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公开(公告)号：US09351965B2
公开(公告)日：2016-05-31
申请号：US13994224
申请日：2011-12-16
申请人： Gerald W. Shipps, Jr. , Xiaohua Huang , Yongqi Deng , Liang Zhu , Alan B. Cooper , Binyuan Sun , Abdelghani Achab , Sie-Mun Lo
发明人： Gerald W. Shipps, Jr. , Xiaohua Huang , Yongqi Deng , Liang Zhu , Alan B. Cooper , Binyuan Sun , Abdelghani Achab , Sie-Mun Lo
IPC分类号： C07D231/56 , C07D401/04 , C07D471/04 , C07D401/14 , C07D403/14 , C07D417/04 , A61K31/416 , A61K31/4439 , A61K45/06 , A61K31/437
CPC分类号： A61K31/4439 , A61K31/416 , A61K31/437 , A61K45/06 , C07D231/56 , C07D401/04 , C07D401/14 , C07D403/14 , C07D417/04 , C07D471/04 , A61K2300/00
摘要： The present invention provides a compound of the Formula I, or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2, R3, m and are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions that comprise the above compounds, and methods of treating cancer using the same.
摘要翻译： 本发明提供式I化合物或其药学上可接受的盐，溶剂化物或酯，其中R，R 1，R 2，R 3，m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的癌症治疗方法。
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公开(公告)号：US20130261125A1
公开(公告)日：2013-10-03
申请号：US13994224
申请日：2011-12-16
申请人： Gerald W. Shipps, JR. , Xiaohua Huang , Yongqi Deng , Liang Zhu , Alan B. Cooper , Binyuan Sun , Abdelghani Achab , Sie-Mun Lo
发明人： Gerald W. Shipps, JR. , Xiaohua Huang , Yongqi Deng , Liang Zhu , Alan B. Cooper , Binyuan Sun , Abdelghani Achab , Sie-Mun Lo
IPC分类号： A61K31/4439 , C07D471/04 , A61K31/437 , C07D401/04
CPC分类号： A61K31/4439 , A61K31/416 , A61K31/437 , A61K45/06 , C07D231/56 , C07D401/04 , C07D401/14 , C07D403/14 , C07D417/04 , C07D471/04 , A61K2300/00
摘要： The present invention provides a compound of the Formula I, or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2, R3, m and are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions that comprise the above compounds, and methods of treating cancer using the same.
摘要翻译： 本发明提供式I化合物或其药学上可接受的盐，溶剂化物或酯，其中R，R 1，R 2，R 3，m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的癌症治疗方法。
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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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公开(公告)号：US08999966B2
公开(公告)日：2015-04-07
申请号：US13881050
申请日：2011-10-24
申请人： Sobhana Babu Boga , Joseph M. Kelly , Hugh Y. Zhu , Abdul-Basit Alhassan , Xin Yao , Xiaolei Gao , James J-S Wang , Jagdish A. Desai , Subrahmanyam Gudipati , Sie-Mun Lo , Liang Zhu , Alan B. Cooper , Yongqi Deng , Gerald W. Shipps, Jr.
发明人： Sobhana Babu Boga , Joseph M. Kelly , Hugh Y. Zhu , Abdul-Basit Alhassan , Xin Yao , Xiaolei Gao , James J-S Wang , Jagdish A. Desai , Subrahmanyam Gudipati , Sie-Mun Lo , Liang Zhu , Alan B. Cooper , Yongqi Deng , Gerald W. Shipps, Jr.
IPC分类号： A61K31/397 , A61K31/5377 , A61K31/506 , A61K31/4545 , A61K31/454 , A61K31/4523 , A61K31/4427 , A61K31/4439 , A61K31/444 , C07D413/14 , C07D401/14 , C07D403/14 , C07D221/00 , C07D221/02 , C07D211/80 , C07D405/14 , C07D409/14 , C07D417/14 , C07D471/04 , A61K45/06
CPC分类号： C07D401/14 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/5377 , A61K45/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof, wherein: A is a five membered monocyclic heteroaryl ring; and B is a monocyclic heterocycloalkyl ring, or a monocyclic heterocycloalkenyl ring, or a bridged monocyclic heterocycloalkyl ring, or a fused (monocyclic heterocycloalkyl ring) cyclopropyl ring. 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，其中：A是五元单环杂芳基环; 和B是单环杂环烷基环，或单环杂环烯基环，或桥连单环杂环烷基环，或稠合（单环杂环烷基环）环丙基环。 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：US20130237518A1
公开(公告)日：2013-09-12
申请号：US13881050
申请日：2011-10-24
申请人： Sobhana Babu Boga , Joseph M. Kelly , Hugh Y. Zhu , Abdul-Basit Alhassan , Xin Yao , Xiaolei Gao , James J-S Wang , Jagdish A. Desai , Subrahmanyam Gudipati , Sie-Mun Lo , Liang Zhu , Alan B. Cooper , Yongqi Deng , Gerald W. Shipps, JR.
发明人： Sobhana Babu Boga , Joseph M. Kelly , Hugh Y. Zhu , Abdul-Basit Alhassan , Xin Yao , Xiaolei Gao , James J-S Wang , Jagdish A. Desai , Subrahmanyam Gudipati , Sie-Mun Lo , Liang Zhu , Alan B. Cooper , Yongqi Deng , Gerald W. Shipps, JR.
