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公开(公告)号：US20070293491A1
公开(公告)日：2007-12-20
申请号：US11735302
申请日：2007-04-13
申请人： Cynthia Shafer , Annette Walter , Mika Lindvall , Thomas Gesner , Laura Doyle
发明人： Cynthia Shafer , Annette Walter , Mika Lindvall , Thomas Gesner , Laura Doyle
IPC分类号： A61K31/5375 , A61K31/44 , A61K31/445 , A61P35/00 , C07D239/20 , C07D295/00 , C07D241/02 , C07D213/02 , A61K31/496 , A61K31/506
CPC分类号： C07D403/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D471/04
摘要： New compounds capable of acting as CDC7 inhibitors are provided. The compounds are useful either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of CDC7 mediated diseases, such as cancer. The compounds have the Formula (I) or (II), where the values of the variables are defined herein.
摘要翻译： 提供能够作为CDC7抑制剂的新化合物。 该化合物可单独使用或与至少一种其它治疗剂组合用于预防或治疗CDC7介导的疾病例如癌症。 化合物具有式（I）或（II），其中变量的值在本文中定义。
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公开(公告)号：US20140249135A1
公开(公告)日：2014-09-04
申请号：US14273595
申请日：2014-05-09
申请人： Matthew Burger , Mika Lindvall , Wooseok Han , Jiong Lan , Gisele Nishiguchi , Cynthia Shafer , Cornelia Bellamacina , Kay Huh , Gordana Atallah , Christopher McBride , William Antonios-McCrea, JR. , Tatiana Zavorotinskaya , Annette Walter , Pablo Dominguez Garcia
发明人： Matthew Burger , Mika Lindvall , Wooseok Han , Jiong Lan , Gisele Nishiguchi , Cynthia Shafer , Cornelia Bellamacina , Kay Huh , Gordana Atallah , Christopher McBride , William Antonios-McCrea, JR. , Tatiana Zavorotinskaya , Annette Walter , Pablo Dominguez Garcia
IPC分类号： C07D401/12 , A61K31/55 , A61K31/497 , A61K31/4545 , A61K31/444 , C07D491/113 , C07D403/12 , A61K31/506 , C07D241/28 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D497/04 , C07D403/14 , A61K31/553
CPC分类号： C07D401/12 , A61K31/444 , A61K31/4545 , A61K31/497 , A61K31/506 , A61K31/55 , A61K31/553 , C07D241/24 , C07D241/28 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D491/113 , C07D497/04
摘要： New compounds, compositions and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
摘要翻译： 提供了在人或动物受试者中抑制与肿瘤发生相关的激酶活性的新化合物，组合物和方法。 在某些实施方案中，化合物和组合物有效抑制至少一种丝氨酸/苏氨酸激酶或受体酪氨酸激酶的活性。 新化合物和组合物可以单独使用或与至少一种另外的药剂组合使用，用于治疗丝氨酸/苏氨酸激酶或受体酪氨酸激酶介导的病症，例如癌症。
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公开(公告)号：US20120208815A1
公开(公告)日：2012-08-16
申请号：US12449701
申请日：2008-03-03
申请人： Matthew Burger , Mika Lindvall , Wooseok Han , Jiong Lan , Gisele Nishiguchi , Cynthia Shafer , Comelia Bellamacina , Kay Huh , Gordana Atallah , Christopher Mcbride , William Antonios-Mccrea, JR. , Tatiana Zavorotinskaya , Annette Walter , Pablo Garcia
发明人： Matthew Burger , Mika Lindvall , Wooseok Han , Jiong Lan , Gisele Nishiguchi , Cynthia Shafer , Comelia Bellamacina , Kay Huh , Gordana Atallah , Christopher Mcbride , William Antonios-Mccrea, JR. , Tatiana Zavorotinskaya , Annette Walter , Pablo Garcia
