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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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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：US08168794B2
公开(公告)日：2012-05-01
申请号：US12380458
申请日：2009-02-26
IPC分类号： A61K31/4545 , C07D213/75 , C07D417/12 , C07D413/14
CPC分类号： C07D417/14 , A61K31/4439 , A61K31/4545 , C07D417/12
摘要： The present invention relates to new compounds of Formulas I and II, their tautomers, stereoisomers and polymorphs, and pharmaceutically acceptable salts, esters, metabolites or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the inhibition of Pim kinase activity and/or the prophylaxis or treatment of cancer.
摘要翻译： 本发明涉及式I和II的新化合物，其互变异构体，立体异构体和多晶型物及其药学上可接受的盐，酯，代谢物或前药，新化合物与药学上可接受的载体的组合物，以及新化合物的用途， 单独或与至少一种另外的治疗剂组合，抑制Pim激酶活性和/或预防或治疗癌症。
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公开(公告)号：US08829193B2
公开(公告)日：2014-09-09
申请号：US13447988
申请日：2012-04-16
IPC分类号： C07D417/14 , A61K31/4545 , A61K31/4439 , C07D417/12
CPC分类号： C07D417/14 , A61K31/4439 , A61K31/4545 , C07D417/12
摘要： The present invention relates to new compounds of Formulas I and II, their tautomers, stereoisomers and polymorphs, and pharmaceutically acceptable salts, esters, metabolites or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the inhibition of Pim kinase activity and/or the prophylaxis or treatment of cancer.
摘要翻译： 本发明涉及式I和II的新化合物，其互变异构体，立体异构体和多晶型物及其药学上可接受的盐，酯，代谢物或前药，新化合物与药学上可接受的载体的组合物，以及新化合物的用途， 单独或与至少一种另外的治疗剂组合，抑制Pim激酶活性和/或预防或治疗癌症。
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公开(公告)号：US20100216839A1
公开(公告)日：2010-08-26
申请号：US12380458
申请日：2009-02-26
IPC分类号： A61K31/4439 , C07D417/14 , C07D417/12 , A61K31/4545 , A61P35/00
CPC分类号： C07D417/14 , A61K31/4439 , A61K31/4545 , C07D417/12
摘要： The present invention relates to new compounds of Formulas I and II, their tautomers, stereoisomers and polymorphs, and pharmaceutically acceptable salts, esters, metabolites or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the inhibition of Pim kinase activity and/or the prophylaxis or treatment of cancer.
摘要翻译： 本发明涉及式I和II的新化合物，其互变异构体，立体异构体和多晶型物及其药学上可接受的盐，酯，代谢物或前药，新化合物与药学上可接受的载体的组合物，以及新化合物的用途， 单独或与至少一种另外的治疗剂组合，抑制Pim激酶活性和/或预防或治疗癌症。
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公开(公告)号：US20100075965A1
公开(公告)日：2010-03-25
申请号：US12279148
申请日：2007-02-14
申请人： Zhi-Jie Ni , Sabina Pecchi , Matthew Burger , Wooseok Han , Aaron Smith , Gordana Atallah , Sarah Bartulis , Kelly Frazier , Joelle Verhagen , Yanchen Zhang , Ed Iwanowicz , Tom Hendrickson , Mark Knapp , Hanne Merritt , Charles Voliva , Marion Wiesmann , Darren Mark Legrand , Ian Bruce , James Dale , Jiong Lan , Barry Levine , Abran Costales , Jui Liu , Teresa Pick , Daniel Menezes
发明人： Zhi-Jie Ni , Sabina Pecchi , Matthew Burger , Wooseok Han , Aaron Smith , Gordana Atallah , Sarah Bartulis , Kelly Frazier , Joelle Verhagen , Yanchen Zhang , Ed Iwanowicz , Tom Hendrickson , Mark Knapp , Hanne Merritt , Charles Voliva , Marion Wiesmann , Darren Mark Legrand , Ian Bruce , James Dale , Jiong Lan , Barry Levine , Abran Costales , Jui Liu , Teresa Pick , Daniel Menezes
IPC分类号： A61K31/5377 , C07D471/04 , C07D487/04 , C07D413/14 , A61K31/437 , A61K31/5025 , A61P35/00
CPC分类号： C07D487/04 , C07D417/04 , C07D417/14 , C07D471/04
摘要： Phosphatidylinositol (PI) 3 kinase inhibitor compounds, their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, phospholipid kinases, G-protein coupled receptors, and phosphatases.
