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：TR9900819T2

公开(公告)日：1999-06-21

申请号：TR9900819

申请日：1997-09-23

Applicant: BASF AG

Inventor： LUBISCH WILFRIED ,  MOELLER ACHIM ,  DELZER JUERGEN

IPC: A61K31/445 ,  A61K31/4523 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/498 ,  A61K31/5355 ,  A61P9/10 ,  A61P25/14 ,  A61P25/28 ,  A61P35/00 ,  A61P43/00 ,  C07D211/62 ,  C07D213/40 ,  C07D295/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D409/06 ,  C07D413/12 ,  C07D413/14

CPC classification number: C07D401/06 ,  C07D211/62 ,  C07D401/12

公开(公告)号：CA2268917A1

公开(公告)日：1998-04-23

申请号：CA2268917

申请日：1997-09-23

Applicant: BASF AG

Inventor： DELZER JUERGEN ,  MOELLER ACHIM ,  LUBISCH WILFRIED

IPC: A61K31/445 ,  A61K31/4523 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/498 ,  A61K31/5355 ,  A61P9/10 ,  A61P25/14 ,  A61P25/28 ,  A61P35/00 ,  A61P43/00 ,  C07D211/62 ,  C07D213/40 ,  C07D295/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D409/06 ,  C07D413/12 ,  C07D413/14

Abstract: Disclosed are piperidine-keto acid derivates of general formula (I) and their tautomeric and isomeric forms, as well as their physiologically well tolerated salts, where R1 can mean -CO-R4, -SO2-R4, -CONH-R4, -COOR4, -C(=N)-R4, -C(=O)-NHR4 and -C(=S)-NHR4; R2 can have the meaning -C1-C6-alkyl, whether branched or not, and can still carry a phenyl, a pyridine or a naphthyl-ring, which can possibly be substituted with no more than two R5 residues, while R5 C1-C4-alkyl, whether branched or not, can mean -O-C1-C4-alkyl, OH, Cl, F, Br, J, CF3, NO2, NH2, CN, COOH, COO-C1-C4-alkyl, -NHCO-C1-C4-alkyl, -NHCOPh, -NHSO2-C1-C4-alkyl, NHSO2-Ph, -SO2-C1-C4-alkyl and -SO2Ph; and R3 can mean -OR6 and NHR6. The preparation of the inventive compounds and their use as drug products are also disclosed.

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：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：PL332720A1

公开(公告)日：1999-10-11

申请号：PL33272097

申请日：1997-09-23

Applicant: BASF AG

Inventor： LUBISCH WILFRIED ,  MOELLER ACHIM ,  DELZER JUERGEN

IPC: A61K31/445 ,  A61K31/4523 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/498 ,  A61K31/5355 ,  A61P9/10 ,  A61P25/14 ,  A61P25/28 ,  A61P35/00 ,  A61P43/00 ,  C07D211/62 ,  C07D213/40 ,  C07D295/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D409/06 ,  C07D413/12 ,  C07D413/14

Abstract: Piperidineketocarboxylic acid derivatives of the general formula Iand their tautomeric and isomeric forms, and physiologically tolerable salts thereof, where the variables have the meanings given in the description, preparation of these compounds and their use as drugs.

公开(公告)号：ZA979175B

公开(公告)日：1999-04-14

申请号：ZA979175

申请日：1997-10-14

Applicant: BASF AG

Inventor： LUBISCH WILFRIED ,  MOELLER ACHIM ,  DELZER JUERGEN

IPC: A61K31/445 ,  A61K31/4523 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/498 ,  A61K31/5355 ,  A61P9/10 ,  A61P25/14 ,  A61P25/28 ,  A61P35/00 ,  A61P43/00 ,  C07D211/62 ,  C07D213/40 ,  C07D295/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D409/06 ,  C07D413/12 ,  C07D413/14 ,  C07D ,  A61K

Abstract: Piperidineketocarboxylic acid derivatives of the general formula Iand their tautomeric and isomeric forms, and physiologically tolerable salts thereof, where the variables have the meanings given in the description, preparation of these compounds and their use as drugs.