AROMATIC AMIDINE DERIVATIVE AND PHARMACEUTICAL COMPOSITION Russian patent published in 1999 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes new aromatic amidine derivatives of the general formula (I) where R₂ means hydrogen atom or lower alkoxy-group; R₂ means hydrogen atom, lower alkyl group, lower alkoxy-group, carboxyl-group, carboxyalkyl-group with 2-5 carbon atoms or alkoxycarbonyl-group with 2-5 carbon atoms; R₃ means hydrogen atom, carboxyl-group, carboxyalkyl-group with 2-5 carbon atoms, alkoxycarbonylalkyl-group with 3-6 carbon atoms, carboxyalkoxyl-group with 2-5 carbon atoms and alkoxycarbonylalkoxyl-group with 3-6 carbon atoms; R₄ means hydrogen atom, hydroxyl group or lower alkoxy-group; n is the whole number from 0 to 2; A is alkylene group with 1-4 carbon atoms that can be substituted with one or two substituents taken among hydroxyalkyl-group with 1-4 carbon atoms, carboxyl, alkoxycarbonyl-group with 2-5 carbon atoms and carboxyalkyl-group with 2-5 carbon atoms; X is a simple bond, oxygen or sulfur atom or carbonyl-group; Y is saturated or unsaturated 5- or 6-membered heterocyclic fragment containing one or two heteroatoms taken among nitrogen, oxygen, sulfur atoms or cyclic hydrocarbon fragment that can be substituted with amino-group, carbamoyl, mono- or dialkylcarbamoyl, alkanoimido-yl, lower alkyl, lower alkanoyl, alkoxycarbonylimine, benzylimidoyl, alkanoylamino-group, alkylamine; saturated or unsaturated 5- or 6-membered cyclic hydrocarbon fragment that can be substituted with aminoalkyl-group or alkanoylamino-alkyl-group; or Y is amino-group that can be substituted with pyrrolidinyl or pyridinyl group; and the group of the formula (II) is taken among indolyl, benzofuranyl, benzothienyl, benzothiazolyl, naphthyl, tetrahydronaphthyl, benzimidazolyl; or its pharmaceutically acceptable salt. The end compounds show the strong anticoagulating effect by reversible inhibition of blood activated clotting factor ("FXA"). Invention describes also an anticoagulating composition based on compounds of the formula (I). EFFECT: new amidine derivatives, an anticlotting activity. 12 cl, 5 tbl, 134 ex