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Claims for Patent: 4,309,432

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Claims for Patent: 4,309,432

Title: Compositions for treating glaucoma containing a carbostyril
Abstract:This invention provides a glaucoma treating composition comprising at least one of carbostyril derivatives represented by the formula ##STR1## wherein R.sup.1 is hydrogen, lower alkyl or lower alkenyl, R.sup.2 is hydrogen or a group ##STR2## wherein R.sup.4 is lower alkyl, cycloalkyl, or lower alkyl substituted by phenyl with or without a lower alkoxy substituent on the phenyl nucleus, R.sup.3 is a group ##STR3## wherein R.sup.4 is as defined above when R.sup.2 is hydrogen, or R.sup.3 is hydrogen, hydroxyl, ureido, lower alkynyloxy, lower alkoxy having a lower alkanoyl substitutent, lower alkanoylamino or lower alkenyloxy when R.sup.2 is ##STR4## and the carbon-to-carbon bond between the 3-position and the 4-position of the carbostyril skeleton is a single bond or double bond, and pharmacologically acceptable acid addition salts thereof; and a method of treating glaucoma comprising administering said composition to a patient with glaucoma.
Inventor(s): Tanaka; Nobuyuki (Tokushima, JP), Nishinakamura; Yoichi (Ibaragi, JP), Nakagawa; Kazuyuki (Tokushima, JP)
Assignee: Otsuka Pharmaceutical Company, Ltd. (Tokyo, JP)
Application Number:06/109,057
Patent Claims: 1. An ophthalmic solution comprising about 0.1 to about 2% by weight of a compound of the formula: ##STR11## wherein R.sup.1 is hydrogen, lower alkyl or lower alkenyl, R.sup.2 is hydrogen or a group ##STR12## wherein R.sup.4 is lower alkyl, cycloalkyl or lower alkyl substituted by phenyl or substituted by phenyl having a lower alkoxy substituent on the phenyl nucleus, R.sup.3 is a group ##STR13## wherein R.sup.4 is as defined above when R.sup.2 is hydrogen, or R.sup.3 is hydrogen, hydroxyl, ureido, lower alkynyloxy, lower alkoxy having a lower alkanoyl substituent, lower alkanoylamino or lower alkenyloxy when R.sup.2 is ##STR14## and the carbon-to-carbon bond between the 3-position and the 4-position of the carbostyril skeleton is a single bond or double bond or a pharmacologically acceptable acid addition salt thereof in combination with a diluent suitable for administration to the eye.

2. An ophthalmic solution of claim 1 wherein R.sup.1 and R.sup.3 are each hydrogen, R.sup.2 is a group ##STR15## wherein R is lower alkyl, and the carbon-to-carbon bond between the 3-position and the 4-position of the carbostyril skeleton is a single bond, or pharmacologically acceptable acid addition salts thereof.

3. An ophthalmic solution of claim 2 wherein the active compound is 5-(2-hydroxy-3-tertbutylamino)-propoxy-3,4-dihydrocarbostyril.

4. An ophthalmic solution as of claim 1 wherein the diluent is water.

5. A method of treating glaucoma wherein the ophthalmic solution of claim 1 is topically administered to a patient with glaucoma.

6. A method of treating glaucoma wherein the ophthalmic solution of claim 3 is topically administered to the patient with glaucoma.

7. A method of treating glaucoma wherein the ophthalmic solution of claim 4 is topically administered to the patient with glaucoma.

8. The method of any one of claims 5 to 7 wherein the composition is instilled to the eye of the patient.

9. The method of claim 8 wherein the composition is instilled at a dose of about 0.01 to about 5 mg per day calculated as the compound for an adult.

10. The method of claim 9 wherein the composition is instilled at a dose of about 0.01 to about 0.5 mg per day calculated as the compound for an adult.
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