INDDE DERIVATIVES, PREPARATION, PHARMACUTICAL AND MEDICAL USE FOR MIGRAINE

摘要

Indole derivatives are disclosed of formula (I): IMAGE (I) wherein R1 represents H, alkyl or alkenyl; R2 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 -NRaRb, or -CONRaRb, wherein Ra and Rb are H, alkyl, alkenyl, or with the nitrogen atom form a saturated monocyclic ring; R3 and R4 are H, alkyl or propenyl or together form an aralkylidene group; Alk represents a Cf2-3 alkyl chain optionally substituted by one or two alkyl groups; and A1 represents a C2-5 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.