IP Library Granted Patent US 9,492,457
Granted Patent B2
US 9,492,457 · App. 14/626,978 · Granted Nov 15, 2016

Substituted xanthine derivatives

Inventors: Roger D. Tung (Lexington, MA); Julie F. Liu (Lexington, MA); Scott L. Harbeson (Cambridge, MA)
Assignee: Concert Pharmaceuticals, Inc.
A61K31/522C07D473/06
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Quick Facts
Patent No.
US 9,492,457
App. No.
14/626,978
Granted
Nov 15, 2016
Kind
B2
Abstract

This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. For example, this invention relates to novel substituted xanthine derivatives that are derivatives of pentoxifylline. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions for which pentoxifylline and related compounds are beneficial.

Claims (26)

1. A method of treating a disease or condition in a patient in need thereof, comprising administering to the patient an effective amount of a compound represented by the following structural formula:

or a pharmaceutically acceptable salt thereof, wherein R 1 is selected from —CH 3 and —CD 3 ; R 2 is selected from —CH 3 and —CD 3 ; Y 1 is deuterium or hydrogen, wherein the isotopic enrichment factor for each designated deuterium atom is at least 5000, wherein the disease is selected from diabetic nephropathy, hypertensive nephropathy and intermittent claudication on the basis of chronic occlusive arterial disease of the limbs; wherein the compound is administered orally; wherein the compound is administered in an amount of 100-800 mg per treatment; and wherein the treatment is administered two times daily.

2. The method of claim 1 , wherein the disease or condition is diabetic nephropathy.

3. The method of claim 2 , wherein R 1 is —CH 3 .

4. The method of claim 2 , wherein R 1 is —CD 3 .

5. The method of claim 2 wherein R 2 is —CH 3 .

6. The method of claim 2 wherein R 2 is —CD 3 .

7. The method of claim 2 , wherein R 1 is —CH 3 and R 2 is —CH 3 .

8. The method of claim 2 , wherein Y 1 is deuterium.

9. The method of claim 2 , wherein Y 1 is hydrogen.

10. The method of claim 2 , wherein the compound is selected from the group consisting of the following compounds:

or a pharmaceutically acceptable salt thereof.

11. A method of treating a disease or condition in a patient in need thereof, comprising administering to the patient an effective amount of a compound represented by the following structural formula:

or a pharmaceutically acceptable salt thereof, wherein R 1 is selected from —CH 3 and —CD 3 ;

R 2 is selected from —CH 3 and —CD 3 ; Y 1 is deuterium or hydrogen;

with the proviso that

(i) if Y 1 is deuterium, then R 2 is CD 3 ; and

(ii) if Y 1 is hydrogen, then R 1 is CH 3 ,

wherein the isotopic enrichment factor for each designated deuterium atom is at least 5000, wherein the disease is selected from diabetic nephropathy, hypertensive nephropathy and intermittent claudication on the basis of chronic occlusive arterial disease of the limbs; wherein the compound is administered orally; wherein the compound is administered in an amount of 100-800 mg per treatment; and wherein the treatment is administered two times daily.

12. The method of claim 11 , wherein the disease or condition is diabetic nephropathy.

13. The method of claim 12 , wherein R 1 is —CH 3 .

14. The method of claim 12 , wherein R 1 is —CD 3 .

15. The method of claim 12 , wherein R 2 is —CH 3 .

16. The method of claim 12 , wherein R 2 is —CD 3 .

17. The method of claim 12 , wherein R 1 is —CH 3 and R 2 is —CH 3 .

18. The method of claim 12 , wherein Y 1 is deuterium.

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 Mar 30, 2015
From: TUNG, ROGER D.; LIU, JULIE F.; HARBESON, SCOTT L.
To: CONCERT PHARMACEUTICALS, INC.
Reel/Frame 035290/0023 →
Continuity (6)
Continuation 13448930 · Apr 17, 2012
Division 12874783 · Sep 2, 2010
Continuation In Part 12873991 · Sep 1, 2010
Continuation In Part 12380579 · Feb 27, 2009
Provisional Application 61239342 · Sep 2, 2009
Related Publication 20150272956A1 · Oct 1, 2015