Indole derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 209/16 (2006.01) C07D 209/08 (2006.01) C07D 209/10 (2006.01) C07D 209/12 (2006.01) C07D 209/18 (2006.01) C07D 209/48 (2006.01)

Patent

CA 1233183

A B S T R A C T Indole derivatives are disclosed of the general formula (I): Image (I) wherein R1 is hydrogen, C1-6 alkyl or C3-6 alkenyl; R2 is a hydrogen, C1-3 alkyl, C3-6 alkenyl, phenyl, phen(C1-4)alkyl or C5-7 cycloalkyl; R3 and R4 are hydrogen, C1-3 alkyl or propenyl groups or together form an aralkylidene group; Alk is C2-C3 alkylene chain and A is C2-C5 alkylene chain and its physiologically acceptable salts and solvates. The compounds may be prepared, for example, by cyclisation of a compound of general formula (II): Image (II) where Q is the group NR3R4 or a protected derivative thereof or a leaving group and R1, R2, R3, R4, A and Alk are as defined for formula (I). The compounds have a selective vosoconstrictor action and are useful in treating pain such as migraine. The compounds may be formulated as pharmaceutical compositions in conventional manner, preferably for oral administration.

469528

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