IPC分类号： A61K31/5377 , A61K31/4545 , A61P35/00 , C07D413/14 , A61K31/496 , C07D417/14 , A61K31/506 , A61K31/497 , C07D401/14 , C12N5/071
CPC分类号： C07D401/12 , C07D213/78 , C07D239/28
摘要： New compounds, compositions and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
摘要翻译： 提供了在人或动物受试者中抑制与肿瘤发生相关的激酶活性的新化合物，组合物和方法。 在某些实施方案中，化合物和组合物有效抑制至少一种丝氨酸/苏氨酸激酶或受体酪氨酸激酶的活性。 新化合物和组合物可以单独使用或与至少一种另外的药剂组合使用，用于治疗丝氨酸/苏氨酸激酶或受体酪氨酸激酶介导的病症，例如癌症。
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公开(公告)号：US08822497B2
公开(公告)日：2014-09-02
申请号：US12449701
申请日：2008-03-03
申请人： Matthew Burger , Mika Lindvall , Wooseok Han , Jiong Lan , Gisele Nishiguchi , Cynthia Shafer , Cornelia Bellamacina , Kay Huh , Gordana Atallah , Christopher McBride , William Antonios-McCrea, Jr. , Tatiana Zavorotinskaya , Annette Walter , Pablo Garcia
发明人： Matthew Burger , Mika Lindvall , Wooseok Han , Jiong Lan , Gisele Nishiguchi , Cynthia Shafer , Cornelia Bellamacina , Kay Huh , Gordana Atallah , Christopher McBride , William Antonios-McCrea, Jr. , Tatiana Zavorotinskaya , Annette Walter , Pablo Garcia
IPC分类号： A61K31/4545 , C07D401/14
CPC分类号： C07D401/12 , C07D213/78 , C07D239/28
摘要： New compounds, compositions and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
摘要翻译： 提供了在人或动物受试者中抑制与肿瘤发生相关的激酶活性的新化合物，组合物和方法。 在某些实施方案中，化合物和组合物有效地抑制至少一种丝氨酸/苏氨酸激酶或受体酪氨酸激酶的活性。 新化合物和组合物可以单独使用或与至少一种另外的药剂组合使用，用于治疗丝氨酸/苏氨酸激酶或受体酪氨酸激酶介导的病症，例如癌症。
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![Substituted pyrrolo[3,4-d]pyrimidines as kinase inhibitors](/abs-image/US/2017/01/17/US09546173B2/abs.jpg.150x150.jpg)
公开(公告)号：US09546173B2
公开(公告)日：2017-01-17
申请号：US14428546
申请日：2013-09-17
申请人： Michael Patrick Dillon , Mika Lindvall , Daniel Poon , Savithri Ramurthy , Vivek Rauniyar , Cynthia Shafer , Sharadha Subramanian , Huw Rowland Tanner
发明人： Michael Patrick Dillon , Mika Lindvall , Daniel Poon , Savithri Ramurthy , Vivek Rauniyar , Cynthia Shafer , Sharadha Subramanian , Huw Rowland Tanner
IPC分类号： A61K31/519 , C07D239/70 , C07D487/04 , C07D207/36 , A61K31/527 , A61K45/06 , C07D487/10
CPC分类号： C07D487/04 , A61K31/519 , A61K31/527 , A61K45/06 , C07D207/36 , C07D487/10
摘要： The present invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof; as further described herein. The present invention further provides pharmaceutical compositions comprising these compounds, and combinations comprising these compounds combined with or used with a therapeutic co-agent, as well as therapeutic uses of these compounds and compositions. These are useful in the treatment of diseases such as cancer that are associated with activation of ERK1 and/or ERK2, and especially for MAPK pathway dependent cancers showing resistance to Raf and/or MEK inhibitory cancer therapeutics.
