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公开(公告)号：US20100144698A1
公开(公告)日：2010-06-10
申请号：US12703610
申请日：2010-02-10
申请人： Thomas Bannister , Cassandra Celatka , Nizal S. Chandrakumar , Hongfeng Deng , Zihong Guo , Lei Jin , Tsveltelina Lazarova , Jian Lin , Scott T. Moe , Pamela Nagafuji , Manuel Navia , Amy Ripka , Michael J. Rynkiewicz , Kerry L. Spear , James E. Stickler , Roger Xie
发明人： Thomas Bannister , Cassandra Celatka , Nizal S. Chandrakumar , Hongfeng Deng , Zihong Guo , Lei Jin , Tsveltelina Lazarova , Jian Lin , Scott T. Moe , Pamela Nagafuji , Manuel Navia , Amy Ripka , Michael J. Rynkiewicz , Kerry L. Spear , James E. Stickler , Roger Xie
IPC分类号： A61K31/397 , C07D205/04 , A61P9/00 , A61P7/00
CPC分类号： C07D405/06 , C07D205/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/14
摘要： Compounds are provided which have the structure Wherein A, B, C, D, m, Y, Ra, Rc, Rd, and Rd′ are as described herein, and which are useful as inhibitors of tryptase, thrombin, trypsin, Factor Xa, Factor VIIa, Factor XIa, and urokinase-type plasminogen activator and may be employed in preventing and/or treating asthma, chronic asthma, allergic rhinitis, and thrombotic disorders.
摘要翻译： 提供具有其中A，B，C，D，m，Y，Ra，Rc，Rd和Rd'如本文所述的结构的化合物，其可用作类胰蛋白酶，凝血酶，胰蛋白酶，因子Xa， 因子VIIa，因子XIa和尿激酶型纤溶酶原激活剂，可用于预防和/或治疗哮喘，慢性哮喘，过敏性鼻炎和血栓形成障碍。
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公开(公告)号：US20090143351A1
公开(公告)日：2009-06-04
申请号：US12359490
申请日：2009-01-26
申请人： Thomas Bannister , Cassandra Celatka , Nizal S. Chandrakumar , Hongfeng Deng , Zihong Guo , Lei Jin , Tsvetelina Lazarova , Jian Lin , Scott T. Moe , Pamela Nagafuji , Manuel Navia , Amy Ripka , Michael J. Rynkiewicz , Kerry L. Spear , James E. Stickler , Roger Xie
发明人： Thomas Bannister , Cassandra Celatka , Nizal S. Chandrakumar , Hongfeng Deng , Zihong Guo , Lei Jin , Tsvetelina Lazarova , Jian Lin , Scott T. Moe , Pamela Nagafuji , Manuel Navia , Amy Ripka , Michael J. Rynkiewicz , Kerry L. Spear , James E. Stickler , Roger Xie
IPC分类号： A61K31/397 , C07D401/06 , C07D205/08 , A61P7/00 , C07D401/04 , A61K31/4427
CPC分类号： C07D405/06 , C07D205/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/14
摘要： Compounds are provided which have the structure Wherein A, B, C, D, m, Y, Ra, Rc, Rd, and Rd′ are as described herein, and which are useful as inhibitors of tryptase, thrombin, trypsin, Factor Xa, Factor VIIa, Factor XIa, and urokinase-type plasminogen activator and may be employed in preventing and/or treating asthma, chronic asthma, allergic rhinitis, and thrombotic disorders.
摘要翻译： 提供具有其中A，B，C，D，m，Y，Ra，Rc，Rd和Rd'如本文所述的结构的化合物，其可用作类胰蛋白酶，凝血酶，胰蛋白酶，因子Xa， 因子VIIa，因子XIa和尿激酶型纤溶酶原激活剂，可用于预防和/或治疗哮喘，慢性哮喘，过敏性鼻炎和血栓形成障碍。
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公开(公告)号：US07501404B2
公开(公告)日：2009-03-10
申请号：US11398438
申请日：2006-04-04
申请人： Thomas Bannister , Cassandra Celatka , Nizal S. Chandrakumar , Hongfeng Deng , Zihong Guo , Lei Jin , Tsvetelina Lazarova , Jian Lin , Scott T. Moe , Pamela Nagafuji , Manuel Navia , Amy Ripka , Michael J. Rynkiewicz , Kerry L. Spear , James E. Stickler , Roger Xie
发明人： Thomas Bannister , Cassandra Celatka , Nizal S. Chandrakumar , Hongfeng Deng , Zihong Guo , Lei Jin , Tsvetelina Lazarova , Jian Lin , Scott T. Moe , Pamela Nagafuji , Manuel Navia , Amy Ripka , Michael J. Rynkiewicz , Kerry L. Spear , James E. Stickler , Roger Xie
IPC分类号： C07D205/08 , C07D205/085 , C07D401/14 , C07D401/12 , C07D401/06 , C07D403/12 , C07D403/14 , C07D403/04 , A61K31/397 , A61K31/506 , A61K31/4427 , A61K31/41
CPC分类号： C07D405/06 , C07D205/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/14
摘要： Compounds are provided which have the structure Wherein A, B, C, D, m, Y, Ra, Rc, Rd, and Rd′ are as described herein, and which are useful as inhibitors of tryptase, thrombin, trypsin, Factor Xa, Factor VIIa, Factor XIa, and urokinase-type plasminogen activator and may be employed in preventing and/or treating asthma, chronic asthma, allergic rhinitis, and thrombotic disorders.
