# US 5,705,530 A · Method for reducing intraocular pressure in the mammalian eye by administration of chloride channel blockers

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- Number: US 5,705,530 A
- Document ID: US5705530A
- Status: Granted
- Kind: A
- Application number: 08/716,756
- Filed: 1996-09-23
- Granted: 1998-01-06
- Earliest claimed: 1994-11-30
- Assignees: Allergan, Inc.
- Inventors: Joseph S. Adorante; Elizabeth WoldeMussie; Guadalupe Ruiz
- Web page: https://patentgrep.com/patent/US5705530A

## CPC

- A61K 31/00: Medicinal preparations containing organic active ingredients
- A61K 31/137: Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine {or methadone}
- A61K 31/192: having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid {(cannabinoids A61K31/658)}
- A61K 31/196: the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
- A61K 31/26: Cyanate or isocyanate esters; Thiocyanate or isothiocyanate esters
- A61P 9/12: Antihypertensives
- A61P 27/02: Ophthalmic agents
- A61P 27/06: Antiglaucoma agents or miotics
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Pharmaceutical compositions and a method are disclosed for treating glaucoma and/or ocular hypertension in the mammalian eye by administering to the mammalian eye the pharmaceutical composition of the invention which contains, as the active ingredient, one or more compounds having chloride channel blocking activity. Examples of chloride channel blockers utilized in the pharmaceutical composition and method of treatment are: ##STR1## wherein R is hydrogen or a pharmaceutically-acceptable cation, e.g. an alkali or alkaline earth metal, or a quaternary amine; or R represents a ester-forming moiety, e.g. a lower alkyl radical, having up to six carbon atoms, that may be derived from a lower alkanol.

## Claims

### Claim 1

A method of treating animals of the mammalian species for glaucoma which comprises administering to the eye of a mammal having glaucoma a pharmaceutical composition comprising as its active ingredient one or more compounds having chloride channel blocking activity.

### Claim 2 (depends on 1)

A method of claim 1 wherein the composition is an ophthalmic solution, adapted for administration to the eye of a mammal in the form of eye droplets.

### Claim 3 (depends on 2)

The method of claim 2 wherein the compound having chloride channel blocking activity is present in the concentration range of 0.0001 to 1 per cent by volume.

### Claim 4 (depends on 1)

The method of claim 1 wherein the compound having chloride channel blocking activity is selected from the group consisting of N-phenylanthranilic acid, DPC (diphenylamine-2-carboxylic acid), IAA-94 (R(+)methylindazone, indanyloxyacetic acid 94), 2-aminomethyl phenols, MK-447 (2-aminomethyl-4-(1,1-dimethyl ethyl)-6-iodophenol hydrochloride (2) disulfonic stilbenes and DIDS (4,4'-diisothiocyanostilbene-2-2'-disulfonic acid) and 5-nitro-2(3 phenyl propyl amino)-benzoate (NPPB).

### Claim 5 (depends on 1)

The method of claim 1 wherein the compound having chloride channel blocking activity is selected from the group consisting of compounds represented by the formula: ##STR3## wherein R is hydrogen or a pharmaceutically-acceptable cation.

### Claim 6 (depends on 5)

The method of claim 5 wherein R is hydrogen or an alkali metal ion or a quaternary amine selected from the group consisting of mono-, di- and trialkyl amines, wherein each alkyl group may comprise up to six carbon atoms, ethanolamine, or caffeine or tromethamine, or a lower alkyl radical having up to six carbon atoms.

### Claim 7 (depends on 6)

The method of claim 6 where the composition is an ophthalmic solution, adapted for administration to the eye of a mammal in the form of eye droplets.

### Claim 8 (depends on 7)

The method of claim 7 wherein the composition contains approximately 0.0001 to 1 per cent weight by volume of said compound having chloride channel blocking activity.

### Claim 9 (depends on 1)

The method of claim 1 wherein the compound having chloride channel blocking activity is selected from the group consisting of MK-447 (2-aminomethyl-4-(1,1-dimethyl ethyl)-6-iodophenol and DIDS (4,4'-diisothiocyanostilbene-2-2'-disulfonic acid).

### Claim 10

A method of treating animals of the mammalian species, including humans, for the purpose of reducing intraocular pressure in the eye of the mammal comprising the step of administering to the mammal a pharmaceutical composition which comprises as its active ingredient one or more compounds having chloride channel blocking activity.

### Claim 11 (depends on 10)

The method of treatment of claim 10 where the composition is an ophthalmic solution adapted for administration to the eye of a mammal in the form of eye droplets.

### Claim 12 (depends on 11)

The method of treatment of claim 11 wherein in the ophthalmic composition the concentration of the compound having chloride channel blocking activity is in the range of approximately 0.0001 to 1 per cent weight by volume.