公开(公告)号：MY117715A

公开(公告)日：2004-07-31

申请号：MYPI9600308

申请日：1996-01-29

Applicant: HOECHST AG

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

IPC: C07C311/29 ,  C07D295/12 ,  A61K31/155 ,  A61K31/18 ,  A61K31/395 ,  A61K31/40 ,  A61K31/415 ,  A61K31/4166 ,  A61K31/4184 ,  A61K31/47 ,  A61K31/495 ,  A61K31/496 ,  A61K31/535 ,  A61K31/5355 ,  A61K31/5375 ,  A61P1/16 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P13/08 ,  A61P13/12 ,  A61P35/00 ,  C07C279/22 ,  C07C311/15 ,  C07C311/18 ,  C07C311/64 ,  C07C317/28 ,  C07C317/46 ,  C07C323/16 ,  C07C323/25 ,  C07C335/22 ,  C07C335/32 ,  C07C381/10 ,  C07D207/09 ,  C07D213/40 ,  C07D213/70 ,  C07D215/36 ,  C07D233/42 ,  C07D233/54 ,  C07D233/60 ,  C07D233/84 ,  C07D235/28 ,  C07D295/22 ,  C07D311/64 ,  C07D521/00

Abstract: COMPOUNDS OF THE FORMULA I FORMULA I AND THE PHANNACEUTICALLY TOLERATED SLATS THREOF, ARE DESCRIBED. A PROCESS FOR THEIR PREPARATION AND THEIR USE AS MEDICAMENTS IN CARDIOVASCULAR DISEASES ARE ALSO DESCRIBED.

公开(公告)号：MY116861A

公开(公告)日：2004-04-30

申请号：MYPI9700835

申请日：1997-03-03

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 ,  A01N1/02 ,  A61K31/55 ,  A61K31/155 ,  A61P3/10 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/08 ,  A61P25/00 ,  A61P35/00 ,  A61P43/00 ,  C07C279/10 ,  C07C279/20 ,  C07C279/22

Abstract: ORTHO-SUBSTITUTED BENZOYLGUANIDINES OF THE FORMULA I: (FORMULA I) IN WHICH R(1) TO R(4) HAVE THE MEANINGS GIVEN IN THE CLAIMS, ARE SUITABLE, AS ANTIARRHYTHMIC PHARMACEUTICALS HAVING A CARDIOPROTECTIVE COMPONENT, FOR THE PROPHYLAXIS AND TREATMENT OF INFRACTION AND FOR THE TREATMENT OF ANGINA PECTORIS. THEY ALSO INHIBIT, IN A PREVENTIVE MANNER, THE PATHOPHYSIOLOGICAL PROCESSES ASSOCIATED WITH THE GENESIS OF ISCHEMICALLY INDUCED DAMAGE, IN PARTICULAR ASSOCIATED WITH THE TRIGGERING OF ISCHEMICALLY INDUCED CARDIAC ARRHYTHMIAS.

公开(公告)号：HU223055B1

公开(公告)日：2004-03-01

申请号：HU9402444

申请日：1994-08-24

Applicant: HOECHST AG

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

IPC: A61K31/155 ,  A61K31/185 ,  A61P9/00 ,  A61P9/10 ,  C07C277/08 ,  C07C279/20 ,  C07C279/22 ,  C07C311/37 ,  C07C311/59 ,  C07C315/04 ,  C07C317/32 ,  C07C317/44 ,  C07C323/65 ,  C07C323/67 ,  C07D207/327 ,  C07D215/54 ,  C07D231/12 ,  C07D233/60 ,  C07D233/61 ,  C07D295/10 ,  C07D295/155 ,  C07D521/00

