2-decarboxyl-2-alkoxyalkyl prostaglandins as ocular hypotensives

Details 2-decarboxyl-2-alkoxyalkyl prostaglandins as ocular hypotensives 2-decarboxyl-2-alkoxyalkyl prostaglandins as ocular hypotensives

1990-12-06

1992-08-18

Green, Randall L.

Surgery

Means for introducing or removing material from body for...

Treating material applied to or removed from external...

604298, 424427, 514573, 514913, A61M 3500

Patent

active

051394910

ABSTRACT:
The present invention relates to 2-decarboxyl-2-alkoxyalkyl prostaglandins that are potent ocular hypotentives, and are particularly suitable for the management of glaucoma. Said 2-decarboxyl-2-alkoxyalkyl prostaglandins are compounds of the 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; R is an aliphatic hydrocarbon group having from 1 to about 6 carbon atoms; one of R.sub.1 and R.sub.2 is=O, --OH or a --O(CO)R.sub.6 group, and the other one is --OH or a --O(CO)R.sub.6 group or R.sub.1 is=O and R.sub.2 is H, R.sub.3 is --OH or --O(CO)R.sub.6 ; R.sub.4 and R.sub.5 independently are hydrogen or an aliphatic hydrocarbon group having from 1 to about 6 carbon atoms; R.sub.6 is a saturated or unsturated acyclic hydrocarbon group having from 1 to about 20 carbon atoms, or --(CH.sub.2).sub.n R.sub.7 wherein n is 0-10, and R.sub.7 is an aliphatic ring from about 3 to about 7 carbon atoms or an aromatic or heteroaromatic ring; or a pharmaceutically acceptable salt of said compound.
The invention also provides a pharmaceutical product including a container adapted to dispense an ophthalmic solution in metered form and containing said 2-decarboxyl-2-alkoxyalkyl prostaglandin in admixture with a non-toxic, ophthalmically acceptable liquid vehicle.

REFERENCES:
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Villumsen et al, "Prostaglandin F.sub.2.alpha. Isopropylester Eye Drops: Effect on Introcular Pressure in Open-Angle Glaucoma", British Journal of Ophthamology; 1989, (Abstract only).

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