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公开(公告)号:US20100256115A1
公开(公告)日:2010-10-07
申请号:US12727218
申请日:2010-03-18
申请人: Frederick Cohen , Kurt Deshayes , Wayne J. Fairbrother , Bainian Feng , John A. Flygare , Lewis J. Gazzard , Vickie Hsiao-Wei Tsui
发明人: Frederick Cohen , Kurt Deshayes , Wayne J. Fairbrother , Bainian Feng , John A. Flygare , Lewis J. Gazzard , Vickie Hsiao-Wei Tsui
IPC分类号: A61K31/55 , C07D209/48 , A61K31/4035 , C07D277/06 , A61K31/427 , C07D487/04 , C07D231/40 , C07D285/06 , A61K31/4155 , A61K31/433 , C07D207/323 , A61K31/40 , C07D249/06 , A61K31/4192 , C07D261/14 , A61K31/42 , C07D257/06 , A61K31/41 , C07D271/04 , A61K31/4245 , C07D417/04 , A61K31/4439 , A61P35/00 , C12N5/071
CPC分类号: C07D417/14 , A61K31/55 , A61K38/177 , C07D403/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D495/04 , C07D513/04 , C07K5/06026 , C07K5/0806 , C07K5/0827 , C07K7/06 , C12N5/0693
摘要: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4′, R5, R5′, R6 and R6′ are as described herein.
摘要翻译: 本发明提供了可用作治疗恶性肿瘤的治疗剂的新的IAP抑制剂,其中化合物具有通式I:其中X,Y,A,R 1,R 2,R 3,R 4,R 4',R 5,R 5',R 6和 R6'如本文所述。
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公开(公告)号:US20120202750A1
公开(公告)日:2012-08-09
申请号:US13356556
申请日:2012-01-23
申请人: Frederick Cohen , Kurt Deshayes , Wayne J. Fairbrother , Bainian Feng , John A. Flygare , Lewis J. Gazzard , Vickie Hsiao-Wei Tsui
发明人: Frederick Cohen , Kurt Deshayes , Wayne J. Fairbrother , Bainian Feng , John A. Flygare , Lewis J. Gazzard , Vickie Hsiao-Wei Tsui
IPC分类号: C07D401/12 , A61K38/06 , A61K31/55 , C12N5/09 , A61K31/42 , A61K31/433 , A61K31/4436 , C07D285/10 , A61K31/426 , C07D261/14 , C07D271/08 , A61K31/415 , A61K31/381 , C07K5/08 , C07D513/04 , A61P35/04 , C07D417/04 , A61K31/4245 , C07D417/12 , C07D277/18 , C07D257/06 , A61K31/41 , C07D249/04 , C07D333/36 , A61K31/506
CPC分类号: C07D417/14 , A61K31/55 , A61K38/177 , C07D403/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D495/04 , C07D513/04 , C07K5/06026 , C07K5/0806 , C07K5/0827 , C07K7/06 , C12N5/0693
摘要: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4′, R5, R5′, R6 and R6′ are as described herein.
摘要翻译: 本发明提供了可用作治疗恶性肿瘤的治疗剂的新的IAP抑制剂,其中化合物具有通式I:其中X,Y,A,R 1,R 2,R 3,R 4,R 4',R 5,R 5',R 6和 R6'如本文所述。
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公开(公告)号:US08110568B2
公开(公告)日:2012-02-07
申请号:US12727218
申请日:2010-03-18
申请人: Frederick Cohen , Kurt Deshayes , Wayne J. Fairbrother , Bainian Feng , John A. Flygare , Lewis J. Gazzard , Vickie Hsiao-Wei Tsui
发明人: Frederick Cohen , Kurt Deshayes , Wayne J. Fairbrother , Bainian Feng , John A. Flygare , Lewis J. Gazzard , Vickie Hsiao-Wei Tsui
IPC分类号: A61K31/55 , A61K31/4035 , A61K31/427 , A61K31/4155 , A61K31/433 , A61K31/40 , A61K31/4192 , A61K31/42 , A61K31/41 , A61K31/4245 , A61K31/4439 , A61P35/00
CPC分类号: C07D417/14 , A61K31/55 , A61K38/177 , C07D403/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D495/04 , C07D513/04 , C07K5/06026 , C07K5/0806 , C07K5/0827 , C07K7/06 , C12N5/0693
摘要: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4′, R5, R5′, R6 and R6′ are as described herein.
