公开(公告)号：CZ290738B6

公开(公告)日：2002-10-16

申请号：CZ28096

申请日：1996-01-30

Applicant: HOECHST AG

Inventor： ENGLERT HEINRICH DR ,  HARTUNG JENS DR ,  CRAUSE PETER DR ,  MANIA DIETER DR ,  GOGELEIN HEINZ DR ,  KAISER JOACHIM DR

IPC: A61K31/38 ,  A61K31/381 ,  A61K31/64 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/10 ,  A61P43/00 ,  C07C335/00 ,  C07D333/34

Abstract: In the present invention, there are described substituted thiophenesulfonyl ureas and thioureas of the general formula I, in which R(1) represents hydrogen, halogen or an alkyl group containing 1 to 2 carbon atoms, R(2) represents hydrogen or methyl, X represents oxygen or sulfur and Y and Z that are the same or different represent each hydrogen, fluorine, chlorine, bromine, iodine an alkyl group containing 1 to 2 carbon atoms or an alkoxyl group having 1 to 2 carbon atoms, and their physiologically acceptable salts. These compounds exhibit activity on cardiovascular system. Disclosed is also a process for preparing these compounds as well as a medicament in which they are comprised.

公开(公告)号：ES2152440T3

公开(公告)日：2001-02-01

申请号：ES96101585

申请日：1996-02-05

Applicant: HOECHST AG

Inventor： ENGLERT HEINRICH DR ,  GERLACH UWE DR ,  CRAUSE PETER DR ,  MANIA DIETER DR ,  GOGELEIN HEINZ DR ,  KAISER JOACHIM DR

IPC: C07D333/20 ,  A61K31/18 ,  A61K31/34 ,  A61K31/35 ,  A61K31/38 ,  A61K31/381 ,  A61K31/395 ,  A61K31/40 ,  A61K31/425 ,  A61K31/426 ,  A61K31/64 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/10 ,  C07C233/00 ,  C07C303/40 ,  C07C311/58 ,  C07C327/40 ,  C07C335/42 ,  C07D207/32 ,  C07D207/335 ,  C07D213/40 ,  C07D277/28 ,  C07D307/52

Abstract: Substd. benzenesulphonylurea or -thiourea cpds. of formula (I) are new: R1 = H, 1-6C alkyl, or 3-6C cycloalkyl; R2 = 1-6C alkyl, 1-6C alkoxy, 1-6C mercaptoalkyl, 3-6C cycloalkyl, or a 1-8C chain in which 1-3C may be replaced by O, NH or S; R3, R4 = H or 1-6C alkyl; or R3 + R4 = (CH2)p; p = 2-5; E, X = O or S; Y = ÄC(R5)2Üm; R5 = H, Me or Et; m = 1 or 2; Ar = phenyl, thienyl, furyl, pyrrolyl, thiazolyl, naphthyl or pyridyl (all opt. substd. by 1-3 Me, Et, MeO, EtO, Cl, Br or F).

公开(公告)号：GR3034513T3

公开(公告)日：2000-12-29

申请号：GR20000402203

申请日：2000-09-29

Applicant: HOECHST AG

Inventor： ENGLERT HEINRICH DR ,  MANIA DIETER DR ,  HARTUNG JENS DR ,  GOEGELEIN HEINZ DR ,  KAISER JOACHIM DR ,  GERLACH UWE DR

IPC: C07D217/24 ,  A61K31/40 ,  A61K31/64 ,  A61P9/00 ,  A61P9/06 ,  A61P9/10 ,  A61P43/00 ,  C07C303/36 ,  C07C311/58 ,  C07C335/42 ,  C07D207/38 ,  C07D521/00

