FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to a substituted azol derivative presented by the following formula (I)
3-(4-benzyloxy-3,5-dimethyl-phenyl)-isoxazol-5-ylmethyl ester of carbamic acid, 3-(4-prop-2-inyl-oxyphenyl)-isoxazol-5-ylmethyl ester of carbamic acid or 2-{[3-(4-benzyloxy-phenyl)-isoxazol-5-ylmethyl]-amino}-propionamide or its pharmaceutically acceptable salt, wherein R is specified in a group consisting of C4-C15 arylalkyl unsubstituted or substituted by at least one substitute specified in a group consisting of halogen, trifluoromethyl, trifluoralkoxy, -NO2, C(=O)OCH3, linear or branched C1-C6 alkyl, C1-C6 alkoxy, phenyl, phenyloxy, benzyloxy, -C(=O)H, -OH and -C=N-OH; C4-C15 heteroarylalkyl unsubstituted or substituted by at least one substitute specified in a group consisting of halogen, C(=O)OCH3, linear or branched C1-C6 alkyl, C1-C6 alkoxy, phenyl, phenyloxy, benzyloxy; linear, branched or cyclic C1-C10 alkyl substituted by at least one substitute specified in a group consisting of C1-C3-alkyloxy, C1-C3 alkylthio, carbamate, tert-butyl-OC(=O)NH-, -NH3 +, -NH2, -OH, -C(=O)OCH2CH3, -NHC(=O)NH2, trifluoromethylsulphanyl, trifluoromethyl and -CN; wherein when R represents C4-C15-heteroarylalkyl, a heteroaryl group is specified in a group consisting of imidazol, chlorthiophen, benzothiazol, pyridine, quinoline, benzotriazol, isoxazol, furan, N-oxopyridine, N-methylpyridine and benzo[1,3]dioxol, and when R means C4-C15 arylalkyl, wherein aryl is specified in a group consisting of phenyl, phenyloxy, benzyloxy and naphthalinyl, Y is specified in a group consisting of O and N - R1, R1 means a substitute specified in a group consisting of H and linear or branched C1-C3 alkyl; R2 is specified in a group consisting of H and halogen; A is specified in a group consisting of O and S; B represents C; Z is specified in a group consisting of imidazol, pyrrolidine and tetrazol unsubstituted or substituted by at least one substitute specified in a group consisting of OH, carbamate, linear or branched C1-C4 alkyl, halogen, NO2, CF3, CN and phenyl; -OC(=O)NR3R4; NC(=NH)NH2 and -NC(=O)NH2; each of R3 and R4 is independently specified in a group consisting of H; C1-C5 alkyl unsubstituted or substituted by at least one substitute specified in a group consisting of NH2 and NR7R8; piperidine, piperazine and diazepane unsubstituted or substituted by C1-C3 alkyl, or R3 and R4 together can form piperidine, piperazine, imidazol, pyrrolidine, triazol, tetrazol, diazepane or morpholine unsubstituted or substituted by C1-C3 alkyl; each of R7 and R8 means at least one substitute independently specified in a group consisting of H and linear or branched C1-C3 alkyl; each m and n independently means 0 or 1. The compounds according to the inventions are active to treat Parkinson's disease.
EFFECT: azol derivatives as a monoamine oxidase B (MAOB) inhibitor.
18 cl, 4 tbl, 207 ex
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