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公开(公告)号：US07645778B2
公开(公告)日：2010-01-12
申请号：US11333050
申请日：2006-01-17
申请人： James C. Sutton , Zulan Pi , Rejean Ruel , Alexandre L'Heureux , Carl Thibault , Patrick Y. S. Lam
发明人： James C. Sutton , Zulan Pi , Rejean Ruel , Alexandre L'Heureux , Carl Thibault , Patrick Y. S. Lam
IPC分类号： A61K31/4436 , C07D417/12
CPC分类号： C07D213/74 , C07D213/75 , C07D213/80 , C07D277/42 , C07D277/56 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/04 , C07D513/04
摘要： The present invention provides novel heteroaryl compounds and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.
摘要翻译： 本发明提供了新的杂芳基化合物及其类似物，它们是人P2Y1受体的选择性抑制剂。 本发明还提供了相同的各种药物组合物以及治疗对P2Y1受体活性调节作用的疾病的方法。
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公开(公告)号：US08273772B2
公开(公告)日：2012-09-25
申请号：US12619702
申请日：2009-11-17
申请人： James C. Sutton , Zulan Pi , Rejean Ruel , Alexandre L'Heureux , Carl Thibeault , Patrick Y. S. Lam
发明人： James C. Sutton , Zulan Pi , Rejean Ruel , Alexandre L'Heureux , Carl Thibeault , Patrick Y. S. Lam
IPC分类号： A61K31/4436 , C07D417/12
CPC分类号： C07D213/74 , C07D213/75 , C07D213/80 , C07D277/42 , C07D277/56 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/04 , C07D513/04
摘要： The present invention provides novel heteroaryl compounds and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.
摘要翻译： 本发明提供了新的杂芳基化合物及其类似物，它们是人P2Y1受体的选择性抑制剂。 本发明还提供了相同的各种药物组合物以及治疗对P2Y1受体活性调节作用的疾病的方法。
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3.发明申请UREA ANTAGONISTS OF P2Y1 RECEPTOR USEFUL IN THE TREATMENT OF THROMBOTIC CONDITIONS 有权P2Y1受体的尿素拮抗剂用于治疗血栓病症公开(公告)号：US20080280905A1
公开(公告)日：2008-11-13
申请号：US12117005
申请日：2008-05-08
申请人： Hannguang J. Chao , Huji Tuerdi , Timothy F. Herpin , Jaques Yves Roberge , Yalei Liu , R. Michael Lawrence , Robert P. Rehfuss , Charles G. Clark , Jennifer X. Qiao , Timur Gungor , Patrick Y. S. Lam , Tammy Wang , Rejean Ruel , Alexandre L'Heureux , Carl Thibeault , Gilles Bouthillier , Dora M. Schnur
发明人： Hannguang J. Chao , Huji Tuerdi , Timothy F. Herpin , Jaques Yves Roberge , Yalei Liu , R. Michael Lawrence , Robert P. Rehfuss , Charles G. Clark , Jennifer X. Qiao , Timur Gungor , Patrick Y. S. Lam , Tammy Wang , Rejean Ruel , Alexandre L'Heureux , Carl Thibeault , Gilles Bouthillier , Dora M. Schnur
IPC分类号： A61K31/5377 , C07D213/72 , C07D413/12 , A61K31/4412 , A61K31/4439 , A61K31/4709 , A61P7/00 , A61P9/00 , A61K31/4725 , A61K31/444 , A61K31/4545 , A61K31/496 , C07D401/12
CPC分类号： C07D409/14 , C07C275/30 , C07C275/32 , C07D213/40 , C07D213/75 , C07D213/89 , C07D231/40 , C07D231/50 , C07D237/22 , C07D333/36 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07F7/1804
摘要： The present invention provides novel pyridyl or phenyl ureas and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.
