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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:US20150258074A1
公开(公告)日:2015-09-17
申请号:US14431485
申请日:2013-09-26
申请人: Kevin J. WILSON , David J. WITTER , Matthew H. DANIELS , Angie R. ANGELES , Phieng SILIPHAIVANH , David L. SLOMAN , Brendan O'BOYLE , Danielle FALCONE , Catherine WHITE , Ron FERGUSON , Wei ZHOU , Kathryn LIPFORD , Umar Faruk MANSOOR , Salem FEVRIRE , Xianhai HUANG , Ravi KURUKULASURIYA , Judson E. RICHARD , Shuyi TANG , Christopher BOYCE , Joseph KOZLOWSKI , Raman Kumar BAKSHI , Ganesh Babu UNAKARAN , Merck Sharp & Dohme Corp.
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: A61K31/437 , A61K45/06 , A61K31/4545 , C07D471/04
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: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: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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公开(公告)号:US20170267695A1
公开(公告)日:2017-09-21
申请号:US15531771
申请日:2015-12-10
申请人: Phieng Siliphaivanh , David L. Sloman , David Witter , Umar Faruk Mansoor , Joseph Kozlowski , Ziping Liu , Jianmin Fu , Zhilong Wan , Wei Liu , Yimin Qian , Xianhai Huang
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 , C07D471/22 , C07D471/18
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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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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