PRODRUGS OF 3-ACYL-2-HYDROXYINDOLE-1-CARBOXAMIDES, PHARMACEUTICAL COMPOSITION Russian patent published in 1999 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to prodrugs of 3-acyl-2-hydroxy- -indole-1-carboxamide of the formula (I) where R means fragments of the formulas (II) , (III) , (IV) , (V) and (VI) where X = 0 or 1; A is C_1-5--alkylene optionally substituted with 1-2 C_3-7--cycloalkyls, or phenylene group; B is C_2-5--alkenylphenyl, pyridyl, piperidinyl, pyrrolidinyl, -OCH₂CO₂-R¹ or -OCH₂CONR²R³ where R¹ - H, alkyl, phenyl-lower alkyl or (CH₂)_pCONR²R³ where R² and R³ - H, alkyl or together with bound nitrogen atom they form morpholine group; R⁴ and R⁵ - H, alkyl, (CH₂)_pCO-NR⁴R³, (CH₂)_pNR⁷R⁸, (CH₂)_pOR⁶ or (CH₂)_pSR⁶ where R⁶ - H, alkyl, C_3-7--cycloalkyl optionally substituted with 1-2 alkyl groups, or taken together with a substituent and bound oxygen atom they form tetrahydrofuran ring; R⁷ and R⁸ - H; R⁹ - H or methyl; R¹⁰ and R¹¹ - halogen; R¹² and R¹³ - H, halogen; p = 1-3. Compounds of the formula (I) are enol ester or ether prodrugs of hydroxyindole showing analgetic and antiinflammatory effect. EFFECT: improved method of synthesis, enhanced effectiveness. 15 cl, 1 tbl, 35 ex