公开(公告)号：TR200102912T2

公开(公告)日：2002-03-21

申请号：TR200102912

申请日：2000-04-05

Applicant: BASF AG

Inventor： BAUKE DORIT ,  MACK HELMUT ,  SEITZ WERNER ,  BACKFISCH GISELA ,  DELZER JUERGEN ,  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 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：NO20020644A

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

CPC classification number: C07D401/06 ,  C07D223/20 ,  C07D243/38 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D495/14

公开(公告)号：BR0009674A

公开(公告)日：2002-01-15

申请号：BR0009674

申请日：2000-04-05

Applicant: BASF AG

Inventor： BAUKE 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 ,  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：NO20014876A

公开(公告)日：2001-12-04

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: C12N9/99 ,  A61K38/00 ,  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 ,  C07K5/06 ,  C07K5/065 ,  A61K38/05

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

公开(公告)号：PL181405B1

公开(公告)日：2001-07-31

申请号：PL31798995

申请日：1995-06-06

Applicant: BASF AG

Inventor： BOEHM HANS-JOACHIM ,  KOSER STEFAN ,  MACK HELMUT ,  PFEIFFER THOMAS ,  SEITZ WERNER ,  HOEFFKEN HANS W ,  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：HU0100082A2

公开(公告)日：2001-06-28

申请号：HU0100082

申请日：1999-01-23

Applicant: BASF AG

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

IPC: A61K38/00 ,  A61P1/18 ,  A61P7/02 ,  A61P11/06 ,  A61P17/04 ,  A61P19/02 ,  A61P27/16 ,  A61P29/00 ,  C07K5/06 ,  C07K5/065

Abstract: Novel five-membered heterocyclic amidines, their preparation and use as competitive inhibitors of trypsin-like serine proteases, especially thrombin and kininogenases such as kallikrein. Pharmaceutical compositions which contain the compounds as active ingredients, and use of the compounds as thrombin inhibitors, anticoagulants and antiinflammatory agents.

公开(公告)号：DE19936780A1

公开(公告)日：2001-02-15

申请号：DE19936780

申请日：1999-08-09

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 ,  C07D487/04

Abstract: The invention relates to novel compounds binding to integrin receptors, to the production thereof and to their use as medicaments.

公开(公告)号：AU3659200A

公开(公告)日：2000-11-14

申请号：AU3659200

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：DE59702414D1

公开(公告)日：2000-11-02

申请号：DE59702414

申请日：1997-07-29

Applicant: BASF AG

Inventor： BAUCKE DORIT ,  LANGE UDO ,  MACK HELMUT ,  PFEIFFER THOMAS ,  SEITZ WERNER ,  ZIERKE THOMAS ,  HOEFFKEN 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.

公开(公告)号：NZ333679A

公开(公告)日：1999-09-29

申请号：NZ33367997

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 ,  C07D417/12 ,  C07D409/12 ,  C07D413/12 ,  C07D407/12 ,  C07D401/12

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.