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1.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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2.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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3.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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4.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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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：US07550499B2
公开(公告)日：2009-06-23
申请号：US11126567
申请日：2005-05-10
IPC分类号： A01N43/38 , A61K31/40 , A61K31/405 , C07D207/00 , C07D209/00 , C07D295/00
CPC分类号： C07D409/04 , C07D209/08 , C07D209/14 , C07D209/96 , C07D215/06 , C07D241/42 , C07D401/04 , C07D401/14 , C07D405/14 , C07D471/10
摘要： The present invention provides novel ureas containing N-aryl or N-heteroaryl substituted heterocycles 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： 本发明提供了含有N-芳基或N-杂芳基取代的杂环及其类似物的新型尿素，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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6.发明授权Lactam-containing cyclic diamines and derivatives as a factor Xa inhibitors 有权含内含物的环状二胺及其衍生物作为Xa因子抑制剂公开(公告)号：US07205318B2
公开(公告)日：2007-04-17
申请号：US10801469
申请日：2004-03-16
申请人： Jennifer X. Qiao , Tammy C. Wang , Gren Z. Wang , Timur Gungor
发明人： Jennifer X. Qiao , Tammy C. Wang , Gren Z. Wang , Timur Gungor
IPC分类号： A61K31/445 , C07D453/02
CPC分类号： C07D213/64 , C07D213/75 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12
摘要： The present application describes lactam-containing cyclic diamines and derivatives thereof of Formula I: P4-M-M4I or pharmaceutically acceptable salt forms thereof, wherein M is a non-aromatic 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环状二胺及其衍生物
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7.发明授权N-linked heterocyclic antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions 有权可用于治疗血栓形成条件的P2Y1受体的N-连接杂环拮抗剂公开(公告)号：US08329718B2
公开(公告)日：2012-12-11
申请号：US12761447
申请日：2010-04-16
申请人： Jennifer X. Qiao , Tammy C. Wang , James C. Sutton , Timur Gungor
发明人： Jennifer X. Qiao , Tammy C. Wang , James C. Sutton , Timur Gungor
IPC分类号： A61K31/44 , A61K31/425 , C07D209/54 , C07D409/10 , C07D401/02 , C07D233/54
CPC分类号： C07D471/10 , C07D401/04 , C07D401/12 , C07D417/12 , C07D417/14
摘要： The present invention provides novel ureas containing N-aryl or N-heteroaryl substituted heterocycles of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, D and W are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.
摘要翻译： 本发明提供了包含式（I）的N-芳基或N-杂芳基取代的杂环的新型脲：或其立体异构体，互变异构体，药学上可接受的盐或溶剂化物形式，其中变量A，B，D和W如本文所定义 。 这些化合物是可用作药物的人P2Y1受体的选择性抑制剂。
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8.发明授权3-arylquinazoline derivatives as selective estrogen receptor beta modulators 有权3-芳基喹唑啉衍生物作为选择性雌激素受体β调节剂公开(公告)号：US07381730B2
公开(公告)日：2008-06-03
申请号：US10387666
申请日：2003-03-13
申请人： Timur Gungor , James R. Corte
发明人： Timur Gungor , James R. Corte
IPC分类号： A61K31/517 , C07D239/88 , C07D239/93
CPC分类号： C07D273/00 , C07D209/38 , C07D239/91 , C07D401/04
摘要： Novel quinazoline derivatives possessing activity as estrogen receptor beta (ERβ) modulators are provided which have the general formula I wherein X is O or S; A and B are each independently CR′″ or N; R, R′ and R″ are each independently hydrogen, alkyl, benzyl, p-methoxybenzyl, allyl, or Si(R4)3, wherein at least one of R, R′ and R″ is hydrogen; R′″ is hydrogen, halogen, CF3, OR5, S(O)nR6, NR7R8, cycloalkyl or alkyl; R1, R2 and R3 are each independently hydrogen, halogen, CF3, OR5, S(O)nR6, NR7R8, cycloalkyl or alkyl; R4 is a alkyl; R5, R6, R7 and R8 in each functional group are each independently hydrogen, cycloalkyl or alkyl; and n is an integer from 0 to 2. In addition, a method is provided for preventing, inhibiting or treating the progression or onset of pathological conditions associated with the estrogen receptor and to pharmaceutical compositions containing such compounds.
摘要翻译： 提供具有雌激素受体β（ERbeta）调节剂活性的新型喹唑啉衍生物，其具有通式I，其中X为O或S; A和B各自独立地为CR“或N; R，R'和R“各自独立地为氢，烷基，苄基，对甲氧基苄基，烯丙基或Si（R 4 N 3）3，其中至少一个 R，R'和R“是氢; R“'是氢，卤素，CF 3或OR 5，S（O）n R 6 R 6， NR 7 R 8，环烷基或烷基; R 1，R 2和R 3各自独立地为氢，卤素，CF 3或OR 3， 5，S（O）n R 6，NR 7 R 8，环烷基或烷基 ; R 4是烷基; 各官能团中的R 5，R 6，R 7和R 8分别独立地为氢，环烷基或 烷基; n为0-2的整数。此外，提供了用于预防，抑制或治疗与雌激素受体相关的病理状况的进展或发作的方法以及含有这些化合物的药物组合物。
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9.发明申请LACTAM CONTAINING CYCLIC DIAMINES AND DERIVATIVES AS FACTOR XA INHIBITORS 审中-公开含有循环二氨基甲酸酯和衍生物的LACTAM作为因子XA抑制剂公开(公告)号：US20070135428A1
公开(公告)日：2007-06-14
申请号：US11675786
申请日：2007-02-16
申请人： Jennifer Qiao , Tammy Wang , Gren Wang , Timur Gungor
发明人： Jennifer Qiao , Tammy Wang , Gren Wang , Timur Gungor
IPC分类号： A61K31/538 , A61K31/501 , A61K31/517 , A61K31/496
CPC分类号： C07D213/64 , C07D213/75 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12
摘要： The present application describes lactam-containing cyclic diamines and derivatives thereof of Formula I: P4-M-M4 I or pharmaceutically acceptable salt forms thereof, wherein M is a non-aromatic 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环状二胺及其式I的衍生物：<？in-line-formula description =“In-line Formulas”end =“lead”？> P 其中M是非芳族碳环或杂环，其中M是非芳族碳环或杂环。 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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10.发明授权Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors 有权磺酰基氨基戊内酰胺及其衍生物作为因子Xa抑制剂公开(公告)号：US07169795B2
公开(公告)日：2007-01-30
申请号：US10952396
申请日：2004-09-28
申请人： Wei Han , Zilun Hu , Timur Gungor
发明人： Wei Han , Zilun Hu , Timur Gungor
IPC分类号： C07D487/12 , C07D401/04 , C07D403/14 , A61K31/445 , A61P7/02
CPC分类号： C07D401/04 , C07D207/38 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D495/04
摘要： The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula Ia–If: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
摘要翻译： 本申请描述了式Ia-If的磺酰基氨基戊内酰胺及其衍生物：或其药学上可接受的盐形式，其中环G是单环或双环碳环或杂环。 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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