| 摘要 |
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 C-Carylalkyl unsubstituted or substituted by at least one substitute specified in a group consisting of halogen, trifluoromethyl, trifluoralkoxy, -NO, C(=O)OCH, linear or branched C-Calkyl, C-Calkoxy, phenyl, phenyloxy, benzyloxy, -C(=O)H, -OH and -C=N-OH; C-Cheteroarylalkyl unsubstituted or substituted by at least one substitute specified in a group consisting of halogen, C(=O)OCH, linear or branched C-Calkyl, C-Calkoxy, phenyl, phenyloxy, benzyloxy; linear, branched or cyclic C-Calkyl substituted by at least one substitute specified in a group consisting of C-C-alkyloxy, C-Calkylthio, carbamate, tert-butyl-OC(=O)NH-, -NH , -NH, -OH, -C(=O)OCHCH, -NHC(=O)NH, trifluoromethylsulphanyl, trifluoromethyl and -CN; wherein when R represents C-C-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 C-Carylalkyl, 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 - R, Rmeans a substitute specified in a group consisting of H and linear or branched C-Calkyl; Ris 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 C-Calkyl, halogen, NO, CF, CN and phenyl; -OC(=O)NRR; NC(=NH)NHand -NC(=O)NH; each of Rand Ris independently specified in a group consisting of H; C-Calkyl unsubstituted or substituted by at least one substitute specified in a group consisting of NHand NRR; piperidine, piperazine and diazepane unsubstituted or substituted by C-Calkyl, or Rand Rtogether can form piperidine, piperazine, imidazol, pyrrolidine, triazol, tetrazol, diazepane or morpholine unsubstituted or substituted by C-Calkyl; each of Rand Rmeans at least one substitute independently specified in a group consisting of H and linear or branched C-Calkyl; 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 |
