公开(公告)号：EP2376085A1

公开(公告)日：2011-10-19

申请号：EP09837907.6

申请日：2009-12-17

申请人： Genentech, Inc. ,  The Walter and Eliza Hall Institute of Medical Research ,  Abbott Laboratories

发明人： BAELL, Jonathan, Bayldon ,  BUI, Chinh, Thien ,  COLMAN, Peter ,  DUDLEY, Danette, A. ,  FAIRBROTHER, Wayne, J. ,  FLYGARE, John, A. ,  LESSENE, Guillaume, Laurent ,  NDUBAKU, Chudi ,  NIKOLAKOPOULOS, George ,  RYE, Carl, Steven ,  SLEEBS, Brad, Edmund ,  SMITH, Brian, John ,  WATSON, Keith, Geoffrey ,  ELMORE, Steven, W. ,  PETROS, Andrew, M. ,  SOUERS, Andrew, J. ,  CZABOTAR, Peter

IPC分类号： A61K31/535

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, the variables X
1 , X
2a , X
2b , X
2c , R
1 , 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-x
L proteins.

公开(公告)号：EP2373163A1

公开(公告)日：2011-10-12

申请号：EP09837920.9

申请日：2009-12-17

申请人： Genentech, Inc. ,  The Walter and Eliza Hall Institute of Medical Research ,  Abbott Laboratories

发明人： BAELL, Jonathan, Bayldon ,  BUI, Chinh, Thien ,  COLMAN, Peter ,  CZABOTAR, Peter ,  DUDLEY, Danette, A. ,  FAIRBROTHER, Wayne, J. ,  FLYGARE, John, A. ,  LESSENE, Guillaume, Laurent ,  NDUBAKU, Chudi ,  NIKOLAKOPOULOS, George ,  SLEEBS, Brad, Edmund ,  SMITH, Brian, John ,  WATSON, Keith, Geoffrey ,  ELMORE, Steven, W. ,  HASVOLD, Lisa, A. ,  PETROS, Andrew, M. ,  SOUERS, Andrew, J. ,  TAO, Zhi-Fu ,  WANG, Le ,  WANG, Xilu ,  DESHAYES, Kurt

IPC分类号： A01N43/00

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 X
1a , X
1b , X
1c , X
1d , Q, A, R
1 , 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-x
L proteins.

公开(公告)号：EP2373163B1

公开(公告)日：2015-06-10

申请号：EP09837920.9

申请日：2009-12-17

申请人： Genentech, Inc. ,  The Walter and Eliza Hall Institute of Medical Research ,  AbbVie Inc.

发明人： BAELL, Jonathan, Bayldon ,  BUI, Chinh, Thien ,  COLMAN, Peter ,  CZABOTAR, Peter ,  DUDLEY, Danette, A. ,  FAIRBROTHER, Wayne, J. ,  FLYGARE, John, A. ,  LESSENE, Guillaume, Laurent ,  NDUBAKU, Chudi ,  NIKOLAKOPOULOS, George ,  SLEEBS, Brad, Edmund ,  SMITH, Brian, John ,  WATSON, Keith, Geoffrey ,  ELMORE, Steven, W. ,  HASVOLD, Lisa, A. ,  PETROS, Andrew, M. ,  SOUERS, Andrew, J. ,  TAO, Zhi-Fu ,  WANG, Le ,  WANG, Xilu ,  DESHAYES, Kurt

IPC分类号： A01N43/00 ,  C07D417/14 ,  C07D471/06 ,  C07D487/04 ,  C07D513/06 ,  C07D495/04 ,  C07D473/00 ,  C07D513/04

CPC分类号： C07D417/14 ,  C07D471/06 ,  C07D473/00 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04 ,  C07D513/06

公开(公告)号：EP2376085B1

公开(公告)日：2014-02-26

申请号：EP09837907.6

申请日：2009-12-17

申请人： Genentech, Inc. ,  The Walter and Eliza Hall Institute of Medical Research ,  AbbVie Inc.

发明人： BAELL, Jonathan, Bayldon ,  BUI, Chinh, Thien ,  COLMAN, Peter ,  DUDLEY, Danette, A. ,  FAIRBROTHER, Wayne, J. ,  FLYGARE, John, A. ,  LESSENE, Guillaume, Laurent ,  NDUBAKU, Chudi ,  NIKOLAKOPOULOS, George ,  RYE, Carl, Steven ,  SLEEBS, Brad, Edmund ,  SMITH, Brian, John ,  WATSON, Keith, Geoffrey ,  ELMORE, Steven, W. ,  PETROS, Andrew, M. ,  SOUERS, Andrew, J. ,  CZABOTAR, Peter

IPC分类号： A61K31/535 ,  C07D417/14 ,  C07D487/04

CPC分类号： C07D417/14 ,  C07D417/12 ,  C07D487/04

公开(公告)号：EP1778718A1

公开(公告)日：2007-05-02

申请号：EP05768304.7

申请日：2005-07-05

申请人： GENENTECH, INC.

