Indole derivatives

US4785016A · kind A · utility

Assignee

• Glaxo Group Limited · GB

Inventors

• Brian Evans · Penarth, GB
• Alexander W. Oxford · Royston, GB
• Darko Butain · Arlesey, GB

Key dates

• Filing date: Dec 3, 1985
• Grant date: Nov 15, 1988
• Expiry date: Dec 3, 2005

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D209/14
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Indole derivatives are disclosed of formula (I): ##STR1## wherein R.sub.1 represents H, alkyl or alkenyl; PA1 R.sub.2 represents H, alkyl, alkenyl, cycloalkyl or phenyl or phenyl alkyl the phenyl ring being optionally substituted by halogen, alkyl, alkoxy, hydroxyl or by a group --NR.sub.a R.sub.b, or --CONR.sub.a R.sub.b, wherein R.sub.a and R.sub.b are H, alkyl, alkenyl, or with the nitrogen atom form a saturated monocyclic ring; PA1 R.sub.3 and R.sub.4 are H, alkyl or propenyl or together form an aralkylidene group; PA1 Alk represents a Cf.sub.2-3 alkyl chain optionally substituted by one or two alkyl groups; and PA1 A.sup.1 represents a C.sub.2-5 alkenyl chain and salts and solvates thereof. The compounds have selective vasoconstrictor activity and are useful in treating and/or preventing pain resulting from dilatation of the cranial vasculature, particularly migraine. The compounds may be formulated in conventional manner with pharmaceutically acceptable carriers or excipients. Various process for the preparation of the compounds (I) are disclosed.