DERIVATIVES OF 4,1-BENZOXAZEPINE Russian patent published in 2001 - IPC

FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to novel derivatives of 4,1-benzoxazepine-2-one of the formula (I) where R¹ is lower alkyl substituted at least with one optionally substituted hydroxyl group; R² and R³ mean independently each of other hydrogen atom or phenyl that is substituted with 1-3 substitutes taken among the group including lower C₁-C₄- alkoxy-groups; X means a bond, methylene group or binding group with chain length 1-7 atoms taken among the group including -(CH₂)_m-E-(CHR₆)_n- where m and n mean independently each of other 1 or 2; E is a bond or oxygen atom, -NR₅-, -CONR₇- where R₅ means methylsulfonyl-group; R₆ and R₇ mean independently each of other: (i) hydrogen atom; (ii) unsubstituted lower alkyl or lower alkyl substituted with substitutes taken among the group including piperidine, indolyl and possibly esterified carboxy-groups; (iii) benzyl; Y means optionally substituted carbamoyl and/or substitutes at N-atom of carbamoyl group taken in common they form a ring that can be substituted, or tetrazolyl, or piperidine, and ring A is substituted with 1-3 substituted taken among the group including halogen atoms, or their salts. Invention relates to also two particular compounds. Compounds show inhibitory effect on activity of squalene synthetase and antifungal effects. Invention can be used in treatment of patients with hyperlipemia and arteriosclerosis. EFFECT: new compounds indicated above, valuable medicinal properties. 6 cl, 8 tbl, 22 ex