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41. 发明申请

US20110098467A1 PYRROLO-TRIAZINE ANILINE COMPOUNDS USEFUL AS KINASE INHIBITORS 审中-公开
标题翻译：吡咯啉 - 三嗪化合物作为激酶抑制剂有用
公开(公告)号：US20110098467A1
公开(公告)日：2011-04-28
申请号：US12983048
申请日：2010-12-31
申请人： Alaric Dyckman , John Hynes , Katerina Leftheris , Chunjian Liu , Stephen T. Wrobleski
发明人： Alaric Dyckman , John Hynes , Katerina Leftheris , Chunjian Liu , Stephen T. Wrobleski
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, X and Z are as described in the specification.
摘要翻译：具有式（I）的化合物及其药学上可接受的盐，前药和溶剂合物可用作激酶抑制剂，其中R1，R2，R3，R4，R5，R6，X和Z如说明书中所述。

42. 发明授权

US07759343B2 Pyrrolo-triazine aniline compounds useful as kinase inhibitors 有权
标题翻译：用作激酶抑制剂的吡咯并三嗪苯胺化合物
公开(公告)号：US07759343B2
公开(公告)日：2010-07-20
申请号：US12259483
申请日：2008-10-28
申请人： Alaric Dyckman , John Hynes , Katerina Leftheris , Chunjian Liu , Stephen T. Wrobleski
发明人： Alaric Dyckman , John Hynes , Katerina Leftheris , Chunjian Liu , Stephen T. Wrobleski
IPC分类号： C07D487/04 , C07D403/12 , C07D413/08 , A61K31/53 , A61P9/10 , A61P19/02 , A61P19/04 , A61P35/00
CPC分类号： C07D487/04
摘要： Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, X and Z are as described in the specification.
摘要翻译：具有式（I）的化合物及其药学上可接受的盐，前药和溶剂合物可用作激酶抑制剂，其中R1，R2，R3，R4，R5，R6，X和Z如说明书中所述。

43. 发明授权

US07592338B2 Pyrazole-amine compounds useful as kinase inhibitors 有权
标题翻译：吡唑胺化合物可用作激酶抑制剂
公开(公告)号：US07592338B2
公开(公告)日：2009-09-22
申请号：US11832924
申请日：2007-08-02
申请人： Alaric J. Dyckman , Jagabandhu Das , Katerina Leftheris , Chunjian Liu , Robert V. Moquin , Stephen T. Wrobleski
发明人： Alaric J. Dyckman , Jagabandhu Das , Katerina Leftheris , Chunjian Liu , Robert V. Moquin , Stephen T. Wrobleski
IPC分类号： A61K31/4155 , A61K31/5377 , C07D403/02 , C07D413/02 , C07D231/56
CPC分类号： C07D231/14 , C07D231/12 , C07D231/40 , C07D401/12 , C07D413/12
摘要： The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where W, X, R1, R2, R3, R4, R5, R6 and m are as defined herein. The invention further pertains to pharmaceutical compositions containing at least one compound according to the invention useful for treating p38 kinase-associated conditions, and methods of inhibiting the activity of p38 kinase in a mammal.
摘要翻译：本发明提供了可用于治疗p38激酶相关病症的式（I）的吡唑衍生化合物，其中W，X，R 1，R 2，R 3，R 4，R 5，R 6和m如本文所定义。本发明还涉及含有至少一种可用于治疗p38激酶相关病症的本发明化合物的药物组合物，以及抑制哺乳动物中p38激酶活性的方法。

44. 发明授权

US07462616B2 Pyrrolo-triazine aniline compounds useful as kinase inhibitors 有权
标题翻译：用作激酶抑制剂的吡咯并三嗪苯胺化合物
公开(公告)号：US07462616B2
公开(公告)日：2008-12-09
申请号：US11585598
申请日：2006-10-24
申请人： Alaric J. Dyckman , John T. Hynes , Katerina Leftheris , Chunjian Liu , Stephen T. Wrobleski
发明人： Alaric J. Dyckman , John T. Hynes , Katerina Leftheris , Chunjian Liu , Stephen T. Wrobleski
IPC分类号： C07D487/04 , C07D403/12 , C07D413/08 , A61K31/53 , A61K31/5377 , A61P19/02 , A61P19/04 , A61P9/10 , A61P35/00
CPC分类号： C07D487/04
摘要： Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, X and Z are as described in the specification.
摘要翻译：具有式（I）的化合物及其药学上可接受的盐，前药和溶剂合物可用作激酶抑制剂，其中R1，R2，R3，R4，R5，R6，X和Z如说明书中所述。

