5-trans-alcohols and their use as ocular hypotensives

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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514438, 514464, 514530, 514573, 514913, 568838, A61K 31435, A61K 3138, A61K 3134, A61K 31215

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active

056566352

ABSTRACT:
The invention relates to the use of alcohol derivatives of F-type prostaglandins as ocular hypotensives. The PGF derivatives used in accordance with the invention are encompassed by the following structure formula I: ##STR1## wherein wavy line attachments indicate either the alpha (.alpha.) or beta (.beta.) configuration; hatched lined indicate .alpha. configuration, solid triangles are used to indicate .beta. configuration, dashed bonds represent a double bond, or a single bond; n is 0, or an integer of from 1 to 3; R is hydrogen or a --(CO)R.sub.4 group; R.sub.1, R.sub.2, and R.sub.3 independently are hydroxyl, or --O(CO)R.sub.5 groups, wherein R.sub.4 and R.sub.5 independently stand for saturated or unsaturated acyclic hydrocarbon having from 1 to 20 carbon atoms, or --(CH.sub.2).sub.m R.sub.6 where m is 0-10 and R.sub.6 is an aliphatic, aromatic or heteroaromatic ring, R.sub.7 and R.sub.8 independently are hydrogen or alkyl of 1 to 6 carbon atoms or pharmaceutically acceptable salts thereof.

REFERENCES:
patent: 4994274 (1991-02-01), Chan et al.
Bito, L.Z., "Prostaglandins and Related Compounds as Potential ocular Therapeutic Agents," Biological Protection with Prostaglandins, Cohen, M.M., ed., Boca Raton, Fla., CRC Press, Inc., 1985, pp. 231-252.
Bito, L.Z., "Prostaglandins, Other Eicosanoids, and Their Derivatives as Potential Antiglaucoma Agents," Applied Pharmacology in the Medical Treatment of Glaucomas Drance, S.M. and Neufeld, A.H. eds., New York, Grune & Stratton, 1984, pp. 477-505.
Nilsson, et al., "PGF.sub.2.alpha. Increase Uveoscleral Outflow," Invest. Ophthalmol. Vis. Sci. (suppl), 284, 1987.
Siebold, et al., "Esterified prostaglandin shows `potent` promise," Prodrug 5 3, 1989.
Bito, L.Z., "Prostaglandins, Old Concepts and New Perspectives," Arch. Ophthalmol. 105, 1036, 1987.

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