IP Library Granted Patent US 8,173,829
Granted Patent B2
US 8,173,829 · App. 12/751,563 · Granted May 8, 2012

Carbamate stereoisomer

Assignee: Sunovion Pharmaceuticals Inc.
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Quick Facts
Patent No.
US 8,173,829
App. No.
12/751,563
Granted
May 8, 2012
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 (19)

1. A pharmaceutical composition comprising a compound of formula (I)

or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, wherein said pharmaceutical composition is an aqueous solution or suspension and wherein said compound of formula (I) constitutes at least 90% by weight of all carbamic acid, [2-hydroxy-5-[1-hydroxy-2-[[(2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]phenyl]-, methyl ester present.

2. A pharmaceutical composition according to claim 1 wherein the aqueous solution or suspension is administered using a nebuliser.

3. A pharmaceutical composition comprising a compound of formula (I)

or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, wherein said pharmaceutical composition is an aerosol formulation and wherein said compound of formula (I) constitutes at least 90% by weight of all carbamic acid, [2-hydroxy-5-[1-hydroxy-2-[[(2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]phenyl]-, methyl ester present.

4. A pharmaceutical composition according to claim 3 wherein the compound of formula (I) is in solution.

5. A pharmaceutical composition according to claim 4 further comprising at least one co-solvent or solubilizing agent.

6. A pharmaceutical composition according to claim 5 wherein said co-solvent or solubilizing agent is selected from glycerol and ethanol.

7. A pharmaceutical composition according to claim 3 further comprising at least one propellant.

8. A pharmaceutical composition according to claim 3 further comprising at least one surfactant suitable for use in aerosol formulations.

9. A pharmaceutical composition according to claim 8 wherein the surfactant is present in an amount between 1:100 to 1:10 surfactant:compound of formula I.

10. A pharmaceutical composition according to claim 8 wherein the surfactant is oleic acid.

11. A pharmaceutical composition of claim 3 further comprising a propellant, a surfactant and an optional co-solvent or solubilizing agent.

12. A pharmaceutical composition comprising a compound of formula (I)

or a pharmaceutically acceptable salt thereof, wherein said pharmaceutical composition is in the form of a dry powder and wherein said compound of formula (I) constitutes at least 90% by weight of all carbamic acid, [2-hydroxy-5-[1-hydroxy-2-[[(2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]phenyl]-, methyl ester present.

13. A pharmaceutical composition according to claim 12 comprising crystals of formula I.

14. A pharmaceutical composition according to claim 13 wherein the crystals have a mass median aerodynamic diameter of from 1 to 10 microns.

15. A pharmaceutical composition according to claim 13 further comprising a pharmaceutically acceptable carrier.

16. A pharmaceutical composition according to claim 15 wherein the pharmaceutically acceptable carrier is selected from a monosaccharide, disaccharide, trisaccharide, oligosaccharide, polysaccharide, polyol, amino acid and protein, optionally in the form of an pharmaceutically acceptable ester, acetal, hydrate or salt.

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 Aug 5, 2010
From: ABOLIN, CRAIG R.; WILKINSON, H. SCOTT; MCGLYNN, PAUL; MCVICAR, WILLIAM K.
To: SEPRACOR INC.
Reel/Frame 024793/0105 →
Continuity (3)
Continuation 12196071 · Aug 21, 2008
Provisional Application 60966391 · Aug 28, 2007
Related Publication 20100215589A1 · Aug 26, 2010