Indole derivatives are disclosed of the formula
wherein
R₁ represents H, or C₁-₆ alkyl or C₃-₆ alkenyl;
R₂ represents a H, C₁-₃ alkyl, C₃-₆ alkenyl or C₅-₇ cycloalkyl, or a phenyl or phen(C₁-₄)alkyl group in which the phenyl ring is optionally substituted by halogen or C₁-₃ alkyl, C₁-₃ alkoxy or hydroxyl, or by a group NRaRb, or CONRaRb, wherein Ra and Rb each independently represents H or C₁-₃ alkyl;
R₃ and R₄, each independently represents H or C₁-₃ alkyl or 2-propenyl;
and physiologically acceptable salts and solvates (e.g. hydrates) thereof.
The compounds have potent and selective vasoconstrictor activity and are indicated as useful for the treatment of migraine. The compounds may be formulate as pharmaceutical compositions with pharmaceuticaly acceptable carriers or excipients for administration by any suitable means. Various methods for the preparation of the compounds are disclosed.
公开了式中的
吲哚衍
生物
其中
R₁ 代表 H、C₁-₆ 烷基或 C₃-₆ 烯基;
R₂ 代表 H、C₁-₃ 烷基、C₃-₆ 烯基或 C₅-₇ 环烷基,或苯基或苯基(C₁-₄)烷基,其中苯基环可任选被卤素或 C₁-₃ 烷基取代、C₁-₃烷氧基或羟基,或被基团 NRaRb 或 CONRaRb 取代,其中 Ra 和 Rb 各自独立地代表 H 或 C₁-₃ 烷基;
R₃ 和 R₄ 各自独立地代表 H 或 C₁-₃ 烷基或 2-
丙烯基;
及其生理上可接受的盐类和溶剂(如
水合物)。
这些化合物具有强效的选择性血管收缩活性,可用于治疗偏头痛。这些化合物可与药物可接受的载体或赋形剂配制成药物组合物,以任何合适的方式给药。公开了制备这些化合物的各种方法。