公开(公告)号：DE59604262D1

公开(公告)日：2000-03-02

申请号：DE59604262

申请日：1996-02-12

Applicant: HOECHST AG

Inventor： ENGLERT DR ,  GERLACH DR ,  MANIA DR ,  GOEGELEIN DR ,  KAISER DR

IPC: A61K31/18 ,  A61K31/64 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/10 ,  C07C233/00 ,  C07C303/40 ,  C07C311/58 ,  C07C311/59 ,  C07C327/40 ,  C07C335/42

Abstract: Substd. benzene sulphonyl urea and thiourea derivs. of formula (I) and their salts are new. R1 = H, Me or CF3; R2 = 4-10C alkoxy with 1-6C replaced by O, S or NH; Q = O or S; Y = ÄC(R3)2Üm; R3 = H, Me or Et; R' = H, halo or 1-6C alkyl; R" = halo, 1-4C alkoxy or 1-4C alkyl; and m = 1-4.

公开(公告)号：DE69329787T2

公开(公告)日：2001-06-13

申请号：DE69329787

申请日：1993-09-20

Applicant: HOECHST AG

Inventor： LAL DR ,  GIDWANI DR ,  RAJAGOPALAN RAMANUJAM ,  PANICKER RADHA ,  SANKAR CHINNAKULANDAI ,  LANG DR ,  ENGLERT DR ,  SCHOLZ DR

IPC: A61K31/472 ,  A61P9/00 ,  A61K31/47 ,  A61P9/04 ,  A61P9/06 ,  A61P9/10 ,  C07D217/26 ,  C07D401/04 ,  C07D401/12 ,  C07D413/04 ,  C07D413/12

Abstract: Described are guanidinocarbonyl isoquinolines I, with R(1) hydrogen, (amino)(cyclo)(aryl)alk(en)yl, (heteroaryl); R(2) hydrogen, halogen, alkyl, or Aryl; G X(2), X(3) and X(4) hydrogen, halogen, nitro, amino, alkyl, sulfonamide, (mono)(di)(lower alkyl)(amino), benzyloxy, hydroxy; X(1) hydrogen, oxygen, sulfur and NR(7)R(8), and their pharmaceutically acceptable salts; described is also the process for their prepara-tion, their use as medicaments, and medicaments containing them for treating congestive heart failure, arrhythmic conditions as well as cardioprotective agents in mammals.

公开(公告)号：DE59605898D1

公开(公告)日：2000-10-26

申请号：DE59605898

申请日：1996-02-15

Applicant: HOECHST AG

Inventor： ENGLERT DR ,  GERLACH DR ,  MANIA DR ,  GOEGELEIN DR ,  KAISER 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：DE59604831D1

公开(公告)日：2000-05-04

申请号：DE59604831

申请日：1996-12-02

Applicant: HOECHST AG

Inventor： ENGLERT DR ,  GERLACH DR ,  MANIA DR ,  LINZ DR ,  GOEGELEIN DR ,  KLAUS DR ,  CRAUSE 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：DE59610691D1

公开(公告)日：2003-10-09

申请号：DE59610691

申请日：1996-01-26

Applicant: HOECHST AG

Inventor： ENGLERT DR ,  HARTUNG DR ,  CRAUSE DR ,  MANIA DR ,  GOEGELEIN DR ,  KAISER DR

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

Abstract: N-((2-Benzamidoethyl)- thiophene-sulphonyl)-urea or-thiourea derivs. of formula (I) are new. R1 = H, halogen, Me, Et, OMe, OEt, SMe, SEt, 1-2C fluoroalkyl or 1-2C fluoroalkoxy; X = O or S; R2 = H, Me or CF3; Y, Z = H, F, Cl, Br, I, Me, Et, OMe or OEt.

