1,11-diesters of prostaglandin-F.sub.2.alpha. having a polar ester group at C-1
AssigneeAllergan, Inc.
InventorsMichael E. Garst, Elizabeth T. Syage, Michael B. Roof, David F. Woodward, Ming Fai Chan
Life of this patent
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AssigneeAllergan, Inc.
InventorsMichael E. Garst, Elizabeth T. Syage, Michael B. Roof, David F. Woodward, Ming Fai Chan
Estimating the term…
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.
A compound which is selected from a group consisting of 11-pivaloyl prostaglandin F.sub.2.alpha. glycolamide and 11-pivaloyl prostaglandin F.sub.2.alpha. hydroxyethyl ester.
A method of treating ocular hypertension which comprises applying to the eye a pharmaceutical composition, said composition comprising an amount sufficient to treat ocular hypertension of a compound which is selected from a group consisting of 11-pivaloyl prostaglandin F2.alpha. glycolamide and 11-pivaloyl prostaglandin F.sub.2.alpha. hydroxyethyl ester.
A pharmaceutical product comprising an ophthalmic solution for the treatment of ocular hypertension, said solution comprising an amount sufficient to treat ocular hypertension of a compound which is selected from a group consisting of 11-pivaloyl prostaglandin F.sub.2.alpha. glycolamide and 11-pivaloyl prostaglandin F.sub.2.alpha. hydroxyethyl ester.
Dependencies are inferred from the claim text.