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公开(公告)号：US08445679B2
公开(公告)日：2013-05-21
申请号：US12104294
申请日：2008-04-16
申请人： Xilu Wang , Xiaohong Song , Steven W. Elmore , Milan Bruncko , David J. Madar , Andrew J. Souers , Lisa A. Hasvold , Le Wang , Zhi-Fu Tao , Aaron K. Kunzer
发明人： Xilu Wang , Xiaohong Song , Steven W. Elmore , Milan Bruncko , David J. Madar , Andrew J. Souers , Lisa A. Hasvold , Le Wang , Zhi-Fu Tao , Aaron K. Kunzer
IPC分类号： C07D403/04 , A61K31/497
CPC分类号： C07D209/42 , A61K31/5377 , C07D209/34 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/06 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/04 , C07D491/113
摘要： Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein are disclosed.
摘要翻译： 公开了抑制抗凋亡Mcl-1蛋白活性的化合物，含有该化合物的组合物，以及治疗涉及过表达或未调节的Mcl-1蛋白的疾病的方法。
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公开(公告)号：US08084607B2
公开(公告)日：2011-12-27
申请号：US12390945
申请日：2009-02-23
申请人： Milan Bruncko , Hong Ding , Steven Elmore , Aaron R. Kunzer , Christopher L. Lynch , William J. McClellan , Cheol-min Park , Andrew M. Petros , Xiaohong Song , Noah P. Tu , Xilu Wang , Michael D. Wendt
发明人： Milan Bruncko , Hong Ding , Steven Elmore , Aaron R. Kunzer , Christopher L. Lynch , William J. McClellan , Cheol-min Park , Andrew M. Petros , Xiaohong Song , Noah P. Tu , Xilu Wang , Michael D. Wendt
IPC分类号： C07D241/04 , C07D295/00
CPC分类号： C07D277/74 , C04B35/632 , C07C323/25 , C07C2601/16 , C07D205/04 , C07D207/16 , C07D211/46 , C07D211/60 , C07D211/74 , C07D213/70 , C07D213/75 , C07D233/06 , C07D233/84 , C07D239/06 , C07D263/58 , C07D277/36 , C07D295/13 , C07D295/192 , C07D307/64 , C07D335/02 , C07D401/12 , C07D403/04 , C07D409/12 , C07D487/04 , C07D487/08
摘要： Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.
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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：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：US07754886B2
公开(公告)日：2010-07-13
申请号：US12364987
申请日：2009-02-03
申请人： David J. Augeri , Steven A. Baumeister , Milan Bruncko , Daniel A. Dickman , Hong Ding , Jurgen Dinges , Stephen W. Fesik , Philip J Hajduk , Aaron R Kunzer , William J. Mcclellan , David D. Nettesheim , Thorsten K. Oost , Andrew M. Petros , Saul Howard Rosenberg , Wang Shen , Sheela A. Thomas , Xilu Wang , Michael D. Wendt
发明人： David J. Augeri , Steven A. Baumeister , Milan Bruncko , Daniel A. Dickman , Hong Ding , Jurgen Dinges , Stephen W. Fesik , Philip J Hajduk , Aaron R Kunzer , William J. Mcclellan , David D. Nettesheim , Thorsten K. Oost , Andrew M. Petros , Saul Howard Rosenberg , Wang Shen , Sheela A. Thomas , Xilu Wang , Michael D. Wendt
IPC分类号： C07C211/00 , A61K31/445
CPC分类号： C07D207/27 , A61K31/18 , A61K31/4015 , A61K31/44 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/541 , C07C311/51 , C07C323/30 , C07C323/37 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/42 , C07C2603/74 , C07D203/26 , C07D207/06 , C07D209/08 , C07D209/52 , C07D209/54 , C07D211/22 , C07D211/74 , C07D213/54 , C07D213/61 , C07D213/64 , C07D213/70 , C07D213/78 , C07D215/12 , C07D221/20 , C07D231/12 , C07D235/08 , C07D235/26 , C07D239/26 , C07D249/04 , C07D263/32 , C07D263/56 , C07D263/58 , C07D277/56 , C07D277/64 , C07D295/205 , C07D295/26 , C07D317/60 , C07D333/28 , C07D333/56 , C07D333/70 , C07D417/12 , C07D451/02
摘要： N-Benzoyl arylsulfonamides having the formula are BCL-Xl inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-Xl inhibiting compositions and methods of promoting apoptosis in a mammal.
