公开(公告)号：AU693861B2

公开(公告)日：1998-07-09

申请号：AU1786195

申请日：1995-05-03

Applicant: HOECHST AG

Inventor： SCHWARK JAN-ROBERT DR ,  KLEEMAN HEINZ-WERNER DR ,  LANG HANS-JOCHEN DR ,  WEICHERT ANDREAS DR ,  SCHOLZ WOLFGANG DR ,  ALBUS UDO DR

IPC: A61K31/165 ,  A61K31/47 ,  A61K31/472 ,  A61P3/08 ,  A61P3/10 ,  A61P9/06 ,  A61P9/10 ,  A61P13/08 ,  A61P35/00 ,  A61P43/00 ,  C07C279/22 ,  C07D215/00 ,  C07D215/48 ,  C07D215/54 ,  C07D215/56 ,  C07D217/00 ,  C07D217/02 ,  C07D217/26 ,  A61K31/135

Abstract: New bicyclic heteroaryl-carboxy-guanidine cpds. and their salts have two fused 6-membered rings contg. up to 4 unsubstd. ring N atoms. The other ring members are C atoms, opt. substd. e.g. by halo, alkyl, alkoxy, alkenyl, alkynyl, amino, carboxyguanidine, cyano, alkylthio, acyl, carboxamido, perfluoroalkyl, (poly)hydroxyalkyl, alkanoylalkyl, aminosulphonyl, (thio)ureidosulphonyl, heteroaryl, phenoxy, phenylthio or phenylamino, where the phenyl rings are opt. substd. by heterocyclyl, (poly)hydroxyalkyl or (poly)hydroxyalkylcarbonyl; or two substits. together form a satd. gp. that completes a fused ring.

公开(公告)号：CZ9701616A3

公开(公告)日：1998-06-17

申请号：CZ161697

申请日：1997-05-26

Applicant: HOECHST AG

Inventor： ALBUS UDO DR ,  BRENDEL JOACHIM DR ,  KLEEMANN HEINZ-WERNER DR ,  LANG HANS JOCHEN DR ,  SCHOLZ WOLFGANG DR ,  SCHWARK JAN ROBERT DR ,  WEICHERT ANDREAS DR

IPC: A61K31/165 ,  A61K31/155 ,  A61P3/06 ,  A61P9/00 ,  A61P9/10 ,  C07C277/06 ,  C07C279/22 ,  C07C311/15 ,  C07C317/44 ,  C07C323/62

CPC classification number: C07C279/22

公开(公告)号：CZ161697A3

公开(公告)日：1998-06-17

申请号：CZ161697

申请日：1997-05-26

Applicant: HOECHST AG

Inventor： ALBUS UDO DR ,  BRENDEL JOACHIM DR ,  KLEEMANN HEINZ-WERNER DR ,  LANG HANS JOCHEN DR ,  SCHOLZ WOLFGANG DR ,  SCHWARK JAN ROBERT DR ,  WEICHERT ANDREAS DR

IPC: A61K31/165 ,  A61K31/155 ,  A61P3/06 ,  A61P9/00 ,  A61P9/10 ,  C07C277/06 ,  C07C279/22 ,  C07C311/15 ,  C07C317/44 ,  C07C323/62

公开(公告)号：CZ9701887A3

公开(公告)日：1998-05-13

申请号：CZ188797

申请日：1997-06-17

Applicant: HOECHST AG

Inventor： WEICHERT ANDREAS DR ,  BRENDEL JOACHIM DR ,  KLEEMANN HEINZ-WERNER DR ,  LANG HANS JOCHEN DR ,  SCHWARK JAN-ROBERT DR ,  ALBUS UDO DR ,  SCHOLZ WOLFGANG DR

IPC: A61K31/165 ,  A01N1/02 ,  A01N47/44 ,  A61K31/10 ,  A61K31/155 ,  A61K31/18 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P35/00 ,  A61P43/00 ,  C07C279/10 ,  C07C279/20 ,  C07C279/22 ,  C07C303/40 ,  C07C311/19 ,  C07C311/47 ,  C07C317/42 ,  C07C317/50

