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Last Updated: May 7, 2024

Claims for Patent: 11,197,853


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Summary for Patent: 11,197,853
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. (Bedminster, NJ)
Application Number:17/238,554
Patent Claims: 1. A pharmaceutical composition comprising about 0.01% (w/v) to about 1.0% (w/v) of a dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate, about 0.005% (w/v) latanoprost, and at least one excipient.

2. The pharmaceutical composition of claim 1, wherein the at least one excipient is a tonicity agent.

3. The pharmaceutical composition of claim 2, wherein the tonicity agent is mannitol.

4. The pharmaceutical composition of claim 3, wherein the mannitol is D-mannitol.

5. The pharmaceutical composition of claim 4, wherein the D-mannitol is about 4.7% (w/v) of the pharmaceutical composition.

6. The pharmaceutical composition of claim 2, further comprising a buffer.

7. The pharmaceutical composition of claim 6, wherein the buffer is boric acid and the pH of the pharmaceutical composition is about 5.0.

8. The pharmaceutical composition of claim 7, wherein the boric acid is about 0.05% (w/v) of the pharmaceutical composition.

9. The pharmaceutical composition of claim 5, further comprising a buffer.

10. The pharmaceutical composition of claim 9, wherein the buffer is boric acid and the pH of the pharmaceutical composition is about 5.0.

11. The pharmaceutical composition of claim 10, wherein the boric acid is about 0.05% (w/v) of the pharmaceutical composition.

12. The pharmaceutical composition of claim 6, further comprising a preservative.

13. The pharmaceutical composition of claim 12, wherein the preservative is benzalkonium chloride.

14. The pharmaceutical composition of claim 13, wherein the benzalkonium chloride is about 0.02% (w/v) of the pharmaceutical composition.

15. The pharmaceutical composition of claim 11, further comprising a preservative.

16. The pharmaceutical composition of claim 15, wherein the preservative is benzalkonium chloride.

17. The pharmaceutical composition of claim 16, wherein the benzalkonium chloride is about 0.02% (w/v) of the pharmaceutical composition.

18. The pharmaceutical composition of claim 1, comprising at least about 0.020% (w/v) to less than about 0.05% (w/v) of the dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate.

19. A pharmaceutical composition comprising: (a) about 0.01% (w/v) to about 1.0% (w/v) of a dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate; (b) about 0.005% (w/v) latanoprost; (c) boric acid; (d) mannitol; and (e) benzalkonium chloride.

20. The pharmaceutical composition of claim 19, comprising at least about 0.020% (w/v) to less than about 0.05% (w/v) of the dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate.

21. A pharmaceutical composition comprising: (a) about 0.01% (w/v) to about 1.0% (w/v) of a dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate; (b) about 0.005% (w/v) latanoprost (c) about 0.05% (w/v) boric acid; (d) about 4.7% (w/v) D-mannitol; and (e) about 0.02% (w/v) benzalkonium chloride, wherein the pharmaceutical composition has a pH of about 5.0.

22. The pharmaceutical composition of claim 21, comprising at least about 0.020% (w/v) to less than about 0.05% (w/v) of the dimesylate salt of (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate.

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