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公开(公告)号：US08618107B2
公开(公告)日：2013-12-31
申请号：US13102720
申请日：2011-05-06
申请人： Antonio J. M. Barbosa , Peter A. Blomgren , Kevin S. Currie , Ravi Krishnamoorthy , Jeffrey E. Kropf , Seung H. Lee , Scott A. Mitchell , Daniel Ortwine , Aaron C. Schmitt , Xiaojing Wang , Jianjun Xu , Wendy Young , Honglu Zhang , Zhongdong Zhao , Pavel E. Zhichkin
发明人： Antonio J. M. Barbosa , Peter A. Blomgren , Kevin S. Currie , Ravi Krishnamoorthy , Jeffrey E. Kropf , Seung H. Lee , Scott A. Mitchell , Daniel Ortwine , Aaron C. Schmitt , Xiaojing Wang , Jianjun Xu , Wendy Young , Honglu Zhang , Zhongdong Zhao , Pavel E. Zhichkin
IPC分类号： A61K31/50 , A61K31/501 , C07D487/00
CPC分类号： C07D519/00 , A61K31/497 , A61K31/4985 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/5377 , A61K31/5383 , A61K31/5386 , A61K31/551 , A61K45/06 , C07C69/65 , C07D209/52 , C07D471/14 , C07D487/04 , C07D495/04 , C07D498/04 , C07F5/04
摘要： Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译： 提供式I的吡啶酮和氮杂 - 吡啶酮化合物，包括其可用于抑制Btk激酶的立体异构体，互变异构体及其药学上可接受的盐，以及用于治疗免疫疾病如Btk激酶介导的炎症。 公开了使用式I化合物进行体外，原位和体内诊断以及哺乳动物细胞或相关病理学条件下的这些疾病的治疗的方法。
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公开(公告)号：US20120010191A1
公开(公告)日：2012-01-12
申请号：US13102720
申请日：2011-05-06
申请人： Antonio J.M. BARBOSA , Peter A. Blomgren , Kevin S. Currie , Ravi Krishnamoorthy , Jeffrey E. Kropf , Seung H. Lee , Scott A. Mitchell , Daniel Ortwine , Aaron C. Schmitt , Xiaojing Wang , Jianjun Xu , Wendy Young , Honglu Zhang , Zhongdong Zhao , Pavel E. Zhichkin
发明人： Antonio J.M. BARBOSA , Peter A. Blomgren , Kevin S. Currie , Ravi Krishnamoorthy , Jeffrey E. Kropf , Seung H. Lee , Scott A. Mitchell , Daniel Ortwine , Aaron C. Schmitt , Xiaojing Wang , Jianjun Xu , Wendy Young , Honglu Zhang , Zhongdong Zhao , Pavel E. Zhichkin
IPC分类号： A61K31/397 , A61K31/501 , C07D495/04 , A61K31/5025 , C07D487/04 , A61K31/551 , A61K31/4365 , C07D413/14 , A61K31/5377 , A61P29/00 , A61P19/02 , A61P9/00 , A61P35/00 , A61P37/06 , A61P11/06 , A61P25/00 , A61P11/00 , A61P17/06 , A61P35/02 , C07D401/14
CPC分类号： C07D519/00 , A61K31/497 , A61K31/4985 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/5377 , A61K31/5383 , A61K31/5386 , A61K31/551 , A61K45/06 , C07C69/65 , C07D209/52 , C07D471/14 , C07D487/04 , C07D495/04 , C07D498/04 , C07F5/04
摘要： Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译： 提供式I的吡啶酮和氮杂 - 吡啶酮化合物，包括其可用于抑制Btk激酶的立体异构体，互变异构体及其药学上可接受的盐，以及用于治疗免疫疾病如Btk激酶介导的炎症。 公开了使用式I化合物进行体外，原位和体内诊断以及哺乳动物细胞或相关病理学条件下的这些疾病的治疗的方法。
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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。
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4.发明申请公开(公告)号：US20110118233A1
公开(公告)日：2011-05-19
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： A61K31/553 , C07D403/14 , A61K31/497 , A61K31/496 , A61K31/501 , C07D413/14 , A61K31/5377 , A61K31/551 , C12N5/00 , C12Q1/48 , A61P35/00 , A61P19/08 , A61P37/08 , A61P37/02 , A61P29/00
CPC分类号： C07D409/12 , C07D213/74 , C07D241/20 , C07D409/14 , C07D417/12 , C07D487/04
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。
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5.发明授权公开(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。
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公开(公告)号：US20110059944A1
公开(公告)日：2011-03-10
申请号：US12939518
申请日：2010-11-04
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： A61K31/497 , A61K31/496 , A61K31/5377 , A61P35/00 , A61P37/00 , A61P29/00 , A61P37/08 , A61P35/02 , A61P19/02 , A61P21/04 , A61P11/06
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.
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7.发明申请公开(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。
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公开(公告)号：US07884108B2
公开(公告)日：2011-02-08
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： A61K31/4965
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。
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9.发明授权公开(公告)号：US08247550B2
公开(公告)日：2012-08-21
申请号：US12939518
申请日：2010-11-04
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： C07D241/36 , A61K31/4965
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。
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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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