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21. 发明申请

US20090082330A1 CERTAIN SUBSTITUTED AMIDES, METHOD OF MAKING, AND METHOD OF USE THEREOF 有权
标题翻译：某些替代的制剂，制备方法及其使用方法
公开(公告)号：US20090082330A1
公开(公告)日：2009-03-26
申请号：US12234281
申请日：2008-09-19
申请人： Peter A. BLOMGREN , Kevin S. Currie , Seung H. Lee , Scott A. Mitchell , Jianjun Xu , Aaron C. Schmitt , Zhongdong Zhao , Pavel E. Zhichkin , Douglas G. Stafford , Jeffrey E. Kropf
发明人： Peter A. BLOMGREN , Kevin S. Currie , Seung H. Lee , Scott A. Mitchell , Jianjun Xu , Aaron C. Schmitt , Zhongdong Zhao , Pavel E. Zhichkin , Douglas G. Stafford , Jeffrey E. Kropf
IPC分类号： C07D403/14 , C07D403/02 , C07D409/02 , C07D407/14 , C07D401/14 , C07D413/14 , A61K31/497 , A61K31/496 , A61K31/5377 , A61P29/00 , A61P37/00 , C12N5/06 , C12Q1/48 , A61P35/00 , A61P19/00
CPC分类号： C07D409/12 , C07D241/08
摘要： Compounds of Formula I that inhibit Btk are described herein. Pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.
摘要翻译：本文描述了抑制Btk的式I化合物。描述了包含至少一种式I化合物的药物组合物以及选自载体，佐剂和赋形剂的至少一种药学上可接受的载体。描述了治疗患有某些对Btk活性和/或B细胞活性的抑制作出反应的某些疾病的患者的方法。描述了确定样品中Btk的存在的方法。

22. 发明授权

US06916830B2 Substituted tetrahydroisoquinolines as C5a receptor modulators 失效
标题翻译：取代的四氢异喹啉作为C5a受体调节剂
公开(公告)号：US06916830B2
公开(公告)日：2005-07-12
申请号：US10824826
申请日：2004-04-15
申请人： Kyungae Lee , Scott A. Mitchell , Robert Ohliger , LuYan Zhang , He Zhao , Kevin S. Currie
发明人： Kyungae Lee , Scott A. Mitchell , Robert Ohliger , LuYan Zhang , He Zhao , Kevin S. Currie
IPC分类号： A61K31/47 , C07D211/14 , C07D211/70 , C07D217/04 , C07D217/14 , C07D221/20 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/04 , C07D417/12 , C07D495/04 , C07D211/68 , A61K31/44
CPC分类号： C07D221/20 , A61K31/47 , C07D211/14 , C07D211/70 , C07D217/04 , C07D217/14 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/04 , C07D417/12 , C07D495/04
摘要： Substituted tetrahydroisoquinolines and related compounds are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies:
摘要翻译：提供了取代的四氢异喹啉和相关化合物。这些化合物是可用于在体内或体外调节C5a受体活性的配体，并且特别可用于治疗与人类，驯养的伴侣动物和家畜中的病理性C5a受体激活相关的病症。还提供了使用它们治疗这些病症的药物组合物和方法，以及使用这些配体进行受体定位研究的方法：

23. 发明授权

US09562056B2 Imidazopyridines Syk inhibitors 有权
标题翻译：咪唑并吡啶类Syk抑制剂
公开(公告)号：US09562056B2
公开(公告)日：2017-02-07
申请号：US13806094
申请日：2011-03-11
申请人： Peter A. Blomgren , Kevin S. Currie , Jeffrey E. Kropf , Seung H. Lee , Scott A. Mitchell , Aaron C. Schmitt , Jianjun Xu , Zhongdong Zhao
发明人： Peter A. Blomgren , Kevin S. Currie , Jeffrey E. Kropf , Seung H. Lee , Scott A. Mitchell , Aaron C. Schmitt , Jianjun Xu , Zhongdong Zhao
IPC分类号： C07D471/04 , C07D519/00 , C07D498/04 , C07D487/04 , C12Q1/48
CPC分类号： A61K31/69 , A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/498 , A61K31/4985 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/538 , A61K31/5383 , C07D471/04 , C07D487/04 , C07D498/04 , C07D519/00 , C12Q1/485
摘要： Certain imidazopyridines (I) and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
摘要翻译：本文提供了某些咪唑并吡啶（I）及其药物组合物。治疗患有某些对抑制Syk活性有作用的疾病和病症的患者的方法，其包括给予这些患者一定量的至少一种有效减少疾病或病症体征或症状的化学实体。还提供了用于确定样品中Syk激酶的存在或不存在的方法。

