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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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14.发明申请SUBSTITUTED BENZAZOLES AND METHODS OF THEIR USE AS INHIBITORS OF RAF KINASE 审中-公开替代苯扎唑及其作为RAF激酶抑制剂的方法公开(公告)号：US20120288501A1
公开(公告)日：2012-11-15
申请号：US13556907
申请日：2012-07-24
申请人： Payman Amiri , Wendy Fantl , Barry Haskell Levine , Daniel J. Poon , Savithri Ramurthy , Paul A. Renhowe , Sharadha Subramanian , Leonard Sung
发明人： Payman Amiri , Wendy Fantl , Barry Haskell Levine , Daniel J. Poon , Savithri Ramurthy , Paul A. Renhowe , Sharadha Subramanian , Leonard Sung
IPC分类号： A61K31/4439 , C07D417/14 , A61K31/5377 , A61K33/24 , A61K31/513 , A61P35/00 , A61K31/506 , A61K31/664 , A61K31/7068 , A61K31/519 , A61K31/4745 , C07D417/12 , A61K39/395
CPC分类号： C04B35/632 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , 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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15.发明授权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：US08299108B2
公开(公告)日：2012-10-30
申请号：US10675927
申请日：2003-09-29
申请人： Payman Amiri , Wendy Fantl , Barry Haskell Levine , Daniel J. Poon , Savithri Ramurthy , Paul A. Renhowe , Sharadha Subramanian , Leonard Sung
发明人： Payman Amiri , Wendy Fantl , Barry Haskell Levine , Daniel J. Poon , Savithri Ramurthy , Paul A. Renhowe , Sharadha Subramanian , Leonard Sung
IPC分类号： A61K31/415 , C07D401/00
CPC分类号： C04B35/632 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , 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：US20090281100A1
公开(公告)日：2009-11-12
申请号：US12317493
申请日：2008-12-23
申请人： Paul A. Barsanti , Dirksen Bussiere , Stephen D. Harrison , Carla C. Heise , Johanna M. Jansen , Elisa Jazan , Timothy D. Machajewski , Christopher McBride , William R. McCrea, JR. , Simon Ng , Zhi-Jie Ni , Sabina Pecchi , Keith B. Pfister , Savithri Ramurthy , Paul A. Renhowe , Cynthia M. Shafer , Joel B. Silver , Allan S. Wagman , Marion Wiesmann , Kelly Wayman
发明人： Paul A. Barsanti , Dirksen Bussiere , Stephen D. Harrison , Carla C. Heise , Johanna M. Jansen , Elisa Jazan , Timothy D. Machajewski , Christopher McBride , William R. McCrea, JR. , Simon Ng , Zhi-Jie Ni , Sabina Pecchi , Keith B. Pfister , Savithri Ramurthy , Paul A. Renhowe , Cynthia M. Shafer , Joel B. Silver , Allan S. Wagman , Marion Wiesmann , Kelly Wayman
IPC分类号： A61K31/5377 , A61K31/497 , A61K31/4709
CPC分类号： C07D401/04 , A61K31/4375 , A61K31/4709 , A61K31/496 , A61K31/52 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D453/02 , C07D453/06 , C07D471/04
摘要： Methods of inhibiting various enzymes and treating various conditions are provided that include administering to a subject a compound of Structure I or IB, a pharmaceutically acceptable salt thereof, a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. Compounds having the Structure I and IB have the following structures and have the variables described herein. Such compounds may be used to prepare medicaments for use in inhibiting various enzymes and for use in treating conditions mediated by such enzymes.
摘要翻译： 提供了抑制各种酶和治疗各种病症的方法，其包括向受试者施用结构I或IB的化合物，其药学上可接受的盐，其互变异构体或互变异构体的药学上可接受的盐。 具有结构I和IB的化合物具有以下结构并具有本文所述的变量。 这些化合物可用于制备用于抑制各种酶的药物，并用于治疗由这些酶介导的病症。
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公开(公告)号：US07470709B2
公开(公告)日：2008-12-30
申请号：US10644055
申请日：2003-08-19
申请人： Paul A. Barsanti , Dirksen Bussiere , Stephen D. Harrison , Carla C. Heise , Johanna M. Jansen , Elisa Jazan , Timothy D. Machajewski , Christopher McBride , William R. McCrea, Jr. , Simon Ng , Zhi-Jie Ni , Sabina Pecchi , Keith B. Pfister , Savithri Ramurthy , Paul A. Renhowe , Cynthia M. Shafer , Joel B. Silver , Allan S. Wagman , Marion Wiesmann , Kelly Wayman
发明人： Paul A. Barsanti , Dirksen Bussiere , Stephen D. Harrison , Carla C. Heise , Johanna M. Jansen , Elisa Jazan , Timothy D. Machajewski , Christopher McBride , William R. McCrea, Jr. , Simon Ng , Zhi-Jie Ni , Sabina Pecchi , Keith B. Pfister , Savithri Ramurthy , Paul A. Renhowe , Cynthia M. Shafer , Joel B. Silver , Allan S. Wagman , Marion Wiesmann , Kelly Wayman
IPC分类号： A61K31/47
CPC分类号： C07D401/04 , A61K31/4375 , A61K31/4709 , A61K31/496 , A61K31/52 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D453/02 , C07D453/06 , C07D471/04
摘要： Methods of inhibiting various enzymes and treating various conditions are provided that include administering to a subject a compound of Structure I or IB, a pharmaceutically acceptable salt thereof, a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. Compounds having the Structure I and IB have the following structures and have the variables described herein. Such compounds may be used to prepare medicaments for use in inhibiting various enzymes and for use in treating conditions mediated by such enzymes.
