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公开(公告)号：US20080114004A1
公开(公告)日：2008-05-15
申请号：US11871472
申请日：2007-10-12
申请人： Guozhang Xu , Lily Searle , Shenlin Huang
发明人： Guozhang Xu , Lily Searle , Shenlin Huang
IPC分类号： A61K31/497 , C07D401/12 , A61P35/00 , A61P17/06 , A61P17/00 , A61P19/02 , A61P25/00
CPC分类号： C07D403/12
摘要： The present invention is directed to novel bicyclic pyrimidine compounds of Formula (I) or a form or composition thereof as inhibitors of ATP-protein kinase interactions, wherein substituents on each side of the iminomethyl double bond in Formula (I) may be in the E or Z configuration; and wherein R1, R2, R3 and R4 are as defined herein.
摘要翻译： 本发明涉及式（I）的新型双环嘧啶化合物或其形式或组成作为ATP-蛋白激酶相互作用的抑制剂，其中式（I）中亚氨基甲基双键各侧的取代基可以在E 或Z配置; 并且其中R 1，R 2，R 3和R 4都如本文所定义。
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公开(公告)号：US20070254896A1
公开(公告)日：2007-11-01
申请号：US11690305
申请日：2007-03-23
申请人： Jeannene Butler , Peter Connolly , Angel Fuentes-Pesquera , Lee Greenberger , Shenlin Huang , Kenneth LaMontagne , Ronghua Li , Guozhang Xu
发明人： Jeannene Butler , Peter Connolly , Angel Fuentes-Pesquera , Lee Greenberger , Shenlin Huang , Kenneth LaMontagne , Ronghua Li , Guozhang Xu
IPC分类号： A61K31/505 , A61P25/00 , A61P35/00 , C07D239/30 , C07D239/34
CPC分类号： C07D401/12 , C07D239/47 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/14 , C07D417/12
摘要： The present invention is directed to substituted pyrimidine compounds of formula (I): and forms thereof, their synthesis and use for treating a chronic or acute protein kinase mediated disease, disorder or condition.
摘要翻译： 本发明涉及式（I）的取代嘧啶化合物及其形式，其用于治疗慢性或急性蛋白激酶介导的疾病，病症或病症的合成和用途。
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公开(公告)号：US08013153B2
公开(公告)日：2011-09-06
申请号：US11690305
申请日：2007-03-23
申请人： Jeannene Butler , Peter J. Connolly , Angel R. Fuentes-Pesquera , Lee M. Greenberger , Shenlin Huang , Kenneth R. LaMontagne, Jr. , Ronghua Li , Guozhang Xu
发明人： Jeannene Butler , Peter J. Connolly , Angel R. Fuentes-Pesquera , Lee M. Greenberger , Shenlin Huang , Kenneth R. LaMontagne, Jr. , Ronghua Li , Guozhang Xu
IPC分类号： C07D403/12 , C07D403/14 , A61K31/506 , A61P19/02
CPC分类号： C07D401/12 , C07D239/47 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/14 , C07D417/12
摘要： The present invention is directed to substituted pyrimidine compounds of formula (I): and forms thereof, their synthesis and use for treating a chronic or acute protein kinase mediated disease, disorder or condition.
摘要翻译： 本发明涉及式（I）的取代嘧啶化合物及其形式，它们用于治疗慢性或急性蛋白激酶介导的疾病，病症或病症的合成和用途。
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公开(公告)号：US07893064B2
公开(公告)日：2011-02-22
申请号：US11871472
申请日：2007-10-12
申请人： Guozhang Xu , Lily Lee Searle , Shenlin Huang
发明人： Guozhang Xu , Lily Lee Searle , Shenlin Huang
IPC分类号： C07D403/12 , A61K31/506
CPC分类号： C07D403/12
摘要： The present invention is directed to novel bicyclic pyrimidine compounds of Formula (I) or a form or composition thereof as inhibitors of ATP-protein kinase interactions, wherein substituents on each side of the iminomethyl double bond in Formula (I) may be in the E or Z configuration; and wherein R1, R2, R3 and R4 are as defined herein.
