SUBSTITUTED 2-NAPHTHOYL GUANIDINES, PROCESS OF THEIR PREPARATION, THEIR USE AS A MEDICAMENT OR A DIAGNOSTIC AGENT, AS WELL AS THE MEDICAMENT IN WHICH THEY ARE COMPRISED

摘要

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.