INCLUSION COMPLEXES OF DERIVATIVES OF 1,2,5-OXA- -DIAZOLE-2-OXIDE WITH POLYCYCLIC DERIVATIVES OF GLUCOPYRANOSE, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION Russian patent published in 2002 - IPC

FIELD: organic chemistry, biochemistry, pharmacy. SUBSTANCE: invention relates to novel inclusion complexes of derivatives of 1,2,5-oxadiazole-2-oxide of the general formula (I) where R¹ = R² is CN or in common with adjacent carbon atoms form annelated 3,6-bis-(lower alkyl)-pyridazine-1,2-dioxide cycle with polycyclic derivatives of glucopyranose of the general formula (II) where if n = 1 then R³ means a fragment of 11-oxo-18β, 20β-olean-12-ene-29-oic acid of the formula (III) R⁴ is H; R⁵ is β-D-glucopyranosyl; R⁶ = R⁷ is H; R⁸ means C(O)OH; and if n = 7 then R³ is H; R⁴ and R⁷ are direct bonds; R⁵ and R⁶ mean H or (CH₂CH(CH₃)O)_mH where m = 1-14; R⁸ means -CH₂OH or CH₂O(CH₂CH(CH₃)O)_mH where m = 1-14. New compounds produce nitrogen oxide and activate the soluble form of guanylate cyclase and relate to spasmolytic, vasodilating and hypotensive agents of rapid effect and they are inhibitors of platelet aggregation. Invention relates to a method of their synthesis and pharmaceutical compositions based on thereof. The proposed compounds are synthesized by the method involving interaction of the parent derivative of 1,2,5-oxadiazole-2-oxide of the above given formula (I) where and R² have the indicated values with the corresponding polycyclic derivative of glucopyranose of the above given general formula (II) where R³-R⁸ have the indicated values. Synthesis is carried out in an aqueous-organic medium (for example, in an aqueous solution of dioxane, lower alkanol, in part ethanol, or a mixture of organic solvents) at increased temperature 30-60 C followed by isolation of the end product by evaporation under decreased pressure, its washing out with low-polar inert organic solvent (diethyl ether or its mixture with hexane) and drying under decreased pressure. Novel inclusion complexes are effective donors of NO and produce its redox-form (nitroxyl) also, form nitrosothiols and activate guanylate cyclase soluble form and show also spasmolytic, vasodialting and rapid hypotensive effect. The described compounds show the expressed anti-aggregative properties also. EFFECT: valuable medicinal properties. 16 cl, 4 dwg, 6 tbl