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公开(公告)号：US08933249B2
公开(公告)日：2015-01-13
申请号：US13534878
申请日：2012-06-27
申请人： Eric L. Stangeland , Priscilla Van Dyke , Timothy J. Church , Lori Jean Patterson , Daisuke Roland Saito
发明人： Eric L. Stangeland , Priscilla Van Dyke , Timothy J. Church , Lori Jean Patterson , Daisuke Roland Saito
IPC分类号： A61K31/40 , C07D207/08
CPC分类号： C07D207/08 , A61K31/40
摘要： In one aspect, the invention relates to compounds of formula I: where a and R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
摘要翻译： 一方面，本发明涉及式I化合物：其中a和R 1-6如说明书中所定义，或其药学上可接受的盐。 式I化合物是5-羟色胺和去甲肾上腺素再摄取抑制剂。 另一方面，本发明涉及包含这些化合物的药物组合物; 使用这些化合物的方法; 以及制备这些化合物的方法和中间体。
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![8-AZABICYCLO[3.2.1]OCTYL-2-HYDROXYBENZAMIDE COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS](/abs-image/US/2014/03/20/US20140080855A1/abs.jpg.150x150.jpg)
2.发明申请8-AZABICYCLO[3.2.1]OCTYL-2-HYDROXYBENZAMIDE COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS 有权8-AZABICYCLO [3.2.1] OCTYL-2-羟基苯甲酸酯化合物作为阿片受体拮抗剂公开(公告)号：US20140080855A1
公开(公告)日：2014-03-20
申请号：US13914093
申请日：2013-06-10
申请人： Daisuke Roland Saito , Daniel D. Long , Lan Jiang , Bryan Frieman
发明人： Daisuke Roland Saito , Daniel D. Long , Lan Jiang , Bryan Frieman
IPC分类号： C07D451/02 , A61K31/485 , A61K31/46
CPC分类号： C07D471/08 , A61K31/46 , A61K31/485 , C07D451/02
摘要： The invention provides 8-azabicyclo[3.2.1]octyl-2-hydroxybenzamide compounds of formula (I): wherein R2, R7, and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
摘要翻译： 本发明提供式（I）的8-氮杂双环[3.2.1]辛基-2-羟基苯甲酰胺化合物：其中R2，R7和m在本说明书中定义，或其药学上可接受的盐，其为在mu 阿片受体。 本发明还提供包含这些化合物的药物组合物，使用这些化合物治疗与阿片样物质受体活性相关的病症的方法，以及可用于制备这些化合物的方法和中间体。
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![Disubstituted alkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists](/abs-image/US/2012/09/18/US08268863B2/abs.jpg.150x150.jpg)
3.发明授权Disubstituted alkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists 有权二取代的烷基-8-氮杂双环[3.2.1]辛烷化合物作为μ阿片受体拮抗剂公开(公告)号：US08268863B2
公开(公告)日：2012-09-18
申请号：US13031873
申请日：2011-02-22
CPC分类号： C07D451/02
摘要： The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): where the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
摘要翻译： 本发明提供了式（I）的新的8-氮杂双环[3.2.1]辛烷化合物：其中变量在说明书中定义，或其药学上可接受的盐，它们是μ阿片受体的拮抗剂。 本发明还提供包含这些化合物的药物组合物，使用这些化合物治疗与阿片样物质受体活性相关的病症的方法，以及可用于制备这些化合物的方法和中间体。
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公开(公告)号：US20120178790A1
公开(公告)日：2012-07-12
申请号：US13424561
申请日：2012-03-20
申请人： Daisuke Roland SAITO
发明人： Daisuke Roland SAITO
CPC分类号： C07D207/08 , A61K31/40 , A61K45/06
摘要： The invention provides a crystalline hydrochloride salt of (S)-3-[(S)-1-(4-chlorophenoxy)-2-methylpropyl]pyrrolidine. This invention also provides pharmaceutical compositions comprising the crystalline salt, processes and intermediates for preparing the crystalline salt, and methods of using the crystalline salt to treat diseases.
