IP Library Granted Patent US 8,501,994
Granted Patent B2
US 8,501,994 · App. 12/196,520 · Granted Aug 6, 2013

Acetamide stereoisomer

Inventors: Craig R. Abolin (Boylston, MA); H. Scott Wilkinson (Westborough, MA); Paul McGlynn (Northborough, MA); William K. McVicar (Sudbury, MA)
Assignee: Sunovion Pharmaceuticals Inc.
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Quick Facts
Patent No.
US 8,501,994
App. No.
12/196,520
Granted
Aug 6, 2013
Kind
B2
Abstract

The compound of formula (I) is a water-stable, long acting β 2 -selective adrenoceptor agonist useful as a bronchodilator in the treatment of bronchoconstriction associated with reversible obstructive airways diseases and the like.

Claims (17)

1. A compound of formula (I)

or a pharmaceutically acceptable salt thereof.

2. A mixture of isomers of N-[2-hydroxy-5-[1-hydroxy-2-[[(2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-phenyl]acetamide, wherein the mixture comprises at least 90% by weight of the isomer

3. A compound of general formula (IV)

or a salt thereof, in which P 1 and P 2 each represents a hydrogen atom or a hydroxyl protecting group, and P 3 represents a hydrogen atom or a benzylic amine protecting group, provided that at least one of P 2 and P 3 represents a protecting group.

4. A pharmaceutical composition, which comprises a compound as claimed in claim 1 or claim 2 and a pharmaceutically acceptable carrier.

5. A pharmaceutical composition as claimed in claim 4 , which further comprises a steroid.

6. A pharmaceutical composition as claimed in claim 5 , in which the steroid is beclomethasone, triamcinolone, funisolide, mometasone, budesonide or fluticasone.

7. A pharmaceutical composition as claimed in any one of claims 4 to 6 , which further comprises a muscarinic receptor antagonist.

8. A pharmaceutical composition as claimed in claim 7 , in which the muscarinic receptor antagonist is ipratropium or tiatropium.

9. A pharmaceutical composition as claimed in any one of claims 4 to 8 which further comprises an anticholinergic.

10. A pharmaceutical composition as claimed in claim 9 , in which the anticholinergic is glycopyrralate.

11. A pharmaceutical composition as claimed in any one of claims 4 to 10 which further comprises a mucolytic.

12. A pharmaceutical composition as claimed in claim 11 , in which the mucolytic is cromoglycate, acetylcysteine, arginine, or 2-mercaptoethanesulphonate.

13. A pharmaceutical composition as claimed in any one of claims 4 to 12 which further comprises an anti-inflammatory agent.

14. A pharmaceutical composition as claimed in claim 13 , in which the anti-inflammatory agent is an inhibitor of tumor necrosis factor alpha (TNFα) or dipeptidyl peptidase IV, and/or antibodies to pro-inflammatory interleukins such as IL4 and IL13.

15. A method for treating bronchoconstriction associated with a reversible obstructive airways disease, which comprises administering to a patient in need of treatment, an effective amount of a compound as claimed in claim 1 .

Assignments (2)
CHANGE OF NAME Recorded Feb 24, 2011
From: SEPRACOR INC.
To: SUNOVION PHARMACEUTICALS INC.
Reel/Frame 025860/0392 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 5, 2008
From: ABOLIN, CRAIG R.; WILKINSON, H. SCOTT; MCGLYNN, PAUL; MCVICAR, WILLIAM K.
To: SEPRACOR INC.
Reel/Frame 021790/0180 →
Continuity (2)
Provisional Application 60966438 · Aug 28, 2007
Related Publication 20090060922A1 · Mar 5, 2009