45. 发明授权

US07414056B2 Pyrazole-amide compounds useful as kinase inhibitors 有权
标题翻译：用作激酶抑制剂的吡唑酰胺化合物
公开(公告)号：US07414056B2
公开(公告)日：2008-08-19
申请号：US10837778
申请日：2004-05-03
申请人： Alaric J. Dyckman , Jagabandhu Das , Katerina Leftheris , Chunjian Liu , Robert V. Moquin , Stephen T. Wrobleski
发明人： Alaric J. Dyckman , Jagabandhu Das , Katerina Leftheris , Chunjian Liu , Robert V. Moquin , Stephen T. Wrobleski
IPC分类号： A61K31/501 , C07F9/02 , C07D401/12 , C07D271/06 , C07D277/84
CPC分类号： C07D231/14 , C07D231/12 , C07D231/40 , C07D401/12 , C07D413/12
摘要： The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where G, X, R1, R2, R3, R4, R5, R6 and m are as defined herein. The invention further pertains to pharmaceutical compositions containing at least one compound according to the invention useful for treating p38 kinase-associated conditions, and methods of inhibiting the activity of p38 kinase in a mammal.
摘要翻译：本发明提供了可用于治疗p38激酶相关病症的式（I）的吡唑衍生化合物，其中G，X，R 1，R 2，R 2， R 3，R 4，R 5，R 6和m如本文所定义。本发明还涉及含有至少一种可用于治疗p38激酶相关病症的本发明化合物的药物组合物，以及抑制哺乳动物中p38激酶活性的方法。

46. 发明申请

US20070185175A1 Benzothiazole and azabenzothiazole compounds useful as kinase inhibitors 有权
标题翻译：可用作激酶抑制剂的苯并噻唑和氮杂苯并噻唑化合物
公开(公告)号：US20070185175A1
公开(公告)日：2007-08-09
申请号：US11494234
申请日：2006-07-27
申请人： Chunjian Liu , Katerina Leftheris , James Lin
发明人： Chunjian Liu , Katerina Leftheris , James Lin
IPC分类号： A61K31/428 , C07D417/02
CPC分类号： C07D513/04 , C07D417/04
摘要： A compound of Formula (I) or an enantiomer, diastereomer or a pharmaceutically-acceptable salt thereof, wherein A is independently selected from: further wherein R1, R2, R3, R4, R5, R6, R7, and W are as described herein. Also disclosed is a compound of Formula (II) or an enantiomer, diastereomer, or a pharmaceutically-acceptable salt thereof, wherein each of G, X and Y are independently CH or N, wherein at each occurrence at least one of G, X or Y is N and the other two of G, X or Y are CH; and B is independently selected from: further wherein R1, R2, R3, R4, R5, R8, R9 and Z are as described herein. Also disclosed are pharmaceutical compositions containing compounds of Formula (I) and Formula (II), and methods of treating conditions associated with the activity of p38 kinase.
摘要翻译：式（I）的化合物或其对映异构体，非对映异构体或其药学上可接受的盐，其中A独立地选自：其中R 1，R 2，R 2， R 4，R 4，R 5，R 6，R 7和/或R 4， W如本文所述。还公开了式（II）的化合物或其对映异构体，非对映异构体或其药学上可接受的盐，其中G，X和Y各自独立地为CH或N，其中在每次出现时，G，X或 Y为N，G，X或Y中的两个为CH; 并且B独立地选自：其中R 1，R 2，R 3，R 4，R 4，R 4， R 5，R 9，R 9和Z如本文所述。还公开了含有式（I）和式（II）化合物的药物组合物，以及治疗与p38激酶活性相关的病症的方法。

47. 发明申请

US20070093537A1 Thiazolyl-based compounds useful as kinase inhibitors 有权
标题翻译：可用作激酶抑制剂的噻唑基化合物
公开(公告)号：US20070093537A1
公开(公告)日：2007-04-26
申请号：US11633337
申请日：2006-12-04
申请人： John Hynes , Hong Wu , Katerina Leftheris , Chunjian Liu , Jagabandhu Das , Robert Moquin
发明人： John Hynes , Hong Wu , Katerina Leftheris , Chunjian Liu , Jagabandhu Das , Robert Moquin
IPC分类号： A61K31/426
CPC分类号： C07D277/56 , C07D417/12
摘要： The present invention provides thiazolyl-based compounds of formula (I), useful for treating p38 kinase-associated conditions, wherein ring A is phenyl or pyridyl, and X, Y, B, R2, R3, Z1 m and n are as defined herein. The invention further pertains to pharmaceutical compositions containing at least one compound according to the invention useful for treating p38 kinase-associated conditions, and methods of inhibiting the activity of p38 kinase in a mammal.
摘要翻译：本发明提供了可用于治疗p38激酶相关病症的式（I）的噻唑基类化合物，其中环A是苯基或吡啶基，X，Y，B，R 2， Z 3，Z 1和Z 3如本文所定义。本发明还涉及含有至少一种可用于治疗p38激酶相关病症的本发明化合物的药物组合物，以及抑制哺乳动物中p38激酶活性的方法。

