IP Library Granted Patent US 11,427,563
Granted Patent B2
US 11,427,563 · App. 16/570,849 · Granted Aug 30, 2022

Aryl cyclopropyl-amino-isoquinolinyl amide compounds

Inventors: Mitchell A. deLong (Chapel Hill, NC); Jill M. Sturdivant (Chapel Hill, NC); Cynthia L. Lichorowic (Raleigh, NC); Andriy Kornilov (Ypsilanti, MI)
Assignee: Aerie Pharmaceuticals, Inc.
C07D401/14A61P27/06C07D401/12C07D405/12C07D413/12C07D417/12C07D417/14
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Quick Facts
Patent No.
US 11,427,563
App. No.
16/570,849
Granted
Aug 30, 2022
Kind
B2
Abstract

Provided herein are amino isoquinolinyl amide and sulfonamide compounds that affect the function of kinases and other proteins in a cell and that are useful as therapeutic agents. In particular, these compounds are useful in the treatment of eye diseases such as glaucoma and retinal diseases, as anti-inflammatory agents, for the treatment of cardiovascular diseases, and for diseases characterized by abnormal growth, such as cancers.

Claims (50)

1. A compound of Formula (I):

or a pharmaceutically acceptable salt thereof,

wherein

R 1 is H, halo, —CN, —C 1-6 alkyl, —C 1-6 alkoxyl, —C 1-6 haloalkyl; —C 1-6 haloalkoxyl;

R 2 is H or halo;

X is —(C 1-5 heteroaryl)-R 3 ; and

R 3 is —C 2-6 heterocyclyl, or —C 1-6 heteroalkyl.

2. The compound of claim 1 , wherein the compound of Formula (I) is a compound of Formula (II):

or a pharmaceutically acceptable salt thereof.

3. The compound of claim 1 , wherein the compound of Formula (I) is a compound of Formula (III):

or a pharmaceutically acceptable salt thereof.

4. The compound of claim 1 , wherein R 1 is H, halo, —CN, —C 1-3 alkyl, —C 1-3 alkoxyl, —C 1-3 haloalkyl, —C 1-3 haloalkoxyl.

5. The compound of claim 1 , wherein R 1 is H, Cl, —CN, —CH 3 , —CH 2 CH 3 , —CH(CH 3 ) 2 , —CHF 2 , —CF 3 , or —OCF 3 .

6. The compound of claim 1 , wherein R 1 is Cl, —CN, —CH 3 , —CH 2 CH 3 , —CH(CH 3 ) 2 , —CHF 2 , —CF 3 , or —OCF 3 .

7. The compound of claim 1 , wherein R 2 is F, Cl, Br, or I.

8. The compound of claim 1 , wherein R 2 is H or F.

9. The compound of claim 1 , wherein X is —(C 3-5 heteroaryl)-R 3 .

10. The compound of claim 1 , wherein X is

11. The compound of claim 1 , wherein R 3 is —C 2-6 heterocyclyl.

12. The compound of claim 1 , wherein R 3 is —C 3-5 heterocycloalkyl.

13. The compound of claim 1 , wherein R 3 is

14. The compound of claim 1 , wherein

R 1 is H, Cl, —CN, —CH 3 , —CH 2 CH 3 , —CH(CH 3 ) 2 , —CF 3 , or —OCF 3 ;

R 2 is H or F;

X is

and R 3 is

15. The compound of claim 1 , wherein

R 1 is Cl, —CN, —CH 3 , —CH 2 CH 3 , —CH(CH 3 ) 2 , —CF 3 , or —OCF 3 ;

R 2 is H or F;

X is

and

R 3 is

16. The compound of claim 1 , selected from:

or a pharmaceutically acceptable salt thereof.

17. A pharmaceutical composition, comprising the compound of claim 1 and a pharmaceutically acceptable carrier.

18. A pharmaceutical composition, comprising the compound of claim 2 and a pharmaceutically acceptable carrier.

19. A pharmaceutical composition, comprising the compound of claim 3 and a pharmaceutically acceptable carrier.

20. A pharmaceutical composition, comprising the compound of claim 4 and a pharmaceutically acceptable carrier.

21. A pharmaceutical composition, comprising the compound of claim 5 and a pharmaceutically acceptable carrier.

22. A pharmaceutical composition, comprising the compound of claim 6 and a pharmaceutically acceptable carrier.

23. A pharmaceutical composition, comprising the compound of claim 7 and a pharmaceutically acceptable carrier.

24. A pharmaceutical composition, comprising the compound of claim 8 and a pharmaceutically acceptable carrier.

25. A pharmaceutical composition, comprising the compound of claim 9 and a pharmaceutically acceptable carrier.

26. A pharmaceutical composition, comprising the compound of claim 10 and a pharmaceutically acceptable carrier.

27. A pharmaceutical composition, comprising the compound of claim 11 and a pharmaceutically acceptable carrier.

28. A pharmaceutical composition, comprising the compound of claim 12 and a pharmaceutically acceptable carrier.

29. A pharmaceutical composition, comprising the compound of claim 13 and a pharmaceutically acceptable carrier.

30. A pharmaceutical composition, comprising the compound of claim 14 and a pharmaceutically acceptable carrier.

31. A pharmaceutical composition, comprising the compound of claim 15 and a pharmaceutically acceptable carrier.

32. A pharmaceutical composition, comprising the compound of claim 16 and a pharmaceutically acceptable carrier.

Assignments (3)
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 Sep 13, 2019
From: DELONG, MITCHELL A.; STURDIVANT, JILL M.; LICHOROWIC, CYNTHIA L.; KORNILOV, ANDRIY
To: AERIE PHARMACEUTICALS, INC.
Reel/Frame 050374/0332 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 13, 2019
From: DELONG, MITCHELL A.; STURDIVANT, JILL M.; LICHOROWIC, CYNTHIA L.; KORNILOV, ANDRIY
To: AERIE PHARMACEUTICALS, INC.
Reel/Frame 050374/0559 →