Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Patent
1992-02-18
1993-12-28
Ivy, C. Warren
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
564347, 564352, A61K 31135, C07C21714, C07C21724
Patent
active
052740030
ABSTRACT:
Optically active or racemic compounds are provided having the formula ##STR1## where R.sub.2, R.sub.3 and R.sub.4 are each selected from the group consisting of H and OH with the provision that at least one of R.sub.2, R.sub.3 and R.sub.4 is H, that R.sub.2 and R.sub.4 are not both OH; X is oxygen; and R.sub.1 is selected from the group consisting of ##STR2## wherein Z is oxygen, nitrogen or sulfur, wherein Y is selected from the group consisting of hydroxy, nitro, cyano, azido, amino, acylamino, carboxyamido, trifluoromethyl, sulfate, sulfonamido, halogen, hydrocarbyl and heteroatom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of halogen, nitrogen, oxygen, sulfur and phosphorus and said hydrocarbyl radicals comprise from 1 to 12 carbon atoms, and a is an integer of from zero to 3. These compounds are capable of binding selectivity of one or more dopamine D.sub.2 receptors, for instance, in humans. They are useful in treatment of disorders of the central nervous, cardiovascular, and endocrine systems, such as elevated intraocular pressure, schizophrenia and Parkinsonism, and for inducing anorexia and weight loss in humans and other mammals.
REFERENCES:
patent: 4880802 (1989-11-01), Schohe
patent: 5070106 (1991-12-01), Casagrande
patent: 5126364 (1992-06-01), Lednicer
McDermed et al. "Synthesis and Pharmacology of Some 2-Aminotetralins Dopamine Agonists" J. Med. Chem. 18(4) 362-367, (1975).
McGonigle et al. "A Comprehensive Method of the Quantitative Determination of Dopamine Receptor Subtypes" N.Y. Aca. Sci. 430 77-89 (1984).
Minaskanian Gevork
Peck James V.
Chang Celia
Hammond Richard J.
Ivy C. Warren
Whitby Research, Inc.
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