Compositions and their use in lowering intraocular pressure

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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514913, A61K 31415

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active

053045696

ABSTRACT:
Compounds of formula: ##STR1## where X is --CH.sub.2 --, --CH(CH.sub.3)--, --CHR.sub.3 --CH.sub.2 -- or --CR.sub.3 .dbd.CH-- and R.sub.1, R.sub.2 and R.sub.3, which can be the same or different, are each H or CH.sub.3 or a stereoisomer or pharmaceutically acceptable salt thereof, and pharmaceutical compositions containing them, are useful for lowering intraocular pressure in a mammal, e.g. in the treatment of glaucoma.

REFERENCES:
patent: 4665085 (1987-05-01), Coquelet et al.
Medline 89390297 (1989), England et al.
Hodapp, Elizabeth et al, "The Effect of Topical Clonidine on Intraocular Pressure", Arch Ophthalmol, vol. 99 (Jul. 1981), pp. 1208-1211.
Arch. Ophthalmol. vol. 108, Sep. 1990, pp. 1264-1267, "Cardiovascular and Intraocular Pressure Effects and Plasma Concentrations of Apraclonidine", Coleman et al.
European Journal of Pharmacology, vol. 150, 1988, pp. 9-14, Elsevier Publishers B.V. (Biomedical Division) R. Virtanen et al: "Characterization of the selectivity, specificity and potency of medetomidine as an alpha2-adrenoceptor agonist".
Journal of Ocular Pharmacology, vol. 6, No. 3, 1990, pp. 251-257, Mary Ann Liebert, Inc., Publishers; D. E. Potter et al: "Review: Alpha2 and DA2 agonists as antiglaucoma agents: Comparative pharmacology and clinical potential".
Physicians' Desk Reference for Ophthamology, 16 Edition, 1988, p. 11.

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