公开(公告)号：WO0011191A2

公开(公告)日：2000-03-02

申请号：PCT/US9918543

申请日：1999-08-13

Applicant: BASF AG ,  MEDICAL RES COUNCIL

Inventor： ALLEN HAMISH JOHN ,  DIXON RICHARD WOODWARD ,  KAMENS JOANNE SARA ,  WICKRAMASINGHE DINELI ,  XU YAJUN ,  BELICH MONICA POLIDORO ,  JOHNSTON LELAND HERRIES ,  LEY STEVEN CHARLES ,  SALMERON ANDRES

IPC: C12N15/09 ,  A61K31/00 ,  A61K31/4439 ,  A61K31/4706 ,  A61K31/4745 ,  A61K38/00 ,  A61K39/395 ,  A61K45/00 ,  A61P1/00 ,  A61P3/10 ,  A61P5/48 ,  A61P17/06 ,  A61P29/00 ,  C07K14/82 ,  C07K16/40 ,  C12N1/15 ,  C12N1/19 ,  C12N1/21 ,  C12N5/10 ,  C12N9/12 ,  C12N15/54 ,  C12Q1/02 ,  G01N33/68 ,  A61K31/44 ,  A61K31/47 ,  A61K38/45 ,  G01N33/50

CPC classification number: G01N33/6872 ,  A61K31/00 ,  A61K31/4439 ,  A61K31/4706 ,  A61K31/4745 ,  A61K38/00 ,  C07K14/82 ,  C12N9/1205

Abstract: It is shown that TPL-2 is responsible for phosphorylation of p105 and its resultant proteolysis, which leads to p50 Rel translocation to the nucleus. Accordingly, the invention provides TPL-2 as a specific regulator of the activation of NF kappa B, and thus as a modulator of inflammatory responses in which p105 is involved, and as a target for the development of compounds capable of influencing NF kappa B activation.

Abstract translation: 这表明TPL-2负责p105的磷酸化和其导致的p50 Rel易位至细胞核的蛋白水解。 因此，本发明提供TPL-2作为NFκB活化的特异性调节剂，并因此作为涉及p105的炎症反应的调节剂，并且作为开发能够影响NFκB活化的化合物的靶标 。

公开(公告)号：TR200103840T2

公开(公告)日：2002-06-21

申请号：TR200103840

申请日：1999-08-13

Applicant: BASF AG ,  MEDICAL RES COUNCIL

Inventor： ALLEN HAMISH JOHN ,  DIXON RICHARD WOODWARD ,  KAMENS JOANNE SARA ,  WICKRAMASINGHE DINELI ,  XU YAJUN ,  BELICH MONICA POLIDORO ,  JOHNSTON LELAND HERRIES ,  LEY STEVEN CHARLES ,  SALMERON ANDRES

IPC: C12N15/09 ,  A61K31/00 ,  A61K31/4439 ,  A61K31/4706 ,  A61K31/4745 ,  A61K38/00 ,  A61K39/395 ,  A61K45/00 ,  A61P1/00 ,  A61P3/10 ,  A61P5/48 ,  A61P17/06 ,  A61P29/00 ,  C07K14/82 ,  C07K16/40 ,  C12N1/15 ,  C12N1/19 ,  C12N1/21 ,  C12N5/10 ,  C12N9/12 ,  C12N15/54 ,  C12Q1/02 ,  G01N33/68

Abstract: It is shown that TPL-2 is responsible for phosphorylation of p105 and its resultant proteolysis, which leads to p50 Rel translocation to the nucleus. Accordingly, the invention provides TPL-2 as a specific regulator of the activation of NFkappaB, and thus as a modulator of inflammatory responses in which p105 is involved, and as a target for the development of compounds capable of influencing NFkappaB activation.

公开(公告)号：SK2242001A3

公开(公告)日：2001-10-08

申请号：SK2242001

申请日：1999-08-13

Applicant: BASF AG ,  MEDICAL RES COUNCIL

Inventor： ALLEN HAMISH JOHN ,  DIXON RICHARD WOODWARD ,  KAMENS JOANNE SARA ,  WICKRAMASINGHE DINELI ,  XU YAJUN ,  BELICH MONICA POLIDORO ,  JOHNSTON LELAND HERRIES ,  LEY STEVEN CHARLES ,  SALMERON ANDRES

