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41.
公开(公告)号:PE20120305A1
公开(公告)日:2012-04-09
申请号:PE2011001249
申请日:2009-12-17
Applicant: ABBOTT LAB , GENENTECH INC , INST MEDICAL W & E HALL
Inventor: BAELL JONATHON BAYLDON , BUI CHIHN THIEN , COLMAN PETER , DUDLEY DANNETE A , FAIRBROTHER WAYNE J , FLYGARE JOHN A , LASSENE GUILLAUME LAURENT , NIKOLAKOPOULOS GEORGE , RYE CARL STEVEN , SLEEBS BRAD EDMUND , SMITH BRIAN JOHN , WATSON KEITH GEOFFREY , ELMORE STEVEN W , PETROS ANDREW M , SOUERS ANDREW J , NDUBAKU CHUDI
IPC: C07D487/04 , A61K31/502 , A61P35/00
Abstract: REFERIDA A UN COMPUESTO HETEROCICLICO DE FORMULA (I), DONDE R1 ES ALQUILO C1-C6, ALQUENILO C2-C6, HALOGENO, ENTRE OTROS; n ES UN ENTERO DE 0 A 2; X1 ES CH2, O, S, SO, ENTRE OTROS; X2a, X2b Y X2c SON CH, CR2 O N; R2 ES CN, HALOGENO, NO2, ENTRE OTROS; A ES UN GRUPO (1), (2), (3), ENTRE OTROS; R3 ES CN, NO2, HALOGENO, ENTRE OTROS; B ES UN GRUPO (a) O (b); X3 ES NH, N(ALQUILO C1-C3), S; R4a ES ALQUILO C1-C4, ALQUINILO C2-C4, HALOGENO, ENTRE OTROS; R4b ES HALOGENO, NO2, CN, ENTRE OTROS; L ES ALQUILENO C1-C6, ALQUENILENO C2-C6, NH, S, ENTRE OTROS; E ES H, HALOGENO, FENILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: ACIDO 6-(4-(BENZO[d]TIAZOL-2-ILCARBAMOIL)-1-METIL-1,2,3,4-TETRAHIDROQUINOXALIN-6-IL)PICOLINICO, ACIDO 6-(1-(BENZO[d]TIAZOL-2-ILCARBAMOIL)-1,2,3,4-TETRAHIDROQUINOLIN-7-IL)-3-(2-FENOXIETOXI)PICOLINICO, ACIDO 6-(1-(BENZO[d]TIAZOL-2-ILCARBAMOIL)-1,2,3,4-TETRAHIDROQUINOLIN-7-IL)-3-(2-(3-(DIMETILAMINO)FENOXI)ETOXI)PICOLINICO, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS INHIBEN LA ACTIVIDAD DE LAS PROTEINAS Bcl-2 Y Bcl-Xl Y SON UTILES EN EL TRATAMIENTO DEL CANCER, TROMBOCITEMIA, ENTRE OTRAS
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42.
公开(公告)号:PE03052012A1
公开(公告)日:2012-04-09
申请号:PE0012492011
申请日:2009-12-17
Applicant: ABBOTT LAB , GENENTECH INC , INST MEDICAL W & E HALL
Inventor: BAELL JONATHON BAYLDON , BUI CHIHN THIEN , COLMAN PETER , DUDLEY DANNETE A , FAIRBROTHER WAYNE J , FLYGARE JOHN A , LASSENE GUILLAUME LAURENT , NIKOLAKOPOULOS GEORGE , RYE CARL STEVEN , SLEEBS BRAD EDMUND , SMITH BRIAN JOHN , WATSON KEITH GEOFFREY , ELMORE STEVEN W , PETROS ANDREW M , SOUERS ANDREW J , NDUBAKU CHUDI
IPC: C07D487/04 , A61K31/502 , A61P35/00
CPC classification number: C07D417/14 , C07D417/12 , C07D487/04