摘要翻译： 本发明提供式（I）的化合物及其药学上可接受的盐; 如本文进一步描述的。 本发明还提供包含这些化合物的药物组合物，以及包含与治疗性助剂组合或与其一起使用的这些化合物的组合，以及这些化合物和组合物的治疗用途。 这些可用于治疗与ERK1和/或ERK2的激活相关的疾病，特别是对显示出对Raf和/或MEK抑制性癌症治疗剂的抗性的MAPK通路依赖性癌症的疾病的治疗
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公开(公告)号：US20150274733A1
公开(公告)日：2015-10-01
申请号：US14428546
申请日：2013-09-17
申请人： Michael Patrick DILLON , Mika LINDVALL , Daniel POON , Savithri RAMURTHY , Vivek RAUNIYAR , Cynthia SHAFER , Sharadha SUBRAMANIAN , Huw TANNER
发明人： Michael Patrick Dillon , Mika Lindvall , Daniel Poon , Savithri Ramurthy , Vivek Rauniyar , Cynthia Shafer , Sharadha Subramanian , Huw Rowland Tanner
IPC分类号： C07D487/04 , A61K45/06 , A61K31/527 , A61K31/519 , C07D487/10
CPC分类号： C07D487/04 , A61K31/519 , A61K31/527 , A61K45/06 , C07D207/36 , C07D487/10
摘要： The present invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof; as further described herein. The present invention further provides pharmaceutical compositions comprising these compounds, and combinations comprising these compounds combined with or used with a therapeutic co-agent, as well as therapeutic uses of these compounds and compositions. These are useful in the treatment of diseases such as cancer that are associated with activation of ERK1 and/or ERK2, and especially for MAPK pathway dependent cancers showing resistance to Raf and/or MEK inhibitory cancer therapeutics
摘要翻译： 本发明提供式（I）的化合物及其药学上可接受的盐; 如本文进一步描述的。 本发明还提供包含这些化合物的药物组合物，以及包含与治疗性助剂组合或与其一起使用的这些化合物的组合，以及这些化合物和组合物的治疗用途。 这些可用于治疗与ERK1和/或ERK2的激活相关的疾病，特别是对显示出对Raf和/或MEK抑制性癌症治疗剂的抗性的MAPK通路依赖性癌症的疾病的治疗
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公开(公告)号：US08592459B2
公开(公告)日：2013-11-26
申请号：US12759578
申请日：2010-04-13
申请人： Mina E. Aikawa , Payman Amiri , Jeffrey H. Dove , Barry Haskell Levine , Christopher McBride , Teresa E. Pick , Daniel J. Poon , Savithri Ramurthy , Paul A. Renhowe , Cynthia Shafer , Darrin Stuart , Sharadha Subramanian
发明人： Mina E. Aikawa , Payman Amiri , Jeffrey H. Dove , Barry Haskell Levine , Christopher McBride , Teresa E. Pick , Daniel J. Poon , Savithri Ramurthy , Paul A. Renhowe , Cynthia Shafer , Darrin Stuart , Sharadha Subramanian
IPC分类号： A61K31/4439 , C07D401/12
CPC分类号： C07D401/14 , Y02P20/55
摘要： New substituted benzimidazole compounds, compositions, and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
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公开(公告)号：US20130210818A1
公开(公告)日：2013-08-15
申请号：US13396339
申请日：2012-02-14
申请人： Zilin Huang , Jeff Jin , Timothy Machajewski , William R. Antonios-McCrea , Maureen McKenna , Daniel Poon , Paul A. Renhowe , Martin Sendzik , Cynthia Shafer , Aaron Smith , Yongjin Xu , Qiong Zhang , Zheng Chen
发明人： Zilin Huang , Jeff Jin , Timothy Machajewski , William R. Antonios-McCrea , Maureen McKenna , Daniel Poon , Paul A. Renhowe , Martin Sendzik , Cynthia Shafer , Aaron Smith , Yongjin Xu , Qiong Zhang , Zheng Chen
