公开(公告)号：WO2010138588A3

公开(公告)日：2011-04-07

申请号：PCT/US2010036198

申请日：2010-05-26

Applicant: ABBOTT LAB ,  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 ,  A61P35/00

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：WO0109103A3

公开(公告)日：2001-05-31

申请号：PCT/US0020053

申请日：2000-07-21

Applicant: ABBOTT LAB

Inventor： WANG LE ,  LI QUN ,  SHAM HING L ,  WOODS KEITH W

IPC: C07D233/64 ,  A61K31/4164 ,  A61P35/00 ,  A61P43/00 ,  C07D233/54

CPC classification number: C07D233/64

Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt or prodrug thereof, wherein R is selected from the group consisting of hydrogen, methyl, ethyl, propyl, and isolpropyl; and one of R or R is 3,4,5-trimethoyxphenyl, and the other is phenyl substituted with one, two, or three substitutents independently selected from the group consisting of alkoxy, halo, and -NR R , wherein R and R are independently selected from the group consisting of hydrogen and alkyl, inhibit celluar proliferation. Processes for the preparation of the compounds, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds are disclosed.

Abstract translation: 式（I）化合物或其药学上可接受的盐或前药，其中R 1选自氢，甲基，乙基，丙基和异丙基; 并且R 2或R 3中的一个是3,4,5-三甲氧基苯基，另一个是被一个，两个或三个取代基取代的苯基，所述取代基独立地选自烷氧基，卤素和-NR 2 R 3; 其中R 4和R 5独立地选自氢和烷基，抑制细胞增殖。 公开了制备该化合物的方法，含有该化合物的药物组合物以及使用该化合物的治疗方法。

公开(公告)号：WO2010138588A9

公开(公告)日：2011-05-05

申请号：PCT/US2010036198

申请日：2010-05-26

Applicant: ABBOTT LAB ,  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 ,  A61P35/00

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：WO2010065824A3

公开(公告)日：2010-10-07

申请号：PCT/US2009066722

申请日：2009-12-04

Applicant: ABBOTT LAB ,  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.

公开(公告)号：WO2010065865A3

公开(公告)日：2010-09-16

申请号：PCT/US2009066790

申请日：2009-12-04

Applicant: ABBOTT LAB ,  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

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 ,  C07D209/32 ,  C07D211/96 ,  C07D213/64 ,  C07D215/20 ,  C07D217/16 ,  C07D235/26 ,  C07D249/04 ,  C07D295/125 ,  C07D295/14 ,  C07D309/14 ,  C07D401/12

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.

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

公开(公告)号：WO2008082839A3

公开(公告)日：2009-01-29

申请号：PCT/US2007086472

申请日：2007-12-05

Applicant: ABBOTT LAB ,  PENNING THOMAS D ,  HASVOLD LISA A ,  HEXAMER LAURA A ,  GIRANDA VINCENT L ,  LIN NAN-HORNG ,  TAO ZHI-FU ,  WANG LE

Inventor： PENNING THOMAS D ,  HASVOLD LISA A ,  HEXAMER LAURA A ,  GIRANDA VINCENT L ,  LIN NAN-HORNG ,  TAO ZHI-FU ,  WANG LE

IPC: A61K31/519 ,  A61P43/00 ,  C07D495/04

CPC classification number: C07D495/04

Abstract: Thieno[3,2-d]pyrimidiii-4-one derivatives as inhibitors of Pim kinases, ways to make them and methods of treating patients using them are disclosed.

Abstract translation: 披露了噻吩并[3,2-d]嘧啶-4-酮衍生物作为Pim激酶的抑制剂，其制备方法和使用它们治疗患者的方法。

公开(公告)号：WO2008131000A3

公开(公告)日：2008-12-18

申请号：PCT/US2008060472

申请日：2008-04-16

Applicant: ABBOTT LAB ,  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 ,  A61K31/404 ,  A61P35/00 ,  C07D401/12 ,  C07D413/06 ,  C07D417/04

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: 公开了抑制抗凋亡McI-1蛋白活性的式（I）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McI-1蛋白的疾病的方法。

公开(公告)号：EP2373163A4

公开(公告)日：2012-10-24

申请号：EP09837920

申请日：2009-12-17

Applicant: GENENTECH INC ,  INST MEDICAL W & E HALL ,  ABBOTT LAB

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

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

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

公开(公告)号：CA2747170C

公开(公告)日：2017-07-18

申请号：CA2747170

申请日：2009-12-17

Applicant: ABBOTT LAB ,  GENENTECH INC ,  THE WALTER AND ELIZA HALL INST OF MEDICAL RES

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: C07D417/14 ,  A61K31/4725 ,  A61P35/00 ,  C07D455/04 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04

Abstract: In one aspect, the present invention provides for a com-pound of Formula I; in which the variable X1a, X1b, X1c, X1d, Q, A, R1, B, L, E, and the subscripts m and n have the meanings as described herein. In another aspect, the present invention provides for pharmaceutical compo-sitions 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-ex-pression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-X L proteins.

公开(公告)号：DOP2012000153A

公开(公告)日：2017-04-30

申请号：DO2012000153

申请日：2012-06-01

Applicant: ABBOTT LAB

Inventor： ELMORE STEVEN W ,  SOUERS ANDREW J ,  BRUNCKO MILAN ,  SONG XIAOHONG ,  WANG XILU ,  WANG LE ,  PARK CHEOL-MIN ,  TAO ZHI-FU ,  DING HONG ,  HASVOLD LISA ,  HEXAMER LAURA ,  MCCLELLAN WILLIAM J ,  PARK CHANG H ,  PETROS ANDREW M ,  SULLIVAN GERARD M ,  WANG GARY T ,  WENDT MICHAEL D ,  MANTEI ROBERT A ,  HANSEN TODD M ,  DOHERTY GEORGE A ,  KUNZER AARON

IPC: A61K31/404 ,  A61P35/00 ,  C07D209/32 ,  C07D211/96 ,  C07D213/64 ,  C07D215/20 ,  C07D217/16 ,  C07D235/26 ,  C07D249/04

Abstract: Compuestos de Fórmula I derivados de sulfonamida, por ejemplo, N-({5-cloro-6-[(4,4-difluorociclohexil)metoxi]piridin-3-il}sulfonil)-4-(4-{[2-(4-clorofenil)-4,4-dimetilciclohex-1-en-1-il]metil}piperazin-1-il)-2-(1H-indazol-4-iloxi)benzamida, que inhiben la actividad de las proteínas anti-apoptóticas Bcl- 2 o Bcl-XL y composiciones que contienen dichos compuestos, los cuales sirven para preparer un medicamento útil en el tratamiento de enfermedades durante las cuales se expresa la proteína anti-apoptótica Bcl-2, por ejemplo, cáncer de vejiga, cáncer de cerebro, cáncer de mamas, cáncer de médula ósea, cáncer cervical, leucemia linfocítica crónica, cáncer colorrectal, cancer de esófago, cáncer hepatocelular, leucemia linfoblástica, linfoma folicular, una malignidad linfoide originada en células T o células B, melanoma, leucemia mielógena, mieloma, cáncer oral, cáncer de ovarios, cáncer de pulmón de células no pequeñas, cáncer de próstata, cáncer de pulmón de células pequeñas o cáncer de bazo, entre otras.