摘要翻译： 本发明提供了新的吡啶基或苯基脲及其类似物，它们是人P2Y 1受体的选择性抑制剂。 本发明还提供了相同的各种药物组合物以及治疗对P2Y受体活性的调节作用的疾病的方法。
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4.发明授权Urea antagonists of P2Y1receptor useful in the treatment of thrombotic conditions 有权P2Y1受体的尿素拮抗剂可用于治疗血栓形成公开(公告)号：US07674828B2
公开(公告)日：2010-03-09
申请号：US12117005
申请日：2008-05-08
申请人： Hannguang J. Chao , Huji Tuerdi , Timothy F. Herpin , Jacques Y. Roberge , Yalei Liu , Michael R. Lawrence , Robert P. Rehfuss , Charles G. Clark , Jennifer X. Qiao , Timur Gungor , Patrick Y. S. Lam , Tammy C. Wang , Rejean Ruel , Alexandre L'Heureux , Carl Thibeault , Gilles Bouthillier , Dora M. Schnur
发明人： Hannguang J. Chao , Huji Tuerdi , Timothy F. Herpin , Jacques Y. Roberge , Yalei Liu , Michael R. Lawrence , Robert P. Rehfuss , Charles G. Clark , Jennifer X. Qiao , Timur Gungor , Patrick Y. S. Lam , Tammy C. Wang , Rejean Ruel , Alexandre L'Heureux , Carl Thibeault , Gilles Bouthillier , Dora M. Schnur
IPC分类号： A61K31/155 , C07C275/28
CPC分类号： C07D409/14 , C07C275/30 , C07C275/32 , C07D213/40 , C07D213/75 , C07D213/89 , C07D231/40 , C07D231/50 , C07D237/22 , C07D333/36 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07F7/1804
摘要： The present invention provides novel pyridyl or phenyl ureas and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.
摘要翻译： 本发明提供了作为人P2Y1受体的选择性抑制剂的新颖的吡啶基或苯基脲及其类似物。 本发明还提供了相同的各种药物组合物以及治疗对P2Y1受体活性调节作用的疾病的方法。
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5.发明授权Urea antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions 有权P2Y1受体的尿素拮抗剂可用于治疗血栓形成公开(公告)号：US07388021B2
公开(公告)日：2008-06-17
申请号：US11126915
申请日：2005-05-10
申请人： Hannguang J. Chao , Huji Tuerdi , Timothy F. Herpin , Jacques Yves Roberge , Yalei Liu , R. Michael Lawrence , Robert P. Rehfuss , Charles G. Clark , Jennifer X. Qiao , Timur Gungor , Patrick Y. S. Lam , Tammy Wang , Rejean Ruel , Alexandre L'Heureux , Carl Thibeault , Gilles Bouthillier , Dora M. Schnur
发明人： Hannguang J. Chao , Huji Tuerdi , Timothy F. Herpin , Jacques Yves Roberge , Yalei Liu , R. Michael Lawrence , Robert P. Rehfuss , Charles G. Clark , Jennifer X. Qiao , Timur Gungor , Patrick Y. S. Lam , Tammy Wang , Rejean Ruel , Alexandre L'Heureux , Carl Thibeault , Gilles Bouthillier , Dora M. Schnur
IPC分类号： A61K31/4412 , A61K31/444 , C07D213/60 , C07D213/72
CPC分类号： C07D409/14 , C07C275/30 , C07C275/32 , C07D213/40 , C07D213/75 , C07D213/89 , C07D231/40 , C07D231/50 , C07D237/22 , C07D333/36 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07F7/1804
摘要： The present invention provides novel pyridyl or phenyl ureas and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.
