The invention relates to tetrahydronaphthalene and indane derivatives with the general formula I:
wherein
R¹ represents zero to four substituents, which may be the same or different and are selected from OH, halogen, NO₂, CN, CF₃, C₁-C₄ alkyl, C₁-C₄ alkoxy and unsubstituted or C₁-C₄ alkyl substituted amino;
R² represents C₁-C₄ alkyl, C₁-C₄ alkenyl and C₁-C₄ alkynyl which may be substituted by halogen;
R³ and R⁴ represent independently H, C₁-C₄ alkyl or form together with the nitrogen atom a 5- or 6-membered ring;
n has the value 0 or 1;
ALK is an aliphatic hydrocarbon with 1-8 carbon atoms and their pharmaceutically acceptable salts.
These new compounds are typical monoamine reuptake blockers with additional α₂ antagonist activity and show strong anti-depressant activity without being sedative. Compounds according to this invention are also suitable for treating patients with anxiety disorders, e.g. panic disorder.
本发明涉及通式 I 的四氢
萘和
茚衍
生物:
其中
R¹ 代表零至四个取代基,它们可以相同或不同,选自 OH、卤素、NO₂、CN、CF₃、C₁-C₄ 烷基、C₁-C₄ 烷氧基和未取代或 C₁-C₄ 烷基取代的
氨基;
R² 代表可被卤素取代的 C₁-C₄ 烷基、C₁-C₄ 烯基和 C₁-C₄ 烷基;
R³ 和 R⁴ 独立地代表 H、C₁-C₄ 烷基或与氮原子一起形成 5 或 6 元环;
n 的值为 0 或 1;
ALK 是具有 1-8 个碳原子的脂肪族烃及其药学上可接受的盐类。
这些新化合物是典型的单胺再摄取阻断剂,具有额外的α₂拮抗剂活性,并显示出很强的抗抑郁活性,但没有镇静作用。本发明的化合物还适用于治疗焦虑症患者,如恐慌症。