# US 5,705,510 A · Use of cabergoline and related ergoline derivatives for controlling intraocular pressure

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 5,705,510 A
- Document ID: US5705510A
- Status: Granted
- Kind: A
- Application number: 08/547,755
- Filed: 1995-10-25
- Granted: 1998-01-06
- Earliest claimed: 1993-08-18
- Assignees: Alcon Laboratories, Inc.
- Inventors: Louis DeSantis, Jr.; Verney L. Sallee; Marsha A. McLaughlin; Manoj L. Maniar
- Web page: https://patentgrep.com/patent/US5705510A

## CPC

- A61K 31/48: Ergoline derivatives, e.g. lysergic acid, ergotamine
- A61K 9/0048: {Eye, e.g. artificial tears}
- 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

The use of certain dopaminergic compounds for controlling elevations of intraocular pressure is disclosed. The compounds are ergoline derivatives. The most preferred compound is cabergoline. The compounds have been found to produce a significant reduction of intraocular pressure.

## Claims

### Claim 1

A method of controlling elevations of intraocular pressure which comprises applying to the eye a therapeutically effective amount of a topical ophthalmic composition comprising an amount of a compound of the following formula effective to control intraocular pressure: ##STR3## wherein: R.sub.1 represents a hydrogen atom or a methyl group;
R.sub.2 represents a hydrogen or halogen atom, a methyl or formyl group or a group of the formula S--R.sub.7 or SO--R.sub.7, wherein R.sub.7 represents an alkyl group having from 1 to 4 carbon atoms or a phenyl group;
R.sub.3 represents a hydrogen atom or a methoxy group;
R.sub.4 represents a hydrocarbon group having from 1 to 4 carbon atoms, benzyl or phenethyl; and
X is OH or NR.sub.5 CONHR.sub.6, wherein each of R.sub..sub.5 and R.sub.6 independently represents an alkyl group having from 1 to 4 carbon atoms, a cyclohexyl group or a substituted or unsubstituted phenyl group or an acid and water-soluble group such as (CH2).sub.n N(CH3).sub.2 in which n is an integer, with the proviso that R.sub.5 and R6 cannot both be a said acid and water soluble group; and a pharmaceutically acceptable vehicle therefor.

### Claim 2 (depends on 1)

A method according to claim 1, wherein X is NR.sub.5 CONHR.sub.6.

### Claim 3 (depends on 2)

A method according to claim 2, wherein the compound comprises cabergoline.

### Claim 4 (depends on 1)

A method according to claim 1, wherein the pharmaceutically acceptable vehicle comprises a non-aqueous microemulsion.

### Claim 5 (depends on 4)

A method according to claim 4, wherein the microemulsion comprises an internal phase, an external phase, and an emulsifying agent, said internal phase comprising a non-aqueous, oxygen-containing, pharmaceutically acceptable polar solvent, and said external phase comprising a lower alkyl ester of a C.sub.8-22 fatty acid, a medium chain triglyceride or a super-refined vegetable oil.

### Claim 6 (depends on 3)

A method according to claim 3, wherein the microemulsion further comprises a monoglyceride in an amount sufficient to enhance the viscosity of the microemulsion when it is topically applied to the eye.

### Claim 7 (depends on 6)

A method according to claim 6, wherein the monoglyceride comprises mono myristoyl glycerol.

### Claim 8 (depends on 5)

A method according to claim 5, wherein the polar solvent is selected from propylene glycol, glycerol, ethylene glycol and polyethylene glycol, and the external phase comprises a super-refined vegetable oil selected from peanut oil and corn oil.

### Claim 9 (depends on 1)

A method according to claim 1, wherein the composition comprises a first part and a second part, the first part comprising said compound in the form of a lyophilized powder, and the second part comprising said pharmaceutically acceptable vehicle in the form of an aqueous, buffered solution.