Allergan, Inc.

Allergan Sales, Inc.

Michael B Roof

Michael E Garst

Ming Fai Chan

Robert M Burk

David Frederick Woodward

Steven Wade Andrews

Todd S Gac

Elizabeth T Syage

The invention relates to the use of omega chain modified prostaglandins as ocular hypotensive. The derivatives used in accordance with the invention are encompassed by the following structure formula I:

Cyclopentane (ene) oic acid, 2-alkenyl derivatives as therapeutic agents

Compounds of the formula ##STR1## where the hatched lines indicate alpha (.alpha.) configuration, a solid triangle is used to indicate beta (.beta.) configuration, lines on both sides of a double bond indicate cis (Z) configuration, and lines on opposite sides of the double bond indicate trans (E) configuration; R.sub.1 is alkyl of 1-10 carbons, C.sub.1 -C.sub.10 alkylphenyl, phenyl-C.sub.1 -C.sub.10 alkyl, or alkenyl of 2 to 10 carbons and having 1 to 3 double bonds; R.sub.2 is Z--OR.sub.3, Z--OCOR.sub.3, Z--OCONHR.sub.3, Z--OCOOR.sub.3, Z--NR.sub.4 R.sub.5, Z--NR.sub.4 COR.sub.3, Z--NR.sub.4 SO.sub.2 R.sub.3, Z--COOR.sub.3, Z--CONR.sub.4 R.sub.5, Z--CHO; Z is (CH.sub.2).sub.n where n is 1-6, or Z is an alkenyl group having 2 to 6 carbons and 1 or 2 double bonds, R.sub.3 is H, alkyl of 1-6 carbons, alkenyl of 2 to 6 carbons or phenyl, R.sub.4 and R.sub.5 independently are H or alkyl of 1 to 6 carbons, have ocular hypotensive activity.

1,11-diesters of prostaglandin-F.sub.2.alpha.  having a polar ester

Intraocular pressure is lowered in the eye of a mammal by administration of a pharmaceutical composition containing as active ingredient a compound of the formula ##STR1## where the dotted line represents a bond or the absence of a bond, wavy lines connected to the olefinic bond represent cis or trans configuration about the olefinic bond; R.sub.1 represents H, or CO-R.sub.3 where R.sub.3 is lower alkyl of 1 to 6 carbons, carbocyclic aryl or heterocyclic aryl; or carbocyclic aryl or heteroaryl substituted lower alkyl group; R.sub.2 represents H or lower alkyl of 1 to 6 carbons, and n is an integer between 0 and 8.

Method of lowering intraocular pressure by administering a

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Los Angeles, CA, United States of America

Michael B Roof