摘要翻译: 本发明提供了可用作治疗恶性肿瘤的治疗剂的新的IAP抑制剂,其中化合物具有通式I:其中X,Y,A,R 1,R 2,R 3,R 4,R 4',R 5,R 5',R 6和 R6'如本文所述。
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公开(公告)号:US07244851B2
公开(公告)日:2007-07-17
申请号:US11174784
申请日:2005-07-05
申请人: Frederick Cohen , Kurt Deshayes , Wayne J. Fairbrother , Bainian Feng , John A. Flygare , Lewis J. Gazzard , Vickie Hsiao-Wei Tsui
发明人: Frederick Cohen , Kurt Deshayes , Wayne J. Fairbrother , Bainian Feng , John A. Flygare , Lewis J. Gazzard , Vickie Hsiao-Wei Tsui
IPC分类号: C07D207/09 , C07D231/12 , C07D233/60 , C07D263/32 , C07D275/02 , C07D257/04 , C07D285/06
CPC分类号: C07D417/14 , A61K31/55 , A61K38/177 , C07D403/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D495/04 , C07D513/04 , C07K5/06026 , C07K5/0806 , C07K5/0827 , C07K7/06 , C12N5/0693
摘要: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4′, R5, R5′, R6 and R6′ are as described herein.
摘要翻译: 本发明提供可用作治疗恶性肿瘤的治疗剂的IAP的新型抑制剂,其中化合物具有通式I:其中X,Y,A,R 1,R 2, R 3,R 4,R 4,R 5,R 5,R 5, R 6,R 6和R 6'如本文所述。
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公开(公告)号:US08980837B2
公开(公告)日:2015-03-17
申请号:US13356556
申请日:2012-01-23
申请人: Frederick Cohen , Kurt Deshayes , Wayne J. Fairbrother , Bainian Feng , John A. Flygare , Lewis J. Gazzard , Vickie Hsiao-Wei Tsui
发明人: Frederick Cohen , Kurt Deshayes , Wayne J. Fairbrother , Bainian Feng , John A. Flygare , Lewis J. Gazzard , Vickie Hsiao-Wei Tsui
IPC分类号: A61K38/06 , A61K31/55 , A61K31/42 , A61K31/433 , A61K31/4436 , A61K31/426 , A61K31/415 , A61K31/381 , A61P35/04 , A61K31/4245 , A61K31/41 , A61K31/506 , C07D417/14 , C12N5/09 , A61K38/17 , C07D403/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D495/04 , C07D513/04 , C07K5/062 , C07K5/083 , C07K5/08 , C07K7/06
CPC分类号: C07D417/14 , A61K31/55 , A61K38/177 , C07D403/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D495/04 , C07D513/04 , C07K5/06026 , C07K5/0806 , C07K5/0827 , C07K7/06 , C12N5/0693
摘要: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4′, R5, R5′, R6 and R6′ are as described herein.
摘要翻译: 本发明提供了可用作治疗恶性肿瘤的治疗剂的新的IAP抑制剂,其中化合物具有通式I:其中X,Y,A,R 1,R 2,R 3,R 4,R 4',R 5,R 5',R 6和 R6'如本文所述。
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公开(公告)号:US08232273B2
公开(公告)日:2012-07-31
申请号:US12641141
申请日:2009-12-17
申请人: Jonathan Bayldon Baell , Chinh Thien Bui , Peter Colman , Peter Czabotar , Danette A. Dudley , Wayne J. Fairbrother , John A. Flygare , Guillaume Laurent Lessene , Chudi Ndubaku , George Nikolakopoulos , Brad Edmund Sleebs , Brian John Smith , Keith Geoffrey Watson , Steven W. Elmore , Lisa A. Hasvold , Andrew M. Petros , Andrew J. Souers , Zhi-Fu Tao , Le Wang , Xilu Wang , Kurt Deshayes
发明人: Jonathan Bayldon Baell , Chinh Thien Bui , Peter Colman , Peter Czabotar , Danette A. Dudley , Wayne J. Fairbrother , John A. Flygare , Guillaume Laurent Lessene , Chudi Ndubaku , George Nikolakopoulos , Brad Edmund Sleebs , Brian John Smith , Keith Geoffrey Watson , Steven W. Elmore , Lisa A. Hasvold , Andrew M. Petros , Andrew J. Souers , Zhi-Fu Tao , Le Wang , Xilu Wang , Kurt Deshayes
IPC分类号: A61K31/5377 , C07D413/14
CPC分类号: C07D417/14 , C07D471/06 , C07D473/00 , C07D487/04 , C07D495/04 , C07D513/04 , C07D513/06
摘要: In one aspect, the present invention provides for a compound of Formula I in which the variable X1a, X1b, X1c, X1d, Q, A, R1, B, L, E, and the subscripts m and n have the meanings as described herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.
