公开(公告)号：WO2004076424A1

公开(公告)日：2004-09-10

申请号：PCT/US2004/005728

申请日：2004-02-26

Applicant: ABBOTT LABORATORIES

Inventor： HASVOLD, Lisa, A. ,  HEXAMER, Laura ,  LI, Gaoquan ,  LIN, Nan-Horng ,  SHAM, Hing ,  SOWIN, Tom ,  SULLIVAN, Gerard, M. ,  WANG, Le ,  XIA, Ping Xia

IPC: C07D243/38

CPC classification number: C07D243/38 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/06 ,  C07D413/10 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D491/10

Abstract: Compounds having the formula (I) are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

Abstract translation: 具有式（I）的化合物可用于抑制蛋白激酶。 还公开了制备化合物，含有化合物的组合物和使用该化合物的处理方法的方法。

公开(公告)号：WO2010080503A1

公开(公告)日：2010-07-15

申请号：PCT/US2009/068496

申请日：2009-12-17

Applicant: GENENTECH, INC. ,  THE WALTER AND ELIZA HALL INSTITUTE OF MEDICAL RESEARCH ,  ABBOTT LABORATORIES ,  BAELL, Jonathon, Bayldon ,  BUI, Chinh, Thien ,  COLMAN, Peter ,  CZABOTAR, Peter ,  DUDLEY, Danette, A. ,  FAIRBROTHER, Wayne, J. ,  FLYGARE, John, A. ,  LASSENE, 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

Inventor： BAELL, Jonathon, Bayldon ,  BUI, Chinh, Thien ,  COLMAN, Peter ,  CZABOTAR, Peter ,  DUDLEY, Danette, A. ,  FAIRBROTHER, Wayne, J. ,  FLYGARE, John, A. ,  LASSENE, 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.

Abstract translation: 一方面，本发明提供式I的化合物; 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。 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。

公开(公告)号：WO2008131000A2

公开(公告)日：2008-10-30

申请号：PCT/US2008/060472

申请日：2008-04-16

Applicant: ABBOTT LABORATORIES ,  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

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

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 which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 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：WO2002074747A1

公开(公告)日：2002-09-26

申请号：PCT/US2001/043168

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

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

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

Abstract translation: 具有式（I）的取代的咪唑和噻唑可用于抑制法呢基转移酶。 还公开了法呢基转移酶抑制组合物和在患者体内抑制法尼基转移酶的方法。

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：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：EP1339695B1

公开(公告)日：2006-04-19

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.

Abstract translation: 具有式（I）的取代的咪唑和噻唑可用于抑制法尼基转移酶。 还公开了法尼基转移酶抑制组合物和抑制患者中法尼基转移酶的方法。

公开(公告)号：EP1606268A1

公开(公告)日：2005-12-21

申请号：EP04715097.4

申请日：2004-02-26

Applicant: ABBOTT LABORATORIES

Inventor： HASVOLD, Lisa, A. ,  HEXAMER, Laura ,  LI, Gaoquan ,  LIN, Nan-Horng ,  SHAM, Hing ,  SOWIN, Tom ,  SULLIVAN, Gerard, M. ,  WANG, Le ,  XIA, Ping Xia

IPC: C07D243/38 ,  A61K31/551 ,  A61P35/00

CPC classification number: C07D243/38 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/06 ,  C07D413/10 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D491/10

Abstract: Compounds having the formula (I) are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.