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公开(公告)号：US06992090B2
公开(公告)日：2006-01-31
申请号：US10462507
申请日：2003-06-16
IPC分类号： A61K31/445 , C07D211/82
CPC分类号： C07D401/06 , C07D211/22 , C07D401/12 , C07F9/59
摘要： Novel 3,4-disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.
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42.发明申请PROCESSES FOR THE PREPARATION OF PERIPHERAL OPIOID ANTAGONIST COMPOUNDS AND INTERMEDIATES THERETO 审中-公开制备外周阿片类拮抗剂化合物及其中间体的方法公开(公告)号：US20150045556A1
公开(公告)日：2015-02-12
申请号：US14233670
申请日：2012-07-17
申请人： Roland E. Dolle , Bertrand Le Bourdonnec , Pierre Martin , Christian Steffen Moessner , Felix Herbert Spindler , Dirk Jost Spielvogel
发明人： Roland E. Dolle , Bertrand Le Bourdonnec , Pierre Martin , Christian Steffen Moessner , Felix Herbert Spindler , Dirk Jost Spielvogel
IPC分类号： C07D211/22
CPC分类号： C07D211/22 , C07D241/44 , C07D317/62
摘要： Novel processes for the preparation of peripheral opioid antagonist compounds and intermediates thereto. The compounds prepared by the present processes may be useful, for example, as antagonists to the mu, kappa and delta opioid receptors, and thereby may be useful in the treatment of gastrointestinal motility disorders, and in preventing peripheral opiate induced side effects. The present processes may offer improved yields, chemical or stereochemical purity, ease of preparation and/or isolation of intermediates and final product, and more industrially useful reaction conditions and workability.
摘要翻译： 用于制备外周阿片样物质拮抗剂化合物及其中间体的新方法。 通过本发明方法制备的化合物可用作例如mu，κ和δ阿片样物质受体的拮抗剂，因此可用于治疗胃肠动力障碍，以及用于预防外周鸦片诱导的副作用。 本方法可以提供改进的产率，化学或立体化学纯度，中间体和最终产物的制备和/或分离的容易程度，以及更具有工业上有用的反应条件和可加工性。
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公开(公告)号：US08288546B2
公开(公告)日：2012-10-16
申请号：US12897824
申请日：2010-10-05
IPC分类号： C07F9/28
CPC分类号： C07D401/06 , C07D211/22 , C07D401/12 , C07F9/59
摘要： Novel 3,4-disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.
摘要翻译： 公开了新的3,4-二取代-4-芳基 - 哌啶化合物。 还公开了含有3,4-二取代-4-芳基 - 哌啶化合物的药物组合物及其药物用途的方法。 所公开的化合物尤其可用作阿片受体的拮抗剂。
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公开(公告)号：US20120165356A1
公开(公告)日：2012-06-28
申请号：US13274616
申请日：2011-10-17
IPC分类号： A61K31/438 , A61P15/00 , A61P13/02
CPC分类号： C07D491/107 , C07D221/20 , C07D311/96 , C07D401/04 , C07D493/10 , C07D495/10
摘要： Spirocyclic heterocyclic derivatives, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the spirocyclic heterocyclic derivatives are ligands of the δ opioid receptor and may be useful, inter alia, for treating and/or preventing pain, anxiety, gastrointestinal disorders, and other δ opioid receptor-mediated conditions.
摘要翻译： 公开了螺环杂环衍生物，含有这些化合物的药物组合物及其制药方法。 在某些实施方案中，螺环杂环衍生物是δ阿片样受体的配体，尤其可用于治疗和/或预防疼痛，焦虑，胃肠道疾病和其他δ阿片受体介导的病症。
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公开(公告)号：US07767814B2
公开(公告)日：2010-08-03
申请号：US11442075
申请日：2006-05-25
IPC分类号： C07D221/22 , C07D221/02 , A01N43/42
CPC分类号： C07D221/22 , A61K31/451 , A61K31/473 , A61K45/06 , C07D221/06 , A61K2300/00
摘要： Certain 4-aryl-piperidine compounds, including N-substituted 9β-substituted-5-(3-substituted-phenyl)morphans and N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines, pharmaceutical compositions, and methods of their use, inter alia, as opioid antagonists are disclosed.