摘要翻译： 本发明提供（S）-3 - [（S）-1-（4-氯苯氧基）-2-甲基丙基]吡咯烷的结晶盐酸盐。 本发明还提供了包含结晶盐，用于制备结晶盐的方法和中间体以及使用结晶盐治疗疾病的方法的药物组合物。
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公开(公告)号：US20120142689A1
公开(公告)日：2012-06-07
申请号：US13308844
申请日：2011-12-01
IPC分类号： A61K31/5377 , C07D413/12 , C07D403/12 , A61K31/40 , A61K31/422 , A61K31/4178 , A61K31/4196 , A61K31/4245 , A61K31/4155 , A61K31/506 , A61K31/41 , A61P9/12 , A61P1/00 , A61P35/00 , A61P29/00 , A61P19/02 , A61P19/10 , A61P3/10 , A61P7/00 , C07D207/09
CPC分类号： C07D207/09 , A61K31/40 , A61K31/41 , A61K31/4155 , A61K31/4178 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D207/08 , C07D403/12 , C07D413/12
摘要： In one aspect, the invention relates to compounds of formula I: where Y, R1, R2, n, and Q are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
摘要翻译： 一方面，本发明涉及式I化合物：其中Y，R 1，R 2，n和Q如说明书中所定义，或其药学上可接受的盐。 式I的化合物是5-羟色胺再摄取抑制剂。 另一方面，本发明涉及包含这些化合物的药物组合物; 使用这些化合物的方法; 以及制备这些化合物的方法和中间体。
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公开(公告)号：US20120088799A1
公开(公告)日：2012-04-12
申请号：US13269790
申请日：2011-10-10
IPC分类号： A61K31/40 , C07D401/12 , A61K31/4439 , A61P9/12 , A61P3/10 , A61P1/00 , A61P29/00 , A61P19/10 , A61P19/02 , C07D207/08 , A61P35/00
CPC分类号： C07D207/08 , C07D207/12 , C07D401/12
摘要： In one aspect, the invention relates to compounds of formula I: where X, Y, R1, R2, R3, R4, R4, and n are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
摘要翻译： 一方面，本发明涉及式I的化合物：其中X，Y，R 1，R 2，R 3，R 4，R 4和n如说明书中所定义，或其药学上可接受的盐。 式I的化合物是5-羟色胺再摄取抑制剂。 另一方面，本发明涉及包含这些化合物的药物组合物; 使用这些化合物的方法; 以及制备这些化合物的方法和中间体。
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公开(公告)号：US20110275694A1
公开(公告)日：2011-11-10
申请号：US12984076
申请日：2011-01-04
申请人： Eric Stangeland , Priscilla Van Dyke , Timothy J. Church , Lori Jean Patterson , Daisuke Roland Saito
发明人： Eric Stangeland , Priscilla Van Dyke , Timothy J. Church , Lori Jean Patterson , Daisuke Roland Saito
CPC分类号： C07D207/08 , A61K31/40
摘要： In one aspect, the invention relates to compounds of formula I: where a and R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
摘要翻译： 一方面，本发明涉及式I化合物：其中a和R 1-6如说明书中所定义，或其药学上可接受的盐。 式I化合物是5-羟色胺和去甲肾上腺素再摄取抑制剂。 另一方面，本发明涉及包含这些化合物的药物组合物; 使用这些化合物的方法; 以及制备这些化合物的方法和中间体。
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公开(公告)号：US07994165B2
公开(公告)日：2011-08-09
申请号：US12574066
申请日：2009-10-06
IPC分类号： A61K31/535 , A61K31/497 , A61K31/47 , A61K31/425 , C07C215/60 , C07D243/10 , C07D265/30
CPC分类号： C07C233/43 , C07D215/24 , C07D265/30
摘要： The invention provides novel β2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with β2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.
摘要翻译： 本发明提供新颖的2肾上腺素能受体激动剂化合物。 本发明还提供了包含这些化合物的药物组合物，使用这些化合物治疗与β-肾上腺素能受体活性有关的疾病的方法，以及可用于制备这些化合物的方法和中间体。
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![8-AZABICYCLO[3.2.1]OCTYL-2-HYDROXYBENZAMIDE COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS](/abs-image/US/2011/05/19/US20110118306A1/abs.jpg.150x150.jpg)
9.发明申请8-AZABICYCLO[3.2.1]OCTYL-2-HYDROXYBENZAMIDE COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS 有权8-AZABICYCLO [3.2.1] OCTYL-2-羟基苯甲酸酯化合物作为阿片受体拮抗剂公开(公告)号：US20110118306A1
公开(公告)日：2011-05-19
申请号：US13014012
申请日：2011-01-26
申请人： Daisuke Roland Saito , Daniel D. Long , Priscilla Van Dyke , Timothy J. Church , Lan Jiang , Bryan Frieman
发明人： Daisuke Roland Saito , Daniel D. Long , Priscilla Van Dyke , Timothy J. Church , Lan Jiang , Bryan Frieman
CPC分类号： C07D471/08 , A61K31/46 , A61K31/485 , C07D451/02
摘要： The invention provides 8-azabicyclo[3.2.1]octyl-2-hydroxybenzamide compounds of formula (I): wherein R2, R7, and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
摘要翻译： 本发明提供式（I）的8-氮杂双环[3.2.1]辛基-2-羟基苯甲酰胺化合物：其中R2，R7和m在本说明书中定义，或其药学上可接受的盐，其为在mu 阿片受体。 本发明还提供包含这些化合物的药物组合物，使用这些化合物治疗与阿片样物质受体活性相关的病症的方法，以及可用于制备这些化合物的方法和中间体。
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![8-azabicyclo[3.2.1]octyl-2-hydroxybenzamide compounds as mu opioid receptor antagonists](/abs-image/US/2011/03/08/US07902220B2/abs.jpg.150x150.jpg)
10.发明授权8-azabicyclo[3.2.1]octyl-2-hydroxybenzamide compounds as mu opioid receptor antagonists 有权8-氮杂双环[3.2.1]辛基-2-羟基苯甲酰胺化合物作为μ阿片受体拮抗剂公开(公告)号：US07902220B2
公开(公告)日：2011-03-08
申请号：US12229664
申请日：2008-08-26
申请人： Daisuke Roland Saito , Daniel D. Long , Priscilla Van Dyke , Timothy J. Church , Lan Jiang , Bryan Frieman
发明人： Daisuke Roland Saito , Daniel D. Long , Priscilla Van Dyke , Timothy J. Church , Lan Jiang , Bryan Frieman
IPC分类号： A61K31/46 , C07D451/02 , A61P1/00
CPC分类号： C07D471/08 , A61K31/46 , A61K31/485 , C07D451/02
摘要： The invention provides 8-azabicyclo[3.2.1]octyl-2-hydroxybenzamide compounds of formula (I): wherein R2, R7, and m are defined in the specification, or a pharmaceutically -acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
摘要翻译： 本发明提供式（I）的8-氮杂双环[3.2.1]辛基-2-羟基苯甲酰胺化合物：其中R2，R7和m在本说明书中定义，或其药学上可接受的盐，其为μ 阿片受体。 本发明还提供包含这些化合物的药物组合物，使用这些化合物治疗与阿片样物质受体活性相关的病症的方法，以及可用于制备这些化合物的方法和中间体。
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