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：CA2317761A1

公开(公告)日：1999-07-29

申请号：CA2317761

申请日：1999-01-23

Applicant: BASF AG

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

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

Abstract: The invention relates to compounds of the formula A-B-D-E-F, in which A, B, D, E and F have the meanings given in the description, and to their production. These new compounds are suitable for producing medicines.

公开(公告)号：CZ9900311A3

公开(公告)日：1999-06-16

申请号：CZ31199

申请日：1997-07-29

Applicant: BASF AG

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

IPC: A61K31/40 ,  A61K31/44 ,  A61K38/00 ,  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 ,  A61K38/02

CPC classification number: C07K5/0222 ,  A61K38/00 ,  C07D207/22 ,  C07D211/78 ,  Y02P20/55

公开(公告)号：ZA977239B

公开(公告)日：1999-02-15

申请号：ZA977239

申请日：1997-08-13

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 ,  C07K ,  A61K

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：ZA9707240B

公开(公告)日：1999-02-15

申请号：ZA9707240

申请日：1997-08-13

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 ,  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 ,  C07K ,  A61K ,  C07D

CPC classification number: C07K5/0222 ,  A61K38/00 ,  C07D207/22 ,  C07D211/78 ,  Y02P20/55

公开(公告)号：ZA9707239B

公开(公告)日：1999-02-15

申请号：ZA9707239

申请日：1997-08-13

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 ,  C07K ,  A61K

CPC classification number: C07K5/06078 ,  A61K38/00

公开(公告)号：NO990662D0

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 ,  C07K

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：CA2263344A1

公开(公告)日：1998-02-19

申请号：CA2263344

申请日：1997-07-29

Applicant: BASF AG

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

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 ,  C07K5/062 ,  C07K5/065

Abstract: Disclosed are compounds having formula (I) wherein the radicals R, R1, R2, R3, R4, R5 and R6, as well as l, m, and n have the meaning indicated in the description, and the production of said compounds. The new compounds can be used to combat illness. Also described are compounds having formula (II) wherein the radicals R, R1, R2, R3, R4, R5 and R6, as well as l, m, and n have the meaning indicated in claim 1, and compounds having formula (III) wherein l and R have the meaning indicated in claim 1 and Y is an N protective group, or N-terminal protected or unprotected amino acid or represents H.