公开(公告)号：CA2747170A1

公开(公告)日：2010-07-15

申请号：CA2747170

申请日：2009-12-17

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

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

Abstract: In one aspect, the present invention provides for a compound 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 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-xL proteins.

公开(公告)号：CA2744708A1

公开(公告)日：2010-06-10

申请号：CA2744708

申请日：2009-12-04

Applicant: ABBOTT LAB

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: C07D405/12 ,  A61K31/395 ,  A61K31/496 ,  A61P35/00 ,  C07D295/04 ,  C07D309/00 ,  C07D401/00 ,  C07D403/12

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：UY26942A1

公开(公告)日：2002-04-26

申请号：UY26942

申请日：2001-09-19

Applicant: ABBOTT LAB

Inventor： AUGERI DAVID J ,  DICKMAN DANIEL A ,  WANG XILU ,  MCCLELLAN WILLIAM ,  FESIK STEPHEN W ,  NETTESHEIM DAVID G ,  SHEN WANG ,  OOST THORSTEN ,  DING HONG ,  HAJDUK PHILIP J ,  PETROS ANDREW M ,  THOMAS SHEELA A ,  BRUNCKO MILAN ,  BAUMEISTE STEVEN A ,  DINGES JURGEN ,  KUNZER AARON R ,  ROSEMBERG SAUL H ,  WENDT MICHAEL D

IPC: A61K31/18 ,  A61K31/428 ,  A61K31/63 ,  A61K31/635 ,  A61P9/10 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/12 ,  A61P31/18 ,  A61P35/00 ,  A61P37/02 ,  C07C311/46 ,  C07C311/51 ,  C07C317/28 ,  C07C323/12 ,  C07C323/17 ,  C07C323/25 ,  C07C323/30 ,  C07C323/37 ,  C07C323/43 ,  C07C323/44 ,  C07C323/48 ,  C07C323/58 ,  C07C323/60 ,  C07D203/10 ,  C07D205/04 ,  C07D205/12 ,  C07D207/09 ,  C07D207/24 ,  C07D207/40 ,  C07D207/404 ,  C07D209/08 ,  C07D209/52 ,  C07D209/54 ,  C07D209/96 ,  C07D211/14 ,  C07D211/44 ,  C07D211/70 ,  C07D211/74 ,  C07D213/56 ,  C07D213/61 ,  C07D213/64 ,  C07D213/69 ,  C07D213/70 ,  C07D213/71 ,  C07D215/14 ,  C07D215/22 ,  C07D215/227 ,  C07D215/38 ,  C07D215/48 ,  C07D217/04 ,  C07D221/20 ,  C07D231/12 ,  C07D233/60 ,  C07D235/08 ,  C07D235/26 ,  C07D241/08 ,  C07D241/16 ,  C07D249/04 ,  C07D263/32 ,  C07D263/56 ,  C07D263/58 ,  C07D277/62 ,  C07D277/64 ,  C07D295/13 ,  C07D295/155 ,  C07D295/16 ,  C07D295/185 ,  C07D295/20 ,  C07D295/205 ,  C07D295/215 ,  C07D295/26 ,  C07D307/14 ,  C07D317/54 ,  C07D333/28 ,  C07D333/68 ,  C07D333/70 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D405/06 ,  C07D417/12 ,  C07D451/02 ,  C07D491/107 ,  C07C311/16 ,  C07D207/00 ,  C07D211/00 ,  C07D307/02 ,  C07D309/00 ,  C07D333/02 ,  C07D335/02

Abstract: Las N - benzoilarilsulfonamidas de la fórmula son inhibidoras de BCL - XI y resultan útiles para promover la apoptosis. Asimismo se revelan composiciones inhibidoras de BCL - XI y métodos para promover la apoptosis en un mamífero.

公开(公告)号：AU9115101A

公开(公告)日：2002-04-02

申请号：AU9115101

申请日：2001-09-20

Applicant: ABBOTT LAB

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: A61K31/18 ,  A61K31/428 ,  A61K31/63 ,  A61K31/635 ,  A61P9/10 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/12 ,  A61P31/18 ,  A61P35/00 ,  A61P37/02 ,  C07C311/46 ,  C07C311/51 ,  C07C317/28 ,  C07C323/12 ,  C07C323/17 ,  C07C323/25 ,  C07C323/30 ,  C07C323/37 ,  C07C323/43 ,  C07C323/44 ,  C07C323/48 ,  C07C323/58 ,  C07C323/60 ,  C07D203/10 ,  C07D205/04 ,  C07D205/12 ,  C07D207/09 ,  C07D207/24 ,  C07D207/40 ,  C07D207/404 ,  C07D209/08 ,  C07D209/52 ,  C07D209/54 ,  C07D209/96 ,  C07D211/14 ,  C07D211/44 ,  C07D211/70 ,  C07D211/74 ,  C07D213/56 ,  C07D213/61 ,  C07D213/64 ,  C07D213/69 ,  C07D213/70 ,  C07D213/71 ,  C07D215/14 ,  C07D215/22 ,  C07D215/227 ,  C07D215/38 ,  C07D215/48 ,  C07D217/04 ,  C07D221/20 ,  C07D231/12 ,  C07D233/60 ,  C07D235/08 ,  C07D235/26 ,  C07D241/08 ,  C07D241/16 ,  C07D249/04 ,  C07D263/32 ,  C07D263/56 ,  C07D263/58 ,  C07D277/62 ,  C07D277/64 ,  C07D295/13 ,  C07D295/155 ,  C07D295/16 ,  C07D295/185 ,  C07D295/20 ,  C07D295/205 ,  C07D295/215 ,  C07D295/26 ,  C07D307/14 ,  C07D317/54 ,  C07D333/28 ,  C07D333/68 ,  C07D333/70 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D405/06 ,  C07D417/12 ,  C07D451/02 ,  C07D491/107 ,  C07C311/00

