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公开(公告)号：US20110189192A1
公开(公告)日：2011-08-04
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 , Joseph M. Kelly , Subrahmanyam Gudipati , Ronald J. Doll , Mehul F. Patel , Jagdish A. Desai , James J-S Wang , Sunil Paliwal , Hon-Chung Tsui , Sobhana Babu Boga , Abdul-Basit Alhassan , Xiaolei Gao , Liang Zhu , Xin Yao
发明人： Alan B. Cooper , Yang Nan , Yongqi Deng , Gerald W. Shipps, JR. , Neng-Yang Shih , Hugh Y. Zhu , Joseph M. Kelly , Subrahmanyam Gudipati , Ronald J. Doll , Mehul F. Patel , Jagdish A. Desai , James J-S Wang , Sunil Paliwal , Hon-Chung Tsui , Sobhana Babu Boga , Abdul-Basit Alhassan , Xiaolei Gao , Liang Zhu , Xin Yao
IPC分类号： A61K31/444 , C07D401/14 , C07D409/14 , C07D417/14 , A61K31/501 , A61K39/395 , A61K31/7052 , A61P35/02 , A61P35/00
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：US20110038876A1
公开(公告)日：2011-02-17
申请号：US12601476
申请日：2008-06-17
申请人： Robert Sun , Alan B. Cooper , Yongqi Deng , Tong Wang , Yang Nan , Hugh Y. Zhu , Sobhana Babu Boga , Xiaolei Gao , Joseph M. Kelly , Sunil Paliwal , Hon-Chung Tsui , Ronald J. Doll , Neng-Yang Shih
发明人： Robert Sun , Alan B. Cooper , Yongqi Deng , Tong Wang , Yang Nan , Hugh Y. Zhu , Sobhana Babu Boga , Xiaolei Gao , Joseph M. Kelly , Sunil Paliwal , Hon-Chung Tsui , Ronald J. Doll , Neng-Yang Shih
IPC分类号： A61K31/519 , C07D487/04 , C07D487/08 , A61K31/496 , A61K39/395 , A61P35/00 , A61P35/02
CPC分类号： C07D487/04 , C07D519/00
摘要： Disclosed are the ERK inhibitors of formula 1.0: [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：[式（1.0）]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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公开(公告)号：US20090118284A1
公开(公告)日：2009-05-07
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： A61K31/496 , C07D403/14 , C07D413/14 , A61K31/506 , A61P35/00 , A61P35/02 , A61K31/4439 , A61K31/5377 , C07D401/14
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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公开(公告)号：US20180141962A1
公开(公告)日：2018-05-24
申请号：US15564349
申请日：2016-04-04
申请人： JIAN LIU , JOSEPH KOZLOWSKI , RONALD KIM , XIAOLEI GAO , SOBHANA BABU BOGA , YOUNONG YU , HAO WU , SHILAN LIU , CHUNDAO YANG , MERCK SHARP & DOHME CORP.
发明人： JIAN LIU , JOSEPH KOZLOWSKI , RONALD KIM , XIAOLEI GAO , SOBHANA BABU BOGA , YOUNONG YU , HAO WU , SHILAN LIU , CHUNDAO YANG
IPC分类号： C07D519/00 , A61P19/02
CPC分类号： C07D519/00 , A61P19/02
摘要： The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, wherein CH, R1, R1a, R1b, R2, R3, and the subscripts m1, m2, p, q, and t are as set forth herein. The present invention also provides pharmaceutical compositions comprising these compounds and their use in therapy. In Cparticular, the present invention relates to the use of Btk inhibitor compounds of Formula (I) in the treatment of Btk mediated dis orders.