摘要翻译： 本发明提供了新的吡啶基或苯基脲及其类似物，它们是人P2Y 1受体的选择性抑制剂。 本发明还提供了相同的各种药物组合物以及治疗对P2Y受体活性的调节作用的疾病的方法。
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6.发明授权Sulfonyl-amidino-containing and tetrahydropyrimidino-containing compounds as factor Xa inhibitors 有权含磺酰基 - 脒基和四氢嘧啶基的化合物作为因子Xa抑制剂公开(公告)号：US07122557B2
公开(公告)日：2006-10-17
申请号：US10801518
申请日：2004-03-16
IPC分类号： A61K31/437 , C07D471/04
CPC分类号： C07D213/75 , C07D207/16 , C07D209/30 , C07D231/14 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/04 , C07D413/12 , C07D471/04
摘要： The present application describes sulfonyl-amidino-containing and tetrahydropyrimidino-containing compounds and derivatives thereof of Formula I: P4-P-M-M4I or pharmaceutically acceptable salt forms thereof, wherein M is a ring, P is an optional ring, and P4 and M4 are as defined below. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
摘要翻译： 本申请描述了具有式I的含磺酰基脒基和四氢嘧啶基的化合物及其衍生物：<？在线公式描述=“在线公式”end =“lead”→> P < 或其药学上可接受的盐形式，其中M是环，P是或其药学上可接受的盐形式，其中M是环，P是 可选环，P 4和M 4如下所定义。 本发明的化合物可用作胰蛋白酶样丝氨酸蛋白酶的抑制剂，特别是因子Xa。
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7.发明授权Lactam-containing compounds and derivatives thereof as factor Xa inhibitors 有权含有内酰胺的化合物及其衍生物作为因子Xa抑制剂公开(公告)号：US07005435B2
公开(公告)日：2006-02-28
申请号：US10970781
申请日：2004-10-21
IPC分类号： C07D471/04 , A61K31/4162 , A61P7/02
CPC分类号： C07D413/14 , A61K31/4365 , A61K31/616 , A61K45/06 , C07D211/40 , C07D211/76 , C07D213/64 , C07D213/75 , C07D213/81 , C07D213/82 , C07D239/10 , C07D241/08 , C07D265/10 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/14 , C07D471/04 , C07D495/04 , A61K2300/00
摘要： The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P—M—M4I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5–7 membered carbocycle or heterocycle and ring M is a 5–7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
摘要翻译： 本申请描述了含有内酰胺的化合物及其衍生物
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公开(公告)号：US06602871B2
公开(公告)日：2003-08-05
申请号：US10007195
申请日：2001-12-04
申请人： Patrick Y. S. Lam , Charles G. Clark , John M. Fevig , Robert A. Galemmo , Qi Han , Irina C. Jacobson , Renhau Li , Donald J. P. Pinto , Ruth R. Wexler
发明人： Patrick Y. S. Lam , Charles G. Clark , John M. Fevig , Robert A. Galemmo , Qi Han , Irina C. Jacobson , Renhau Li , Donald J. P. Pinto , Ruth R. Wexler
IPC分类号： C07D47104
CPC分类号： C07D213/74 , C07D221/04 , C07D401/04 , C07D401/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D471/04 , C07D491/04 , C07D495/04
摘要： This invention relates generally to inhibitors of trypsin-like serine protease enzymes, especially factor Xa or thrombin, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders.
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公开(公告)号：US06403583B1
公开(公告)日：2002-06-11
申请号：US09469835
申请日：1999-12-22
申请人： Patrick Y. S. Lam , Charles G. Clark , John M. Fevig , Robert A. Galemmo , Qi Han , Irina C. Jacobson , Renhau Li , Donald J. P. Pinto , Ruth R. Wexler
发明人： Patrick Y. S. Lam , Charles G. Clark , John M. Fevig , Robert A. Galemmo , Qi Han , Irina C. Jacobson , Renhau Li , Donald J. P. Pinto , Ruth R. Wexler
IPC分类号： C07D40300
CPC分类号： C07D213/74 , C07D221/04 , C07D401/04 , C07D401/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D471/04 , C07D491/04 , C07D495/04
摘要： This invention relates generally to inhibitors of trypsin-like serine protease enzymes, especially factor Xa or thrombin, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders.
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公开(公告)号：US08901115B2
公开(公告)日：2014-12-02
申请号：US14236968
申请日：2012-08-06
申请人： Patrick Y. S. Lam , Charles G. Clark , James R. Corte , William R. Ewing , Paul J. Gilligan , Yoon Jeon , Wu Yang , Leon M. Smith, II , Yufeng Wang
发明人： Patrick Y. S. Lam , Charles G. Clark , James R. Corte , William R. Ewing , Paul J. Gilligan , Yoon Jeon , Wu Yang , Leon M. Smith, II , Yufeng Wang
IPC分类号： C07D471/06 , C07D487/06 , A61K31/505 , A61K31/5365 , A61K31/4985 , A61P7/00 , C07D498/06
CPC分类号： C07D498/08 , C07D471/06 , C07D471/08 , C07D487/06 , C07D487/08 , C07D498/06
摘要： The present invention provides compounds of Formula (Ia): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
摘要翻译： 本发明提供式（Ia）化合物或其立体异构体，互变异构体或其药学上可接受的盐，其中所有变量如本文所定义。 这些化合物是选择性因子XIa抑制剂或FXIa和血浆激肽释放酶的双重抑制剂。 本发明还涉及包含这些化合物的药物组合物和使用其制备血栓栓塞和/或炎症性疾病的方法。
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