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公开(公告)号:US07271165B2
公开(公告)日:2007-09-18
申请号:US11020870
申请日:2004-12-22
申请人: John H. van Duzer , Arthur F. Michaelis , William B. Geiss , Douglas G. Stafford , Joseph Raker , Xiang Y. Yu , James M. Siedlecki , Yingfei Yang
发明人: John H. van Duzer , Arthur F. Michaelis , William B. Geiss , Douglas G. Stafford , Joseph Raker , Xiang Y. Yu , James M. Siedlecki , Yingfei Yang
IPC分类号: C07D498/18 , A61K31/535 , A61K31/54
CPC分类号: C07D498/18 , C07D513/18 , C07D519/00
摘要: The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3′-hydroxy analogs, 4′- and/or 6′ halo and/or alkoxy analogs, and various 5′ substituents that incorporate a cyclic amine moiety.
摘要翻译: 本发明的特征是利福霉素类似物可用作治疗或预防各种微生物感染的治疗剂。 在一种形式中,类似物在25位被乙酰化,就像利福霉素一样。 在另一种形式中,类似物在25位脱乙酰化。 在其他形式中,苯并恶嗪利霉素,苯并噻嗪可的霉素和苯并二氮霉素霉素类似物在苯环的各个位置衍生化,包括3'-羟基类似物,4'-和/或6'卤素和/或烷氧基类似物,以及各种5'取代基 加入环胺部分。
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公开(公告)号:US20100273765A1
公开(公告)日:2010-10-28
申请号:US11821368
申请日:2007-06-21
申请人: John H. van Duzer , Arthur F. Michaelis , William B. Geiss , Douglas G. Stafford , Joseph Raker , Xiang Y. Yu , James M. Siedlecki , Yingfei Yang
发明人: John H. van Duzer , Arthur F. Michaelis , William B. Geiss , Douglas G. Stafford , Joseph Raker , Xiang Y. Yu , James M. Siedlecki , Yingfei Yang
IPC分类号: A61K31/397 , C07D413/14 , A61K31/496 , A61K31/542 , A61K31/5383 , A61K31/4985 , A61K31/551 , A61P29/00 , A61P31/04 , A61P7/02 , A61P3/06 , A61P9/10 , A61P31/10 , A61P31/12 , A61P31/00
CPC分类号: C07D498/18 , C07D513/18 , C07D519/00
摘要: The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3′-hydroxy analogs, 4′- and/or 6′ halo and/or alkoxy analogs, and various 5′ substituents that incorporate a cyclic amine moiety.
摘要翻译: 本发明的特征是利福霉素类似物可用作治疗或预防各种微生物感染的治疗剂。 在一种形式中,类似物在25位被乙酰化,就像利福霉素一样。 在另一种形式中,类似物在25位脱乙酰化。 在其他形式中,苯并恶嗪利霉素,苯并噻嗪可的霉素和苯并二氮霉素霉素类似物在苯环的各个位置衍生化,包括3'-羟基类似物,4'-和/或6'卤素和/或烷氧基类似物,以及各种5'取代基 加入环胺部分。
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公开(公告)号:US07547692B2
公开(公告)日:2009-06-16
申请号:US11638756
申请日:2006-12-14
申请人: John H. van Duzer , Arthur F. Michaelis , William B. Geiss , Douglas G. Stafford , Joseph Raker , Xiang Y. Yu , James M. Siedlecki , Yingfei Yang
发明人: John H. van Duzer , Arthur F. Michaelis , William B. Geiss , Douglas G. Stafford , Joseph Raker , Xiang Y. Yu , James M. Siedlecki , Yingfei Yang
IPC分类号: C07D498/18 , A61K31/535 , A61P31/04
CPC分类号: C07D498/18 , C07D519/00
摘要: The present invention features rifamycin analogs and methods of using these compounds to treat a variety of microbial infections.
