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公开(公告)号:US08609675B2
公开(公告)日:2013-12-17
申请号:US13379685
申请日:2010-06-30
申请人: Cliff C. Cheng , Hongbo Zeng , Gerald W. Shipps, Jr. , Yongqi Deng , Zhaoyang Meng , Lianyun Zhao , Yang Nan , Binyuan Sun , Duan Liu , Panduranga A. Reddy , M. Arshad Siddiqui
发明人: Cliff C. Cheng , Hongbo Zeng , Gerald W. Shipps, Jr. , Yongqi Deng , Zhaoyang Meng , Lianyun Zhao , Yang Nan , Binyuan Sun , Duan Liu , Panduranga A. Reddy , M. Arshad Siddiqui
IPC分类号: A01N43/54 , C07D491/00
CPC分类号: C07D487/14
摘要: The present invention provides Fused Tricyclic Compounds of the Formula (I) wherein Q, R1, R2, R3, and R4 are as defined herein, and pharmaceutically acceptable salts of such Fused Tricyclic Compounds. The Fused Tricyclic Compounds are useful in the treatment of cancer and other proliferative disorders.
摘要翻译: 本发明提供了其中Q,R 1,R 2,R 3和R 4如本文所定义的式(I)的稠合三环化合物和这种稠合三环化合物的药学上可接受的盐。 融合的三环化合物可用于治疗癌症和其他增殖性疾病。
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公开(公告)号:US20120178744A1
公开(公告)日:2012-07-12
申请号:US13379685
申请日:2010-06-30
申请人: Cliff C. Cheng , Hongbo Zeng , Gerald W. Shipps, JR. , Yongqi Deng , Zhaoyang Meng , Lianyun Zhao , Yang Nan , Binyuan Sun , Duan Liu , Panduranga A. Reddy , M. Arshad Siddiqui
发明人: Cliff C. Cheng , Hongbo Zeng , Gerald W. Shipps, JR. , Yongqi Deng , Zhaoyang Meng , Lianyun Zhao , Yang Nan , Binyuan Sun , Duan Liu , Panduranga A. Reddy , M. Arshad Siddiqui
IPC分类号: A61K31/541 , A61K31/519 , A61P35/00 , C07D487/14
CPC分类号: C07D487/14
摘要: The present invention provides Fused Tricyclic Compounds of the Formula (I) wherein Q, R1, R2, R3, and R4 are as defined herein, and pharmaceutically acceptable salts of such Fused Tricyclic Compounds. The Fused Tricyclic Compounds are useful in the treatment of cancer and other proliferative disorders.
摘要翻译: 本发明提供了其中Q,R 1,R 2,R 3和R 4如本文所定义的式(I)的稠合三环化合物和这种稠合的三环化合物的药学上可接受的盐。 融合的三环化合物可用于治疗癌症和其他增殖性疾病。
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公开(公告)号:US08591943B2
公开(公告)日:2013-11-26
申请号:US13263193
申请日:2010-04-08
申请人: Yongqi Deng , Binyuan Sun , Hongbo Zeng , Matthew Richards , Gerald W. Shipps, Jr. , Cliff C. Cheng , Yinyan Zhao , Andrew McRiner , Zhaoyang Meng , Yang Nan , Mehul F. Patel , Iwona E. Wrona , Panduranga Adulla Reddy , Brian M. Eklov , Shuyi Tang , Duan Liu , Amit K. Mandal , Lianyun Zhao , M. Arshad Siddiqui
发明人: Yongqi Deng , Binyuan Sun , Hongbo Zeng , Matthew Richards , Gerald W. Shipps, Jr. , Cliff C. Cheng , Yinyan Zhao , Andrew McRiner , Zhaoyang Meng , Yang Nan , Mehul F. Patel , Iwona E. Wrona , Panduranga Adulla Reddy , Brian M. Eklov , Shuyi Tang , Duan Liu , Amit K. Mandal , Lianyun Zhao , M. Arshad Siddiqui
IPC分类号: A61K9/127 , A61K39/395 , A61K31/554 , A61K31/541 , A61K31/5377 , A61K38/50 , A61K31/553 , A61K33/24 , A61K31/704 , A61K31/551 , A61K31/538 , A61K31/519
CPC分类号: C07D487/04 , C07D519/00
摘要: The present invention provides methods for inhibiting mTOR using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with mTOR using such compounds.
摘要翻译: 本发明提供使用吡唑并[1,5-a]嘧啶化合物抑制mTOR的方法以及使用这些化合物治疗,预防,抑制或改善与mTOR相关的一种或多种疾病的方法。
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公开(公告)号:US20120114739A1
公开(公告)日:2012-05-10
申请号:US13263193
申请日:2010-04-08
申请人: Yongqi Deng , Binyuan Sun , Hongbo Zeng , Matthew Richards , Gerald W. Shipps, JR. , Cliff C. Cheng , Yinyan Zhao , Andrew McRiner , Zhaoyang Meng , Yang Nan , Mehul F. Patel , Iwona E. Wrona , Panduranga Adulla Reddy , Brian M. Eklov , Shuyi Tang , Duan Liu , Amit K. Mandal , Lianyun Zhao , M. Asshad Siddiqui
发明人: Yongqi Deng , Binyuan Sun , Hongbo Zeng , Matthew Richards , Gerald W. Shipps, JR. , Cliff C. Cheng , Yinyan Zhao , Andrew McRiner , Zhaoyang Meng , Yang Nan , Mehul F. Patel , Iwona E. Wrona , Panduranga Adulla Reddy , Brian M. Eklov , Shuyi Tang , Duan Liu , Amit K. Mandal , Lianyun Zhao , M. Asshad Siddiqui
IPC分类号: A61K9/127 , A61K31/519 , A61K31/5377 , C07D491/048 , C07D495/04 , A61K31/538 , A61K31/551 , A61K31/553 , A61K31/541 , A61K31/554 , C07D498/04 , C12N9/99 , A61K31/704 , A61K39/395 , A61K33/36 , A61K38/50 , A61K33/24 , A61P29/00 , A61P37/08 , A61P11/00 , A61P37/06 , A61P35/00 , A61P35/02 , C07D487/04
CPC分类号: C07D487/04 , C07D519/00
摘要: The present invention provides methods for inhibiting mTOR using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with mTOR using such compounds.
