IP Library › Patent Application 17841433
Patent Application
App. No. 17/841,433

OPHTHALMIC COMPOSITIONS

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Patent No.
US None
App. No.
17/841,433
Abstract

The present disclosure provides an ophthalmic composition comprising 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate or its pharmaceutically acceptable salts; about 0.01% weight/volume to about 1.0% weight/volume of a buffer; and about 0.01% weight/volume to about 10% weight/volume of a tonicity agent.

Claims (265)

1 . An ophthalmic formulation, consisting essentially of:

A) 0.0285 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.015 weight/volume % of benzalkonium chloride,

water, and

a pH of 5;

B) 0.057 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.015 weight/volume % of benzalkonium chloride,

water, and

a pH of 5;

C) 0.0285 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.005 weight/volume % of latanoprost,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.015 weight/volume % of benzalkonium chloride,

water, and

a pH of 5;

D) 0.0285 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.005 weight/volume % of latanoprost,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.02 weight/volume % of benzalkonium chloride,

water, and

a pH of 5;

E) 0.0233 weight/volume % of a dihydrochloride salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.015 weight/volume % of benzalkonium chloride,

water, and

a pH of 4.8; or

F) 0.0143 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.0116 weight/volume % of a dihydrochloride salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.008 weight/volume % of benzalkonium chloride,

water, and

a pH of 4.9.

2 . The ophthalmic formulation of claim 1 , wherein the 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate is (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate.

3 . The ophthalmic formulation of claim 1 , wherein the mannitol is D-mannitol.

4 . The ophthalmic formulation of claim 1 , wherein the polyoxyl 40 stearate is Myrj-52.

5 . The ophthalmic formulation of claim 1 , wherein the polyethoxylated castor oil is Cremophor RH 40.

6 . The ophthalmic formulation of claim 1 , which is a topical ophthalmic formulation.

7 . The ophthalmic formulation of claim 1 , which is packaged in a unit dose form.

8 . The ophthalmic formulation of claim 1 , which is packaged in a multidose form.

9 . The ophthalmic formulation of claim 1 , which is in a plastic storage container.

10 . The ophthalmic formulation of claim 1 , consisting of:

A) 0.0285 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.015 weight/volume % of benzalkonium chloride,

water, and

a pH of 5;

B) 0.057 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.015 weight/volume % of benzalkonium chloride,

water, and

a pH of 5;

C) 0.0285 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.005 weight/volume % of latanoprost,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.015 weight/volume % of benzalkonium chloride,

water, and

a pH of 5;

D) 0.0285 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.005 weight/volume % of latanoprost,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.02 weight/volume % of benzalkonium chloride,

water, and

a pH of 5;

E) 0.0233 weight/volume % of a dihydrochloride salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.015 weight/volume % of benzalkonium chloride,

water, and

a pH of 4.8; or

F) 0.0143 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.0116 weight/volume % of a dihydrochloride salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.008 weight/volume % of benzalkonium chloride,

water, and

a pH of 4.9.

11 . A method of treating an ophthalmic disease in a subject in need thereof, comprising topically administering to an eye of the subject an ophthalmic formulation consisting essentially of:

A) 0.0285 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.015 weight/volume % of benzalkonium chloride,

water, and

a pH of 5;

B) 0.057 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.015 weight/volume % of benzalkonium chloride,

water, and

a pH of 5;

C) 0.0285 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.005 weight/volume % of latanoprost,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.015 weight/volume % of benzalkonium chloride,

water, and

a pH of 5;

D) 0.0285 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.005 weight/volume % of latanoprost,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.02 weight/volume % of benzalkonium chloride,

water, and

a pH of 5;

E) 0.0233 weight/volume % of a dihydrochloride salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.015 weight/volume % of benzalkonium chloride,

water, and

a pH of 4.8; or

F) 0.0143 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.0116 weight/volume % of a dihydrochloride salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.008 weight/volume % of benzalkonium chloride,

water, and

a pH of 4.9.

12 - 24 . (canceled)

25 . The method of claim 11 , wherein the 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate is (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate.

26 . The method of claim 11 , wherein the mannitol is D-mannitol.

27 . The method of claim 11 , wherein the polyoxyl 40 stearate is myrj-52.

28 . The method of claim 11 , wherein the polyethoxylated castor oil is cremophor RH

40 .

29 . The method of claim 11 , wherein the ophthalmic formulation is a topical ophthalmic formulation.

