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：EP2376197B1

公开(公告)日：2017-02-15

申请号：EP09768289.2

申请日：2009-12-04

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

发明人： BRUNCKO, Milan ,  DAI, Yujia ,  DING, Hong ,  DOHERTY, George, A. ,  ELMORE, Steven, W. ,  HASVOLD, Lisa ,  HEXAMER, Laura ,  KUNZER, Aaron, R. ,  MANTEI, Robert, A. ,  MCCLELLAN, William, J. ,  PARK, Chang, H. ,  PARK, Cheol-Min ,  PETROS, Andrew, M. ,  SONG, Xiaohong ,  SOUERS, Andrew, J. ,  SULLIVAN, Gerard, M. ,  TAO, Zhi-Fu ,  WANG, Gary, T. ,  WANG, Le ,  WANG, Xilu ,  WENDT, Michael, D. ,  CZABOTAR, Peter Edward ,  LESSENE, Guillaume Laurent ,  COLMAN, Peter Malcom

IPC分类号： A61P35/00 ,  A61K31/496 ,  C07D403/12

CPC分类号： C07D405/12 ,  C07D209/08 ,  C07D211/58 ,  C07D213/74 ,  C07D213/84 ,  C07D231/56 ,  C07D235/06 ,  C07D277/24 ,  C07D295/30 ,  C07D309/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04

公开(公告)号：EP3112361A1

公开(公告)日：2017-01-04

申请号：EP16175661.4

申请日：2009-12-04

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

发明人： BRUNCKO, Milan ,  DAI, Yujia ,  DING, Hong ,  DOHERTY, George, A. ,  ELMORE, Steven, W. ,  HASVOLD, Lisa ,  HEXAMER, Laura ,  KUNZER, Aaron, R. ,  MANTEI, Robert, A. ,  MCCLELLAN, William, J. ,  PARK, Chang, H. ,  PARK, Cheol-Min ,  PETROS, Andrew, M. ,  SONG, Xiaohong ,  SOUERS, Andrew, J. ,  SULLIVAN, Gerard, M. ,  TAO, Zhi-Fu ,  WANG, Gary, T. ,  WANG, Le ,  WANG, Xilu ,  WENDT, Michael, D. ,  CZABOTAR, Peter Edward ,  LESSENE, Guillaume Laurent ,  COLMAN, Peter Malcom

IPC分类号： C07D401/14 ,  C07D405/14 ,  C07D213/74 ,  C07D309/04 ,  C07D213/84 ,  C07D235/06 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D277/24 ,  C07D209/08 ,  C07D211/58 ,  C07D295/30 ,  A61P35/00 ,  A61K31/496 ,  C07D231/56

CPC分类号： C07D405/12 ,  C07D209/08 ,  C07D211/58 ,  C07D213/74 ,  C07D213/84 ,  C07D231/56 ,  C07D235/06 ,  C07D277/24 ,  C07D295/30 ,  C07D309/04 ,  C07D401/14 ,  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.

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其中表达抗凋亡Bcl-2蛋白的疾病的方法。

公开(公告)号：EP2387559A1

公开(公告)日：2011-11-23

申请号：EP10701283.3

申请日：2010-01-15

申请人： Abbott Laboratories

发明人： KUNZER, Aaron, R. ,  ELMORE, Steven, W. ,  HEXAMER, Laura ,  PARK, Cheol-Min ,  SOUERS, Andrew, J. ,  SULLIVAN, Gerard, M. ,  WANG, Gary, T. ,  WANG, Xilu ,  WENDT, Michael, D.

IPC分类号： C07C311/51 ,  C07D207/36 ,  C07D211/96 ,  C07D231/18 ,  C07D261/10 ,  C07D275/03 ,  C07D277/36 ,  C07D333/34 ,  C07D285/135 ,  C07D295/155 ,  C07D285/125 ,  C07D295/26 ,  A61K31/18 ,  A61P35/00

CPC分类号： C07D277/54 ,  C07C311/00 ,  C07C311/51 ,  C07D207/36 ,  C07D211/96 ,  C07D231/18 ,  C07D261/10 ,  C07D275/03 ,  C07D277/36 ,  C07D277/60 ,  C07D285/125 ,  C07D285/135 ,  C07D295/155 ,  C07D295/26 ,  C07D333/34 ,  C07D333/36 ,  C07D333/42 ,  C07D333/62 ,  C07D409/12 ,  C07D413/04 ,  C07D413/06 ,  C07D417/14 ,  C07D487/04 ,  C07D513/04

摘要： Disclosed are compounds of Formula (1), in which A
1 , Z
1 , Z
1A , Z
2 , Z
2A , L
1 and Z
3 are as defined in the claims, which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and their use in treating diseases during which anti-apoptotic Bcl-2 protein is expressed.