Abstract: There are described substituted benzenesulphonylureas and -thioureas of the formula I where R(1) is H, (cyclo)(CH2)a(fluoro)alk(en)yl, R(2) is H, Hal, (fluoro)(mercapto)(CH2)e(cyclo)alk(oxy)(yl), NR(4)R(5) where R(4) and R(5) together are a (CH2)2-7 chain, or R(4), R(5), R(6) are H, (alkyl)(cyclo)(fluoro)alk(en)yl, E is O, S; Y is -[CR(7)2]n-R(3) B is (C3-C6)-alkenyl, or R(3) is X is H, Hal, alkyl; Z is Hal, (cyclo)alk(yl)(oxy). Compounds I are used for the treatment of cardiac arrhythmias and for the prevention of sudden heart death caused by arrhythmia and can therefore be used as antiarrhythmics. They are particularly suitable in those cases in which arrhythmias are the result of constriction of a coronary vessel, such as in angina pectoris or in acute cardiac infarct.

公开(公告)号：AT197291T

公开(公告)日：2000-11-15

申请号：AT96101585

申请日：1996-02-05

Applicant: HOECHST AG

Inventor： ENGLERT HEINRICH DR ,  GERLACH UWE DR ,  CRAUSE PETER DR ,  MANIA DIETER DR ,  GOEGELEIN HEINZ DR ,  KAISER JOACHIM DR

IPC: C07D333/20 ,  A61K31/18 ,  A61K31/34 ,  A61K31/35 ,  A61K31/38 ,  A61K31/381 ,  A61K31/395 ,  A61K31/40 ,  A61K31/425 ,  A61K31/426 ,  A61K31/64 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/10 ,  C07C233/00 ,  C07C303/40 ,  C07C311/58 ,  C07C327/40 ,  C07C335/42 ,  C07D207/32 ,  C07D207/335 ,  C07D213/40 ,  C07D277/28 ,  C07D307/52

Abstract: Substd. benzenesulphonylurea or -thiourea cpds. of formula (I) are new: R1 = H, 1-6C alkyl, or 3-6C cycloalkyl; R2 = 1-6C alkyl, 1-6C alkoxy, 1-6C mercaptoalkyl, 3-6C cycloalkyl, or a 1-8C chain in which 1-3C may be replaced by O, NH or S; R3, R4 = H or 1-6C alkyl; or R3 + R4 = (CH2)p; p = 2-5; E, X = O or S; Y = ÄC(R5)2Üm; R5 = H, Me or Et; m = 1 or 2; Ar = phenyl, thienyl, furyl, pyrrolyl, thiazolyl, naphthyl or pyridyl (all opt. substd. by 1-3 Me, Et, MeO, EtO, Cl, Br or F).

公开(公告)号：AT196467T

公开(公告)日：2000-10-15

申请号：AT96102255

申请日：1996-02-15

Applicant: HOECHST AG

Inventor： ENGLERT HEINRICH DR ,  GERLACH UWE DR ,  MANIA DIETER DR ,  GOEGELEIN HEINZ DR ,  KAISER JOACHIM DR

IPC: C07D331/02 ,  A61K31/18 ,  A61K31/38 ,  A61K31/64 ,  A61P9/00 ,  A61P9/02 ,  A61P9/06 ,  A61P9/10 ,  C07C233/00 ,  C07C303/40 ,  C07C311/58 ,  C07C327/46 ,  C07C335/42 ,  C07D203/08 ,  C07D295/00 ,  C07D303/48

Abstract: N-(3-substd. benzensulphonyl)-urea or -thiourea derivs. of formula (I) and their salts are new. R1 = H, 1-7C alkyl or 3-7C cycloalkyl; R2 = H, F, Cl, 1-6C alkyl, 1-6C alkoxy, 1-6C mercaptoalkyl, 3-6C cycloalkyl or CbH2b+1, in which one or more C can be replaced by Het; Het = heteroatoms, e.g. O, NH or S; b = 1-8; 1-8C alkyl in which 1-4C may be replaced by O, N or S; R3 = H, 1-12C alkyl, 3-10C cycloalkyl, 1-6C fluoroalkyl, 3-6C fluorocycloalkyl or CaH2a+1 in which 1-4C are replaced by Het; a = 1-10; R4 = aryl or as R3; or R3+R4 = CbH2b, in which one or more CH2 can be replaced by Het; R5 = as R4; R6 = as R4 but not 3-10C cycloalkyl; Q, X = O or S; Y = -(C(R7)2)c, O, S or NH; c = 1-4; R7 = H, 1-4C alkyl, F, Cl or Br.