30 . The method of claim 11 , wherein the ophthalmic formulation is packaged in a unit dose form.

31 . The method of claim 11 , wherein the ophthalmic formulation is packaged in a multidose form.

32 . The method of claim 11 , wherein the ophthalmic formulation is in a plastic storage container.

33 . The method of claim 11 , wherein the ophthalmic formulation consists of:

A) 0.0285 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.015 weight/volume % of benzalkonium chloride,

water, and

a pH of 5;

B) 0.057 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.015 weight/volume % of benzalkonium chloride,

water, and

a pH of 5;

C) 0.0285 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.005 weight/volume % of latanoprost,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.015 weight/volume % of benzalkonium chloride,

water, and

a pH of 5;

D) 0.0285 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.005 weight/volume % of latanoprost,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.02 weight/volume % of benzalkonium chloride,

water, and

a pH of 5;

E) 0.0233 weight/volume % of a dihydrochloride salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.015 weight/volume % of benzalkonium chloride,

water, and

a pH of 4.8; or

F) 0.0143 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.0116 weight/volume % of a dihydrochloride salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.008 weight/volume % of benzalkonium chloride,

water, and

a pH of 4.9.

34 . A method of treating glaucoma in a subject in need thereof, comprising topically administering to an eye of the subject an ophthalmic formulation consisting essentially of:

A) 0.0285 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.015 weight/volume % of benzalkonium chloride,

water, and

a pH of 5;

B) 0.057 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.015 weight/volume % of benzalkonium chloride,

water, and

a pH of 5;

C) 0.0285 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.005 weight/volume % of latanoprost,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.015 weight/volume % of benzalkonium chloride,

water, and

a pH of 5;

D) 0.0285 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.005 weight/volume % of latanoprost,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.02 weight/volume % of benzalkonium chloride,

water, and

a pH of 5;

E) 0.0233 weight/volume % of a dihydrochloride salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.015 weight/volume % of benzalkonium chloride,

water, and

a pH of 4.8; or

F) 0.0143 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.0116 weight/volume % of a dihydrochloride salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.008 weight/volume % of benzalkonium chloride,

water, and

a pH of 4.9.

35 . The method of claim 34 , wherein the 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate is (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate.

36 . The method of claim 34 , wherein the mannitol is D-mannitol.

37 . The method of claim 34 , wherein the polyoxyl 40 stearate is myrj-52.

38 . The method of claim 34 , wherein the polyethoxylated castor oil is cremophor RH 40.

39 . The method of claim 34 , wherein the ophthalmic formulation is a topical ophthalmic formulation.

40 . The method of claim 34 , wherein the ophthalmic formulation is packaged in a unit dose form.

41 . The method of claim 34 , wherein the ophthalmic formulation is packaged in a multidose form.

42 . The method of claim 34 , wherein the ophthalmic formulation is in a plastic storage container.

43 . The method of claim 34 , wherein the ophthalmic formulation consists of:

A) 0.0285 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.015 weight/volume % of benzalkonium chloride,

water, and

a pH of 5;

B) 0.057 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.015 weight/volume % of benzalkonium chloride,

water, and

a pH of 5;

C) 0.0285 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.005 weight/volume % of latanoprost,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.015 weight/volume % of benzalkonium chloride,

water, and

a pH of 5;

D) 0.0285 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.005 weight/volume % of latanoprost,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.02 weight/volume % of benzalkonium chloride,

water, and

a pH of 5;

E) 0.0233 weight/volume % of a dihydrochloride salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.015 weight/volume % of benzalkonium chloride, water, and

a pH of 4.8; or

F) 0.0143 weight/volume % of a dimesylate salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.0116 weight/volume % of a dihydrochloride salt of 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate,

0.05 weight/volume % of boric acid,

4.7 weight/volume % of mannitol,

0.008 weight/volume % of benzalkonium chloride,

water, and

a pH of 4.9.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 24, 2024
From: AERIE PHARMACEUTICALS, INC.
To: ALCON INC.
Reel/Frame 067822/0168 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 15, 2022
From: LIN, CHENG-WEN; KOPCZYNSKI, CASEY; DELONG, MITCHELL A.; STURDIVANT, JILL M.; KRISHNAMOORTHY, RAMESH
To: AERIE PHARMACEUTICALS, INC.
Reel/Frame 060216/0156 →