IPC: C12N15/09 ,  A61K31/00 ,  A61K31/4439 ,  A61K31/4706 ,  A61K31/4745 ,  A61K38/00 ,  A61K39/395 ,  A61K45/00 ,  A61P1/00 ,  A61P3/10 ,  A61P5/48 ,  A61P17/06 ,  A61P29/00 ,  C07K14/82 ,  C07K16/40 ,  C12N1/15 ,  C12N1/19 ,  C12N1/21 ,  C12N5/10 ,  C12N9/12 ,  C12N15/54 ,  C12Q1/02 ,  G01N33/68 ,  A61K38/45 ,  G01N33/50 ,  A61K31/47 ,  A61K31/44

Abstract: It is shown that TPL-2 is responsible for phosphorylation of p105 and its resultant proteolysis, which leads to p50 Rel translocation to the nucleus. Accordingly, the invention provides TPL-2 as a specific regulator of the activation of NFkappaB, and thus as a modulator of inflammatory responses in which p105 is involved, and as a target for the development of compounds capable of influencing NFkappaB activation.

公开(公告)号：AU9691198A

公开(公告)日：1999-04-27

申请号：AU9691198

申请日：1998-10-06

Applicant: BASF AG

Inventor： ARNOLD LEE D ,  XU YAJUN ,  BARLOZZARI TERESA

IPC: A61K31/416 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4439 ,  A61P1/04 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P17/02 ,  A61P17/06 ,  A61P19/02 ,  A61P19/08 ,  A61P27/00 ,  A61P35/00 ,  A61P43/00 ,  C07D231/54 ,  C07D231/56 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04 ,  A61K31/415 ,  A61K31/44

Abstract: Chemical compounds that are derivatives of indeno[1,2-c]-, naphtho[1,2-c]- and benzo[6,7]cyclohepta[1,2-c]pyrazole are inhibitors of tyrosine kinase activity. Several of the tyrosine kinases, whose activity is inhibited by these chemical compounds, are involved in hyperproliferative, angiogenic or in vascular hyperpermeability processes. Thus, these chemical compounds can ameliorate disease states where tumor formation, metastasis, angiogenesis, vascular hyperpermeability or endothelial cell proliferation is a factor.

公开(公告)号：CA2304466A1

公开(公告)日：1999-04-15

申请号：CA2304466

申请日：1998-10-06

Applicant: BASF AG

Inventor： HOCKLEY MICHAEL ,  ARNOLD LEE D ,  TURNER ALLYSON ,  BARLOZZARI TERESA ,  RAFFERTY PAUL ,  XU YAJUN

IPC: C07D231/54 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4427 ,  A61K31/4439 ,  A61P1/02 ,  A61P1/04 ,  A61P9/00 ,  A61P9/10 ,  A61P15/00 ,  A61P17/06 ,  A61P19/00 ,  A61P19/02 ,  A61P27/02 ,  A61P35/00 ,  A61P43/00 ,  C07D401/04 ,  C07D403/04

Abstract: Chemical compounds that are derivatives of indeno1,2-c!pyrazole are inhibitors of tyrosine kinase activity. Several of the tyrosine kinases, whose activity is inhibited by these chemical compounds, are involved in angiogenic processes. Thus, these chemical compounds can ameliorate disease states where angiogenesis or endothelial cell proliferation is a factor. Compounds of this invention also inhibit the induction of vascular hyperpermeability and the associated formation of edema, ascites, and exudates.

公开(公告)号：ZA200102200B

公开(公告)日：2002-05-23

申请号：ZA200102200

申请日：2001-03-16

Applicant: BASF AG ,  MEDICAL RES COUNCIL

Inventor： JOHN ALLEN HAMISH ,  WOODWARD DIXON RICHARD ,  SARA KAMENS JOANNE ,  WICKRAMASINGHE DINELI ,  XU YAJUN ,  POLIDORO BELICH MONICA ,  HERRIES JOHNSON LELAND ,  CHARLES LEY STEVEN ,  SALMERO ANDRES

IPC: A61K20060101 ,  A61P20060101 ,  C07K20060101 ,  C12N20060101 ,  G01N20060101 ,  C12N ,  A61K ,  A61P ,  C07K ,  G01N

公开(公告)号：CZ2001625A3

公开(公告)日：2002-02-13

申请号：CZ2001625

申请日：1999-08-13

Applicant: BASF AG ,  MEDICAL RES COUNCIL

Inventor： ALLEN HAMISH JOHN ,  DIXON RICHARD WOODWARD ,  KAMENS JOANNE SARA ,  WICKRAMASINGHE DINELLI ,  XU YAJUN ,  BELICH MONICA POLIDORO ,  JOHNSTON LELAND HERRIES ,  LEY STEVEN CHARLES ,  SALMERON ANDRES

