Polar C-1 esters of prostaglandins

Details Polar C-1 esters of prostaglandins Polar C-1 esters of prostaglandins

1992-02-04

1994-02-22

Gerstl, Robert

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Ester doai

514120, 560121, A61K 31557

Patent

active

052887545

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 O, NH, S and NR, where R is an aliphatic hydrocarbon group of about 1 to about 6 carbon atoms; Y is a polar functional group; one of R.sub.1 and R.sub.2 is .dbd.O, --OH or a --O(CO)R.sub.4 group, and the other one is --OH or a --O(CO)R.sub.4 group or R.sub.1 is .dbd.O and R.sub.2 is 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.
Also disclosed are pharmaceutical compositions including an effective amount of the compound of formula I or a pharmaceutically-acceptable salt thereof, in admixture with a nontoxic pharmaceutical carrier and ophthalmic solutions comprising a compound of formula I packaged for metered application. Finally, novel compounds according to Formula I are disclosed.

REFERENCES:
patent: 4599353 (1986-07-01), Bito
patent: 4783480 (1988-11-01), Wakatsuka
patent: 4994274 (1991-02-01), Chan et al.
patent: 5139491 (1992-08-01), Chan et al.
Bito, L. Z., "Prostaglandins and Related Compounds as Potential Ocular Therapeutic Agents," Biological Protection with Prostaglandins, Cohen, M. M., ed., Boca 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, Drance, S. M. and Neufeld, A. H. eds., New York, Grune & Stratton, 1984, pp. 477-505.
Nilsson, et al., "Increases Uveoscleral Outflow," Invest. Ophthalmol. 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, 5, 3, 1989.

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