公开(公告)号：BG105986A

公开(公告)日：2002-06-28

申请号：BG10598601

申请日：2001-10-05

Applicant: BASF AG

Inventor： BAUCKE DORIT ,  MACK HELMUT ,  SEITZ WERNER ,  HORNBERGER WILFRIED ,  BACKFISCH GISELA ,  DELZER JUERGEN

IPC: C12N9/99 ,  A61K38/00 ,  A61K38/55 ,  A61P7/02 ,  A61P9/06 ,  A61P9/10 ,  A61P25/00 ,  A61P25/28 ,  A61P29/00 ,  A61P35/00 ,  A61P35/04 ,  A61P43/00 ,  C07B43/00 ,  C07K5/02 ,  C07K5/062 ,  C07K5/065 ,  A61K38/05

Abstract: The invention relates to prodrugs of pharmaceutically active, five-membered heterocyclic amidines from which in vivo compounds are obtained, these compounds being competitive inhibitors of trypsin-type serin proteases, especially thrombin and kininogenases such as kallikrein, as well as to their preparation and utilization as medicamentous means. The invention also relates to the production of these prodrugs and to their use as medicaments, to pharmaceutical compositions that contain the prodrugs of the active compounds as components, and to the use of the compounds as thrombin inhibitors, anti-coagulants and anti-inflammatory agents. 10 claims

公开(公告)号：BG105985A

公开(公告)日：2002-06-28

申请号：BG10598501

申请日：2001-10-05

Applicant: BASF AG

Inventor： BAUCKE DORIT ,  MACK HELMUT ,  SEITZ WERNER ,  HORNBERGER WILFRIED ,  BACKFISCH GISELA ,  DELZER JUERGEN

IPC: C12N9/99 ,  A61K38/00 ,  A61K38/55 ,  A61K47/48 ,  A61P7/02 ,  A61P43/00 ,  C07B43/00 ,  C07D401/12 ,  C07K5/062 ,  C07K5/065 ,  A61K31/4427

Abstract: The present invention relates to prodrugs of general formula (I) given in the description. Disclosed are the prodrugs of pharmaceutically active, heterocyclic amidines. In vivo compounds, which are competitive inhibitors of trypsin-like serine proteases, especially thrombin, are produced from the amidines. The invention also relates to the production and use of the prodrugs as medicaments. 10 claims

公开(公告)号：NO20020644L

公开(公告)日：2002-03-18

申请号：NO20020644

申请日：2002-02-08

Applicant: BASF AG

Inventor： KLING ANDREAS ,  GENESTE HERVE ,  LANGE UDO ,  LAUTERBACH ARNULF ,  GRAEF CLAUDIA ISABELLA ,  SUBKOWSKI THOMAS ,  HOLZENKAMP UTA ,  MACK HELMUT ,  SADOWSKI JENS ,  HORNBERGER WILFRIED ,  LAUX VOLKER

IPC: A61K31/4402 ,  A61K31/55 ,  A61K31/5513 ,  A61P3/14 ,  A61P5/18 ,  A61P7/02 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P9/14 ,  A61P13/12 ,  A61P17/02 ,  A61P17/06 ,  A61P19/00 ,  A61P19/08 ,  A61P19/10 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P33/00 ,  A61P35/00 ,  A61P35/04 ,  A61P43/00 ,  C07D213/74 ,  C07D223/20 ,  C07D243/38 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D495/14 ,  C07D

Abstract: The invention relates to novel compounds which bind to integrin receptors, and to the preparation thereof and the use thereof as drugs.

公开(公告)号：NO20020644D0

公开(公告)日：2002-02-08

申请号：NO20020644

申请日：2002-02-08

Applicant: BASF AG

Inventor： KLING ANDREAS ,  GENESTE HERVE ,  LANGE UDO ,  LAUTERBACH ARNULF ,  GRAEF CLAUDIA ISABELLA ,  SUBKOWSKI THOMAS ,  HOLZENKAMP UTA ,  MACK HELMUT ,  SADOWSKI JENS ,  HORNBERGER WILFRIED ,  LAUX VOLKER

IPC: A61K31/4402 ,  A61K31/55 ,  A61K31/5513 ,  A61P3/14 ,  A61P5/18 ,  A61P7/02 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P9/14 ,  A61P13/12 ,  A61P17/02 ,  A61P17/06 ,  A61P19/00 ,  A61P19/08 ,  A61P19/10 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P33/00 ,  A61P35/00 ,  A61P35/04 ,  A61P43/00 ,  C07D213/74 ,  C07D223/20 ,  C07D243/38 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D495/14 ,  C07D

Abstract: The invention relates to novel compounds which bind to integrin receptors, and to the preparation thereof and the use thereof as drugs.

公开(公告)号：DE10027514A1

公开(公告)日：2002-01-03

申请号：DE10027514

申请日：2000-06-06

Applicant: BASF AG

Inventor： GENESTE HERVE ,  KLING ANDREAS ,  LANGE UDO ,  LAUTERBACH ARNULF ,  SEITZ WERNER ,  GRAEF CLAUDIA ISABELLA ,  SUBKOWSKI THOMAS ,  HORNBERGER WILFRIED

IPC: C07D223/10 ,  A61K31/55 ,  A61K31/5513 ,  A61K45/00 ,  A61K45/06 ,  A61P3/10 ,  A61P5/18 ,  A61P7/00 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P13/12 ,  A61P17/00 ,  A61P17/02 ,  A61P17/06 ,  A61P19/00 ,  A61P19/02 ,  A61P29/00 ,  A61P31/00 ,  A61P31/12 ,  A61P33/00 ,  A61P35/00 ,  A61P43/00 ,  C07D263/48 ,  C07D277/08 ,  C07D307/68 ,  C07D333/38 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07K5/023 ,  C07D405/12

Abstract: The invention relates to the use of cyclic compounds as ligands of integrin receptors, in particular as ligands of the alpha vss3 integrin receptor. The invention also relates to the novel compounds, to the use thereof and to pharmaceutical preparations which contain said compounds.

