# US 4,400,378 A · Pharmaceutical composition for the treatment of glaucoma

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

- Number: US 4,400,378 A
- Document ID: US4400378A
- Status: Granted
- Kind: A
- Application number: 06/317,260
- Filed: 1981-11-02
- Granted: 1983-08-23
- Earliest claimed: 1981-11-02
- Assignees: Karl Thomae GmbH
- Inventors: Hendricus C. Innemee; Jacobus C. A. van Meel; Adriaan De Jonge; Petrus B. M. W. M. Timmermans; Pieter A. van Zwieten
- Web page: https://patentgrep.com/patent/US4400378A

## CPC

- A61K 31/42: Oxazoles
- A61K 31/425: Thiazoles
- 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

The method of treating glaucoma with compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, alkyl of 1 to 4 carbon atoms, hydroxy-(alkyl of 1 to 4 carbon atoms), benzyl, halo-benzyl, methyl-benzyl, methoxy-benzyl or allyl; X is oxygen or sulfur; and n is 2 or, when X is sulfur, also 1; or non-toxic, pharmacologically acceptable acid addition salts thereof, and pharmaceutical compositions for use in said treatment.

## Claims

### Claim 1

The method of treating glaucoma in a warm-blooded animal, which comprises topically administering to the affected eye of said animal an effective intraocular pressure reducing amount of a compound of the formula ##STR3## wherein R.sub.1 is hydrogen, alkyl of 1 to 4 carbon atoms, hydroxy-(alkyl of 1 to 4 carbon atoms), benzyl, halo-benzyl, methyl-benzyl, methoxy-benzyl or allyl;
X is oxygen or sulfur; and
n is 2;
or a non-toxic, pharmacologically acceptable acid addition salt thereof.

### Claim 2 (depends on 1)

The method of claim 1, wherein
R.sub.1 is hydrogen, alkyl of 1 to 4 carbon atoms or allyl,
n is 2, and
X is oxygen or sulfur.

### Claim 3 (depends on 1)

The method of claim 1, where said compound is 2-amino-6-ethyl-5,6,7,8-tetrahydro-4H-oxazolo[5,4-d]azepine or a non-toxic, pharmacologically acceptable acid addition salt thereof.

### Claim 4 (depends on 1)

The method of claim 1, where said compound is 2-amino-6-allyl-5,6,7,8-tetrahydro-4H-oxazolo[5,4-d]azepine or a non-toxic, pharmacologically acceptable acid addition salt thereof.

### Claim 5 (depends on 1)

The method of claim 1, wherein said compound is 2-amino-6-allyl-5,6,7,8-tetrahydro-4H-thiazolo[5,4-d]azepine or a non-toxic, pharmacologically acceptable acid addition salt thereof.

### Claim 6 (depends on 1)

The method of claim 1, where said intraocular pressure reducing amount is 5 to 600 .mu.gm.

### Claim 7 (depends on 1)

The method of claim 1, where said intraocular pressure reducing amount is 20 to 500 .mu.gm.