IP Library Granted Patent US 11,040,024
Granted Patent B2
US 11,040,024 · App. 16/805,196 · Granted Jun 22, 2021

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

Inventors: George W. Muller (Rancho Sante Fe, CA); Peter H. Schafer (Belle Mead, NJ); Hon-Wah Man (Princeton, NJ); Chuansheng Ge (Belle Mead, NJ)
Assignee: AMGEN INC.
A61K31/4035A61K45/06C07C317/28C07D209/48C07B2200/07Y02A50/30
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Quick Facts
Patent No.
US 11,040,024
App. No.
16/805,196
Granted
Jun 22, 2021
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 (9)

1. A pharmaceutical composition comprising stereomerically pure (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, or a pharmaceutically acceptable salt, solvate or hydrate thereof, and a propellant, wherein the pharmaceutical composition is an aerosol dosage form.

2. The pharmaceutical composition of claim 1 , wherein the propellant comprises a halogenated hydrocarbon.

3. The pharmaceutical composition of claim 2 , wherein the propellant is selected from the group consisting of trichloromonofluoromethane, dichlorodifluoromethane, dichlorotetrafluoroethane, and combinations thereof.

4. The pharmaceutical composition of claim 1 , wherein the propellant is trichloromonofluoromethane, dichlorodifluoromethane, and dichlorotetrafluoromethane.

5. The pharmaceutical composition of claim 1 comprising:

a. 0.17 wt. % (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione,

b. 24.20 wt. % trichloromonofluoromethane,

c. 53.11 wt. % dichlorodifluoromethane, and

d. 22.52 wt. % dichlorotetrafluoroethane.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 26, 2020
From: CELGENE CORPORATION
To: AMGEN INC.
Reel/Frame 053061/0390 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 26, 2020
From: SCHAFER, PETER H.; MULLER, GEORGE W.; MAN, HON-WAH; GE, CHUANSHENG
To: CELGENE CORPORATION
Reel/Frame 053708/0156 →
Continuity (12)
Continuation 16125571 · Sep 7, 2018
Continuation 15629678 · Jun 21, 2017
Continuation 15016856 · Feb 5, 2016
Continuation 14316160 · Jun 26, 2014
Continuation 13682652 · Nov 20, 2012
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 20200306226A1 · Oct 1, 2020