DERIVATIVES OF 4,1-BENZOXAZEPINE, PHARMACEUTICAL COMPOSITION, METHOD OF INHIBITION OF ACTIVITY OF SQUALENE SYNTHETASE IN MAMMALS, METHOD OF INHIBITION OF FUNGI GROWTH IN MAMMALS Russian patent published in 2000 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to derivatives of 4,1-benzoxazepine-2-one of the formula (I) where R¹ - hydrogen atom or lower alkyl, alkene, alkyne, C_3-9-cycloalkyl that can be substituted with 1-5 substituents as phenyl, naphthyl, C_1-6-cycloalkyl, furyl, indoline or halogen atom; R² and R³ - hydrogen atom, lower alkyl, phenyl possibly substituted with 1-3 substituents as halogen atom, alkyl, C_1-4-alkoxy-, hydroxy-group; and two vicinal substituents at phenyl group can form in common a ring or pyridine; X - a bond or group -(CH₂)_m-E-(CHR₆)_n-; m and n = 0, 1, 2 or 3; E - a bond or oxygen, sulfur atom, sulfoxide, sulfone, -NR₅-, -NHCO-, -CONR₇-, -NHCONH- (other values see p. 1 of the invention claim. Compounds of the formula (I) are useful for inhibition of activity of squalene synthetase and growth of fungi. EFFECT: enhanced antifungal effectiveness of compounds. 22 cl, 90 tbl, 167 ex