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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:US08907092B2
公开(公告)日:2014-12-09
申请号:US12598027
申请日:2008-04-29
申请人: John A. Flygare , Frederick Cohen , Kurt Deshayes , Michael F. T. Koehler , Lewis J. Gazzard , Lan Wang , Chudi Ndubaku
发明人: John A. Flygare , Frederick Cohen , Kurt Deshayes , Michael F. T. Koehler , Lewis J. Gazzard , Lan Wang , Chudi Ndubaku
IPC分类号: C07D277/46 , C07D513/04 , C07D417/14 , A61K31/4365 , A61K31/4436 , A61K31/427 , C07D207/16 , C07D519/00
CPC分类号: C07D417/14 , C07D207/16 , C07D519/00
摘要: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds having the general formula U1-M-U2 wherein M is a linking group covalently joining R2, R3, R4 or R5 of U1 to an R2, R3, R4 or R5 group of U2; U1 and U2 have the general formula (I) and G, X1, X2, R2, R3, R3′, R4, R4′ and R5, 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,其中具有通式U1-M-U2的化合物,其中M是共价连接U1的R2,R3,R4或R5的连接基团与R2,R3 ,R4或R5组的U2; U1和U2具有通式(I),G,X 1,X 2,R 2,R 3,R 3',R 4,R 4'和R 5如本文所述。
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公开(公告)号:US20110039324A1
公开(公告)日:2011-02-17
申请号:US12835605
申请日:2010-07-13
申请人: Kurt Deshayes , Wayne Fairbrother , John Flygare , Matthew C. Franklin , Saloumeh Fischer , Domagoj Vucic
发明人: Kurt Deshayes , Wayne Fairbrother , John Flygare , Matthew C. Franklin , Saloumeh Fischer , Domagoj Vucic
CPC分类号: A61K38/08 , A61K38/00 , C07K7/08 , C07K14/001 , C07K14/4747 , C07K2319/00
摘要: The present invention is directed to compositions of matter useful for the enhancement of apoptosis in mammals and to methods of using those compositions of matter for the same.
摘要翻译: 本发明涉及用于增强哺乳动物细胞凋亡的物质组合物,以及使用这些物质组合物的方法。
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公开(公告)号:US20070299052A1
公开(公告)日:2007-12-27
申请号:US11739030
申请日:2007-04-23
申请人: Frederick Cohen , Kurt Deshayes , Wayne Fairbrother , Bainian Feng , John Flygare , Lewis Gazzard , Vickie Tsui
发明人: Frederick Cohen , Kurt Deshayes , Wayne Fairbrother , Bainian Feng , John Flygare , Lewis Gazzard , Vickie Tsui
IPC分类号: A61K31/55 , A61K31/351 , A61K31/40 , A61K31/41 , A61P35/00 , C07D207/30 , C07D223/14 , C07D277/02 , C07D309/02 , C12N9/00 , C12N5/00 , C07D285/06 , C07D231/02 , C07D221/00 , A61P43/00 , A61K31/415 , A61K31/426 , A61K31/445
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.
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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:US20110077265A1
公开(公告)日:2011-03-31
申请号:US12598027
申请日:2008-04-29
申请人: John A. Flygare , Frederick Cohen , Kurt Deshayes , Michael F. T. Koehler , Lewis J. Gazzard , Lan Wang , Chudi Ndubaku
发明人: John A. Flygare , Frederick Cohen , Kurt Deshayes , Michael F. T. Koehler , Lewis J. Gazzard , Lan Wang , Chudi Ndubaku
IPC分类号: A61K31/437 , C07D417/14 , C07D513/04 , C07D403/12 , C12N5/071 , C07K2/00 , A61K31/4545 , A61K31/433 , A61K31/4025 , A61K31/427 , A61P35/00
CPC分类号: C07D417/14 , C07D207/16 , C07D519/00
摘要: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds having the general formula U1-M-U2 wherein M is a linking group covalently joining R2, R3, R4 or R5 of U1 to an R2, R3, R4 or R5 group of U2; U1 and U2 have the general formula (I) and G, X1, X2, R2, R3, R3′, R4, R4′ and R5, 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,其中具有通式U1-M-U2的化合物,其中M是共价连接U1的R2,R3,R4或R5的连接基团与R2,R3 ,R4或R5组的U2; U1和U2具有通式(I),G,X 1,X 2,R 2,R 3,R 3',R 4,R 4'和R 5如本文所述。
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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:US20120058953A1
公开(公告)日:2012-03-08
申请号:US13274142
申请日:2011-10-14
申请人: Kurt Deshayes , Wayne Fairbrother , John Flygare , Matthew C. Franklin , Saloumeh Fischer , Domagoj Vucic
发明人: Kurt Deshayes , Wayne Fairbrother , John Flygare , Matthew C. Franklin , Saloumeh Fischer , Domagoj Vucic
IPC分类号: A61K38/08 , C07K5/103 , C07K7/06 , A61P35/02 , C12N9/96 , C12N5/09 , A61K38/07 , A61P35/00 , C07K4/00 , C07K19/00
CPC分类号: A61K38/08 , A61K38/00 , C07K7/08 , C07K14/001 , C07K14/4747 , C07K2319/00
摘要: The present invention is directed to compositions of matter useful for the enhancement of apoptosis in mammals and to methods of using those compositions of matter for the same.
摘要翻译: 本发明涉及用于增强哺乳动物细胞凋亡的物质组合物,以及使用这些物质组合物的方法。
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公开(公告)号:US20060233804A1
公开(公告)日:2006-10-19
申请号:US11473753
申请日:2006-06-23
申请人: Kurt Deshayes , Henry Lowman , Michelle Schaffer , Sachdev Sidhu
发明人: Kurt Deshayes , Henry Lowman , Michelle Schaffer , Sachdev Sidhu
IPC分类号: A61K39/395 , A61K38/22
CPC分类号: C07K14/4743 , A61K38/00 , C07K2299/00
摘要: Peptides are provided that antagonize the interaction of IGF-1 with its binding proteins, insulin receptor, and IGF receptor. These IGF antagonist peptides are useful in treating disorders involving IGF-1 as a causative agent, such as, for example, various cancers.
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公开(公告)号:US20060014700A1
公开(公告)日:2006-01-19
申请号:US11174784
申请日:2005-07-05
申请人: Frederick Cohen , Kurt Deshayes , Wayne Fairbrother , Bainian Feng , John Flygare , Lewis Gazzard , Vickie Tsui
发明人: Frederick Cohen , Kurt Deshayes , Wayne Fairbrother , Bainian Feng , John Flygare , Lewis Gazzard , Vickie Tsui
IPC分类号: A61K38/05 , C07K5/04 , A61K31/421 , A61K31/426
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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