申请人:Glaxo Group Limited
公开号:US04876267A1
公开(公告)日:1989-10-24
Indole derivatives are disclosed of the formula (I): ##STR1## wherein R.sub.1 represents H, or C.sub.1-6 alkyl or C.sub.3-6 Alkenyl; R.sub.2 represents a H, C.sub.1-3 alkyl, C.sub.3-6 alkenyl or C.sub.5-7 cycloalkyl, or a phenyl or phen(C.sub.1-4)alkyl group in which the phenyl ring is optionally substituted by halogen or C.sub.1-3 alkyl, C.sub.1-3 alkoxy or hydroxyl, or by a group NR.sup.a R.sup.b, or CONR.sup.a R.sup.b, wherein R.sup.a and R.sup.b each independently represents H or C.sub.1-3 alkyl; R.sub.3 and R.sub.4, each independently represents H or C.sub.1-3 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 formulated as pharmaceutical compositions with pharmaceutically acceptable carriers or excipients for administration by any suitable means. Various methods for the preparation of the compounds are disclosed.
公开了式(I)的吲哚衍生物:##STR1## 其中R.sub.1表示H,或C.sub.1-6烷基或C.sub.3-6烯基;R.sub.2表示H,C.sub.1-3烷基,C.sub.3-6烯基或C.sub.5-7环烷基,或者是苯基或苯(C.sub.1-4)烷基,其中苯环可选地被卤素或C.sub.1-3烷基,C.sub.1-3烷氧基或羟基,或者被NR.sup.a R.sup.b或CONR.sup.a R.sup.b基取代,其中R.sup.a和R.sup.b各自独立地表示H或C.sub.1-3烷基;R.sub.3和R.sub.4各自独立地表示H或C.sub.1-3烷基或2-丙烯基;以及其生理上可接受的盐和溶剂(例如水合物)。这些化合物具有强效和选择性的血管收缩活性,并被指示为治疗偏头痛有用。这些化合物可以与药物学上可接受的载体或赋形剂配制成制药组合物,以通过任何适当的途径进行给药。公开了制备这些化合物的各种方法。