公开(公告)号：EP2376480A2

公开(公告)日：2011-10-19

申请号：EP09795606.4

申请日：2009-12-04

Applicant: Abbott Laboratories

Inventor： BRUNCKO, Milan ,  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.

IPC: C07D405/12 ,  A61K31/404 ,  A61P35/00

CPC classification number: C07D405/12 ,  C07D209/32 ,  C07D211/96 ,  C07D213/64 ,  C07D215/20 ,  C07D217/16 ,  C07D231/56 ,  C07D235/26 ,  C07D249/04 ,  C07D295/125 ,  C07D295/14 ,  C07D309/14 ,  C07D401/12 ,  C07D417/12

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

公开(公告)号：EP2376197A2

公开(公告)日：2011-10-19

申请号：EP09768289.2

申请日：2009-12-04

Applicant: Abbott Laboratories

Inventor： 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.

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

CPC classification number: 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

Abstract: 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.

Abstract translation: 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：EP2373163A1

公开(公告)日：2011-10-12

申请号：EP09837920.9

申请日：2009-12-17

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

Inventor： 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: A01N43/00

CPC classification number: C07D417/14 ,  C07D471/06 ,  C07D473/00 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04 ,  C07D513/06

Abstract: 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：EP2134685A1

公开(公告)日：2009-12-23

申请号：EP08745934.3

申请日：2008-04-16

Applicant: Abbott Laboratories

Inventor： BRUNCKO, Milan ,  SONG, Xiaohong ,  DING, Hong ,  TAO, Zhi-fu ,  KUNZER, Aaron R ,  ELMORE, Steven, W. ,  PARK, Cheol-Min ,  MADAR, David ,  WANG, Xilu ,  SOUERS, Andrew, J.

IPC: C07D209/42 ,  C07D403/04 ,  A61K31/404 ,  A61K31/405 ,  A61P35/00

CPC classification number: C07D209/42 ,  C07D403/04

Abstract: Compounds of formula (I) which inhibit the activity of anti-apoptotic Mcl-1 protein, compositins containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein are disclosed.

公开(公告)号：EP2134684A2

公开(公告)日：2009-12-23

申请号：EP08745970.7

申请日：2008-04-16

Applicant: Abbott Laboratories

Inventor： ELMORE, Steven, W. ,  SOUERS, Andrew, J. ,  BRUNCKO, Milan ,  SONG, Xiaohong ,  WANG, Xilu ,  HASVOLD, Lisa, A. ,  WANG, Le ,  KUNZER, Aaron, R. ,  PARK, Cheol-min ,  WENDT, Michael, D. ,  TAO, Zhi-fu ,  MADAR, David

IPC: C07D209/34 ,  C07D401/12 ,  C07D413/06 ,  C07D417/04 ,  A61P35/00 ,  A61K31/404

CPC classification number: 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

Abstract: Compounds of formula (I) which inhibit the activity of anti-apoptotic McI-I protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated McI-I protein are disclosed.

Abstract translation: 公开了抑制抗细胞凋亡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。

公开(公告)号：EP1339695A1

公开(公告)日：2003-09-03

申请号：EP01273519.7

申请日：2001-11-30

Applicant: Abbott Laboratories

Inventor： CLAIBORNE, Akiyo, K. ,  GWALTNEY, Stephen, L, II ,  HASVOLD, Lisa, A. ,  LI, Qun ,  LI, Tomgmei ,  LIN, Nan-Horng ,  MANTEI, Robert, A. ,  ROCKWAY, Todd, W. ,  SHAM, Hing, L. ,  SULLIVAN, Gerard, M. ,  TONG, Yunsong ,  WANG, Gary, T. ,  WANG, Le ,  WANG, Xilu ,  WANG, Weibo

IPC: C07D233/64 ,  A61K31/4164 ,  C07D401/12 ,  A61P35/00

CPC classification number: C07D233/64 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12

Abstract: Substituted imidazoles and thiazoles having the formula are useful for inhibiting farnesyltransferase. Also disclosed are farnesyltransferase-inhibiting compositions and methods of inhibiting farnesyltransferase in a patient.

公开(公告)号：EP1318978A2

公开(公告)日：2003-06-18

申请号：EP01971244.7

申请日：2001-09-20

Applicant: Abbott Laboratories

Inventor： MCCLELLAN, William ,  OOST, Thorsten ,  BRUNCKO, Milan ,  WANG, Xilu ,  AUGERI, David, J. ,  BAUMEISTER, Steven, A. ,  DICKMAN, Daniel, A. ,  DING, Hong ,  DINGES, Jurgen ,  FESIK, Stephen, W. ,  HAJDUK, Philip, J. ,  KUNZER, Aaron, R. ,  NETTESHEIM, David, G. ,  PETROS, Andrew, M. ,  ROSENBERG, Saul, H. ,  SHEN, Wang ,  THOMAS, Sheela, A. ,  WENDT, Michael, D.

IPC: C07C311/51 ,  C07C317/28 ,  C07C323/12 ,  C07C323/17 ,  C07C323/25 ,  C07C323/30 ,  C07C323/37 ,  C07C323/58 ,  C07C323/60

CPC classification number: C07D207/404 ,  C07C311/51 ,  C07C317/28 ,  C07C323/12 ,  C07C323/17 ,  C07C323/25 ,  C07C323/30 ,  C07C323/37 ,  C07C323/58 ,  C07C323/60 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2601/18 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2602/28 ,  C07C2602/42 ,  C07C2602/44 ,  C07C2603/74 ,  C07D203/10 ,  C07D205/12 ,  C07D207/24 ,  C07D209/08 ,  C07D209/96 ,  C07D211/44 ,  C07D211/70 ,  C07D211/74 ,  C07D213/61 ,  C07D213/70 ,  C07D213/71 ,  C07D215/14 ,  C07D215/227 ,  C07D215/48 ,  C07D217/04 ,  C07D221/20 ,  C07D231/12 ,  C07D235/08 ,  C07D235/26 ,  C07D241/16 ,  C07D249/04 ,  C07D263/56 ,  C07D263/58 ,  C07D277/62 ,  C07D277/64 ,  C07D295/13 ,  C07D295/155 ,  C07D295/185 ,  C07D295/205 ,  C07D295/215 ,  C07D295/26 ,  C07D307/14 ,  C07D317/54 ,  C07D333/28 ,  C07D333/68 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D417/12 ,  C07D451/02

Abstract: N-Benzoyl arylsulfonamides having the formula (I) 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.

Abstract translation: 具有式（I）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。