Abstract: Benzoyl-guanidine derivatives (III) are new. (III) are of formula X2-CO-N=C(NH2)2 X2 = R101 = hydrogen, fluoro, chloro, hydroxy, amino or trifluoromethyl; R102 = hydrogen, fluoro, chloro, bromo, cyano, CqF2qCF3, R13SO2, R14R15NCO, R16CO or R17R18NSO2; R13, R14, R16 and R17 = 1-8C alkyl, 3-4C alkenyl, CnH2n-R20, trifluoromethyl or, except for R13, hydrogen; n = 0 or 1; q = 1-5; R20 = 3-6C cycloalkyl or phenyl, optionally substituted by 1-2 of fluoro, chloro, trifluoromethyl, methyl, methoxy or NR21R22; R21 and R22 = hydrogen or methyl; R104 = 1-8C alkyl, CnH2nR20, trifluoromethyl, (iso)quinolyl, pyrrolyl, pyridyl or imidazolyl (all these rings bonded via carbon or nitrogen and optionally substituted by 1 or 2 fluoro, chloro, trifluoromethyl, methoxy, hydroxy or amino (optionally substituted by 1 or 2 methyl)), R87SO2, R88R89NSO2, or R93-ethynyl; R87 = 1-4C alkyl or trifluoromethyl; R88 = hydrogen, 1-4C alkyl, trifluoromethyl, or (CH2)anR90; an = 0 or 1; R90 and R93 = phenyl, optionally substituted as in R20; R103 = any of a wide range of substituents . The full definitions are given in the DEFINITIONS (Full Definitions) Field.

公开(公告)号：ES2184770T3

公开(公告)日：2003-04-16

申请号：ES95100675

申请日：1995-01-19

Applicant: HOECHST AG

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

IPC: A61K31/165 ,  A01N1/02 ,  A61B10/00 ,  A61K31/155 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P35/00 ,  A61P43/00 ,  C07C277/00 ,  C07C279/10 ,  C07C279/22 ,  C07D241/26 ,  G01N33/50

Abstract: Perfluoroalkyl-substd. phenylalkanoic acid guanidides of formula (I) and their salts are new: Ra, Rb = H, halogen, CN, OR6, 1-8C alkyl, 3-8C cycloalkyl, Or(CH2)aCbF2b+1 or NR7R8; r = 0 or 1; a = 0-4; b = 1-8; R6-R8 = H, 1-8C alkyl, 3-8C alkenyl, 3-8C cycloalkyl, or phenyl or benzyl opt. substd. by 1-3 of F, Cl, CF3, Me, OMe and NR9R10; R9, R10 = H, 1-4C alkyl or 1-4C perfluoroalkyl; x = 1-3; R1-R5 = H, 1-8C alkyl, 3-8C cycloalkyl, Or(CH2)aCbH2b+1, halogen or CN; provided that ≥ 1 of R1-R5, Ra and Rb = Or(CH2)aCbH2b+1.

公开(公告)号：CZ291188B6

公开(公告)日：2003-01-15

申请号：CZ231595

申请日：1995-09-08

Applicant: HOECHST AG

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

IPC: C07C279/22 ,  A01N1/02 ,  A61K31/155 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/47 ,  A61P1/16 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  A61P41/00 ,  A61P43/00 ,  C07D213/89 ,  C07D215/60 ,  C07D401/10

Abstract: In the present invention, there are disclosed benzoylguanidines of the general formula I, in which the general substituents have specific meanings, exhibit remarkable effect on heart circulation system. These compounds are obtained by reacting the compound of the general formula II, in which L represents a cleavable group, with guanidine. There is also described the use of these compounds for preparing medicaments and these medicaments per se containing such compounds. The compounds can be used particularly when treating heart arrhythmias.

公开(公告)号：ES2169453T3

公开(公告)日：2002-07-01

申请号：ES98105453

申请日：1998-03-26

Applicant: HOECHST AG

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

IPC: A61K31/155 ,  A61K31/165 ,  A61P3/06 ,  A61P9/00 ,  A61P9/06 ,  A61P9/10 ,  A61P11/00 ,  A61P13/02 ,  A61P15/00 ,  A61P25/00 ,  A61P35/00 ,  C07C279/10 ,  C07C279/20 ,  C07C279/22

Abstract: Benzoyl-guanidines of formula (I) and their salts are new. One of R2,R3 = H; and the other = -C(OH)MeCH2OH, -CHMeCH2OH or -C(OH)(Me)2; and R4 = Me, OMe, Cl or CF3 (preferably Me).

