NITROCATECHOL DERIVATIVES AS COMP INHIBITORS Russian patent published in 2012 - IPC C07D413/04 C07D413/06 C07D413/14 C07D417/14 C07D401/04 C07D213/89 C07D407/04 C07D271/06 C07D271/10 A61K31/421 A61K31/4425 A61K31/4439 A61K31/506 A61P25/16 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of formula (I): where R₁ and R₂ represent hydrogen and a group which is hydrolysed in a physiological environment, optionally substituted lower alkanoyl or aroyl; X represents a methylene group; Y represents oxygen atom; n represents the number 0, 1, 2 or 3 and m represents the number 0 or 1; R₃ represents a group of pyridine N-oxide according to formula A, B or C which is attached as shown by an unmarked linking: where R₄, R₅, R₆ and R₇ independently represent aryl, heterocycle, hydrogen, C₁-C₆-alkyl, C₁-C₆-alkylthio, C₆-C₁₂-aryloxy or C₆-C₁₂-arylthio group, C₁-C₆-alkylsulphonyl or C₆-C₁₂-arylsulphonyl, halogen, C₁-C₆-haloalkyl, trifluoromethyl, or heteroaryl group; or where two or more residues R₄, R₅, R₆ and R₇ taken together represent an aromatic ring, and where P represents a central part, preferentially chosen from regioisomers 1,3,4-oxadiazol-2,5-diyl, 1,2,4-oxadiazol-3,5-diyl, 4-methyl-4H-1,2,4-triazol-3,5-diyl, 1,3,5-triazine-2,4-diyl, 1,2,4-triazine-3,5-diyl, 2H-tetrazol-2,5-diyl, 1,2,3-thiadiazol-4,5-diyl, 1-alkyl-3-(alkoxycarbonyl)-1R-pyrrol-2,5-diyl, where alkyl is presented by methyl, thiazol-2,4-diyl, 1H-pyrazol-1,5-diyl, pyrimidine-2,4-diyl, oxazol-2,4-diyl, carbonyl, 1H-imidazol-1,5-diyl, isoxazol-3,5-diyl, furan-2,4-diyl, benzole-1,3-diyl and (Z)-1-cyanoethene-1,2-diyl, and where the regioisomers of the central part include both regioisomers produced by exchanging the nitrocatechol fragment and the -(X)_n-(Y)_m-R₃ fragment. Also, the invention refers to a method for making a compound of formula I, as well as to a method for treating an individual suffering central and peripheral nervous system disorders, to a pharmaceutical composition based on the compounds of formula I, and also to their application for preparing the drug and as COMT inhibitor.

EFFECT: there are produced and described new compounds which show a potentially effective pharmaceutical properties in treating a number of central and peripheral nervous system disorders.

25 cl, 64 ex, 3 tbl