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公开(公告)号：US20170362243A1
公开(公告)日：2017-12-21
申请号：US15538925
申请日：2015-12-17
申请人： JIAN LIU , JOSEPH A. KOZLOWSKI , SOBHANA BABU BOGA , XIAOLEI GAO , DEODIAL GUY GUIADEEN , JYHSHING WANG , SHILAN LIU
发明人： JIAN LIU , JOSEPH A. KOZLOWSKI , SOBHANA BABU BOGA , XIAOLEI GAO , DEODIAL GUY GUIADEEN , JYHSHING WANG , SHILAN LIU
IPC分类号： C07D487/04 , A61K31/4985
CPC分类号： C07D487/04 , A61K31/4985 , A61K45/06 , A61P3/10 , A61P11/00 , A61P11/06 , A61P19/02 , A61P29/00 , A61P37/00 , A61P37/06
摘要： The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula (I) in the treatment of Btk mediated disorders.
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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：US10208047B2
公开(公告)日：2019-02-19
申请号：US15538910
申请日：2015-12-17
申请人： Jian Liu , Joseph A. Kozlowski , Brian M. Andresen , Sobhana Babu Boga , Xiaolei Gao , Deodial Guy Guiadeen , Jiaqiang Cai , Shilan Liu , Dahai Wang , Hao Wu , Chundao Yang
发明人： Jian Liu , Joseph A. Kozlowski , Brian M. Andresen , Sobhana Babu Boga , Xiaolei Gao , Deodial Guy Guiadeen , Jiaqiang Cai , Shilan Liu , Dahai Wang , Hao Wu , Chundao Yang
IPC分类号： C07D487/04 , A61K31/4985 , A61K45/06
摘要： The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I, or pharmaceutically acceptable salts thereof, Formula I or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula I in the treatment of Btk mediated disorders.
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公开(公告)号：US20180079752A1
公开(公告)日：2018-03-22
申请号：US15578775
申请日：2016-05-31
申请人： ADRIANUS PETRUS ANTONIUS DE MAN , RONALD KIM , JIAN LIU , JOSEPH A. KOZLOWSKI , SOBHANA BABU BOGA , THIERRY FISCHMANN , DEODIAL Guy GUIADEEN , ILSE HENDRICA MARIA POLS-DE ROOIJ , SHILAN LIU , HAO WU
发明人： ADRIANUS PETRUS ANTONIUS DE MAN , RONALD KIM , JIAN LIU , JOSEPH A. KOZLOWSKI , SOBHANA BABU BOGA , THIERRY FISCHMANN , DEODIAL Guy GUIADEEN , ILSE HENDRICA MARIA POLS-DE ROOIJ , SHILAN LIU , HAO WU
IPC分类号： C07D487/04 , A61K31/4985 , A61K31/5377
CPC分类号： C07D487/04 , A61K31/4985 , A61K31/5377 , A61P19/02
摘要： The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula I in the treatment of Btk mediated disorders.
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公开(公告)号：US20170362242A1
公开(公告)日：2017-12-21
申请号：US15538902
申请日：2015-12-17
申请人： JIAN LIU , JOSEPH A. KOZLOWSKI , ABDUL-BASIT ALHASSAN , SOBHANA BABU BOGA , XIAOLEI GAO , DEODIAL GUY GUIADEEN , JYHSHING WANG , WENSHENG YU , JIAQIANG CAI , SHILAN LIU , DAHAI WANG , HAO WU , CHUNDAO YANG
发明人： JIAN LIU , JOSEPH A. KOZLOWSKI , ABDUL-BASIT ALHASSAN , SOBHANA BABU BOGA , XIAOLEI GAO , DEODIAL GUY GUIADEEN , JYHSHING WANG , WENSHENG YU , JIAQIANG CAI , SHILAN LIU , DAHAI WANG , HAO WU , CHUNDAO YANG
IPC分类号： C07D487/04 , A61K31/4985 , A61K31/5377 , C07D519/00
CPC分类号： C07D487/04 , A61K31/4985 , A61K31/5377 , A61K45/06 , A61P37/02 , C07D519/00
摘要： The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula (I) in the treatment of Btk mediated disorders.
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