# US 10,765,750 B2 · Pharmaceutical composition containing pyridylaminoacetic acid compound

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- Number: US 10,765,750 B2
- Document ID: US10765750B2
- Status: Granted
- Kind: B2
- Application number: 16/658,585
- Filed: 2019-10-21
- Published: 2020-02-13
- Granted: 2020-09-08
- Earliest claimed: 2014-01-10
- Assignees: Santen Pharmaceutical Co., Ltd.
- Applicants: Santen Pharmaceutical Co., Ltd.
- Inventors: Yoko Endo
- Web page: https://patentgrep.com/patent/US10765750B2

## CPC

- A61K 47/183: {Amino acids, e.g. glycine, EDTA or aspartame}
- A61K 9/0048: {Eye, e.g. artificial tears}
- A61K 31/444: containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
- A61K 47/22: Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
- A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
- A61K 47/44: Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin (synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14)
- A61P 9/12: Antihypertensives
- A61P 27/02: Ophthalmic agents
- A61P 27/06: Antiglaucoma agents or miotics
- A61K 47/02: Inorganic compounds
- A61K 47/12: Carboxylic acids; Salts or anhydrides thereof
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- 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
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

The purpose of the present invention is to provide a pharmaceutical composition that comprises a specific compound and exhibits a superior preservation efficacy, the specific compound being stable within the pharmaceutical composition, and to provide methods for improving the stability of the specific compound within the pharmaceutical composition and the preservation efficacy of the pharmaceutical composition. The pharmaceutical composition according to the present invention comprises isopropyl (6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate or a salt thereof, and further comprises edetic acid or a salt thereof.

## Claims

### Claim 1

A pharmaceutical composition comprising isopropyl (6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate or a salt thereof and a nonionic surfactant, which further comprises edetic acid or a salt thereof,
wherein the nonionic surfactant includes polyoxyethylene castor oil,
wherein the pharmaceutical composition does not comprise sorbic acid;
wherein the content of the nonionic surfactant is in a range of 0.001 to 5% (w/v), and
wherein the content of the edetic acid or a salt thereof is in a range of 0.001 to 1% (w/v).

### Claim 2 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the polyoxyethylene castor oil includes polyoxyethylene castor oil selected from the group consisting of polyoxyl 5 castor oil, polyoxyl 9 castor oil, polyoxyl 15 castor oil, polyoxyl 35 castor oil, and polyoxyl 40 castor oil.

### Claim 3 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the content of the nonionic surfactant is in a range of 0.5 to 3% (w/v).

### Claim 4 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the content of the nonionic surfactant is in a range of 1 to 20,000 parts by mass relative to 1 part by mass of isopropyl 6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate or a salt thereof.

### Claim 5 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the content of isopropyl 6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate or a salt thereof is in a range of 0.0001 to 0.1% (w/v).

### Claim 6 (depends on 5)

The pharmaceutical composition according to claim 5, wherein the content of isopropyl 6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate or a salt thereof is in a range of 0.001 to 0.003% (w/v).

### Claim 7 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the content of edetic acid or a salt thereof is in a range of 0.01 to 0.1% (w/v).

### Claim 8 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the content of edetic acid or a salt thereof is in a range of 0.1 to 1,000 parts by mass relative to 1 part by mass of isopropyl 6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate or a salt thereof.

### Claim 9 (depends on 1)

The pharmaceutical composition according to claim 1, which further comprises boric acid or a salt thereof, citric acid or a salt thereof, or acetic acid or a salt thereof.

### Claim 10 (depends on 1)

The pharmaceutical composition according to claim 1, which is filled into a container made of polyethylene.

### Claim 11 (depends on 1)

The pharmaceutical composition according to claim 1, for prevention or treatment of glaucoma or ocular hypertension, or for reduction of intraocular pressure.

### Claim 12

A method for stabilizing isopropyl (6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate or a salt thereof comprising adding edetic acid or a salt thereof and polyoxyethylene castor oil into a pharmaceutical composition comprising isopropyl (6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate or a salt thereof,
wherein the pharmaceutical composition does not comp rise sorbic acid,
wherein the content of the nonionic surfactant is in a range of 0.001 to 5% (w/v); and
wherein the content of the edetic acid or a salt thereof is in a range of 0.001 to 1% (w/v).