Fluoro-alkyl/alkenyl-substituted benzoylguanidinens and their use as medicament or diagnostic agent

摘要

Benzoylguanidines of formula (I) and their salts are new. R1 and R3 = H, halogen, CN, NO2, 1-8C alkyl, 3-8C cycloalkyl, Oa(CH2)b(CF2)cCF3, S(O)mR5, SO2NR6R7, SR11, OR11, CR11R12R13 or phenyl, naphthyl, biphenylyl or C- or N-bonded 1-9C heteroaryl gps. opt. substd. by 1-3 of F, Cl, CF3, Me, OMe, OH, NH2, NHMe and NMe2; a = 0 or 1; b = 0-2; c = 0-3; m = 0-2; R5 = 1-8C alkyl, 3-6C alkenyl, CF3 or CnH2n-R8; R6 = H, or as for R5; R7 = H or 1-4C alkyl; or R6+R7 = tetra- or pentamethylene, opt. with a CH2 gp. replaced by O, S, NH, NMe or NCH2Ph; n = 0-4; R8 = 3-7C cycloalkyl, or phenyl opt. substd. by 1-3 of F, Cl, CF3, Me, OMe and NR9R10; R9 and R10 = H or 1-4C alkyl; R11 = 3-8C cycloalkyl; (3-8C)cycloalkyl(1-2C)alkyl; or 1-9C heteroaryl or phenyl opt. substd. by 1-3 of F, Cl, CF3, OMe, OH, NH2, NHMe and NMe2; R12 and R13 = H, 1-4C alkyl or gps. as defined for R11; R2 = CF2R14, CF(R15)(R16), CF(Rf)-R15 or CRf=C(R15)(R16); R14 = 1-4C alkyl or 3-6C cycloalkyl; R15 and R16 = H or 1-4C alkyl; Rf = 1-3C perfluoro-n-alkyl; R4 = H, 1-3C alkyl, F, Cl, Br, I, CN or (CH2)s(CF2)tCF3; s = 0 or 1; t = 0-2.