公开(公告)号：WO2011150016A1

公开(公告)日：2011-12-01

申请号：PCT/US2011/037849

申请日：2011-05-25

Applicant: ABBOTT LABORATORIES ,  TAO, Zhi-Fu ,  WANG, Xilu ,  SOUERS, Andrew J. ,  CATRON, Nathaniel D. ,  SULLIVAN, Gerard

Inventor： TAO, Zhi-Fu ,  WANG, Xilu ,  SOUERS, Andrew J. ,  CATRON, Nathaniel D. ,  SULLIVAN, Gerard

IPC: A01N43/42 ,  A01N43/40 ,  A61K31/44 ,  A01N43/38

CPC classification number: C07D471/04 ,  A61K31/18 ,  A61K31/44 ,  A61K31/496 ,  A61P35/00 ,  C07F9/65616 ,  Y02A50/385 ,  Y02A50/401 ,  Y02A50/411 ,  Y02A50/463

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.

公开(公告)号：WO2011149492A1

公开(公告)日：2011-12-01

申请号：PCT/US2010/057587

申请日：2010-11-22

Applicant: ABBOTT LABORATORIES ,  BRUNCKO, Milan ,  DING, Hong ,  DOHERTY, George ,  ELMORE, Steven ,  HASVOLD, Lisa ,  HEXAMER, Laura ,  KUNZER, Aaron R. ,  SONG, Xiaohong ,  SOUERS, Andrew, J. ,  SULLIVAN, Gerard ,  TAO, Zhi-Fu ,  WANG, Gary, T. ,  WANG, Le ,  WANG, Xilu ,  WENDT, Michael ,  MANTEI, Robert ,  HANSEN, Todd, M.

Inventor： BRUNCKO, Milan ,  DING, Hong ,  DOHERTY, George ,  ELMORE, Steven ,  HASVOLD, Lisa ,  HEXAMER, Laura ,  KUNZER, Aaron R. ,  SONG, Xiaohong ,  SOUERS, Andrew, J. ,  SULLIVAN, Gerard ,  TAO, Zhi-Fu ,  WANG, Gary, T. ,  WANG, Le ,  WANG, Xilu ,  WENDT, Michael ,  MANTEI, Robert ,  HANSEN, Todd, M.

IPC: C07D471/04 ,  A61K31/437 ,  A61K35/00

CPC classification number: C07D401/12 ,  A61K31/496 ,  C07D209/82 ,  C07D401/14 ,  C07D403/12 ,  C07D471/04 ,  C07D519/00 ,  Y02A50/463

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.

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：WO2011068561A1

公开(公告)日：2011-06-09

申请号：PCT/US2010/036919

申请日：2010-06-01

Applicant: ABBOTT LABORATORIES ,  BRUNCKO, Milan ,  DING, Hong ,  DOHERTY, George A. ,  ELMORE, Steven, W. ,  HASVOLD, Lisa ,  HEXAMER, Laura ,  KUNZER, Aaron ,  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. ,  HANSEN, Todd, M.

Inventor： BRUNCKO, Milan ,  DING, Hong ,  DOHERTY, George A. ,  ELMORE, Steven, W. ,  HASVOLD, Lisa ,  HEXAMER, Laura ,  KUNZER, Aaron ,  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. ,  HANSEN, Todd, M.

IPC: 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 classification number: 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

Abstract: 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.

Abstract translation: 公开了抑制抗凋亡Bc1-2或Bc1 xL蛋白活性的化合物（I），含有该化合物的组合物和治疗其中表达抗凋亡Bc1-2蛋白的疾病的方法。

公开(公告)号：WO2010138588A2

公开(公告)日：2010-12-02

申请号：PCT/US2010/036198

申请日：2010-05-26

Applicant: ABBOTT LABORATORIES ,  BRUNCKO, Milan ,  DING, Hong ,  DOHERTY, George ,  ELMORE, Steven ,  HASVOLD, Lisa ,  HEXAMER, Laura ,  KUNZER, Aaron R. ,  SONG, Xiaohong ,  SOUERS, Andrew J. ,  SULLIVAN, Gerard ,  TAO, Zhi-Fu ,  WANG, Gary T. ,  WANG, Le ,  WANG, Xilu ,  WENDT, Michael ,  MANTEI, Robert ,  HANSEN, Todd M.

Inventor： BRUNCKO, Milan ,  DING, Hong ,  DOHERTY, George ,  ELMORE, Steven ,  HASVOLD, Lisa ,  HEXAMER, Laura ,  KUNZER, Aaron R. ,  SONG, Xiaohong ,  SOUERS, Andrew J. ,  SULLIVAN, Gerard ,  TAO, Zhi-Fu ,  WANG, Gary T. ,  WANG, Le ,  WANG, Xilu ,  WENDT, Michael ,  MANTEI, Robert ,  HANSEN, Todd M.