摘要翻译： 提供了抑制各种酶和治疗各种病症的方法，其包括向受试者施用结构I或IB的化合物，其药学上可接受的盐，其互变异构体或互变异构体的药学上可接受的盐。 具有结构I和IB的化合物具有以下结构并具有本文所述的变量。 这些化合物可用于制备用于抑制各种酶的药物，并用于治疗由这些酶介导的病症。
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18.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：US08735599B2
公开(公告)日：2014-05-27
申请号：US13613977
申请日：2012-09-13
申请人： Weibo Wang , Paul A. Barsanti , Xia Yia , Rustum S. Boyce , Sabina Pecchi , Nathan Brammeier , Megan C. Phillips , Kris Mendenhall , Kelly Wayman , Liana Marie Lagnition , Ryan N. Constantine , Hong Yang , Elizabeth Mieuli , Savithri Ramurthy , Elisa Jazan , Anu Sharma , Rama Jain , Sharadha Subramanian , Paul A. Renhowe , Kenneth W. Bair , David Duhl , Annette Walter , Tinya Abrams , Kay Huh , Eric Martin , Mark Knapp , Vincent P. Le
发明人： Weibo Wang , Paul A. Barsanti , Xia Yia , Rustum S. Boyce , Sabina Pecchi , Nathan Brammeier , Megan C. Phillips , Kris Mendenhall , Kelly Wayman , Liana Marie Lagnition , Ryan N. Constantine , Hong Yang , Elizabeth Mieuli , Savithri Ramurthy , Elisa Jazan , Anu Sharma , Rama Jain , Sharadha Subramanian , Paul A. Renhowe , Kenneth W. Bair , David Duhl , Annette Walter , Tinya Abrams , Kay Huh , Eric Martin , Mark Knapp , Vincent P. Le
IPC分类号： A61K31/4174 , C07D233/00 , C07D233/54
CPC分类号： C07D233/54 , C07D233/24 , C07D233/64 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/06 , C07D405/12 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D498/10
摘要： The present invention relates to new substituted imidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds. The compounds of the invention have the following general formula:
摘要翻译： 本发明涉及新的取代的咪唑化合物及其药学上可接受的盐，酯或前药，新化合物的组合物和药学上可接受的载体，以及新化合物的用途。 本发明的化合物具有以下通式：
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公开(公告)号：US07626040B2
公开(公告)日：2009-12-01
申请号：US11502303
申请日：2006-08-09
申请人： Paul A. Barsanti , Yi Xia , Weibo Wang , Kris G. Mendenhall , Liana M. Lagniton , Savithri Ramurthy , Megan C. Phillips , Sharadha Subramanian , Rustum Boyce , Nathan M. Brammeier , Ryan Constantine , David Duhl , Annette O. Walter , Tinya J. Abrams , Paul A. Renhowe
发明人： Paul A. Barsanti , Yi Xia , Weibo Wang , Kris G. Mendenhall , Liana M. Lagniton , Savithri Ramurthy , Megan C. Phillips , Sharadha Subramanian , Rustum Boyce , Nathan M. Brammeier , Ryan Constantine , David Duhl , Annette O. Walter , Tinya J. Abrams , Paul A. Renhowe
IPC分类号： C07D233/64 , C07D401/12 , C07D279/12 , C07D413/12 , C07D403/12
CPC分类号： C07D401/14 , C07D233/64 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： The present invention relates to new substituted imidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses of the compounds. The compounds of the invention have the following general formula:
摘要翻译： 本发明涉及新的取代的咪唑化合物及其药学上可接受的盐，酯或前药，衍生物的组合物和药学上可接受的载体，以及该化合物的用途。 本发明的化合物具有以下通式：
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