DERIVATIVES OF BENZAMIDINE, METHOD OF THEIR SYNTHESIS AND PHARMACEUTICAL COMPOSITION Russian patent published in 2002 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes derivatives of benzamidine of the general formula (I) where R¹ means C(=NH)-NH₂ that can be substituted once with group COA or -COOA; R² means H or A; R³ means A, cycloalkyl, -[C(R⁶)₂]_n-Ar, -[C(R⁶)₂]_n-O-Ar, -[C(R⁶)₂]_n-Het or -C(R⁶)₂-Ar; R⁶ means H; X is absent or means -CO-, -C(R⁶)₂-, -C(R⁶)₂-C(R⁶)₂, -C(R⁶)₂-CO-, -C(R⁶)₂, -C(R⁶)₂-CO- or NR⁶-CO-; Y means -C(R⁶)₂,-SO₂-, -CO-, -COO- or -CONR⁶-; A means alkyl with 1-20 C-atoms where one or two CH₂-groups can be substituted for O- or S-atoms either for CR⁶=CR⁶-groups and/or 1-7 H-atoms can be substituted for F; Ar means unsubstituted phenyl or naphthyl or said groups are mono-, di- or trisubstituted with group A, phenyl, OR⁶,N(R⁶)₂, Hal, NHCOA or COOR⁶; Het means 2-thienyl, 1,2,3,4-tetra-hydroquinoline-8-yl, 2,2,5,7,8-pentamethylchroman-6-yl, camphor-10-yl, 5-(1-methyl-5-trifluoromethyl-3-pyrazolyl)-2-thienyl, 5-benz-amidomethyl-2-thienyl, 1,3-dimethyl-5-chloro-4-pyrazolyl, 3,5-di-methyl-4-isoxazolyl, 3-methoxy-4-methoxycarbonyl-2-thienyl, pyridyl, benzo-[b]-thiophene-2-yl, 1,3-benzodioxol-5-yl, dibenzofuran-2-yl; Hal means F, Cl, Br or J; n = 0, 1 or 2. Invention relates also to method of their synthesis and pharmaceutical composition. Said compounds are inhibitors of coagulating factor Xa and can be used for prophylaxis and therapy of thromboembolic diseases. EFFECT: improved method of synthesis, valuable medicinal properties. 5 cl