4-indole derivatives as serotonin agonists and antagonists

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 209/04 (2006.01) A61K 31/495 (2006.01) A61K 31/53 (2006.01) A61K 31/535 (2006.01) C07D 209/08 (2006.01) C07D 209/12 (2006.01) C07D 209/18 (2006.01) C07D 209/42 (2006.01) C07D 401/00 (2006.01) C07D 401/04 (2006.01) C07D 401/12 (2006.01) C07D 403/00 (2006.01) C07D 405/14 (2006.01) C07D 409/14 (2006.01) C07D 413/00 (2006.01) C07D 413/04 (2006.01) C07D 413/14 (2006.01) C07D 417/14 (2006.01) C07D 419/14 (2006.01) C07D 471/04 (2006.01)

Patent

CA 2194984

The present invention relates to compounds of formula (I) wherein X is oxygen or (Ia); R1 is a group of formula (II, III, IV or V); the compounds of formula (I) and the pharmaceutically acceptable salts thereof are useful psychotherapeutics and are potent serotonin (5-HT1) agonists and antagonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, chronic paroxysmal hemicrania and headache associated with vascular disorders, pain, and other disorders arising from insufficient or deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators.

La présente invention concerne les composés de formule (I) dans laquelle X représente un oxygène ou un groupe de la formule (Ia) et R?1¿ représente un groupe de formule (II, III, IV ou V). Les composés de formule (I) et leurs sels acceptables sur le plan pharmaceutique sont des agents psychothérapeutiques utiles, car ce sont de puissants agonistes et antagonistes de la sérotonine (5-HT¿1?) et ils peuvent être utilisés pour le traitement des dépressions, de l'anxiété, des troubles de l'alimentation, de l'obésité, des toxicomanies, des céphalées vasculaires de Horton, des migraines, d'hémicrânies chroniques paroxysmales, des maux de tête associés avec des troubles vasculaires, de la douleur et de troubles associés à une neurotransmission sérotoninergique déficiente ou insuffisante. Les composés peuvent également être utilisés comme agents antihypertensifs et vasodilatateurs agissant sur le système nerveux central.

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