公开(公告)号：WO0061609B1

公开(公告)日：2001-04-26

申请号：PCT/EP0003009

申请日：2000-04-05

Applicant: BASF AG ,  BAUCKE DORIT ,  MACK HELMUT ,  SEITZ WERNER ,  HORNBERGER WILFRIED ,  BACKFISCH GISELA ,  DELZER JUERGEN

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

CPC classification number: C07K5/06078 ,  A61K38/00 ,  C07B43/00 ,  C07K5/0222

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.

Abstract translation: 本发明涉及从其中出现在其是胰蛋白酶样丝氨酸蛋白酶，特别是凝血酶和kininogenases为激肽释放酶，其制备方法及其作为药物的用途的竞争性抑制剂的化合物的体内药理学活性的五元杂环脒的药物前体。 本发明还涉及含有该活性化合物作为成分，以及使用该化合物作为凝血酶抑制剂，抗凝血剂的前药的药物组合物和作为抗炎剂。

公开(公告)号：WO0061609A3

公开(公告)日：2001-03-15

申请号：PCT/EP0003009

申请日：2000-04-05

Applicant: BASF AG ,  BAUCKE DORIT ,  MACK HELMUT ,  SEITZ WERNER ,  HORNBERGER WILFRIED ,  BACKFISCH GISELA ,  DELZER JUERGEN

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

CPC classification number: C07K5/06078 ,  A61K38/00 ,  C07B43/00 ,  C07K5/0222

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.

Abstract translation: 本发明涉及从其中出现在其是胰蛋白酶样丝氨酸蛋白酶，特别是凝血酶和kininogenases为激肽释放酶，其制备方法及其作为药物的用途的竞争性抑制剂的化合物的体内药理学活性的五元杂环脒的药物前体。 本发明还涉及含有该活性化合物作为成分，以及使用该化合物作为凝血酶抑制剂，抗凝血剂的前药的药物组合物和作为抗炎剂。

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：BR9907112A

公开(公告)日：2000-10-24

申请号：BR9907112

申请日：1999-01-23

Applicant: BASF AG

Inventor： BAUCKE DORIT ,  LAUNGE UDO ,  MACK HELMUT ,  SEITZ WERNER ,  HOFFKEN HANS WOLFGANG ,  HORNBERGER WILFRIED

IPC: A61K38/00 ,  A61P1/18 ,  A61P7/02 ,  A61P11/06 ,  A61P17/04 ,  A61P19/02 ,  A61P27/16 ,  A61P29/00 ,  C07K5/06 ,  C07K5/065 ,  A61K38/05

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：NO20003814A

公开(公告)日：2000-07-25

申请号：NO20003814

申请日：2000-07-25

Applicant: BASF AG

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

IPC: A61K38/00 ,  A61P1/18 ,  A61P7/02 ,  A61P11/06 ,  A61P17/04 ,  A61P19/02 ,  A61P27/16 ,  A61P29/00 ,  C07K5/06 ,  C07K5/065 ,  C07K5/08 ,  A61K38/06

CPC classification number: C07K5/06191 ,  A61K38/00 ,  C07K5/06078

公开(公告)号：BG103096A

公开(公告)日：1999-09-30

申请号：BG10309699

申请日：1999-01-19

Applicant: BASF AG

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

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

Abstract: The invention relates to compounds with the formulawhere A,B,E & D have the meanings listed in the description, aswell as to their preparation. These compounds can be used for thetreatment of diseases.7 claims

公开(公告)号：SK899A3

公开(公告)日：1999-06-11

申请号：SK899

申请日：1997-07-29

Applicant: BASF AG

Inventor： BAUCKE DORIT ,  LANGE UDO ,  MACK HELMUT ,  SEITZ WERNER ,  ZIERKE THOMAS ,  HOFFKEN HANS W ,  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：NO990667L

公开(公告)日：1999-04-12

申请号：NO990667

申请日：1999-02-12

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.

公开(公告)号：NO990662A

公开(公告)日：1999-02-12

申请号：NO990662

申请日：1999-02-12

Applicant: BASF AG

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

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

CPC classification number: C07K5/06078 ,  A61K38/00