公开(公告)号：WO0127077A3

公开(公告)日：2002-05-23

申请号：PCT/US0027361

申请日：2000-10-04

Applicant: BASF AG ,  TAYLOR NEIL R ,  BORHANI DAVID ,  EPSTEIN DAVID ,  RUDOLPH JOHANNES ,  RITTER KURT ,  FUJIMORI TARO ,  ROBINSON SIMON ,  ECKSTEIN JENS ,  HAUPT ANDREAS ,  WALKER NIGEL ,  DIXON RICHARD W ,  CHOQUETTE DEBORAH ,  BLANCHARD JILL ,  KLUGE ARTHUR ,  PAL KOLLOL ,  BOCKOVICH NICHOLAS ,  COME JON ,  HEDIGER MARK

Inventor： TAYLOR NEIL R ,  BORHANI DAVID ,  EPSTEIN DAVID ,  RUDOLPH JOHANNES ,  RITTER KURT ,  FUJIMORI TARO ,  ROBINSON SIMON ,  ECKSTEIN JENS ,  HAUPT ANDREAS ,  WALKER NIGEL ,  DIXON RICHARD W ,  CHOQUETTE DEBORAH ,  BLANCHARD JILL ,  KLUGE ARTHUR ,  PAL KOLLOL ,  BOCKOVICH NICHOLAS ,  COME JON ,  HEDIGER MARK

IPC: A61K38/00 ,  C07C309/24 ,  C07D307/85 ,  C07F9/38 ,  C07K5/02 ,  C07K5/113 ,  C12N9/16 ,  A61K31/185 ,  A61K31/343 ,  A61K31/662

CPC classification number: C12N9/16 ,  A61K38/00 ,  C07C309/24 ,  C07D307/85 ,  C07F9/3882 ,  C07K5/0205 ,  C07K5/0207 ,  C07K5/021 ,  C07K5/1021 ,  C07K2299/00

Abstract: The present application relates to compounds of the fornula (VII), wherein the substituents R -R , X and Y are as defined in the description and to compounds of formula (VIII) or formula (IX) and when R is in the ortho position to X, R and R are taken together with the atoms to which are each attached to form an aromatic heterocyclic ring. The application further relates to polypeptides which comprise the ligand binding domain of Cdc25, crystalline forms of these polypeptides and the use of these crystalline forms to determine the three dimensional structure of the catalytic domain of Cdc25. The invention also relates to the use of the three dimensional structure of the Cdc25 catalytic domain in methods of designing and/or identifying potential inhibitors of Cdc25 activity, for example, compounds which inhibit the binding of a native substrate to the Cdc25 catalytic domain.

Abstract translation: 本申请涉及式（VII）的化合物，其中取代基R 1 -R 5，X和Y如说明书和式（VIII）或式（IX）的化合物所定义，并且当 R 3位于X的邻位，R 3和R 4与各自连接的原子一起形成芳族杂环。 本申请还涉及包含Cdc25的配体结合结构域，这些多肽的结晶形式以及这些结晶形式用于确定Cdc25催化结构域的三维结构的多肽。 本发明还涉及Cdc25催化结构域的三维结构在设计和/或鉴定Cdc25活性的潜在抑制剂的方法中的用途，例如抑制天然底物与Cdc25催化结构域结合的化合物。

公开(公告)号：WO0158956A3

公开(公告)日：2002-03-07

申请号：PCT/US0104170

申请日：2001-02-09

Applicant: BASF AG ,  GHAYUR TARIQ ,  DIXON RICHARD W ,  ROGUSKA MIKE ,  WHITE MICHAEL ,  LABKOVSKY BORIS ,  SALFELD JOCHEN ,  DUNCAN ALEXANDER ROBERT ,  BROCKLEHURST SIMON MARK ,  MANKOVICH JOHN ,  SHORROCK CELIA PATRICIA ,  THOMPSON JULIA ELIZABETH ,  LENNARD SIMON NICHOLAS

Inventor： GHAYUR TARIQ ,  DIXON RICHARD W ,  ROGUSKA MIKE ,  WHITE MICHAEL ,  LABKOVSKY BORIS ,  SALFELD JOCHEN ,  DUNCAN ALEXANDER ROBERT ,  BROCKLEHURST SIMON MARK ,  MANKOVICH JOHN ,  SHORROCK CELIA PATRICIA ,  THOMPSON JULIA ELIZABETH ,  LENNARD SIMON NICHOLAS

