AMIDINONAPHTYL DERIVATIVES AND PHARMACEUTICAL COMPOSITION Russian patent published in 2000 - IPC

FIELD: pharmaceutical industry. SUBSTANCE: described are amidinonaphthyl derivatives of general formula I wherein R¹ is hydrogen or -A-W-R⁴; A is group of formula , group of formula or -SO₂-; X is oxygen or sulfur atom; W is single bond or group of formula NR⁵, R⁴ is hydroxyl, lower alkoxy, lower alkyl which is substituted, or heteroaryl containing 1-2 heteroatoms selected from sulfur and nitrogen which is substituted provided that when w is group of formula NR⁵, R⁴ is further hydrogen atom, but is not hydroxy or lower alkoxy group; R⁵ is hydrogen atom, carbamoyl, lower alkoxycarbonyl, mono-or dilower alkylaminocarbonyl, lower alkylsulfonyl, mono- or dilower alkylaminothiocarbonyl, lower alkyl which is substituted, or lower alkanoyl which is substituted; R² is lower alkyl; R³ is hydrogen atom or lower alkoxycarbonyl; B is lower alkylene or carbonyl; n is 0 or 1, or pharmaceutically acceptable salts thereof. Said derivatives produce inhibiting effect against aggregation of thrombocytes caused by effect of activated factor X of coagulating blood system, and are useful as agents for preventing formation of thrombuses. Also described are intermediate products for preparing said derivatives and pharmaceutical compositions comprising said derivatives. EFFECT: improved properties of the pharmaceutical composition. 12 cl, 102 ex, 11 tbl