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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:US20090054402A1
公开(公告)日:2009-02-26
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 R. 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 R. Kunzer
IPC分类号: A61K31/55 , C07D209/04 , A61K31/404 , C07D413/02 , A61K31/5377 , C07D401/02 , A61K31/4439 , C07D215/00 , A61K31/4709 , C07D403/02 , A61K31/496 , C07D413/14 , C07D265/36 , A61K31/538 , A61K31/517 , C07D417/02 , A61K31/541 , C07D223/16 , A61P43/00
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:US5972898A
公开(公告)日:1999-10-26
申请号:US49458
申请日:1998-03-27
申请人: Daryl R. Sauer , Fortuna Haviv , John Randolph , Nicholas A. Mort , Christopher R. Dalton , Milan Bruncko , Michele A. Kaminski , Bradley W. Crawford , Lisa Marie Frey , Jonathan Greer
发明人: Daryl R. Sauer , Fortuna Haviv , John Randolph , Nicholas A. Mort , Christopher R. Dalton , Milan Bruncko , Michele A. Kaminski , Bradley W. Crawford , Lisa Marie Frey , Jonathan Greer
IPC分类号: A61K31/7042 , A61K31/7048 , A61P5/00 , A61P15/00 , A61P43/00 , C07H17/08 , A61K31/70 , C07H1/00
CPC分类号: C07H17/08
摘要: Disclosed are 3',3'-N-bisdesmethyl-3',3'-N-bis-substituted-6-O-methyl-11-deoxy-11,12-cyclic carbamate erythromycin A derivatives which are antagonists of lutenizing hormone-releasing hormone (LHRH). Also disclosed are pharmaceutical compositions comprising the compounds, to methods of using the compounds and to the process of making the same.
摘要翻译: 公开了3',3'-N-双甲基-3',3'-N-双取代-6-O-甲基-11-脱氧-11,12-环氨基甲酸酯红霉素A衍生物,其是促黄体激素 - 释放激素(LHRH)。 还公开了包含该化合物的药物组合物,使用该化合物的方法及其制备方法。
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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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公开(公告)号:US5955440A
公开(公告)日:1999-09-21
申请号:US49963
申请日:1998-03-27
申请人: Daryl R. Sauer , Fortuna Haviv , John Randolph , Nicholas A. Mort , Christopher R. Dalton , Milan Bruncko , Michele A. Kaminski , Bradley W. Crawford , Lisa Marie Frey , Jonathan Greer
发明人: Daryl R. Sauer , Fortuna Haviv , John Randolph , Nicholas A. Mort , Christopher R. Dalton , Milan Bruncko , Michele A. Kaminski , Bradley W. Crawford , Lisa Marie Frey , Jonathan Greer
IPC分类号: A61K31/7042 , A61K31/7048 , A61K31/7056 , A61P5/24 , A61P13/08 , A61P15/00 , A61P35/00 , A61P43/00 , C07H17/08 , A61K31/70 , C07H1/00
CPC分类号: C07H17/08
摘要: Disclosed are 3'-N-desmethyl-3'-N-substituted-6-O-methyl-11-deoxy-11,12-cyclic carbamate erythromycin A derivatives which are antagonists of lutenizing hormone-releasing hormone (LHRH). Also disclosed are pharmaceutical compositions comprising the compounds, to methods of using the compounds and to the process of making the same.
摘要翻译: 公开了作为促黄体激素释放激素(LHRH)的拮抗剂的3'-N-去甲基-3'-N-取代-6-O-甲基-11-脱氧-11,12-环状氨基甲酸酯红霉素A衍生物。 还公开了包含该化合物的药物组合物,使用该化合物的方法及其制备方法。
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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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48.Apoptosis inducing agents for the treatment of cancer and immune and autoimmune diseases 有权
标题翻译: 凋亡诱导剂用于治疗癌症和免疫和自身免疫性疾病公开(公告)号:US08546399B2
公开(公告)日:2013-10-01
申请号:US12787682
申请日:2010-05-26
申请人: Milan Bruncko , Hong Ding , George A. Doherty , Steven W. Elmore , Lisa A. Hasvold , Laura Hexamer , Aaron R. Kunzer , Xiaohong Song , Andrew J. Souers , Gerard M. Sullivan , Zhi-Fu Tao , Gary T. Wang , Le Wang , Xilu Wang , Michael D. Wendt , Robert Mantei , Todd M. Hansen
发明人: Milan Bruncko , Hong Ding , George A. Doherty , Steven W. Elmore , Lisa A. Hasvold , Laura Hexamer , Aaron R. Kunzer , Xiaohong Song , Andrew J. Souers , Gerard M. Sullivan , Zhi-Fu Tao , Gary T. Wang , Le Wang , Xilu Wang , Michael D. Wendt , Robert Mantei , Todd M. Hansen
IPC分类号: A61K31/407 , C07D401/12
CPC分类号: C07D401/12 , A61K31/496 , C07D209/82 , C07D401/14 , C07D403/12 , C07D471/04 , C07D519/00 , Y02A50/463
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.
