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公开(公告)号：US10975084B2
公开(公告)日：2021-04-13
申请号：US16341313
申请日：2017-10-06
申请人： Merck Sharp & Dohme Corp. , Umar Faruk Mansoor , Christian Fischer , Phieng Siliphaivanh , Luis Torres , Hakan Gunaydin , David L. Sloman
发明人： Umar Faruk Mansoor , Christian Fischer , Phieng Siliphaivanh , Luis Torres , Hakan Gunaydin , David L. Sloman
IPC分类号： C07D487/04
摘要： The present invention provides a compound of Formula (I) (represented as tautomers Ia and Ib) or the pharmaceutically acceptable salts thereof, which are KDM5 inhibitors.
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公开(公告)号：US20200048258A1
公开(公告)日：2020-02-13
申请号：US16341313
申请日：2017-10-06
申请人： UMAR Faruk MANSOOR , Christian Fischer , Phieng Siliphaivanh , Luis Torres , Hakan Gunaydin , David Sloman , Merck Sharp & Dohme Corp.
发明人： UMAR FARUK MANSOOR , Christian Fischer , Phieng Siliphaivanh , Luis Torres , Hakan Gunaydin , David L. Sloman
IPC分类号： C07D487/04
摘要： The present invention provides a compound of Formula (I) (represented as tautomers Ia and Ib) or the pharmaceutically acceptable salts thereof, which are KDM5 inhibitors.
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公开(公告)号：US20200048259A1
公开(公告)日：2020-02-13
申请号：US16341323
申请日：2017-10-06
申请人： Umar Faruk MANSOOR , Christian FISCHER , Phieng SILIPHAIVANH , Hakan GUNAYDIN , Merck Sharp & Dohme Corp.
IPC分类号： C07D487/04
摘要： The present invention provides a compound of Formula (I) (represented as tautomers Ia and Ib): (I) or the pharmaceutically acceptable salts thereof, which are KDM5 inhibitors.
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公开(公告)号：US09023865B2
公开(公告)日：2015-05-05
申请号：US14353381
申请日：2012-10-25
申请人： Jongwon Lim , Elizabeth Helen Kelley , Joey L. Methot , Hua Zhou , Alessia Petrocchi , Umar 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
发明人： Jongwon Lim , Elizabeth Helen Kelley , Joey L. Methot , Hua Zhou , Alessia Petrocchi , Umar 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： C07D401/14 , A61K31/437 , C07D471/04 , C07D519/00 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K45/06
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：US08999957B2
公开(公告)日：2015-04-07
申请号：US13703250
申请日：2011-06-22
申请人： Yongqi Deng , Liang Zhu , Gerald W. Shipps, Jr. , Sie-Mun Lo , Binyuan Sun , Xiaohua Huang , Corey Bienstock , Alan B. Cooper , Xiaolei Gao , Xin Yao , Hugh Y. Zhu , Joseph M. Kelly , Sobhana Babu Boga , Abdul-Basit Alhassan , Jayaram R. Tagat , Umar Faruk Mansoor , Kevin J. Wilson , Brendan M. O'Boyle , Matthew Hersh Daniels , Adam Schell , Phieng Siliphaivanh , Christian Fischer
发明人： Yongqi Deng , Liang Zhu , Gerald W. Shipps, Jr. , Sie-Mun Lo , Binyuan Sun , Xiaohua Huang , Corey Bienstock , Alan B. Cooper , Xiaolei Gao , Xin Yao , Hugh Y. Zhu , Joseph M. Kelly , Sobhana Babu Boga , Abdul-Basit Alhassan , Jayaram R. Tagat , Umar Faruk Mansoor , Kevin J. Wilson , Brendan M. O'Boyle , Matthew Hersh Daniels , Adam Schell , Phieng Siliphaivanh , Christian Fischer
IPC分类号： C07D401/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D401/14 , C07D405/14 , A61K31/454 , A61K31/4545 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/695 , A61K45/06 , C07F7/18
CPC分类号： C07D401/14 , A61K31/454 , A61K31/4545 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/695 , A61K45/06 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07F7/1804
摘要： The present invention provides a compound of the Formula I: (Formular I should be inserted here) or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2 and R3 are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.