公开(公告)号：DE59703220D1

公开(公告)日：2001-05-03

申请号：DE59703220

申请日：1997-05-16

Applicant: HOECHST AG

Inventor： BRENDEL DR ,  KLEEMANN DR ,  ENGLERT DR ,  LANG DR ,  ALBUS DR ,  LAL DR ,  GHATE VASANTRAO ANIL

IPC: C07D295/14 ,  A01N1/02 ,  A01N47/44 ,  A61K31/155 ,  A61K31/165 ,  A61K31/445 ,  A61P3/06 ,  A61P9/00 ,  A61P9/06 ,  A61P9/10 ,  C07C271/22 ,  C07C279/20 ,  C07C279/22 ,  C07C303/40 ,  C07C311/19 ,  C07C315/04 ,  C07C317/50 ,  C07C319/20 ,  C07C323/62

Abstract: 1-Naphthoyl-guanidines (I) and their salts are new: R2-R8 = H; F; Cl; Br; I; CN; NO2; CF3; C2F5; or XaYbZ; X = O; S; or NR10, CR11R12, CO, CONR10, COO, SO; SO2, SO2NR10, OCO, NR10CO or NR10SO2 attached to the ring via the left hand atom; R10-R12 = H; 1-6C alkyl; 1-4C perfluoroalkyl; or 3-7C cycloalkyl; Y = 1-8C alkylene with 1 CH2 optionally replaced by O, S, NR13 or o-, m- or p-phenylene; R13 = H; 1-6C alkyl; 1-4C perfluoroalkyl; or 3-6C cycloalkyl; Z = H; 1-7C alkyl; 3-7C cycloalkyl; COR15; SO2R15; NR16R17; or is Ph or a C- or N-linked N-containing 1-9C heterocycle (each optionally mono-, di- or trisubstituted by F, Cl, Br, CF3, Me, OMe or NR21R22); a, b = 0 or 1; R15 = N=C(NH2)2; NR18R19; N(CH2)cNR18R19; or OR20; c = 2 or 3; R16 - R19 = H; 1-8C alkyl; or 1-4C perfluoroalkyl; or R16+R17 or R18+R19 = tetra- or pentamethylene with 1 CH2 optionally replaced by O, S or NQ; Q = H; Me; benzyl; or p-Cl-Ph; R20 = H; 1-6C alkyl; 1-4C perfluoroalkyl; or 3-7C cycloalkyl; R21, R22 = H; 1-4C alkyl; or 1-4C perfluoroalkyl; provided that when R4 = alkoxy, at least one of R2, R3 and R5-R8 is not H.

公开(公告)号：DE69329787D1

公开(公告)日：2001-02-01

申请号：DE69329787

申请日：1993-09-20

Applicant: HOECHST AG

Inventor： LAL DR ,  GIDWANI DR ,  RAJAGOPALAN RAMANUJAM ,  PANICKER RADHA ,  SANKAR CHINNAKULANDAI ,  LANG DR ,  ENGLERT DR ,  SCHOLZ DR

IPC: A61K31/472 ,  A61P9/00 ,  A61K31/47 ,  A61P9/04 ,  A61P9/06 ,  A61P9/10 ,  C07D217/26 ,  C07D401/04 ,  C07D401/12 ,  C07D413/04 ,  C07D413/12

Abstract: Described are guanidinocarbonyl isoquinolines I, with R(1) hydrogen, (amino)(cyclo)(aryl)alk(en)yl, (heteroaryl); R(2) hydrogen, halogen, alkyl, or Aryl; G X(2), X(3) and X(4) hydrogen, halogen, nitro, amino, alkyl, sulfonamide, (mono)(di)(lower alkyl)(amino), benzyloxy, hydroxy; X(1) hydrogen, oxygen, sulfur and NR(7)R(8), and their pharmaceutically acceptable salts; described is also the process for their prepara-tion, their use as medicaments, and medicaments containing them for treating congestive heart failure, arrhythmic conditions as well as cardioprotective agents in mammals.

