Syntex (u.s.a.) Inc.

L David Waterbury

Robin D Clark

John H Fried

Gary F Cooper

Joseph M Muchowski

Howard J Ringold

A Peter Roszkowski

This invention covers a compound of the formula ##STR1## wherein R is hydrogen, lower alkyl or a pharmaceutically acceptable, non-toxic salt of a compound wherein R is hydrogen; X is hydrogen, halo, trifluoromethyl, lower alkyl or lower alkoxy, Y is lower alkyl or ##STR2## wherein Z is hydrogen, halo, methyl, methoxy or trifluoromethyl; and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is .alpha. the other is .beta..

11-substituted-16-phenoxy and 16-substituted phenoxy-prostatrienoic acid

Intraocular hypertensive diseases such as glaucoma are treated with compounds represented by formula I ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein

Method for treating intraocular hypertension

N-(lower alkyl)-2-(3'-ureidobenzyl)pyrrolidines and N-(lower alkyl)-2-(3'-ureidobenzyl)-5-(lower alkyl)pyrrolidines are useful for lowering intraocular pressure in mammals, for example, in the treatment of glaucoma.

N-(lower alkyl)-2-(3'ureidobenzyl)pyrrolidines

11-substituted-16-phenoxy and 16-substituted phenoxy-prostatrienioc acid

Intraocular hypertensive diseases such as glaucoma are treated with compounds represented by formula I ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein R.sub.1 is alkyl of two to four carbon atoms;

Arylalkyl amines useful for lowering intraocular pressure

Elevated intraocular pressure diseases such as glaucoma are treated with compounds represented by formula I ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein R.sub.1 is alkyl of two to four carbon atoms; and

This invention relates to a method of treatment of ocular hypertension and to a topical ophthalmic pharmaceutical composition useful for management of ocular hypertension. When administered topically to an eye with increased intraocular pressure, .+-.2-[(3,4-methylenedioxy)phenethyl]-5-[(3-carboxamido-4-hydroxy)-.alpha. -hydroxybenzyl]pyrrolidines effectively decrease intraocular pressure, inhibit the deterioration of the eye due to intraocular hypertension or glaucoma and relieve the symptoms of already existing glaucoma or other ophthalmic disease.

Treatment and prevention of ocular hypertension

This invention concerns the novel use of certain known thiazoles, particularly acylaminothiazoles and thiazolecarboxamides, as intraocular pressure lowering agents. When administered topically to the eye with increased intraocular pressure the compounds are effective in decreasing intraocular pressure, in preventing development of acute or chronic ocular hypertension including glaucoma, in inhibiting the further deterioration of the eye due to intraocular hypertension, or in relieving the symptoms of already existing ophthalmic disease.

Topical treatment of ocular hypertension

The present invention concerns a new use of certain pyrrolo-pyrrole compounds of chemical formulas (A), (B), (C), and (D): ##STR1## for the treatment of microvascular complications associated with diabetes such as, for example, diabetic retinopathy, diabetic nephropathy and diabetic neuropathy. Pyrrolo-pyrrole compounds prevent development, restrain further progress and relieve symptoms of already developed microvascular complications of diabetes.

Use of pyrrolo-pyrrole in treating microvascular diseases associated

Certain known pyrroles have been found to be useful in the topical treatment of various ophthalmic diseases in mammals; especially those originating from or associated with inflammation such as, for example, cystoid macular edema, glaucoma, conjunctivitis, uveitis, diabetic retinopathy and eye surgery or trauma.

Use of pyrrolo pyrroles in treatment of ophthalmic diseases

Methods of and compositions for lowering intraocular pressure using compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each independently selected from the group consisting of hydrogen, lower alkyl, optionally substituted phenyl, and optionally substituted phenyl lower alkyl; or wherein R.sup.1 and R.sup.2 taken together form an optionally substituted benzo;

Method for lowering intraocular pressure

Compositions containing and methods of employing as the essential ingredients substituted xanthone carboxylic acid compounds which are useful in the prevention of complications of diabetes. Methods for preparing these compounds and the compositions and intermediates therein are also disclosed.

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San Mateo, CA, United States of America

L David Waterbury