摘要翻译： 提供具有其中A，B，C，D，m，Y，Ra，Rc，Rd和Rd'如本文所述的结构的化合物，其可用作类胰蛋白酶，凝血酶，胰蛋白酶，因子Xa， 因子VIIa，因子XIa和尿激酶型纤溶酶原激活剂，可用于预防和/或治疗哮喘，慢性哮喘，过敏性鼻炎和血栓形成障碍。
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公开(公告)号：US20070105832A1
公开(公告)日：2007-05-10
申请号：US11398438
申请日：2006-04-04
申请人： Thomas Bannister , Cassandra Celatka , Nizal Chandrakumar , Hongfeng Deng , Zihong Guo , Lei Jin , Tsvetelina Lazarova , Jian Lin , Scott Moe , Pamela Nagafuji , Manuel Navia , Amy Ripka , Michael Rynkiewicz , Kerry Spear , James Stickler , Roger Xie
发明人： Thomas Bannister , Cassandra Celatka , Nizal Chandrakumar , Hongfeng Deng , Zihong Guo , Lei Jin , Tsvetelina Lazarova , Jian Lin , Scott Moe , Pamela Nagafuji , Manuel Navia , Amy Ripka , Michael Rynkiewicz , Kerry Spear , James Stickler , Roger Xie
IPC分类号： A61K31/397 , C07D205/08
CPC分类号： C07D405/06 , C07D205/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/14
摘要： Compounds are provided which have the structure Wherein A, B, C, D, m, Y, Ra, Rc, Rd, and Rd′ are as described herein, and which are useful as inhibitors of tryptase, thrombin, trypsin, Factor Xa, Factor VIIa, Factor XIa, and urokinase-type plasminogen activator and may be employed in preventing and/or treating asthma, chronic asthma, allergic rhinitis, and thrombotic disorders.
摘要翻译： 提供具有其中A，B，C，D，m，Y，Ra，Rc，Rd和Rd'如本文所述的结构的化合物，其可用作类胰蛋白酶，凝血酶，胰蛋白酶，因子Xa， 因子VIIa，因子XIa和尿激酶型纤溶酶原激活剂，可用于预防和/或治疗哮喘，慢性哮喘，过敏性鼻炎和血栓形成障碍。
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公开(公告)号：US20050143317A1
公开(公告)日：2005-06-30
申请号：US10817248
申请日：2004-04-02
申请人： Sherin Abdel-Meguid , Robert Babine , Hongfeng Deng , Lei Jin , Jian Lin , Scott Magee , Harold Meyers , Pramod Pandey , Michael Rynkiewicz , David Weaver , Zihong Gho , Thomas Bannister
发明人： Sherin Abdel-Meguid , Robert Babine , Hongfeng Deng , Lei Jin , Jian Lin , Scott Magee , Harold Meyers , Pramod Pandey , Michael Rynkiewicz , David Weaver , Zihong Gho , Thomas Bannister
IPC分类号： A61K20060101 , A61K38/00 , A61K38/04 , C07K2/00 , C07K5/04 , C07K5/06 , C07K5/065 , C07K5/078
CPC分类号： C07K5/06078 , A61K38/00 , C07K5/06034 , C07K5/06139 , C07K5/06191
摘要： The present invention provides compounds that inhibit Factor XIa and methods of preventing or treating undesired thrombosis by administering a compound of the invention to a mammal. The invention also provides three-dimensional structures of Factor XIa and methods for designing or selecting additional Factor XIa inhibitors using these structures.
摘要翻译： 本发明提供了通过向哺乳动物施用本发明的化合物来抑制因子XIa的化合物和预防或治疗不期望的血栓形成的方法。 本发明还提供了因子XIa的三维结构以及使用这些结构设计或选择另外的因子XIa抑制剂的方法。
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公开(公告)号：US20060211864A1
公开(公告)日：2006-09-21
申请号：US11364506
申请日：2006-02-28
申请人： Brian Aquila , Thomas Bannister , Gregory Cuny , James Hauske , Michele Heffernan , Michael Hoemann , Donald Kessler , Liming Shao , Xinhe Wu , Roger Xie
发明人： Brian Aquila , Thomas Bannister , Gregory Cuny , James Hauske , Michele Heffernan , Michael Hoemann , Donald Kessler , Liming Shao , Xinhe Wu , Roger Xie
IPC分类号： C07D211/06 , C07D211/60 , C07D211/26 , C07D211/28
CPC分类号： C07D211/22 , C07D211/26
摘要： One aspect of the present invention relates to methods of synthesizing substituted piperidines. A second aspect of the present invention relates to stereoselective methods of synthesizing substituted piperidines. The methods of the present invention will find use in the synthesis of compounds useful for treatment of numerous ailments, conditions and diseases that afflict mammals, including but not limited to addiction and pain. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the substituted piperidines using the methods of the present invention. An additional aspect of the present invention relates to enantiomerically substituted pyrrolidines, piperidines, and azepines.
