公开(公告)号：US20080226550A1

公开(公告)日：2008-09-18

申请号：US12017328

申请日：2008-01-21

Applicant: Ashfaq Mahmood ,  Matthias Friebe ,  Cristina Bolzati ,  Alun G. Jones ,  Alan Davison

Inventor： Ashfaq Mahmood ,  Matthias Friebe ,  Cristina Bolzati ,  Alun G. Jones ,  Alan Davison

IPC: A61K51/04 ,  C07F5/00 ,  C07D211/00 ,  A61P35/00 ,  C07D295/00

CPC classification number: C07D295/13 ,  A61K51/0478 ,  C07C323/41 ,  C07F13/005 ,  C07K5/06026

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20070009432A1

公开(公告)日：2007-01-11

申请号：US11517676

申请日：2006-09-08

Applicant: Peter Meltzer ,  Paul Blundell ,  Bertha Madras ,  Alan Fischman ,  Alun Jones ,  Ashfaq Mahmood

Inventor： Peter Meltzer ,  Paul Blundell ,  Bertha Madras ,  Alan Fischman ,  Alun Jones ,  Ashfaq Mahmood

IPC: A61K51/00 ,  C07F13/00 ,  C07D451/02

CPC classification number: A61K31/46 ,  A61B6/506 ,  A61K51/0448 ,  A61K51/0478 ,  A61K51/0497 ,  C07D451/02 ,  C07F13/005

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US06548041B1

公开(公告)日：2003-04-15

申请号：US09568106

申请日：2000-05-10

Applicant: Peter C. Meltzer ,  Paul Blundell ,  Bertha K. Madras ,  Alan J. Fischman ,  Alun G. Jones ,  Ashfaq Mahmood

Inventor： Peter C. Meltzer ,  Paul Blundell ,  Bertha K. Madras ,  Alan J. Fischman ,  Alun G. Jones ,  Ashfaq Mahmood

IPC: A61K5100

CPC classification number: A61K31/46 ,  A61B6/506 ,  A61K51/0448 ,  A61K51/0478 ,  A61K51/0497 ,  C07D451/02 ,  C07F13/005

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20060159617A1

公开(公告)日：2006-07-20

申请号：US10534225

申请日：2003-11-08

Applicant: Ashfaq Mahmood ,  Zhen Cheng ,  Alun Jones ,  Alan Davison

Inventor： Ashfaq Mahmood ,  Zhen Cheng ,  Alun Jones ,  Alan Davison

IPC: A61K51/00 ,  C07F13/00 ,  C07F5/00 ,  C07D211/26

CPC classification number: C07C323/41 ,  A61K51/0455 ,  A61K51/0478 ,  C07C323/25 ,  C07D211/14 ,  C07D211/52 ,  C07D211/58 ,  C07F13/005

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US08747810B2

公开(公告)日：2014-06-10

申请号：US13325051

申请日：2011-12-13

Applicant: Ashfaq Mahmood ,  Alun G. Jones ,  Naengnoi Limpa-Amara ,  Yijie Peng ,  Zeynep Akgun

Inventor： Ashfaq Mahmood ,  Alun G. Jones ,  Naengnoi Limpa-Amara ,  Yijie Peng ,  Zeynep Akgun

IPC: A61K49/00 ,  A61K51/04 ,  A61K51/02

CPC classification number: 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

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20120269724A1

公开(公告)日：2012-10-25

申请号：US13325051

申请日：2011-12-13

Applicant: Ashfaq Mahmood ,  Alun G. Jones ,  Naengnoi Limpa-Amara ,  Yijie Peng ,  Zeynep Akgun

Inventor： Ashfaq Mahmood ,  Alun G. Jones ,  Naengnoi Limpa-Amara ,  Yijie Peng ,  Zeynep Akgun

IPC: 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 classification number: 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

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US07321027B2

公开(公告)日：2008-01-22

申请号：US10279214

申请日：2002-10-23

Applicant: Ashfaq Mahmood ,  Matthias Friebe ,  Cristina Bolzati ,  Alun G. Jones ,  Alan Davison

Inventor： Ashfaq Mahmood ,  Matthias Friebe ,  Cristina Bolzati ,  Alun G. Jones ,  Alan Davison

IPC: C07F13/00

CPC classification number: C07D295/13 ,  A61K51/0478 ,  C07C323/41 ,  C07F13/005 ,  C07K5/06026

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US07177822B2

公开(公告)日：2007-02-13

申请号：US09923646

申请日：2001-08-07

Applicant: Syed Ashfaq Mahmood ,  Susan I Stallard ,  Richard W Everett

Inventor： Syed Ashfaq Mahmood ,  Susan I Stallard ,  Richard W Everett

IPC: G06F17/30

CPC classification number: G06Q30/02 ,  G06Q30/0204

Abstract: A marketing system with a centralized database for compiling and distributing marketing data. The system compiles marketing data from a plurality of internal and external data sources into a centralized database. Internal and external sources include legacy systems. Data in the centralized database is distributed to a plurality of client venues by using an extract engine to extract a subset of data from the centralized database and creating a venue specific database. Access to the venue specific database is facilitated by use of a application programmers interface for allowing the development of applications for venue specific use of the venue specific database. Both the compilation and distribution process is performed on a periodic basis to provide timely, accurate, and consistent marketing data across the plurality of client venues.

Abstract translation: 具有集中数据库的营销系统，用于编制和分发营销数据。 该系统将来自多个内部和外部数据源的营销数据编译为集中式数据库。 内部和外部来源包括遗留系统。 集中式数据库中的数据通过使用提取引擎从集中式数据库提取数据子集并创建场地特定数据库来分发到多个客户场所。 通过使用应用程序员界面来促进访问特定于场地的数据库，以允许开发针对场地特定数据库的场地特定使用的应用。 编译和分发过程都是定期进行的，以便在多个客户场所提供及时，准确和一致的营销数据。

公开(公告)号：US06171576B2

公开(公告)日：2001-01-09

申请号：US08552584

申请日：1995-11-03

Applicant: Peter C. Meltzer ,  Bertha K. Madras ,  Alan Davison ,  Paul Blundell ,  Ashfaq Mahmood ,  Alun G. Jones

Inventor： Peter C. Meltzer ,  Bertha K. Madras ,  Alan Davison ,  Paul Blundell ,  Ashfaq Mahmood ,  Alun G. Jones

IPC: A61K5100

CPC classification number: A61K51/0448 ,  A61K2123/00 ,  C07C69/753 ,  C07C2602/44 ,  C07D451/02

Abstract: 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.

Abstract translation: 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。