公开(公告)号：EP1493744B1

公开(公告)日：2009-11-25

申请号：EP04018348.5

申请日：1998-07-10

申请人： ORGANIX, INC. ,  President and Fellows of Harvard College ,  Meltzer, Peter C.

发明人： Madras, Bertha K. ,  Blundell, Paul ,  Chen, Zhengming ,  Meltzer, Peter C.

IPC分类号： C07D451/02 ,  C07D311/00 ,  C07C255/00 ,  C07C69/74 ,  C07C233/00 ,  C07C205/00 ,  C07C49/115 ,  C07C49/105 ,  C07C41/00 ,  C07C33/34 ,  C07D493/08 ,  C07F7/22 ,  A61K31/46 ,  A61K31/35 ,  A61P25/30

CPC分类号： C07D451/02 ,  A61K31/18 ,  A61K31/198 ,  A61K31/405 ,  A61K38/00 ,  A61K51/0448 ,  A61K2123/00 ,  C07C69/753 ,  C07C2602/44 ,  C07D451/06 ,  C07D471/08 ,  C07D493/08

公开(公告)号：EP1493744A1

公开(公告)日：2005-01-05

申请号：EP04018348.5

申请日：1998-07-10

申请人： ORGANIX, INC. ,  PRESIDENT AND FELLOWS OF HARVARD COLLEGE ,  Meltzer, Peter C.

发明人： Madras, Bertha K. ,  Blundell, Paul ,  Chen, Zhengming ,  Meltzer, Peter C.

IPC分类号： C07D451/02 ,  C07D311/00 ,  C07C255/00 ,  C07C69/74 ,  C07C233/00 ,  C07C205/00 ,  C07C49/115 ,  C07C49/105 ,  C07C41/00 ,  C07C33/34 ,  C07D493/08 ,  C07F7/22 ,  A61K31/46 ,  A61K31/35 ,  A61P25/30

CPC分类号： C07D451/02 ,  A61K31/18 ,  A61K31/198 ,  A61K31/405 ,  A61K38/00 ,  A61K51/0448 ,  A61K2123/00 ,  C07C69/753 ,  C07C2602/44 ,  C07D451/06 ,  C07D471/08 ,  C07D493/08

摘要： New tropane analogs that bind to monoamine transporters are described, particularly, 8-thio and 8-oxy tropanes, and especially those having 6- or 7-substituents. The compounds of the present invention can be racemic, pure R-enantiomers, or pure S-enantiomers. Certain preferred compounds of the present invention have a high selectivity for the DAT versus the SERT. Also described are pharmaceutical therapeutic compositions comprising the compounds formulated in a pharmaceutically acceptable carrier and a method for inhibiting 5-hydroxytryptamine reuptake of a monoamine transporter by contacting the monoamine transporter with a 5-hydroxytryptamine reuptake inhibiting amount of a compound of the present invention. Preferred monoamine transporters for the practice of the present invention include the dopamine transporter, the serotonin transporter and the norepinephrine transporter.

摘要翻译： 本发明涉及结合SERT以治疗神经精神障碍的非胺托烷类似物的治疗用途。

公开(公告)号：EP1518561A3

公开(公告)日：2005-04-06

申请号：EP04026679.3

申请日：1999-10-21

申请人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE ,  ORGANIX, INC. ,  THE GENERAL HOSPITAL CORPORATION

发明人： Meltzer, Peter C. ,  Blundell, Paul ,  Madras, Bertha K. ,  Fischman, Alan J. ,  Jones, Alun G. ,  Mahmmod, Ashfaq

IPC分类号： A61K51/04

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。 莨菪烷化合物通过8位的N原子连接至能够络合锝或铼的螯合配体，以产生中性标记复合物，其以10或更高的比率选择性结合至5-羟色胺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：EP1518562A3

公开(公告)日：2005-04-06

申请号：EP04026685.0

申请日：1999-10-21

申请人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE ,  ORGANIX, INC. ,  THE GENERAL HOSPITAL CORPORATION

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

IPC分类号： A61K51/04

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.

公开(公告)号：EP1081147A2

公开(公告)日：2001-03-07

申请号：EP00123641.3

申请日：1994-10-24

申请人： THE GENERAL HOSPITAL CORPORATION ,  THE PRESIDENT AND FELLOWS OF HARVARD COLLEGE ,  ORGANIX, INC. ,  NORTHEASTERN UNIVERSITY

发明人： Elmaleh, David R. ,  Madras, Bertha K. ,  Meltzer, Peter ,  Hanson, Robert N.

IPC分类号： C07D451/02 ,  A61K51/02 ,  A61K31/41 ,  A61K101/02 ,  A61P25/16

CPC分类号： A61K51/0448 ,  A61K2123/00 ,  C07D451/02

摘要： Disclosed are certain cocaine analogs useful for imaging of cocaine receptors and dopamine receptors. Also disclosed are analogs useful for imaging diagnostics for Parkinson's disease.

摘要翻译： 公开了可用于成像可卡因受体和多巴胺受体的某些可卡因类似物。 还公开了可用于帕金森病成像诊断的类似物。

公开(公告)号：EP1051980B1

公开(公告)日：2010-12-15

申请号：EP99121068.3

申请日：1999-10-21

申请人： President and Fellows of Harvard College ,  ORGANIX, INC. ,  THE GENERAL HOSPITAL CORPORATION

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

IPC分类号： A61K51/04

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

公开(公告)号：EP1051980A3

公开(公告)日：2002-05-22

申请号：EP99121068.3

申请日：1999-10-21

申请人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE ,  ORGANIX, INC. ,  THE GENERAL HOSPITAL CORPORATION

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

IPC分类号： A61K51/04

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.

公开(公告)号：EP1518562A2

公开(公告)日：2005-03-30

申请号：EP04026685.0

申请日：1999-10-21

申请人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE ,  ORGANIX, INC. ,  THE GENERAL HOSPITAL CORPORATION

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

IPC分类号： A61K51/04

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-位上的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。 这些化合物可以作为单独的非对映异构体以及非对映异构体的混合物制备。 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：EP1518561A2

公开(公告)日：2005-03-30

申请号：EP04026679.3

申请日：1999-10-21

申请人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE ,  ORGANIX, INC. ,  THE GENERAL HOSPITAL CORPORATION

发明人： Meltzer, Peter C. ,  Blundell, Paul ,  Madras, Bertha K. ,  Fischman, Alan J. ,  Jones, Alun G. ,  Mahmmod, Ashfaq

IPC分类号： A61K51/04

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.

公开(公告)号：EP1051980A2

公开(公告)日：2000-11-15

申请号：EP99121068.3

申请日：1999-10-21

申请人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE ,  ORGANIX, INC. ,  THE GENERAL HOSPITAL CORPORATION

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

IPC分类号： A61K51/04

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-位上的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。 这些化合物可以作为单独的非对映异构体以及非对映异构体的混合物制备。 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。