| 摘要 |
FIELD: organic chemistry, chemical technology, pharmacy. SUBSTANCE: invention relates to derivatives of N-(4-carbamimidophenyl)glycine-amide of the formula (I) where E means hydrogen atom or OH; Q means hydrogen atom or alkyl; R means alkyl, cycloalkyl or alkyl substituted with radicals R1, R2, R3 where R1 means hydrogen atom, COOH, COO-alkyl or aryl; R2 means hydrogen atom, aryl, cycloalkyl or heteroaryl; R3 means hydrogen atom, aryl or OH (at position distinct from alpha-position as regards to nitrogen atom to which alkyl group R is linked) or optionally substituted amino-group; three of radicals X1-X4 mean group C(Ra), C(Rb) or C(Rc) and fourth radical means C(Rd); Ra-Rd mean hydrogen atom, OH, NO2, dialkylamino-group, halogen atom, alkyl, alkoxy-group, aryloxy-group, aralkyloxy-group, heteroarylalkyloxy- group, hetero-cyclylalkyloxy-group, COOH, COO-alkyl, NH-SO2-alkyl, NH-SO2-aryl-group; two adjacent groups Ra-Rd mean alkylenedioxy-group; G1 and G2 mean hydrogen atom, hydroxy-group. Invention relates also to intermediate compounds of the formula (IV) , (V) , (VI) that are used in methods of synthesis of compounds of the formula (I) that involve interaction of aldehyde of the formula (II) with isonitrile of the formula R1NC and aminobenzamidine of the formula (III) and cyano-group CN in nitrile of the formula (IV) is converted to amidino-group of the formula C(N-G1)NH-G2. Except for, compounds of the formula (I) show inhibitory amidolytic activity with regards to the complex factor VIIa/tissue factor and owing to this property these compounds can be active substance in pharmaceutical composition. EFFECT: improved method of synthesis, valuable medicinal property of compounds. 12 cl
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