IP Library Granted Patent US 8,802,717
Granted Patent B2
US 8,802,717 · App. 13/682,652 · Granted Aug 12, 2014

Methods of treating arthritic conditions using (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline 1,3-dione

Inventors: George W. Muller (Rancho Santa Fe, CA); Peter H. Schafer (Somerset, NJ); Hon-Wah Man (Princeton, NJ); Chuansheng Ge (Belle Mead, NJ)
Assignee: Celgene Corporation
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Quick Facts
Patent No.
US 8,802,717
App. No.
13/682,652
Granted
Aug 12, 2014
Kind
B2
Abstract

Stereomerically pure (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, substantially free of its (−) isomer, and prodrugs, metabolites, polymorphs, salts, solvates, hydrates, and clathrates thereof are discussed. Also discussed are methods of using and pharmaceutical compositions comprising the (+) enantiomer of 2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-α or the inhibition of PDE4.

Claims (22)

1. A method of treating an arthritic condition, which comprises administering to a patient having an arthritic condition a therapeutically effective amount of a compound which is stereomerically pure (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione.

2. The method of claim 1 , wherein the arthritic condition is rheumatoid spondylitis.

3. The method of claim 1 , wherein the compound is administered orally.

4. The method of claim 3 , wherein about 5 mg to about 500 mg of the compound is administered per day.

5. The method of claim 3 , wherein about 10 mg to about 200 mg of the compound is administered per day.

6. The method of claim 3 , wherein about 10 mg to about 100 mg of the compound is administered per day.

7. The method of claim 3 , wherein the compound is administered twice daily in equally divided doses.

8. The method of claim 3 , wherein the stereomerically pure compound comprises greater than about 90% by weight of (+) isomer based on the total weight percent of the compound.

9. The method of claim 3 , wherein the stereomerically pure compound comprises greater than about 95% by weight of (+) isomer based on the total weight percent of the compound.

10. The method of claim 3 , wherein the stereomerically pure compound comprises greater than about 97% by weight of (+) isomer based on the total weight percent of the compound.

11. The method of claim 3 , wherein the compound is administered in capsule form.

12. The method of claim 1 , wherein the capsule contains about 10 mg of the compound.

13. The method of claim 11 , wherein the capsule contains about 20 mg of the compound.

14. The method of claim 11 , wherein the capsule contains about 25 mg of the compound.

15. The method of claim 11 , wherein the capsule contains about 50 mg of the compound.

16. The method of claim 1 , wherein the compound is administered in tablet form.

17. The method of claim 16 , wherein the tablet contains about 10 mg of the compound.

18. The method of claim 16 , wherein the tablet contains about 20 mg of the compound.

19. The method of claim 16 , wherein the tablet contains about 25 mg of the compound.

20. The method of claim 16 , wherein the tablet contains about 50 mg of the compound.

21. A method of treating an arthritic condition, which comprises orally administering to a patient having an arthritic condition about 10 mg to about 100 mg of a compound which is stereomerically pure (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione comprising greater than about 97% by weight of (+) isomer wherein the compound is administered in the form of a tablet or capsule twice daily in equally divided doses.

22. The method of claim 21 , wherein the arthritic condition is rheumatoid spondylitis.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 4, 2019
From: CELGENE CORPORATION
To: AMGEN INC.
Reel/Frame 051181/0038 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 5, 2013
From: MULLER, GEORGE W.; SCHAFER, PETER H.; MAN, HON-WAH; GE, CHUANSHENG
To: CELGENE CORPORATION
Reel/Frame 029759/0887 →
Continuity (7)
Continuation 12630788 · Dec 3, 2009
Continuation 12098379 · Apr 4, 2008
Division 11170308 · Jun 28, 2005
Division 10392195 · Mar 19, 2003
Provisional Application 60438450 · Jan 7, 2003
Provisional Application 60366515 · Mar 20, 2002
Related Publication 20140024695A1 · Jan 23, 2014