摘要翻译： 具有下式的N-苯甲酰基芳基磺酰胺是BCL-X1抑制剂，可用于促进凋亡。 还公开了BCL-X1抑制组合物和促进哺乳动物细胞凋亡的方法。
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26.发明授权公开(公告)号：US08557983B2
公开(公告)日：2013-10-15
申请号：US12793413
申请日：2010-06-03
申请人： George A. Doherty , Laura A. Hexamer , Robert A. Mantei , Gerard M. Sullivan , Zhi-Fu Tao , Gary T. Wang , Le Wang , Xilu Wang , Todd M. Hansen
发明人： George A. Doherty , Laura A. Hexamer , Robert A. Mantei , Gerard M. Sullivan , Zhi-Fu Tao , Gary T. Wang , Le Wang , Xilu Wang , Todd M. Hansen
IPC分类号： C07D403/14 , C07D413/14
CPC分类号： C07D213/76 , A61K31/495 , A61K31/496 , A61K31/5377 , A61K45/06 , C07D209/08 , C07D211/06 , C07D211/58 , C07D213/74 , C07D213/84 , C07D231/56 , C07D235/06 , C07D277/24 , C07D295/14 , C07D295/30 , C07D309/04 , C07D309/32 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/12 , C07D471/04
摘要： Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
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公开(公告)号：US07504512B2
公开(公告)日：2009-03-17
申请号：US10820097
申请日：2004-04-07
申请人： David J. Augeri , Steven A. Baumeister , Milan Bruncko , Daniel A. Dickman , Hong Ding , Jurgen Dinges , Stephen W. Fesik , Philip J. Hajduk , Aaron R. Kunzer , William McClellan , David G. Nettesheim , Thorsten Oost , Andrew M. Petros , Saul H. Rosenberg , Wang Shen , Sheela A. Thomas , Xilu Wang , Michael D. Wendt
发明人： David J. Augeri , Steven A. Baumeister , Milan Bruncko , Daniel A. Dickman , Hong Ding , Jurgen Dinges , Stephen W. Fesik , Philip J. Hajduk , Aaron R. Kunzer , William McClellan , David G. Nettesheim , Thorsten Oost , Andrew M. Petros , Saul H. Rosenberg , Wang Shen , Sheela A. Thomas , Xilu Wang , Michael D. Wendt
IPC分类号： C07C211/00 , A61K31/445
CPC分类号： C07D207/27 , A61K31/18 , A61K31/4015 , A61K31/44 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/541 , C07C311/51 , C07C323/30 , C07C323/37 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/42 , C07C2603/74 , C07D203/26 , C07D207/06 , C07D209/08 , C07D209/52 , C07D209/54 , C07D211/22 , C07D211/74 , C07D213/54 , C07D213/61 , C07D213/64 , C07D213/70 , C07D213/78 , C07D215/12 , C07D221/20 , C07D231/12 , C07D235/08 , C07D235/26 , C07D239/26 , C07D249/04 , C07D263/32 , C07D263/56 , C07D263/58 , C07D277/56 , C07D277/64 , C07D295/205 , C07D295/26 , C07D317/60 , C07D333/28 , C07D333/56 , C07D333/70 , C07D417/12 , C07D451/02
摘要： N-Benzoyl arylsulfonamides having the formula are BCL-X1 inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-X1 inhibiting compositions and methods of promoting apoptosis in a mammal.
摘要翻译： 具有下式的N-苯甲酰基芳基磺酰胺是BCL-X1抑制剂，可用于促进凋亡。 还公开了BCL-X1抑制组合物和促进哺乳动物细胞凋亡的方法。
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公开(公告)号：US20090137585A1
公开(公告)日：2009-05-28
申请号：US12364987
申请日：2009-02-03
申请人： David J. Augeri , Steven A. Baumeister , Milan Bruncko , Daniel A. Dickman , Hong Ding , Jurgen Dinges , Stephen W. Fesik , Philip J. Hajduk , Aaron R. Kunzer , William Mcclellan , David G. Nettesheim , Thorsten Oost , Andrew M. Petros , Saul H. Rosenberg , Wang Shen , Sheela A. Thomas , Xilu Wang , Michael D. Wendt
发明人： David J. Augeri , Steven A. Baumeister , Milan Bruncko , Daniel A. Dickman , Hong Ding , Jurgen Dinges , Stephen W. Fesik , Philip J. Hajduk , Aaron R. Kunzer , William Mcclellan , David G. Nettesheim , Thorsten Oost , Andrew M. Petros , Saul H. Rosenberg , Wang Shen , Sheela A. Thomas , Xilu Wang , Michael D. Wendt
IPC分类号： A61K31/445 , C07D211/60 , C07D241/04 , A61K31/5375 , A61P35/00 , A61K31/495 , C07D413/02
CPC分类号： C07D207/27 , A61K31/18 , A61K31/4015 , A61K31/44 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/541 , C07C311/51 , C07C323/30 , C07C323/37 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/42 , C07C2603/74 , C07D203/26 , C07D207/06 , C07D209/08 , C07D209/52 , C07D209/54 , C07D211/22 , C07D211/74 , C07D213/54 , C07D213/61 , C07D213/64 , C07D213/70 , C07D213/78 , C07D215/12 , C07D221/20 , C07D231/12 , C07D235/08 , C07D235/26 , C07D239/26 , C07D249/04 , C07D263/32 , C07D263/56 , C07D263/58 , C07D277/56 , C07D277/64 , C07D295/205 , C07D295/26 , C07D317/60 , C07D333/28 , C07D333/56 , C07D333/70 , C07D417/12 , C07D451/02
摘要： N-Benzoyl arylsulfonamides having the formula are BCL-Xl inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-Xl inhibiting compositions and methods of promoting apoptosis in a mammal.