公开(公告)号：ES2168324T3

公开(公告)日：2002-06-16

申请号：ES95113845

申请日：1995-09-04

Applicant: HOECHST AG

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

IPC: C07C279/22 ,  A01N1/02 ,  A61K31/155 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/47 ,  A61P1/16 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  A61P41/00 ,  A61P43/00 ,  C07D213/89 ,  C07D215/60 ,  C07D401/10

Abstract: Benzoyl guanidine derivs. of formula (I) and their salts are new: one of R1-R3 = Het (linked by C or N), SR10, OR10, NR10R11 or CR10R11R12; and the other two of R1-R3 = H, halo, CN, X(CH2)p(CqF2q+1), SOuR22, CONR23R24, COR25, SO2NR26R27, 1-8C alkyl, 2-8C alkenyl, CmH2mR14, OR35 or NR35R36; R4, R5 = H, 1-4C alkyl, Fl, Cl, OR32, NR33R34 or CrF2r+1; R10 = CnH2n-Het; Het = 1-9C heteroaryl-N-oxide (opt. substd. by 1-3 F, Cl, CF3, OMe, OH, NH2, NHMe or NMe2); R11, R12 = as R10, H or 1-4C alkyl; R14 = 3-9C cycloalkyl or phenyl (opt. by 1-3 F, Cl, CF3, Me, OMe, NH2, NHMe or NMe2); R11, R12 = as R10, H or 1-4C alkyl; R14 = 3-8C cycloalkyl or phenyl (opt. substd. by 1-3 F, Cl, CF3, Me, OMe, NH2, NHMe or NMe2); X = a bond, O, S or NR28; R22 = 1-8C alkyl, 2-6C alkenyl, CmH2mR29 or CF3; R23, R25, R26 = H or as R22; R24, R27 = H or 1-4C alkyl; or R23 + R24, R26 + R27 = (CH2)4 or (CH2)5 (both opt. with a CH2 replaced by O, S, NH, NMe or N-benzyl); R28 = H or 1-3C alkyl; R29 = 3-7C cycloalkyl or phenyl (opt. mono- or tri-substd. by F, Cl, CF3, Me, OMe or NR30R31; R30, R31 = H or 1-4C alkyl; R35, R36 = H or 1-6C alkyl; or R35 + R36 = (CH2)y (opt with a CH2 replaced by O, S, NH, NMe or N-benzyl); R32-R34 = H or 1-3C alkyl; n, p, u = 0-2; m = 0-4; r = 1-4; q = 0-6; y = 4-7. Also claimed are cpds. of formula (IIIA); A = Cl, OR45, OH, OM or imidazol-1-yl; M = alkali or alkaline earth metal ion; and R45 = 1-8C alkyl or 1-4C alkylphenyl.

公开(公告)号：SI0811610T1

公开(公告)日：2002-04-30

申请号：SI9730284

申请日：1997-05-22

Applicant: HOECHST AG

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

IPC: A61K31/165 ,  A01N1/02 ,  A01N47/44 ,  A61K31/155 ,  A61P3/00 ,  A61P3/06 ,  A61P7/04 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P35/00 ,  C07C279/22 ,  C07C319/20 ,  C07C323/62

Abstract: Ortho-substituted benzoyl-guanidines of formula (I) and their salts are new: R = H; F; Cl; Br; I; CN; NO2; 1-8 C alkyl; 1-8 C alkoxy; 3-8 C cycloalkyl; 3-8 C cycloalkoxy; Xa-(CH2)b-(CF2)c-CF3; SR ; OR ; CR R R ; Ph, etc.;R or R = OCOR and the other = R ;R , R = H; 1-4C alkyl; 1-4C alkoxy; etc.;X = e.g. O; a = 0 or 1;b = 0-2;c = 0-3;R = -CfH2f-Q;Q = e.g. 3-8 C cycloalkyl;f = 0-2; R , R = H; 1-4 C alkyl; or R ; R = e.g. 1-8C alkyl.

