Patent US4309432A successfully refreshed from Google Patents.
US4309432A
Expired / Lapsed
US
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Compositions for treating glaucoma containing a carbostyril
Assignee: Otsuka Pharmaceutical Co Ltd
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Filing: 1980-01-02
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Granted: 1982-01-05
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Expires: 2000-01-02
Abstract
Abstract This invention provides a glaucoma treating composition comprising at least one of carbostyril derivatives represented by the formula ##STR1## wherein R 1 is hydrogen, lower alkyl or lower alkenyl, R 2 is hydrogen or a group ##STR2## wherein R 4 is lower alkyl, cycloalkyl, or lower alkyl substituted by phenyl with or without a lower alkoxy substituent on the phenyl nucleus, R 3 is a group ##STR3## wherein R 4 is as defined above when R 2 is hydrogen, or R 3 is hydrogen, hydroxyl, ureido, lower alkynyloxy, lower alkoxy having a lower alkanoyl substitutent, lower alkanoylamino or lower alkenyloxy when R 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.
Inventors
- 👤 Nobuyuki Tanaka
- 👤 Yoichi Nishinakamura
- 👤 Kazuyuki Nakagawa
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-03 09:06
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/47
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
146 words
An ophthalmic solution comprising about 0.1 to about 2% by weight of a compound of the formula: ##STR11## wherein R 1 is hydrogen, lower alkyl or lower alkenyl, R 2 is hydrogen or a group ##STR12## wherein R 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 3 is a group ##STR13## wherein R 4 is as defined above when R 2 is hydrogen, or R 3 is hydrogen, hydroxyl, ureido, lower alkynyloxy, lower alkoxy having a lower alkanoyl substituent, lower alkanoylamino or lower alkenyloxy when R 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.
Claim 2
Dependent Claim
146 words
An ophthalmic solution comprising about 0.1 to about 2% by weight of a compound of the formula: ##STR11## wherein R 1 is hydrogen, lower alkyl or lower alkenyl, R 2 is hydrogen or a group ##STR12## wherein R 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 3 is a group ##STR13## wherein R 4 is as defined above when R 2 is hydrogen, or R 3 is hydrogen, hydroxyl, ureido, lower alkynyloxy, lower alkoxy having a lower alkanoyl substituent, lower alkanoylamino or lower alkenyloxy when R 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.
Claim 3
Dependent Claim
51 words
An ophthalmic solution of claim 1 wherein R 1 and R 3 are each hydrogen, R 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.
Claim 4
Dependent Claim
12 words
An ophthalmic solution of claim 2 wherein the active compound is 5-(2-hydroxy-3-tertbutylamino)-propoxy-3,4-dihydrocarbostyril.
Claim 5
Dependent Claim
12 words
An ophthalmic solution as of claim 1 wherein the diluent is water.
Claim 6
Dependent Claim
20 words
A method of treating glaucoma wherein the ophthalmic solution of claim 1 is topically administered to a patient with glaucoma.
Claim 7
Dependent Claim
20 words
A method of treating glaucoma wherein the ophthalmic solution of claim 3 is topically administered to the patient with glaucoma.
Claim 8
Dependent Claim
20 words
A method of treating glaucoma wherein the ophthalmic solution of claim 4 is topically administered to the patient with glaucoma.
Claim 9
Independent Claim
21 words
The method of any one of claims 5 to 7 wherein the composition is instilled to the eye of the patient.
Claim 10
Dependent Claim
29 words
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.
Claim 11
Dependent Claim
29 words
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.
References Cited (Backward Citations)
US3910924A
Cited
US3919239A
Cited
US3953456A
Cited
US3969507A
Cited
US3975391A
Cited
US3994901A
Cited
US4081447A
Cited
US4210753A
Cited
US4147869A
Cited
JPS552631A
Cited
WO1980000215A1
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1985-01-04 | 1985-07-06 | 1986-01-05 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1989-01-04 | 1989-07-06 | 1990-01-05 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1993-01-04 | 1993-07-06 | 1994-01-05 | $7700.00 | Window Closed / Lapsed |