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Details for Patent: 5,194,429

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Details for Patent: 5,194,429

Title: Ocular hypotensive agents
Abstract:The present invention relates to an ocular hypotensive composition and a composition for treatment of glaucoma which comprising an amount of 20-substituted-PGs or 20-substituted-15-keto-PGs effective as an ocular hypotensive agent; these compounds exhibit no or little side effects such as transient ocular hypertensive response, hyperemia of conjunctiva or of iris, dacryops, lema, closed eye and the like.
Inventor(s): Ueno; Ryuzo (Nishinomiya, JP), Ueno; Ryuji (Nishinomiya, JP), Oda; Tomio (Sanda, JP)
Assignee: K.K. Ueno Seiyaku Oyo Kenkyujo (Osaka, JP)
Filing Date:Nov 19, 1990
Application Number:07/615,515
Claims:1. A method for treating ocular hypertension in a patient needing such treating which comprises administering to said patient an amount of a prostaglandin effective to treat ocular hypertension, wherein the prostaglandin is represented by formula (I):

(in which R is hydroxy, hydroxy C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.2 alkyl); Y is a saturated or unsaturated C.sub.2-6 hydrocarbon chain; Z is a saturated or unsaturated C.sub.7-9 (aliphatic) hydrocarbon straight chain; or a physiologically acceptable salt or esterified carboxyl group derivative selected from the group consisting of C.sub.1-8 alkyl, C.sub.3-6 cycloalkyl, benzyl, phenyl, C.sub.1-3 hydroxyalkyl, C.sub.1-2 alkoxy C.sub.1-3 alkyl, tri C.sub.1-2 alkylsilyl, and tetrahydropyranyl.

2. The method of claim 1, wherein the esterified carboxyl group derivative is a C.sub.1 -C.sub.4 alkyl group.

3. The method of claim 1, wherein the Z is represented by a formula (II): ##STR7## (in which R.sub.2 is a C.sub.2-4 alkyl group).

4. The method of claim 3, wherein the R.sub.2 is an ethyl group.

5. The method for treating glaucoma in a patient needing such treatment which comprises administering to said patient an amount of a prostaglandin effective to treat glaucoma, wherein the prostaglandin is represented by a formula (I): ##STR8## (in which R is hydroxy, hydroxy C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.2 alkyl); Y is a saturated or unsaturated C.sub.2-6 hydrocarbon chain; Z is a saturated or unsaturated C.sub.7-9 (aliphatic) hydrocarbon straight chain; or a physiologically acceptable salt or esterified carboxyl group derivative selected from the group consisting of C.sub.1-8 alkyl, C.sub.3-6 cycloalkyl, benzyl, phenyl, C.sub.1-3 hydroxyalkyl, C.sub.1-2 alkoxy C.sub.1-3 alkyl, tri C.sub.1-2 alkylsilyl, and tetrahydropyranyl.

6. An ocular hypotensive composition comprising an amount of a prostaglandin effective as an ocular hypotensive agent and a pharmaceutically acceptable carrier, wherein the prostaglandin is represented by a formula (IV): ##STR9## (in which R is hydroxy, hydroxy C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.2 alkyl); or a physiologically acceptable salt or a C.sub.1-4 alkyl ester.

7. The composition of claim 6, wherein the A is ##STR10##

8. A method for treating ocular hypertension in a patient needing such treating which comprises administering to said patient an amount of a 13,14-unsaturated-15-keto-prostaglandin A, E or F having a C.sub.2 -C.sub.4 alkyl group substituent at the 20-position effective to treat ocular hypertension.

9. The method of claim 8, wherein the carboxyl group at the end of the .alpha.-chain in the 13,14-unsaturated-15-keto-prostaglandin A, E or F having a C.sub.2 -C.sub.4 alkyl group substituent at the 20-position is in the form of an alkyl ester.

10. The method of claim 8, wherein the 13,14-unsaturated-15-keto-prostaglandin A, E or F having a C.sub.2 -C.sub.4 alkyl group substituent at the 20-position is a 13,14-unsaturated-15-keto-20-ethyl-prostaglandin A, E or F.

11. A method for treating glaucoma in a patient needing such treating which comprises administering to said patient an amount of a 13,14-unsaturated-15-keto-prostaglandin A, E or F having a C.sub.2 -C.sub.4 alkyl group substituent at the 20-position effective to treat glaucoma.

12. An ocular hypotensive composition comprising an amount of a 13,14-unsaturated-15-keto-prostaglandin A, E or F effective as an ocular hypotensive agent and a pharmaceutically acceptable carrier.

13. A method for treating ocular hypertension in a patient needing such treating which comprises administering to said patient an amount of a prostaglandin effective to treat ocular hypertension, wherein the prostaglandin is represented by a formula (II): ##STR11## (in which R is hydroxy, hydroxy C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.2); Y is a saturated or unsaturated C.sub.2-6 hydrocarbon chain; Z is a C.sub.7 -C.sub.9 saturated or unsaturated aliphatic, alicyclic, aralkyl or aromatic hydrocarbon; or a physiologically acceptable salt or esterified carboxyl group derivative thereof.
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