24. 发明授权

US08598174B2 Pyridazinones, method of making, and method of use thereof 有权
标题翻译：哒嗪酮，制法及其使用方法
公开(公告)号：US08598174B2
公开(公告)日：2013-12-03
申请号：US13128726
申请日：2009-11-12
申请人： Antonio J. M. Barbosa, Jr. , Peter A. Blomgren , Kevin S. Currie , Seung Lee , Jeffrey E. Kropf , Scott A. Mitchell , Daniel Ortwine , William M. Rennells , Aaron C. Schmitt , Jianjun Xu , Wendy B. Young , Zhongdong Zhao , Pavel E. Zhichkin
发明人： Antonio J. M. Barbosa, Jr. , Peter A. Blomgren , Kevin S. Currie , Seung Lee , Jeffrey E. Kropf , Scott A. Mitchell , Daniel Ortwine , William M. Rennells , Aaron C. Schmitt , Jianjun Xu , Wendy B. Young , Zhongdong Zhao , Pavel E. Zhichkin
IPC分类号： A61K31/50 , A61K31/501 , C07D237/30
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , C07D498/04 , C07D513/04 , C07D519/00
摘要： Compounds of Formula I that inhibit Btk are described herein. Pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.
摘要翻译：本文描述了抑制Btk的式I化合物。描述了包含至少一种式I化合物的药物组合物以及选自载体，佐剂和赋形剂的至少一种药学上可接受的载体。描述了治疗患有某些对Btk活性和/或B细胞活性的抑制作出反应的某些疾病的患者的方法。描述了确定样品中Btk的存在的方法。

25. 发明申请

US20130210802A1 IMIDAZOPYRIDINES SYK INHIBITORS 有权
标题翻译：咪唑吡啶SYK抑制剂
公开(公告)号：US20130210802A1
公开(公告)日：2013-08-15
申请号：US13806094
申请日：2011-03-11
申请人： Peter A. Blomgren , Kevin S. Currie , Jeffrey E. Kropf , Seung H. Lee , Scott A. Mitchell , Aaron C. Schmitt , Jianjun Xu , Zhongdong Zhao
发明人： Peter A. Blomgren , Kevin S. Currie , Jeffrey E. Kropf , Seung H. Lee , Scott A. Mitchell , Aaron C. Schmitt , Jianjun Xu , Zhongdong Zhao
IPC分类号： C07D498/04 , C07D471/04 , C12Q1/48 , C07D487/04
CPC分类号： A61K31/69 , A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/498 , A61K31/4985 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/538 , A61K31/5383 , C07D471/04 , C07D487/04 , C07D498/04 , C07D519/00 , C12Q1/485
摘要： Certain imidazopyridines (I) and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
摘要翻译：本文提供了某些咪唑并吡啶（I）及其药物组合物。治疗患有某些对抑制Syk活性有作用的疾病和病症的患者的方法，其包括给予这些患者一定量的至少一种有效减少疾病或病症体征或症状的化学实体。还提供了用于确定样品中Syk激酶的存在或不存在的方法。

