IP Library Granted Patent US 8,124,646
Granted Patent B2
US 8,124,646 · App. 12/816,295 · Granted Feb 28, 2012

Substituted isoindoline-1,3-dione derivatives

Assignee: Concert Pharmaceuticals, Inc.
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Quick Facts
Patent No.
US 8,124,646
App. No.
12/816,295
Granted
Feb 28, 2012
Kind
B2
Abstract

This invention relates to novel substituted isoindoline-1,3-dione derivatives and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel substituted isoindoline-1,3-dione derivatives that are analogues of apremilast. This invention also provides compositions comprising a compound of this invention and a carrier and the use of disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering apremilast.

Claims (39)

1. A compound of Formula I:

or a pharmaceutically acceptable salt thereof, wherein:

R 1 is selected from CH 3 , CH 2 D, CHD 2 , and CD 3 ;

R 2 is methyl or CD 3 ;

R 3 is CD 3 ;

R 4 is an ethyl group substituted with zero to five deuterium, or is a cyclopentyl group substituted with zero to nine deuterium;

X is C═O;

each of Y 1a , Y 1b , Y 2 , Y 3 , Y 4 , Y 5 , Y 7 and Y 8 is independently selected from H and D; and

Y 6 is selected from Cl, H, and D.

2. The compound of claim 1 , wherein Y 6 , Y 7 and Y 8 are the same; Y 1a and Y 1b are the same; and Y 3 , Y 4 and Y 5 are the same.

3. The compound of claim 1 , wherein the compound of Formula I is a compound of Formula II:

or a pharmaceutically acceptable salt thereof, wherein:

R 1 is selected from CH 3 and CD 3 ;

R 3 is CD 3 ;

R 4 is selected from CH 2 CH 3 , CD 2 CD 3 , CD 2 CH 3 , and CH 2 CD 3 ; and

each Y is independently selected from H and D.

4. The compound of claim 2 , wherein the compound of Formula I is a compound of Formula Ia, having predominantly the (S) configuration at the carbon attached to Y 2 :

or a pharmaceutically acceptable salt thereof.

5. The compound of claim 2 , wherein the compound of Formula I is a compound of Formula Ia, having predominantly the (R) configuration at the carbon attached to Y 2 :

or a pharmaceutically acceptable salt thereof.

6. The compound of claim 1 , wherein Y 6 , Y 7 and Y 8 are the same.

7. The compound of claim 1 , wherein Y 1a and Y 1b are the same.

8. The compound of claim 1 , wherein Y 3 , Y 4 and Y 5 are the same.

9. The compound of claim 1 , wherein R 1 is CH 3 or CD 3 .

10. The compound of claim 1 , wherein R 4 is CD 2 CD 3 .

11. A compound selected from the group consisting of :

or a pharmaceutically acceptable salt of any of the foregoing.

12. A compound of claim 11 , having predominantly the (S) configuration.

13. A compound of claim 11 , having predominantly the (R) configuration.

14. A compound selected from the group consisting of

or a pharmaceutically acceptable salt of any of the foregoing.

15. A compound of claim 1 , wherein any atom not designated as deuterium is present at its natural isotopic abundance.

16. A composition comprising an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt of said compound; and an acceptable carrier.

17. A method of treating a disease selected from the group consisting of psoriasis and psoriatic arthritis in a patient in need thereof comprising administering to the patient an effective amount of a compound of claim 1 or a pharmaceutically acceptable salt thereof.

18. The method of claim 17 , wherein psoriasis is plaque-type psoriasis or refractory psoriasis.

19. The compound of claim 1 , wherein the compound of Formula I is a compound of Formula Ia, having predominantly the (S) configuration at the carbon attached to Y 2 :

or a pharmaceutically acceptable salt thereof.

20. The compound of claim 1 , wherein the compound of Formula I is a compound of Formula Ib, having predominantly the (R) configuration at the carbon attached to Y 2 :

or a pharmaceutically acceptable salt thereof.

Assignments (2)
MERGER Recorded Aug 2, 2023
From: CONCERT PHARMACEUTICALS, INC.
To: SUN PHARMACEUTICAL INDUSTRIES, INC.
Reel/Frame 064465/0383 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 27, 2010
From: LIU, JULIE F.
To: CONCERT PHARMACEUTICALS, INC.
Reel/Frame 024897/0949 →
Continuity (2)
Provisional Application 61268953 · Jun 18, 2009
Related Publication 20100324108A1 · Dec 23, 2010