发明人： COHEN, Frederick ,  DESHAYES, Kurt ,  FAIRBROTHER, Wayne, J. ,  FENG, Bainian ,  FLYGARE, John ,  GAZZARD, Lewis, J. ,  TSUI, Vickie, Hsiao-Wei

IPC分类号： C07K5/08 ,  A61K38/06 ,  A61P35/00

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.

公开(公告)号：EP1778718B1

公开(公告)日：2014-10-08

申请号：EP05768304.7

申请日：2005-07-05

申请人： Genentech, Inc.

发明人： COHEN, Frederick ,  DESHAYES, Kurt ,  FAIRBROTHER, Wayne, J. ,  FENG, Bainian ,  FLYGARE, John ,  GAZZARD, Lewis, J. ,  TSUI, Vickie, Hsiao-Wei

IPC分类号： C07K5/08 ,  A61K38/06 ,  A61P35/00

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

公开(公告)号：EP1590666B1

公开(公告)日：2008-07-09

申请号：EP03815888.7

申请日：2003-02-07

申请人： GENENTECH, INC.

发明人： FAIRBROTHER, Wayne, J. ,  DESHAYES, Kurt ,  FISCHER, Saloumeh ,  FLYGARE, John, A. ,  FRANKLIN, Matthew, C. ,  VUCIC, Domagoj

IPC分类号： G01N33/53 ,  G01N33/68 ,  C07K14/47 ,  C07K5/083 ,  C07K5/103 ,  A61K38/06 ,  A61K38/07 ,  A61K38/17

CPC分类号： C07K14/4747 ,  A61K38/00 ,  C07K5/0806 ,  C07K5/0827 ,  C07K5/1008 ,  G01N2500/04 ,  G01N2510/00

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.

公开(公告)号：EP1590666A1

公开(公告)日：2005-11-02

申请号：EP03815888.7

申请日：2003-02-07

申请人： GENENTECH, INC.

发明人： FAIRBROTHER, Wayne, J. ,  DESHAYES, Kurt ,  FISCHER, Saloumeh ,  FLYGARE, John, A. ,  FRANKLIN, Matthew, C. ,  VUCIC, Domagoj

IPC分类号： G01N33/53

CPC分类号： C07K14/4747 ,  A61K38/00 ,  C07K5/0806 ,  C07K5/0827 ,  C07K5/1008 ,  G01N2500/04 ,  G01N2510/00

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.

公开(公告)号：EP0970207A1

公开(公告)日：2000-01-12

申请号：EP98907337.4

申请日：1998-02-10

申请人： Genentech, Inc.

发明人： BALLINGER, Marcus, D. ,  JONES, Jennifer, T. ,  FAIRBROTHER, Wayne, J. ,  SLIWKOWSKI, Mark, X. ,  WELLS, James, A.

IPC分类号： C12N15/12 ,  C07K14/475 ,  C12N15/86 ,  C12N5/10 ,  A61K38/18 ,  G01N33/68

CPC分类号： G01N33/74 ,  A61K38/00 ,  C07K14/4756 ,  G01N2333/485

摘要： The present invention provides heregulin variants that are capable of binding an ErbB receptor. Included in the invention are variants of human heregulins, and, in particular, variants of human heregulin-β1 having enhanced affinity for the ErbB-3 and ErbB-4 receptors. These variants include at least one amino acid substitution and can include further modifications. The invention also provides nucleic acid molecules encoding heregulin variants and related vectors, host cells, pharmaceutical compositions, and methods.

公开(公告)号：EP1943257A2

公开(公告)日：2008-07-16

申请号：EP06760294.6

申请日：2006-05-18

申请人： GENENTECH, INC.

发明人： COHEN, Frederick ,  FAIRBROTHER, Wayne, J. ,  QUAN, Clifford ,  SUTHERLIN, Daniel P. ,  WOLF, Beni

IPC分类号： C07F5/02 ,  A61K31/00 ,  A61P35/00

CPC分类号： C07F5/025

摘要： Amino terminus-blocked peptide boronate compounds of Formulas (I) and (II) are useful for inhibiting Fibroblast Activation Protein (FAP) and other proteases, and for treating disorders mediated by FAP. Methods of using the amino terminus blocked peptide boronate compounds, and stereoisomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.