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公开(公告)号：US08815872B2
公开(公告)日：2014-08-26
申请号：US13062413
申请日：2009-09-03
申请人： Henry Yu , Lizbeth Celeste De Selm , Xuliang Jiang , Benny C. Askew, Jr. , Srinivasa R. Karra , Andreas Goutopoulos
发明人： Henry Yu , Lizbeth Celeste De Selm , Xuliang Jiang , Benny C. Askew, Jr. , Srinivasa R. Karra , Andreas Goutopoulos
IPC分类号： A61K31/529 , C07D239/42 , C07D487/08 , C07D487/18 , C07D498/08 , C07D498/18 , C07D513/08 , C07D513/18 , C07D515/08
CPC分类号： C07D498/08 , C07D487/08 , C07D487/18 , C07D498/18 , C07D513/08 , C07D513/18 , C07D515/08
摘要： Macrocyclic derivative compounds that inhibit protein kinase enzymes are disclosed along with pharmaceutical compositions comprising these compounds and methods for synthesizing the same. Such compounds have utility in the treatment of proliferative diseases resulting from unregulated and/or disturbed kinase activity such as cancers, psoriasis, viral and bacterial infections, inflammatory and autoimmune diseases.
摘要翻译： 公开了抑制蛋白激酶的大环衍生物化合物以及包含这些化合物的药物组合物及其合成方法。 这些化合物可用于治疗由不稳定和/或受干扰的激酶活性如癌症，牛皮癣，病毒和细菌感染，炎性和自身免疫性疾病引起的增殖性疾病。
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公开(公告)号：US20140142097A1
公开(公告)日：2014-05-22
申请号：US14118845
申请日：2012-04-11
IPC分类号： C07D401/12 , A61K31/4545 , A61K31/5377 , C07D401/14 , A61K31/496 , A61K45/06 , A61K31/497 , A61K31/444 , A61K31/501 , C07D491/048 , C07D471/04 , C07D409/14 , C07D405/14
CPC分类号： C07D401/12 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/5377 , A61K45/06 , C07D401/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D471/04 , C07D491/048
摘要： Compounds of the formula (I) in which R, R1 and X have the meanings indicated in claim 1, are inhibitors of TBK1 and IKKε and can be employed, inter alia, for the treatment of cancer and inflammatory diseases
摘要翻译： 其中R，R 1和X具有权利要求1所示含义的式（I）化合物是TBK1和IKK的抑制剂; 并且可以用于治疗癌症和炎性疾病
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公开(公告)号：US20140107156A1
公开(公告)日：2014-04-17
申请号：US14105974
申请日：2013-12-13
申请人： Amanda E. Sutton , Thomas E. Richardson , Bayard R. Huck , Srinivasa R. Karra , Xiaoling Chen , Yufang Xiao , Andreas Goutopoulos , Ruoxi Lan , David Perrey , Harold George Vandeveer , Lesley Liu-Bujalski , Frank Steiber , Hui Qiu , Reinaldo C. Jones , Brian H. Heasley
发明人： Amanda E. Sutton , Thomas E. Richardson , Bayard R. Huck , Srinivasa R. Karra , Xiaoling Chen , Yufang Xiao , Andreas Goutopoulos , Ruoxi Lan , David Perrey , Harold George Vandeveer , Lesley Liu-Bujalski , Frank Steiber , Hui Qiu , Reinaldo C. Jones , Brian H. Heasley
IPC分类号： C07D215/04 , A61K31/47
CPC分类号： C07D215/04 , A61K31/47 , C07D239/94 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04
摘要： The invention provides novel substituted amino azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
摘要翻译： 本发明提供根据式（I）的新型取代的氨基氮杂环甲酰胺化合物，其用于治疗过度增殖性疾病如癌症的制备和用途。
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公开(公告)号：US20210214339A1
公开(公告)日：2021-07-15
申请号：US16756954
申请日：2018-10-17
发明人： Srinivasa R. KARRA , Yufang XIAO , Brian SHERER , Eugene CHECKLER
IPC分类号： C07D401/14 , C07D405/14 , C07D419/14 , C07D498/18
摘要： The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as TBK/IKKε inhibitors.