摘要翻译: 本发明特征为利福霉素类似物和使用这些化合物治疗各种微生物感染的方法。
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公开(公告)号:US07220738B2
公开(公告)日:2007-05-22
申请号:US11008597
申请日:2004-12-09
申请人: John H. van Duzer , Arthur F. Michaelis , William B. Geiss , Douglas G. Stafford , Xiang Y. Yu , James M. Siedlecki , Yingfei Yang
发明人: John H. van Duzer , Arthur F. Michaelis , William B. Geiss , Douglas G. Stafford , Xiang Y. Yu , James M. Siedlecki , Yingfei Yang
IPC分类号: C07D498/14 , C07D491/14 , A61K31/542 , A61K31/498 , A61P31/04
CPC分类号: C07D498/16 , C07D498/22 , C07D513/22
摘要: The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3′-hydroxy analogs, and/or various fused ring systems with the benzene ring at the 4′,5′ or 5′,6′ positions.
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公开(公告)号:US07494991B2
公开(公告)日:2009-02-24
申请号:US11804141
申请日:2007-05-17
申请人: John H. van Duzer , Arthur F. Michaelis , William B. Geiss , Douglas G. Stafford , Xiang Y. Yu , James M. Siedlecki , Yingfei Yang
发明人: John H. van Duzer , Arthur F. Michaelis , William B. Geiss , Douglas G. Stafford , Xiang Y. Yu , James M. Siedlecki , Yingfei Yang
IPC分类号: C07D498/14 , C07D491/14 , A61K31/542 , A61K31/498 , A61P31/04
CPC分类号: C07D498/16 , C07D498/22 , C07D513/22
摘要: The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3′-hydroxy analogs, and/or various fused ring systems with the benzene ring at the 4′,5′ or 5′,6′ positions.
摘要翻译: 本发明的特征是利福霉素类似物可用作治疗或预防各种微生物感染的治疗剂。 在一种形式中,类似物在25位被乙酰化,就像利福霉素一样。 在另一种形式中,类似物在25位脱乙酰化。 在其它形式中,苯并恶嗪利霉素,苯并噻嗪可霉素和苯并二氮霉素类似物在苯环的不同位置衍生化,包括3'-羟基类似物和/或各种稠合环体系,其中苯环为4',5'或5' ,6'位。
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公开(公告)号:US07342011B2
公开(公告)日:2008-03-11
申请号:US10915919
申请日:2004-08-11
申请人: John H. van Duzer , Arthur F. Michaelis , William B. Geiss , Douglas G. Stafford , Joseph Raker
发明人: John H. van Duzer , Arthur F. Michaelis , William B. Geiss , Douglas G. Stafford , Joseph Raker
IPC分类号: C07D498/18 , A61K31/535 , A61P31/54
CPC分类号: C07D498/18 , C07D491/18 , C07D513/18 , C07D519/00
摘要: The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3′-hydroxy analogs, 4′- and/or 6′ halo and/or alkoxy analogs, and various 5′ substituents that incorporate a cyclic amine moiety.
摘要翻译: 本发明的特征是利福霉素类似物可用作治疗或预防各种微生物感染的治疗剂。 在一种形式中,类似物在25位被乙酰化,就像利福霉素一样。 在另一种形式中,类似物在25位脱乙酰化。 在其他形式中,苯并恶嗪利霉素,苯并噻嗪可的霉素和苯并二氮霉素霉素类似物在苯环的各个位置衍生化,包括3'-羟基类似物,4'-和/或6'卤素和/或烷氧基类似物,以及各种5'取代基 加入环胺部分。
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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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公开(公告)号:US08440667B2
公开(公告)日:2013-05-14
申请号:US12632151
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
发明人: Scott A. Mitchell , Kevin S. Currie , Peter A. Blomgren , Jeffrey E. Kropf , Seung H. Lee , Jianjun Xu , Douglas G. Stafford
IPC分类号: A61K31/495
CPC分类号: C07D519/00 , A61K9/0053 , C07D471/04 , C07D487/04 , G01N2333/9121
摘要: Certain imidazopyrazines of Formula (I): and pharmaceutical compositions thereof are provided herein. Methods of treating patients responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity of Formula (I) 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。 治疗响应于抑制Syk活性的患者的方法,其包括给予这些患者一定数量的至少一种有效减少疾病或病症体征或症状的式(I)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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9.
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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