公开(公告)号：AU8574801A

公开(公告)日：2001-12-24

申请号：AU8574801

申请日：2001-06-15

Applicant: BASF AG

Inventor： GENESTE HERVE ,  KLING ANDREAS ,  LANGE UDO ,  LAUTERBACH ARNULF ,  SEITZ WERNER ,  GRAEF CLAUDIA ISABELLA ,  SUBKOWSKI THOMAS ,  HORNBERGER WILFRIED

IPC: A61K45/06 ,  A61P9/00 ,  C07D223/16 ,  C07D403/12 ,  A61K31/55

Abstract: The invention relates to novel compounds which bind to integrin receptors, their use as ligands of integrin receptors, in particular as ligands of the αv&bgr;3 integrin receptor, and pharmaceutical preparations comprising these compounds.

公开(公告)号：NO20014961L

公开(公告)日：2001-11-07

申请号：NO20014961

申请日：2001-10-12

Applicant: BASF AG

Inventor： ZECHEL JOHANN-CHRISTIAN ,  KLING ANDREAS ,  GENESTE HERVE ,  LANGE UDO ,  LAUTERBACH ARNULF ,  GRAEF CLAUDIA ISABELLA ,  SUBKOWSKI THOMAS ,  SADOWSKI JENS ,  HORNBERGER WILFRIED

IPC: A61K31/505 ,  C07D239/36 ,  A61K45/00 ,  A61K45/06 ,  A61P3/14 ,  A61P7/02 ,  A61P9/10 ,  A61P9/12 ,  A61P13/12 ,  A61P17/02 ,  A61P17/06 ,  A61P19/08 ,  A61P19/10 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P33/00 ,  A61P35/00 ,  C07D239/34 ,  C07D239/60 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14 ,  C07D233/54

Abstract: The invention relates to novel compounds which bind to integrin receptors, to their preparation, to their use as integrin receptor ligands and for treating diseases, to pharmaceutical preparations comprising these compounds, and to pharmaceutical preparations comprising at least one other active compound.

公开(公告)号：NO20014961D0

公开(公告)日：2001-10-12

申请号：NO20014961

申请日：2001-10-12

Applicant: BASF AG

Inventor： ZECHEL JOHANN-CHRISTIAN ,  KLING ANDREAS ,  GENESTE HERVE ,  LANGE UDO ,  LAUTERBACH ARNULF ,  GRAEF CLAUDIA ISABELLA ,  SUBKOWSKI THOMAS ,  SADOWSKI JENS ,  HORNBERGER WILFRIED

IPC: A61K31/505 ,  C07D239/36 ,  A61K45/00 ,  A61K45/06 ,  A61P3/14 ,  A61P7/02 ,  A61P9/10 ,  A61P9/12 ,  A61P13/12 ,  A61P17/02 ,  A61P17/06 ,  A61P19/08 ,  A61P19/10 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P33/00 ,  A61P35/00 ,  C07D239/34 ,  C07D239/60 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14 ,  C07D

Abstract: The invention relates to novel compounds which bind to integrin receptors, to their preparation, to their use as integrin receptor ligands and for treating diseases, to pharmaceutical preparations comprising these compounds, and to pharmaceutical preparations comprising at least one other active compound.

公开(公告)号：DE59409847D1

公开(公告)日：2001-10-04

申请号：DE59409847

申请日：1994-11-25

Applicant: BASF AG

Inventor： SCHWEDEN JUERGEN ,  ECKES PETER ,  HORNBERGER WILFRIED ,  SUBKOWSKI THOMAS

IPC: A61K38/00 ,  A61K47/48 ,  A61P7/02

Abstract: PCT No. PCT/EP94/03901 Sec. 371 Date May 31, 1996 Sec. 102(e) Date May 31, 1996 PCT Filed Nov. 25, 1994 PCT Pub. No. WO95/15183 PCT Pub. Date Jun. 8, 1995The invention relates to novel hirudin conjugates formed from a hirudin and one or more lipophilic compounds, where the lipophilic compound has an octanol/water partition coefficient of more than 1.8 and is chemically linked to the hirudin, to the preparation thereof and to the use thereof.

公开(公告)号：CA2386230A1

公开(公告)日：2001-04-12

申请号：CA2386230

申请日：2000-10-02

Applicant: BASF AG

Inventor： HORNBERGER WILFRIED ,  GENESTE HERVE

IPC: A61K38/00 ,  A61K45/00 ,  A61K45/06 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P19/02 ,  A61P29/00 ,  A61P37/06 ,  A61P43/00 ,  C07D239/34 ,  C07D263/34 ,  C07D277/48 ,  C07D307/68 ,  C07D333/38 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07K5/02 ,  A61K38/19

Abstract: The invention relates to the use of modulators of cytokine mediated signalli ng pathways in combination with integrin .alpha.v.beta.3 receptor antagonists f or the treatment or prevention of diseases, particularly to the use of pharmaceutical composition, comprising a modulator of cytokine mediated signalling pathways and an integrin .alpha.v.beta.3 receptor antagonist, for the treatment or prevention of inflammatory or autoimmune disorders, particularly for the treatment or prevention of rheumatoid arthritis and to the pharmaceutical composition itself.