IPC: C12N15/02 ,  A61K39/395 ,  A61K45/00 ,  A61P1/04 ,  A61P3/10 ,  A61P5/14 ,  A61P7/00 ,  A61P7/02 ,  A61P7/06 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P15/00 ,  A61P17/00 ,  A61P17/06 ,  A61P17/14 ,  A61P19/02 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P29/00 ,  A61P31/00 ,  A61P31/04 ,  A61P31/12 ,  A61P33/00 ,  A61P35/00 ,  A61P37/00 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  A61P39/00 ,  A61P39/02 ,  C07K16/24 ,  C12N1/15 ,  C12N1/19 ,  C12N1/21 ,  C12N5/10 ,  C12P21/08 ,  A61K31/445 ,  A61K31/505 ,  A61K31/56 ,  A61K38/13 ,  A61K38/17 ,  A61P1/00 ,  A61P3/00 ,  A61P5/00 ,  A61P9/00 ,  A61P13/00 ,  A61P19/00 ,  A61P21/00 ,  A61P25/00 ,  C12N15/13 ,  C12N15/85

CPC classification number: C07K16/244 ,  A61K31/519 ,  A61K31/56 ,  A61K38/13 ,  A61K39/3955 ,  A61K2039/505 ,  C07K2317/21 ,  C07K2317/34 ,  C07K2317/565 ,  C07K2317/622 ,  C07K2317/76 ,  C07K2317/92 ,  A61K39/395 ,  A61K31/00

Abstract: Antibodies that bind human interleukin-18 (hIL-18) are provided, in particular antibodies that bind epitope(s) of human IL-18. The antibodies can be, for example, entirely human antibodies, recombinant antibodies, or monoclonal antibodies. Preferred antibodies have high affinity for hIL-18 and neutralize hIL-18 activity in vitro and in vivo . An antibody of the invention can be a full-length antibody or an antigen-binding portion thereof. Method of making and method of using the antibodies of the invention are also provided. The antibodies, or antibody portions, of the invention are useful for detecting hIL-18 and for inhibiting hIL-18 activity, e.g., in a human subject suffering from a disorder in which hIL-18 activity is detrimental.

Abstract translation: 提供了结合人白细胞介素-18（hIL-18）的抗体，特别是结合人IL-18表位的抗体。 抗体可以是例如完全是人抗体，重组抗体或单克隆抗体。 优选的抗体对hIL-18具有高亲和力，并且在体外和体内<！ - SIPO - >中和hIL-18活性。 本发明的抗体可以是全长抗体或其抗原结合部分。 还提供了制备方法和使用本发明抗体的方法。 本发明的抗体或抗体部分可用于检测hIL-18和抑制hIL-18活性，例如在患有hIL-18活性有害的病症的人类受试者中。

公开(公告)号：WO0116300A3

公开(公告)日：2002-05-30

申请号：PCT/US0023473

申请日：2000-08-25

Applicant: BASF AG ,  GPC BIOTECH INC ,  TAYLOR NEIL R ,  BORHANI DAVID ,  EPSTEIN DAVID ,  RUDOLPH JOHANNES ,  RITTER KURT ,  FUJIMORI TARO ,  ROBINSON SIMON ,  ECKSTEIN JENS ,  HAUPT ANDREAS ,  WALKER NIGEL ,  DIXON RICHARD W ,  CHOQUETTE DEBORAH ,  BLANCHARD JILL ,  KLUGE ARTHUR ,  PAL KOLLOL ,  BOCKOVICH NICHOLAS ,  COME JON ,  HEDIGER MARK

Inventor： TAYLOR NEIL R ,  BORHANI DAVID ,  EPSTEIN DAVID ,  RUDOLPH JOHANNES ,  RITTER KURT ,  FUJIMORI TARO ,  ROBINSON SIMON ,  ECKSTEIN JENS ,  HAUPT ANDREAS ,  WALKER NIGEL ,  DIXON RICHARD W ,  CHOQUETTE DEBORAH ,  BLANCHARD JILL ,  KLUGE ARTHUR ,  PAL KOLLOL ,  BOCKOVICH NICHOLAS ,  COME JON ,  HEDIGER MARK

IPC: C12N15/09 ,  A61K38/00 ,  A61K45/00 ,  A61P9/08 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07K5/10 ,  C07K5/107 ,  C12N9/16 ,  C12N9/99 ,  C12N15/55 ,  C07K7/06 ,  C30B29/58 ,  G06F17/50

CPC classification number: C07K5/1016 ,  A61K38/00 ,  C07K5/1027 ,  C12N9/16

Abstract: The present invention relates to polypeptides which comprise the ligand binding domain of Cdc25, crystalline forms of these polypeptides and the use of these crystalline forms to determine the three dimensional structure of the catalytic domain of Cdc25. The invention also relates to the use of the three dimensional structure of the Cdc25 catalytic domain in methods of designing and/or identifying potential inhibitors of Cdc25 activity, for example, compounds which inhibit the binding of a native substrate to the Cdc25 catalytic domain.

