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公开(公告)号：US20150266895A1
公开(公告)日：2015-09-24
申请号：US14431462
申请日：2013-09-26
申请人： Kevin J. WILSON , David J. WITTER , Phieng SILIPHAIVANH , Kathryn KIPFORD , David SLOMAN , Danielle FALCONE , Brendan O'BOYLE , Umar Faruk MANSOOR , Jongwon LIM , Joey L. METHOT , Christopher BOYCE , Lei CHEN , Matthew H. DANIELS , Salem FEVRIER , Xianhai HUANG , Ravi KURUKULASURIYA , Ling TONG , Wei ZHOU , Joseph KOZLOWSKI , Milana M. MALETIC , Bidhan A. SHINKRE , Jayanth Thiruvellore THATAI , Raman Kumar BAKSHI , Ganesh Babu KARUNAKARAN , MERCK SHARP & DOHME CORP.
发明人： Kevin J. Wilson , David J. Witter , Phieng Siliphaivanh , Kathryn Lipford , David Sloman , Danielle Falcone , Brendan O'Boyle , Umar Faruk Mansoor , Jongwon Lim , Joey L. Methot , Christopher Boyce , Lei Chen , Matthew H. Daniels , Salem Fevrier , Xianhai Huang , Ravi Kurukulasuriya , Ling Tong , Wei Zhou , Joseph Kozlowski , Milana M. Maletic , Bidhan A. Shinkre , Jayanth Thiruvellore Thatai , Raman Kumar Bakshi , Ganesh Babu Karunakaran
IPC分类号： C07D498/18 , A61K31/437 , A61K31/5377 , A61K31/496 , A61K45/06 , A61K31/4375 , C07D498/14 , A61K31/553 , C07D519/00 , C07D471/04 , C07D471/14
CPC分类号： C07D498/18 , A61K31/437 , A61K31/4375 , A61K31/496 , A61K31/5377 , A61K31/553 , A61K45/06 , C07D471/04 , C07D471/14 , C07D471/16 , C07D498/14 , C07D498/16 , C07D519/00 , A61K2300/00
摘要： Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1).
摘要翻译： 公开了式（1）的ERK抑制剂及其药学上可接受的盐。 还公开了使用式（1）的化合物治疗癌症的方法。
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公开(公告)号：US10059705B2
公开(公告)日：2018-08-28
申请号：US14778055
申请日：2014-03-19
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.
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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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4.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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5.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：US09226922B2
公开(公告)日：2016-01-05
申请号：US14431485
申请日：2013-09-26
发明人： Kevin J. Wilson , David J. Witter , Matthew H. Daniels , Angie R. Angeles , Phieng Siliphaivanh , David Sloman , Brendan O'Boyle , Danielle Falcone , Catherine White , Ron Ferguson , Wei Zhou , Kathryn Lipford , Umar Faruk Mansoor , Salem Fevrier , Xianhai Huang , Ravi Kurukulasuriya , Judson E. Richard , Shuyi Tang , Christopher Boyce , Joseph Kozlowski , Raman Kumar Bakshi , Ganesh Babu Karunakaran
IPC分类号： C07D401/14 , A61K31/437 , C07D471/04 , A61K45/06 , A61K31/4545
CPC分类号： A61K31/437 , A61K31/4545 , A61K45/06 , C07D471/04
摘要： Disclosed are the ERK inhibitors of formula (1.0), having a pyrazolopyridine base structure, and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1.0).
摘要翻译： 公开了具有吡唑并吡啶基结构的式（1.0）的ERK抑制剂及其药学上可接受的盐。 还公开了使用式（1.0）化合物治疗癌症的方法。
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公开(公告)号：US20140296203A1
公开(公告)日：2014-10-02
申请号：US14353381
申请日：2012-10-25
发明人： Jongwon Lim , Elizabeth Helen Kelley , Joey L. Methot , Hua Zhou , Alessia Petrocchi , Faruk Mansoor , Christian Fischer , Brendan O'Boyle , David Joseph Guerin , Corey E. Bienstock , Christopher W. Boyce , Matthew H. Daniels , Danielle Falcone , Ronald D. Ferguson , Salem Fevrier , Xianhai Huang , Kathryn Ann Lipford , David L. Sloman , Kevin Wilson , Wei Zhou , David Witter , Milana M. Maletic , Phieng Siliphaivanh
IPC分类号： C07D471/04 , A61K31/444 , A61K31/437 , A61K45/06 , A61K31/501 , A61K31/4709 , A61K31/5377 , A61K31/496 , A61K31/4545 , A61K31/506
CPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D519/00
摘要： Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1).
摘要翻译： 公开了式（1）的ERK抑制剂及其药学上可接受的盐。 还公开了使用式（1）的化合物治疗癌症的方法。
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公开(公告)号：US09957265B2
公开(公告)日：2018-05-01
申请号：US14778052
申请日：2014-03-19
发明人： Christopher Dinsmore , Peter Fuller , David Guerin , Christopher F. Thompson , Qinglin Pu , Mark E. Scott , Jason David Katz , Ravi Kurukulasuriya , 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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公开(公告)号：US09546168B2
公开(公告)日：2017-01-17
申请号：US15103893
申请日：2014-12-12
IPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K45/06
CPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K45/06 , A61K2300/00
摘要： Disclosed are the ERK inhibitors of formula (1.0) and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1.0). This invention provides compounds that are ERK inhibitors (i.e., ERK2 inhibitors). This invention also provides a pharmaceutical composition comprising an effective amount of at least one (e.g., 1) compound of formula (1.0) and a pharmaceutically acceptable carrier.
摘要翻译： 公开了式（1.0）的ERK抑制剂及其药学上可接受的盐。 还公开了使用式（1.0）化合物治疗癌症的方法。 本发明提供了作为ERK抑制剂（即ERK2抑制剂）的化合物。 本发明还提供了包含有效量的至少一种（例如1）式（1.0）化合物和药学上可接受的载体的药物组合物。
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公开(公告)号：US20160311819A1
公开(公告)日：2016-10-27
申请号：US15103893
申请日：2014-12-12
IPC分类号： C07D471/04 , A61K31/444 , A61K45/06 , A61K31/437
CPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K45/06 , A61K2300/00
摘要： Disclosed are the ERK inhibitors of formula (1.0) and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1.0). This invention provides compounds that are ERK inhibitors (i.e., ERK2 inhibitors). This invention also provides a pharmaceutical composition comprising an effective amount of at least one (e.g., 1) compound of formula (1.0) and a pharmaceutically acceptable carrier.
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