摘要翻译: 本发明提供使用吡唑并[1,5-a]嘧啶化合物抑制mTOR的方法以及使用这些化合物治疗,预防,抑制或改善与mTOR相关的一种或多种疾病的方法。
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公开(公告)号:US07446195B2
公开(公告)日:2008-11-04
申请号:US11505263
申请日:2006-08-16
申请人: Yongqi Deng , Lianyun Zhao , Gerald W. Shipps, Jr. , Patrick J. Curran , M. Arshad Siddiqui , Rumin Zhang , Charles W. McNemar , Todd W. Mayhood , William T. Windsor , Emma M. Lees , David A. Parry
发明人: Yongqi Deng , Lianyun Zhao , Gerald W. Shipps, Jr. , Patrick J. Curran , M. Arshad Siddiqui , Rumin Zhang , Charles W. McNemar , Todd W. Mayhood , William T. Windsor , Emma M. Lees , David A. Parry
IPC分类号: C07D413/12 , C07D403/12 , C07D409/12 , C07D405/12
CPC分类号: C07D405/12 , C07D333/40 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要: Inhibitors of cyclin dependent kinase 2, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions including them are useful for treating disease or disease symptoms. The invention also provides for methods of making CDK-2 inhibitor compounds, methods of inhibiting CDK-2, and methods for treating disease or disease symptoms.
摘要翻译: 描述了细胞周期蛋白依赖性激酶2的抑制剂,包括抑制剂的组合物,以及使用抑制剂和抑制剂组合物的方法。 包括它们的抑制剂和组合物可用于治疗疾病或疾病症状。 本发明还提供了制备CDK-2抑制剂化合物的方法,抑制CDK-2的方法以及治疗疾病或疾病症状的方法。
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公开(公告)号:US07511063B2
公开(公告)日:2009-03-31
申请号:US11504869
申请日:2006-08-16
申请人: Yongqi Deng , Patrick J. Curran , Gerald W. Shipps, Jr. , Lianyun Zhao , M. Arshad Siddiqui , Janeta Popovici-Muller , Jose S. Duca , Alan W. Hruza , Thierry O. Fischmann , Vincent S. Madison , Rumin Zhang , Charles W. McNemar , Todd W. Mayhood , William T. Windsor , Emma M. Lees , David A. Parry
发明人: Yongqi Deng , Patrick J. Curran , Gerald W. Shipps, Jr. , Lianyun Zhao , M. Arshad Siddiqui , Janeta Popovici-Muller , Jose S. Duca , Alan W. Hruza , Thierry O. Fischmann , Vincent S. Madison , Rumin Zhang , Charles W. McNemar , Todd W. Mayhood , William T. Windsor , Emma M. Lees , David A. Parry
IPC分类号: A61K31/47 , C07D215/14
CPC分类号: C07D409/04 , C07D215/48 , C07D215/50 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D409/12 , C07D409/14 , C07D413/10 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/10
摘要: Quinoline-based inhibitors of cyclin dependent kinase 2, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions including them are useful for treating disease or disease symptoms. The invention also provides for methods of making CDK-2 inhibitor compounds, methods of inhibiting CDK-2, and methods for treating disease or disease symptoms.
摘要翻译: 描述了基于喹啉的细胞周期蛋白依赖性激酶2抑制剂,包括抑制剂的组合物,以及使用抑制剂和抑制剂组合物的方法。 包括它们的抑制剂和组合物可用于治疗疾病或疾病症状。 本发明还提供了制备CDK-2抑制剂化合物的方法,抑制CDK-2的方法以及治疗疾病或疾病症状的方法。
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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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公开(公告)号:US07807672B2
公开(公告)日:2010-10-05
申请号:US11705709
申请日:2007-02-13
申请人: Yongqi Deng , Gerald W. Shipps, Jr. , Alan Cooper , Yang Nan , Tong Wang , M. Arshad Siddiqui , Hugh Zhu , Robert Sun , Joseph M. Kelly , Ronald Doll , Jagdish Desai , James J-S Wang , Youhao Dong , Vincent Madison , Li Xiao , Alan Hruza , Neng-Yang Shih
发明人: Yongqi Deng , Gerald W. Shipps, Jr. , Alan Cooper , Yang Nan , Tong Wang , M. Arshad Siddiqui , Hugh Zhu , Robert Sun , Joseph M. Kelly , Ronald Doll , Jagdish Desai , James J-S Wang , Youhao Dong , Vincent Madison , Li Xiao , Alan Hruza , Neng-Yang Shih
IPC分类号: A61K31/506 , A61K31/5377 , A61K31/4025 , A61K31/496 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/06 , C07D417/12
CPC分类号: C07D207/16 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/08
摘要: Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts 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 substituents 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。 所有其它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: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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