公开(公告)号：GR3033300T3

公开(公告)日：2000-09-29

申请号：GR20000400982

申请日：2000-04-21

Applicant: HOECHST AG

Inventor： ENGLERT HEINRICH CHRISTIAN DR ,  GERLACH UWE DR ,  MANIA DIETER DR ,  LINZ WOLFGANG DR ,  GOEGELEIN HEINZ DR ,  KLAUS ERIK DR ,  CRAUSE PETER DR

IPC: C07D311/58 ,  A61K31/35 ,  A61K31/352 ,  A61K31/353 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/4025 ,  A61K31/4412 ,  A61K31/443 ,  A61K31/445 ,  A61P9/00 ,  A61P9/06 ,  A61P9/10 ,  C07D311/64 ,  C07D311/70 ,  C07D405/12

Abstract: N-(4-Amidoalkyl-chroman-5-yl-sulphonyl)-urea or -thiourea derivatives of formula (I) and their salts are new. R1 = H, alkyl, alkoxy, F, Cl, Br, I, CF3, NH2, mono- or dialkylamino or alkylthio; R2a = H, Me or Et; R2b, R2d = H, Me or Et; or phenyl or benzyl (both optionally ring-substituted by 1-3 of halogen, Me, Et, OMe and OEt); R2c,R2e = H, Me or Et; R3 = H, alkyl, cycloalkyl, cycloalkylmethyl or CF3; n = 1 or 2; Z = O or S; A = phenyl (optionally substituted by 1-3 of halogen, Me, OMe, Et or OEt), a lactam residue of formula (a), 1-oxo-1,2,3,4-tetrahydroisoquinolin-2-yl, 1-oxo-per-hydro-isoquinolin-2-yl, 1-oxo-1,2-dihydro-iso-indol-2-yl or 1-oxo-per-hydro-iso-indol-2-yl; B = 3-6C alkylene or 3-6C alkenylene (both optionally substituted by 1-3 alkyl); unless specified otherwise alkyl moieties have 1-4C and cycloalkyl moieties 3-6C.

公开(公告)号：ES2146348T3

公开(公告)日：2000-08-01

申请号：ES96119262

申请日：1996-12-02

Applicant: HOECHST AG

Inventor： ENGLERT HEINRICH CHRISTIAN DR ,  GERLACH UWE DR ,  MANIA DIETER DR ,  LINZ WOLFGANG DR ,  GOGELEIN HEINZ DR ,  KLAUS ERIK DR

IPC: C07D311/58 ,  A61K31/35 ,  A61K31/352 ,  A61K31/353 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/4025 ,  A61K31/4412 ,  A61K31/443 ,  A61K31/445 ,  A61P9/00 ,  A61P9/06 ,  A61P9/10 ,  C07D311/64 ,  C07D311/70 ,  C07D405/12

Abstract: N-(4-Amidoalkyl-chroman-5-yl-sulphonyl)-urea or -thiourea derivatives of formula (I) and their salts are new. R1 = H, alkyl, alkoxy, F, Cl, Br, I, CF3, NH2, mono- or dialkylamino or alkylthio; R2a = H, Me or Et; R2b, R2d = H, Me or Et; or phenyl or benzyl (both optionally ring-substituted by 1-3 of halogen, Me, Et, OMe and OEt); R2c,R2e = H, Me or Et; R3 = H, alkyl, cycloalkyl, cycloalkylmethyl or CF3; n = 1 or 2; Z = O or S; A = phenyl (optionally substituted by 1-3 of halogen, Me, OMe, Et or OEt), a lactam residue of formula (a), 1-oxo-1,2,3,4-tetrahydroisoquinolin-2-yl, 1-oxo-per-hydro-isoquinolin-2-yl, 1-oxo-1,2-dihydro-iso-indol-2-yl or 1-oxo-per-hydro-iso-indol-2-yl; B = 3-6C alkylene or 3-6C alkenylene (both optionally substituted by 1-3 alkyl); unless specified otherwise alkyl moieties have 1-4C and cycloalkyl moieties 3-6C.

