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：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：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：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：WO2010083441A3

公开(公告)日：2010-09-10

申请号：PCT/US2010021243

申请日：2010-01-15

Applicant: ABBOTT LAB ,  HEXAMER LAURA ,  DING HONG ,  ELMORE STEVEN W ,  KUNZER AARON R ,  SONG XIAOHONG ,  SOUERS ANDREW J ,  SULLIVAN GERARD M ,  TAO ZHI-FU ,  WENDT MICHAEL D

Inventor： HEXAMER LAURA ,  DING HONG ,  ELMORE STEVEN W ,  KUNZER AARON R ,  SONG XIAOHONG ,  SOUERS ANDREW J ,  SULLIVAN GERARD M ,  TAO ZHI-FU ,  WENDT MICHAEL D

IPC: C07D209/08 ,  A61K31/635 ,  A61P35/00 ,  C07D213/71 ,  C07D231/56 ,  C07D235/04 ,  C07D265/02 ,  C07D285/14 ,  C07D295/155 ,  C07D311/14

CPC classification number: C07D295/155 ,  C07D209/08 ,  C07D213/71 ,  C07D231/56 ,  C07D235/04 ,  C07D265/02 ,  C07D285/14 ,  C07D311/14

Abstract: Disclosed are compounds of formula (I) 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蛋白活性的式（I）化合物，含有该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：BR112012012918A2

公开(公告)日：2015-09-08

申请号：BR112012012918

申请日：2010-06-01

Applicant: ABBOTT LAB

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

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: agente indutor de apoptose para o tratamento de câncer e de doenças imunes e autoimunes. a presente invenção descreve compostos que inibem a atividade de proteínas anti-apoptóticas da família bcl-2, além de composições contendo os compostos e métodos para tratar doenças que cursam com a expressão da proteína antiapoptótica bcl-2.

公开(公告)号：BRPI0810365A2

公开(公告)日：2014-10-29

申请号：BRPI0810365

申请日：2008-04-16

Applicant: ABBOTT LAB

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 ,  A61K31/404 ,  A61P35/00 ,  C07D401/12 ,  C07D413/06 ,  C07D417/04

Abstract: 7-substituted indole derivatives which inhibit the activity of anti-apoptotic Mcl-1 protein and compositions containing the compounds are disclosed.

公开(公告)号：NZ579833A

公开(公告)日：2012-11-30

申请号：NZ57983308

申请日：2008-04-16

Applicant: ABBOTT LAB

Inventor： TAO ZHI-FU ,  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 ,  MADAR DAVID

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

Abstract: Disclosed is an indole compound of formula (I) where the substituents are as disclosed in the specification. Examples of compounds are: 7-(3-((4-(4-Acetylpiperazin-1-yl)phenoxy)methyl)-1,5-dimethyl-1H-pyrazol-4-yl)-3-(3-(1-naphthyloxy)propyl)-1-yridine-3-ylmethyl)-1H-indole-2-carboxylic acid; 7-(2-((4-(4-carboxyphenyl)piperazin-1-yl)methyl)phenyl)-3-(3-(1-naphthyloxy)propyl)-1H-indole-2-carboxylic acid; 3-(3-(1-naphthyloxy)propyl)-7-(2-piperazin-1-ylpyridin-3-yl)-1H-indole-2-carboxylic acid; and 7-(2-(1H-imidazol-1-yl)-4-methylpyridin-3-yl)-3-(3-(1-naphthyloxy)propyl)-1-(yridin-3-ylmethyl)-1H-indole-2-carboxylic acid. Also disclosed is a composition comprising a compound of formula (I).

公开(公告)号：PE13852012A1

公开(公告)日：2012-11-09

申请号：PE0007592012

申请日：2010-06-01

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 ,  PARK CHEOLMIN ,  PETROS ANDREW M ,  SONG XIAOHONG ,  SOUERS ANDRES J ,  SULLIVAN GERAR M ,  TAO ZHI-FU ,  WANG GARY T ,  WANG LE ,  WENDT MICHAEL D ,  HANSEN TODD M ,  PARK CHANG H ,  WANG XILU

IPC: 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 ,  C07D405/12 ,  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: SE REFIERE A COMPUESTOS DERIVADOS DE SULFONAMIDA DE FORMULA (I) DONDE A2, B1, D1 Y E1 SON CADA UNO R1, OR1, SR1, S(O)R1, ENTRE OTROS, DONDE R1 ES R2, R3, R4 O R5, EN DONDE R2 ES FENILO OPCIONALMENTE FUSIONADO CON ARENO, HETEROARENO, ENTRE OTROS; R3 ES HETEROARILO OPCIONALMENTE FUSIONADO CON BENCENO, HETEROARENO, ENTRE OTROS; R4 ES CICLOALQUILO, CICLOALQUENILO, HETEROCICLOALQUILO, ENTRE OTROS; R5 ES ALQUILO, ALQUENILO O ALQUINILO; Y1 ES H, CN, NO2, F, CF3, OCF3, ENTRE OTROS; Z1 ES R26 O R27, EN DONDE R26 ES FENILO OPCIONALMENTE FUSIONADO CON ARENO O HETEROARENO; R27 ES HETEROARENO OPCIONALMENTE FUSIONADO CON ARENO O HETEROARENO. SON COMPUESTOS PREFERIDOS: 4-(4-((4'-CLORO-1,1'-BIFENIL-2-IL)METIL)PIPERAZIN-1-IL)-N-((3-NITRO-4-((TETRAHIDRO-2H-PIRAN-4-ILMETIL)AMINO)FENIL)SULFONIL)-2-FENOXIBENZAMIDA; 4-(4-((4'-CLORO-1,1'-BIFENIL-2-IL)METIL)PIPERAZIN-1-IL)-2-FENOXI-N-((4-((TETRAHIDRO-2H-PIRAN-4-ILMETIL)AMINO)FENIL)SULFONIL)BENZAMIDA; 2-(BENCILOXI)-4-(4-((4'-CLORO-1,1'-BIFENIL-2-IL)METIL)PIPERAZIN-1-IL)-N-((3-NITRO-4-((TETRAHIDRO-2H-PIRAN-4-ILMETIL)AMINO)FENIL)SULFONIL)BENZAMIDA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA ACTIVIDAD DE LAS PROTEINAS ANTI-APOPTOTICAS Bcl-2 SIENDO UTILES EN EL TRATAMIENTO DE CANCER DE VEJIGA, LEUCEMIA LINFOCITICA CRONICA, MELANOMA