# US 5,346,887 A · Glaucoma treatment

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- Number: US 5,346,887 A
- Document ID: US5346887A
- Status: Granted
- Kind: A
- Application number: 07/690,148
- Filed: 1991-04-23
- Granted: 1994-09-13
- Earliest claimed: 1987-10-06
- Assignees: Abbott Laboratories
- Inventors: Herman H. Stein; Jacob J. Plattner; Steven R. Crowley
- Web page: https://patentgrep.com/patent/US5346887A

## CPC

- A61K 38/553: {Renin inhibitors}
- 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)

## Abstract

A method and a composition for treating or reducing and/or controlling intraocular pressure comprising administering an effective amount of a renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; W is CO or CHOH and U is CH.sub.2 or NR.sub.2 wherein R.sub.2 is hydrogen or loweralkyl; with the proviso that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloalkylmethyl, benzyl, (alpha, alpha) -dimethylbenzyl, 4-hydroxybenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, 1-benzyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R.sub.3 is loweralkyl, loweralkenyl, ((alkoxy)alkoxy)loweralkyl, (thioalkoxy)alkyl, benzyl or heterocyclic ring substituted methyl; and R.sub.4 is substituted hydroxyalkylamino.

## Claims

### Claim 1

A method for treating glaucoma or reducing and/or controlling intraocular pressure comprising administering to a patient in need a therapeutically effective amount of the renin inhibiting compound H-((beta,beta-dimethyl)-beta-Ala)-(4-OCH.sub.3)Phe-His amide of 2(S)-amino-1-cyclohexyl-3(R),4(S)-dihydroxy-6-methylheptane, or a pharmaceutically acceptable salt or ester thereof in combination with a therapeutically effective amount of a steroidal antiinflammatory agent.

### Claim 2 (depends on 1)

The method of claim 1 wherein the steroidal antiinflammatory agent and the renin inhibiting compound are administered as components of the same composition or the steroidal antiinflammatory agent and the renin inhibiting compound are administered as separate compositions.

### Claim 3 (depends on 1)

The method of claim 1 further comprising administering a therapeutically effective amount of a beta-adrenergic antagonist compound.

### Claim 4

A method for treating glaucoma or reducing and/or controlling intraocular pressure comprising administering to a patient in need a therapeutically effective amount of the renin inhibiting compound H-((beta,beta-dimethyl)-beta-Ala)-(4-OCH.sub.3)Phe-His amide of 2(S)-amino-1-cyclohexyl-3(R),4(S)-dihydroxy-6-methylheptane, or a pharmaceutically acceptable salt or ester thereof in combination with a therapeutically effective amount of an angiotensin converting enzyme inhibiting compound.

### Claim 5 (depends on 4)

The method of claim 4 wherein the angiotensin converting enzyme inhibiting compound is selected from captopril and enalapril.

### Claim 6

A composition for treating glaucoma or reducing and/or controlling intraocular pressure comprising a pharmaceutical vehicle suitable for topical ocular administration and a therapeutically effective amount of the renin inhibiting compound H-((beta,beta-dimethyl)-beta-Ala)-(4-OCH.sub.3)Phe-His amide of 2(S)-amino-1-cyclohexyl-3(R),4(S)-dihydroxy-6-methylheptane, or a pharmaceutically acceptable salt or ester thereof in combination with a therapeutically effective amount of a steroidal antiinflammatory agent.

### Claim 7 (depends on 6)

The composition of claim 6 further comprising a therapeutically effective amount of a beta-adrenergic antagonist compound.

### Claim 8

A composition for treating glaucoma or reducing and/or controlling intraocular pressure comprising a pharmaceutical vehicle suitable for topical ocular administration and a therapeutically effective amount of the renin inhibiting compound H-((beta,beta-dimethyl)-beta-Ala)-(4-OCH.sub.3)Phe-His amide of 2(S)-amino-1-cyclohexyl-3(R),4(S)-dihydroxy-6-methylheptane, or a pharmaceutically acceptable salt or ester thereof in combination with a therapeutically effective amount of an angiotensin converting enzyme inhibiting compound.