C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/319.6
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
Coates Ian H.
Dowle Michael D.
Evans Brian
Oxford Alexander W.
Glaxo Group Limited
Riches Mckenzie & Herbert Llp
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