26. 发明授权

US08426424B2 Certain substituted amides, method of making, and method of use thereof 有权
标题翻译：某些取代的酰胺，制备方法及其使用方法
公开(公告)号：US08426424B2
公开(公告)日：2013-04-23
申请号：US12991232
申请日：2009-05-06
申请人： Peter A. Blomgren , David R. Brittelli , Kevin S. Currie , Seung H. Lee , Jeffrey E. Kropf , Scott A. Mitchell , Aaron C. Schmitt , Xiaojing Wang , Jianjun Xu , Zhongdong Zhao , Pavel E. Zhichkin
发明人： Peter A. Blomgren , David R. Brittelli , Kevin S. Currie , Seung H. Lee , Jeffrey E. Kropf , Scott A. Mitchell , Aaron C. Schmitt , Xiaojing Wang , Jianjun Xu , Zhongdong Zhao , Pavel E. Zhichkin
IPC分类号： A61K31/4965 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00
CPC分类号： C07D409/12 , C07D213/74 , C07D241/20 , C07D409/14 , C07D417/12 , C07D487/04
摘要： The invention relates to compounds of the following Formula I wherein R1, R2, Z, W, and D are defined herein, that inhibit Btk and therefore are useful in the treatment of diseases responsive to inhibition of Btk activity such as cancer. The invention also relates to pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, as well as methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described, and methods for determining the presence of Btk in a sample.
摘要翻译：本发明涉及下式I的化合物，其中R1，R2，Z，W和D在本文中定义，其抑制Btk，因此可用于治疗对抑制Btk活性如癌症的疾病。本发明还涉及包含至少一种式I化合物的药物组合物，以及选自载体，佐剂和赋形剂的至少一种药学上可接受的载体的方法，以及治疗患有某些对Btk活性抑制作用的患者的患者的方法和/或B细胞活性，以及用于确定样品中Btk存在的方法。

27. 发明授权

US08058446B2 Certain substituted amides, method of making, and method of use thereof 有权
标题翻译：某些取代的酰胺，制备方法及其使用方法
公开(公告)号：US08058446B2
公开(公告)日：2011-11-15
申请号：US11853485
申请日：2007-09-11
申请人： Peter A. Blomgren , Kevin S. Currie , Jeffrey E. Kropf , Tony Lee , James W. Darrow , Scott A. Mitchell , Jianjun Xu , Aaron C. Schmitt
发明人： Peter A. Blomgren , Kevin S. Currie , Jeffrey E. Kropf , Tony Lee , James W. Darrow , Scott A. Mitchell , Jianjun Xu , Aaron C. Schmitt
IPC分类号： C07D409/00 , A61K31/44
CPC分类号： C07D213/64 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： At least one chemical entity chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof is described herein. Pharmaceutical compositions comprising at least one chemical entity of the invention, together with at least one pharmaceutically acceptable vehicle chosen from carriers adjuvants, and excipients, are described.Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.
摘要翻译：本文描述了至少一种选自式1化合物的化学实体及其可药用盐，溶剂合物，螯合物，非共价复合物，前药及其混合物。描述了包含本发明的至少一个化学实体的药物组合物以及选自载体佐剂和赋形剂的至少一种药学上可接受的载体。描述了治疗患有某些对Btk活性和/或B细胞活性的抑制作出反应的某些疾病的患者的方法。描述了确定样品中Btk的存在的方法。

28. 发明申请

US20100160292A1 Kinase Inhibitors, and Methods of Using and Identifying Kinase Inhibitors 审中-公开
标题翻译：激酶抑制剂和使用和鉴定激酶抑制剂的方法
公开(公告)号：US20100160292A1
公开(公告)日：2010-06-24
申请号：US12440695
申请日：2007-09-11
申请人： James A. Whitney , Julie Di Paolo , Mark Velleca , David R. Brittelli , Kevin S. Currie , James W. Darrow , Jeffrey E. Krope , Seung H. Lee , Steven L. Gallion , Scott A. Mitchell , Doughlas A.I. Pippen , Peter A. Blomgren , Doughlas Gregory Stafford
发明人： James A. Whitney , Julie Di Paolo , Mark Velleca , David R. Brittelli , Kevin S. Currie , James W. Darrow , Jeffrey E. Krope , Seung H. Lee , Steven L. Gallion , Scott A. Mitchell , Doughlas A.I. Pippen , Peter A. Blomgren , Doughlas Gregory Stafford
IPC分类号： A61K31/4418 , G01N33/53 , C12N9/96 , C12N5/00 , A61K31/553 , A61K31/551 , A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/4965 , A61K31/4545 , C07D403/12 , C07D413/12 , C07D241/20 , C07D401/12 , C07D213/72 , A61P37/00
CPC分类号： A61K31/00 , A61K31/44 , A61K31/4965 , A61K31/497 , A61K31/4985 , A61K31/5377 , C12Q1/485 , G01N2500/04
摘要： Methods of inhibiting BTK activity by inhibiting phosphorylation of Y551 of BTK, methods of treating patients by inhibiting BTK activity by inhibiting phosphorylation of Y551 of BTK, chemical entities that bind to BTK and inhibited complexes are provided.
摘要翻译：通过抑制BTK的Y551的磷酸化抑制BTK活性的方法，提供了通过抑制BTK的Y551的磷酸化，结合BTK的化学实体和抑制复合物来抑制BTK活性来治疗患者的方法。

