Method of treating ocular hypertension with 8-epi prostaglandins

Details Method of treating ocular hypertension with 8-epi prostaglandins Method of treating ocular hypertension with 8-epi prostaglandins

1992-11-12

2000-09-26

Cintins, Marianne

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Ester doai

514573, 514913, A61K 31215, A61K 3119

Patent

active

061243531

ABSTRACT:
The present invention provides a method of treating ocular hypertension which comprises applying to the eye an amount sufficient to treat ocular hypertension of a compound of formula (I) ##STR1## wherein the wavy line attachments indicate either alpha (.alpha.) or beta (.beta.) configuration; hatched lines indicate .alpha. configuration, solid triangles are used to indicate .beta. configuration; the dashed bonds represent a single bond or a double bond which can be in the cis or trans configuration; X is selected from the group consisting of H, R or a pharmaceutically-acceptable cation, and R is an aliphatic hydrocarbon group of about 1 to about 6 carbon atoms; one of R.sub.1 and R.sub.2 is .dbd.O, --OH or an --O(CO)R.sub.4 group, and the other one is --OH or an --O(CO)R.sub.4 group or R.sub.1 is .dbd.O and R.sub.2 is H; R.sub.3 is --OH or --O(CO)R.sub.4, wherein R.sub.4 is a saturated or unsaturated acyclic hydrocarbon group having from 1 to about 20 carbon atoms, or --(CH.sub.2).sub.n R.sub.5 wherein n is 0-10, and R.sub.5 is an aliphatic ring from about 3 to about 7 carbon atoms, or an aromatic or heteroaromatic ring; or a pharmaceutically acceptable salt thereof.

REFERENCES:
patent: 4599353 (1986-07-01), Bito
patent: 4994274 (1991-02-01), Chan
patent: 5139491 (1992-08-01), Chan
AM. J. Physiol.,263(3,PT.2), H660-H663 1992 Banerjee, Mukul et al 'Effects of a novel prostaglandin, 8-epi-PGF2. alpha., in rabbit lung in situ'.
Prostaglandins, 44(2), 155-63 1992 Morrow, J.D. et al 'The F2-isoprostane, 8-epi-prostaglandin F2. alpha., a potent agonist of the vascular thromboxane/endoperoxide receptor, is a platelet thromboxane/endoperoxide receptor antagonist'.
Bito, L.Z., Prostaglandins and Related Compounds as Potential Ocular Therapeutic Agents; . Biological Protection with Prostaglandins, Cohen, M.M.; ed.; Boca Ratan, 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, Drace, S.M. & Neufeld, A.H.eds., New York, Grune & Stratton, 1984, pp. 477-505.
Nilsson, et. al., "Increases Uveoscleral Outflow," Invest. Opthalmol. Vis.Sci, 28 (suppl), 284, 1987.
Bito, L.Z., "Prostaglandins, Old concepts and New Perspectives," Arch. Ophthalmol 105, 1036, 1987.
Siebold, et.al., "Esterified prostaglandin shows 'potent' promise," Prodrug, May 3, 1989.

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