摘要翻译： 某些4-芳基哌啶化合物，包括N-取代的9'-双（5-取代的苯基）吗啉和N-取代的八氢-4a-（3-羟基苯基）-10a-甲基 - 苯并[g]异喹啉 ，药物组合物及其使用方法，特别是作为阿片样物质拮抗剂。
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公开(公告)号：US20100120808A1
公开(公告)日：2010-05-13
申请号：US12483781
申请日：2009-06-12
IPC分类号： A61K31/438 , C07D401/02 , A61P1/00 , A61P37/02 , A61P25/04 , A61P9/12
CPC分类号： C07D491/107 , C07D221/20 , C07D311/96 , C07D401/04 , C07D493/10 , C07D495/10
摘要： Spirocyclic heterocyclic derivatives, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the spirocyclic heterocyclic derivatives are ligands of the δ opioid receptor and may be useful, inter alia, for treating and/or preventing pain, anxiety, gastrointestinal disorders, and other δ opioid receptor-mediated conditions.
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公开(公告)号：US20090233959A1
公开(公告)日：2009-09-17
申请号：US12388982
申请日：2009-02-19
IPC分类号： A61K31/4353 , A61P25/00
CPC分类号： A61K31/4353
摘要： This present disclosure provides methods of treating pain with beloxepin and/or beloxepin analogs.
摘要翻译： 本公开内容提供了用贝洛塞平和/或贝洛塞平类似物治疗疼痛的方法。
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公开(公告)号：US20090233957A1
公开(公告)日：2009-09-17
申请号：US12388903
申请日：2009-02-19
IPC分类号： A61K31/4353 , C07D491/044 , C07K14/47 , A61P25/00
CPC分类号： C07D491/044
摘要： This present disclosure provides compositions comprising (−)-beloxepin, methods for their synthesis and methods for their use.
摘要翻译： 本公开提供包含（ - ） - 贝洛塞平的组合物，其合成方法及其使用方法。
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公开(公告)号：US07576207B2
公开(公告)日：2009-08-18
申请号：US11696585
申请日：2007-04-04
IPC分类号： C07D401/00 , A01N43/42
CPC分类号： C07D491/107 , C07D487/10
摘要： Spirocyclic heterocyclic derivatives, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the spirocyclic heterocyclic derivatives are ligands of the δ-opioid receptor and may be useful, inter alia, for treating and/or preventing pain, anxiety, gastrointestinal disorders, and other δ-opioid receptor-mediated diseases, disorders, and/or conditions.
摘要翻译： 公开了螺环杂环衍生物，含有这些化合物的药物组合物及其制药方法。 在某些实施方案中，螺环杂环衍生物是δ-阿片受体受体的配体，尤其可用于治疗和/或预防疼痛，焦虑，胃肠道疾病和其他δ-阿片受体介导的疾病，病症和 /或条件。
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公开(公告)号：US07381721B2
公开(公告)日：2008-06-03
申请号：US10390522
申请日：2003-03-17
IPC分类号： A61K31/445 , C07D211/00
CPC分类号： C07D401/04 , C07D211/34 , C07D211/58 , C07D401/06 , C07D401/10 , C07D401/14 , C07D409/14 , C07D413/14
摘要： 3,4-Disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.
摘要翻译： 公开了3,4-二取代-4-芳基 - 哌啶化合物。 还公开了含有3,4-二取代-4-芳基 - 哌啶化合物的药物组合物及其药物用途的方法。 所公开的化合物尤其可用作阿片受体的拮抗剂。
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