-
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。
-
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。
-
公开(公告)号:US20120184541A1
公开(公告)日:2012-07-19
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: A61K31/4709 , A61K31/519 , A61P9/00 , A61P35/00 , A61P35/02 , A61P7/02 , A61K31/538 , A61K31/498
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。
-
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.
-
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。
-
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。
-
公开(公告)号:US08168645B2
公开(公告)日:2012-05-01
申请号:US12513835
申请日:2007-11-15
申请人: Jonathan Bayldon Baell , Guillaume Laurent Lessene , Brad Edmund Sleebs , Wayne J. Fairbrother , John A. Flygare , Michael F. T. Koehler
发明人: Jonathan Bayldon Baell , Guillaume Laurent Lessene , Brad Edmund Sleebs , Wayne J. Fairbrother , John A. Flygare , Michael F. T. Koehler
IPC分类号: A61K31/517 , C07D239/72
CPC分类号: C07D239/94
摘要: The invention relates generally to small molecules that mimic the biological activity of certain peptides and proteins, to compositions containing them and to their use. In particular, the invention relates to compounds of the general formula (I) that mimic the biological activity of BH3-only proteins and are capable of binding to and neutralizing pro-survival Bcl-2 proteins: wherein A1, A2, B1, B2, B3, X, Z, R1, R2, R3 and t are as described herein. The invention also relates to processes of preparing the benzenesulfonamide compounds that mimic portions of peptides and proteins, and to the use of such compounds in the regulation of cell death and the treatment and/or prophylaxis of diseases or conditions associated with the deregulation of cell death.
摘要翻译: 本发明一般涉及模拟某些肽和蛋白质的生物学活性的小分子,含有它们的组合物及其用途。 特别地,本发明涉及模拟仅含BH3蛋白的生物学活性的通式(I)的化合物,并能够结合并中和原生存Bcl-2蛋白:其中A1,A2,B1,B2, B3,X,Z,R1,R2,R3和t如本文所述。 本发明还涉及制备模仿肽和蛋白质的一部分的苯磺酰胺化合物的方法,以及这些化合物在调节细胞死亡中的用途以及治疗和/或预防与细胞死亡调节相关的疾病或病症 。
-
公开(公告)号:US20100056517A1
公开(公告)日:2010-03-04
申请号:US12513835
申请日:2007-11-15
申请人: Jonathan Bayldon Baell , Guillaume Laurent Lessene , Brad Edmund Sleebs , Wayne J. Fairbrother , John A. Flygare , Michael F.T. Koeler
发明人: Jonathan Bayldon Baell , Guillaume Laurent Lessene , Brad Edmund Sleebs , Wayne J. Fairbrother , John A. Flygare , Michael F.T. Koeler
IPC分类号: A61K31/5377 , A61K31/496 , C07D413/14 , C07D239/86 , A61P35/00
CPC分类号: C07D239/94
摘要: The invention relates generally to small molecules that mimic the biological activity of certain peptides and proteins, to compositions containing them and to their use. In particular, the invention relates to compounds of the general formula (I) that mimic the biological activity of BH3-only proteins and are capable of binding to and neutralizing pro-survival Bcl-2 proteins: wherein A1, A2, B1, B2, B3, X, Z, R1, R2, R3 and t are as described herein. The invention also relates to processes of preparing the benzenesulfonamide compounds that mimic portions of peptides and proteins, and to the use of such compounds in the regulation of cell death and the treatment and/or prophylaxis of diseases or conditions associated with the deregulation of cell death.
摘要翻译: 本发明一般涉及模拟某些肽和蛋白质的生物学活性的小分子,含有它们的组合物及其用途。 特别地,本发明涉及模拟仅含BH3蛋白的生物学活性的通式(I)的化合物,并能够结合并中和原生存Bcl-2蛋白:其中A1,A2,B1,B2, B3,X,Z,R1,R2,R3和t如本文所述。 本发明还涉及制备模仿肽和蛋白质的一部分的苯磺酰胺化合物的方法,以及这些化合物在调节细胞死亡中的用途以及治疗和/或预防与细胞死亡调节相关的疾病或病症 。
-
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。
-
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。
-
-
-
-
-
-
-
-
-