摘要翻译: 公开了抑制抗凋亡Bcl-2蛋白活性的化合物,含有化合物的组合物和治疗疾病的方法,其中表达抗凋亡Bcl-2蛋白。
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49.APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES 审中-公开
标题翻译: 用于治疗癌症和免疫和自发性疾病的病毒诱导剂公开(公告)号:US20120190688A1
公开(公告)日:2012-07-26
申请号:US13430610
申请日:2012-03-26
申请人: Milan Bruncko , Hong Ding , George A. Doherly , Steven W. Elmore , Lisa Hasvold , Laura Hexamer , Aaron R. Kunzer , Xiaohong Song , Andrew J. Souers , Gerard M. Sullivan , Zhi-Fu Tao , Gary T. Wang , Le Wang , Xilu Wang , Michael D. Wendt , Robert A. Mantei , Todd M. Hansen
发明人: Milan Bruncko , Hong Ding , George A. Doherly , Steven W. Elmore , Lisa Hasvold , Laura Hexamer , Aaron R. Kunzer , Xiaohong Song , Andrew J. Souers , Gerard M. Sullivan , Zhi-Fu Tao , Gary T. Wang , Le Wang , Xilu Wang , Michael D. Wendt , Robert A. Mantei , Todd M. Hansen
IPC分类号: A61K31/496 , A61P37/00 , A61P35/02 , C07D471/04 , A61P35/00
CPC分类号: C07D401/12 , A61K31/496 , C07D209/82 , C07D401/14 , C07D403/12 , C07D471/04 , C07D519/00 , Y02A50/463
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.
摘要翻译: 公开了抑制抗凋亡Bcl-2蛋白活性的化合物,含有化合物的组合物和治疗疾病的方法,其中表达抗凋亡Bcl-2蛋白。
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50.APOPTOSIS INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES 有权
标题翻译: 用于治疗癌症和免疫和自发性疾病的病毒诱导剂公开(公告)号:US20100305122A1
公开(公告)日:2010-12-02
申请号:US12787682
申请日:2010-05-26
申请人: Milan Bruncko , Hong Ding , George A. Doherty , Steven W. Elmore , Lisa Hasvold , Laura Hexamer , Aaron R. Kunzer , Xiaohong Song , Andrew J. Souers , Gerard M. Sullivan , Zhi-Fu Tao , Gary T. Wang , Le Wang , Xilu Wang , Michael D. Wendt , Robert A. Mantei , Todd M. Hansen
发明人: Milan Bruncko , Hong Ding , George A. Doherty , Steven W. Elmore , Lisa Hasvold , Laura Hexamer , Aaron R. Kunzer , Xiaohong Song , Andrew J. Souers , Gerard M. Sullivan , Zhi-Fu Tao , Gary T. Wang , Le Wang , Xilu Wang , Michael D. Wendt , Robert A. Mantei , Todd M. Hansen
IPC分类号: A61K31/5377 , A61P35/00 , A61P35/04 , C07D471/04 , A61K31/496
CPC分类号: C07D401/12 , A61K31/496 , C07D209/82 , C07D401/14 , C07D403/12 , C07D471/04 , C07D519/00 , Y02A50/463
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.
摘要翻译: 公开了抑制抗凋亡Bcl-2蛋白活性的化合物,含有化合物的组合物和治疗疾病的方法,其中表达抗凋亡Bcl-2蛋白。
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