CPC classification number: A61K31/155 ,  Y10S514/821 ,  Y10S514/825

公开(公告)号：CZ9700654A3

公开(公告)日：1998-05-13

申请号：CZ65497

申请日：1997-03-03

Applicant: HOECHST AG

Inventor： ALBUS UDO DR ,  BRENDEL JOACHIM DR ,  KLEEMANN HEINZ WERNER DR ,  LANG HANS JOCHEN DR ,  SCHOLZ WOLFGANG DR ,  SCHWARK JAN ROBERT DR ,  WEICHERT ANDREAS DR

IPC: A61K31/165 ,  A01N1/02 ,  A61K31/155 ,  A61P3/10 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/08 ,  A61P25/00 ,  A61P35/00 ,  A61P43/00 ,  C07C279/10 ,  C07C279/20 ,  C07C279/22

CPC classification number: C07C279/22

公开(公告)号：CZ9700653A3

公开(公告)日：1998-05-13

申请号：CZ65397

申请日：1997-03-03

Applicant: HOECHST AG

Inventor： ALBUS UDO DR ,  BRENDEL JOACHIM DR ,  KLEEMANN HEINZ-WERNER DR ,  LANG HANS JOCHEN DR ,  SCHOLZ WOLFGANG DR ,  SCHWAFK JAN ROBERT DR ,  WEICHERT ANDREAS DR

IPC: A61K31/165 ,  A01N1/02 ,  A61K31/155 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P35/00 ,  A61P43/00 ,  C07C279/22

CPC classification number: C07C279/22

公开(公告)号：CZ9603382A3

公开(公告)日：1998-05-13

申请号：CZ338296

申请日：1996-11-18

Applicant: HOECHST AG

Inventor： KLEEMANN HEINZ-WERNER DR ,  BRENDEL JOACHIM DR ,  SCHWARK JAN-ROBERT DR ,  WEICHERT ANDREAS DR ,  LANG HANS JOCHEN DR ,  ALBUS UDO DR ,  SCHOLZ WOLFGANG DR

IPC: A61K31/165 ,  A61P1/16 ,  A61P3/08 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  A61P43/00 ,  C07C279/20 ,  C07C279/22

CPC classification number: C07C279/22

公开(公告)号：DK0556672T3

公开(公告)日：1998-03-02

申请号：DK93101840

申请日：1993-02-05

Applicant: HOECHST AG

Inventor： LINZ WOLFGANG DR ,  SCHOLZ WOLFGANG DR ,  LANG HANS-JOCHEN DR ,  ENGLERT HEINRICH DR ,  ALBUS UDO DR ,  MANIA DIETER DR

IPC: A61K31/155 ,  A61K31/165 ,  A61K31/445 ,  A61P1/16 ,  A61P3/08 ,  A61P3/10 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  C07C279/22 ,  C07D213/65 ,  C07D295/14 ,  C07D295/155

Abstract: There are described benzoylguanidines of the formula I in which R(1) or R(2) is an amino group -NR(3)R(4), where R(3) and R(4) are equal to H, (cyclo)alkyl or R(3) is equal to phenyl-(CH2)p- where p = 0, 1, 2, 3 or 4, or phenyl, or R(3) and R(4) together can also be a methylene chain, and in which the other substituent R(1) or R(2) in each case is H, F, Cl, alkyl, alkoxy, CF3, CmF2m+1-CH2-, benzyl or phenoxy, and their pharmaceutically tolerable salts. The compounds according to the invention have very good antiarrhythmic properties, such as they show, for example, in the case of oxygen deficiency symptoms. The compounds are used as antiarrhythmic medicaments having a cardioprotective component for infarct prophylaxis and infarct treatment and also for the treatment of angina pectoris, where they preventively inhibit or strongly decrease the pathophysiological processes during the formation of ischaemically induced damage, in particular during the induction of ischaemically induced cardiac arrhythmias.

