Acylaminoindole derivatives as 5-ht1 agonists

Details Acylaminoindole derivatives as 5-ht1 agonists Acylaminoindole derivatives as 5-ht1 agonists

1994-09-14

1996-03-12

Haley, Jacqueline

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514323, 514397, 546201, 548468, 5483121, C07D40306, C07D40314, A61K 3140

Patent

active

054986265

ABSTRACT:
##STR1## Compounds of formula (I) where n is 0, 1, or 2; m is 0 or 1; Y and W are each an amino acid residue; R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, aryl, C.sub.1 -C.sub.3 alkylaryl, or C.sub.1 -C.sub.3 alkylheteroaryl, and --(CH.sub.2).sub.p R.sub.3 ; R.sub.2 is CF.sub.3, C.sub.1 -C.sub.6 alkyl, aryl, C.sub.1 -C.sub.3 alkylaryl, and --OR.sub.5 ; R.sub.3 is cyano, trifluoromethyl, or --OR.sub.4 ; R.sub.4 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.3 alkylaryl, or aryl; R.sub.5 is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.3 alkylaryl, or aryl; R.sub.6 is hydrogen, --OR.sub.7, or --NHCOR.sub.7 ; R.sub.7 is hydrogen, C.sub.1 to C.sub.6 alkyl, aryl or C.sub.1 to C.sub.3 alkyl-aryl; p is 1, 2, or 3; and the above aryl groups and the aryl moieties of the above alkyl-aryl groups are independently selected from phenyl and substituted phenyl, wherein said substituted phenyl may be substituted with one to three groups selected from C.sub.1 to C.sub.4 alkyl, halogen, hydroxy, cyano, carboxamide, nitro, and C.sub.1 to C.sub.4 alkoxy and the pharmaceutically acceptable salts thereof. These compounds are useful in treating migraine and other disorders. These compound are useful psychotherapeutics and are potent serotonin (5-HT.sub.1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, and chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators.

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W. Feniuk, et al., P. P. A. Humphrey & M. J. Perren-Br. J. Pharmacol. (1989), 96, 83-90.
P. P. A. Humphrey, et al.-Br. J. Pharmacol. (1988), 94, 1123-1132.
R. E. Hearing et al. J. Neuroscience, 7, 894 (1987).

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