48. 发明授权

US07169771B2 Thiazolyl-based compounds useful as kinase inhibitors 有权
公开(公告)号：US07169771B2
公开(公告)日：2007-01-30
申请号：US10773790
申请日：2004-02-06
申请人： John Hynes , Hong Wu , Katerina Leftheris , Chunjian Liu , Jagabandhu Das , Robert V. Moquin
发明人： John Hynes , Hong Wu , Katerina Leftheris , Chunjian Liu , Jagabandhu Das , Robert V. Moquin
IPC分类号： A61K31/425 , C07D277/20
CPC分类号： C07D277/56 , C07D417/12
摘要： The present invention provides thiazolyl-based compounds of formula (I), useful for treating p38 kinase-associated conditions, wherein ring A is phenyl or pyridyl, and X, Y, B, R2, R3, Z1 m and n are as defined herein. The invention further pertains to pharmaceutical compositions containing at least one compound according to the invention useful for treating p38 kinase-associated conditions, and methods of inhibiting the activity of p38 kinase in a mammal.

49. 发明授权

US07151113B2 Pyrazole-amine compounds useful as kinase inhibitors 有权
标题翻译：吡唑胺化合物可用作激酶抑制剂
公开(公告)号：US07151113B2
公开(公告)日：2006-12-19
申请号：US10838006
申请日：2004-05-03
申请人： Alaric J. Dyckman , Jagabandhu Das , Katerina Leftheris , Chunjian Liu , Robert V. Moquin , Stephen T. Wrobleski
发明人： Alaric J. Dyckman , Jagabandhu Das , Katerina Leftheris , Chunjian Liu , Robert V. Moquin , Stephen T. Wrobleski
IPC分类号： C07D271/113 , A61K31/4155
CPC分类号： C07D231/14 , C07D231/12 , C07D231/40 , C07D401/12 , C07D413/12
摘要： The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where W, X, R1, R2, R3, R4, R5, R6 and m are as defined herein. The invention further pertains to pharmaceutical compositions containing at least one compound according to the invention useful for treating p38 kinase-associated conditions, and methods of inhibiting the activity of p38 kinase in a mammal.
摘要翻译：本发明提供了可用于治疗p38激酶相关病症的式（I）的吡唑衍生化合物，其中W，X，R 1，R 2，R 2， R 3，R 4，R 5，R 6和m如本文所定义。本发明还涉及含有至少一种可用于治疗p38激酶相关病症的本发明化合物的药物组合物，以及抑制哺乳动物中p38激酶活性的方法。

50. 发明申请

US20060178388A1 Phenyl-substituted pyrimidine compounds useful as kinase inhibitors 审中-公开
标题翻译：可用作激酶抑制剂的苯基取代的嘧啶化合物
公开(公告)号：US20060178388A1
公开(公告)日：2006-08-10
申请号：US11344881
申请日：2006-02-01
申请人： Stephen Wrobleski , Shuqun Lin , Katerina Leftheris , Liqi He , Steven Seitz , Tai-An Lin , Wayne Vaccaro
发明人： Stephen Wrobleski , Shuqun Lin , Katerina Leftheris , Liqi He , Steven Seitz , Tai-An Lin , Wayne Vaccaro
IPC分类号： A61K31/506 , C07D239/32 , C07D403/02
CPC分类号： C07D417/14 , C07D401/04 , C07D413/04 , C07D417/04
摘要： Compounds having the formula (I), and pharmaceutically acceptable salts, and solvates thereof, are useful as kinase inhibitors, wherein: two of X1, X2, and X3 are N, and the remaining one of X1, X2, and X3 is —CR1; R1 is hydrogen or —CN; and N, G, Z, R2, R3, R4, R5, and R6 are described in the specification. Also disclosed are pharmaceutical compositions containing compounds of formula (I), and methods of treating conditions associated with the activity of p38 kinase and/or conditions associated with the activity of LIM kinase.
摘要翻译：具有式（I）的化合物及其药学上可接受的盐及其溶剂化物可用作激酶抑制剂，其中：X 1，X 2和X 2中的两个， SUB> 3 是N，X 1，X 2和X 3中的剩余的一个是-CR _{1 ; R 1是氢或-CN; 和N，G，Z，R 2，R 3，R 4，R 5和R 5， SUB> 6 在说明书中描述。还公开了含有式（I）化合物的药物组合物，以及治疗与p38激酶活性相关的病症和/或与LIM激酶活性相关的病症的方法。}

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