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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: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: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: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: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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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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7.
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.DIARYL ETHER DERIVATIVES AS NOTCH SPARING GAMMA SECRETASE INHIBITORS 有权
标题翻译: 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: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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10.Substituted diazine and triazine spleen tyrosine kinease (Syk) inhibitors 有权
标题翻译: 取代的二嗪和三嗪脾脏酪氨酸激酶(Syk)抑制剂公开(公告)号:US09416111B2
公开(公告)日:2016-08-16
申请号:US14409200
申请日:2013-06-17
发明人: Andrew M. Haidle , Michael D. Altman , Solomon D. Kattar , Matthew Christopher , John Michael Ellis , Christian Fischer , Alan B. Northrup , Kaleen Konrad Childers
IPC分类号: A61K31/506 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D417/14 , C07D239/42 , A61K45/06 , C07D413/14 , C07D409/14 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/551 , C07D239/47 , C07D239/48 , C07D401/12 , C07D403/04 , C07D405/12 , C07D409/12 , C07D413/12
CPC分类号: C07D239/42 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/551 , A61K45/06 , C07D239/47 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14
摘要: The invention provides certain substituted diazine and triazine compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
摘要翻译: 本发明提供了式(I)(I)的某些取代的二嗪和三嗪化合物或其药学上可接受的盐,其中R1,R2,R3,R4,Rcy,Cy和t如本文所定义。 本发明还提供包含这些化合物的药物组合物,以及使用该化合物治疗由脾脏酪氨酸激酶(Syk)激酶介导的疾病或病症的方法。
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