IP Library Granted Patent US 9,993,470
Granted Patent B2
US 9,993,470 · App. 15/627,238 · Granted Jun 12, 2018

Combination therapy

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Quick Facts
Patent No.
US 9,993,470
App. No.
15/627,238
Granted
Jun 12, 2018
Kind
B2
Abstract

Described herein are compounds and compositions for treating glaucoma and/or reducing intraocular pressure. Compositions may comprise an isoquinoline compound and a prostaglandin or a prostaglandin analog. Compounds described herein include those in which an isoquinoline compound is covalently linked to a prostaglandin or a prostaglandin analog, and those in which an isoquinoline compound and a prostaglandin free acid together form a salt.

Claims (24)

1. A composition comprising:

a) a dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate, a dimesylate salt of (R)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethyl benzoate, or a dimesylate salt of (rac)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate; and

b) latanoprost, bimatoprost, travoprost, tafluprost, AR-102, cloprostenol, latanoprostene bunod, unoprostone, PGF 2α , fluprostenol, or a pharmaceutically acceptable salt thereof.

2. The composition of claim 1 , wherein the composition comprises latanoprost or a pharmaceutically acceptable salt thereof.

3. The composition of claim 1 , wherein the composition comprises a dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate.

4. The composition of claim 1 , wherein the composition comprises a dimesylate salt of (R)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate.

5. The composition of claim 1 , wherein the composition comprises a dimesylate salt of (rac)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate.

6. The composition of claim 1 , wherein the composition comprises a dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate, and latanoprost or a pharmaceutically acceptable salt thereof.

7. The composition of claim 1 , wherein the composition further comprises at least one of a buffer, a chelating agent, a tonicity agent, a preservative, a viscosity enhancer, a sugar, a sugar alcohol, or a surfactant.

8. A method of treating an ocular disorder in a subject in need thereof, comprising administering to the subject a composition comprising:

a) a dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethyl benzoate, a dimesylate salt of (R)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethyl benzoate, or a dimesylate salt of (rac)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate; and

b) latanoprost, bimatoprost, travoprost, tafluprost, AR-102, cloprostenol, latanoprostene bunod, unoprostone, PGF 2α , fluprostenol, or a pharmaceutically acceptable salt thereof.

9. The method of claim 8 , wherein the composition comprises latanoprost or a pharmaceutically acceptable salt thereof.

10. The method of claim 8 , wherein the composition comprises a dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate.

11. The method of claim 8 , wherein the composition comprises a dimesylate salt of (R)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate.

12. The method of claim 8 , wherein the composition comprises a dimesylate salt of (rac)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate.

13. The method of claim 8 , wherein the composition comprises a dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate, and latanoprost or a pharmaceutically acceptable salt thereof.

14. The method of claim 8 , wherein the composition further comprises at least one of a buffer, a chelating agent, a tonicity agent, a preservative, a viscosity enhancer, a sugar, a sugar alcohol, or a surfactant.

15. The method of claim 8 , wherein the ocular disorder is glaucoma.

16. The method of claim 10 , wherein the ocular disorder is glaucoma.

17. The method of claim 13 , wherein the ocular disorder is glaucoma.

18. The method of claim 8 , wherein the composition is administered topically to an eye of the subject.

19. The method of claim 16 , wherein the composition is administered topically to an eye of the subject.

20. The method of claim 17 , wherein the composition is administered topically to an eye of the subject.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 24, 2024
From: AERIE PHARMACEUTICALS, INC.
To: ALCON INC.
Reel/Frame 067822/0168 →
RELEASE OF SECURITY INTEREST Recorded Sep 5, 2019
From: DEERFIELD PRIVATE DESIGN FUND III, L.P.
To: AERIE PHARMACEUTICALS, INC.
Reel/Frame 050276/0807 →
SECURITY INTEREST Recorded Jul 23, 2018
From: AERIE PHARMACEUTICALS, INC.
To: DEERFIELD PRIVATE DESIGN FUND III, L.P.
Reel/Frame 046432/0307 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 19, 2017
From: KOPCZYNSKI, CASEY; LIN, CHENG-WEN; STURDIVANT, JILL MARIE; DELONG, MITCHELL A.
To: AERIE PHARMACEUTICALS, INC.
Reel/Frame 042751/0849 →