公开(公告)号：SI0754680T1

公开(公告)日：2002-04-30

申请号：SI9630424

申请日：1996-07-15

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

Abstract: Benzoyl-guanidine derivs. of formula (I) and their salts are new: R1 = R4-SOm, R5R6N-SO2-, -Op-(CH2)q-(CF2)r-CF3, -SR10, -OR10 or -CR10R11R12; m = 1-2; R4, R5 = 1-8C alkyl, 3-6C alkenyl, CF3 or -CnH2n-R7; n = 0-4; R6 = H or 1-4C alkyl; R7 = 3-8C cycloalkyl or Ph (opt. substd. with 1-3 substits. from F, Cl, CF3, Me, OMe and NR8R9; R8, R9 = H or 1-4C alkyl; R5 = H; or R5 + R6 = 4-5C methylene group (with opt. replacement of a CH2 by O, S, NH, NMe or N-benzyl; ; p = 0-1; q = 0-2; r = 0-3;R10, R11, R12 = H, 1-8C alkyl, CsH2s-(3-8C cycloalkyl) or an aromatic gp. chosen from pyridyl, pyrrolyl, quinolyl, isoquinolyl, imidazolyl or Ph (in which the aromatic system may be opt. 1-3 times substd. by F, Cl, CF3, Me, OMe, OH, NH2, NHMe or N(Me)2; s = 0-2; R2 = -(CH2)u-(CF2)t-CF3; t = 0-3; u = 0-1; R3 = H or as for R1.

公开(公告)号：DK0700904T3

公开(公告)日：2002-03-18

申请号：DK95113845

申请日：1995-09-04

Applicant: HOECHST AG

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

IPC: C07C279/22 ,  A01N1/02 ,  A61K31/155 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/47 ,  A61P1/16 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  A61P41/00 ,  A61P43/00 ,  C07D213/89 ,  C07D215/60 ,  C07D401/10

Abstract: Benzoyl guanidine derivs. of formula (I) and their salts are new: one of R1-R3 = Het (linked by C or N), SR10, OR10, NR10R11 or CR10R11R12; and the other two of R1-R3 = H, halo, CN, X(CH2)p(CqF2q+1), SOuR22, CONR23R24, COR25, SO2NR26R27, 1-8C alkyl, 2-8C alkenyl, CmH2mR14, OR35 or NR35R36; R4, R5 = H, 1-4C alkyl, Fl, Cl, OR32, NR33R34 or CrF2r+1; R10 = CnH2n-Het; Het = 1-9C heteroaryl-N-oxide (opt. substd. by 1-3 F, Cl, CF3, OMe, OH, NH2, NHMe or NMe2); R11, R12 = as R10, H or 1-4C alkyl; R14 = 3-9C cycloalkyl or phenyl (opt. by 1-3 F, Cl, CF3, Me, OMe, NH2, NHMe or NMe2); R11, R12 = as R10, H or 1-4C alkyl; R14 = 3-8C cycloalkyl or phenyl (opt. substd. by 1-3 F, Cl, CF3, Me, OMe, NH2, NHMe or NMe2); X = a bond, O, S or NR28; R22 = 1-8C alkyl, 2-6C alkenyl, CmH2mR29 or CF3; R23, R25, R26 = H or as R22; R24, R27 = H or 1-4C alkyl; or R23 + R24, R26 + R27 = (CH2)4 or (CH2)5 (both opt. with a CH2 replaced by O, S, NH, NMe or N-benzyl); R28 = H or 1-3C alkyl; R29 = 3-7C cycloalkyl or phenyl (opt. mono- or tri-substd. by F, Cl, CF3, Me, OMe or NR30R31; R30, R31 = H or 1-4C alkyl; R35, R36 = H or 1-6C alkyl; or R35 + R36 = (CH2)y (opt with a CH2 replaced by O, S, NH, NMe or N-benzyl); R32-R34 = H or 1-3C alkyl; n, p, u = 0-2; m = 0-4; r = 1-4; q = 0-6; y = 4-7. Also claimed are cpds. of formula (IIIA); A = Cl, OR45, OH, OM or imidazol-1-yl; M = alkali or alkaline earth metal ion; and R45 = 1-8C alkyl or 1-4C alkylphenyl.