IPC: C07D471/04

CPC classification number: C07D471/04 ,  C07D491/052 ,  C07D519/00

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，含有该化合物的组合物和治疗表达抗凋亡Bcl-2蛋白的疾病的方法。

公开(公告)号：WO2011068560A1

公开(公告)日：2011-06-09

申请号：PCT/US2010/036844

申请日：2010-06-01

Applicant: ABBOTT LABORATORIES ,  BRUNCKO, Milan ,  DAI, Yujia ,  DING, Hong ,  DOHERTY, George A. ,  ELMORE, Steven W. ,  HASVOLD, Lisa ,  HEXAMER, Laura ,  KUNZER, Aaron ,  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. ,  HANSEN, Todd M.

Inventor： BRUNCKO, Milan ,  DAI, Yujia ,  DING, Hong ,  DOHERTY, George A. ,  ELMORE, Steven W. ,  HASVOLD, Lisa ,  HEXAMER, Laura ,  KUNZER, Aaron ,  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. ,  HANSEN, Todd M.

IPC: C07D209/08 ,  C07D211/58 ,  C07D213/74 ,  C07D213/84 ,  C07D231/56 ,  C07D235/06 ,  C07D277/24 ,  C07D309/04 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04

CPC classification number: C07D209/08 ,  A61K31/635 ,  C07D211/58 ,  C07D213/74 ,  C07D213/84 ,  C07D231/56 ,  C07D235/06 ,  C07D277/24 ,  C07D295/30 ,  C07D309/04 ,  C07D309/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  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.

公开(公告)号：WO2010065824A2

公开(公告)日：2010-06-10

申请号：PCT/US2009/066722

申请日：2009-12-04

Applicant: ABBOTT LABORATORIES ,  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.

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疾病的方法，其中表达抗凋亡Bcl-2蛋白。

公开(公告)号：WO2005047294A1

公开(公告)日：2005-05-26

申请号：PCT/US2004/036582

申请日：2004-11-03

Applicant: ABBOTT LABORATORIES ,  TAO, Zhi-Fu ,  LIN, Nan-Horng ,  WANG, Le ,  SOWIN, Thomas, J. ,  SULLIVAN, Gerard M. ,  TONG, Yunsong ,  PRZYTULINSKA, Magdalenna ,  LI, Gaoquan

Inventor： TAO, Zhi-Fu ,  LIN, Nan-Horng ,  WANG, Le ,  SOWIN, Thomas, J. ,  SULLIVAN, Gerard M. ,  TONG, Yunsong ,  PRZYTULINSKA, Magdalenna ,  LI, Gaoquan

IPC: C07D498/08

CPC classification number: C07D498/08 ,  C07D498/18

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：WO2004080973A1

公开(公告)日：2004-09-23

申请号：PCT/US2004/006921

申请日：2004-03-04

Applicant: ABBOTT LABORATORIES

Inventor： TONG, Yunsung ,  CLAIBORNE, Akiyo, K. ,  LI, Gaoquan ,  LIN, Nan-Horng ,  SHAM, Hing ,  TAO, Zhi-Fu ,  SOWIN, Tom

IPC: C07D231/54

CPC classification number: C07D249/08 ,  C07D231/12 ,  C07D231/54 ,  C07D233/56 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

Abstract: Compounds having the formula (I) (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）（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：EP2507211A1

公开(公告)日：2012-10-10

申请号：EP10722500.5

申请日：2010-06-01

Applicant: Abbott Laboratories

Inventor： BRUNCKO, Milan ,  DAI, Yujia ,  DING, Hong ,  DOHERTY, George A. ,  ELMORE, Steven W. ,  HASVOLD, Lisa ,  HEXAMER, Laura ,  KUNZER, Aaron ,  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. ,  HANSEN, Todd M.

IPC: C07D209/08 ,  C07D211/58 ,  C07D213/74 ,  C07D213/84 ,  C07D231/56 ,  C07D235/06 ,  C07D277/24 ,  C07D309/04 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04

CPC classification number: C07D209/08 ,  A61K31/635 ,  C07D211/58 ,  C07D213/74 ,  C07D213/84 ,  C07D231/56 ,  C07D235/06 ,  C07D277/24 ,  C07D295/30 ,  C07D309/04 ,  C07D309/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  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，含有该化合物的组合物和治疗表达抗凋亡Bcl-2蛋白的疾病的方法。