# US 4,396,625 A · Treatment of glaucoma or ocular hypertension and ophthalmic composition

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- Number: US 4,396,625 A
- Document ID: US4396625A
- Status: Granted
- Kind: A
- Application number: 06/257,563
- Filed: 1981-04-27
- Granted: 1983-08-02
- Earliest claimed: 1980-05-13
- Assignees: Sumitomo Chemical Company, Limited
- Inventors: Kaoru Yamamori; Yoshihiro Komuro; Yoshiya Yamahira; Takeshi Noguchi
- Web page: https://patentgrep.com/patent/US4396625A

## CPC

- A61K 31/425: Thiazoles
- A61K 9/0048: {Eye, e.g. artificial tears}
- 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

Method for the treatment of glaucoma or ocular hypertension by topically applying to the eye an effective amount of 2-(3-tert.-butylamino-2-hydroxypropylthio)-4-(5-carbamoyl-2-thienyl)-thiaz ole or its acid addition salt to lower the intraocular pressure of the diseased eye.

## Claims

### Claim 1

The method of treating glaucoma or ocular hypertension by topically applying to the eye an effective amount of 2-(3-tert.-butylamino-2-hydroxypropylthio)-4-(5-carbamoyl-2-thienyl)-thiaz ole or its acid addition salt to lower the intra-ocular pressure of the diseased eye.

### Claim 2 (depends on 1)

The method of claim 1 wherein an inorganic or organic acid salt is used as an acid addition salt.

### Claim 3 (depends on 2)

The method of claim 2 wherein the inorganic acid salt is borate, hydrochloride, sulfate, nitrate or phosphate.

### Claim 4 (depends on 2)

The method of claim 2, wherein the organic acid salt is acetate, oxalate, lactate, maleate, succinate, tartarate, fumarate, citrate, glutarate, L-glutamate, d-camphorsulfonate or gluconate.

### Claim 5 (depends on 1)

The method of claim 1, wherein a hydrochloride is used as the acid addition salt.

### Claim 6 (depends on 1)

The method of claim 1, wherein an acetate is used as the acid addition salt.

### Claim 7 (depends on 1)

The method of claim 1, wherein a maleate is used as the acid addition salt.

### Claim 8

The ophthalmic composition for the treatment of glaucoma comprising an aqueous solution of an effective amount of acid addition salt of 2-(3-tert.-butylamino-2-hydroxypropylthio)-4-(5-carbamoyl-2-thienyl)-thiaz ole to lower the intra-ocular pressure of the eye and an isotonic agent.

### Claim 9 (depends on 8)

The composition of claim 8, wherein an inorganic or organic acid salt is used as the acid addition salt.

### Claim 10 (depends on 9)

The composition of claim 9, wherein the inorganic acid salt is borate, hydrochloride, sulfate, nitrate or phosphate.

### Claim 11 (depends on 9)

The composition of claim 9, wherein the organic acid salt is acetate, oxalate, lactate, maleate, succinate, tartarate, fumarate, citrate, glutarate, L-glutamate, d-camphorsulfonate or gluconate.

### Claim 12 (depends on 8)

The composition of claim 8, wherein a hydrochloride is used as the acid addition salt.

### Claim 13 (depends on 8)

The composition of claim 8, wherein an acetate is used as the acid addition salt.

### Claim 14 (depends on 8)

The composition of claim 8, wherein a maleate is used as the acid addition salt.

### Claim 15 (depends on 8)

The ophthalmic composition of claim 8, wherein the composition contains D-mannitol as an isotonic agent.

### Claim 16 (depends on 8)

The ophthalmic composition of claim 8, wherein the composition contains a combination of glycine and hydrochloric acid as buffer.

### Claim 17 (depends on 15)

The ophthalmic composition according to claim 15, wherein the composition contains a combination of glycine and hydrochloric acid as buffer.