摘要翻译： 本发明提供了式I化合物：（式I应在此插入）或其药学上可接受的盐，溶剂化物或酯，其中R，R 1，R 2和R 3如本文所定义。 这些化合物是ERK抑制剂。 还公开了包含上述化合物的药物组合物和使用其治疗癌症的方法。
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公开(公告)号：US20130096084A1
公开(公告)日：2013-04-18
申请号：US13703250
申请日：2011-06-22
申请人： Yongqi Deng , Liang Zhu , Gerald W. Shipps, JR. , Sie-Mun Lo , Binyuan Sun , Xiaohua Huang , Corey Bienstock , Alan B. Cooper , Xiaolei Gao , Xin Yao , Hugh Y. Zhu , Joseph M. Kelly , Sobhana Babu Boga , Abdul-Basit Alhassan , Jayaram R. Tagat , Umar Faruk Mansoor , Kevin J. Wilson , Brendan M. O'Boyle , Matthew Hersh Daniels , Adam Schell , Phieng Siliphaivanh , Christian Fischer
发明人： Yongqi Deng , Liang Zhu , Gerald W. Shipps, JR. , Sie-Mun Lo , Binyuan Sun , Xiaohua Huang , Corey Bienstock , Alan B. Cooper , Xiaolei Gao , Xin Yao , Hugh Y. Zhu , Joseph M. Kelly , Sobhana Babu Boga , Abdul-Basit Alhassan , Jayaram R. Tagat , Umar Faruk Mansoor , Kevin J. Wilson , Brendan M. O'Boyle , Matthew Hersh Daniels , Adam Schell , Phieng Siliphaivanh , Christian Fischer
IPC分类号： C07D401/14 , A61K45/06 , C07D405/14 , A61K31/454 , A61K31/55 , A61K31/551 , C07D401/12 , C07D409/14 , C07D417/14 , A61K31/506 , C07D471/04 , C07F7/18 , A61K31/695 , C07D413/14 , A61K31/5377 , A61K31/4545
CPC分类号： C07D401/14 , A61K31/454 , A61K31/4545 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/695 , A61K45/06 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07F7/1804
摘要： The present invention provides a compound of the Formula I: (Formular I should be inserted here) or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2 and R3 are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.
摘要翻译： 本发明提供了式I化合物：（式I应在此插入）或其药学上可接受的盐，溶剂化物或酯，其中R，R 1，R 2和R 3如本文所定义。 这些化合物是ERK抑制剂。 还公开了包含上述化合物的药物组合物和使用其治疗癌症的方法。
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7.发明授权公开(公告)号：US08871796B2
公开(公告)日：2014-10-28
申请号：US13501628
申请日：2010-10-05
申请人： William Colby Brown , Jason Brubaker , Christian Fischer , Richard W. Heidebrecht , John T. Hendrix , Elizabeth H. Kelley , Rachel N. MacCoss , Joey L. Methot , Thomas Miller , Karin M. Otte , Phieng Siliphaivanh , Thomas Reger , Peter D. Williams , Catherine M. Wiscount
发明人： William Colby Brown , Jason Brubaker , Christian Fischer , Richard W. Heidebrecht , John T. Hendrix , Elizabeth H. Kelley , Rachel N. MacCoss , Joey L. Methot , Thomas Miller , Karin M. Otte , Phieng Siliphaivanh , Thomas Reger , Peter D. Williams , Catherine M. Wiscount
IPC分类号： A61K31/415 , C07D401/00 , C07D421/00 , C07D405/10 , C07D413/12 , C07D409/12 , C07D417/12 , C07D231/22 , C07D413/14 , C07D491/113 , C07D405/12 , C07D401/04 , C07D405/14 , C07D401/12
CPC分类号： C07D231/22 , C07D231/20 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D491/113
摘要： The invention encompasses a novel class of diaryl ether derivatives which inhibit the processing of APP by the putative γ-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.
