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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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公开(公告)号:US20080194691A1
公开(公告)日:2008-08-14
申请号:US11914772
申请日:2006-05-17
IPC分类号: A61K31/18 , C07C311/19 , A61P35/00
CPC分类号: C07D273/02 , C07D273/00 , C07D413/12
摘要: Compounds of formula (I), in which B1 and X1 are together alkylene which is unsubstituted or substituted with ═O and having one CH2 moiety unreplaced or replaced with CH═CH, O, NH or N(alkyl), which inhibit the activity of antiapoptotic Bcl-2 family protein members, compositions containing the compounds and methods of treating diseases during which are expressed one or more than one of an anti-apoptotic family protein member are disclosed.
摘要翻译: 其中B 1和X 2的式(I)化合物在一起是未被取代或被-O取代并具有一个CH2部分的亚烷基未置换或被CH- CH,O,NH或N(烷基),其抑制抗凋亡Bcl-2家族蛋白质成员的活性,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成员 被披露。
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公开(公告)号:US07906505B2
公开(公告)日:2011-03-15
申请号:US12772951
申请日:2010-05-03
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: C07D413/02 , C07D403/02 , A61K31/553 , A61K31/55 , A61K31/5377
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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公开(公告)号:US07709467B2
公开(公告)日:2010-05-04
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: C07D241/04 , A61K31/496
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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公开(公告)号:US07777076B2
公开(公告)日:2010-08-17
申请号:US11914772
申请日:2006-05-17
IPC分类号: C07C321/00
CPC分类号: C07D273/02 , C07D273/00 , C07D413/12
摘要: Macrocyclic compounds of formula (I), in which B1 and X1 taken together are alkylene which is unsubstituted or substituted with ═O and having one CH2 moiety unreplaced or replaced with CH═CH, O, NH or N(alkyl), which inhibit the activity of antiapoptotic Bcl-2 family protein members, compositions containing the compounds and methods of treating diseases during which are expressed one or more than one of an anti-apoptotic family protein member are disclosed.
摘要翻译: 式(I)的大环化合物,其中B1和X1一起是未被取代或被= O取代且具有一个CH2部分未被置换或被CH = CH,O,NH或N(烷基)取代的亚烷基,其抑制 公开了抗凋亡性Bcl-2家族蛋白质成员的活性,含有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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公开(公告)号:US07390799B2
公开(公告)日:2008-06-24
申请号:US11432937
申请日:2006-05-12
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: C07D413/02 , C07D403/02 , A61K31/553 , A61K31/55 , A61K31/5377 , A61K31/496
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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公开(公告)号:US20100249133A1
公开(公告)日:2010-09-30
申请号:US12772951
申请日:2010-05-03
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: A61K31/496 , A61K31/4965 , A61K31/5377
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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公开(公告)号:US20110124628A1
公开(公告)日:2011-05-26
申请号:US12951344
申请日:2010-11-22
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: A61K31/496 , C07D471/04 , C07D401/14 , C07D403/14 , C07D405/14 , A61K31/5377 , A61K31/517 , A61K31/541 , A61P35/00 , A61P35/02
CPC分类号: C07D471/04 , C07D491/052 , C07D519/00
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: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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10.
公开(公告)号:US20100160322A1
公开(公告)日:2010-06-24
申请号:US12631367
申请日:2009-12-04
申请人: Milan Bruncko , Yujia Dai , Hong Ding , George A. Doherty , Steven W. Elmore , Lisa Hasvold , Laura Hexamer , Aaron Kunzer , Robert A. Mantei , William J. McClellan , Chang H. Park , Cheol-Min Park , Andrew M. Petros , Xiaohong Song , Andrew J. Souers , Gerard M. Sullivan , Zhi-Fu Tao , Gary T. Wang , Le Wang , Xilu Wang , Michael D. Wendt
发明人: Milan Bruncko , Yujia Dai , Hong Ding , George A. Doherty , Steven W. Elmore , Lisa Hasvold , Laura Hexamer , Aaron Kunzer , Robert A. Mantei , William J. McClellan , Chang H. Park , Cheol-Min Park , Andrew M. Petros , Xiaohong Song , Andrew J. Souers , Gerard M. Sullivan , Zhi-Fu Tao , Gary T. Wang , Le Wang , Xilu Wang , Michael D. Wendt
IPC分类号: A61K31/5377 , C07D405/02 , A61K31/496 , C07D403/02 , C07D401/02 , C07D413/02 , A61P35/00
CPC分类号: C07D209/08 , A61K31/635 , C07D211/58 , C07D213/74 , C07D213/84 , C07D231/56 , C07D235/06 , C07D277/24 , C07D295/30 , C07D309/04 , C07D309/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/12 , C07D471/04 , Y02A50/401 , Y02A50/409 , Y02A50/411
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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