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1. 发明授权

US06184219B2 Composition and methods employing it for the treatment of 5-HT-mediated disorders 失效
标题翻译：使用它来治疗5-HT介导的病症的组合物和方法
公开(公告)号：US06184219B2
公开(公告)日：2001-02-06
申请号：US09351071
申请日：1999-07-09
申请人： John Evenden , Seth-Olov Thorberg
发明人： John Evenden , Seth-Olov Thorberg
IPC分类号： A61K3135
CPC分类号： A61K31/35 , A61K31/445 , A61K31/55 , A61K31/34 , A61K31/135 , A61K2300/00
摘要： The invention relates to a composition comprising a first component (a) which is (R)-5-carbamoyl-8-fluoro-3-N,N-dicyclobutylamino-3,4-dihydro-2H-1-benzopyran in the form of the free base, or a pharmaceutically acceptable salt and/or solvate thereof, and a second component (b) which is (+)-1-[3-(dimethylamino)propyl]-1-(p-fluorophenyl)-5-phthalancarbonitrile in the form of the free base, or a pharmaceutically acceptable salt and/or solvate thereof. The invention is further directed to the preparation of the composition, pharmaceutical formulations containing said composition, and a method of treatment of affective disorders such as mood disorders and anxiety disorders with said composition, as well as a kit containing said composition.
摘要翻译：本发明涉及包含第一组分（a）的组合物，其为（R）-5-氨基甲酰基-8-氟-3-N，N-二环丁基氨基-3,4-二氢-2H-1-苯并吡喃，其形式为游离碱或其药学上可接受的盐和/或溶剂合物，以及作为（+）-1- [3-（二甲基氨基）丙基] -1-（对氟苯基）-5-邻苯二甲腈的第二组分（b）游离碱的形式，或其药学上可接受的盐和/或溶剂化物。本发明还涉及组合物的制备，含有所述组合物的药物制剂，以及用所述组合物治疗情绪障碍如情绪障碍和焦虑症的方法，以及含有所述组合物的试剂盒。

2. 发明授权

US5962514A Combination of 5-HT uptake inhibitor with a selective 5-HT1A antagonist 失效
标题翻译： 5-HT摄取抑制剂与选择性5-HT1A拮抗剂的组合
公开(公告)号：US5962514A
公开(公告)日：1999-10-05
申请号：US640896
申请日：1997-05-09
申请人： John Evenden , Seth-Olov Thorberg
发明人： John Evenden , Seth-Olov Thorberg
IPC分类号： C07D311/58 , A61K31/35 , A61K31/352 , A61K31/4406 , A61K31/445 , A61K31/55 , A61K45/00 , A61P25/24 , A61P25/26 , A61K31/40
CPC分类号： A61K31/35 , A61K31/445 , A61K31/55
摘要： The invention relates to a combination of a first component (a) which is a 5-HT reuptake inhibitor and a second component (b) which is selective 5-HT.sub.1A antagonist of the general formula ##STR1## wherein R.sub.1 is n-propyl or cyclobutyl;R.sub.2 is isopropyl, tertiary butyl, cyclobutyl, cyclopentyl or cyclohexyl;R.sub.3 is hydrogen;R.sub.4 is hydrogen or methyl;as (R)-enantiomer in the form of free base or pharmaceutically acceptable salts thereof, the preparation thereof, pharmaceutical formulations containing said combination, use of and method of treatment of affective disorders such as depression, anxiety and OCD with said combination as well as a kit containing said combination.
摘要翻译： PCT No.PCT / SE96 / 00526 Sec。 371日期：1996年5月9日 102（e）日期1996年5月9日PCT提交1996年4月23日PCT公布。第WO96 / 33710号公报日期1996年10月31日本发明涉及作为5-HT再摄取抑制剂的第一组分（a）和作为通式的选择性5-HT 1A拮抗剂的第二组分（b）的组合，其中R 1是正丙基或环丁基; R2是异丙基，叔丁基，环丁基，环戊基或环己基; R3是氢; R4是氢或甲基; 作为游离碱或其药学上可接受的盐形式的（R） - 对映体，其制备方法，含有所述组合的药物制剂，用所述组合治疗情感障碍如抑郁症，焦虑和OCD的用途和方法，以及包含所述组合的试剂盒。

3. 发明授权

US06172105B2 Composition and methods employing it for the treatment of 5-HT-mediated disorders 失效
标题翻译：使用它来治疗5-HT介导的病症的组合物和方法
公开(公告)号：US06172105B2
公开(公告)日：2001-01-09
申请号：US09351070
申请日：1999-07-09
申请人： John Evenden , Seth-Olov Thorberg
发明人： John Evenden , Seth-Olov Thorberg
IPC分类号： A61K3135
CPC分类号： A61K31/35 , A61K31/445 , A61K31/55 , A61K31/34 , A61K31/135 , A61K2300/00
摘要： The invention relates to a composition comprising a first component (a) which is (R)-3-N,N-dicyclobutylamino-8-fluoro-3,4-dihydro-2H-1-benzopyran-5-carboxamide hydrogen (2R,3R)-tartrate monohydrate and a second component (b) which is a 5-HT reuptake inhibitor, excluding citalopram and paroxetine. The invention is further directed to the preparation of the composition, pharmaceutical formulations containing said composition, and a method of treatment of affective disorders such as mood disorders and anxiety disorders with said composition, as well as a kit containing said composition.
摘要翻译：本发明涉及包含第一组分（a）的组合物，其为（R）-3-N，N-二环丁基氨基-8-氟-3,4-二氢-2H-1-苯并吡喃-5-甲酰胺氢（2R， 3R） - 酒石酸盐一水合物和第二组分（b），其为5-HT再摄取抑制剂，不包括西酞普兰和帕罗西汀。本发明还涉及组合物的制备，含有所述组合物的药物制剂，以及用所述组合物治疗情绪障碍如情绪障碍和焦虑症的方法，以及含有所述组合物的试剂盒。

