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, 514399, 514415, 514427, 514471, 514521, 514523, 546 21, 546 22, 546329, 546334, 546335, 548111, 548112, 548341, 548412, 548413, 548414, 548503, 548561, 549 6, 549 74, 549 75, 549 77, A61K 3138, A61K 3134, C07C 906, C07D21170

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active

047436182

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 selected from the group consisting of hydrocarbyl radicals; ##STR2## where X is S or O: 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.

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patent: 4465692 (1984-08-01), Horn
patent: 4564628 (1986-01-01), Horn
McDermed John D, McKenzie Gerald M., Phillips Arthur P., (1974) Synthesis and Pharmacology of Some 2-Aminotetralins. Dopamine Receptor Agonists, Journal of Medicinal Chemistry, 1975, vol. 18, No. 4, at pp. 362-367.
Hacksell Uli, Svensson Uno, Nilsson G., Lars J., (1979), N-Alkylated 2-Aminotetralins: Gentral Dopamine-Receptor Stimulating Activity., Journal of Medicinal Chemistry (1979), vol. 22, No. 12 at pp. 1469-1475.
Seiler et al., J. Med. Chem., 1986, 29, at pp. 912-917., Structure-Activity Relationships of Dopaminergic 5-Hydroxy-2-Aminotetralin Derivatives with Functionalized N-Alkyl Substituents.
Beaulieu M. et al., (1984), N,N-Disubstituted 2-Aminotetralins are Potent D-2 Dopamine Receptor Agonists, European Journal of Pharmacolory, 105 (1984) 15-21.
Horn, A. S. et al., (1985) Synthesis and Radioreceptor Binding Activity of N-0437, a New, Extremely Potent and Selective D.sub.2 Dopamine Receptor Agonist, Short Communications., Pharmaceutisch Weekblad Scientific Edition, vol. 7, (1985), pp. 208-211.
VanOene Joop C. et al., In Vivo Dopamine Autoreceptor Selectivity Appears to be Critically Dependent Upon the Aromatic Hydroxyl Position in a Series of N,N-Disubstituted 2-Aminotetralins., European Journal of Pharmacology, 102 (1984) pp. 101-115.

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