NOVEL INHIBITORS OF METALLOPROTEINASES Russian patent published in 2003 - IPC

FIELD: organic chemistry, biochemistry, enzymes. SUBSTANCE: invention relates to novel compounds of the general formula (I): where R¹ is taken among a group consisting of hydrogen atom, unsubstituted or optionally substituted aralkyl, substituted or optionally substituted aralkyloxycarbonyl, unsubstituted or optionally substituted alkyloxy-carbonyl, unsubstituted or optionally substituted alkyl and hydroxy-protective group; R² is taken among a group consisting of hydrogen atom, unsubstituted or optionally substituted aralkyloxycarbonyl, unsubstituted or optionally substituted alkyloxycarbonyl, amino-protecting group; R³ is taken among a group consisting of hydrogen atom, unsubstituted or optionally substituted alkyl and unsubstituted or optionally substituted aralkyl; R⁴ is taken among a group consisting of unsubstituted or optionally substituted alkyl and unsubstituted or optionally substituted aralkyl; R⁵ and R⁶ can be similar or different being each is taken independently among a group consisting of hydrogen atom, unsubstituted or optionally substituted alkyl, unsubstituted or optionally substituted cycloalkyl, unsubstituted or optionally substituted heterocyclic group and amino-protecting group; or R⁵ and R⁶ taken in common with nitrogen atom to which they are bound form unsubstituted or optionally substituted heterocyclic group; R⁷ is taken among a group consisting of hydrogen atom, hydroxy-group, unsubstituted or optionally substituted alkyl and unsubstituted or optionally substituted aralkyl; R⁸ is taken among a group consisting of hydrogen atom, hydroxy-group, unsubstituted or optionally substituted alkyl and unsubstituted or optionally substituted aralkyl; R⁹ is taken among a group consisting of hydrogen atom, hydroxy-group, amino-group and group of the formula: -X-Y where X is taken among a group consisting of unsubstituted or optionally substituted (C₁-C₆)-alkylene and unsubstituted or optionally substituted phenylene; Y means a group of the formula: -A-B or B where A is taken among a group consisting of unsubstituted or optionally substituted (C₁-C₆)-alkylene, imino-group and unsubstituted or optionally substituted (C₁-C₆)- alkyleneimino-group; B is taken among a group consisting of hydrogen atom, amino-group, amidino-group, acylamidoyl-group, unprotected or optionally protected bis-(phosphono)-methyl under condition that R⁷, R⁸ and R do not mean simultaneously methyl, or its pharmaceutically acceptable salts. Invention relates also to two different methods of synthesis of compounds of the formula (I), intermediate compounds of formulas (III) , (IV) and (VI) used for synthesis of compounds of the formula (I), method of synthesis of compound of the formula (I), to pharmaceutical or veterinary composition and inhibitor of metalloproteinase. EFFECT: improved methods of synthesis, valuable biochemical properties of compounds. 15 cl, 4 tbl, 107 ex