申请人:GLAXO GROUP LIMITED
公开号:EP0533268A1
公开(公告)日:1993-03-24
The invention provides compounds of the general formula (I) :-
or a physiologically acceptable salt or solvate thereof
wherein
R¹ represents a hydrogen atom or a halogen atom or a group selected from C₁₋₆alkyl and C₁₋₆alkoxy;
R² represents a phenyl group substituted by a group selected from
and optionally further substituted by one or two substituents selected from halogen atoms, C₁₋₆alkoxy, hydroxy, and C₁₋₆alkyl;
R³ represents the group
R⁴ and R⁵, which may be the same or different, each independently represent a hydrogen atom or a halogen atom or a group selected from hydroxy, C₁₋₆alkoxy and C₁₋₆alkyl;
R⁶ represents a hydrogen atom or a group selected from -NR⁹R¹⁰ and a C₁₋₆alkyl group optionally substituted by one or two substituents selected from C₁₋₆alkoxy, hydroxy, C₁₋₆acyloxy and -SO₂R¹¹;
R⁷, R⁸ and R⁹, which may be the same or different, each independently represent a hydrogen atom or a C₁₋₆alkyl group;
R¹⁰ represents a hydrogen atom or a group selected from C₁₋₆alkyl, C₁₋₆acyl, benzoyl and -SO₂R¹¹;
R¹¹ represents a C₁₋₆alkyl group or a phenyl group;
Z represents an oxygen atom or a group selected from NR⁸ and S(O)k; and
k represents zero, 1 or 2.
The compounds may be used in the treatment or prophylaxis of depression and other CNS disorders.
本发明提供了通式 (I) :- 的化合物。
或其生理上可接受的盐或溶液
其中
R¹ 代表氢原子、卤素原子或选自 C₁₋₆ 烷基和 C₁₋₆ 烷氧基的基团;
R² 代表被选自以下各项的基团取代的苯基
并可选择地进一步被一个或两个选自卤素原子、C₁₋₆烷氧基、羟基和 C₁₋₆烷基的取代基取代;
R³ 代表以下基团
R⁴ 和 R⁵ 可以相同或不同,各自独立地代表氢原子或卤原子或选自羟基、C₁₋₆烷氧基和 C₁₋₆ 烷基的基团;
R⁶ 代表氢原子或选自-NR⁹R¹⁰ 的基团和任选被一个或两个选自 C₁₋₆ 烷氧基、羟基、C₁₋₆acyloxy 和-SO₂R¹¹ 的取代基取代的 C₁₋₆ 烷基;
R⁷、R⁸ 和 R𠞙 可以相同或不同,各自独立地代表氢原子或 C₁₋₆ 烷基;
R¹⁰ 代表氢原子或选自 C₁₋₆烷基、C₁₋₆酰基、苯甲酰基和 -SO₂R¹¹ 的基团;
R¹¹ 代表 C₁₋₆烷基或苯基;
Z 代表氧原子或选自 NR⁸ 和 S(O)k 的基团;以及
k 代表 0、1 或 2。
这些化合物可用于治疗或预防抑郁症和其他中枢神经系统疾病。