公开(公告)号：PE05042002A1

公开(公告)日：2002-06-20

申请号：PE0009402001

申请日：2001-09-19

Applicant: ABBOTT LAB

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

IPC: C07C311/00 ,  C07C311/51 ,  C07C317/28 ,  C07C323/12 ,  C07C323/17 ,  C07C323/25 ,  C07C323/30 ,  C07C323/37 ,  C07C323/58 ,  C07C323/60 ,  C07D203/10 ,  C07D205/12 ,  C07D207/24 ,  C07D207/40 ,  C07D207/404 ,  C07D209/08 ,  C07D209/96 ,  C07D211/44 ,  C07D211/70 ,  C07D211/74 ,  C07D213/61 ,  C07D213/70 ,  C07D213/71 ,  C07D215/14 ,  C07D215/22 ,  C07D215/227 ,  C07D215/48 ,  C07D217/04 ,  C07D221/20 ,  C07D231/12 ,  C07D235/08 ,  C07D235/26 ,  C07D241/16 ,  C07D249/04 ,  C07D263/56 ,  C07D263/58 ,  C07D277/62 ,  C07D277/64 ,  C07D295/13 ,  C07D295/155 ,  C07D295/185 ,  C07D295/205 ,  C07D295/215 ,  C07D295/26 ,  C07D307/14 ,  C07D317/54 ,  C07D333/28 ,  C07D333/68 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D417/12 ,  C07D451/02

CPC classification number: C07D207/404 ,  C07C311/51 ,  C07C317/28 ,  C07C323/12 ,  C07C323/17 ,  C07C323/25 ,  C07C323/30 ,  C07C323/37 ,  C07C323/58 ,  C07C323/60 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2601/18 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2602/28 ,  C07C2602/42 ,  C07C2602/44 ,  C07C2603/74 ,  C07D203/10 ,  C07D205/12 ,  C07D207/24 ,  C07D209/08 ,  C07D209/96 ,  C07D211/44 ,  C07D211/70 ,  C07D211/74 ,  C07D213/61 ,  C07D213/70 ,  C07D213/71 ,  C07D215/14 ,  C07D215/227 ,  C07D215/48 ,  C07D217/04 ,  C07D221/20 ,  C07D231/12 ,  C07D235/08 ,  C07D235/26 ,  C07D241/16 ,  C07D249/04 ,  C07D263/56 ,  C07D263/58 ,  C07D277/62 ,  C07D277/64 ,  C07D295/13 ,  C07D295/155 ,  C07D295/185 ,  C07D295/205 ,  C07D295/215 ,  C07D295/26 ,  C07D307/14 ,  C07D317/54 ,  C07D333/28 ,  C07D333/68 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D417/12 ,  C07D451/02

Abstract: SE REFIERE A N-ACILSULFONAMIDAS DE FORMULA I DONDE A ES FENILO, ANILLO CARBOCICLICO AROMATICO DE 5-6 MIEMBROS; R1 ES ALQUILO, HALOALQUILO, NITRO, NR5R6; R2 Y R3 SON H, ALQUENILO, ALCOXI, ALQUILO, ALQUILSULFANILO, ALQUINILO, ARILO, ARILALCOXI, ENTRE OTROS; R4 ES ARILO, ARILALQUENILO, ARILALCOXI, ARILOXI, ARILOXIALCOXI, ENTRE OTROS; R5 Y R6 SON HIDROGENO, ALQUENILO, ALCOXIALQUILO, ENTRE OTROS; R5 Y R6 JUNTO A N FORMAN UN IMIDAZOLILO, MORFOLINILO, PIPERAZINILO, PIPERIDINILO, ENTRE OTROS; R15 ES H, ALQUILO, HALO. SON COMPUESTOS PREFERIDOS 4-((2,2-DIMETILCICLOPENTIL)AMINO)-N-((4´FLUORO(1,1'-BIFENIL)-4-IL)CARBONIL)-3-NITROBENCENSULFONAMIDA, 4-(CICLOHEXILAMINO)-N-((4´FLUORO(1,1'-BIFENIL)-4-IL)CARBONIL)-3-NITROBENCENSULFONAMIDA, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. LOS COMPUESTOS MENCIONADOS SON PROMOTORES DE LA APOPTOSIS Y SON UTILES PARA EL TRATAMIENTO DEL CANCER

