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    Substituted benzoylguanidines, process for their preparation, their use as medicaments as well as medicament containing them.
    96.
    发明专利
    Substituted benzoylguanidines, process for their preparation, their use as medicaments as well as medicament containing them. 未知

    公开(公告)号：GR3024927T3

    公开(公告)日：1998-01-30

    申请号：GR970402568

    申请日：1997-10-03

    Applicant: HOECHST AG

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

    IPC: A61K31/165 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  C07C277/08 ,  C07C279/22 ,  C07C311/15 ,  C07C317/44 ,  C07C317/46 ,  C07C323/62 ,  C07D241/28

    Abstract: There are described benzoylguanidines of the formula I where R(1) is H, Hal, -NO2, -C IDENTICAL N, Xo-(CH2)p-(CF2)q-CF3, R(5)- SOm, R(6)-CO- or R(6)R(7)NO-SO2-, where X is O, S, NR(14), m is 0-2, o is 0, 1, p is 0-2, q is 0-6, R(5) and R(6) are alk(en)yl, -CnH2n-R(8), CF3, n is 0-4, R(8) is cycloalkyl, phenyl, R(6) also being H, R(2) is where Y is O, -S- or -NR(12)-; R(11), R(12) = H, alkyl, and h is zero or 1, and i, j and k are 0-4, but where h, i and k are not simultaneously zero, R(3) is defined as R(1), or is alkyl, -X-R(13) where X is O, S, NR(14), R(14) is H, alkyl, R(13) is H, (cyclo)alkyl, -CbH2b-R(15) where b is 0-4, R(15) is phenyl, R(4) is H, -OR(16) or -NR(16)R(17) where R(16), R(17) are H, alkyl and their pharmaceutically tolerable salts. They are obtained from a compound II by reaction with guanidine, in which R(1) to R(4) have the meaning indicated and L is a leaving group which can be easily nucleophilically substituted. The compounds are outstandingly suitable as antiarrhythmic medicaments having a cardioprotective component for infarct prophylaxis and infarct treatment and also for the treatment of angina pectoris, where they also preventively inhibit or severely decrease the pathophysiological processes in the formation of ischaemically induced damage, in particular in the elicitation of ischaemically induced cardiac arrhythmias.

    99.
    发明专利
    未知

    公开(公告)号：DE19621483A1

    公开(公告)日：1997-12-04

    申请号：DE19621483

    申请日：1996-05-29

    Applicant: HOECHST AG

    Inventor： BRENDEL JOACHIM DR ,  KLEEMANN HEINZ-WERNER DR ,  ENGLERT HEINRICH CHRISTIAN DR ,  LANG HANS JOCHEN DR ,  SCHWARK JAN-ROBERT DR ,  WEICHERT ANDREAS DR ,  LAL BANSI

    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.

    100.
    发明专利
    未知

    公开(公告)号：DE19608161A1

    公开(公告)日：1997-09-11

    申请号：DE19608161

    申请日：1996-03-04

    Applicant: HOECHST AG

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

    IPC: A61K31/165 ,  A01N1/02 ,  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 ,  C07C277/08 ,  C07D215/02 ,  C07D217/02 ,  C07D213/04

    Abstract: Ortho-substituted benzoyl-guanidines of formula (I) and their salts are new: where R1 = H, F, Cl, Br, I, CN, NO2, 1-8C alkyl, 1-8C alkoxy, 3-8C cycloalkyl, 3-8C cycloalkoxy, Xa-(CH2)b-(CF2)c-CF3, SR10, OR10, CR10R11R12; or phenyl, naphthyl, biphenylyl, or 1-9C (sic) heteroaryl bonded via C or N and all optionally mono- to tri-substituted with F, Cl, CF3, CH3, methoxy, OH, NH2, NHCH3, NH(CH3)2; or SR13, OR13, NHR13, NR13R14, CHR13R15, CR15R16-OH, C IDENTICAL CR18, CR19=CHR18, ÄCR20R21Ük-CO, ÄCR22R23Ül-R24; one of R2, R3 = hydroxy the other as R1; R4 = 1-4C alkyl, 1-4C alkoxy, F, Cl, Br, I or (CH2)n-(CF2)o-CF3; X = O, S, NR5; a = 0-1; b = 0-2; c = 0-3; R5 = H, 1-4C alkyl, CdH2d-R6; d = 0-4; R6 = 3-8C cycloalkyl; or phenyl, biphenylyl or naphthyl (each optionally mono- to tri-substituted with F, Cl, CF3, methyl, methoxy, or NR7R8); R7, R8 = H or 1-4C alkyl; R10 = CfH2f-3-8C cycloalkyl; or phenyl optionally mono- to tri-substituted with F, Cl, CF3, CH3, methoxy, OH, NH2, NHCH3, NH(CH3)2; f = 0-2; R11, R12 = as R10, H or 1-4C alkyl; k = 0-4; l = 0-4; R13, R14 = (CH2)g-(CHOH)h-(CH2)i-(CHOH)j-R17, or (CH2)g-O-(CH2CH2O)h-R24; R17 = H, CH3; g, h, i = 0-4; j = 1-4; R15, R16 = H or 1-6C alkyl; or CR15R16 = 3-8C cycloalkyl; R18 = phenyl optionally mono- to tri-substituted with F, Cl, CF3, CH3, OCH3 or NR25R26; or 3-8C cycloalkyl; or 1-9C (sic) heteroaryl optionally substituted as for phenyl; or 1-6C alkyl optionally substituted by 1-3 OH; R25, R26 = H or 1-4C alkyl; R19-R23 = H or CH3; R24 = H, 1-6C alkyl, 3-8C cycloalkyl, CmH2m-R18; m = 1-4; n = 0-1; and o = 0-1.

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