摘要翻译: 一方面,本发明提供了其中变量X1a,X1b,X1c,X1d,Q,A,R1,B,L,E和下标m和n具有如本文所述的含义的式I化合物 。 另一方面,本发明提供包含式I化合物的药物组合物以及使用式I化合物治疗以表达或过表达为特征的疾病和病症(例如,癌症,血小板增多症等)的方法 的Bcl-2抗凋亡蛋白,例如抗凋亡Bcl-xL蛋白。
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公开(公告)号:US20100210622A1
公开(公告)日:2010-08-19
申请号:US12641141
申请日:2009-12-17
申请人: Jonathan Bayldon Baell , Chinh Thien Bui , Peter Colman , Peter Czabotar , Danette A. Dudley , Wayne J. Fairbrother , John A, Flygare , Guillaume Laurent Lessene , Chudi Ndubaku , George Nikolakopoulos , Brad Edmund Sleebs , Brian John Smith , Keith Geoffrey Watson , Steven W. Elmore , Lisa A. Hasvold , Andrew M. Petros , Andrew J. Souers , Zhi-Fu Tao , Le Wang , Xilu Wang , Kurt Deshayes
发明人: Jonathan Bayldon Baell , Chinh Thien Bui , Peter Colman , Peter Czabotar , Danette A. Dudley , Wayne J. Fairbrother , John A, Flygare , Guillaume Laurent Lessene , Chudi Ndubaku , George Nikolakopoulos , Brad Edmund Sleebs , Brian John Smith , Keith Geoffrey Watson , Steven W. Elmore , Lisa A. Hasvold , Andrew M. Petros , Andrew J. Souers , Zhi-Fu Tao , Le Wang , Xilu Wang , Kurt Deshayes
IPC分类号: A61K31/4725 , C07D417/14 , A61P35/02 , A61P35/00 , A61P9/00 , A61P7/02 , C07D471/04 , A61K31/5377 , C07D487/04 , A61K31/519 , A61K31/496 , C07D471/06 , A61K31/4745
CPC分类号: C07D417/14 , C07D471/06 , C07D473/00 , C07D487/04 , C07D495/04 , C07D513/04 , C07D513/06
摘要: In one aspect, the present invention provides for a compound of Formula I in which the variable X1a, X1b, X1c, X1d, Q, A, R1, B, L, E, and the subscripts m and n have the meanings as described herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.
摘要翻译: 一方面,本发明提供了其中变量X1a,X1b,X1c,X1d,Q,A,R1,B,L,E和下标m和n具有如本文所述的含义的式I化合物 。 另一方面,本发明提供包含式I化合物的药物组合物以及使用式I化合物治疗以表达或过表达为特征的疾病和病症(例如,癌症,血小板增多症等)的方法 的Bcl-2抗凋亡蛋白,例如抗凋亡Bcl-xL蛋白。
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公开(公告)号:US08114893B2
公开(公告)日:2012-02-14
申请号:US12641063
申请日:2009-12-17
申请人: Jonathan Bayldon Baell , Chinh Thien Bui , Peter Colman , Danette A. Dudley , Wayne J. Fairbrother , John A. Flygare , Guillaume Laurent Lessene , Chudi Ndubaku , George Nikolakopoulos , Carl Steven Rye , Brad Edmund Sleebs , Brian John Smith , Keith Geoffrey Watson , Steven W. Elmore , Andrew M. Petros , Andrew J. Souers , Peter Czabotar
发明人: Jonathan Bayldon Baell , Chinh Thien Bui , Peter Colman , Danette A. Dudley , Wayne J. Fairbrother , John A. Flygare , Guillaume Laurent Lessene , Chudi Ndubaku , George Nikolakopoulos , Carl Steven Rye , Brad Edmund Sleebs , Brian John Smith , Keith Geoffrey Watson , Steven W. Elmore , Andrew M. Petros , Andrew J. Souers , Peter Czabotar
IPC分类号: C07D417/14 , A61K31/5377 , A61K31/538 , A61K31/496 , A61K31/498 , A61K31/4709
CPC分类号: C07D417/14 , C07D417/12 , C07D487/04
摘要: In one aspect, the present invention provides for a compound of Formula I in which in Formula I, the variables X1, X2a, X2b, X2c, R1, B, L, E, A and the subscript n are as defined herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.
