(1-Arylcyclobutyl) alkylamine derivatives, their preparation and their use as therapeutic agents
申请人:The Boots Company PLC
公开号:EP0111994A1
公开(公告)日:1984-06-27
Compounds of formula I
in which n = 0 or 1;
in which, when n = 0, R1 is H, an alkyl, a cycloalkyl, a cycloalkylmethyl, an alkenyl or, an alkynyl group a heterocyclic ring or an optionally substituted phenyl ring or when n = 1, R1 is H or an alkyl group;
in which R2 and R3 are H or an alkyl group;
in which A is a group of formula III
in which W is an oxygen atom or a group of formula -S(O)m-, a group of formula -CR12R13-, a cycloalkylidene group or a cycloalkylene group; x is 0 or an integer from 1 to 5; y is 0 or an integer from 1 to 5.
in which R4 is a carbocyclic ring, a heterocyclic ring, a cyano group, a carbamoyl group, an alkoxycarbonyl group, an amido group, an acyloxy group, a hydroxy group, a thiol group, or a group of formula -OR20, -SR20, -SOR20 or SO2R20.
in which R5, R6 and R7 are H, halo, trifluoromethyl, hydroxy, an alkyl group, an alkoxy or alkylthio group, phenyl or R5 and R6, together with the carbon atoms to which they are attached, form an optionally substituted second benzene ring;
in which R8 and R9 are H or an alkyl group containing 1 to 3 carbon atoms;
and pharmaceutically acceptable salts thereof have utility in the treatment of depression. Processes for their preparation and compositions containing them are disclosed.
式 I 的化合物
其中 n = 0 或 1;
其中,当 n = 0 时,R1 为 H、烷基、环烷基、环烷基甲基、烯基或炔基、杂环或任选取代的苯基;或当 n = 1 时,R1 为 H 或烷基;
其中 R2 和 R3 为 H 或烷基;
其中 A 是式 III 的基团
其中 W 是氧原子或式 -S(O)m- 的基团、式 -CR12R13- 的基团、亚环烷基或亚环烷基;x 是 0 或 1 至 5 的整数;y 是 0 或 1 至 5 的整数。
其中 R4 是碳环基、杂环基、氰基、氨基甲酰基、烷氧羰基、氨基、酰氧基、羟基、硫醇基或式 -OR20、-SR20、-SOR20 或 SO2R20 的基团。
其中 R5、R6 和 R7 是 H、卤素、三氟甲基、羟基、烷基、烷氧基或烷硫基、苯基,或 R5 和 R6 与它们所连接的碳原子一起形成任选取代的第二苯环;
其中 R8 和 R9 为 H 或含有 1 至 3 个碳原子的烷基;
及其药学上可接受的盐类可用于治疗抑郁症。本文公开了其制备方法和含有它们的组合物。