Substituted 2-aminotetralins

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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514357, 514415, 514427, 514399, 514471, 514521, 514523, 549 74, 549 75, 549 77, 549492, 549494, 549495, 546329, 546335, 546334, 548503, 548561, 548341, 560138, 560139, 560110, 564308, 260465E, 260465D, A61K 3138, C07D33312, C07D33322, C07D30702

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active

045646287

ABSTRACT:
Novel compounds useful as dopamine receptor agonists for the treatment of various diseases of the central nervous system such as Parkinson's disease and related disorders having the structural formula ##STR1## where R.sub.2, R.sub.3 and R.sub.4 are each selected from the group consisting of H, and OA; A is H or ##STR2## R.sub.5 is selected from the group consisting of alkyl and aromatic residues; n is 2 or 3; and R.sub.1 is selected from the group consisting of 3-hydroxyphenyl, 4-hydroxyphenyl, 3-pyridyl, 4-pyridyl, ##STR3## where X is S, O or NH; and pharmaceutically acceptable salts thereof. Also disclosed is a method for inducing a dopaminergic response in a patient by adminstering a pharmacologically-effective amount of one of the foregoing compounds.

REFERENCES:
patent: 3704323 (1979-11-01), Krapcho
patent: 4314082 (1982-02-01), Stout
Hacksell et al., "N-Alkylated 2-Aminotetralins: Central Dopamine Receptor Stimulating Activity", Journal of Medicinal Chemistry, vol. 22, No. 12, 1979.
Sumners, et al., "Neurochemical and Behavioral Profiles of Five Dopamine Analogues", Archives of Pharmacology, Spring, 1981.
Feenstra et al., "Effect of Dihydroxy-2-Aminotetralin Derivatives on Dopamine Metabolism in the Rat Striatum", Archives of Pharmacology, Spring, 1980.
McDermed et al., "Synthesis and Pharmacology of Some 2-Aminotetralins. Dopamine Receptor Agonists.", Journal of Medicinal Chemistry, vol. 18, No. 4, 1975.
McDermed et al., "Synthesis and Dopaminergic Activity of (.+-.)-, (+)-, and (-)-2-Dipropylamino-5-Hydroxy, etc . . . ", Journal of Medicinal Chemistry, vol. 19, No. 4, 1976.

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