Ortho-substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them.

摘要

2-Alkoxy-benzoylguanidines of formula (I) and their salts are new. R1-R3 = 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, Ar, SR13, OR13, NHR13, NR13R14, CHR13R15, C(R15)(R16)OH, CCR18, CR19=CHR18 or (CR20R21)k-CO-(CR22R23)l-R24; R4 = 1-4C alkyl; Ar = phenyl, naphthyl, biphenylyl, or 1-9C heteroaryl (bonded via C or N) all optionally mono- to - tri-substituted by Z; Z = F, Cl, CF3, CH3, methoxy, OH, NH2, NHCH3, NH(CH3)2; X = O, S or NR5; R5 = H, 1-4C alkyl or CdH2d-R6; R6 = phenyl, biphenylyl, naphthyl (all optionally mono- to tri-substituted by Z') or 3-8C cycloalkyl; Z' = 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 by Z); R11, R12 = as R10, H, or 1-4C alkyl; R13, R14 = (CH2)g-(CHOH)h-(CH2)i-(CHOH)j-R17, (CH2)g-O-(CH2CH2O)h-R24; R15, R16 = H or 1-6C alkyl; or CR15R16 = 3-8C cycloalkyl; R17 = H or CH3; R18 = phenyl, 1-9C heteroaryl (optionally mono- to tri-substituted by Z'), 1-6C alkyl (optionally mono- to tri-substituted by OH) or 3-8C cycloalkyl; R19 - R23 = H or CH3; R24 = H, 1-6C alkyl, 3-8C cycloalkyl or CmH2m-R18; a = 0 or 1; b, f = 0-2; c =0-3; d, g, h, i, k, l = 0-4; j, m = 1-4;