IPC分类号： C07D401/14 , C07D471/04 , C07D417/14 , C07D409/14 , A61K31/5377 , A61K45/06 , A61K31/4545 , A61K31/444 , A61K31/454 , C07D413/14 , C07D405/14
CPC分类号： C07D401/14 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/5377 , A61K45/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof, wherein: A is a five membered monocyclic heteroaryl ring; and B is a monocyclic heterocycloalkyl ring, or a monocyclic heterocycloalkenyl ring, or a bridged monocyclic heterocycloalkyl ring, or a fused (monocyclic heterocycloalkyl ring) cyclopropyl ring. 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，其中：A是五元单环杂芳基环; 和B是单环杂环烷基环，或单环杂环烯基环，或桥连单环杂环烷基环，或稠合（单环杂环烷基环）环丙基环。 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：US20130158020A1
公开(公告)日：2013-06-20
申请号：US13819366
申请日：2011-08-29
申请人： Yongqi Deng , Gerald W. Shipps, JR. , Sie-Mun Lo , Liang Zhu , Alan B. Cooper , Kiran Muppalla
发明人： Yongqi Deng , Gerald W. Shipps, JR. , Sie-Mun Lo , Liang Zhu , Alan B. Cooper , Kiran Muppalla
IPC分类号： A61K31/541 , A61K31/5377 , A61K45/06 , C07D401/14 , A61K31/4545 , A61K31/496 , C07D413/14 , C07D417/14
CPC分类号： A61K31/541 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K45/06 , C07D401/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D491/113
摘要： The present invention provides a compound of the Formula I: Formula I or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2, R3, R4, X, m and n 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： 本发明提供式I化合物：式I或其药学上可接受的盐，溶剂合物或酯，其中R，R 1，R 2，R 3，R 4，X，m和n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：US20130172341A1
公开(公告)日：2013-07-04
申请号：US13821149
申请日：2011-09-12
申请人： Gerald W. Shipps, JR. , Yongqi Deng , Alan B. Cooper , Xiaolei Gao , Binyuan Sun , James Wang , Liang Zhu
发明人： Gerald W. Shipps, JR. , Yongqi Deng , Alan B. Cooper , Xiaolei Gao , Binyuan Sun , James Wang , Liang Zhu
IPC分类号： C07D471/04 , C07D405/04 , C07D401/04 , C07D401/14 , C07D417/14
CPC分类号： C07D471/04 , C07D401/04 , C07D401/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D417/14 , C07D519/00
摘要： Disclosed are the ERK inhibitors of Formula (I): (Formula (I)) and the pharmaceutically acceptable salts thereof. All substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of Formula (I).
摘要翻译： 公开了式（I）：（式（I））的ERK抑制剂及其药学上可接受的盐。 所有取代基如本文所定义。 还公开了使用式（I）的化合物治疗癌症的方法。
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公开(公告)号：US08716483B2
公开(公告)日：2014-05-06
申请号：US12918099
申请日：2009-02-19
申请人： Alan B. Cooper , Yang Nan , Yongqi Deng , Gerald W. Shipps, Jr. , Neng-Yang Shih , Hugh Y. Zhu , Jagdish A. Desai , James J-S Wang , Sunil Paliwal , Hon-Chung Tsui , Sobhana Babu Boga , Abdul-Basit Alhassan , Xiaolei Gao , Liang Zhu , Ahmed Samatar
发明人： Alan B. Cooper , Yang Nan , Yongqi Deng , Gerald W. Shipps, Jr. , Neng-Yang Shih , Hugh Y. Zhu , Jagdish A. Desai , James J-S Wang , Sunil Paliwal , Hon-Chung Tsui , Sobhana Babu Boga , Abdul-Basit Alhassan , Xiaolei Gao , Liang Zhu , Ahmed Samatar
IPC分类号： C07D401/04 , A61K31/444
CPC分类号： C07D403/14
摘要： Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts, and solvates thereof. Q is a tetrahydropyridinyl ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.
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和溶剂化物。 Q是四氢吡啶环。 所有其他取代基如本文所定义。 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：US08546404B2
公开(公告)日：2013-10-01
申请号：US11810282
申请日：2007-06-05
申请人： Alan B. Cooper , Yongqi Deng , Gerald W. Shipps, Jr. , Neng-Yang Shih , Hugh Y. Zhu , Robert Sun , Joseph M. Kelly , Ronald J. Doll , Yang Nan , Tong Wang , Jagdish A. Desai , James J-S Wang , Youhao Dong , Vincent S. Madison , Li Xiao , Alan W. Hruza , M. Arshad Siddiqui , Ahmed A. Samatar , Sunil Paliwal , Hon-Chung Tsui , Azim Alan Celebi , Yiji Wu , Sobhana Babu Boga , Abdul-Basit Alhassan , Xiaolei Gao , Liang Zhu , Mehul Patel
发明人： Alan B. Cooper , Yongqi Deng , Gerald W. Shipps, Jr. , Neng-Yang Shih , Hugh Y. Zhu , Robert Sun , Joseph M. Kelly , Ronald J. Doll , Yang Nan , Tong Wang , Jagdish A. Desai , James J-S Wang , Youhao Dong , Vincent S. Madison , Li Xiao , Alan W. Hruza , M. Arshad Siddiqui , Ahmed A. Samatar , Sunil Paliwal , Hon-Chung Tsui , Azim Alan Celebi , Yiji Wu , Sobhana Babu Boga , Abdul-Basit Alhassan , Xiaolei Gao , Liang Zhu , Mehul Patel
IPC分类号： A01N43/54 , C07D239/42 , C07D401/04
CPC分类号： C07D231/56 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/14
摘要： Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.
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，酯和溶剂化物。 Q是可以具有桥或稠合环的哌啶或哌嗪环。 哌啶环可以在环中具有双键。 所有其他取代基如本文所定义。 还公开了使用式1.0化合物治疗癌症的方法。
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