IP Library › Granted Patent US 12,636,367
Granted Patent B2
US 12,636,367 · App. 18/479,338 · Granted May 26, 2026

Pharmaceutical composition containing pyridylaminoacetic acid compound

Inventor: Yoko Endo (Ikoma, JP)
Assignee: SANTEN PHARMACEUTICAL CO., LTD.
A61K47/183A61K9/0048A61K31/444A61K47/22A61K47/26A61K47/44A61K47/02A61K47/12Y02A50/30
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Quick Facts
Patent No.
US 12,636,367
App. No.
18/479,338
Granted
May 26, 2026
Kind
B2
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 (19)

1 . A method for stabilizing isopropyl (6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate or a salt thereof, the method comprising preparing a pharmaceutical composition by combining (i) isopropyl (6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate or a salt thereof as a sole active ingredient, (ii) citric acid or a salt thereof, (iii) polyoxyethylene castor oil, (iv) edetic acid or a salt thereof, and (v) glycerin, wherein

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

the content of the citric acid or the salt thereof is in a range of 0.1 to 0.2% (w/v),

the content of the polyoxyethylene castor oil in the pharmaceutical composition is in a range of 0.1 to 3% (w/v),

the content of the edetic acid or a salt thereof in the pharmaceutical composition is in a range of 0.01 to 0.02% (w/v),

the content of the glycerin is in a range of 2.2 to 3% (w/v),

the polyoxyethylene castor oil is not polyoxyethylene hardened castor oil,

a number of polymerization of ethylene oxide of the polyoxyethylene castor oil is in a range of 5 to 100, and

the pharmaceutical composition does not comprise sorbic acid.

2 . The method 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.

3 . The method according to claim 1 , wherein the content of the polyoxyethylene castor oil in the pharmaceutical composition is in a range of 0.8 to 2% (w/v).

4 . The method according to claim 3 , wherein the content of the polyoxyethylene castor oil in the pharmaceutical composition is in a range of 0.5 to 3% (w/V).

5 . The method according to claim 1 , wherein the content of the polyoxyethylene castor oil in the pharmaceutical composition is in a range of 50 to 2,000 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.

6 . The method according to claim 1 , wherein the content of edetic acid or a salt thereof in the pharmaceutical composition is 0.01 or 0.02% (w/v).

7 . The method according to claim 1 , wherein the content of edetic acid or a salt thereof in the pharmaceutical composition is in a range of 3 to 50 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.

8 . The method according to claim 1 , wherein the pharmaceutical composition is filled into a container made of polyethylene.

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

10 . The method according to claim 2 , wherein the polyoxyethylene castor oil includes polyoxyl 35 castor oil.

11 . The method according to claim 5 , wherein the content of the polyoxyethylene castor oil in the pharmaceutical composition is in a range of 200 to 2,000 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.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 2, 2023
From: ENDO, YOKO
To: SANTEN PHARMACEUTICAL CO., LTD.
Reel/Frame 065095/0749 →
Priority Claims (1)
JP 2014-002810 · Jan 10, 2014 · national
Continuity (6)
Continuation 16942877 · Jul 30, 2020
Continuation 16658585 · Oct 21, 2019
Continuation 16173299 · Oct 29, 2018
Continuation 15204507 · Jul 7, 2016
Continuation PCTJP2015050334 · Jan 8, 2015
Related Publication 20240024484A1 · Jan 25, 2024
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