公开(公告)号：DE19621319A1

公开(公告)日：1997-12-04

申请号：DE19621319

申请日：1996-05-28

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 ,  A01N1/02 ,  C07C277/08

公开(公告)号：DK0603650T3

公开(公告)日：1997-10-20

申请号：DK93119784

申请日：1993-12-08

Applicant: HOECHST AG

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

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

公开(公告)号：ES2104971T3

公开(公告)日：1997-10-16

申请号：ES93101840

申请日：1993-02-05

Applicant: HOECHST AG

Inventor： ENGLERT HEINRICH DR ,  MANIA DIETER DR ,  LANG HANS-JOCHEN DR ,  SCHOLZ WOLFGANG DR ,  LINZ WOLFGANG DR ,  ALBUS UDO 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：ID15889A

公开(公告)日：1997-08-14

申请号：ID970354

申请日：1997-02-05

Applicant: HOECHST AG

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

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

Abstract: Thiophenylalkenylcarboxylic acid guanidide derivatives of formula (I) and their salts are new. at least one of R1-R3 = Op(CH2)sCqF2q+1, R40CO or R31SOk; and the others = H, F, Cl, Br, I, CN, OnaCmaH2ma+1 or OgaCraH2raR10; p = 0 or 1; s = 0-4; q = 1-8; k = 0-2; R40, R31 = 1-8C alkyl, 1-8C perfluoroalkyl, 3-8C cycloalkyl or Ph (optionally substituted by 1-3 F, Cl, CF3, Me or OMe) or NR41R42; R41,R42 = H, 1-4C alkyl or 1-4C perfluoroalkyl; or R41+R42 = (CH2)x in which a CH2 group may be replaced by O, S, NH, NMe or N-benzyl; x = 4 or 5; na = 0 or 1; ma = 0-8; ga = 0 or 1; ra = 0-4; R10 = 3-8C cycloalkyl or Ph (optionally substituted by 1-3 F, Cl, CF3, Me or OMe); R4, R5 = H, F, Cl, Br, I, CN, 1-8C alkyl, 1-8C perfluoroalkyl, 3-8C cycloalkyl or Ph (optionally substituted by 1-3 F, Cl, CF3, Me, OMe or NR14R15); R14, R15 = H, 1-4C alkyl or 1-4C perfluoroalkyl.

公开(公告)号：DE19603425A1

公开(公告)日：1997-08-07

申请号：DE19603425

申请日：1996-01-31

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 ,  A61K31/155 ,  A61K31/17 ,  A61K31/18 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P43/00 ,  C07C279/22 ,  C07C311/21 ,  C07C311/60 ,  A61K31/44 ,  A61K31/47 ,  A61K31/495 ,  A61K31/505 ,  A61K49/00 ,  C07C277/08 ,  C07C311/19 ,  C07D207/327 ,  C07D207/33

公开(公告)号：ES2100435T3

公开(公告)日：1997-06-16

申请号：ES93119784

申请日：1993-12-08

Applicant: HOECHST AG

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

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

公开(公告)号：DK0602523T3

公开(公告)日：1997-06-02

申请号：DK93119782

申请日：1993-12-08

Applicant: HOECHST AG

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

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

公开(公告)号：CZ9602120A3

公开(公告)日：1997-04-16

申请号：CZ212096

申请日：1996-07-17

Applicant: HOECHST AG

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

IPC: A61K49/00 ,  A01N1/02 ,  A61K31/155 ,  A61K31/165 ,  A61K31/18 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P41/00 ,  C07C303/40 ,  C07C311/16 ,  C07C315/04 ,  C07C317/44

CPC classification number: C07C317/44

公开(公告)号：ES2097409T3

公开(公告)日：1997-04-01

申请号：ES93114774

申请日：1993-09-14

Applicant: HOECHST AG

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

IPC: A61K31/00 ,  A61K31/155 ,  A61K31/445 ,  A61P1/16 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  C07C311/16 ,  C07C311/21 ,  C07C311/29 ,  C07C317/24 ,  C07C317/44 ,  C07C317/46 ,  C07C317/48 ,  C07C323/22 ,  C07C323/65 ,  C07D211/14 ,  C07D211/70 ,  C07D295/14 ,  C07D295/155 ,  A61K31/54 ,  A61K31/45 ,  A61K49/00

Abstract: The invention relates to benzoylguanidines of the formula I where R(1) or R(2) is equal to R(3)-S(O)n- or R(4)R(5)N-O2S- and the other substituent R(1) or R(2) is in each case equal to H, OH, F, Cl, Br, I, alkyl, alkoxy, benzyloxy or phenoxy, R(3)-S(O)n or R(4)R(5)N- or 3,4-dehydropiperidine and R(3) is equal to alkyl, cycloalkyl, cyclopentylmethyl, cyclohexylmethyl or phenyl, R(4) and R(5) are equal to alkyl or phenylalkyl or phenyl, and in which R(4) and R(5) together can also be a C4-C7-chain, and in which R(4) and R(5), together with the nitrogen atom to which they are bonded, can denote a dihydroindol, tetrahydroquinoline or tetrahydroisoquinoline system, and where n is equal to zero, 1 or 2 and their pharmaceutically tolerable salts are outstanding antiarrhythmic agents. They are obtained by a process in which compounds of the formula II in which X stands for a leaving group which can be easily nucleophilically substituted, are reacted with guanidine.

公开(公告)号：GR3021397T3

公开(公告)日：1997-01-31

申请号：GR960402615

申请日：1996-10-17

Applicant: HOECHST AG

Inventor： WEICHERT ANDREAS DR ,  LANG HANS-JOCHEN ,  SCHOLZ WOLFGANG DR ,  ALBUS UDO DR ,  LANG FLORIAN PROF DR

IPC: A61K31/155 ,  A61K31/18 ,  A61K31/33 ,  A61K31/435 ,  A61K31/44 ,  A61P1/16 ,  A61P3/08 ,  A61P3/10 ,  A61P9/00 ,  A61P9/02 ,  A61P9/06 ,  A61P9/10 ,  A61P11/00 ,  A61P15/04 ,  A61P43/00 ,  C07C277/08 ,  C07C279/22 ,  C07C311/37 ,  C07C315/04 ,  C07C317/32 ,  C07C317/44 ,  C07C323/60 ,  C07D213/56

Abstract: Benzoylguanidines of the formula I with R(1) equal to R(4)-SOm or R(5)R(6)N-SO2- with R(4) and R(5) equal to alk(en)yl, -CnH2n-R(7), and with R(7) equal to cycloalkyl or phenyl, where R(5) can also mean H, R(6) equals H or C1-C4-alkyl, R(2) is hydrogen, (cyclo)alk(en)(yn)yl, aryl and hetaryl R(3) is defined as R(2), and their pharmaceutically tolerated salts, are described. Compounds I are obtained by reacting compounds of the formula II with guanidine, in which L is a leaving group which can easily undergo nuclophilic substitution. Compounds I are outstandingly suitable as antiarrhythmic drugs with cardioprotective component for the treatment and prophylaxis of infarct and for treating angina pectoris, and they also greatly reduce preventively the pathophysiological processes in the development of ischaemia-induced damage. Furthermore, I are distinguished by a potent inhibitory action on cell proliferation. They can thus be used as antiatherosclerotics, remedies for the late complications of diabetes, cancers, fibrotic disorders such as pulmonary, hepatic or renal fibrosis. They are effective inhibitors of the cellular sodium-proton antiporter (Na /H exchanger).