摘要翻译： 本发明包括一类新的二芳基醚衍生物，其抑制通过推定的γ-分泌酶处理APP，同时保留Notch信号通路，因此可用于治疗或预防阿尔茨海默病而不发展Notch抑制介导的胃肠道问题。 还包括药物组合物和使用方法。
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8.发明申请DIARYL ETHER DERIVATIVES AS NOTCH SPARING GAMMA SECRETASE INHIBITORS 有权DIARYL醚衍生物作为Notch SPARING GAMMA秘密酶抑制剂公开(公告)号：US20130053386A1
公开(公告)日：2013-02-28
申请号：US13501628
申请日：2010-10-05
申请人： William Colby Brown , Richard W. Heidebrecht , Jason Brubaker , Christian Fischer , John T. Hendrix , Elizabeth H. Kelley , Rachel N. MacCoss , Joey L. Methot , Thomas Miller , Karin M. Otte , Phieng Siliphaivanh , Thomas Reger , Peter D. Williams , Catherine M. Wiscount
发明人： William Colby Brown , Richard W. Heidebrecht , Jason Brubaker , Christian Fischer , John T. Hendrix , Elizabeth H. Kelley , Rachel N. MacCoss , Joey L. Methot , Thomas Miller , Karin M. Otte , Phieng Siliphaivanh , Thomas Reger , Peter D. Williams , Catherine M. Wiscount
IPC分类号： C07D231/20 , C07D403/12 , A61K31/4155 , C07D401/12 , A61K31/4439 , A61K31/454 , A61K31/506 , C07D401/04 , C07D405/12 , C07D413/12 , A61K31/4245 , A61K31/422 , A61K31/5377 , C07D491/113 , A61K31/438 , A61K31/496 , C07D413/14 , A61P25/28 , A61K31/415
CPC分类号： C07D231/22 , C07D231/20 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D491/113
摘要： The invention encompasses a novel class of diaryl ether derivatives which inhibit the processing of APP by the putative γ-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.
摘要翻译： 本发明包括一类新的二芳基醚衍生物，其抑制通过推定的γ-分泌酶处理APP，同时保留Notch信号通路，因此可用于治疗或预防阿尔茨海默病而不发展Notch抑制介导的胃肠道问题。 还包括药物组合物和使用方法。
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公开(公告)号：US10442819B2
公开(公告)日：2019-10-15
申请号：US15532549
申请日：2015-12-01
申请人： Christian Fischer , Stephane L. Bogen , Matthew L. Childers , Francesc Xavier Fradera Llinas , J. Michael Ellis , Sara Esposite , Qingmei Hong , Chunhui Huang , Alexander J. Kim , John W. Lampe , Michelle R. Machacek , Daniel R. McMasters , Ryan D. Otte , Dann L. Parker, Jr. , Michael Reutershan , Nunzio Sciammetta , Pengcheng P. Shao , David L. Sloman , Feroze Ujjainwalla , Catherine White , Zhicai Wu , Yang Yu , Kake Zhao , Craig Gibeau , Tesfaye Biftu , Purakkattle Biju , Lei Chen , Joshua Close , Peter H. Fuller , Xianhai Huang , Min K. Park , Valdimir Simov , David J. Witter , Hongjun Zhang
发明人： Christian Fischer , Stephane L. Bogen , Matthew L. Childers , Francesc Xavier Fradera Llinas , J. Michael Ellis , Sara Esposite , Qingmei Hong , Chunhui Huang , Alexander J. Kim , John W. Lampe , Michelle R. Machacek , Daniel R. McMasters , Ryan D. Otte , Dann L. Parker, Jr. , Michael Reutershan , Nunzio Sciammetta , Pengcheng P. Shao , David L. Sloman , Feroze Ujjainwalla , Catherine White , Zhicai Wu , Yang Yu , Kake Zhao , Craig Gibeau , Tesfaye Biftu , Purakkattle Biju , Lei Chen , Joshua Close , Peter H. Fuller , Xianhai Huang , Min K. Park , Valdimir Simov , David J. Witter , Hongjun Zhang
IPC分类号： A61K31/351 , A61K31/4353 , A61K31/5355 , A61K31/551 , C07D471/04 , C07D471/14 , C07D498/08 , C07D471/08 , C07D498/04 , C07D498/10 , A01N43/00
摘要： The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
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公开(公告)号：US11274111B2
公开(公告)日：2022-03-15
申请号：US16973623
申请日：2019-06-14
发明人： Abdelghani Abe Achab , Jared N. Cumming , Christian Fischer , Symon Gathiaka , Charles A. Lesburg , Derun Li , Min Lu , Matthew J. Mitcheltree , Anandan Palani , Rachel L. Palte , David L. Sloman , Hongjun Zhang
摘要： Described herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof. The compounds of Formula (I) act as arginase inhibitors and can be useful in preventing, treating or acting as a remedial agent for arginase-related diseases.
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