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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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12.发明申请公开(公告)号：US20080153834A1
公开(公告)日：2008-06-26
申请号：US11853502
申请日：2007-09-11
申请人： Peter A. Blomgren , Seung H. Lee , Scott A. Mitchell , Jianjun Xu , Aaron C. Schmitt , Jeffrey E. Kropf , Kevin S. Currie
发明人： Peter A. Blomgren , Seung H. Lee , Scott A. Mitchell , Jianjun Xu , Aaron C. Schmitt , Jeffrey E. Kropf , Kevin S. Currie
IPC分类号： A61K31/501 , C07D211/86 , A61K31/4412 , C07D413/14 , A61P35/00 , C12N5/06 , A61P37/00 , C12Q1/48 , A61K31/5377 , C07D401/14
CPC分类号： C07D401/12 , C07D401/14 , C07D405/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D495/04 , C07D498/04 , C12Q1/485
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。
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公开(公告)号：US20080125417A1
公开(公告)日：2008-05-29
申请号：US11853488
申请日：2007-09-11
申请人： Kevin S. Currie , Tony Lee , James W. Darrow , Peter A. Blomgren
发明人： Kevin S. Currie , Tony Lee , James W. Darrow , Peter A. Blomgren
IPC分类号： A61K31/541 , C07D295/00 , C07D239/02 , A61K31/496 , C12Q1/48 , A61P29/00 , A61P37/00 , A61P35/00 , C12N5/00 , A61K31/505 , A61K31/5377
CPC分类号： C07D239/42 , C07D401/12 , C07D403/12 , C07D409/12 , C07D409/14
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 Formula 1, 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药学上可接受的盐，溶剂合物，螯合物，非共价复合物，前药及其混合物。 描述了包含至少一种式1的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。
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14.发明申请公开(公告)号：US20130281432A1
公开(公告)日：2013-10-24
申请号：US13819864
申请日：2011-08-31
申请人： Kevin S. Currie , Xiaojing Wang , Wendy B. Young
发明人： Kevin S. Currie , Xiaojing Wang , Wendy B. Young
IPC分类号： C07D401/14 , C07D495/04 , C07D487/04 , C07D403/14 , C07D513/04 , C07D498/04 , A61K45/06 , A61K31/5377 , A61K31/497 , A61K31/4985 , A61K31/4439 , A61K31/506 , A61K31/501 , A61K31/542 , C07D413/14
CPC分类号： C07D401/14 , A61K31/4439 , A61K31/497 , A61K31/4985 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/542 , A61K45/06 , C07D401/10 , C07D403/14 , C07D413/14 , C07D487/04 , C07D495/04 , C07D498/04 , C07D513/04 , C07D519/00
摘要： Pyridone and pyrazinone compounds of Formula I 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： 式I的吡啶酮和吡嗪酮化合物包括可用于抑制Btk激酶和用于治疗免疫疾病如Btk激酶介导的炎症的立体异构体，互变异构体和其药学上可接受的盐。 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：US20110301145A1
公开(公告)日：2011-12-08
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 Kropf , Scott A. Mithchell , 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 Kropf , Scott A. Mithchell , Daniel Ortwine , William M. Rennells , Aaron C. Schmitt , Jianjun Xu , Wendy B. Young , Zhongdong Zhao , Pavel E. Zhichkin
IPC分类号： A61K31/5377 , C07D487/04 , C07D495/04 , C07D413/14 , C07D401/14 , C07D403/14 , C07D403/12 , C07D417/14 , C07D405/14 , C07D498/04 , A61K31/506 , A61K31/501 , A61K31/5383 , A61K31/55 , A61P35/00 , A61P35/02 , A61P29/00 , A61P37/08 , A61P19/08 , C12N5/071 , C12Q1/70 , G01N33/573 , C07D409/14
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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17.发明授权公开(公告)号：US07947835B2
公开(公告)日：2011-05-24
申请号：US11371180
申请日：2006-03-09
申请人： David R. Brittelli , Kevin S. Currie , James W. Darrow , Jeffrey E. Kropf , Seung H. Lee , Steven L. Gallion , Scott A. Mitchell , Douglas A. I. Pippin , Peter A. Blomgren , Douglas Gregory Stafford
发明人： David R. Brittelli , Kevin S. Currie , James W. Darrow , Jeffrey E. Kropf , Seung H. Lee , Steven L. Gallion , Scott A. Mitchell , Douglas A. I. Pippin , Peter A. Blomgren , Douglas Gregory Stafford
IPC分类号： C07D403/12 , C07D403/14 , C07D401/12 , C07D401/14 , A61K31/501 , A61P17/06
CPC分类号： C07D213/74 , C07D241/20 , C07D241/24 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/04
摘要： At least one chemical entity chosen from compounds of Formula 2 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2化合物的化学实体及其药学上可接受的盐，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。
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18.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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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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公开(公告)号：US20100222323A1
公开(公告)日：2010-09-02
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
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
IPC分类号： A61K31/5377 , C07D487/04 , A61K31/495 , G01N33/53 , C12N5/02 , A61K31/538 , A61K31/553
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 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.
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