摘要翻译： 具有下式的N-苯甲酰基芳基磺酰胺是BCL-X1抑制剂，可用于促进凋亡。 还公开了BCL-X1抑制组合物和促进哺乳动物细胞凋亡的方法。
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公开(公告)号：US06720338B2
公开(公告)日：2004-04-13
申请号：US09957276
申请日：2001-09-20
申请人： David J. Augeri , Steven A. Baumeister , Milan Bruncko , Daniel A. Dickman , Hong Ding , Jurgen Dinges , Stephen W. Fesik , Philip J. Hajduk , Aaron R. Kunzer , William McClellan , David G. Nettesheim , Thorsten Oost , Andrew M. Petros , Saul H. Rosenberg , Wang Shen , Sheela A. Thomas , Xilu Wang , Michael D. Wendt
发明人： David J. Augeri , Steven A. Baumeister , Milan Bruncko , Daniel A. Dickman , Hong Ding , Jurgen Dinges , Stephen W. Fesik , Philip J. Hajduk , Aaron R. Kunzer , William McClellan , David G. Nettesheim , Thorsten Oost , Andrew M. Petros , Saul H. Rosenberg , Wang Shen , Sheela A. Thomas , Xilu Wang , Michael D. Wendt
IPC分类号： A61K31445
CPC分类号： C07D207/27 , A61K31/18 , A61K31/4015 , A61K31/44 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/541 , C07C311/51 , C07C323/30 , C07C323/37 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/42 , C07C2603/74 , C07D203/26 , C07D207/06 , C07D209/08 , C07D209/52 , C07D209/54 , C07D211/22 , C07D211/74 , C07D213/54 , C07D213/61 , C07D213/64 , C07D213/70 , C07D213/78 , C07D215/12 , C07D221/20 , C07D231/12 , C07D235/08 , C07D235/26 , C07D239/26 , C07D249/04 , C07D263/32 , C07D263/56 , C07D263/58 , C07D277/56 , C07D277/64 , C07D295/205 , C07D295/26 , C07D317/60 , C07D333/28 , C07D333/56 , C07D333/70 , C07D417/12 , C07D451/02
摘要： N-Benzoyl arylsulfonamides having the formula: are BCL-X1 inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-X1 inhibiting compositions and methods of promoting apoptosis in a mammal.
摘要翻译： 具有下式的N-苯甲酰基芳基磺酰胺是BCL-X1抑制剂，可用于促进细胞凋亡。 还公开了BCL-X1抑制组合物和促进哺乳动物细胞凋亡的方法。
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公开(公告)号：US20080287419A1
公开(公告)日：2008-11-20
申请号：US12120914
申请日：2008-05-15
申请人： Milan Bruncko , Hong Ding , Steven W. Elmore , Aaron R. Kunzer , Christopher L. Lynch , William J. McClellan , Cheol Min Park , Xiahong Song , Xilu Wang
发明人： Milan Bruncko , Hong Ding , Steven W. Elmore , Aaron R. Kunzer , Christopher L. Lynch , William J. McClellan , Cheol Min Park , Xiahong Song , Xilu Wang
IPC分类号： A61K31/553 , C07D413/02 , A61K31/5377 , C07D223/02 , A61K31/496 , A61P35/00 , C07D295/00 , A61K31/55 , C07D267/02
CPC分类号： C07D295/155 , C07D487/08 , C07D491/08
摘要： Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than one of an anti-apoptotic family protein member are disclosed.
摘要翻译： 公开了抑制抗凋亡家族蛋白成员的活性的化合物，含有该化合物的组合物和治疗疾病的方法，其中表达一种或多种抗凋亡家族蛋白质成员。
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