公开(公告)号：CA2197628C

公开(公告)日：2006-05-16

申请号：CA2197628

申请日：1997-02-14

Applicant: HOECHST AG

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

IPC: C07D333/24 ,  C07D333/30 ,  A61K31/38 ,  A61K31/381 ,  A61K31/395 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P35/00 ,  A61P43/00 ,  C07C279/22 ,  C07D333/02 ,  C07D333/06 ,  C07D333/34

Abstract: Substituted thiophenylalkenylcarboxylic acid guanidides, processes for the ir preparation, their use as a medicament or diagnostic, and a medicament containing them. There are described substituted thiophenylalkenylcarboxylic acid guanidides of the formula I in which R(1) to R(5) have the meanings given in the claims, which are outstandingly active antiarrhythmic pharmaceuticals having a cardioprotectiv e component and are outstandingly suitable for infarct prophylaxis and infarct treatment and also for the treatment of angina pectoris, where they also inhibit or greatly reduce the pathophysiological processes in the formation of ischemically induced damage, in particular in the initiation of ischemically induced cardiac arrhythmias, in a preventive manner.

公开(公告)号：NZ329606A

公开(公告)日：1999-10-28

申请号：NZ32960698

申请日：1998-01-20

Applicant: HOECHST AG

Inventor： KLEEMAN HEINZ-WERNER ,  LANG HANS JOCHEN ,  SCHWARK JAN-ROBERT ,  WEICHERT ANDREAS ,  FABER SABINE ,  JANSEN HANS-WILLI

IPC: C07D233/60 ,  A01N1/02 ,  A61K31/415 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P43/00 ,  C07D233/54 ,  C07D233/61 ,  C07D233/64 ,  C07D233/66 ,  C07D233/68 ,  C07D233/70 ,  C07D233/84 ,  C07D233/90 ,  C07D233/10 ,  C07D233/06 ,  C07D233/08 ,  C07D233/40 ,  C07D233/42 ,  C07D233/38 ,  C07D233/44 ,  C07D233/50 ,  C07D233/58 ,  C07D233/86 ,  C07D233/91

Abstract: 1-Benzylimidazole derivatives of formula (I) and their salts are new. R1 = H, 1-8C alkyl, -CaH2a-Ar or -CaH2a-(3-7C)cycloalkyl; a = 0-2; Ar = phenyl or 1-9C heteroaryl (both optionally substituted by 1-3 F, Cl, Br, I, CF3, Me, OMe, OH or NR8R9); R8, R9 = H or 1-4C alkyl; R2, R3 = H, F, Cl, Br, I, CF3, CN, NO2, CH2OR17, COR6 or OR7, 1-8C alkyl, 3-7C cycloalkyl, -CaH2a-Ar or -SOa-R22; R17= H or 1-8C alkyl; R6 = H, 1-8C alkyl, OR30 or phenyl (optionally substituted as in Ar); R7 = H, 1-8C alkyl or Ar; R22 = 1-8C alkyl, 3-7C cycloalkyl or -CaH2a-Ph; R4, R5 = H, 1-8C alkyl, F, Cl, Br, I, CF3, CN, NO2, SOa-R16, COR23 or OR24; R16 = 1-8C alkyl or phenyl (optionally substituted as in Ar); R23 = H, 1-8C alkyl or OR25; R24 = H, 1-8C alkyl or phenyl (optionally substituted as in Ar); and R25 = H or 1-8C alkyl. Also claimed is the treatment or prophylaxis of ischaemia-mediated conditions or the treatment of respiratory disorders using a tetrazole derivative.

公开(公告)号：NO970798L

公开(公告)日：1997-08-25

申请号：NO970798

申请日：1997-02-21

Applicant: HOECHST AG

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

IPC: A61K31/165 ,  A61K31/155 ,  A61P1/16 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  A61P43/00 ,  C07C279/10 ,  C07C279/20 ,  C07C279/22

Abstract: Ortho-substituted benzoylguanidines of formula (I) and their salts are new: R2, R3 = H, Cl, Br, I, 1-8C alkyl, 3-8C cycloalkyl or OR5; provided that one, but not both of R2 or R3 = H; R5 = 1-8C alkyl, or CdH2d-(3-8C cycloalkyl); and d = 0-2.