公开(公告)号：NO20014691A

公开(公告)日：2001-12-10

申请号：NO20014691

申请日：2001-09-27

Applicant: ABBOTT LAB

Inventor： FESIK STEPHEN W ,  AUGERI DAVID J

IPC: C12N15/09 ,  C07B59/00 ,  C07C51/09 ,  C07C51/353 ,  C07C59/185 ,  C07C229/08 ,  C07K1/107 ,  C07K1/13 ,  C07K14/47 ,  C12N9/64 ,  C12P13/04 ,  C12P13/06 ,  C12P13/08 ,  C12P21/00 ,  C12P21/02

CPC classification number: C12N9/6491 ,  C07B59/001 ,  C07B2200/05 ,  C07B2200/07 ,  C07C229/08 ,  C07K1/1075 ,  C07K1/1077 ,  C07K1/13 ,  C12P13/04 ,  C12P13/06 ,  C12P13/08 ,  C12P21/02

Abstract: Site-specific isotopically-labeled valine, leucine, and isoleucine and biosynthetic precursors for these amino acids are provided. The amino acids are labeled with C or C at the methyl group carbon atom(s) most remote from the carboxyl group. Also disclosed are the biochemical precursors of these labeled amino acids, 2-keto-4-( C)butyric acid and 2-keto-3-( C-methyl)-4-( C)-butyric acid in which n, at each occurrence, is 13 or 14. Also disclosed are proteins, protein fragments, and polypeptides containing these site-specifically isotopically labeled amino acids, and methods for preparing the biochemical precursors, the amino acids, and the proteins, protein fragments, and polypeptides.

公开(公告)号：GR3036454T3

公开(公告)日：2001-11-30

申请号：GR20010401304

申请日：2001-08-27

Applicant: ABBOTT LAB

Inventor： FESIK STEPHEN W ,  HAJDUK PHILIP J ,  OLEJNICZAK EDWARD T

IPC: G01R33/465 ,  G01N33/15 ,  G01N33/50 ,  G01N33/53 ,  G01N33/543 ,  G01N33/68 ,  G01N33/94 ,  G01R33/32 ,  G01R33/46 ,  G01N33/48 ,  G01N24/08

公开(公告)号：NZ337126A

公开(公告)日：2001-05-25

申请号：NZ33712698

申请日：1998-04-17

Applicant: ABBOTT LAB

Inventor： FESIK STEPHEN W ,  HAJDUK PHILIP J ,  OLEJNICZAK EDWARD T

IPC: G01R33/32 ,  A61K45/00 ,  C07K14/705 ,  C12N9/00 ,  C12Q1/68 ,  G01N24/08 ,  G01N33/15 ,  G01N33/50 ,  G01N33/53 ,  G01N33/68 ,  G01R33/44

Abstract: A process for identifying compounds which bind to a specific target molecule. The process comprises the steps of: a) generating a first T2- or diffusion-filtered proton spectrum of one or a mixture of chemical compounds; b) exposing one or a mixture of chemical compounds to the target molecule; c) generating a second T2- or diffusion-filtered proton spectrum of one or a mixture of chemical compounds that has been exposed the target molecule in step (b); and d) comparing said first and second T2- or diffusion-filtered proton spectra to determine differences between said first and said second spectra, the differences identifying the presence of one or more compounds that are ligands which have bound to the target molecule.

公开(公告)号：BG103856A

公开(公告)日：2000-07-31

申请号：BG10385699

申请日：1999-11-04

Applicant: ABBOTT LAB

Inventor： FESIK STEPHEN W ,  HAJDUK PHILIP J ,  OLEJNICZAK EDWARD T

IPC: G01R33/32 ,  A61K45/00 ,  C07K14/705 ,  C12N9/00 ,  C12Q1/68 ,  G01N24/08 ,  G01N33/15 ,  G01N33/50 ,  G01N33/53 ,  G01N33/68 ,  G01R33/44

Abstract: The invention relates to a method for the identification of compounds which are bound to a specific molecule target. It includes the following stages: (a) production of first T2- or diffusion filtered proton spectrum of one or of a mixture of chemical compounds; (b) subjection of one or of a mixture of chemical compounds to the effect of a target molecule; (c) production of a second T2- or diffusion filtered proton spectrum of one or of a mixture of chemical compounds which are subjected to the effect of a molecule target in stage (b), and (d) comparison of the first and the second T2- or the diffusion filtered proton spectra in order to determine the differences between the first and the second spectrum, the differences identifying the presence of one or more compounds which are ligands bound to the target molecule. 29 claims