摘要翻译： 本发明涉及式（I）的新型双环嘧啶化合物或其形式或组成作为ATP-蛋白激酶相互作用的抑制剂，其中式（I）中亚氨基甲基双键各侧的取代基可以在E 或Z配置; 并且其中R 1，R 2，R 3和R 4如本文所定义。
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5.发明授权N-(pyridin-2-yl)sulfonamides and compositions thereof as protein kinase inhibitors 有权N-（吡啶-2-基）磺酰胺及其组合物作为蛋白激酶抑制剂公开(公告)号：US09181238B2
公开(公告)日：2015-11-10
申请号：US13577209
申请日：2011-02-04
申请人： Shifeng Pan , John E. Tellew , Yongqin Wan , Yongping Xie , Xing Wang , Xia Wang , Shenlin Huang , Zuosheng Liu , Qiong Zhang
发明人： Shifeng Pan , John E. Tellew , Yongqin Wan , Yongping Xie , Xing Wang , Xia Wang , Shenlin Huang , Zuosheng Liu , Qiong Zhang
IPC分类号： A61K31/444 , C07D213/75 , C07D471/04 , C07D401/14 , A61K31/506 , A61K31/519 , A61K45/06
CPC分类号： C07D471/04 , A61K31/444 , A61K31/506 , A61K31/519 , A61K45/06 , C07D401/14
摘要： The invention provides a novel class of compounds of Formula (I) (wherein A, Y, R2, R3, R4 and R5 are defined in the summary of the invention), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf.
摘要翻译： 本发明提供了一类新颖的式（I）化合物（其中A，Y，R 2，R 3，R 4和R 5在本发明概述中定义），包含这些化合物的药物组合物和使用这些化合物治疗或 预防与异常或失调的激酶活性相关的疾病或病症，特别是涉及B-Raf异常活化的疾病或病症。
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公开(公告)号：US20140011825A1
公开(公告)日：2014-01-09
申请号：US14022540
申请日：2013-09-10
申请人： Abran Q. Costales , Shenlin Huang , Jeff Xianming Jin , Zuosheng Liu , Sabina Pecchi , Daniel Poon , John Tellew
发明人： Abran Q. Costales , Shenlin Huang , Jeff Xianming Jin , Zuosheng Liu , Sabina Pecchi , Daniel Poon , John Tellew
IPC分类号： C07D403/04 , A61K45/06 , A61K31/506
CPC分类号： C07D403/04 , A61K31/506 , A61K45/06
摘要： The present invention provides compounds of Formula I or II: wherein R1, R1b, R2, R3, R4, R5, R6 and R7 are defined herein. The compounds of Formula (I) or (II) and pharmaceutical compositions thereof are useful for the treatment of B-Raf-associated diseases.
摘要翻译： 本发明提供式I或II的化合物：其中R1，R1b，R2，R3，R4，R5，R6和R7如本文所定义。 式（I）或（II）的化合物及其药物组合物可用于治疗B-Raf相关疾病。
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公开(公告)号：US08202876B2
公开(公告)日：2012-06-19
申请号：US12444129
申请日：2007-09-24
申请人： Pamela Albaugh , Gregory B. Chopiuk , Qiang Ding , Shenlin Huang , Zuosheng Liu , Shifeng Pan , Pingda Ren , Xia Wang , Xing Wang , Yongping Xie , Chengzhi Zhang , Qiong Zhang , Guobao Zhang , Daniel Poon , Paul Renhowe , Martin Sendzik
发明人： Pamela Albaugh , Gregory B. Chopiuk , Qiang Ding , Shenlin Huang , Zuosheng Liu , Shifeng Pan , Pingda Ren , Xia Wang , Xing Wang , Yongping Xie , Chengzhi Zhang , Qiong Zhang , Guobao Zhang , Daniel Poon , Paul Renhowe , Martin Sendzik
IPC分类号： C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00 , C07D231/00 , C07D403/02 , A01N43/56 , A61K31/415
CPC分类号： C07D403/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D417/14
摘要： The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, ARG, BCR-Abl, BRK, EphB, Fms, Fyn, KDR, c-Kit, LCK, PDGF-R, b-Raf, c-Raf, SAPK2, Src, Tie2 and TrkB kinases.
