DERIVATIVES OF N-(4-CARBAMIMIDOPHENYL)GLYCINE-AMIDE, INTERMEDIATE COMPOUNDS, METHOD OF SYNTHESIS AND PHARMACEUTICAL COMPOSITION Russian patent published in 2003 - IPC

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 α-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(R^a), C(R^b) or C(R^c) and fourth radical means C(R^d); R^a-R^d 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 R^a-R^d 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