公开(公告)号：GR3024927T3

公开(公告)日：1998-01-30

申请号：GR970402568

申请日：1997-10-03

Applicant: HOECHST AG

Inventor： LANG HANS-JOCHEN DR ,  KLEEMANN HEINZ-WERNER DR ,  SCHOLZ WOLFGANG DR ,  ALBUS UDO DR

IPC: A61K31/165 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  C07C277/08 ,  C07C279/22 ,  C07C311/15 ,  C07C317/44 ,  C07C317/46 ,  C07C323/62 ,  C07D241/28

Abstract: There are described benzoylguanidines of the formula I where R(1) is H, Hal, -NO2, -C IDENTICAL N, Xo-(CH2)p-(CF2)q-CF3, R(5)- SOm, R(6)-CO- or R(6)R(7)NO-SO2-, where X is O, S, NR(14), m is 0-2, o is 0, 1, p is 0-2, q is 0-6, R(5) and R(6) are alk(en)yl, -CnH2n-R(8), CF3, n is 0-4, R(8) is cycloalkyl, phenyl, R(6) also being H, R(2) is where Y is O, -S- or -NR(12)-; R(11), R(12) = H, alkyl, and h is zero or 1, and i, j and k are 0-4, but where h, i and k are not simultaneously zero, R(3) is defined as R(1), or is alkyl, -X-R(13) where X is O, S, NR(14), R(14) is H, alkyl, R(13) is H, (cyclo)alkyl, -CbH2b-R(15) where b is 0-4, R(15) is phenyl, R(4) is H, -OR(16) or -NR(16)R(17) where R(16), R(17) are H, alkyl and their pharmaceutically tolerable salts. They are obtained from a compound II by reaction with guanidine, in which R(1) to R(4) have the meaning indicated and L is a leaving group which can be easily nucleophilically substituted. The compounds are outstandingly suitable as antiarrhythmic medicaments having a cardioprotective component for infarct prophylaxis and infarct treatment and also for the treatment of angina pectoris, where they also preventively inhibit or severely decrease the pathophysiological processes in the formation of ischaemically induced damage, in particular in the elicitation of ischaemically induced cardiac arrhythmias.

公开(公告)号：AT161532T

公开(公告)日：1998-01-15

申请号：AT94111575

申请日：1994-07-25

Applicant: HOECHST AG

Inventor： KLEEMANN HEINZ-WERNER DR ,  LANG HANS-JOCHEN DR ,  SCHWARK JAN-ROBERT DR ,  WEICHERT ANDREAS DR ,  SCHOLZ WOLFGANG DR ,  ALBUS UDO DR

IPC: C07D233/64 ,  A01N1/02 ,  A61K31/40 ,  A61K31/41 ,  A61K31/415 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4418 ,  A61P1/16 ,  A61P3/10 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P13/02 ,  A61P13/08 ,  A61P13/12 ,  A61P15/00 ,  A61P25/28 ,  A61P35/00 ,  A61P43/00 ,  C07C279/22 ,  C07D207/333 ,  C07D207/337 ,  C07D213/30 ,  C07D231/12 ,  C07D233/54 ,  C07D233/58 ,  C07D521/00

Abstract: The invention relates to benzoylguanidines of the formula I where R(1) is H, Hal, -NO2, -C IDENTICAL N, Xo-(CH2)p-(CF2)q-CF3, R(5)SOm, R(6)-CO-, R(6)R(7)N-CO- or R(6)R(7)N-SO2-, where X is oxygen, S, NR(14), m is zero, 1 or 2, o is zero, 1, p is zero, 1, 2, q is zero, 1, 2, 3, 4, 5, 6, R(5) and R(6) are alk(en)yl, -CnH2n-R(8), CF3, n is zero, 1, 2, 3 or 4, R(8) is cycloalkyl, phenyl, where R(6) also has the meaning of H, R(7) is H or alkyl; R(2) is R(11) is (C1-C9)-heteroaryl, Y is oxygen, -S- or NR(12)-, R(12) is H, (C1-C4)-alkyl; R(3) is defined as R(1), or is alkyl, -X-R(13) where X is oxygen, S, NR(14), R(14) is H, (C1-C3)-alkyl, R(13) is H, (cyclo)alkyl, -CbH2b-R(15) where b is zero to 4 and R(15) is phenyl; R(4) is hydrogen, -OR(16), -NR(16)R(17) or CrF2r+1 where R(16), R(17) independently are hydrogen, (C1-C3)-alkyl, r is 1-4 and their pharmaceutically tolerable salts. The compounds I are outstandingly suitable as antiarrhythmic medicaments having a cardioprotective component for infarct prophylaxis and for infarct treatment and for the treatment of angina pectoris.