公开(公告)号：AT237631T

公开(公告)日：2003-05-15

申请号：AT95923231

申请日：1995-06-06

Applicant: BASF AG

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

IPC: A61K31/40 ,  A61K38/00 ,  A61K38/05 ,  A61K38/55 ,  A61K47/48 ,  A61P7/02 ,  C07C279/00 ,  C07D205/04 ,  C07D207/06 ,  C07D207/16 ,  C07D207/48 ,  C07D211/60 ,  C07K5/06 ,  C07K5/065 ,  C07K5/072 ,  C07K5/078

Abstract: Compounds of the formula and the salts thereof with physiologically tolerated acids and the stereoisomers thereof, in which the substituents have the meanings stated in the description, are described. Also disclosed are intermediates for their preparation. The compounds are suitable for controlling diseases.

公开(公告)号：SK14222001A3

公开(公告)日：2002-07-02

申请号：SK14222001

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 ,  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 ,  C07K5/06

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：BR0009653A

公开(公告)日：2002-01-08

申请号：BR0009653

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 ,  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：NO20014876D0

公开(公告)日：2001-10-08

申请号：NO20014876

申请日：2001-10-08

Applicant: BASF AG

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

IPC: A61K38/00 ,  C12N9/99 ,  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 ,  C07K

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：NO20014875D0

公开(公告)日：2001-10-08

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 ,  C07K

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：NO20014807D0

公开(公告)日：2001-10-03

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 ,  C07D

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：AU735364B2

公开(公告)日：2001-07-05

申请号：AU3941797

申请日：1997-07-29

Applicant: BASF AG

Inventor： BAUCKE DORIT ,  LANGE UDO ,  MACK HELMUT ,  SEITZ WERNER ,  ZIERKE THOMAS ,  HOFFKEN HANS WOLFGANG ,  HORNBERGER WILFRIED

IPC: A61K38/00 ,  A61K38/05 ,  A61P7/02 ,  A61P29/00 ,  A61P35/00 ,  A61P35/04 ,  C07K5/06 ,  C07K5/062 ,  C07K5/065

Abstract: PCT No. PCT/EP97/04104 Sec. 371 Date Feb. 10, 1999 Sec. 102(e) Date Feb. 10, 1999 PCT Filed Jul. 29, 1997 PCT Pub. No. WO98/06741 PCT Pub. Date Feb. 19, 1998Compounds of the formula where A, B, E and D have the meanings indicated in the description, and their preparation are described. The substances are suitable for controlling diseases.

公开(公告)号：AU4111700A

公开(公告)日：2000-11-14

申请号：AU4111700

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: 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

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：CA2368830A1

公开(公告)日：2000-10-19

申请号：CA2368830

申请日：2000-04-05

Applicant: BASF AG

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

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 meanin g 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：AT196637T

公开(公告)日：2000-10-15

申请号：AT97934552

申请日：1997-07-29

Applicant: BASF AG

Inventor： BAUCKE DORIT ,  LANGE UDO ,  MACK HELMUT ,  PFEIFFER THOMAS ,  SEITZ WERNER ,  ZIERKE THOMAS ,  HOEFFKEN HANS WOLFGANG ,  HORNBERGER WILFRIED

IPC: A61K31/40 ,  A61K31/44 ,  A61K38/00 ,  A61K38/05 ,  A61P1/18 ,  A61P7/02 ,  A61P11/02 ,  A61P11/06 ,  A61P17/00 ,  A61P19/02 ,  A61P29/00 ,  A61P43/00 ,  C07D207/22 ,  C07D211/78 ,  C07K5/00 ,  C07K5/02 ,  C07K5/083

Abstract: Compounds of the formula Iwhere R, R1, R2, R3, R4, R5 and R6, and l, m and n have the meanings stated in the description, and their preparation are described. The novel compounds are suitable for controlling diseases.