公开(公告)号：DE59702802D1

公开(公告)日：2001-02-01

申请号：DE59702802

申请日：1997-05-16

Applicant: HOECHST AG

Inventor： BRENDEL DR ,  KLEEMANN DR ,  ENGLERT DR ,  LANG DR ,  SCHWARK DR ,  WEICHERT DR ,  LAL DR

IPC: C07D295/14 ,  A01N1/02 ,  A01N47/44 ,  A61K31/155 ,  A61K31/165 ,  A61K31/27 ,  A61K31/44 ,  A61K31/495 ,  A61K31/535 ,  A61K31/5375 ,  A61P3/06 ,  A61P9/00 ,  A61P9/06 ,  A61P9/10 ,  A61P35/00 ,  A61P43/00 ,  C07C271/22 ,  C07C277/08 ,  C07C279/20 ,  C07C279/22 ,  C07C311/19 ,  C07C317/50 ,  C07C323/62 ,  C07D213/40 ,  C07D213/75 ,  C07D295/08 ,  C07D295/088

Abstract: 2-Naphthoyl-guanidines (I) and their salts are new: R1 and R3-R8 = H; F; Cl; Br; I; CN; NO2; CF3; C2F5; VpQqU; XYaWZ; or X'YaWZ' (at least 1 is XYaWZ or X'YaWZ'); V = O; S; SO; SO2; NR60; OCO; CO; CONR60; COO; or CR66R67; Q = 1-8C alkylene with 1 CH2 optionally replaced by O, S, NR13 or o-, m- or p-phenylene; U = H; 1-7C alkyl; 3-7C cycloalkyl; COR65; SO2R65; NR61R62; or Ph or a N- or C-linked N-containing 1-9C heterocycle optionally mono-, di- or trisubstituted by F, Cl, Br, CF3, Me, OMe or NR63R64; p, q = 0 or 1; X = O; S; NR10; or CR11R12; Y = 1-8C alkylene with 1 CH2 optionally replaced by O, S, NR13 or o-, m- or p-phenylene; W = CH2; SO2; S(O)(NH); or (when W is not attached directly to a hetero atom of XYa) O or NR14; Z = COR15; SO2R15; or (when W is not O or NR14) NR16R17; a = 0 or 1; X' = CO, CONR30, COO, SO, SO2, SO2NR30, OCO, NR30CO or NR30SO2 linked with the ring via the left hand atom; Z' = COR15; SO2R15; a N- or C-linked N-containing 1-9C heterocycle optionally mono-, di- or trisubstituted by F, Cl, Br, CF3, Me, OMe or NR21R22; or (when W is not O or NR14) Z' is NR16R17; R10-R12 = H; 1-6C alkyl; 1-4C perfluoroalkyl; or 3-7C cycloalkyl; R13, R14, R68 = H; 1-6C alkyl; 1-4C perfluoroalkyl; or 3-6C cycloalkyl; R15 = N=C(NH2)2; NR18R19; N(CH2)bNR18R19; or OR20; b = 2 or 3; R16 - R19 = H; 1-8C alkyl; or 1-4C perfluoroalkyl; or R16+R17 or R18+R19 = tetra- or pentamethylene with 1 CH2 optionally replaced by O, S or NA; A = H; Me; benzyl; or p-Cl-Ph; R20, R30; R60; R66; R67 = H; 1-6C alkyl; 1-4C perfluoroalkyl; or 3-7C cycloalkyl; R21, R22; R63, R64 = H; 1-4C alkyl; or 1-4C perfluoroalkyl; R65 = N=C(NH2)2; NR61R62; or OR60; R61, R62 = H; 1-8C alkyl; or 1-4C perfluoroalkyl; or R61+R62 = tetra- or pentamethylene with 1 CH2 optionally replaced by O, S or NA; provided that at least one of R5-R8 is not H.

公开(公告)号：DE59409440D1

公开(公告)日：2000-08-17

申请号：DE59409440

申请日：1994-12-27

Applicant: HOECHST AG

Inventor： ENGLERT DR ,  MANIA DR ,  HARTUNG DR ,  GOEGELEIN DR ,  KAISER DR ,  GERLACH 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.