IPC: C12N15/09 ,  A61K31/00 ,  A61K31/4439 ,  A61K31/4706 ,  A61K31/4745 ,  A61K38/00 ,  A61K39/395 ,  A61K45/00 ,  A61P1/00 ,  A61P3/10 ,  A61P5/48 ,  A61P17/06 ,  A61P29/00 ,  C07K14/82 ,  C07K16/40 ,  C12N1/15 ,  C12N1/19 ,  C12N1/21 ,  C12N5/10 ,  C12N9/12 ,  C12N15/54 ,  C12Q1/02 ,  G01N33/68 ,  A61K38/45 ,  G01N33/50 ,  A61K31/47 ,  A61K31/44

Abstract: It is shown that TPL-2 is responsible for phosphorylation of p105 and its resultant proteolysis, which leads to p50 Rel translocation to the nucleus. Accordingly, the invention provides TPL-2 as a specific regulator of the activation of NFkappaB, and thus as a modulator of inflammatory responses in which p105 is involved, and as a target for the development of compounds capable of influencing NFkappaB activation.

公开(公告)号：BG105345A

公开(公告)日：2001-12-31

申请号：BG10534501

申请日：2001-03-15

Applicant: BASF AG ,  MEDICAL RES COUNCIL

Inventor： ALLEN HAMISH J ,  DIXON RICHARD W ,  KAMENS JOANNE S ,  WICKRAMASINGHE DINELI ,  XU YAJUN ,  BELICH MONICA P ,  JOHNSTON LELAND H ,  LEY STEVEN C ,  SALMERON ANDRES

IPC: C12N15/09 ,  A61K31/00 ,  A61K31/4439 ,  A61K31/4706 ,  A61K31/4745 ,  A61K38/00 ,  A61K39/395 ,  A61K45/00 ,  A61P1/00 ,  A61P3/10 ,  A61P5/48 ,  A61P17/06 ,  A61P29/00 ,  C07K14/82 ,  C07K16/40 ,  C12N1/15 ,  C12N1/19 ,  C12N1/21 ,  C12N5/10 ,  C12N9/12 ,  C12N15/54 ,  C12Q1/02 ,  G01N33/68 ,  A61K38/45 ,  G01N33/50 ,  A61K31/47 ,  A61K31/44

Abstract: It is shown that TPL-2 is responsible for phosphorylation of p105 and its resultant proteolysis, which leads to p50 Rel translocation to the nucleus. Accordingly, the invention provides TPL-2 as a specific regulator of the activation of NFkB, and thus as a modulator of inflammatory responses in which p105 is involved, as a target for the development of compounds capable of influencing NFkB activation. 68 claims, 14 figures

公开(公告)号：BR9913070A

公开(公告)日：2001-05-08

申请号：BR9913070

申请日：1999-08-13

Applicant: BASF AG ,  MEDICAL RES COUNCIL

Inventor： ALLEN HAMISH JOHN ,  DIXON RICHARD WOODWARD ,  KAMENS JOANNE SARA ,  WICKRAMASINGHE DINELLI ,  XU YAJUN ,  BELICH MONICA POLIDORO ,  JOHNSTON LELAND HERRIES ,  LEY STEVEN CHARLES ,  SALMERON ANDRES

IPC: C12N15/09 ,  A61K31/00 ,  A61K31/4439 ,  A61K31/4706 ,  A61K31/4745 ,  A61K38/00 ,  A61K39/395 ,  A61K45/00 ,  A61P1/00 ,  A61P3/10 ,  A61P5/48 ,  A61P17/06 ,  A61P29/00 ,  C07K14/82 ,  C07K16/40 ,  C12N1/15 ,  C12N1/19 ,  C12N1/21 ,  C12N5/10 ,  C12N9/12 ,  C12N15/54 ,  C12Q1/02 ,  G01N33/68 ,  A61K38/45 ,  G01N33/50 ,  A61K31/47 ,  A61K31/44

Abstract: It is shown that TPL-2 is responsible for phosphorylation of p105 and its resultant proteolysis, which leads to p50 Rel translocation to the nucleus. Accordingly, the invention provides TPL-2 as a specific regulator of the activation of NFkappaB, and thus as a modulator of inflammatory responses in which p105 is involved, and as a target for the development of compounds capable of influencing NFkappaB activation.

公开(公告)号：AU9603998A

公开(公告)日：1999-04-27

申请号：AU9603998

申请日：1998-10-06

Applicant: BASF AG

Inventor： ARNOLD LEE D ,  XU YAJUN ,  BARLOZZARI TERESA ,  RAFFERTY PAUL ,  HOCKLEY MICHAEL ,  TURNER ALLYSON

IPC: A61K31/415