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公开(公告)号：US06919369B2
公开(公告)日：2005-07-19
申请号：US10224114
申请日：2002-08-19
申请人： Ignacio Aliagas-Martin , Dean R. Artis , Michael S. Dina , John A. Flygare , Richard A. Goldsmith , Regina A. Munroe , Alan G. Olivero , Richard Pastor , Thomas E. Rawson , Kirk D. Robarge , Daniel P. Sutherlin , Kenneth J. Weese , Aihe Zhou , Yan Zhu
发明人： Ignacio Aliagas-Martin , Dean R. Artis , Michael S. Dina , John A. Flygare , Richard A. Goldsmith , Regina A. Munroe , Alan G. Olivero , Richard Pastor , Thomas E. Rawson , Kirk D. Robarge , Daniel P. Sutherlin , Kenneth J. Weese , Aihe Zhou , Yan Zhu
IPC分类号： C07D333/34 , A61K31/18 , A61K31/196 , A61K31/216 , A61K31/381 , A61P7/02 , A61P9/10 , C07C257/18 , C07C311/05 , C07C311/08 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/51
CPC分类号： C07C257/18 , C07C311/05 , C07C311/08 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/51
摘要： Compounds having the structure shown below are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.
摘要翻译： 具有如下结构的化合物可用于抑制丝氨酸蛋白酶，例如TF /因子VIIa，因子Xa，凝血酶和激肽释放酶。 这些化合物可用于预防和/或治疗凝血障碍的方法。
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公开(公告)号：US06472393B1
公开(公告)日：2002-10-29
申请号：US09509104
申请日：2000-03-21
申请人： Ignacio Aliagas-Martin , Dean R. Artis , Michael S. Dina , John A. Flygare , Richard A. Goldsmith , Regina A. Munroe , Alan G. Olivero , Richard Pastor , Thomas E. Rawson , Kirk D. Robarge , Daniel P. Sutherlin , Kenneth J. Weese , Aihe Zhou , Yan Zhu
发明人： Ignacio Aliagas-Martin , Dean R. Artis , Michael S. Dina , John A. Flygare , Richard A. Goldsmith , Regina A. Munroe , Alan G. Olivero , Richard Pastor , Thomas E. Rawson , Kirk D. Robarge , Daniel P. Sutherlin , Kenneth J. Weese , Aihe Zhou , Yan Zhu
IPC分类号： A61K3118
CPC分类号： C07C257/18 , C07C311/05 , C07C311/08 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/51
摘要： Compounds having the structure shown below wherein A, B, N1, N2, X, Y, Q, R2, R5 and R6 are as defined herein are useful to inhibit serine protease enzymes, such as TF/factor VIIa factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.
摘要翻译： 具有下述结构的化合物其中A，B，N1，N2，X，Y，Q，R2，R5和R6如本文所定义，可用于抑制丝氨酸蛋白酶，如TF /因子VIIa因子Xa，凝血酶和激肽释放酶 。 这些化合物可用于预防和/或治疗凝血障碍的方法。
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公开(公告)号：US20050186198A1
公开(公告)日：2005-08-25
申请号：US11088511
申请日：2005-03-24
申请人： Ignacio Aliagas-Martin , Dean Artis , Michael Dina , John Flygare , Richard Goldsmith , Regina Munroe , Alan Olivero , Richard Pastor , Thomas Rawson , Kirk Robarge , Daniel Sutherlin , Kenneth Weese , Aihe Zhou , Yan Zhu
发明人： Ignacio Aliagas-Martin , Dean Artis , Michael Dina , John Flygare , Richard Goldsmith , Regina Munroe , Alan Olivero , Richard Pastor , Thomas Rawson , Kirk Robarge , Daniel Sutherlin , Kenneth Weese , Aihe Zhou , Yan Zhu
IPC分类号： C07D333/34 , A61K31/18 , A61K31/196 , A61K31/216 , A61K31/381 , A61P7/02 , A61P9/10 , C07C257/18 , C07C311/05 , C07C311/08 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/51 , A61K38/48 , A61K31/445 , A61K31/54 , A61K31/60
CPC分类号： C07C257/18 , C07C311/05 , C07C311/08 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/51
摘要： Compounds having the structure shown below are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.