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公开(公告)号：US09273029B2
公开(公告)日：2016-03-01
申请号：US14118845
申请日：2012-04-11
IPC分类号： C07D401/12 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/5377 , A61K45/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D471/04 , C07D491/048 , C07D409/04
CPC分类号： C07D401/12 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/5377 , A61K45/06 , C07D401/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D471/04 , C07D491/048
摘要： Compounds of the formula (I) in which R, R1 and X have the meanings indicated in claim 1, are inhibitors of TBK1 and IKKε and can be employed, inter alia, for the treatment of cancer and inflammatory diseases
摘要翻译： 其中R，R 1和X具有权利要求1所示含义的式（I）化合物是TBK1和IKK的抑制剂; 并且可以用于治疗癌症和炎性疾病
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公开(公告)号：US09249114B2
公开(公告)日：2016-02-02
申请号：US14118756
申请日：2012-04-12
IPC分类号： C07D417/04 , C07D417/14 , C07D413/14 , C07D277/56 , A61K31/426 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K45/06 , A61N5/10
CPC分类号： C07D277/56 , A61K31/426 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K45/06 , A61N5/10 , C07D417/04 , C07D417/14
摘要： Compounds of the formula I in which R, R1, X and Y have the meanings indicated in Claim 1, are inhibitors of TBK1 and IKKε and can be employed, inter alia, for the treatment of cancer and inflammatory diseases.
摘要翻译： 其中R，R 1，X和Y具有权利要求1所示含义的式I化合物是TBK1和IKK的抑制剂; 并且可以用于治疗癌症和炎性疾病。
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公开(公告)号：US11440899B2
公开(公告)日：2022-09-13
申请号：US16756954
申请日：2018-10-17
发明人： Srinivasa R. Karra , Yufang Xiao , Brian Sherer , Eugene Checkler
IPC分类号： C07D401/14 , C07D405/14 , C07D419/14 , C07D498/18
摘要： The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as TBK/IKKε inhibitors.
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公开(公告)号：US08710044B2
公开(公告)日：2014-04-29
申请号：US13703276
申请日：2011-07-01
申请人： Bayard R. Huck , Constantin Neagu , Reinaldo Jones , Lizbeth Celeste DeSelm , Yufang Xiao , Srinivasa R. Karra , Ruoxi Lan , Igor Mochalkin , Amanda E. Sutton , Thomas E. Richardson
发明人： Bayard R. Huck , Constantin Neagu , Reinaldo Jones , Lizbeth Celeste DeSelm , Yufang Xiao , Srinivasa R. Karra , Ruoxi Lan , Igor Mochalkin , Amanda E. Sutton , Thomas E. Richardson
IPC分类号： A61K31/00 , A61K31/519 , C07D239/72
CPC分类号： C07D239/94 , A61K31/517 , A61K45/06 , C07D239/74 , C07D403/12
摘要： The invention provides novel bicyclic azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
摘要翻译： 本发明提供了根据式（I）的新型双环氮杂杂环甲酰胺化合物，其用于治疗过度增殖性疾病如癌症的制备和用途。
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公开(公告)号：US08637532B2
公开(公告)日：2014-01-28
申请号：US13148903
申请日：2010-02-04
申请人： Amanda E. Sutton , Ruoxi Lan , Thomas E. Richardson , David Perrey , Harold George Vandeveer , Bayard R. Huck , Srinivasa R. Karra , Xiaoling Chen , Yufang Xiao , Lesley Liu-Bujalski , Andreas Goutopoulos , Frank Stieber , Brian L. Hodous , Hui Qiu , Reinaldo Jones , Brian H. Heasley
发明人： Amanda E. Sutton , Ruoxi Lan , Thomas E. Richardson , David Perrey , Harold George Vandeveer , Bayard R. Huck , Srinivasa R. Karra , Xiaoling Chen , Yufang Xiao , Lesley Liu-Bujalski , Andreas Goutopoulos , Frank Stieber , Brian L. Hodous , Hui Qiu , Reinaldo Jones , Brian H. Heasley
IPC分类号： A01N43/54 , A61K31/517 , C07D239/72 , C07D401/00
CPC分类号： C07D215/04 , A61K31/47 , C07D239/94 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04
摘要： The invention provides novel substituted amino azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
摘要翻译： 本发明提供根据式（I）的新型取代的氨基氮杂环甲酰胺化合物，其用于治疗过度增殖性疾病如癌症的制备和用途。
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公开(公告)号：US08569295B2
公开(公告)日：2013-10-29
申请号：US13388952
申请日：2010-07-28
申请人： Xiaoling Chen , Srinivasa R. Karra , Bayard R. Huck , Ruoxi Lan , Amanda E. Sutton , Andreas Goutopoulos , Brian L. Hodous , Reinaldo Jones
发明人： Xiaoling Chen , Srinivasa R. Karra , Bayard R. Huck , Ruoxi Lan , Amanda E. Sutton , Andreas Goutopoulos , Brian L. Hodous , Reinaldo Jones
IPC分类号： C07D471/04 , C07D498/14 , A61K31/519
CPC分类号： C07D471/04 , C07D498/14
摘要： The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
摘要翻译： 本发明提供根据式（I）的新型取代的氮杂环化合物，其用于治疗过度增殖性疾病如癌症的制备和用途。
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