公开(公告)号：CA2210337C

公开(公告)日：2004-04-27

申请号：CA2210337

申请日：1996-01-20

Applicant: BASF AG

Inventor： SEITZ WERNER ,  KARL ULRICH

IPC: C07B57/00 ,  C07C253/34 ,  C07C255/43

Abstract: A process is disclosed for separating racemates of phenyl acetonitriles havi ng the formula (I), in which R1, R2, R3 and n have the meaning given in the description. The process consists in dissolving the racemates (I) in a polar solvent, adding thereto 0.5 to 1.0 mole of optically active camphosulphonic acid per mole of compound (I), heating the mixture up to 40 to 100 .degree.C, letting it cool down and extracting the optically active phenyl acetonitrile (I) from the thus obtained salt.

公开(公告)号：SK14092001A3

公开(公告)日：2002-05-09

申请号：SK14092001

申请日：2000-04-05

Applicant: BASF AG

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

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). 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：TR200102914T2

公开(公告)日：2002-01-21

申请号：TR200102914

申请日：2000-04-05

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

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：TR200102913T2

公开(公告)日：2002-01-21

申请号：TR200102913

申请日：2000-03-28

Applicant: BASF AG

Inventor： HILLEN HEINZ ,  SCHMIDT MARTIN ,  MACK HELMUT ,  SEITZ WERNER ,  HAUPT ANDREAS ,  ZECHEL JOHANN-CHRISTIAN ,  KLING ANDREAS

IPC: A61K38/00 ,  A61K38/55 ,  A61P1/04 ,  A61P1/18 ,  A61P5/14 ,  A61P7/02 ,  C12N9/99 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P15/00 ,  A61P17/02 ,  A61P19/02 ,  A61P21/04 ,  A61P25/00 ,  A61P25/28 ,  A61P29/00 ,  A61P37/02 ,  C07B43/00 ,  C07D401/12 ,  C07D409/12 ,  C07K5/06 ,  C07K5/062 ,  C07K5/065 ,  C07K5/068 ,  C07K5/072 ,  C07K5/078 ,  A61K38/05

Abstract: Peptide substances, their preparation and their use as complement inhibitors are described. These are in particular substances having a guanidine or amidine radical as a terminal group. In particular, inhibitors of the complement proteases C1s and C1r are described.

公开(公告)号：NO20014807L

公开(公告)日：2001-12-04

申请号：NO20014807

申请日：2001-10-03

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). 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：NO20014807A

公开(公告)日：2001-12-04

申请号：NO20014807

申请日：2001-10-03

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

CPC classification number: C07K5/06078 ,  A61K38/00 ,  C07B43/00 ,  C07D401/12

公开(公告)号：NO20014875L

公开(公告)日：2001-11-13

申请号：NO20014875

申请日：2001-10-08

Applicant: BASF AG

Inventor： BAUCKE DORIT ,  MACK HELMUT ,  SEITZ WERNER ,  HORNBERGER WILFRIED ,  BACKFISH 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 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.

公开(公告)号：CA2370267A1

公开(公告)日：2000-10-19

申请号：CA2370267

申请日：2000-04-05

Applicant: BASF AG

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

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 pharmacologically 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. 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, anticoagulants and anti-inflammatory agents.

公开(公告)号：CA2369378A1

公开(公告)日：2000-10-19

申请号：CA2369378

申请日：2000-03-28

Applicant: BASF AG

Inventor： HILLEN HEINZ ,  SCHMIDT MARTIN ,  SEITZ WERNER ,  MACK HELMUT ,  ZECHEL JOHANN-CHRISTIAN ,  KLING ANDREAS ,  HAUPT ANDREAS

IPC: C12N9/99 ,  A61K38/00 ,  A61K38/55 ,  A61P1/04 ,  A61P1/18 ,  A61P5/14 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P15/00 ,  A61P17/02 ,  A61P19/02 ,  A61P21/04 ,  A61P25/00 ,  A61P25/28 ,  A61P29/00 ,  A61P37/02 ,  C07B43/00 ,  C07D401/12 ,  C07D409/12 ,  C07K5/06 ,  C07K5/062 ,  C07K5/065 ,  C07K5/068 ,  C07K5/072 ,  C07K5/078 ,  A61K38/05

Abstract: The invention relates to peptidic substances, to the production of said substances and to their use as complement inhibitors. In particular, the invention relates to substances with a guanidine or amidine radical as the terminal group, especially inhibitors of the complement proteases C1s and C1 r.

公开(公告)号：DE59507755D1

公开(公告)日：2000-03-09

申请号：DE59507755

申请日：1995-11-25

Applicant: BASF AG

Inventor： BOEHM HANS JOACHIM ,  KOSER STEFAN ,  MACK HELMUT ,  PFEIFFER THOMAS ,  SEITZ WERNER ,  HOEFFKEN HANS WOLFGANG ,  HORNBERGER WILFRIED ,  ZIERKE THOMAS

IPC: A61K38/00 ,  A61K38/05 ,  A61K38/55 ,  A61P7/02 ,  C07K5/06 ,  C07K5/062 ,  C07K5/065 ,  C07K5/072 ,  C07K5/087