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公开(公告)号：US09884048B2
公开(公告)日：2018-02-06
申请号：US15531759
申请日：2015-12-10
发明人： Phieng Siliphaivanh , Joey Methot , Kathryn Ann Lipford , Danielle Molinari , David L. Sloman , David Witter , Hua Zhou , Christopher Boyce , Xianhai Huang , Jongwon Lim , David Guerin , Ganesh Babu Karunakaran , Raman Kumar Bakshi , Ziping Liu , Jianmin Fu , Zhilong Wan , Wei Liu
IPC分类号： A61K31/437 , A61K31/4545 , A61K31/444 , C07D471/04 , C07D519/00
CPC分类号： A61K31/437 , A61K31/444 , A61K31/4545 , C07D471/04 , C07D519/00
摘要： The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and a pharmaceutically acceptable carrier. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier.
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公开(公告)号：US20210309687A1
公开(公告)日：2021-10-07
申请号：US17266515
申请日：2019-08-05
申请人： Michelle MACHACEK , David WITTER , Chunhui HUANG , Shuhei KAWAMURA , Sebastian SCHNEIDER , Mrray WAN , Merck Sharp & Dohme Corp.
发明人： Michelle Machacek , David Witter , Chunhui Huang , Shuhei Kawamura , Sebastian Schneider , Murray Wan
摘要： The present invention provides a compound of formula (I) Formula (I) and the pharmaceutically acceptable salts, esters, and prodrugs thereof, are PRMT5 inhibitors. Also provided are methods of making compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I), and methods of using these compounds to treat cancer, sickle cell, and hereditary persistence of foetal hemoglobin (HPFH) mutations.
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公开(公告)号：US20140303142A1
公开(公告)日：2014-10-09
申请号：US14349377
申请日：2012-09-28
发明人： John W. Butcher , David Witter , Christopher Dinsmore , June Kim , John Hendrix , Raksha Acharya , Sean P. Ahearn , Joon Jung , Alexey Rivkin , Philip Jones
IPC分类号： C07D471/04
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：US20220363707A1
公开(公告)日：2022-11-17
申请号：US17266521
申请日：2019-08-05
发明人： Michelle Machacek , David Witter , Craig Gibeau , Chunhui Huang , Shuhei Kawamura , David L. Sloman , Phieng Siliphaivanh , Ryan Quiroz , Murray Wan , Sebastian Schneider , Charles S. Yeung , Michael H. Reutershan , Timothy J. Henderson , Jean-Laurent Paparin , Houcine Rahali , Jonathan M. E. Hughes , Sulagna Sanyal , Yingchun Ye , David A. Candito , Patrick S. Fier , Steven M. Silverman
IPC分类号： C07H19/14 , C07D487/04 , A61P35/00
摘要： The present invention provides a compound of Formula (I) and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are PRMT5 inhibitors. Also provided are methods of making compounds of Formula I, pharmaceutical compositions comprising compounds of Formula I, and methods of using these compounds to treat cancer, sickle cell, and hereditary persistence of foetal hemoglobin (HPFH) mutations.
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公开(公告)号：US20170266167A1
公开(公告)日：2017-09-21
申请号：US15531759
申请日：2015-12-10
发明人： Phieng Siliphaivanh , Joey Methot , Kathryn Ann Lipford , Danielle Molinari , David L. Sloman , David Witter , Hua Zhou , Christopher Boyce , Xianhai Huang , Jongwon Lim , David Guerin , Ganesh Babu Karunakaran , Raman Kumar Bakshi , Ziping Liu , Jianmin Fu , Zhilong Wan , Wei Liu
IPC分类号： A61K31/437 , C07D519/00 , C07D471/04 , A61K31/4545 , A61K31/444
CPC分类号： A61K31/437 , A61K31/444 , A61K31/4545 , C07D471/04 , C07D519/00
摘要： The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and a pharmaceutically acceptable carrier. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier.
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公开(公告)号：US09096598B2
公开(公告)日：2015-08-04
申请号：US14349377
申请日：2012-09-28
发明人： John W. Butcher , David Witter , Christopher Dinsmore , June Kim , John Hendrix , Raksha Archarya , Sean P. Ahearn , Joon Jung , Alexey Rivkin , Philip Jones
IPC分类号： C07D401/10 , A61K31/437 , 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：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：US20210277009A1
公开(公告)日：2021-09-09
申请号：US17266474
申请日：2019-08-05
申请人： David WITTER , Shuhei KAWAMURA , Michelle MACHACEK , Ryan QUIROZ , Michael H. REUTERSHAN , Sebastian SCHNEIDER , Phieng SILIPHAIVANH , Yingchun YE , Charles S. YEUNG , Merck Sharp & Dohme Corp.
发明人： David Witter , Shuhei Kawamura , Michelle Machacek , Ryan Quiroz , Michael H. Reutershan , Sebastian Schneider , Phieng Siliphaivanh , Yingchun Ye , Charles S. Yeung
IPC分类号： C07D487/04 , C07D519/00
摘要： The present invention provides a compound of Formula (I) Formula (I) or the pharmaceutically acceptable salts thereof, which are PRMT5 inhibitors.
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公开(公告)号：US09988397B2
公开(公告)日：2018-06-05
申请号：US15531771
申请日：2015-12-10
发明人： Phieng Siliphaivanh , David L. Sloman , David Witter , Umar Faruk Mansoor , Joseph Kozlowski , Ziping Liu , Jianmin Fu , Zhilong Wan , Wei Liu , Yimin Qian , Xianhai Huang
IPC分类号： C07D498/18 , C07D471/18 , C07D471/22
CPC分类号： C07D498/18 , A61K31/437 , A61K31/444 , C07D471/18 , C07D471/22
摘要： The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a method of inhibiting ERK2 in a patient in need of such treatment comprising administering to said patient an effective amount of at least one compound of Formula (I). The invention also provides a method for treating cancer in a patient in need of such treatment, said method comprising administering to said patient an effective amount of at least one compound of Formula (I).
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