公开(公告)号：HU0202431A2

公开(公告)日：2002-11-28

申请号：HU0202431

申请日：2000-04-05

Applicant: BASF AG

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

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

Abstract: The present invention relates to prodrugs of general formula (I). The meaning of said formula is 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.

公开(公告)号：HU0202401A2

公开(公告)日：2002-10-28

申请号：HU0202401

申请日：2000-04-05

Applicant: BASF AG

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

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

Abstract: The present invention relates to prodrugs of pharmacologically active five-membered heterocyclic amidines from which are produced in vivo compounds which are competitive inhibitors of trypsin-like serine proteases, in particular thrombin and kininogenases such as kallikrein, to the preparation thereof and to the use thereof as medicines. The invention also relates to pharmaceutical compositions which comprise the prodrugs of the active compounds as ingredients, and to the use of the compounds as thrombin inhibitors, anticoagulants and as antiinflammatory agents.