FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to derivatives of benzamidine of the formula (I) or its pharmaceutically acceptable salts wherein R1 means hydrogen, halogen atom, C1-C6-alkyl group or hydroxyl group; R2 means hydrogen, halogen atom or C1-C6-alkyl group; R3 means hydrogen atom, C1-C6-alkyl group, C1-C6-alkyl group that is substituted with hydroxyl group, carboxyl group or (C1-C6-alkoxy)-carbonyl group, C7-C15-aralkyl group, C1-C6-alkanoyl group, hydroxy-C2-C6-alkanoyl group, C1-C6-alkylsulfonyl group or C1-C6-alkylsulfonyl group that is substituted with carboxyl group or (C1-C6-alkoxy)-carbonyl group; R4 and R5 are similar or different and each means hydrogen, halogen atom, C1-C6-alkyl group, halogen-C1-C6-alkyl group, C1-C6-alkoxy-group, carboxyl group, (C1-C6-alkoxy)-carbonyl group, carbamoyl group, (C1-C6-alkyl)-carbamoyl group or di-(C1-C6-alkyl)-carbamoyl group; R6 means 1-acetimidoylpyrrolidine-3-yl group or 1-acetimdoylpiperidine-4-yl group. Compounds of the formula (I) elicit inhibitory activity with respect to Xa factor that allows their using in pharmaceutical composition for treatment and prophylaxis of blood coagulation disorders. EFFECT: valuable medicinal properties of compounds. 42 cl, 3 tbl, 200 ex
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Authors
Dates
2004-01-27—Published
2000-10-25—Filed