Abstract translation: 本发明涉及包含Cdc25的配体结合结构域，这些多肽的结晶形式以及这些结晶形式用于确定Cdc25催化结构域的三维结构的多肽。 本发明还涉及Cdc25催化结构域的三维结构在设计和/或鉴定Cdc25活性的潜在抑制剂的方法中的用途，例如抑制天然底物与Cdc25催化结构域结合的化合物。

公开(公告)号：WO0172778A2

公开(公告)日：2001-10-04

申请号：PCT/US0108853

申请日：2001-03-20

Applicant: BASF AG ,  BUMP NANCY J ,  ARNOLD LEE D ,  DIXON RICHARD W ,  HOEFFKEN HANS WOLFGANG ,  ALLEN KAREN ,  BELLAMACINA CORNELIA

Inventor： BUMP NANCY J ,  ARNOLD LEE D ,  DIXON RICHARD W ,  HOEFFKEN HANS WOLFGANG ,  ALLEN KAREN ,  BELLAMACINA CORNELIA

IPC: G01N33/48 ,  A61K38/00 ,  A61K45/00 ,  A61P1/00 ,  A61P1/04 ,  A61P1/16 ,  A61P5/00 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P13/12 ,  A61P15/00 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P27/02 ,  A61P27/10 ,  A61P29/00 ,  A61P31/04 ,  A61P35/00 ,  A61P35/02 ,  A61P43/00 ,  C07K14/71 ,  C12N9/12 ,  C12N9/99 ,  C12N15/09 ,  G01N33/15 ,  G01N33/50 ,  G01N33/68 ,  C07K14/00

CPC classification number: C07K14/71 ,  A61K38/00 ,  C07K2299/00

Abstract: The present invention relates to polypeptides which comprise the ligand binding domain of Tie-2, crystalline forms of these polypeptides and the use of these crystalline forms to determine the three dimensional structure of the catalytic domain of Tie-2. The invention also relates to the use of the three dimensional structure of the Tie-2 catalytic domain both alone, or in complex with inhibitors, in methods of designing and/or identifying potential inhibitors of Tie-2 activity, for example, compounds which inhibit the binding of a native substrate to the Tie-2 catalytic domain.

Abstract translation: 本发明涉及包含Tie-2的配体结合结构域，这些多肽的结晶形式以及这些结晶形式用于确定Tie-2催化结构域的三维结构的多肽。 本发明还涉及在设计和/或鉴定Tie-2活性的潜在抑制剂的方法中单独或与抑制剂复合的Tie-2催化结构域的三维结构的用途，例如抑制 天然底物与Tie-2催化结构域的结合。

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：AU3680701A

公开(公告)日：2001-08-20

申请号：AU3680701

申请日：2001-02-09

Applicant: BASF AG

Inventor： GHAYUR TARIQ ,  DIXON RICHARD W ,  ROGUSKA MIKE ,  WHITE MICHAEL ,  LABKOVSKY BORIS ,  SALFELD JOCHEN ,  DUNCAN ALEXANDER ROBERT ,  BROCKLEHURST SIMON MARK ,  MANKOVICH JOHN ,  SHORROCK CELIA PATRICIA ,  THOMPSON JULIA ELIZABETH ,  LENNARD SIMON NICHOLAS

IPC: C12N15/02 ,  A61K39/395 ,  A61K45/00 ,  A61P1/04 ,  A61P3/10 ,  A61P5/14 ,  A61P7/00 ,  A61P7/02 ,  A61P7/06 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P15/00 ,  A61P17/00 ,  A61P17/06 ,  A61P17/14 ,  A61P19/02 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P29/00 ,  A61P31/00 ,  A61P31/04 ,  A61P31/12 ,  A61P33/00 ,  A61P35/00 ,  A61P37/00 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  A61P39/00 ,  A61P39/02 ,  C07K16/24 ,  C12N1/15 ,  C12N1/19 ,  C12N1/21 ,  C12N5/10 ,  C12P21/08 ,  C07K16/00