摘要翻译： 磷脂酰肌醇（PI）3激酶抑制剂化合物，其药学上可接受的盐和前药; 单独或与至少一种另外的治疗剂组合的新化合物与药学上可接受的载体的组合物; 以及单独或与至少一种另外的治疗剂联合使用的新化合物在预防或治疗以生长因子，蛋白丝氨酸/苏氨酸激酶，磷脂激酶，G蛋白偶联的异常活性为特征的增殖性疾病中的用途 受体和磷酸酶。
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公开(公告)号：US20120202851A1
公开(公告)日：2012-08-09
申请号：US13447988
申请日：2012-04-16
IPC分类号： A61K31/4545 , A61P35/04 , A61P35/02 , A61K31/4436
CPC分类号： C07D417/14 , A61K31/4439 , A61K31/4545 , C07D417/12
摘要： The present invention relates to new compounds of Formulas I and II, their tautomers, stereoisomers and polymorphs, and pharmaceutically acceptable salts, esters, metabolites or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the inhibition of Pim kinase activity and/or the prophylaxis or treatment of cancer.
摘要翻译： 本发明涉及式I和II的新化合物，其互变异构体，立体异构体和多晶型物及其药学上可接受的盐，酯，代谢物或前药，新化合物与药学上可接受的载体的组合物，以及新化合物的用途， 单独或与至少一种另外的治疗剂组合，抑制Pim激酶活性和/或预防或治疗癌症。
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公开(公告)号：US09079889B2
公开(公告)日：2015-07-14
申请号：US14081132
申请日：2013-11-15
申请人： Matthew T. Burger , Wooseok Han , Jiong Lan , Gisele Nishiguchi
发明人： Matthew T. Burger , Wooseok Han , Jiong Lan , Gisele Nishiguchi
IPC分类号： A61K31/4418 , C07D401/14 , C07D401/12 , A61K31/444 , A61K31/4545 , A61K45/06 , C07D213/81
CPC分类号： C07D213/81 , A61K31/4418 , A61K31/444 , A61K31/4545 , A61K45/06 , C07D401/12 , C07D401/14
摘要： New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM 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 PIM 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： 提供了新的化合物，组合物和方法抑制Provirus与人或动物受试者中与肿瘤发生相关的Maloney激酶（PIM激酶）活性的整合。 在某些实施方案中，化合物和组合物有效抑制至少一种PIM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：US20150315150A1
公开(公告)日：2015-11-05
申请号：US14797534
申请日：2015-07-13
申请人： Matthew T. Burger , Wooseok Han , Jiong Lan , Gisele Nishiguchi
发明人： Matthew T. Burger , Wooseok Han , Jiong Lan , Gisele Nishiguchi
IPC分类号： C07D213/81 , A61K31/4545 , C07D401/14 , A61K45/06 , A61K31/444
CPC分类号： C07D213/81 , A61K31/4418 , A61K31/444 , A61K31/4545 , A61K45/06 , C07D401/12 , C07D401/14
摘要： New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM 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 PIM 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： 提供了新的化合物，组合物和方法抑制Provirus与人或动物受试者中与肿瘤发生相关的Maloney激酶（PIM激酶）活性的整合。 在某些实施方案中，化合物和组合物有效抑制至少一种PIM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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