IP Library Granted Patent US 9,849,122
Granted Patent B2
US 9,849,122 · App. 15/142,461 · Granted Dec 26, 2017

Combination therapy

Inventors: Casey Kopczynski (Chapel Hill, NC); Cheng-Wen Lin (Raleigh, NC); Jill Marie Sturdivant (Chapel Hill, NC); Mitchell A. deLong (Chapel Hill, NC)
Assignee: Aerie Pharmaceuticals, Inc.
A61K31/472A61K9/0048A61K9/08A61K31/4725A61K31/557A61K31/559A61K31/5575A61K47/481C07D217/22C07D409/12
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 9,849,122
App. No.
15/142,461
Granted
Dec 26, 2017
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 (38)

1. A compound according to formula (II):

or a pharmaceutically acceptable salt thereof, wherein:

Y is phenylene;

B is —NR 1 R 2 or —CH 2 NR 1 R 2 ;

R 1 and R 2 are each independently hydrogen or C 1 -C 4 alkyl;

X 1 and X 2 are hydrogen; and

PG is an acyl radical of latanoprost, bimatoprost, travoprost, tafluprost, AR-102, cloprostenol, unoprostone, or PGF 2α .

2. The compound of claim 1 , wherein:

B is —CH 2 NR 1 R 2 ; and

R 1 and R 2 are hydrogen.

3. The compound of claim 1 , wherein

PG is an acyl radical of latanoprost.

4. The compound of claim 1 , wherein PG is an acyl radical of AR-102.

5. The compound of claim 1 , wherein PG is an acyl radical of bimatoprost.

6. A composition comprising a compound of claim 1 , and at least one of a buffer, a chelating agent, a tonicity agent, a preservative, a viscosity enhancer, a sugar or a sugar alcohol, or a surfactant.

7. The compound of claim 1 , wherein PG is an acyl radical of travoprost.

8. A method of treating glaucoma in a subject in need thereof, comprising administering to the subject a compound of claim 1 .

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

10. A method of reducing intraocular pressure in a subject in need thereof, comprising topically administering to an eye of the subject a compound of claim 1 .

11. A compound, wherein the compound is:

or a pharmaceutically acceptable salt thereof.

12. A composition comprising a compound of claim 11 , further comprising at least one of a buffer, a chelating agent, a tonicity agent, a preservative, a viscosity enhancer, a sugar or a sugar alcohol, or a surfactant.

13. A method of treating glaucoma in a subject in need thereof, comprising administering to the subject a compound of claim 11 .

14. The method of claim 13 , wherein the compound is administered topically to an eye of the subject.

15. A method of reducing intraocular pressure in a subject in need thereof, comprising topically administering to an eye of the subject a compound of claim 11 .

16. A compound according to formula (II):

or a pharmaceutically acceptable salt thereof;

wherein

Y is phenylene;

B is —CH 2 NR 1 R 2 ;

R 1 and R 2 are hydrogen;

X 1 and X 2 are hydrogen; and

PG is an acyl radical of latanoprost.

17. A composition comprising a compound of claim 16 , further comprising at least one of a buffer, a chelating agent, a tonicity agent, a preservative, a viscosity enhancer, a sugar or a sugar alcohol, or a surfactant.

18. A method of treating glaucoma in a subject in need thereof, comprising administering to the subject a compound of claim 16 .

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

20. A method of reducing intraocular pressure in a subject in need thereof, comprising topically administering to an eye of the subject a compound of claim 16 .

21. The compound of claim 2 , wherein PG is an acyl radical of bimatoprost.

Assignments (5)
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 →
RELEASE OF SECURITY INTEREST Recorded Jul 23, 2018
From: DEERFIELD PARTNERS, L.P.; DEERFIELD PRIVATE DESIGN FUND III, L.P.; DEERFIELD SPECIAL SITUATIONS FUND, L.P.; DEERFIELD MANAGEMENT COMPANY, L.P.
To: AERIE DISTRIBUTION, INC.
Reel/Frame 046431/0500 →
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 7, 2016
From: KOPCZYNSKI, CASEY; LIN, CHENG-WEN; STURDIVANT, JILL MARIE; DELONG, MITCHELL A.
To: AERIE PHARMACEUTICALS, INC.
Reel/Frame 038830/0138 →
Continuity (3)
Continuation 14213940 · Mar 14, 2014
Provisional Application 61787883 · Mar 15, 2013
Related Publication 20160243105A1 · Aug 25, 2016