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公开(公告)号：US20160272634A1
公开(公告)日：2016-09-22
申请号：US14778055
申请日：2014-03-19
申请人： Christopher DINSMORE , Peter FULLER , David GUERIN , Jason David KATZ , Christopher F. THOMPSON , Danielle FALCONE , Wei DENG , Luis TORRES , Hongbo ZENG , Yunfeng BAI , Jianmin FU , Norman KONG , Yumei LIU , Zhixiang ZHENG , Mark E. SCOTT , MERCK SHARP & DOHME CORP.
发明人： Christopher Dinsmore , Peter Fuller , David Guerin , Jason David Katz , Christopher F. Thompson , Danielle Falcone , Wei Deng , Luis Torres , Hongbo Zeng , Yunfeng Bai , Jianmin Fu , Norman Kong , Yumei Liu , Zhixiang Zheng , Mark E. Scott
IPC分类号： C07D471/04 , C07D519/00
CPC分类号： C07D471/04 , C07D519/00
摘要： The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
摘要翻译： 本发明提供了作为JAK抑制剂的式I化合物，因此可用于治疗JAK介导的疾病如类风湿性关节炎，哮喘，COPD和癌症。
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公开(公告)号：US07851626B2
公开(公告)日：2010-12-14
申请号：US11604558
申请日：2006-11-27
申请人： Qingjie Ding , Bradford James Graves , Norman Kong , Jin-Jun Liu , Allen John Lovey , Giacomo Pizzolato , John Lawson Roberts , Sung-Sau So , Binh Thanh Vu , Peter Michael Wovkulich
发明人： Qingjie Ding , Bradford James Graves , Norman Kong , Jin-Jun Liu , Allen John Lovey , Giacomo Pizzolato , John Lawson Roberts , Sung-Sau So , Binh Thanh Vu , Peter Michael Wovkulich
IPC分类号： C07D403/02 , C07D233/06 , A61K31/497 , A01N43/50
CPC分类号： C07D233/22 , C07D233/26 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/06 , C07D407/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D487/04
摘要： There is provided a compound of formula I and the pharmaceutically acceptable salts and esters thereof wherein X1, X2, R1, R2, R3, R4, R5 and R6 are herein described. The compounds exhibit activity as anticancer agents.
摘要翻译： 提供式I化合物及其药学上可接受的盐和酯，其中本文描述了X1，X2，R1，R2，R3，R4，R5和R6。 化合物表现出抗癌作用。
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公开(公告)号：US20090170920A1
公开(公告)日：2009-07-02
申请号：US12331538
申请日：2008-12-10
IPC分类号： A61K31/4166 , C07D403/06 , A61P35/00
CPC分类号： C07D233/74 , C07D233/78 , C07D417/14
摘要： The present invention relates to compounds of the formula methods for the preparation thereof, and methods for their use. The compounds are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as cancer, cognitive and CNS disorders, and inflammatory/autoimmune diseases.
摘要翻译： 本发明涉及其制备方法的化合物及其使用方法。 该化合物可用于治疗以MEK多动症为特征的疾病。 因此，该化合物可用于治疗诸如癌症，认知和CNS疾病以及炎性/自身免疫性疾病的疾病。
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公开(公告)号：US20090048452A1
公开(公告)日：2009-02-19
申请号：US12186648
申请日：2008-08-06
IPC分类号： C07D403/06 , C07D409/14
CPC分类号： C07D403/06
摘要： This invention relates to compounds of formula I: or pharmaceutically acceptable salts thereof,wherein R1, R2, R3, R4, R5, and R6 are described in this application. These compounds inhibit the enzymes MEK 1 and MEK2, protein kinases that are components of the MAP kinase signal transduction pathway and as such the compounds will have anti-hyperproliferative cellular activity.
摘要翻译： 本发明涉及式I化合物或其药学上可接受的盐，其中本申请中描述了R1，R2，R3，R4，R5和R6。 这些化合物抑制作为MAP激酶信号转导途径成分的蛋白激酶MEK1和MEK2，因此这些化合物将具有抗过度增殖的细胞活性。
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公开(公告)号：US20070129416A1
公开(公告)日：2007-06-07
申请号：US11604558
申请日：2006-11-27
申请人： Qingjie Ding , Bradford Graves , Norman Kong , Jin-Jun Liu , Allen Lovey , Giacomo Pizzolato , John Roberts , Sung-Sau So , Binh Vu , Peter Wovkulich
发明人： Qingjie Ding , Bradford Graves , Norman Kong , Jin-Jun Liu , Allen Lovey , Giacomo Pizzolato , John Roberts , Sung-Sau So , Binh Vu , Peter Wovkulich
IPC分类号： A61K31/4164 , C07D233/22 , C07D233/06
CPC分类号： C07D233/22 , C07D233/26 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/06 , C07D407/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D487/04
摘要： There is provided a compound of formula I and the pharmaceutically acceptable salts and esters thereof wherein X1, X2, R1, R2, R3, R4, R5 and R6 are herein described. The compounds exhibit activity as anticancer agents.
