BENZAMIDINE DERIVATIVES, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION, METHOD FOR ITS PREPARING AND MEDICINAL AGENT

摘要

FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to derivatives of benzamidine of the formula (I) where R¹ means C(=NH); NH₂ R² means hydrogen atom; R³ means -[C(R⁵)₂]_m-COOR⁵; R³ and X in common mean also - CO-N- forming 5-membered ring being R³ means C=O and X means nitrogen atom; R⁴ means A, cycloalkyl, -[C(R⁵)₂]_mAr; X means oxygen atom, NR⁵ or CH₂; Y means oxygen atom, ; W means linkage, -SO₂-, - CO- or -CONR⁵-. Compounds are inhibitor of blood coagulation factor Xa and can be used for prophylaxis and therapy of thromboembolic diseases. Invention describes also method of synthesis of compounds, pharmaceutical composition based on thereof and medicinal agent. EFFECT: improved method of synthesis and preparing, valuable medicinal property of compounds. 7 cl, 1 tbl, 29 ex