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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.
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.
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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
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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
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。
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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
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。
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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
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.
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公开(公告)号：EP1196083B1
公开(公告)日：2008-03-19
申请号：EP00944946.3
申请日：2000-06-28
CPC分类号： A61K51/0497 , A61K51/0448
摘要： A method of diagnosing attention deficient-hyperactivity disorder (AD-HD) in a human patient by assessing dopamine transporter in at least one region of the patient's central nervous system, where an elevated level of dopamine transporter in the patient is indicative of AD-HD. In embodiments of the invention, assessment of dopamine transporter levels includes assessing binding of a dopamine transporter ligand to dopamine transporter using PET or SPECT.
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7.发明授权
公开(公告)号：EP0996619B1
公开(公告)日：2005-01-05
申请号：EP98934396.7
申请日：1998-07-10
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-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.
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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
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.
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公开(公告)号：EP1429811A1
公开(公告)日：2004-06-23
申请号：EP02753490.8
申请日：2002-08-16
IPC分类号： A61K49/00
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。
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公开(公告)号：EP1196083A1
公开(公告)日：2002-04-17
申请号：EP00944946.3
申请日：2000-06-28
IPC分类号： A61B5/00
CPC分类号： A61K51/0497 , A61K51/0448
摘要： A method of diagnosing attention deficient-hyperactivity disorder (AD-HD) in a human patient by assessing dopamine transporter in at least one region of the patient's central nervous system, where an elevated level of dopamine transporter in the patient is indicative of AD-HD. In embodiments of the invention, assessment of dopamine transporter levels includes assessing binding of a dopamine transporter ligand to dopamine transporter using PET or SPECT.
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