| 摘要 |
The invention relates to new imidazolylmethyl-cycloalkane[b]indolones having formula <CHEM> wherein - R0 is alkyl or alkoxy having 1-4 C-atoms, hydroxy, halogen, trifluoromethyl, a group R6R7N or R6R7-N-CO, wherein R6 and R7 are hydrogen or alkyl having 1-4 C-atoms or wherein R6R7N is a saturated 5-6 ring and n has the value 0, 1 or 2, - R1 is hydrogen, 1-8 C alkyl, 3-7 C cycloalkyl, 3-7 C cycloalkyl-(1-3 C)- alkyl, 3-6 C alkenyl, 3-8 C alkynyl, phenyl or phenyl-(1-3 C) alkyl, wherein the phenyl group may be substituted with one or more alkyl groups, alkoxy groups or OH-groups or with one or more halogen atoms, or R1 is a group COOR8, COR8, SO2R8, wherein R8 is 1-4 C alkyl, 3-7 C cycloalkyl, phenyl or phenyl-(1-2 C)alkyl wherein the phenyl group may be substituted with one or more 1-4 C alkyl groups, 1-4 C alkoxy groups, hydroxyl groups or halogen atoms, or R1 is a group R9R10N-C <0> wherein R9 and R10 independently of each other are hydrogen, 1-4 C alkyl, phenyl or phenyl-(1-2 C)alkyl wherein the phenyl group may be substituted, or wherein R9 and R10 together with the nitrogen atom to which they are bound constitute a saturated 5-6 ring, - one of the groups R2, R3 and R4 is hydrogen, alkyl having 1-4 C atoms, cycloalkyl having 3-6 C-atoms, alkenyl having 2-4 C-atoms or phenyl-alkyl having 1-2 C-atoms in the alkyl group and the two other groups, independently of each other, are hydrogen or alkyl having 1-4 C-atoms, - m has the value 3 to 8 inclusive, and the pharmaceutically acceptable acid addition salts thereof. The compounds have a longer-lasting selective antagonistic activity on "neuronal" 5-hydroxytryptamine (5-HT) receptors as compared with related known compounds, and they are less toxic. |
