BASE-SUBSTITUTED BENZOYLGUANIDINES, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION, METHOD OF ITS PREPARING AND METHOD OF INHIBITION OF CELLULAR Na/H-ANTIPORTER Russian patent published in 2001 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes novel base- -substituted benzoylguanidines of the formula (I) where one of three substituents R(1), R(2) and R(3) has values R(6)-A-B-D- where R(6) means basic protonable residue, i. e. amino-group NR(7)R(8), amino-group R(7)R(8)N-C/=NR(9)/- or guanidine-group (a) where R(7), R(8), R(9) and R(10) mean independently each of other hydrogen atom or alkyl with 1-4 C-atoms; or R(7) and R(8) in common mean C_aH_2a where "a" = 4,5,6 or 7 being if a = 5, 6 or 7 then one methylene group of the group C_aH_2a can be replaced with heteroatom group O or NR(11) or R(8) and R(9) or R(9) and R(10( or R(7) and R(10) mean the group C_aH_2a where "a" = 2, 3, 4 or 5 being if a = 3, 4 or 5 then one methylene group of the group C_aH_2a can be replaced with heteroatom group O or NR(11); R(11) means hydrogen atom or methyl-group; or R(6) means imidazolyl, dihydroimidazolyl, benzimidazolyl, pyridyl, quinolyl, pyrrolidinyl or phenyl that if necessary can be substituted with (C₁-C₄)-alkyl; A means C_BH_2B where "b" = 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10 being in the group C_VH_2B one or two methylene groups can be replaced with one of the group taken among (d) or -So_aa/NR(19)/bb- where "aa" = 1 or 2; "bb" = 0 or 1; aa + bb = 2; R(19) means hydrogen atom or alkyl with 1-4 C-atoms; R(20) means hydrogen atom or methyl-group; B means phenylene residue of the formula (II) where R(12) and R(13) means hydrogen atom; D means C_dH_2d-X_f-; "d" = 0; "x" = -O-; "f" = 1 and other substituents R(1) and R(3) mean independently each of other hydrogen atom, F, Cl, Br, J, (C₁-C₈)-alkyl or R(17) means C_gH_gCO₂ where "g" = 0, 1, 2 ,3 or 4; R(17) means hydrogen atom or C_kF_2k+1- where "k" = 1, 2 or 3; R(4) and R(5) mean hydrogen atom. Invention relates to also pharmacologically tolerated salts of these compounds. Invention describes also method of their synthesis, pharmaceutical composition and method of its preparing and method of inhibition of cellular Na⁺/H⁺-antiporter. Compounds can be used as drug in diseases of cardio-vascular system. EFFECT: improved method of synthesis and inhibition, valuable medicinal properties. 9 cl, 4 tbl, 66 ex