IP Library Granted Patent US 11,691,950
Granted Patent B2
US 11,691,950 · App. 17/339,828 · Granted Jul 4, 2023

Isoquinoline-steroid conjugates and uses thereof

Inventors: Mitchell A. deLong (Chapel Hill, NC); Eric Carlson (Irvine, CA); Casey Kopczynski (Chapel Hill, NC); Jill M. Sturdivant (Chapel Hill, NC); Cynthia Lichorowic (Raleigh, NC)
Assignee: Aerie Pharmaceuticals, Inc.
C07D217/22A61K47/28A61K9/0048
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Quick Facts
Patent No.
US 11,691,950
App. No.
17/339,828
Granted
Jul 4, 2023
Kind
B2
Abstract

Provided herein are compounds and pharmaceutical compositions useful in modulating kinase activity, and related diseases. Also provided herein are methods of treating an eye disease or disorder in a subject. Also provided herein are methods of reducing intraocular pressure in a subject. Also provided herein are methods of modulating kinase activity in a cell. Also provided herein are methods of making the compounds provided herein, and compounds useful for the preparation of the compounds provided herein.

Claims (48)

1. A method of treating an eye disease or disorder in a subject in need thereof, comprising administering to the subject an effective amount of a compound having the formula:

or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 , wherein the eye disease or disorder comprises glaucoma, a neurodegenerative eye disease or disorder, dry eye, ocular hypertension, an ocular inflammatory disease or disorder, or a combination thereof.

3. The method of claim 2 , wherein the ocular inflammatory disease or disorder comprises uveitis, a corneal ulcer, endophthalmitis, an autoimmune disease of the cornea or ocular surface, an ophthalmic manifestation of HIV disease, or a combination thereof.

4. The method of claim 1 , wherein the administration is topical administration to the eye.

5. A method of treating an eye disease or disorder in a subject in need thereof, comprising administering to the subject an effective amount of a compound having the formula:

R 8 —R 10 —R 11

or a pharmaceutically acceptable salt thereof;

wherein

R 8 is

R 10 is

 and

R 11 is

6. The method of claim 5 , wherein

R 10 is

 and

R 11 is

7. The method of claim 5 , wherein

R 10 is

 and

R 11 is

8. The method of claim 5 , wherein

R 11 is

9. The method of claim 5 , wherein

R 10 is

 and

R 11 is

10. The method of claim 5 , wherein

R 10 is

 and

R 11 is

11. The method of claim 5 , wherein

R 11 is

12. The method of claim 5 , wherein

R 10 is

 and

R 11 is

13. The method of claim 5 , wherein

R 10 is

 and

R 11 is

14. The method of claim 5 , wherein the compound is selected from:

or a pharmaceutically acceptable salt thereof.

15. The method of claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

16. The method of claim 5 , wherein the eye disease or disorder comprises glaucoma, a neurodegenerative eye disease or disorder, dry eye, ocular hypertension, an ocular inflammatory disease or disorder, or a combination thereof.

17. The method of claim 16 , wherein the ocular inflammatory disease or disorder comprises uveitis, a corneal ulcer, endophthalmitis, an autoimmune disease of the cornea or ocular surface, an ophthalmic manifestation of HIV disease, or a combination thereof.

18. The method of claim 5 , wherein the administration is topical administration to the eye.

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 4, 2021
From: DELONG, MITCHELL A.; CARLSON, ERIC; KOPCZYNSKI, CASEY; STURDIVANT, JILL M.; LICHOROWIC, CYNTHIA
To: AERIE PHARMACEUTICALS, INC.
Reel/Frame 056446/0600 →