摘要翻译： 公开了式（1）化合物，其中A 1，Z 1，Z 1A，Z 2，Z 2A，L 1和Z 3如权利要求中所定义，其抑制抗凋亡Bcl-2蛋白的活性 含有该化合物的组合物及其在治疗表达抗凋亡Bcl-2蛋白的疾病中的用途。

公开(公告)号：EP1534703A2

公开(公告)日：2005-06-01

申请号：EP03760268.7

申请日：2003-06-11

申请人： ABBOTT LABORATORIES

发明人： BLACKBURN, Christopher ,  LAI, Su-jen ,  LEE, Jennifer, G. ,  MAGUIRE, Martin ,  PATANE, Michael, A. ,  LAMARCHE, Matthew, J. ,  CULLIS, Courtney, A. ,  BROWN, James ,  VASUDEVAN, Anil ,  FREEMAN, Jennifer, C. ,  MULHERN, Mathew, M. ,  LYNCH, John, K. ,  GAO, Ju ,  WODKA, Dariusz ,  SOUERS, Andrew, J. ,  IYENGAR, Rajesh

IPC分类号： C07D405/00

CPC分类号： C07D405/14 ,  C07D401/14 ,  C07D405/12 ,  C07D409/14 ,  C07D413/14

摘要： This invention provides compounds that are antagonists of melanin concentrating hormone receptor-1 (MCH-R1). The compounds are represented by formula (I): where m is zero or one, n is zero to two, Y is oxygen or -N (R )-, R , R , R , R , R , R , and Ring A are defined in the specification. Coumarin and quinolone compounds where R and R together form a fused benzo ring are preferred. The invention also provides compounds of formula (VI) where the coumarin moiety is replaced by a quinazolinone ring. The compounds are useful for treating MCH-R1-related disorders, particularly overweight conditions including obesity.

公开(公告)号：EP2507229A1

公开(公告)日：2012-10-10

申请号：EP10727241.1

申请日：2010-06-01

申请人： Abbott Laboratories

发明人： PARK, Chang, H. ,  BRUNCKO, Milan ,  DING, Hong ,  DOHERTY, George A. ,  ELMORE, Steven, W. ,  HASVOLD, Lisa ,  HEXAMER, Laura ,  KUNZER, Aaron ,  MANTEI, Robert, A. ,  McCLELLAN, William, J. ,  PARK, Cheol-Min ,  PETROS, Andrew, M. ,  SONG, Xiaohong ,  SOUERS, Andrew, J. ,  SULLIVAN, Gerard, M. ,  TAO, Zhi-Fu ,  WANG, Gary, T. ,  WANG, Le ,  WANG, Xilu ,  WENDT, Michael, D. ,  HANSEN, Todd, M.

IPC分类号： C07D405/12 ,  A61K31/404 ,  A61P35/00 ,  C07D209/32 ,  C07D211/96 ,  C07D213/64 ,  C07D215/20 ,  C07D217/16 ,  C07D235/26 ,  C07D249/04 ,  C07D295/14 ,  C07D309/14 ,  C07D401/12 ,  C07D295/125 ,  C07D231/56 ,  C07D405/14

CPC分类号： C07D401/12 ,  A61K31/407 ,  A61K31/495 ,  A61K31/496 ,  A61K31/501 ,  A61K31/5377 ,  A61K45/06 ,  C07D209/08 ,  C07D209/32 ,  C07D211/58 ,  C07D211/96 ,  C07D213/64 ,  C07D215/20 ,  C07D217/16 ,  C07D231/56 ,  C07D235/26 ,  C07D241/04 ,  C07D249/04 ,  C07D295/125 ,  C07D295/14 ,  C07D295/155 ,  C07D309/04 ,  C07D309/14 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D413/06 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04

摘要： Disclosed are compounds (I) which inhibit the activity of anti-apoptotic Bc1-2 or Bc1 xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti apoptotic Bc1-2 protein.

公开(公告)号：EP2387560A2

公开(公告)日：2011-11-23

申请号：EP10701083.7

申请日：2010-01-15

申请人： Abbott Laboratories

发明人： HEXAMER, Laura ,  DING, Hong ,  ELMORE, Steven, W. ,  KUNZER, Aaron, R. ,  SONG, Xiaohong ,  SOUERS, Andrew, J. ,  SULLIVAN, Gerard, M. ,  TAO, Zhi-fu ,  WENDT, Michael, D.

IPC分类号： C07D209/08 ,  C07D311/14 ,  C07D295/155 ,  A61P35/00 ,  A61K31/635 ,  C07D213/71 ,  C07D231/56 ,  C07D235/04 ,  C07D265/02 ,  C07D285/14

CPC分类号： C07D295/155 ,  C07D209/08 ,  C07D213/71 ,  C07D231/56 ,  C07D235/04 ,  C07D265/02 ,  C07D285/14 ,  C07D311/14

摘要： Disclosed are compounds of formula (I) 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蛋白质活性的式（I）化合物，含有该化合物的组合物和治疗表达抗凋亡Bcl-2蛋白质的疾病的方法。