公开(公告)号：GR3034646T3

公开(公告)日：2001-01-31

申请号：GR20000402333

申请日：2000-10-20

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：ES2151614T3

公开(公告)日：2001-01-01

申请号：ES96102255

申请日：1996-02-15

Applicant: HOECHST AG

Inventor： ENGLERT HEINRICH DR ,  GERLACH UWE DR ,  MANIA DIETER DR ,  GOGELEIN 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：SI0779288T1

公开(公告)日：2000-10-31

申请号：SI9630206

申请日：1996-12-02

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: A61K31/35 ,  A61K31/352 ,  A61K31/353 ,  C07D311/58 ,  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：DE59307039D1

公开(公告)日：1997-09-11

申请号：DE59307039

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：DK0556674T3

公开(公告)日：1996-10-14

申请号：DK93101842

申请日：1993-02-05

Applicant: HOECHST AG

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

IPC: A61K31/155 ,  A61K31/18 ,  A61K31/275 ,  A61P1/16 ,  A61P3/08 ,  A61P3/10 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  A61P35/04 ,  C07C217/44 ,  C07C311/16 ,  C07C311/37 ,  C07C311/39 ,  C07C311/47 ,  C07C317/42 ,  C07C317/44 ,  C07C323/65

Abstract: There are described benzoylguanidines of the formula I where R(1) is equal to R(4)-SOm or R(5)R(6)N-SO2-, where R(4) and R(5) are equal to alk(en)yl, -CnH2n-R(7), and where R(7) is equal to cycloalkyl or phenyl, where R(5) also denotes H, R(6) is equal to H or C1-C4-alkyl, R(2) is hydrogen, halogen, alkyl, -O-(CH2)mCpF2p+1, -X-R(10), where X is equal to O, S, NR(11), R(10) is equal to H, (cyclo)alkyl(methyl), -CnH2n-R(12) where R(12) is equal to phenyl, R(3), inter alia, is defined as R(1), and their pharmaceutically tolerable salts. The compounds I are prepared by reaction of compounds of the formula II in which L represents a leaving group which can be easily substituted nucleophilically, with guanidine. Compounds I are outstandingly suitable as antiarrhythmic medicaments having a cardioprotective component for infarct prophylaxis and infract treatment and for the treatment of angina pectoris, where they also preventively inhibit or strongly decrease the pathophysiological processes during the formation of ischaemically induced damage. They are moreover distinguished by a strong inhibitory action on cell proliferation. They can therefore be used as antiatherosclerotics, agents against diabetic late complications, cancers, fibrotic disorders such as pulmonary fibrosis, fibrosis of the liver or fibrosis of the kidneys. They are effective inhibitors of the cellular sodium/protons antiporter (Na /H exchanger).

公开(公告)号：GR3020290T3

公开(公告)日：1996-09-30

申请号：GR960401455

申请日：1996-06-20

Applicant: HOECHST AG

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

IPC: A61K31/155 ,  A61K31/18 ,  A61K31/275 ,  A61P1/16 ,  A61P3/08 ,  A61P3/10 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  A61P35/04 ,  C07C217/44 ,  C07C311/16 ,  C07C311/37 ,  C07C311/39 ,  C07C311/47 ,  C07C317/42 ,  C07C317/44 ,  C07C323/65

Abstract: There are described benzoylguanidines of the formula I where R(1) is equal to R(4)-SOm or R(5)R(6)N-SO2-, where R(4) and R(5) are equal to alk(en)yl, -CnH2n-R(7), and where R(7) is equal to cycloalkyl or phenyl, where R(5) also denotes H, R(6) is equal to H or C1-C4-alkyl, R(2) is hydrogen, halogen, alkyl, -O-(CH2)mCpF2p+1, -X-R(10), where X is equal to O, S, NR(11), R(10) is equal to H, (cyclo)alkyl(methyl), -CnH2n-R(12) where R(12) is equal to phenyl, R(3), inter alia, is defined as R(1), and their pharmaceutically tolerable salts. The compounds I are prepared by reaction of compounds of the formula II in which L represents a leaving group which can be easily substituted nucleophilically, with guanidine. Compounds I are outstandingly suitable as antiarrhythmic medicaments having a cardioprotective component for infarct prophylaxis and infract treatment and for the treatment of angina pectoris, where they also preventively inhibit or strongly decrease the pathophysiological processes during the formation of ischaemically induced damage. They are moreover distinguished by a strong inhibitory action on cell proliferation. They can therefore be used as antiatherosclerotics, agents against diabetic late complications, cancers, fibrotic disorders such as pulmonary fibrosis, fibrosis of the liver or fibrosis of the kidneys. They are effective inhibitors of the cellular sodium/protons antiporter (Na /H exchanger).

