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Last Updated: December 6, 2019

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Claims for Patent: 9,993,470

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Summary for Patent: 9,993,470
Title:Combination therapy
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.
Inventor(s): Kopczynski; Casey (Chapel Hill, NC), Lin; Cheng-Wen (Raleigh, NC), Sturdivant; Jill Marie (Chapel Hill, NC), deLong; Mitchell A. (Chapel Hill, NC)
Assignee: Aerie Pharmaceuticals, Inc. (Durham, NC)
Application Number:15/627,238
Patent Claims: 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.sub.2.alpha., 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.sub.2.alpha., 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)benzy- l 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.

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