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：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：EP0996619A1

公开(公告)日：2000-05-03

申请号：EP98934396.7

申请日：1998-07-10

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

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

IPC分类号： C07D451/02 ,  C07D311/00 ,  C07C255/00 ,  C07C69/74 ,  C07C233/00 ,  C07C205/00 ,  C07C49/115 ,  C07C49/105 ,  C07C41/00 ,  C07C33/34 ,  C07C35/22 ,  C07C35/18 ,  C07C19/08 ,  C07C22/00

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-aza, 8-carbo and 8-oxy tropanes 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-hydroxy-tryptamine 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： 描述了与单胺转运蛋白结合的新的托烷类似物，特别是具有6或7个取代基的8-氮杂，8-碳和8-氧托烷。 本发明的化合物可以是外消旋的，纯的R-对映体或纯的S-对映体。 本发明的某些优选化合物对于DAT对SERT具有高选择性。 还描述了包含配制于药学上可接受的载体中的化合物的药物治疗组合物以及通过使单胺转运蛋白与5-羟色胺再摄取抑制量的本发明化合物接触来抑制5-胺 - 色胺再摄取单胺转运蛋白的方法 。 用于实施本发明的优选单胺转运蛋白包括多巴胺转运蛋白，血清素转运蛋白和去甲肾上腺素转运蛋白。

公开(公告)号：EP0859641A1

公开(公告)日：1998-08-26

申请号：EP96941959.0

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 ,  C07C69 ,  C07D451 ,  C07F13

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.

公开(公告)号：EP3174864A4

公开(公告)日：2018-02-14

申请号：EP15827677

申请日：2015-07-31

申请人： UNIV OREGON HEALTH & SCIENCE ,  UNITED STATES DEPT OF VETERANS AFFAIRS ,  ORGANIX INC

发明人： JANOWSKY AARON ,  MELTZER PETER

IPC分类号： C07D239/96 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61P25/00 ,  C07D401/06 ,  C07D403/06 ,  C07D495/04

CPC分类号： C07D401/06 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14

摘要： Disclosed herein are compounds that bind to the vesicular monoamine transporter 2 (VMAT2), pharmaceutical compositions comprising those compounds, and methods of treatment using said compounds and pharmaceutical compositions.

公开(公告)号：EP2254865A1

公开(公告)日：2010-12-01

申请号：EP09710775.9

申请日：2009-02-11

申请人： ORGANIX, INC. ,  Tufts University ,  University Of North Carolina, Chapel Hill

发明人： SARD, Howard, P. ,  ZHANG, Yiliang ,  LI, Jie ,  SHUSTER, Louis ,  ROTH, Bryan ,  JENSEN, Niels

IPC分类号： C07D209/16 ,  A61K31/405 ,  A61P25/00 ,  A61P3/04

CPC分类号： C07D209/16

摘要： Novel indole compounds are disclosed. Also disclosed are methods for using the compounds to treat human and animal disease, pharmaceutical compositions of the compounds, and kits including the compounds.

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：EP1478356A4

公开(公告)日：2005-03-16

申请号：EP03710964

申请日：2003-02-10

申请人： HARVARD COLLEGE ,  ORGANIX INC

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

IPC分类号： A61K31/35 ,  A61K31/46 ,  A61K47/48 ,  A61P25/00 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/36 ,  A61P43/00 ,  C07D451/02 ,  C07D493/08 ,  A61K31/352 ,  A61K31/382 ,  A61K31/445

CPC分类号： C07D451/02 ,  A61K47/54 ,  C07D493/08

公开(公告)号：EP1478356A2

公开(公告)日：2004-11-24

申请号：EP03710964.2

申请日：2003-02-10

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

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

IPC分类号： A61K31/352 ,  A61K31/382 ,  A61K31/445

CPC分类号： C07D451/02 ,  A61K47/54 ,  C07D493/08

摘要： This invention to antagonists that inhibit transporters and receptors. The invention also relates to partial inhibitors of transporters and receptors that allow partial transport or partial binding of a compound to the transporter or receptor. The invention also relates to compounds that differentially prevent transport or binding through a transporter or to a receptor. The invention also relates to the use of these compounds for treating certain diseases and disorders.