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Last Updated: April 25, 2024

Claims for Patent: 5,166,178


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Summary for Patent: 5,166,178
Title: Ocular hypotensive agents
Abstract:The present invention relates to ocular hypotensive agents which contains 13,14-dihydro-15-keto-prostagrandins, which shows no transient ocular hypertensive response that PGs usually show.
Inventor(s): Ueno; Ryuzo (Nishinomiya, JP), Ueno; Ryuji (Nishinomiya, JP)
Assignee: K.K. Ueno Seiyaku Oyo Kenkyujo (Osaka, JP)
Application Number:07/760,269
Patent Claims: 1. A topical ocular composition comprising an amount effective as an ocular hypotensive agent of a 13,14-dihydro-15-keto-prostaglandin represented by the following formula (I): ##STR16## wherein A is ##STR17## wherein R is hydroxy, hydroxy C.sub.1-3 alkyl or C.sub.1-2 alkyl; Y is a saturated or unsaturated C.sub.2-6 hydrocarbon chain which is unsubstituted or substituted by oxo, halogen, an alkyl group or hydroxyl; Z is C.sub.1-10 saturated or unsaturated hydrocarbon forming a straight-chain, a branched-chain or a ring, which is unsubstituted or substituted by halogen, an alkyl group, an alkoxy group, hydroxyl, a phenyl group or a phenoxy group; or the physiologically acceptable salts and carboxylic acid esters of the compounds of formula (I); and a pharmaceutically acceptable carrier.

2. The ocular hypotensive composition according to claim 1, wherein the carboxyl group at the end of the .alpha.-chain in the 13,14-dihydro-15-keto-prostaglandin is in the form of an alkyl ester.

3. The ocular hypotensive composition according to claim 1, wherein the 13,14-dihydro-15-keto-prostaglandin is in the form of 20-alkyl having an alkyl group at the C-20 position.

4. A method for treating ocular hypertension in a human patient needing such treating which comprises administering to said patient an amount of a 13,14-dihydro-15-keto-prostaglandin of the formula (I) effective to treat ocular hypertension ##STR18## wherein A is ##STR19## wherein R is hydroxy, hydroxy C.sub.1-3 alkyl or C.sub.1-2 alkyl; Y is a saturated or unsaturated C.sub.2-6 hydrocarbon chain which is unsubstituted or substituted by oxo, halogen, an alkyl group or hydroxyl; Z is a C.sub.1-10 saturated or unsaturated hydrocarbon forming a straight-chain, a branched-chain or a ring, which is unsubstituted or substituted by halogen, an alkyl group, an alkoxy group, hydroxyl, a phenyl group or a phenoxy group; or the physiologically acceptable salts and carboxylic acid esters of the compounds of formula (I).

5. A method for treating glaucoma in a human patient needing such treatment which comprises administering to said patient an amount of a 13,14-dihydro-15-keto-prostaglandin of the following formula (I) effective to treat glaucoma ##STR20## wherein A is ##STR21## wherein A is hydroxy, hydroxy C.sub.1-3 alkyl or C.sub.1-2 alkyl; Y is a saturated or unsaturated C.sub.2-6 hydrocarbon chain which is unsubstituted or substituted by oxo, halogen, an alkyl group or hydroxyl; Z is a C.sub.1-10 saturated or unsaturated hydrocarbon forming a straight-chain, a branched-chain or a ring, which is unsubstituted or substituted by halogen, an alkyl group, an alkoxy group, hydroxyl, a phenyl group or a phenoxy group; or the physiologically acceptable salts and carboxylic acid esters of the compounds of formula (I).

6. The method of claim 4, wherein the carboxyl group at the end of the .alpha.-chain in the 13,14-dihydro-15-keto-prostaglandin is in the form of an alkyl ester.

7. The method of claim 4, wherein the 13,14-dihydro-15-keto-prostaglandin is in the form of a 20-alkyl having an alkyl group at the C-20 position.

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