| 摘要 |
<p>Bicyclic benzamide derivatives of 3- or 4-substituted 4-(aminomethyl)piperidine derivatives of formula (I) and their stereoisomers, N-oxides and acidic and basic addition salts are new. R1 + R2 = OCH2O, OCH2CH2O, OCH2CH2, OCH2CH2CH2, OCH2CH2CH2O or OCH2CH2CH2CH2 in which one or two H atoms are optionally substituted by 1-6C alkyl; R3 = H or halo; R4 = H or 1-6C alkyl; R5 = H or 1-6C alkyl; L = 3-6C cycloalkyl, 5-6C cycloalkanone, 2-6C alkenyl or Alk-R6, Alk-X-R7, Alk-Y-COR9 or Alk-Y-CONR11R12; Alk = 1-12C alkanediyl; R6 = H, OH, CN, 1-6C alkylsulphonylamino, 3-6C cycloalkyl, 5-6C cycloalkanone or Het1; R7 = H, 1-6C alkyl, hydroxy(1-6C alkyl), 3-6C cycloalkyl or Het2; X = O, S, SO2 or NR8; R8 = H or 1-6C alkyl; R9 = H, 1-6C alkyl, 3-6C cycloalkyl, 1-6C alkyloxy or OH; Y = NR10 or a bond; R10 = H or 1-6C alkyl; R11, R12 = H, 1-6C alkyl, 3-6C cycloalkyl or NR11R12 = pyrrolidinyl or piperidinyl (both optionally substituted by 1-6C alkyl, amino or mono- or di-(1-6C alkyl)amino) or piperazinyl or 4-morpholinyl (both optionally substituted by 1-6C alkyl); Het1, Het2 = furan (optionally substituted by 1-6C alkyl or halo) or tetrahydrofuran, dioxolane, dioxane or tetrahydropyran (all optionally substituted by 1-6C alkyl), pyrrolidinyl or pyridinyl (both optionally substituted by 1 or 2 halo, OH, CN or 1-6C alkyl); pyrimidinyl (optionally substituted by 1 or 2 halo, OH, CN, 1-6C alkyl, 1-6C alkyloxy, amino or mono- or di-(1-6C alkyl)amino), pyridazinyl (optionally substituted by 1 or 2 OH, 1-6C alkyloxy, 1-6C alkyl or halo) or pyrazinyl (optionally substituted by 1 or 2 halo, OH, CN, 1-6C alkyl, 1-6C alkyloxy, amino, mono- or di-(1-6C alkyl)amino or 1-6C alkyloxycarbonyl); Het1 can also be a group of formulae (a)-(d); Het1, Het2 can also be a group of formulae (e)-(g); R13, R14 = H or 1-4C alkyl. One compound (I) is specifically claimed i.e. trans-(-)-4-amino-5-chloro- 2,3-dihydro-N-[[3-hydroxy-1- (3-methoxypropyl)-4-piperidinyl] -methyl]-2,2-dimethyl-7- benzofurancarboxamide.</p> |
