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    52.
    发明专利
    未知

    公开(公告)号：AT138646T

    公开(公告)日：1996-06-15

    申请号：AT93119781

    申请日：1993-12-08

    Applicant: HOECHST AG

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

    IPC: A61K31/165 ,  A61K31/155 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  C07C279/22 ,  C07C311/08 ,  C07C317/44 ,  C07C317/46 ,  C07C317/48 ,  C07C323/62 ,  C07C323/65 ,  C07D213/56 ,  C07D233/54 ,  C07D239/26 ,  C07D257/02 ,  C07D257/04

    Abstract: Benzoylguanidines of the formula I where R(1) is hydrogen, Hal, -NO2, -CN, -CF3, R(4)-SOm or R(5)R(6)N-SO2-, where m is zero to 2, R(4) and R(5) are alk(en)yl or -CnH2n-R(7), n is zero to 4, with R(5) also having the meaning of H, and R(6) is H or (C1-C4)-alkyl, with R(5) and R(6) together being able to be 4 or 5 methylene groups, R(2) is -SR(10), -OR(10), -NHR(10), -NR(10)R(11), -CHR(10)R(12), with R(10) and R(11) being identical or different and being -[CHR(16)]s-(CH2)p-(CHOH)q-(CH2)r-(CH2OH)t-R(21) or -(CH2)p-O(CH2-CH2O)q-R(21), R(12) and R(13) being hydrogen or alkyl, or forming a cycloalkyl together with the carbon atom carrying them, R(14) being H, (cyclo)alkyl or -CnH2n-R(15), R(3) is defined as R(1) or is alkyl, hydrogen or -X-R(22), where X is oxygen, S or NR(16), are described, as are the pharmaceutically tolerated salts thereof. The compounds I possess very good anti-arrhythmic properties but do not have any undesirable salidiuretic properties. In addition to this, they are notable for their strong inhibitory effect on the proliferation of cells.

    58.
    发明专利
    未知

    公开(公告)号：DE4318658A1

    公开(公告)日：1994-12-08

    申请号：DE4318658

    申请日：1993-06-04

    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 ,  C07C313/10 ,  C07C317/14 ,  C07C321/28 ,  A61K31/155

    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.

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