Abstract: Antibodies that bind human interleukin-18 (hIL-18) are provided, in particular, antibodies that bind epitope(s) of human IL-18. The antibodies can be, for example, entirely human antibodies, recombinant antibodies, or monoclonal antibodies. Preferred antibodies have high affinity for hIL-18 and neutralize hIL-18 activity in vitro and in vivo. An antibody of the invention can be a full-length antibody or an antigen-binding portion thereof. Method of making and method of using the antibodies of the invention are also provided. The antibodies, or antibody portions, of the invention are useful for detecting hIL-18 and for inhibiting hIL-I8 activity, e.g., in a human subject suffering from a disorder in which hIL-18 activity is detrimental.

公开(公告)号：AU1073001A

公开(公告)日：2001-04-23

申请号：AU1073001

申请日：2000-10-04

Applicant: BASF AG

Inventor： TAYLOR NEIL R ,  BORHANI DAVID ,  EPSTEIN DAVID ,  RUDOLPH JOHANNES ,  RITTER KURT ,  FUJIMORI TARO ,  ROBINSON SIMON ,  ECKSTEIN JENS ,  HAUPT ANDREAS ,  WALKER NIGEL ,  DIXON RICHARD W ,  CHOQUETTE DEBORAH ,  BLANCHARD JILL ,  KLUGE ARTHUR ,  PAL KOLLOL ,  BOCKOVICH NICHOLAS ,  COME JON ,  HEDIGER MARK

IPC: A61K38/00 ,  C07C309/24 ,  C07D307/85 ,  C07F9/38 ,  C07K5/02 ,  C07K5/113 ,  C12N9/16

公开(公告)号：CA2383603A1

公开(公告)日：2001-03-08

申请号：CA2383603

申请日：2000-08-25

Applicant: GPC BIOTECH INC ,  BASF AG

Inventor： BOCKOVICH NICHOLAS ,  ECKSTEIN JENS ,  BORHANI DAVID ,  FUJIMORI TARO ,  PAL KOLLOL ,  RITTER KURT ,  ROBINSON SIMON ,  HEDIGER MARK ,  HAUPT ANDREAS ,  RUDOLPH JOHANNES ,  COME JON ,  DIXON RICHARD W ,  CHOQUETTE DEBORAH ,  EPSTEIN DAVID ,  KLUGE ARTHUR ,  WALKER NIGEL ,  BLANCHARD JILL ,  TAYLOR NEIL R

IPC: C12N15/09 ,  A61K38/00 ,  A61K45/00 ,  A61P9/08 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07K5/10 ,  C07K5/107 ,  C12N9/16 ,  C12N9/99 ,  C12N15/55 ,  A61K38/43

Abstract: The present invention relates to polypeptides which comprise the ligand binding domain of Cdc25, crystalline forms of these polypeptides and the use of these crystalline forms to determine the three dimensional structure of t he catalytic domain of Cdc25. The invention also relates to the use of the thre e dimensional structure of the Cdc25 catalytic domain in methods of designing and/or identifying potential inhibitors of Cdc25 activity, for example, compounds which inhibit the binding of a native substrate to the Cdc25 catalytic domain.

公开(公告)号：ID28955A

公开(公告)日：2001-07-19

申请号：ID20010645

申请日：1999-08-13

Applicant: BASF AG CS

Inventor： ALLEN HAMISH JOHN ,  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 ,  G01M33/50 ,  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：AU7077400A

公开(公告)日：2001-03-26

申请号：AU7077400

申请日：2000-08-25

Applicant: BASF AG ,  GPC BIOTECH INC

Inventor： TAYLOR NEIL R ,  BORHANI DAVID ,  EPSTEIN DAVID ,  RUDOLPH JOHANNES ,  RITTER KURT ,  FUJIMORI TARO ,  ROBINSON SIMON ,  ECKSTEIN JENS ,  HAUPT ANDREAS ,  WALKER NIGEL ,  DIXON RICHARD W ,  CHOQUETTE DEBORAH ,  BLANCHARD JILL ,  KLUGE ARTHUR ,  PAL KOLLOL ,  BOCKOVICH NICHOLAS ,  COME JON ,  HEDIGER MARK

IPC: C12N15/09 ,  A61K38/00 ,  A61K45/00 ,  A61P9/08 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07K5/10 ,  C07K5/107 ,  C12N9/16 ,  C12N9/99 ,  C12N15/55 ,  A61K38/43