公开(公告)号：EP1429811A4

公开(公告)日：2006-05-17

申请号：EP02753490

申请日：2002-08-16

申请人： HARVARD COLLEGE ,  ORGANIX INC

发明人： MADRAS BERTHA K ,  MELTZER PETER C ,  BLUNDELL PAUL

IPC分类号： A61K31/439 ,  A61K31/46 ,  A61K49/00 ,  A61P25/06 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30

CPC分类号： A61K31/439 ,  A61K31/46

摘要： The invention relates to theurapeutic uses of boat tropane analogs, e.g, treatment of neurodegenerative disorders. More specifically the invention relates to a method of treating a neurological disorder in a patient comprising administering to the patient an effective amount of a boat tropane compound. Figure 1 illustrates a general scheme for preparing 2-carbomethoxy tropanes.

摘要翻译： 本发明涉及托丙烷类似物的治疗用途，例如神经变性疾病的治疗。 更具体地说，本发明涉及治疗患者的神经疾病的方法，包括给患者施用有效量的托丙烷化合物。 图1显示了制备2-甲酯基托烷的一般方案。

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：EP1483237A2

公开(公告)日：2004-12-08

申请号：EP03755327.8

申请日：2003-03-27

申请人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE ,  Organix, Inc.

发明人： BLUNDELL, Paul ,  MELTZER, Peter, C. ,  MADRAS, Bertha, K.

IPC分类号： C07D201/00

CPC分类号： A61K51/0448 ,  C07D451/02 ,  G01N33/9406 ,  G01N2500/04

摘要： The present invention provides novel tropane compounds and methods for their use.

摘要翻译： 本发明提供新的托品烷化合物及其使用方法。

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。

公开(公告)号：EP0859641A4

公开(公告)日：1999-05-26

申请号：EP96941959

申请日：1996-10-31

申请人： HARVARD COLLEGE ,  ORGANIX INC ,  MASSACHUSETTS INST TECHNOLOGY

发明人： MELTZER PETER C ,  MADRAS BERTHA K ,  DAVISON ALAN ,  BLUNDELL PAUL ,  MAHMOOD ASHFAQ ,  JONES ALUN G

IPC分类号： A61K51/00 ,  A61K51/04 ,  C07C69/753 ,  C07D451/02 ,  C07F13/00 ,  A61M36/14

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-位上的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：EP0734385A4

公开(公告)日：1997-05-07

申请号：EP95900419

申请日：1994-10-24

申请人： GEN HOSPITAL CORP ,  HARVARD COLLEGE ,  ORGANIX INC ,  UNIV NORTHEASTERN

发明人： ELMALEH DAVID R ,  MADRAS BERTHA K ,  MELTZER PETER ,  HANSON ROBERT N

IPC分类号： A61K51/04 ,  A61P25/16 ,  C07D451/02 ,  A61K31/41 ,  A61K51/02 ,  A61K101/02

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.

公开(公告)号：EP0859641B1

公开(公告)日：2012-10-17

申请号：EP96941959.7

申请日：1996-10-31

申请人： President and Fellows of Harvard College ,  ORGANIX, INC. ,  MASSACHUSETTS INSTITUTE OF TECHNOLOGY

发明人： MELTZER, Peter, C. ,  MADRAS, Bertha, K. ,  DAVISON, Alan ,  BLUNDELL, Paul ,  MAHMOOD, Ashfaq ,  JONES, Alun, G.

IPC分类号： A61K51/00 ,  A61M36/14 ,  A61K51/04 ,  C07C69/753 ,  C07D451/02

CPC分类号： A61K51/0448 ,  A61K2123/00 ,  C07C69/753 ,  C07C2602/44 ,  C07D451/02

公开(公告)号：EP1799640A4

公开(公告)日：2009-09-02

申请号：EP05851213

申请日：2005-09-27

申请人： ORGANIX INC ,  UNIV CASE WESTERN RESERVE ,  TRUSTEES OF THE TUFTS COLLEGE

发明人： SARD HOWARD P ,  SHUSTER LOUIS ,  ROTH BRYAN ,  MORENCY CYNTHIA ,  KUMARAN GOVINDARAJ ,  XU LIANG

IPC分类号： C07D209/16 ,  A61K31/4045 ,  A61P25/00 ,  C07F9/06

CPC分类号： C07D209/16 ,  C07D209/14 ,  C07D209/30 ,  C07D209/32 ,  C07F9/5728

公开(公告)号：EP1670755A2

公开(公告)日：2006-06-21

申请号：EP04809902.2

申请日：2004-10-08

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

发明人： MADRAS, Bertha, K. ,  MELTZER, Peter, C. ,  BUTLER, David

IPC分类号： C07D207/06

CPC分类号： C07D207/325 ,  C07D295/108 ,  C07D307/46 ,  C07D333/22

摘要： New compounds that bind to monoamine transporters are described. The compounds of the present invention can be racemic or pure R-or S-enantiomers. Certain preferred compounds of the present invention have a high selectively dopamine transporter versus the serotonin transporter. Preferred monoamine transporters for the practice of the present invention include the dopamine transporter, the serotonin transporter and the norepinephrine transporter.