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公开(公告)号：US20070037813A1
公开(公告)日：2007-02-15
申请号：US11537482
申请日：2006-09-29
申请人： Ignacio Aliagas-Martin , Dean Artis , Michael Dina , John Flygare , Richard Goldsmith , Regina Munroe , Alan Olivero , Richard Pastor , Thomas Rawson , Kirk Robarge , Daniel Sutherlin , Kenneth Weese , Aihe Zhou , Yan Zhu
发明人： Ignacio Aliagas-Martin , Dean Artis , Michael Dina , John Flygare , Richard Goldsmith , Regina Munroe , Alan Olivero , Richard Pastor , Thomas Rawson , Kirk Robarge , Daniel Sutherlin , Kenneth Weese , Aihe Zhou , Yan Zhu
IPC分类号： A61K31/50 , A61K31/44 , A61K31/165 , C07D237/02
CPC分类号： C07C257/18 , C07C311/05 , C07C311/08 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/51
摘要： Compounds having the structure shown below are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.
摘要翻译： 具有如下结构的化合物可用于抑制丝氨酸蛋白酶，例如TF /因子VIIa，因子Xa，凝血酶和激肽释放酶。 这些化合物可用于预防和/或治疗凝血障碍的方法。
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公开(公告)号：US08999998B2
公开(公告)日：2015-04-07
申请号：US13382145
申请日：2010-07-02
申请人： Paul Gibbons , Emily Hanan , Wendy Liu , Joseph P. Lyssikatos , Steven R. Magnuson , Rohan Mendonca , Richard Pastor , Thomas E. Rawson , Michael Siu , Mark Zak , Aihe Zhou , Bing-Yan Zhu
发明人： Paul Gibbons , Emily Hanan , Wendy Liu , Joseph P. Lyssikatos , Steven R. Magnuson , Rohan Mendonca , Richard Pastor , Thomas E. Rawson , Michael Siu , Mark Zak , Aihe Zhou , Bing-Yan Zhu
IPC分类号： C07D487/04 , A61K31/519
CPC分类号： C07D487/04
摘要： A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient are disclosed.
摘要翻译： 其中R 1，R 2和R 3在本文中定义的式I化合物，对映异构体，非对映异构体，互变异构体或其药学上可接受的盐可用作一种或多种Janus激酶的抑制剂。 公开了包含式I化合物和药学上可接受的载体，佐剂或媒介物的药物组合物，以及对患者中Janus激酶活性的抑制作出反应的疾病或病症的严重程度的治疗或减轻的方法。
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公开(公告)号：US20120190665A1
公开(公告)日：2012-07-26
申请号：US13382145
申请日：2010-07-02
申请人： Paul Gibbons , Emily Hanan , Wendy Liu , Joseph P. Lyssikatos , Steven R. Magnuson , Rohan Mendonca , Richard Pastor , Thomas E. Rawson , Michael Siu , Mark Zak , Aihe Zhou , Bing-Yan Zhu
发明人： Paul Gibbons , Emily Hanan , Wendy Liu , Joseph P. Lyssikatos , Steven R. Magnuson , Rohan Mendonca , Richard Pastor , Thomas E. Rawson , Michael Siu , Mark Zak , Aihe Zhou , Bing-Yan Zhu
IPC分类号： A61K31/519 , A61K31/5377 , A61P35/00 , A61P35/02 , A61P7/00 , A61P1/00 , A61P17/06 , A61P17/00 , A61P19/02 , C07D487/04 , A61P29/00
CPC分类号： C07D487/04
摘要： A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient are disclosed.
摘要翻译： 其中R 1，R 2和R 3在本文中定义的式I化合物，对映异构体，非对映异构体，互变异构体或其药学上可接受的盐可用作一种或多种Janus激酶的抑制剂。 公开了包含式I化合物和药学上可接受的载体，佐剂或媒介物的药物组合物，以及对患者中Janus激酶活性的抑制作出反应的疾病或病症的严重程度的治疗或减轻的方法。
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公开(公告)号：US08637526B2
公开(公告)日：2014-01-28
申请号：US13099179
申请日：2011-05-02
申请人： Jeffrey Blaney , Paul A. Gibbons , Emily Hanan , Joseph P. Lyssikatos , Steven R. Magnuson , Richard Pastor , Thomas E. Rawson , Aihe Zhou , Bing-Yan Zhu
发明人： Jeffrey Blaney , Paul A. Gibbons , Emily Hanan , Joseph P. Lyssikatos , Steven R. Magnuson , Richard Pastor , Thomas E. Rawson , Aihe Zhou , Bing-Yan Zhu
IPC分类号： A01N43/90 , A61K31/519 , C07D487/00
CPC分类号： C07D487/04
摘要： The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R7 and Z are defined herein, a pharmaceutical composition that includes a compound of Formula Ia and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a JAK kinase activity in a patient.
