DERIVATIVES OF OCTAHYDRONAPHTHALENE OXIME, PHARMACEUTICAL COMPOSITION, METHOD OF THEIR SYNTHESIS, METHOD OF PATIENT TREATMENT

摘要

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to derivatives of octahydronaphthalene oxime of the formula (I) where X is C1-C10-alkyl; A is C1-C10-alkylene; R - hydrogen; Y - hydrogen, phenyl possibly substituted with substituents including: halogen, C1-C4-alkoxy or means heterocyclic group with 5 or 6 ring atoms, 1-3 of which are nitrogen and/or oxygen, and/or sulfur. Heterocyclic group can be substituted with at least a single C1-C5-alkyl. Invention describes a pharmaceutical composition for inhibition of cholesterol biosynthesis where an active component has a compound of the formula (I) or its pharmaceutically acceptable salts or esters taken at effective amount. Invention proposes a method of suppression of disorders as a result of cholesterol balance disturbance by administration to mammalian a compound of the formula (I) at the dose 1-10 mg/day. Invention proposes also a method of synthesis of derivatives of octahydronaphthalene oxime of the formula (I) by oxidation of compound of the formula (II) where R, X, Y and A are indicated above and R - a lower alkyl, lower alkenyl or phenyl resulting to synthesis of compound of the formula (III) where R, Y, R and A are indicated above followed by if necessary its deesterification or conversion to salt. EFFECT: improved method of synthesis, enhanced effectiveness of compounds. 19 cl, 1 dwg, 4 tbl, 23 ex