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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：US20070161680A1
公开(公告)日：2007-07-12
申请号：US11513959
申请日：2006-08-30
申请人： Mina Alkawa , Payman Amiri , Jeffrey Dove , Barry Levine , Christopher McBride , Teresa Pick , Daniel Poon , Savithri Ramurthy , Paul Renhowe , Cynthia Shafer , Darrin Stuart , Sharadha Subramanian
发明人： Mina Alkawa , Payman Amiri , Jeffrey Dove , Barry Levine , Christopher McBride , Teresa Pick , Daniel Poon , Savithri Ramurthy , Paul Renhowe , Cynthia Shafer , Darrin Stuart , Sharadha Subramanian
IPC分类号： A61K31/4439 , C07D403/14
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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4.发明申请Substituted benzazoles and methods of their use as inhibitors of Raf kinase 失效取代的苯并唑及其作为Raf激酶抑制剂的方法公开(公告)号：US20050192287A1
公开(公告)日：2005-09-01
申请号：US10967089
申请日：2004-10-15
申请人： Abran Costales , Teresa Hansen , Barry Levine , Christopher McBride , Daniel Poon , Savithri Ramurthy , Paul Renhowe , Cynthia Shafer , Sharadha Subramanian , Joelle Verhagen
发明人： Abran Costales , Teresa Hansen , Barry Levine , Christopher McBride , Daniel Poon , Savithri Ramurthy , Paul Renhowe , Cynthia Shafer , Sharadha Subramanian , Joelle Verhagen
IPC分类号： A61K31/4439 , A61K31/4745 , A61K31/496 , A61K31/506 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/12
CPC分类号： C07D401/12 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/551 , A61K45/06 , C04B35/632 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14
摘要： New substituted benzazole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds 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： 提供了新的取代的苯唑化合物，抑制人或动物受试者中的Raf激酶活性的组合物和方法。 新化合物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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5.发明申请Substituted benz-azoles and methods of their use as inhibitors of Raf kinase 失效取代的苯并唑及其用作Raf激酶抑制剂的方法公开(公告)号：US20070299039A1
公开(公告)日：2007-12-27
申请号：US11282939
申请日：2005-11-18
申请人： Payman Amiri , Wendy Fantl , Teresa Hansen , Barry Levine , Christopher McBride , Daniel Poon , Savithri Ramurthy , Paul Renhowe , Cynthia Shafer , Sharadha Subramanian , Leonard Sung
发明人： Payman Amiri , Wendy Fantl , Teresa Hansen , Barry Levine , Christopher McBride , Daniel Poon , Savithri Ramurthy , Paul Renhowe , Cynthia Shafer , Sharadha Subramanian , Leonard Sung
IPC分类号： A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/5377 , A61K31/55 , A61K31/665 , A61P35/00 , C07D401/10 , C07D401/14 , C07D413/10 , C07D413/14 , C07D417/10
CPC分类号： C07D401/14 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/12 , C07D417/14 , C07D453/02
摘要： New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds 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： 提供了新的取代的苯并唑化合物，抑制人或动物受试者中Raf激酶活性的组合物和方法。 新化合物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：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：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：US20090170904A1
公开(公告)日：2009-07-02
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 , A61P35/00
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：US20100234394A1
公开(公告)日：2010-09-16
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： A61K31/496 , C07D401/14 , A61K31/4439 , A61K31/444 , A61P35/00
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中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：US07482367B2
公开(公告)日：2009-01-27
申请号：US11513959
申请日：2006-08-30
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 , C07D401/14
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中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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