29. 发明申请

US20090221612A1 CERTAIN SUBSTITUTED AMIDES, METHOD OF MAKING, AND METHOD OF USE THEREOF 审中-公开
标题翻译：某些替代的制剂，制备方法及其使用方法
公开(公告)号：US20090221612A1
公开(公告)日：2009-09-03
申请号：US12370103
申请日：2009-02-12
申请人： Scott A. Mitchell , Kevin S. Currie , Peter A. Blomgren , David M. Armistead , Joseph Raker
发明人： Scott A. Mitchell , Kevin S. Currie , Peter A. Blomgren , David M. Armistead , Joseph Raker
IPC分类号： A61K31/519 , C07D487/04 , A61P35/00
CPC分类号： C07D487/04
摘要： Certain chemical entities chosen from compounds represented by Formula I and pharmaceutically acceptable salts and mixtures thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer (e.g., B-cell lymphoma and leukemia), autoimmune diseases, inflammatory diseases, acute inflammatory reactions, and allergic disorders. Methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
摘要翻译：在本文中提供了选自由式I表示的化合物的某些化学实体及其药学上可接受的盐及其混合物。包含至少一种化学实体和一种或多种药学上可接受的载体的药物组合物。公开了治疗患有对抑制Syk活性有反应的某些疾病和病症的患者的方法，所述方法包括向所述患者施用一定量的至少一种有效减少疾病或病症体征或症状的化学实体。这些疾病包括癌症（例如B细胞淋巴瘤和白血病），自身免疫疾病，炎性疾病，急性炎症反应和过敏性疾病。治疗方法包括给予至少一种化学实体作为单一活性剂或与一种或多种其它治疗剂组合施用至少一种化学实体。还提供了用于确定样品中Syk激酶的存在或不存在的方法。

30. 发明授权

US08455493B2 Imidazopyrazine Syk inhibitors 有权
标题翻译：咪唑吡嗪Syk抑制剂
公开(公告)号：US08455493B2
公开(公告)日：2013-06-04
申请号：US12632140
申请日：2009-12-07
申请人： Scott A. Mitchell , Kevin S. Currie , Peter A. Blomgren , Jeffrey E. Kropf , Seung H. Lee , Jianjun Xu , Douglas G. Stafford , James P. Harding , Antonio J. M. Barbosa, Jr. , Zhongdong Zhao , Soumya Mitra , David M. Armistead
发明人： Scott A. Mitchell , Kevin S. Currie , Peter A. Blomgren , Jeffrey E. Kropf , Seung H. Lee , Jianjun Xu , Douglas G. Stafford , James P. Harding , Antonio J. M. Barbosa, Jr. , Zhongdong Zhao , Soumya Mitra , David M. Armistead
IPC分类号： A61K31/495
CPC分类号： C07D487/04 , A61K31/495 , C07D471/04 , C07D491/107 , C07D498/04 , C07D519/00 , C12Q1/485 , G01N33/573 , G01N2333/91205
摘要： Certain imidazopyrazines of Formula (I) and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
摘要翻译：本文提供了式（I）的某些咪唑并嗪及其药物组合物。治疗患有某些对抑制Syk活性有作用的疾病和病症的患者的方法，其包括给予这些患者一定量的至少一种有效减少疾病或病症体征或症状的化学实体。还提供了用于确定样品中Syk激酶的存在或不存在的方法。

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