfaq Mahmood , Zhen Cheng , Alun Jones , Alan Davison
发明人： Ashfaq Mahmood , Zhen Cheng , Alun Jones , Alan Davison
IPC分类号： A61K51/00 , C07F13/00 , C07F5/00 , C07D211/26
CPC分类号： C07C323/41 , A61K51/0455 , A61K51/0478 , C07C323/25 , C07D211/14 , C07D211/52 , C07D211/58 , C07F13/005
摘要： The present invention relates to compounds and related technetium and rhenium complexes thereof which are suitable for imaging or therapeutic treatment of tissues, organs, or tumors. In another embodiment, the invention relates the methods of imaging tissues, organs or tumors using radiolabeled metal complexes, particularly tissues, organs, or tumors which express certain receptors to which the compounds or complexes of the invention have an affinity. The present invention also relates to methods of treating cancer, particularly those cancer lines which express certain receptors to which the compounds or complexes of the invention have an affinity. In yet another embodiment, the present invention provides methods of imaging and/or inhibiting receptors or neuroreceptors using compounds or complexes of the invention which have an affinity for the receptor or neuroreceptor to be imaged and/or inhibited.
摘要翻译： 本发明涉及适用于组织，器官或肿瘤的成像或治疗性治疗的化合物及其相关锝和铼络合物。 在另一个实施方案中，本发明涉及使用放射性标记的金属络合物，特别是表达本发明的化合物或复合物具有亲和力的某些受体的组织，器官或肿瘤来成像组织，器官或肿瘤的方法。 本发明还涉及治疗癌症的方法，特别是那些表达本发明化合物或复合物具有亲和力的某些受体的那些癌症系。 在另一个实施方案中，本发明提供使用对受体或神经受体成像和/或抑制的亲和力的本发明化合物或复合物成像和/或抑制受体或神经受体的方法。
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公开(公告)号：US20070009432A1
公开(公告)日：2007-01-11
申请号：US11517676
申请日：2006-09-08
申请人： Peter Meltzer , Paul Blundell , Bertha Madras , Alan Fischman , Alun Jones , Ashfaq Mahmood
发明人： Peter Meltzer , Paul Blundell , Bertha Madras , Alan Fischman , Alun Jones , Ashfaq Mahmood
IPC分类号： A61K51/00 , C07F13/00 , C07D451/02
CPC分类号： A61K31/46 , A61B6/506 , A61K51/0448 , A61K51/0478 , A61K51/0497 , C07D451/02 , C07F13/005
摘要： Radiopharmaceutical compounds are disclosed. A tropane compound is linked through the N atom at the 8-position to a chelating ligand capable of complexing technetium or rhenium to produce a neutral labeled complex that selectively binds to the dopamine transporter over the serotonin transporter with a ratio of 10 or more. These compounds can be prepared as separate diastereoisomers as well as a mixture of diastereoisomers. Also disclosed are radiopharmaceutical kits for preparing the labeled radiopharmaceutical compounds.
摘要翻译： 公开了放射性药物化合物。 托烷化合物通过8-位的N原子连接到能够络合锝或铼的螯合配体，以产生中性标记的复合物，其以比例为10或更高的比例选择性地结合血清素转运蛋白上的多巴胺转运蛋白。 这些化合物可以制备成单独的非对映异构体以及非对映异构体的混合物。 还公开了用于制备标记的放射性药物化合物的放射性药物试剂盒。
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