摘要翻译： 提供式I化合物及其药学上可接受的盐和酯，其中X 1，X 2，R 1，R 2， > 2，R 3，R 4，R 5和R 6在本文中进行了描述。 化合物表现出抗癌作用。
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公开(公告)号：US06281356B1
公开(公告)日：2001-08-28
申请号：US09737685
申请日：2000-12-15
申请人： Nader Fotouhi , Norman Kong , Allen John Lovey
发明人： Nader Fotouhi , Norman Kong , Allen John Lovey
IPC分类号： C07D40114
CPC分类号： C07D403/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要： Disclosed are substituted pyrroles having the formula These compounds and their pharmaceutically acceptable salts are useful in the treatment and/or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing the foregoing compounds.
摘要翻译： 公开了具有下式的取代吡咯。这些化合物及其药学上可接受的盐可用于治疗和/或控制细胞增殖性疾病，特别是癌症。 还公开了含有上述化合物的药物组合物。
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7.发明申请N-(2-CYANO HETEROCYCLYL) PYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS 有权N-（2-氰基杂环基）吡唑并吡喃酮作为甘薯激酶抑制剂公开(公告)号：US20160272633A1
公开(公告)日：2016-09-22
申请号：US14778052
申请日：2014-03-19
申请人： Christopher DINSMORE , Peter FULLER , David GUERIN , Christopher F. THOMPSON , Qinglin PU , Mark E. SCOTT , Jason David KATZ , Ravi KURUKLASURIYA , Joshua T. CLOSE , Danielle FALCONE , Jason BRUDAKER , Hongbo ZENG , Yunfeng BAI , Jianmin FU , Norman KONG , Yumei LIU , Zhixiang ZHENG , MERCK SHARP & DOHME CORP.
发明人： Christopher Dinsmore , Peter Fuller , David Guerin , Christopher F. Thompson , Qinglin Pu , Mark E. Scott , Jason David Katz , Ravi Kuruklasuriya , Joshua T. Close , Danielle Falcone , Jason Brubaker , Hongbo Zeng , Yunfeng Bai , Jianmin Fu , Norman Kong , Yumei Liu , Zhixiang Zheng
IPC分类号： C07D471/04 , C07D519/00
CPC分类号： C07D471/04 , C07D519/00
摘要： Provided are compounds of Formula I, a JAK inhibitor, and use thereof for the treatment of JAK-mediated diseases by the application.
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8.发明申请GEMINALLY SUBSTITUTED CYANOETHYLPYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS 有权作为JANUS KINASE抑制剂的GEMYALLY取代的氰基乙基吡唑啉吡啶公开(公告)号：US20160272632A1
公开(公告)日：2016-09-22
申请号：US14778046
申请日：2014-03-19
申请人： Matthew Lloyd CHILDERS , Peter FULLER , David GUERIN , Jason David KATZ , Qinglin PU , Mark E. SCOTT , Christopher E. THOMPSON , Michelle MARTINEZ , Danielle FALCONE , Luis TORRES , Yongqi DENG , Ravi KURUKULASURIYA , Hongbo ZENG , Yunfeng BAI , Norman KONG , Yumei LIU , MERCK SHARP & DOHME CORP.
发明人： Matthew Lloyd Childers , Peter Fuller , David Guerin , Jason David Katz , Qinglin Pu , Mark E. Scott , Christopher F. Thompson , Michelle Martinez , Danielle Falcone , Luis Torres , Yongqi Deng , Ravi Kurukulasuriya , Hongbo Zeng , Yunfeng Bai , Norman Kong , Yumei Liu , Zhixiang Zheng
IPC分类号： C07D471/04 , C07D519/00
CPC分类号： C07D471/04 , C07D519/00
摘要： The instant invention provides compounds of Formula (I) which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
摘要翻译： 本发明提供了作为JAK抑制剂的式（I）化合物，因此可用于治疗JAK介导的疾病如类风湿性关节炎，哮喘，COPD和癌症。
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公开(公告)号：US08063085B2
公开(公告)日：2011-11-22
申请号：US12331538
申请日：2008-12-10
IPC分类号： A01N43/50 , A61K31/415 , C07D407/00
CPC分类号： C07D233/74 , C07D233/78 , C07D417/14
摘要： The present invention relates to compounds of the formula methods for the preparation thereof, and methods for their use. The compounds are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as cancer, cognitive and CNS disorders, and inflammatory/autoimmune diseases.
摘要翻译： 本发明涉及其制备方法的化合物及其使用方法。 该化合物可用于治疗以MEK多动症为特征的疾病。 因此，该化合物可用于治疗诸如癌症，认知和CNS疾病以及炎性/自身免疫性疾病的疾病。
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公开(公告)号：US06559164B1
公开(公告)日：2003-05-06
申请号：US09678521
申请日：2000-10-03
IPC分类号： A61K31405
CPC分类号： C07D401/14 , C07D403/14
摘要： Disclosed are novel substituted pyrroles having the formula These compounds and their pharmaceutically acceptable salts are suitable for administration to patients as continuous infusion solution and are useful in the treatment and/or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing the foregoing compounds and methods for the treatment and/or control of cancer.
摘要翻译： 公开了具有下式的新颖的取代的吡咯。这些化合物及其药学上可接受的盐适于作为连续输注溶液施用于患者，并且可用于治疗和/或控制细胞增殖性疾病，特别是癌症。 还公开了含有前述化合物的药物组合物和用于治疗和/或控制癌症的方法。
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