摘要翻译: 一方面,本发明提供式I化合物,其中在式I中,变量X1,X2a,X2b,X2c,R1,B,L,E,A和下标n如本文所定义。 另一方面,本发明提供包含式I化合物的药物组合物以及使用式I化合物治疗以表达或过表达为特征的疾病和病症(例如,癌症,血小板增多症等)的方法 的Bcl-2抗凋亡蛋白,例如抗凋亡Bcl-xL蛋白。
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公开(公告)号:US20100190782A1
公开(公告)日:2010-07-29
申请号:US12641063
申请日:2009-12-17
申请人: Jonathan Bayldon Baell , Chinh Thien Bui , Peter Colman , Danette A. Dudley , Wayne J. Fairbrother , John A. Flygare , Guillaume Laurent Lessene , Chudi Ndubaku , George Nikolakopoulos , Carl Steven Rye , Brad Edmund Sleebs , Brian John Smith , Keith Geoffrey Watson , Steven W. Elmore , Andrew M. Petros , Andrew J. Souers
发明人: Jonathan Bayldon Baell , Chinh Thien Bui , Peter Colman , Danette A. Dudley , Wayne J. Fairbrother , John A. Flygare , Guillaume Laurent Lessene , Chudi Ndubaku , George Nikolakopoulos , Carl Steven Rye , Brad Edmund Sleebs , Brian John Smith , Keith Geoffrey Watson , Steven W. Elmore , Andrew M. Petros , Andrew J. Souers
IPC分类号: A61K31/536 , C07D417/14 , A61K31/4709 , C07D487/04 , A61K31/519 , A61K31/502 , A61K31/428 , A61K31/5377 , A61P35/02 , A61P35/00 , A61P7/02 , A61P9/00
CPC分类号: C07D417/14 , C07D417/12 , C07D487/04
摘要: In one aspect, the present invention provides for a compound of Formula I in which in Formula I, the variables X1, X2a, X2b, X2c, R1, B, L, E, A and the subscript n are as defined herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.
摘要翻译: 一方面,本发明提供式I化合物,其中在式I中,变量X1,X2a,X2b,X2c,R1,B,L,E,A和下标n如本文所定义。 另一方面,本发明提供包含式I化合物的药物组合物以及使用式I化合物治疗以表达或过表达为特征的疾病和病症(例如,癌症,血小板增多症等)的方法 的Bcl-2抗凋亡蛋白,例如抗凋亡Bcl-xL蛋白。
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公开(公告)号:US08518970B2
公开(公告)日:2013-08-27
申请号:US13347364
申请日:2012-01-10
申请人: Jonathan Bayldon Baell , Chinh Thien Bui , Peter Colman , Danette A. Dudley , Wayne J. Fairbrother , John A. Flygare , Guillaume Laurent Lessene , Chudi Ndubaku , George Nikolakopoulos , Carl Steven Rye , Brad Edmund Sleebs , Brian John Smith , Keith Geoffrey Watson , Steven W. Elmore , Andrew M. Petros , Andrew J. Souers , Peter Czabotar
发明人: Jonathan Bayldon Baell , Chinh Thien Bui , Peter Colman , Danette A. Dudley , Wayne J. Fairbrother , John A. Flygare , Guillaume Laurent Lessene , Chudi Ndubaku , George Nikolakopoulos , Carl Steven Rye , Brad Edmund Sleebs , Brian John Smith , Keith Geoffrey Watson , Steven W. Elmore , Andrew M. Petros , Andrew J. Souers , Peter Czabotar
IPC分类号: C07D417/14 , A61K31/5377 , A61K31/538 , A61K31/496 , A61K31/498 , A61K31/4709
CPC分类号: C07D417/14 , C07D417/12 , C07D487/04
摘要: In one aspect, the present invention provides for a compound of Formula I in which in Formula I, the variables X1, X2a, X2b, X2c, R1, B, L, E, A and the subscript n are as defined herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.
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