| 摘要 |
of the disclosure Substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament containing them Benzoylguanidines of the formula I <IMG> I are described in which: R(1) is R(6)-CO or R(7)R(8)N-CO, with R(6), R(7) and R(8) being (perfluoro)alk(en)yl or -(CH)2n-R(9), R(9) being cycloalkyl, phenyl, biphenylyl or naphthyl, where R(7) and R(8) can together be 4 or 5 methylene groups of which one CH2 group can be replaced by oxygen, S, NH, N-CH3 or N-benzyl; R(2) is defined as R(1), or is H, Hal, CN, NO2, (per fluoro)alk(en)yl or -(CH)2R(15) with R(15) being cycloalkyl, phenyl, biphenylyl or naphthyl, or R(2) is (C1-C9)-heteroaryl, or R(2) is SR(18), -OR(18), -NR(18)R(19) or -CR(18)R(19)R(20); R(18) is -(CH2)-heteroaryl, R(19) and R(20) are defined as R(18) or are H or (perfluoro)alkyl, or R(2) is R(21)-SOm or R(22)R(23)N-SO2-, with R(21) being (perfluoro)alk(en)yl or -CH2-R(24), R(24) being cycloalkyl, phenyl, biphenylyl or naphthyl, R(22) being H, (perfluoro)alk(en)yl or -(CH2)n-R(29), R(29) being (C3-C8)-cycloalkyl, phenyl, biphenylyl or naphthyl, R(23) being H or (perfluoro)alkyl, where R(22) and R(23) can together be 4 or 5 methylene groups of which one CH2 group can be replaced by oxygen, S, NH, N-CH3 or N-benzyl; or R(2) is R(33)X-, where X is oxygen, S, NR(34), (D=O)A- or NR(34)C=MN(+)R(35)-, with M being oxygen or S, A being oxyyen or NR(34), D being C or SO R(33) and R(35) being (perfluoro)alk(en)yl or -(CH2)n-R(36), where R(36) is cycloalkyl, phenyl, biphenylyl or naphthyl, R(34) being H or (perfluoro)alkyl, where A and N(*) are bonded to the phenyl nucleus of the benzoylguanidine parent substance; or R(2) is -SR(40), -OR(40), -NHR(40), -NR(40)R(41), -CHR(40)R(42), <IMG> <IMG> , <IMG> , <IMG> where R(40) and R(41) are identical or different and are -(CH2)p-(CHOH)q-(CH2)r-(CH OH)tR(51) or -(CH2)p-O-(CH2-CH2O)q-R(51), R(51) is hydrogen or methyl, R(42) and R(43) are hydrogen or alkyl, or, together with the carbon atom carrying them, form a (C3-C8)-cycloalkyl; R(44) is H, (C1-C6)-alkyl, (C3-C8)-cycloalkyl or -CeH2e-R(45) with R(45) being phenyl, heteroaryl or alkyl, R(46), R(47), R(48), R(49) and R(50) are hydrogen or methyl; or R(2) is R(55)-NH-SO2-, R(3), R(4) and R(5) are, independently of each other, defined as R(1) or R(2); and pharmaceutically tolerated salts thereof.
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