Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1996-10-07
1997-11-18
Richter, Johann
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
5142225, 5142238, 514241, 514242, 514252, 514255, 514259, 514266, 514269, 514307, 514311, 514338, 514361, 514362, 514363, 514364, 514365, 514367, 514372, 514374, 514375, 514378, 514381, 514383, 544 2, 544180, 544238, 544242, C07D40304, C07D47104, A61K 31415, A61K 3144
Patent
active
056888090
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE INVENTION
The present invention relates to indole derivatives, intermediates for their preparation, pharmaceutical compositions containing them, and their medicinal use. The active compounds of the present invention are potent agonists and antagonists at the benzodiazepine receptor. Agonists and antagonists of the benzodiazepine receptor are useful in the treatment, prevention and diagnosis of anxiety, memory loss, sleep disorders or seizures. The compounds of the invention are also useful in the treatment of an overdose of benzodiazepine drugs.
The use of benzodiazepine receptor ligands in the treatment of anxiety and other disorders has been discussed in "New Trends in Benzodiazepine Research", 24 Drugs of Today, 649-663 (1988).
European Patent Publication 499,527, which was published on Aug. 19, 1992, refers to .beta.-carboline derivatives which possess an affinity for benzodiazepine receptors and as such are useful agents in the treatment of degenerative central nervous system disorders, such as Alzheimer's disease.
U.S. Pat. No. 5,243,049, which issued on Sep. 7, 1993, refers to pyrroloquinoline derivatives which are .gamma.-amino butyric acid (GABA) receptor antagonists. These pyrroloquinoline derivatives are claimed to be useful for the treatment of anxiety, sleep disorders, seizures and for enhancing memory.
U.S. Pat. No. 5,066,654, which issued on Nov. 19, 1991, refers to be useful as anxiolytics and anticonvulsants.
A series of planar azadiindoles, benzannelated pyridoindoles, and indolopyridoimidazoles have been described as molecular probes that are useful for the definition of the molecular recognition elements of the benzodiazepine receptor in J. Med. Chem., 35, 4105-4117 (1992).
International Patent Application WO 93/23396; published Nov. 25, 1993, refers to fused imidazole and triazole derivatives as 5-HT.sub.1 receptor agonists that are useful for the treatment of migraine and other disorders.
SUMMARY OF THE INVENTION
The present invention relates to compounds of the formula ##STR2## wherein X and Y are independently carbon or nitrogen;
R.sup.1 and R.sup.2 are independently selected from hydrogen, (C.sub.1 -C.sub.6)alkyl, aryl, --(C.sub.1 -C.sub.3)alkylaryl, --(CH.sub.2).sub.n --(C.sub.4 -C.sub.7)cycloalkyl, --(CH.sub.2).sub.n CHO, --(CH.sub.2).sub.n CO.sub.2 R.sup.7, --(CH.sub.2).sub.n CONR.sup.7 R.sup.8, 3-succinamido, unsaturated heterocycle, benzo-fused heterocycle, --(C.sub.1 -C.sub.3)alkyl-unsaturated heterocycle, and --(C.sub.1 -C.sub.3)alkyl-benzo-fused heterocycle; wherein said unsaturated heterocycle and unsaturated heterocycle moiety of said --(C.sub.1 -C.sub.3)alkyl-unsaturated heterocycle are selected, independently, from pyrrolyl, furyl, thienyl, oxazolyl, isoxazolyl, imidazolyl, thiazolyl, isothiazolyl, pyrazolyl, triazolyl, tetrazolyl, 1,3,5-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,5-thiadiazolyl, 1,2,4-thiadiazolyl, pyridyl, pyrazinyl, pyrimidinyl, pyridazinyl, 1,2,4-triazinyl, 1,2,3-triazinyl, 1,3,5-triazinyl, 1,2,5-thiadiazinyl, 1,2,5-oxathiazinyl, and 1,2,6-oxathiazinyl; wherein said benzo-fused heterocycle and the benzo-fused heterocyclic moiety of said --(C.sub.1 -C.sub.3)alkyl-benzo-fused heterocycle are selected, independently, from benzoxazolyl, benzothiazolyl, benzimidazolyl, thianaphthenyl, isothianaphthenyl, benzofuranyl, isobenzofuranyl, chromenyl, isoindolyl, indolyl, indazolyl, isoquinolyl, quinolyl, phthalazinyl, quinoxalinyl, quinazolinyl, cinnolinyl and benzoxazinyl; wherein each of said unsaturated heterocycle, benzo-fused heterocycle, --(C.sub.1 -C.sub.3)alkyl-unsaturated heterocycle and --(C.sub.1 -C.sub.3)alkyl-benzo-fused heterocycle may optionally be substituted on one or more ring carbon atoms with from zero to three substituents, said substituents being independently selected from bromo, chloro, fluoro, (C.sub.1 -C.sub.5)alkyl, (C.sub.1 -C.sub.5)alkoxy, (C.sub.1 -C.sub.5)alkylthio, (C.sub.1 -C.sub.5)alkylamino, (C.sub.1 -C.sub.4)alkylsulfonyl, (C.sub.1 -C.sub.5)dialkylamino, hydroxy, amino, nitro, cyano, trifluoromethyl, ##STR3## w
Creagan B. Timothy
Ginsburg Paul H.
Pfizer Inc.
Richardson Peter C.
Richter Johann
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