Methods and compositions for treating excessive sleepiness

Patent metadata

Field	Value
Publication number	US-10912754-B2
Application number	US-202016877717-A
Country	US
Kind code	B2
Filing date	May 19, 2020
Priority date	Jun 2, 2017
Publication date	Feb 9, 2021
Grant date	Feb 9, 2021

Abstract

The present invention relates to carbamoyl phenylalaninol compounds and methods of using the same to treat disorders. The invention further relates to the development of methods for treating excessive sleepiness in a subject, e.g., due to narcolepsy or obstructive sleep apnea, with the surprising outcome that “normal” levels of wakefulness are achieved based on standard objective and subjective sleepiness tests.

First claim

What is claimed is:

1. A method of treating excessive sleepiness in a human patient with obstructive sleep apnea (OSA) in need thereof, said method comprising orally administering [R]-2-amino-3-phenylpropylcarbamate (APC) or a pharmaceutically acceptable salt thereof to the human patient in accordance with a dosing regimen comprising a once-daily dose of 75 mg for at least 3 days followed by a once-daily dose of 150 mg, wherein the once-daily dose of 150 mg is the maximum dose in the dosing regimen, and wherein the APC or pharmaceutically acceptable salt thereof effects a reduction in excessive sleepiness as measured by Epworth Sleepiness Scale (ESS) score to below 10 points at the 12th week of the dosing regimen.

2. The method of claim 1 , wherein the dosing regimen comprises a once-daily dose of 75 mg for 3 days followed by a once-daily dose of 150 mg.

3. The method of claim 1 , wherein the patient with OSA has a baseline ESS score greater than 10.

4. The method of claim 1 , wherein the APC or pharmaceutically acceptable salt thereof effects a reduction in excessive sleepiness as measured by ESS score by at least 5 points at the 12th week of the dosing regimen.

5. The method of claim 1 , wherein the excessive sleepiness is excessive daytime sleepiness.

6. The method of claim 1 , wherein the APC is provided as a pharmaceutically acceptable salt of APC.

7. The method of claim 1 , wherein the APC is provided in the form of APC hydrochloride salt.

8. The method of claim 1 , wherein the daily dose is administered at least 10 hours before the patient's bedtime.

9. The method of claim 1 , wherein the daily dose is administered within 1 hour of the patient waking.

10. The method of claim 1 , wherein the patient is an adult.

Assignees

• Jazz Pharmaceuticals Ireland Ltd

Inventors

• Carter Lawrence Patrick
• Lu Yuan
• Zomorodi Katayoun

Classifications

• A61K9/2013

  Organic compounds, e.g. phospholipids, fats · CPC title

• A61K9/2054

  Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose · CPC title

• A61P25/00 Primary

  Drugs for disorders of the nervous system · CPC title

• A61K31/27 Primary

  of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine · CPC title

• A61K9/20

  Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)} · CPC title