公开(公告)号：FI935578A0

公开(公告)日：1993-12-13

申请号：FI935578

申请日：1993-12-13

Applicant: HOECHST AG

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

IPC: A61K31/165 ,  A61K31/415 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4412 ,  A61K31/47 ,  A61K31/472 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  C07C279/22 ,  C07C311/08 ,  C07C317/44 ,  C07C323/62 ,  C07D207/32 ,  C07D213/64 ,  C07D213/643 ,  C07D213/65 ,  C07D213/66 ,  C07D213/68 ,  C07D213/70 ,  C07D215/20 ,  C07D215/26 ,  C07D217/02 ,  C07D217/24 ,  C07D233/54 ,  C07D249/08 ,  C07D521/00 ,  C07D ,  C07C

公开(公告)号：CA2197628A1

公开(公告)日：1997-08-16

申请号：CA2197628

申请日：1997-02-14

Applicant: HOECHST AG

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

IPC: C07D333/24 ,  A61K31/38 ,  A61K31/381 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P35/00 ,  A61P43/00 ,  C07C279/22 ,  C07D333/02 ,  C07D333/34 ,  C07D333/30 ,  C07D333/06 ,  A61K31/395

Abstract: Substituted thiophenylalkenylcarboxylic acid guanidides, processes for their preparation, their use as a medicament or diagnostic, and a medicament containing them. There are described substituted thiophenylalkenylcarboxylic acid guanidides of the formula I (see fig. I) in which R(1) to R(5) have the meanings given in the claims, which are outstandingly active antiarrhythmic pharmaceuticals having a cardioprotective component and are outstandingly suitable for infarct prophylaxis and infarct treatment and also for the treatment of angina pectoris, where they also inhibit or greatly reduce the pathophysiological processes in the formation of ischemicallyinduced damage, in particular in the initiation of ischemically induced cardiac arrhythmias, in a preventive manner.

公开(公告)号：AU1239097A

公开(公告)日：1997-08-07

申请号：AU1239097

申请日：1997-01-29

Applicant: HOECHST AG

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

IPC: A61K31/165 ,  A61K31/155 ,  A61K31/17 ,  A61K31/18 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P43/00 ,  C07C279/22 ,  C07C311/21 ,  C07C311/60 ,  A61K31/135

公开(公告)号：ZA9507549B

公开(公告)日：1996-04-17

申请号：ZA9507549

申请日：1995-09-08

Applicant: HOECHST AG

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

IPC: A61K31/165 ,  A61K31/155 ,  A61K31/18 ,  A61K31/275 ,  A61P3/08 ,  A61P3/10 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P25/00 ,  A61P25/02 ,  A61P35/00 ,  A61P41/00 ,  A61P43/00 ,  C07C22/00 ,  C07C277/08 ,  C07C279/22 ,  C07C311/29 ,  C07C311/38 ,  C07C317/44 ,  C07C323/62 ,  C07C ,  A01N ,  A61K ,  C07D

CPC classification number: C07C317/44 ,  C07C279/22

公开(公告)号：FI943548A

公开(公告)日：1995-02-01

申请号：FI943548

申请日：1994-07-28

Applicant: HOECHST AG

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

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.

公开(公告)号：FI935577A

公开(公告)日：1994-06-16

申请号：FI935577

申请日：1993-12-13

Applicant: HOECHST AG

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

IPC: A61K31/165 ,  A61K31/155 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  C07C279/22 ,  C07C311/08 ,  C07C317/44 ,  C07C317/46 ,  C07C317/48 ,  C07C323/62 ,  C07C323/65 ,  C07D213/56 ,  C07D233/54 ,  C07D239/26 ,  C07D257/02 ,  C07D257/04

Abstract: Benzoylguanidines of the formula I where R(1) is hydrogen, Hal, -NO2, -CN, -CF3, R(4)-SOm or R(5)R(6)N-SO2-, where m is zero to 2, R(4) and R(5) are alk(en)yl or -CnH2n-R(7), n is zero to 4, with R(5) also having the meaning of H, and R(6) is H or (C1-C4)-alkyl, with R(5) and R(6) together being able to be 4 or 5 methylene groups, R(2) is -SR(10), -OR(10), -NHR(10), -NR(10)R(11), -CHR(10)R(12), with R(10) and R(11) being identical or different and being -[CHR(16)]s-(CH2)p-(CHOH)q-(CH2)r-(CH2OH)t-R(21) or -(CH2)p-O(CH2-CH2O)q-R(21), R(12) and R(13) being hydrogen or alkyl, or forming a cycloalkyl together with the carbon atom carrying them, R(14) being H, (cyclo)alkyl or -CnH2n-R(15), R(3) is defined as R(1) or is alkyl, hydrogen or -X-R(22), where X is oxygen, S or NR(16), are described, as are the pharmaceutically tolerated salts thereof. The compounds I possess very good anti-arrhythmic properties but do not have any undesirable salidiuretic properties. In addition to this, they are notable for their strong inhibitory effect on the proliferation of cells.

公开(公告)号：FI935617A0

公开(公告)日：1993-12-14

申请号：FI935617

申请日：1993-12-14

Applicant: HOECHST AG

Inventor： LANG HANS-JOCHEN ,  ENGLERT HEINRICH ,  WEICHERT ANDREAS ,  KLEEMAN HEINZ-WERNER ,  SCHOLZ WOLFGANG ,  ALBUS UDO

IPC: A61K31/165 ,  A61K31/155 ,  A61K49/00 ,  A61P1/04 ,  A61P9/00 ,  A61P9/10 ,  A61P35/00 ,  A61P43/00 ,  C07C279/22 ,  C07C