公开(公告)号：CZ9600486A3

公开(公告)日：1996-09-11

申请号：CZ48696

申请日：1996-02-19

Applicant: HOECHST AG

Inventor： ENGLERT HEINRICH DR ,  GERLACH UWE DR ,  MANIA DIETER DR ,  GOGELEIN 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 ,  C07D295/00 ,  C07D303/48 ,  A61K31/445 ,  A61K31/495 ,  A61K31/535 ,  C07C303/36 ,  C07C311/57 ,  C07D203/12 ,  C07D295/08

CPC classification number: C07D303/48 ,  C07C335/42 ,  C07C2601/02

公开(公告)号：CZ38296A3

公开(公告)日：1996-08-14

申请号：CZ38296

申请日：1996-02-08

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 ,  C07C311/57 ,  C07C303/36 ,  C07C327/42

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：AT139526T

公开(公告)日：1996-07-15

申请号：AT93101842

申请日：1993-02-05

Applicant: HOECHST AG

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

IPC: A61K31/155 ,  A61K31/18 ,  A61K31/275 ,  A61P1/16 ,  A61P3/08 ,  A61P3/10 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  A61P35/04 ,  C07C217/44 ,  C07C311/16 ,  C07C311/37 ,  C07C311/39 ,  C07C311/47 ,  C07C317/42 ,  C07C317/44 ,  C07C323/65

Abstract: There are described benzoylguanidines of the formula I where R(1) is equal to R(4)-SOm or R(5)R(6)N-SO2-, where R(4) and R(5) are equal to alk(en)yl, -CnH2n-R(7), and where R(7) is equal to cycloalkyl or phenyl, where R(5) also denotes H, R(6) is equal to H or C1-C4-alkyl, R(2) is hydrogen, halogen, alkyl, -O-(CH2)mCpF2p+1, -X-R(10), where X is equal to O, S, NR(11), R(10) is equal to H, (cyclo)alkyl(methyl), -CnH2n-R(12) where R(12) is equal to phenyl, R(3), inter alia, is defined as R(1), and their pharmaceutically tolerable salts. The compounds I are prepared by reaction of compounds of the formula II in which L represents a leaving group which can be easily substituted nucleophilically, with guanidine. Compounds I are outstandingly suitable as antiarrhythmic medicaments having a cardioprotective component for infarct prophylaxis and infract treatment and for the treatment of angina pectoris, where they also preventively inhibit or strongly decrease the pathophysiological processes during the formation of ischaemically induced damage. They are moreover distinguished by a strong inhibitory action on cell proliferation. They can therefore be used as antiatherosclerotics, agents against diabetic late complications, cancers, fibrotic disorders such as pulmonary fibrosis, fibrosis of the liver or fibrosis of the kidneys. They are effective inhibitors of the cellular sodium/protons antiporter (Na /H exchanger).

公开(公告)号：ES2058149T3

公开(公告)日：1994-11-01

申请号：ES88101345

申请日：1988-01-30

Applicant: HOECHST AG

Inventor： ENGLERT HEINRICH CHRISTIAN DR ,  LANG HANS-JOCHEN DR ,  MANIA DIETER DR ,  SCHOLKENS BERNWARD DR

IPC: A61K31/40 ,  A61K31/4025 ,  A61K31/41 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/535 ,  A61K31/54 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D417/04

Abstract: 3,4-Dihydro-2H-benzo[b]pyrans of the formula I I are described, in which R1 is H, OH, (C1-C2)-alkoxy, (C1-C2)-alkyl or NR4R5, R4 and R5 being identical or different and representing H, (C1-C2)-alkyl or (C1-C3)-alkylcarbonyl, R2 and R3 are identical or different and are alkyl having 1-4 carbon atoms, Ar is an aromatic or heteroaromatic system which is unsubstituted or substituted, n is 1 or 2 and X is a (CH2)r chain which can be interrupted by a heteroatom O, S or NR6, R6 being H or (C1-C4)-alkyl and r being one of the numbers 2, 3, 4 or 5. Processes for the preparation of these compounds, their use and pharmaceutical products based on these compounds are also described.