5-trans-prostaglandins of the F series and their use as ocular h

Details 5-trans-prostaglandins of the F series and their use as ocular h 5-trans-prostaglandins of the F series and their use as ocular h

1997-03-24

1998-06-16

Gerstl, Robert

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Ester doai

514277, 514428, 514464, 514573, 514913, A61K 31435

Patent

active

057671540

ABSTRACT:
The invention relates to the use of 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 (a) or beta (b) configuration; hatched lines indicate a configuration, solid triangles are used to indicate b configuration, dashed bonds represent a double bond, or a single bond; n is 0, or an integer of from 1 to 3; X is NH.sub.2 or OR; R is hydrogen, R.sub.4 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 together are .dbd.O, or independently are hydrogen or alkyl of one to 6 carbon atoms or pharmaceutically acceptable salts thereof.

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patent: 4994274 (1991-02-01), Chan et al.
patent: 5656635 (1997-08-01), Chan
Crawford et al;"Effects of topical PGF.sub.2.alpha. an aqueous humor dynamics in cynomolgus monkeys"; Current Eye Research vol. 6, No. 8, 1987, pp. 1035-1044.
Crawford et al; "Dose-Related Effects of Prostaglandin F.sub.2.alpha. Isopropylester on Intraocular Pressure, Refraction, and Pupil Diameter in Monkeys", Investigative Ophthalmology & Visual Science; vol. 32, No. 3, Mar. 1991, pp. 510-519.
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. 231-525.
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. Increases 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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