Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1995-04-27
1999-03-23
Mach, D. Margaret M.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514243, 514246, 514250, 514249, 514253, 514248, 514257, 514266, 514267, 514293, 544179, 544183, 544234, 544236, 544251, 544256, 544345, 544350, 546 83, 546118, 546199, 5483021, 5483051, A61K 3144, A61K 3152, C07D47102, C07D49102
Patent
active
058860088
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE INVENTION
The present invention relates to Indole derivatives, intermediates for their preparation, pharmaceutical compositions containing therm, and to their medicinal use. The active compounds of the present invention are useful in treating migraine and other disorders.
U.S. Pat. Nos. 4,839,377 and 4,855,314 and European Patent Application Publication Number 313397 refer to 5-substituted 3-aminoalkyl indoles. The compounds are said to be useful for the treatment of migraine.
British Patent Application 040279 refers to 3-aminoalkyl-1H-indole-5-thioamides and carboxamides. The compounds are said to be useful in treating hypertension, Raymond's disease and migraine.
European Patent Application Publication Number 303506 refers to 3-poly:hydropyridyl-5-substituted-1 H-indoles. The compounds are said to have 5-HT.sub.1 receptor agonist and vasoconstrictor activity and to be useful in treating migraine.
European Patent Application Publication Number 354777 refers to N-piperidinyl:indolyl:ethyl-alkane sulfonamide derivatives. The compounds are said to have 5-HT.sub.1 receptor agonist and vasoconstrictor activity and to be useful in treating cephalic pain.
European Patent Application Publication Number 438230 refers to indole-substituted five-membered heteroaromatic compounds. The compounds are said to have 5-HT.sub.1 -like receptor agonist activity and to be useful in the treatment of migraine and other disorders for which a selective agonist of these receptors is indicated.
European Patent Application Publication Number 313397 refers to 5-heterocyclic indole derivatives. The compounds are said to have exceptional propertes for the treatment and prophylaxis of migraine, cluster headache, and headache associated with vascular disorders. These compound are also said to have exceptional "5-HT.sub.1 -like" receptor agonism.
International Patent Application WO 91/18897 refers to 5-heterocyclic indole derivatives. The compounds are said to have exceptional properties for the treatment and prophylaxis of migraine, cluster headache, and headache associated with vascular disorders. These compound are also said to have exceptional "5-HT.sub.1 -like" receptor agonism. European Patent Application Publication Number 457701 refers to aryloxy amine rivatives as having high affinity for 5HT.sub.1D serotonin receptors. These compounds are said to be useful for treating diseases related to serotonin receptor dysfunction, for example, migraine.
European Patent Application Publication Number 497512 A2 refers to a class of imidazole, triazole, and tetrazole derivatives which are selective agonists for 5-HT.sub.1-like receptors. These compounds are said to be useful for treating migraine and associated disorders.
"New Trends in Benzodiazepine Research" in Drugs of Today, Vol. 24, 649-663 (1987) discusses the use of benzodiazepine receptor ligands in the treatment of anxiety and other disorders.
European Patent Application EP-499527-A1 refers to novel .beta.-carboline derivatives with affinity for benzodiazepine receptors as useful in the treatment of degenerative central nervous system disorders, e.g. Alzheimer's disease.
SUMMARY OF THE INVENTION
The present invention relates to compounds of the formula ##STR2## wherein R.sub.1 is ##STR3## n is 0, 1, or 2; A, B, C, and D are each independently nitrogen or carbon; R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are each independently hydrogen, C.sub.1 to C.sub.6 alkyl, aryl, C.sub.1 to C.sub.3 alkyl-aryl, halogen (e.g. fluorine, chlorine, bromine or iodine), cyano, nitro, --(CH.sub.2).sub.m NR.sub.14 R.sub.15, --(CH.sub.2).sub.m OR.sub.9, --SR.sub.9, --SO.sub.2 NR.sub.14 R.sub.15, --(CH.sub.2).sub.m NR.sub.14 SO.sub.2 R.sub.15, --(CH.sub.2).sub.m NR.sub.14 CO.sub.2 R.sub.9, --(CH.sub.2).sub.m NR.sub.14 COR.sub.9, --(CH.sub.2).sub.m NR.sub.14 CONHR.sub.9, --CONR.sub.14 R.sub.15, or --CO.sub.2 R.sub.9 ; R.sub.2 and R.sub.3, R.sub.3 and R.sub.4, or R.sub.4 and R.sub.5 may be taken together to form a five- to seven-membered alkyl ring, a six-membered aryl ring, a five- to sev
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Fuller Jr. Grover F.
Ginsburg Paul H.
M. Mach D. Margaret
Pfizer Inc.
Richardson Peter C.
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