| 摘要 |
FIELD: organic chemistry, biochemistry, medicine, pharmacy. ^ SUBSTANCE: invention relates to new derivatives of phenylglycine of the formula (I) , to their hydrates or solvates, and/or to physiologically acceptable salts and/or physiologically acceptable esters possessing inhibitory effect on amidolytic activity of the complex factor VIIa/tissue factor that can be used for therapeutic and/or prophylactic treatment of diseases, for example, thrombosis. In the formula (I) R1 means (C1-C6)-alkyl; R2 means hydrogen atom, hydroxy-(C1-C6)-alkoxy-, (C1-C6)-alkoxycarbonyloxy-, (C1-C6)-alkoxy-group or halogen-(C1-C6)-alkoxycarbonyloxy-(C1-C6)-alkoxy-group; R3 means hydrogen atom, (C1-C6)-alkoxy- or heterocycloalkyloxy-group wherein heterocycloalkyl group means 5-6-membered ring comprising a heteroatom taken among nitrogen and oxygen atom; R4 means hydrogen atom or ester residue that is cleaved off under physiological conditions. R5 means hydrogen atom, hydroxy-group, (C1-C6)-alkoxycarbonyl, halogen-(C1-C6)-alkoxycarbonyl, (C6)-aryloxycarbonyl,(C6)-arylalkoxycarbonyl, (C1-C6)-alkoxy-(C1-C6)-alkoxy(C1-C6)-alkoxycarbonyl, (C3-C6)-cycloalkyloxycarbonyl, (C2-C6)-alkynyloxycarbonyl, 5-methyl-2-oxo[1,3]dioxol-4-yl-methoxycarbonyl, (C6)-arylcarbonyloxy-, (C1-C6)-alkylaminocarbonyloxy-group, (C1-C6)-alkylcarbonyl, arylcarbonyl, arylaminocarbonyl or heteroarylcarbonyl wherein heteroaryl represents 5-6-membered ring comprising nitrogen atom the cycle; X means atom F, Cl or Br. Also, invention relates to a method for preparing compounds, intermediates substances and pharmaceutical composition and a method for treatment. ^ EFFECT: improved preparing method, valuable medicinal properties of agents and composition. ^ 29 cl, 5 ex |
