Benzocycloalkylazolethione derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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5142315, 514255, 514326, 514392, 514398, 544132, 544139, 544366, 544370, 546210, 5482632, 5482638, 5483147, 5483245, A61K 3141, A61K 31415, C07D23384, C07D24912

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active

055389880

ABSTRACT:
The present invention relates to novel benzocycloalkylazolethione compounds which are dopamine .beta.-hydroxylase inhibitors in which the benzocycloalkyl portion of the compound is selected from indanyl, 1,2,3,4-tetrahydronaphthalenyl and 6,7,8,9-tetrahydro-5H-benzocycloheptenyl (in which the benzo is optionally substituted with one to three substituents) and the azolethione portion of the compound is selected from 2-thioxo-2,3-dihydro-1H-imidazol-3-yl, 5-thioxo-4,5-dihydro-1H-[1,2,4]triazol-4-yl and 5-thioxo-4,5-dihydro-1H-[1,2,4]triazol-1-yl (each optionally substituted with one to three substituents); and the prodrugs, pharmaceutically acceptable salts, individual isomers and mixtures of isomers and the methods of using and preparing such benzocycloalkylazolethione compounds.

REFERENCES:
patent: 4994103 (1991-02-01), De Bruyn et al.
Kruse, L. I.; Kaiser, C.; DeWolf, W. E.; Finkelstein, J. A.; Frazee, J. S.; Hilbert, E. L.; Ross, S. T.; Flaim, K. E.; Sawyer, J. L. Some Benzyl-Substituted Imidazoles, Tirazoles, Tetrazoles, Pyridinethiones, and Structural Relatives as Multisubstrate Inhibitors of Dopamine .beta.-Hydroxylase. 4. Structural-Activity Relationships at the Copper Binding Site. J. Med. Chem. 1990, 33, 781-789.
Kruse, L. I.; Kaiser, C.; DeWolf, W. E.; Frazee, J. S.; Erickson, R. W.; Ezekiel, M.; Ohlstein, E. H.; Ruffolo, R. R.; Berkowitz, B. A. Substituted -Benzylimidazole-2-thiols as Potent and Orally Active Inhibitors of Dopamine .beta.-Hydroxylase. J. Med. Chem. 1986, 29, 887-889.

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