FIELD: organic chemistry, chemical technology, pharmacy. SUBSTANCE: invention describes derivatives of biphenyl of the formula (I) wherein each of R1, R4 means independently each of other the group C(=NH)-NH2, that can be substituted with group OH or the group CO-N=C(NH2)2, R3 means hydrogen atom, COOR6, -O-[C(R6)2]m-COOR6; X means [C(R6)2]n-, [C(R6)2]n-O-, -O-C(R6)2]n-; each of R2, R5 means hydrogen atom; R6 means hydrogen atom or A wherein A means alkyl with 1-6 carbon atoms; n = 0, 1 or 2; m = 1or 2 and their salts also. Invention describes method for preparing these compounds and their salts that involves conversion of compounds of the formula (I) wherein R1 and/or R4 means amidine group substituted with hydroxy-group to other compound of the formula (I) wherein R1 and/or R4 means amidine group and, if necessary, in prepared compounds of the formula (I) comprising ester group is hydrolyzed to carboxyl group, and/or, if necessary, prepared compounds as base or acid form are converted to one of their salts. Invention describes also pharmaceutical composition eliciting inhibitory effect on blood coagulating factor Xa based on compounds of the formula (I) and/or one of its physiologically acceptable salts and to method for its preparing from compound of he formula (I) and/or one of its physiologically acceptable salts and at least one solid, liquid or semiliquid carrier or accessory substance, and medicinal agent that is an inhibitor of blood coagulating factor Xa. Proposed compounds are inhibitors of blood coagulating factor. EFFECT: improved preparing method, valuable medicinal properties of compounds. 7 cl, 1 tbl, 14 ex
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Authors
Dates
2003-12-20—Published
1999-04-12—Filed