公开(公告)号：TR9902167T2

公开(公告)日：2000-07-21

申请号：TR9902167

申请日：1998-04-17

Applicant: ABBOTT LAB

Inventor： FESIK STEPHEN W ,  HAJDUK PHILIP J ,  OLEJNICZAK EDWARD T

IPC: G01R33/32 ,  A61K45/00 ,  C07K14/705 ,  C12N9/00 ,  C12Q1/68 ,  G01N24/08 ,  G01N33/15 ,  G01N33/50 ,  G01N33/53 ,  G01N33/68 ,  G01R33/44

CPC classification number: G01R33/44 ,  G01N24/08 ,  G01N33/6803 ,  G01N2500/20 ,  Y10S435/81

公开(公告)号：TR199902167T2

公开(公告)日：2000-07-21

申请号：TR9902167

申请日：1998-04-17

Applicant: ABBOTT LAB

Inventor： FESIK STEPHEN W ,  HAJDUK PHILIP J ,  OLEJNICZAK EDWARD T

IPC: G01R33/32 ,  A61K45/00 ,  C07K14/705 ,  C12N9/00 ,  C12Q1/68 ,  G01N24/08 ,  G01N33/15 ,  G01N33/50 ,  G01N33/53 ,  G01N33/68 ,  G01R33/44

Abstract: The present invention provides a process for identifying compounds which bind to a specific target molecule. The process comprises the steps of: a) generating a first T2- or diffusion-filtered proton spectrum of one or a mixture of chemical compounds; b) exposing one or a mixture of chemical compounds to the target molecule; c) generating a second T2- or diffusion-filtered proton spectrum of one or a mixture of chemical compounds that has been exposed the target molecule in step (b); and d) comparing said first and second T2- or diffusion-filtered proton spectra to determine differences between said first and said second spectra, the differences identifying the presence of one or more compounds that are ligands which have bound to the target molecule.

公开(公告)号：ZA9802919B

公开(公告)日：1998-10-12

申请号：ZA9802919

申请日：1998-04-06

Applicant: ABBOTT LAB

Inventor： FESIK STEPHEN W ,  OLEJNICZAK EDWARD T ,  HAJDUK PHILIP J

IPC: G01R33/32 ,  A61K45/00 ,  C07K14/705 ,  C12N9/00 ,  C12Q1/68 ,  G01N24/08 ,  G01N33/15 ,  G01N33/50 ,  G01N33/53 ,  G01N33/68 ,  G01R33/44 ,  G01N ,  A61K

CPC classification number: G01R33/44 ,  G01N24/08 ,  G01N33/6803 ,  G01N2500/20 ,  Y10S435/81

公开(公告)号：CA2653959C

公开(公告)日：2012-03-13

申请号：CA2653959

申请日：1996-11-13

Applicant: ABBOTT LAB

Inventor： FESIK STEPHEN W ,  HAJDUK PHILIP J ,  OLEJNICZAK EDWARD T

IPC: G01N24/08 ,  C40B30/04 ,  G01N33/53 ,  G01N33/68 ,  G01N33/94 ,  G01R33/46 ,  G06F19/16

Abstract: The present invention provides a process of designing compounds which bind to a specific target molecule. The process includes the steps of a) identifying a first ligand to the target molecule using two-dimensional 15N/1H NMR correlation spectroscopy; b) identifying a second ligand to the target molecule using two-dimensional 15N/1H NMR correlation spectroscopy; c) forming a ternary complex by binding the first and second ligands to the target molecule; d) determining the three-dimensional structure of the ternary complex and thus the spatial orientation of the first and second ligands on the target molecule; and e) linking the first and second ligands to form the drug, wherein the spatial orientation of step (d) is maintained.

公开(公告)号：CA2423103C

公开(公告)日：2010-08-24

申请号：CA2423103

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: 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 ,  C07D317/58 ,  C07D333/28 ,  C07D333/68 ,  C07D333/70 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D405/06 ,  C07D417/12 ,  C07D451/02 ,  C07D491/107

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.