摘要翻译： 本发明提供了一类新颖的化合物，包含这些化合物的药物组合物和使用这些化合物治疗或预防与异常或失调的激酶活性相关的疾病或病症的方法，特别是涉及Abl，ARG，BCR异常活化的疾病或病症 -Abl，BRK，EphB，Fms，Fyn，KDR，c-Kit，LCK，PDGF-R，b-Raf，c-Raf，SAPK2，Src，Tie2和TrkB激酶。
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公开(公告)号：US07888380B2
公开(公告)日：2011-02-15
申请号：US11245314
申请日：2005-10-06
申请人： Shenlin Huang , Ronghui Lin , Peter J. Connolly , Stuart L. Emanuel , Steven A. Middleton , Robert H. Gruninger , Steven K. Wetter
发明人： Shenlin Huang , Ronghui Lin , Peter J. Connolly , Stuart L. Emanuel , Steven A. Middleton , Robert H. Gruninger , Steven K. Wetter
IPC分类号： A61K31/4196 , A61K31/496 , A61K33/42 , C07D249/14 , C07D257/04 , C07F9/572 , C07F9/6515 , C07F9/6518 , C07F9/6509
CPC分类号： C07D403/12 , C07D249/14
摘要： 1,2,4-Triazolylaminoaryl(heteroaryl)sulfonamide derivatives of formula (I), pharmaceutically acceptable salts thereof, processes for the manufacture of 1,2,4-triazolylaminoaryl(heteroaryl)sulfonamide derivatives and pharmaceutical compositions containing 1,2,4-triazolylaminoaryl(heteroaryl)sulfonamide derivatives are disclosed: The 1,2,4-triazolylaminoaryl(heteroaryl)sulfonamide derivatives of formula (I) possess cell cycle inhibitory activity and are accordingly useful for their anti cell proliferation (such as anti cancer) activity.
摘要翻译： 式（I）的1,2,4-三唑基氨基芳基（杂芳基）磺酰胺衍生物，其药学上可接受的盐，制备1,2,4-三唑基氨基芳基（杂芳基）磺酰胺衍生物的方法和含有1,2,4-三唑基氨基芳基 三唑基氨基芳基（杂芳基）磺酰胺衍生物：式（I）的1,2,4-三唑基氨基芳基（杂芳基）磺酰胺衍生物具有细胞周期抑制活性，因此可用于其抗细胞增殖（如抗癌）活性。
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9.发明授权Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders 有权用于治疗激酶障碍的嘧啶基取代的稠合吡咯基化合物公开(公告)号：US07855205B2
公开(公告)日：2010-12-21
申请号：US11260986
申请日：2005-10-28
IPC分类号： C07D403/04 , A61K31/407
CPC分类号： C07D471/04
摘要： The present invention provides pyrimidinyl substituted fused-pyrrolyl compounds of Formula (I) and pharmaceutical compositions comprising the compounds and methods of synthesis and use thereof. The compounds are kinase inhibitors useful in treating or ameliorating a kinase mediated, angiogenesis-mediated or hyperproliferative disorder. The invention thus also provides a therapeutic or prophylactic method of use for the compounds and/or pharmaceutical compositions to treat such disorders.
摘要翻译： 本发明提供式（I）的嘧啶基取代的稠合吡咯基化合物和包含该化合物的药物组合物及其合成和使用方法。 该化合物是可用于治疗或改善激酶介导的血管生成介导的或过度增殖性疾病的激酶抑制剂。 因此，本发明还提供了用于治疗这些疾病的化合物和/或药物组合物的治疗或预防方法。
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公开(公告)号：US07317031B2
公开(公告)日：2008-01-08
申请号：US11047800
申请日：2005-02-01
申请人： Ronghui Lin , Shenlin Huang , Steven K. Wetter , Peter J. Connolly , Stuart L. Emanuel , Robert H. Gruninger , Steven A. Middleton
发明人： Ronghui Lin , Shenlin Huang , Steven K. Wetter , Peter J. Connolly , Stuart L. Emanuel , Robert H. Gruninger , Steven A. Middleton
IPC分类号： A61K31/41 , C07D249/14
CPC分类号： C07D401/06 , A61K31/4178 , A61K31/4196 , A61K31/427 , A61K31/4439 , C07D249/14 , C07D405/06 , C07D409/06 , C07D409/14 , C07D413/06 , C07D417/06
摘要： The present invention provides substituted triazole diamine derivatives as selective kinase or dual-kinase inhibitors and a method for treating or ameliorating a selective kinase or dual-kinase mediated disorder.
摘要翻译： 本发明提供了作为选择性激酶或双重激酶抑制剂的取代的三唑二胺衍生物以及治疗或改善选择性激酶或双重激酶介导的病症的方法。
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