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公开(公告)号：US20110038835A1
公开(公告)日：2011-02-17
申请号：US12808052
申请日：2008-12-18
申请人： Yangbo Feng , Philip LoGrasso , Thomas Bannister , Thomas Schroeter , Xingang Fang , Yen ting Chen , Yan Yin , Michael P. Smolinski , Lei Yao , Bo Wang , Hampton Sessions
发明人： Yangbo Feng , Philip LoGrasso , Thomas Bannister , Thomas Schroeter , Xingang Fang , Yen ting Chen , Yan Yin , Michael P. Smolinski , Lei Yao , Bo Wang , Hampton Sessions
IPC分类号： A61K31/5377 , C07D231/12 , A61K31/415 , C07D471/02 , A61K31/437 , C07D487/04 , A61K31/519 , C07D401/12 , A61K31/4439 , C07D217/00 , A61K31/47 , C07D413/10 , C07D413/14 , A61P9/00 , A61P9/12 , A61P9/10 , A61P25/00 , A61P25/16 , A61P11/06 , A61P19/02 , A61P3/00 , A61K39/395 , A61K33/24 , A61K31/675 , A61K38/21
CPC分类号： C07D405/12 , C07D405/14 , C07D409/14 , C07D471/04 , C07D487/04
摘要： Compounds useful as Rho kinase inhibitors of formula (I): wherein variable are as defined herein are provided. Methods of treatment of malconditions mediated by Rho kinase, and methods of preparation of the compounds, are also provided.
摘要翻译： 可用作式（I）的Rho激酶抑制剂的化合物：其中变量如本文所定义。 还提供了由Rho激酶介导的病症治疗方法和化合物的制备方法。
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公开(公告)号：US09162981B2
公开(公告)日：2015-10-20
申请号：US13636415
申请日：2011-03-23
IPC分类号： C07D209/34 , A61K31/55 , A61K31/454 , A61K31/496 , A61K31/439 , A61K45/06 , A61K31/404 , A61K31/5377 , C07D403/06 , C07D453/02 , C07D403/14 , C07D495/04
CPC分类号： A61K31/404 , A61K31/439 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D209/34 , C07D403/06 , C07D403/14 , C07D453/02 , C07D495/04 , A61K2300/00
摘要： Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.
摘要翻译： 公开了用于治疗与神经变性或眼部疾病相关的病症的化合物，组合物，试剂盒和方法。
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公开(公告)号：US20110150833A1
公开(公告)日：2011-06-23
申请号：US12746776
申请日：2008-12-18
申请人： Yangbo Feng , Philip LoGrasso , Thomas Bannister , Thomas Schroeter , Yen Ting Chen , Yan Yin , Hampton Sessions , Michael P. Smolinski , Lei Yao , Bo Wang , Bozena Frackowiak-Wojtasek
发明人： Yangbo Feng , Philip LoGrasso , Thomas Bannister , Thomas Schroeter , Yen Ting Chen , Yan Yin , Hampton Sessions , Michael P. Smolinski , Lei Yao , Bo Wang , Bozena Frackowiak-Wojtasek
IPC分类号： A61K31/4155 , C07D405/12 , A61K31/4433 , C07D405/14 , A61K31/496 , A61K31/506 , A61K31/519 , C07D471/02 , A61K31/4375 , A61K31/501 , A61K38/21 , A61K39/395 , A61K31/56 , A61P9/00 , A61P15/10 , A61P29/00 , A61P25/00 , A61P19/02 , A61P11/00 , A61P35/00 , A61P31/04
CPC分类号： C07D405/12 , C07D405/14 , C07D409/14 , C07D471/04 , C07D487/04
摘要： Compounds useful as Rho kinase inhibitors of formula (1) wherein the variables are as defined herein are provided. Methods of treatment of malconditions mediated by Rho kinase, and methods of preparation of the compounds, are also provided.
摘要翻译： 提供了可用作式（1）的Rho激酶抑制剂的化合物，其中变量如本文所定义。 还提供了由Rho激酶介导的病态治疗方法和化合物的制备方法。
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公开(公告)号：US09539239B1
公开(公告)日：2017-01-10
申请号：US14886938
申请日：2015-10-19
IPC分类号： A61K9/00 , A61K31/404 , A61K45/06 , C07D403/06
CPC分类号： A61K31/404 , A61K31/439 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D209/34 , C07D403/06 , C07D403/14 , C07D453/02 , C07D495/04 , A61K2300/00
摘要： Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.
摘要翻译： 公开了用于治疗与神经变性或眼部疾病相关的病症的化合物，组合物，试剂盒和方法。
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