公开(公告)号：CA2744711C

公开(公告)日：2017-06-27

申请号：CA2744711

申请日：2009-12-04

Applicant: ABBOTT LAB

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

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：NZ593536A

公开(公告)日：2013-07-26

申请号：NZ59353609

申请日：2009-12-17

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

Inventor： 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: A61K31/535 ,  A61K31/435 ,  A61K31/495 ,  A61K31/5375 ,  A61K31/538 ,  A61K31/5383 ,  C07D215/00 ,  C07D401/14 ,  C07D413/02

Abstract: Disclosed herein are quinoline compounds of formula I, wherein the substituents are as defined within the specification, processes for their preparation, compositions comprising said compounds and uses thereof. Said compounds are useful in the treatment or prevention of a disease or condition caused, exacerbated by or resulting from an excess of, or undesired activation of, platelets in a patient, as such is useful for treating essential thrombocythemia, polycythemia vera, restenosis, perioperative antiplatelet therapy and device-associated thrombi and also small cell lung cancer. Examples of particularly preferred compounds include: 6-(1-(Benzo[d]thiazol-2-ylcarbamoyl)-1,2,3,4-tetrahydroquinolin-7-yl)-3-(3-(4-(dimethylamino)phenoxy)propoxy)picolinic acid 2-(1-(benzo[d]thiazol-2-ylcarbamoyl)-1,2,3,4-tetrahydroquinolin-7-yl)thiazole-4-carboxylic acid; 6-(1-(benzo[d]thiazol-2-ylcarbamoyl)-1,2,3,4-tetrahydroquinolin-7-yl)-3-hydroxypicolinic acid; 6-(4-(benzo[d]thiazol-2-ylcarbamoyl)-1-methyl-1,2,3,4-tetrahydroquinoxalin-6-yl)picolinic acid; 6-(1-(benzo[d]thiazol-2-ylcarbamoyl)-1,2,3,4-tetrahydroquinolin-7-yl)-3-(1-benzyl-1H-pyrazol-4-yl)picolinic acid; (E)-2-(1-(benzo[d]thiazol-2-ylcarbamoyl)-1,2,3,4-tetrahydroquinolin-7-yl)-5-(prop-1-enyl)thiazole-4-carboxylic acid; 5-(3-(4-(aminomethyl)phenoxy)propyl)-2-(4-(benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl)thiazole-4-carboxylic acid.

公开(公告)号：ZA201104463B

公开(公告)日：2012-09-26

申请号：ZA201104463

申请日：2011-06-15

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

Inventor： BAELL JONATHAN BAYLDON ,  BUI CHINH THIEN ,  COLMAN PETER ,  DUDLEY DANETTE ANDREA ,  FAIRBROTHER WAYNE J ,  FLYGARE JOHN A ,  LESSENE GUILLAUME LAURENT ,  NDUBAKU CHUDI ,  NIKOLAKOPOULOS GEORGE ,  RYE CARL STEVEN ,  SLEEBS BRAD EDMUND ,  SMITH BRIAN JOHN EDWARD ,  WATSON KEITH GEOFFREY ,  ELMORE STEVEN W ,  PETROS ANDREW M ,  SOUERS ANDRE J ,  CZABOTAR PETER

IPC: A61K20060101

公开(公告)号：CR20120346A

公开(公告)日：2012-09-03

申请号：CR20120346

申请日：2012-06-25

Applicant: ABBOTT LAB

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

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

Abstract: Compuestos que inhiben la actividad de las proteínas anti-apoptóticas Bcl-2 o Bcl-XL, composiciones que contienen dichos compuestos y métodos para tratar enfermedades durante las cuales se expresa la proteína anti-apoptótica Bcl-2.

公开(公告)号：ECSP12012017A

公开(公告)日：2012-08-31

申请号：ECSP12012017

申请日：2012-07-03

Applicant: ABBOTT LAB

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

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

Abstract: Compuestos que inhiben la actividad de las proteínas anti-apoptóticas Bcl-2 o Bcl-XL, composiciones que contienen dichos compuestos y métodos para tratar enfermedades durante las cuales se expresa la proteína anti-apoptótica Bcl-2.

公开(公告)号：MX2012006391A

公开(公告)日：2012-06-19

申请号：MX2012006391

申请日：2010-06-01

Applicant: ABBOTT LAB

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

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

Abstract: Se describen los compuestos que inhiben la actividad de las proteínas anti-apoptóticas BcI-2, las composiciones que contienen los compuestos, y los métodos para tratar las enfermedades durante las cuales se expresa la proteína anti-apoptótica Bcl-2.