IP Library › Granted Patent US 8,969,581
Granted Patent B2
US 8,969,581 · App. 14/211,905 · Granted Mar 3, 2015

5-deutero-2,4-thiazolidinedione derivatives and compositions comprising and methods of using the same

Inventor: Sheila DeWitt (Auburn, NH)
Assignee: DeuteRx, LLC
C07D417/12C07D277/34
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Quick Facts
Patent No.
US 8,969,581
App. No.
14/211,905
Granted
Mar 3, 2015
Kind
B2
Abstract

The invention provides 5-deuterium-enriched 2,4-thiazolidinediones (e.g., 5-[4-[2-(5-ethyl-2-pyridyl)-2-oxoethoxy]benzyl]-5-deutero-thiazolidine-2,4-dione), deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treatment using the same.

Claims (38)

1. A deuterium-enriched compound represented by:

or a stereoisomer or pharmaceutically acceptable salt form thereof; wherein Z is H or D, provided that the abundance of deuterium in Z is at least 30%.

2. The deuterium-enriched compound of claim 1 , wherein the compound is

or a stereoisomer or pharmaceutically acceptable salt form thereof, wherein Z is H or D, provided that the abundance of deuterium in Z is at least 50%.

3. The deuterium-enriched compound of claim 1 , wherein the compound is

or a stereoisomer thereof, wherein Z is H or D, provided that the abundance of deuterium in Z is at least 50%.

4. The deuterium-enriched compound of claim 2 , wherein the abundance of deuterium in Z is at least 80%.

5. The deuterium-enriched compound of claim 2 , wherein the abundance of deuterium in Z is at least 90%.

6. The deuterium-enriched compound of claim 2 , wherein the abundance of deuterium in Z is at least 95%.

7. The deuterium-enriched compound of claim 1 , wherein the compound is

or a pharmaceutically acceptable salt form thereof, wherein the compound has an enantiomeric excess, with respect to the C—Z carbon, of at least 80%, and Z is H or D, provided that the abundance of deuterium in Z is at least 50%.

8. The deuterium-enriched compound of claim 1 , wherein the compound is

wherein the compound has an enantiomeric excess, with respect to the C—Z carbon, of at least 80%, and Z is H or D, provided that the abundance of deuterium in Z is at least 50%.

9. The deuterium-enriched compound of claim 7 , wherein the abundance of deuterium in Z is at least 80%.

10. The deuterium-enriched compound of claim 7 , wherein the abundance of deuterium in Z is at least 90%.

11. The deuterium-enriched compound of claim 7 , wherein the abundance of deuterium in Z is at least 95%.

12. The deuterium-enriched compound of claim 10 , wherein the compound has an enantiomeric excess, with respect to the C—Z carbon, of at least 90%.

13. The deuterium-enriched compound of claim 11 , wherein the compound has an enantiomeric excess, with respect to the C—Z carbon, of at least 95%.

14. The deuterium-enriched compound of claim 1 , wherein the compound is

or a pharmaceutically acceptable salt form thereof, wherein the compound has an enantiomeric excess, with respect to the C—Z carbon, of at least 80%, and Z is H or D, provided that the abundance of deuterium in Z is at least 50%.

15. The deuterium-enriched compound of claim 1 , wherein the compound is

wherein the compound has an enantiomeric excess, with respect to the C—Z carbon, of at least 80%, and Z is H or D, provided that the abundance of deuterium in Z is at least 50%.

16. The deuterium-enriched compound of claim 14 , wherein the abundance of deuterium in Z is at least 80%.

17. The deuterium-enriched compound of claim 14 , wherein the abundance of deuterium in Z is at least 90%.

18. The deuterium-enriched compound of claim 14 , wherein the abundance of deuterium in Z is at least 95%.

19. The deuterium-enriched compound of claim 17 , wherein the compound has an enantiomeric excess, with respect to the C—Z carbon, of at least 90%.

20. The deuterium-enriched compound of claim 18 , wherein the compound has an enantiomeric excess, with respect to the C—Z carbon, of at least 95%.

21. The deuterium-enriched compound of claim 1 wherein the abundance of deuterium in Z is at least 80%.

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

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

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

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

26. A method of treating a metabolic inflammation mediated disease selected from the group consisting of Type I diabetes, Type II diabetes, insulin resistance, and inadequate glucose tolerance, comprising administering to a patient in need thereof a therapeutically effective amount a compound of claim 1 to treat the disease.

27. The method of claim 26 , wherein the disease is Type II diabetes.

28. The method of claim 26 , wherein the compound is a compound of claim 2 .

29. The method of claim 27 , wherein the compound is a compound of claim 2 .

30. The method of claim 26 , wherein the compound is a compound of claim 7 .

31. The method of claim 26 , wherein the compound is a compound of claim 14 .

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 27, 2019
From: DEUTERX, LLC
To: POXEL SA
Reel/Frame 048453/0967 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 28, 2018
From: JACQUES, VINCENT; VAN DER PLOEG, LEONARDUS
To: DEUTERX, LLC
Reel/Frame 046727/0500 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 19, 2014
From: DEWITT, SHEILA
To: DEUTERX, LLC
Reel/Frame 033141/0122 →
Continuity (2)
Provisional Application 61786118 · Mar 14, 2013
Related Publication 20140275180A1 · Sep 18, 2014