IPC分类号： A61K31/444 , A61K31/506 , C07D403/14 , C07D405/14 , A61K31/4439 , C07D417/14 , C07D471/04 , C07D413/14 , A61K31/496 , C07D487/04 , A61K31/4985 , C07D498/04 , A61K31/5383 , A61K31/4709 , A61K31/5377 , A61P35/00 , C07D401/14
CPC分类号： A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/497 , A61K31/506 , A61K31/5383 , A61K45/06 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D498/04 , A61K2300/00
摘要： New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
摘要翻译： 提供了新的取代的杂环化合物，含有它们的组合物，以及使用它们来抑制Raf激酶活性的方法。 新化合物和组合物可以单独使用或与至少一种另外的药物组合使用，用于治疗Raf激酶介导的病症，例如癌症。
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公开(公告)号：US07732465B2
公开(公告)日：2010-06-08
申请号：US12315779
申请日：2008-12-05
申请人： Mina E. Aikawa , Payman Amiri , Jeffrey H. Dove , Barry Haskell Levine , Christopher McBride , Teresa E. Pick , Daniel J. Poon , Savithri Ramurthy , Paul A. Renhowe , Cynthia Shafer , Darrin Stuart , Sharadha Subramanian
发明人： Mina E. Aikawa , Payman Amiri , Jeffrey H. Dove , Barry Haskell Levine , Christopher McBride , Teresa E. Pick , Daniel J. Poon , Savithri Ramurthy , Paul A. Renhowe , Cynthia Shafer , Darrin Stuart , Sharadha Subramanian
IPC分类号： A61K31/4439
CPC分类号： C07D401/14 , Y02P20/55
摘要： New substituted benzimidazole compounds, compositions, and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
摘要翻译： 提供了新的取代的苯并咪唑化合物，组合物和抑制与人或动物受试者的肿瘤发生相关的激酶活性的方法。 在某些实施方案中，化合物和组合物有效地抑制至少一种丝氨酸/苏氨酸激酶或受体酪氨酸激酶的活性。 新化合物和组合物可以单独使用或与至少一种另外的药剂组合使用，用于治疗丝氨酸/苏氨酸激酶或受体酪氨酸激酶介导的病症，例如癌症。
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公开(公告)号：US20080070906A1
公开(公告)日：2008-03-20
申请号：US11866296
申请日：2007-10-02
申请人： Paul Renhowe , Sabina Pecchi , Timothy Machajewski , Cynthia Shafer , Clarke Taylor , William McCrea , Christopher McBride , Elisa Jazan
发明人： Paul Renhowe , Sabina Pecchi , Timothy Machajewski , Cynthia Shafer , Clarke Taylor , William McCrea , Christopher McBride , Elisa Jazan
IPC分类号： A61K31/4709 , A61K31/439 , A61K31/496 , A61K31/5377 , A61K31/541 , A61P35/00
CPC分类号： C07D471/04 , A61K31/19 , A61K31/439 , A61K31/47 , A61K31/4709 , A61K31/4745 , A61K31/496 , A61K31/513 , A61K31/5377 , A61K31/541 , C07D401/04 , C07D401/14 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D453/02 , A61K2300/00
摘要： Organic compounds having the formulas I and II are provided where the variables have the values described herein. Pharmaceutical formulations include the organic compounds or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier and may be prepared by mixing the organic compounds or pharmaceutically acceptable salts of the organic compounds with a carrier and water. A method of treating a patient includes administering a pharmaceutical formulation according to the invention to a patient in need thereof.
摘要翻译： 提供具有式I和II的有机化合物，其中变量具有本文所述的值。 药物制剂包括有机化合物或其药学上可接受的盐和药学上可接受的载体，并且可以通过将有机化合物的有机化合物或药学上可接受的盐与载体和水混合来制备。 治疗患者的方法包括向有需要的患者施用本发明的药物制剂。
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