Abstract: REFERIDA A UN COMPUESTO HETEROCICLICO DE FORMULA (I), DONDE R1 ES ALQUILO C1-C6, ALQUENILO C2-C6, HALOGENO, ENTRE OTROS; n ES UN ENTERO DE 0 A 2; X1 ES CH2, O, S, SO, ENTRE OTROS; X2a, X2b Y X2c SON CH, CR2 O N; R2 ES CN, HALOGENO, NO2, ENTRE OTROS; A ES UN GRUPO (1), (2), (3), ENTRE OTROS; R3 ES CN, NO2, HALOGENO, ENTRE OTROS; B ES UN GRUPO (a) O (b); X3 ES NH, N(ALQUILO C1-C3), S; R4a ES ALQUILO C1-C4, ALQUINILO C2-C4, HALOGENO, ENTRE OTROS; R4b ES HALOGENO, NO2, CN, ENTRE OTROS; L ES ALQUILENO C1-C6, ALQUENILENO C2-C6, NH, S, ENTRE OTROS; E ES H, HALOGENO, FENILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: ACIDO 6-(4-(BENZO[d]TIAZOL-2-ILCARBAMOIL)-1-METIL-1,2,3,4-TETRAHIDROQUINOXALIN-6-IL)PICOLINICO, ACIDO 6-(1-(BENZO[d]TIAZOL-2-ILCARBAMOIL)-1,2,3,4-TETRAHIDROQUINOLIN-7-IL)-3-(2-FENOXIETOXI)PICOLINICO, ACIDO 6-(1-(BENZO[d]TIAZOL-2-ILCARBAMOIL)-1,2,3,4-TETRAHIDROQUINOLIN-7-IL)-3-(2-(3-(DIMETILAMINO)FENOXI)ETOXI)PICOLINICO, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS INHIBEN LA ACTIVIDAD DE LAS PROTEINAS Bcl-2 Y Bcl-Xl Y SON UTILES EN EL TRATAMIENTO DEL CANCER, TROMBOCITEMIA, ENTRE OTRAS
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公开(公告)号:ECSP11011213A
公开(公告)日:2011-09-30
申请号:ECSP11011213
申请日:2011-07-18
Applicant: GENENTECH INC , INST MEDICAL W & E HALL , ABBOTT LAB
Inventor: DUDLEY DANETTE ANDREA , HASVOLD LISA A , WANG XILU , ELMORE STEVEN W , SOUERS ANDREW J , TAO ZHI-FU , PETROS ANDREW M , BAELL JONATHAN BAYLDON , BUI CHINH THIEN , COLMAN PETER , FAIRBROTHER WAYNE J , FLYGARE JOHN A , LESSENE GUILLAUME LAURENT , NDUBAKU CHUDI , NIKOLAKOPOULOS S GEORGE , SLEEBS BRAD EDMUND , SMITH BRIAN JOHN , WATSON KEITH GEOFFREY , CZABOTAR PETER , DESHAYES KURT
IPC: A01N43/00
Abstract: En un aspecto, la presente invención proporciona un compuesto de la fórmula I; en la que la variable X1a, X1b, X1c, X1d, Q, A, R1, B, L, E y los subíndices m y n tienen los significados descritos en la presente. En otro aspecto, la presente invención proporciona composiciones farmacéuticas que comprenden compuestos de la fórmula I, así como métodos de uso de compuestos de la fórmula I para el tratamiento de enfermedades y condiciones (por ejemplo, cáncer, trombocitemia, etc.) caracterizadas por expresión o sobreexpresión de proteínas antiapoptóticas Bcl-2, por ejemplo, de proteínas antiapoptóticas Bcl-xL.
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44.
公开(公告)号:ECSP11011173A
公开(公告)日:2011-08-31
申请号:ECSP11011173
申请日:2011-07-04
Applicant: ABBOTT LAB
Inventor: DOHERTY GEORGE ANDREW , 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 , DAI YUJIA , DING HONG , HEXAMER LAURA , MCCLELLAN WILLIAM J , PARK CHANG H , PETROS ANDREW M
IPC: A61P35/00 , A61K31/496 , C07D403/12
Abstract: Compuestos que inhiben la actividad de proteínas anti-apoptóticas Bcl-2, composiciones que contienen a dichos compuestos y métodos de tratamiento de enfermedades durante cuyo transcurso hay expresión de la proteína anti-apoptótica Bcl-2.
