INHIBITORS OF XA FACTOR Russian patent published in 2000 - IPC

FIELD: organic chemistry. SUBSTANCE: invention describes compound of unnatural origin that inhibits activity of Xa factor and has the general formula (I): A1-A2-(A3)_m-B where m = 0 or 1; A1 means R₁-R₂-R₃; A3 means A3; R₇-R₈-R₉ is taken among the group including R₁; where X means N and and are taken independently among the group including H, alkyl, acyl, aryl, arylalkyl and groups protecting amino-group; R₂ means -CR₉₉R₁₀₀ where R₉₉ and R₁₀₀ are taken independently among the group including H, alkyl, arylalkyl, heteroarylalkyl and heteroaryl; R₃ means -C(O)- or -CH₂-;R₄ means -NR₅₀- where R₅₀ means H; R₅ means -CR₂₀₁R₂₀₂ where R₂₀₁ and R₂₀₂ are taken independently among the group including H, alkyl, aryl and arylalkyl; R₆ means -C(O)- or -CH₂-; R₇ means -NR₅₁ where R₅₁ means H; R₈ means -CR₂₁₀R₂₁₁- where R₂₁₀ and R₂₁₁ are taken independently among the group including H, alkyl, arylalkyl and heterocycle being alkyl, alkylaryl and heterocycle can be substituted with Q or -(CH₂)_n-Q where n = 1-5 and Q is taken among the group including amine-, amidine-, imidazole- or guanidine-group that can be substituted and mono-, di-, tri- or tetraalkylammonium of pharmaceutically acceptable salt, its isoureide or isothioureide; R₉ means -C(O)- or -CH₂-; B means -NHR₅₂ where R₅₂ is taken among the group including H, alkyl, arylalkyl, heteroarylalkyl, heteroaryl, one amino acid or two amino acids, or its pharmaceutically acceptable salt, amide, ester, alcohol or aldehyde. Compound of the formula (I) prevents blood clot formation and it is the specific low-molecular inhibitor of Xa factor. EFFECT: enhanced effectiveness of compound, absence of nondesirable adverse effects, valuable pharmacological properties. 28 cl, 5 tbl, 4 dwg, 38 ex