Indole derivatives

US5270333A · kind A · utility

Assignee

• Glaxo Group Limited · GB

Inventors

• David E. Bays · Ware, GB
• Alexander W. Oxford · Royston, GB

Key dates

• Filing date: Aug 16, 1991
• Grant date: Dec 14, 1993
• Expiry date: Aug 16, 2011

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D209/16
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Compounds are disclosed of general formula: ##STR1## wherein R.sup.1 is H, C.sub.1-6 alkyl or C.sub.3-6 alkenyl; R.sup.2 is H, C.sub.1-3 alkyl, C.sub.3-6 alkenyl, aryl, ar(C.sub.1-4)-alkylene, or C.sub.5-7 cycloalkyl; PA0 R.sup.3 is H or C.sub.1-3 alkyl; PA0 R.sup.4 and R.sup.5 each represents H, C.sub.1-3 alkyl or 2-propenyl, or R.sup.4 and R.sup.5 together form an aralkylidene group; PA0 R.sup.6 represents --CO.sub.2 R.sup.7, COR.sup.7, --COCO.sub.2 R.sup.7, or --CONHR.sup.7, where PA0 R.sup.7 represents H, C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-4 alkenyl, aryl or ar(C.sub.1-4)alkylene (with the provisos that (a) R.sup.7 does not represent H or benzyl when R.sup.6 is --CO.sub.2 R.sup.7 and (b) R.sup.7 does not represent alkenyl when R.sup.6 is --CONHR.sup.7); and Alk represents an alkylene chain containing two or three carbon atoms which may be unsubstituted or substituted by not more than two C.sub.1-3 alkyl group, 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 composition…