公开(公告)号：DK0779288T3

公开(公告)日：2000-07-31

申请号：DK96119262

申请日：1996-12-02

Applicant: HOECHST AG

Inventor： CRAUSE PETER DR ,  ENGLERT HEINRICH CHRISTIAN DR ,  GERLACH UWE DR ,  MANIA DIETER DR ,  LINZ WOLFGANG DR ,  GOEGELEIN HEINZ DR ,  KLAUS ERIK DR

IPC: C07D311/58 ,  A61K31/35 ,  A61K31/352 ,  A61K31/353 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/4025 ,  A61K31/4412 ,  A61K31/443 ,  A61K31/445 ,  A61P9/00 ,  A61P9/06 ,  A61P9/10 ,  C07D311/64 ,  C07D311/70 ,  C07D405/12

Abstract: N-(4-Amidoalkyl-chroman-5-yl-sulphonyl)-urea or -thiourea derivatives of formula (I) and their salts are new. R1 = H, alkyl, alkoxy, F, Cl, Br, I, CF3, NH2, mono- or dialkylamino or alkylthio; R2a = H, Me or Et; R2b, R2d = H, Me or Et; or phenyl or benzyl (both optionally ring-substituted by 1-3 of halogen, Me, Et, OMe and OEt); R2c,R2e = H, Me or Et; R3 = H, alkyl, cycloalkyl, cycloalkylmethyl or CF3; n = 1 or 2; Z = O or S; A = phenyl (optionally substituted by 1-3 of halogen, Me, OMe, Et or OEt), a lactam residue of formula (a), 1-oxo-1,2,3,4-tetrahydroisoquinolin-2-yl, 1-oxo-per-hydro-isoquinolin-2-yl, 1-oxo-1,2-dihydro-iso-indol-2-yl or 1-oxo-per-hydro-iso-indol-2-yl; B = 3-6C alkylene or 3-6C alkenylene (both optionally substituted by 1-3 alkyl); unless specified otherwise alkyl moieties have 1-4C and cycloalkyl moieties 3-6C.

公开(公告)号：DE59407559D1

公开(公告)日：1999-02-11

申请号：DE59407559

申请日：1994-12-01

Applicant: HOECHST AG

Inventor： ENGLERT HEINRICH DR ,  MANIA DIETER DR ,  HARTUNG JENS DR ,  GOEGELEIN HEINZ DR ,  KAISER JOACHIM DR

IPC: A61K31/64 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  C07C303/36 ,  C07C311/57 ,  C07C311/58 ,  C07C335/42 ,  C07D295/135

Abstract: Amino-substituted benzenesulphonylureas and -thioureas of the formula I are described. The compounds I are used for treating cardiac dysrhythmias and for preventing sudden heart death due to arrhythmias and can therefore be used as antiarrhythmics. They are particularly suitable for cases in which arrhythmias are the consequence of a constriction of a coronary vessel, such as in angina pectoris or acute myocardial infarct.

公开(公告)号：AT175192T

公开(公告)日：1999-01-15

申请号：AT94118931

申请日：1994-12-01

Applicant: HOECHST AG

Inventor： ENGLERT HEINRICH DR ,  MANIA DIETER DR ,  HARTUNG JENS DR ,  GOEGELEIN HEINZ DR ,  KAISER JOACHIM DR

IPC: A61K31/64 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  C07C303/36 ,  C07C311/57 ,  C07C311/58 ,  C07C335/42 ,  C07D295/135

Abstract: Amino-substituted benzenesulphonylureas and -thioureas of the formula I are described. The compounds I are used for treating cardiac dysrhythmias and for preventing sudden heart death due to arrhythmias and can therefore be used as antiarrhythmics. They are particularly suitable for cases in which arrhythmias are the consequence of a constriction of a coronary vessel, such as in angina pectoris or acute myocardial infarct.