4. 发明授权

US06184218B2 Composition and methods employing it for the treatment of 5-HT-mediated disorders 失效
标题翻译：使用它来治疗5-HT介导的病症的组合物和方法
公开(公告)号：US06184218B2
公开(公告)日：2001-02-06
申请号：US09349590
申请日：1999-07-09
申请人： John Evenden , Seth-Olov Thorberg
发明人： John Evenden , Seth-Olov Thorberg
IPC分类号： A61K3135
CPC分类号： A61K31/35 , A61K31/445 , A61K31/55 , A61K31/34 , A61K31/135 , A61K2300/00
摘要： The invention relates to a composition comprising a first component (a) which is (R)-3N,N-dicyclobutylamino-8-fluoro-3,4-dihydro-2H-1-benzopyran-5-carboxamide hydrogen (2R,3R)-tartrate monohydrate and a second component (b) which is 1-[3-(dimethylamino)propyl]-1-(p-fluorophenyl)-5-phthalancarbonitrile, as the racemate or an enantiomer thereof, in the form of the free base, or a pharmaceutically acceptable salt and/or solvate thereof The invention further concerns the preparation of the composition, pharmaceutical formulations containing said composition, and a method of treatment of affective disorders such as mood disorders and anxiety disorders with said composition, as well as a kit containing said composition.
摘要翻译：本发明涉及包含（R）-3N，N-二环丁基氨基-8-氟-3,4-二氢-2H-1-苯并吡喃-5-甲酰胺氢（2R，3R）的第一组分（a） - 酒石酸盐一水合物和第二组分（b），其为游离碱形式的1- [3-（二甲基氨基）丙基] -1-（对氟苯基）-5-邻苯二甲酰亚胺作为外消旋体或其对映异构体，或其药学上可接受的盐和/或溶剂化物。本发明还涉及组合物的制备，含有所述组合物的药物制剂，以及用所述组合物治疗情绪障碍（例如情绪障碍和焦虑症）的方法，以及包含所述组合物的试剂盒。

5. 发明申请

US20080085888A1 Therapeutic Combinations 审中-公开
标题翻译：治疗组合
公开(公告)号：US20080085888A1
公开(公告)日：2008-04-10
申请号：US11855175
申请日：2007-09-14
申请人： Scott Breining , John Evenden , Edwin Johnson , Kristen Jordan , Sharon Letchworth , Craig Miller , Ladislav Mrzljak , James Wamsley , Dan Widzowski , Yun-De Xiao
发明人： Scott Breining , John Evenden , Edwin Johnson , Kristen Jordan , Sharon Letchworth , Craig Miller , Ladislav Mrzljak , James Wamsley , Dan Widzowski , Yun-De Xiao
IPC分类号： A61K31/44 , A61K31/451 , A61K31/554 , A61P25/18
CPC分类号： A61K31/44 , A61K31/451 , A61K31/554 , A61K45/06 , A61K2300/00
摘要： The present invention provides a combination of (a) an antipsychotic and (b) an alpha4/beta2 (α4β2)-neuronal nicotinic receptor agonist. The invention further relates to pharmaceutical compositions comprising said combination and to the use of the combination in therapy. The invention further relates to a kit comprising the combination and use of said kit in therapy.
摘要翻译：本发明提供了（a）抗精神病药和（b）α4/β2（α4β2） - 神经元烟碱受体激动剂的组合。本发明还涉及包含所述组合的药物组合物和在治疗中使用该组合物。本发明还涉及一种试剂盒，其包括在治疗中组合和使用所述试剂盒。

6. 发明授权

US06169098A Composition and methods employing it for the treatment of 5-HT-mediated disorders 失效
标题翻译：使用它来治疗5-HT介导的病症的组合物和方法
公开(公告)号：US06169098A
公开(公告)日：2001-01-02
申请号：US09351069
申请日：1999-07-09
申请人： John Evenden , Seth-Olov Thorberg
发明人： John Evenden , Seth-Olov Thorberg
IPC分类号： A61K31445
CPC分类号： A61K31/35 , A61K31/445 , A61K31/55 , A61K31/34 , A61K31/135 , A61K2300/00
摘要： The invention relates to a composition comprising a first component (a) which is (R)-3-N,N-dicyclobutylamino-8-fluoro-3,4-dihydro-2H-1-benzopyran-5-carboxamide hydrogen (2R,3R)-tartrate monohydrate and a second component (b) which is paroxetine, in the form of its free base, or a pharmaceutically acceptable salt and/or solvate thereof The invention is further directed to the preparation of the composition, pharmaceutical formulations containing said composition, and a method of treatment of affective disorders such as mood disorders and anxiety disorders with said composition, as well as a kit containing said composition.
摘要翻译：本发明涉及包含第一组分（a）的组合物，其为（R）-3-N，N-二环丁基氨基-8-氟-3,4-二氢-2H-1-苯并吡喃-5-甲酰胺氢（2R， 3R） - 酒石酸盐一水合物和第二组分（b），其为游离碱形式的帕罗西汀，或其药学上可接受的盐和/或溶剂化物。本发明还涉及组合物的制备，含有所述组合物，以及使用所述组合物治疗情绪障碍如情绪障碍和焦虑症的方法，以及含有所述组合物的试剂盒。

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