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公开(公告)号:UY32680A
公开(公告)日:2011-02-28
申请号:UY32680
申请日:2010-06-02
Applicant: ABBOTT LAB
Inventor: WANG GARY T , MANTEI ROBERT A , MILAN BRUNCKO , HONG DING , DOHERTY GEORGE A , ELMORE STEVEN W , LISA HASVOLD , LAURA HEXAMER , KUNZER AARON R , MCCLELLAN WILLIAM J , PARK CHANG H , PARK CHEOL-MIN , PETROS ANDREW M , XIAOHONG SONG , SOUERS ANDREW J , SULLIVAN GERARD M , TAO ZHI-FU , XILU WANG , WENDT MICHAEL D , HANSEN TODD M , LE WANG
IPC: A61P35/00 , C07D205/00 , C07D205/08 , C07D207/04 , C07D209/04 , C07D215/00 , C07D217/00 , C07D231/54 , C07D235/04 , C07D241/10 , C07D295/00 , C07D309/04 , C07D333/02 , C07D499/00
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.
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公开(公告)号:CA2427658C
公开(公告)日:2011-01-04
申请号:CA2427658
申请日:2001-11-15
Applicant: ABBOTT LAB
Inventor: FESIK STEPHEN W , PETROS ANDREW M , YOON HOSUP , NETTESHEIM DAVID G
IPC: C07K14/47 , G01N33/50 , G01N33/15 , G01N33/566
Abstract: Mutant peptides derived from wild-type human Bcl-2 are disclosed. Assays to identify substances which block the ability of Bcl-2 to inhibit apoptosis also are disclosed.
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公开(公告)号:DK1318978T3
公开(公告)日:2006-06-06
申请号:DK01971244
申请日:2001-09-20
Applicant: ABBOTT LAB
Inventor: WANG XILU , AUGERI DAVID J , DICKMAN DANIEL A , DINGES JUERGEN , FESIK STEPHEN W , ROSENBERG SAUL H , SHEN WANG , THOMAS SHEELA A , WENDT MICHAEL D , MCCLELLAN WILLIAM , OOST THORSTEN , BRUNCKO MILAN , BAUMEISTER STEVEN A , DING HONG , HAJDUK PHILIP J , KUNZER AARON R , NETTESHEIM DAVID G , PETROS ANDREW M
IPC: C07C311/51 , 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 , 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 , C07D295/14 , 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
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公开(公告)号:AT317382T
公开(公告)日:2006-02-15
申请号:AT01971244
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
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公开(公告)号:CA2423103A1
公开(公告)日:2002-03-28
申请号:CA2423103
申请日:2001-09-20
Applicant: ABBOTT LAB
Inventor: THOMAS SHEELA A , PETROS ANDREW M , DING HONG , BAUMEISTER STEVEN A , AUGERI DAVID J , DICKMAN DANIEL A , MCCLELLAN WILLIAM , SHEN WANG , FESIK STEPHEN W , WENDT MICHAEL D , WANG XILU , BRUNCKO MILAN , NETTESHEIM DAVID G , KUNZER AARON R , DINGES JURGEN , ROSENBERG SAUL H , HAJDUK PHILIP J , OOST THORSTEN
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 , C07D295/14 , C07D317/58
Abstract: N-Benzoyl arylsulfonamides having the formula (I) are BCL-Xl inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-Xl inhibiting compositions and methods of promoting apoptosis in a mammal.
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公开(公告)号:BRPI0110101B1
公开(公告)日:2016-08-23
申请号:BR0110101
申请日:2001-09-20
Applicant: ABBOTT LAB , ABBVIE INC
Inventor: KUNZER AARON R , PETROS ANDREW M , DICKMAN DANIEL A , NETTESHEIM DAVID G , AUGERI DAVID J , DING HONG , DINGES JURGEN , WENDT MICHAEL D , BRUNCKO MILAN , HAJDUK PHILIP J , ROSENBERG SAUL H , THOMAS SHEELA A , FESIK STEPHEN W , BAUMEISTER STEVEN A , OOST THORSTEN , SHEN WANG , MCCLELLAN WILLIAM , WANG XILU
IPC: C07C311/00 , 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
Abstract: "n-acil-sulfonamidas promotoras de apoptose". descreve-se n-benzoil-aril-sulfonamidas que têm a fórmula (i), são inibidores de bcl-x1, e úteis para promover apoptose. descreve-se também composições e métodos inibidores de bcl-xl para promover apoptose em um mamífero.
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