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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:US06190920B1
公开(公告)日:2001-02-20
申请号:US08967910
申请日:1997-11-12
IPC分类号: G01N3300
CPC分类号: C07K5/081 , C07K5/0808 , C07K5/1013 , C12Q1/37
摘要: A method for detecting cyclization of acyclic compounds is disclosed. In particular, the invention relates to a method of screening for macrocyclic peptidase inhibitors, and is useful for screening a combinatorial library of compounds.
摘要翻译: 公开了一种检测无环化合物环化的方法。 特别地,本发明涉及筛选大环肽酶抑制剂的方法,并且可用于筛选化合物的组合文库。
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公开(公告)号:US09809610B2
公开(公告)日:2017-11-07
申请号:US15397787
申请日:2017-01-04
IPC分类号: C07D403/12 , C07D213/74 , C07D413/04 , C07D413/14 , A61K31/675 , C07F9/6558
CPC分类号: C07F9/65583 , A61K31/675 , C07D213/74 , C07D403/12 , C07D413/04 , C07D413/14
摘要: The present invention provides a compound of Formula I: wherein X, Y, Z, R1 and R2 are as described herein, and salts thereof and therapeutic uses of these compounds for treatment of disorders associated with RAF kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.
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4.
公开(公告)号:US07326711B2
公开(公告)日:2008-02-05
申请号:US10870707
申请日:2004-06-17
申请人: Weibo Wang , Ryan N. Constantine , Liana Marie Lagniton , Sabina Pecchi , Matthew T. Burger , Manoj C. Desai
发明人: Weibo Wang , Ryan N. Constantine , Liana Marie Lagniton , Sabina Pecchi , Matthew T. Burger , Manoj C. Desai
IPC分类号: A61K31/519 , A61K35/00 , C07D487/04
CPC分类号: C07D471/04
摘要: Pyridin[1,2-a]pyrimidinyl compounds, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the pyridino[1,2-a]pyrimidinyl compounds, either alone or in combination with at least one additional therapeutic agent. Methods of using the pyridino[1,2-a]pyrimidinyl compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases.
摘要翻译: 吡啶并[1,2-a]嘧啶基化合物,其药学上可接受的盐和前药; 包括药学上可接受的载体和一种或多种吡啶并[1,2-a]嘧啶基化合物的组合物,单独或与至少一种另外的治疗剂组合。 单独或与至少一种其它治疗剂组合使用吡啶并[1,2-a]嘧啶基化合物在预防或治疗增殖性疾病中的方法。
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公开(公告)号:US20170114083A1
公开(公告)日:2017-04-27
申请号:US15397787
申请日:2017-01-04
IPC分类号: C07F9/6558 , A61K31/675
CPC分类号: C07F9/65583 , A61K31/675 , C07D213/74 , C07D403/12 , C07D413/04 , C07D413/14
摘要: The present invention provides a compound of Formula I: wherein X, Y, Z, R1 and R2 are as described herein, and salts thereof and therapeutic uses of these compounds for treatment of disorders associated with RAF kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.
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公开(公告)号:US08329732B2
公开(公告)日:2012-12-11
申请号:US12584158
申请日:2009-08-31
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: A61K31/444 , C07D213/74
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:US20100056576A1
公开(公告)日:2010-03-04
申请号:US12584158
申请日:2009-08-31
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: A61K31/444 , C07D401/12
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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公开(公告)号:US20140079693A1
公开(公告)日:2014-03-20
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: C07D401/14 , A61K45/06 , A61K31/4545 , C07D213/81 , 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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公开(公告)号:US08592455B2
公开(公告)日:2013-11-26
申请号:US13327358
申请日:2011-12-15
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: A61K31/4545 , C07D401/14
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.
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