IP Library › Granted Patent US 9,732,031
Granted Patent B2
US 9,732,031 · App. 15/103,144 · Granted Aug 15, 2017

Methods of treating neurological and other disorders using enantiopure deuterium-enriched bupropion

Inventors: Sheila DeWitt (Auburn, NH); Vincent Jacques (Somerville, MA); Leonardus H. T. van der Ploeg (Newton, MA)
Assignee: DeuteRx, LLC
C07C225/10A61K31/137C07B2200/07
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Quick Facts
Patent No.
US 9,732,031
App. No.
15/103,144
Granted
Aug 15, 2017
Kind
B2
Abstract

The invention provides enantiopure deuterium-enriched bupropion, pharmaceutical compositions, and methods of treating neurological disorders, movement disorders, cardiovascular disorders, metabolic disorders, and other disorders using enantiopure deuterium-enriched bupropion. A preferred aspect of the invention provides methods of treating obesity and sexual dysfunction using enantiopure deuterium-enriched bupropion.

Claims (15)

1. A method of treating obesity, comprising administering to a patient in need thereof a therapeutically effective amount of a deuterium-enriched compound of Formula I-A having an optical purity of at least 75% enantiomeric excess to treat the obesity, wherein Formula I-A is represented by:

or a pharmaceutically acceptable salt thereof, wherein Z is H or D, provided that the abundance of deuterium in Z is at least 60%.

2. A method of treating obesity, comprising administering to a patient in need thereof a therapeutically effective amount of a deuterium-enriched compound of Formula II-A having an optical purity of at least 75% enantiomeric excess to treat the obesity, wherein Formula II-A is represented by:

or a pharmaceutically acceptable salt thereof, wherein Z is H or D, provided that the abundance of deuterium in Z is at least 60%.

3. The method of claim 2 , wherein the abundance of deuterium in Z is at least 90%.

4. The method of claim 3 , wherein the compound has an enantiomeric excess of at least 85%.

5. The method of claim 2 , wherein the compound is:

or a pharmaceutically acceptable salt thereof, each having an optical purity of at least 90% enantiomeric excess.

6. The method of claim 2 , wherein the compound is:

having an optical purity of at least 90% enantiomeric excess.

7. The method of claim 2 , wherein the compound is:

or pharmaceutically acceptable salt thereof, each having an optical purity of at least 95% enantiomeric excess.

8. The method of claim 2 , wherein the compound is:

having an optical purity of at least 95% enantiomeric excess.

9. The method of claim 5 , wherein the compound is administered at a daily dose in the range of about 50 mg to 75 mg, 75 mg to 100 mg, 100 mg to 125 mg, 125 mg to 150 mg, 150 mg to 175 mg, 175 mg to 200 mg, 200 mg to 225 mg, 225 mg to 250 mg, 250 mg to 275 mg, or 275 mg to 300 mg.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 20, 2026
From: DEUTERX, LLC
To: AXSOME THERAPEUTICS, INC.
Reel/Frame 073523/0608 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 18, 2016
From: DEWITT, SHEILA; JACQUES, VINCENT; VAN DER PLOEG, LEONARDUS
To: DEUTERX, LLC
Reel/Frame 039475/0749 →
Continuity (2)
Provisional Application 61919155 · Dec 20, 2013
Related Publication 20160311757A1 · Oct 27, 2016