摘要翻译： 本发明提供了式Ia的JAK激酶抑制剂，其对映体，非对映异构体或其药学上可接受的盐，其中R1，R2，R7和Z在本文中定义，药物组合物包括式Ia化合物和药学上可接受的载体，佐剂或载体 以及对患者中JAK激酶活性的抑制作出反应的疾病或病症的严重程度的治疗或减轻的方法。
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公开(公告)号：US20120022043A1
公开(公告)日：2012-01-26
申请号：US13099179
申请日：2011-05-02
申请人： Jeffrey Blaney , Paul A. Gibbons , Emily Hanan , Joseph P. Lyssikatos , Steven R. Magnuson , Richard Pastor , Thomas E. Rawson , Aihe Zhou , Bing-Yan Zhu
发明人： Jeffrey Blaney , Paul A. Gibbons , Emily Hanan , Joseph P. Lyssikatos , Steven R. Magnuson , Richard Pastor , Thomas E. Rawson , Aihe Zhou , Bing-Yan Zhu
IPC分类号： A61K31/519 , A61K31/5377 , A61P37/00 , A61P37/06 , A61P11/06 , A61P17/06 , A61P17/00 , A61P25/00 , C07D487/04 , A61P29/00
CPC分类号： C07D487/04
摘要： The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R7 and Z are defined herein, a pharmaceutical composition that includes a compound of Formula Ia and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a JAK kinase activity in a patient.
摘要翻译： 本发明提供了式Ia的JAK激酶抑制剂，其对映体，非对映异构体或其药学上可接受的盐，其中R1，R2，R7和Z在本文中定义，药物组合物包括式Ia化合物和药学上可接受的载体，佐剂或载体 以及对患者中JAK激酶活性的抑制作出反应的疾病或病症的严重程度的治疗或减轻的方法。
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公开(公告)号：US08609687B2
公开(公告)日：2013-12-17
申请号：US13471269
申请日：2012-05-14
申请人： Bing-Yan Zhu , Michael Siu , Steven R. Magnuson , Richard Pastor , He Haiying , Xiao Yisong , Zheng Jifu , Xu Xing , Zhao Junping , Christopher Hurley , Jun Liang , Wendy Liu , Joseph P. Lyssikatos
发明人： Bing-Yan Zhu , Michael Siu , Steven R. Magnuson , Richard Pastor , He Haiying , Xiao Yisong , Zheng Jifu , Xu Xing , Zhao Junping , Christopher Hurley , Jun Liang , Wendy Liu , Joseph P. Lyssikatos
IPC分类号： A61K31/437 , C07D471/02
CPC分类号： C07D471/04 , A61K31/437 , A61K31/496 , A61K31/5377 , C07D487/04
摘要： A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed.
摘要翻译： 其中R 1，R 2，R 3，R 4和R 5在本文中定义的式I化合物，对映异构体，非对映异构体，互变异构体或其药学上可接受的盐可用作JAK激酶抑制剂。 公开了包含式I化合物和药学上可接受的载体，佐剂或载体的药物组合物，以及治疗或减轻对患者中JAK激酶活性的抑制作用的疾病或病症的严重程度的方法。
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公开(公告)号：US20120225855A1
公开(公告)日：2012-09-06
申请号：US13471269
申请日：2012-05-14
申请人： Bing-Yan Zhu , Michael Siu , Steven R. Magnuson , Richard Pastor , He Haiying , Xiao Yisong , Zheng Jifu , Xu Xing , Zhao Junping , Christopher Hurley , Jun Liang , Wendy Liu , Joseph P. Lyssikatos
发明人： Bing-Yan Zhu , Michael Siu , Steven R. Magnuson , Richard Pastor , He Haiying , Xiao Yisong , Zheng Jifu , Xu Xing , Zhao Junping , Christopher Hurley , Jun Liang , Wendy Liu , Joseph P. Lyssikatos
IPC分类号： C07D471/04 , A61K31/496 , A61K31/5377 , A61P9/00 , A61P3/10 , A61P37/00 , A61P25/00 , A61P1/16 , A61P37/08 , A61P25/28 , A61P19/08 , A61P31/00 , A61P35/04 , A61P35/02 , A61P9/10 , A61P25/16 , A61P17/00 , A61K31/437
CPC分类号： C07D471/04 , A61K31/437 , A61K31/496 , A61K31/5377 , C07D487/04
摘要： A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed.
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