IP Library Granted Patent US 10,774,031
Granted Patent B2
US 10,774,031 · App. 16/831,086 · Granted Sep 15, 2020

Prodrugs of gamma-hydroxybutyric acid, compositions and uses thereof

Inventors: Jia-Ning Xiang (Wuhan, CN); Xuesong Xu (Wuhan, CN); Xuan Zhang (Wuhan, CN)
Assignee: XW LABORATORIES INC.
C07C69/78C07B59/001C07C69/22C07C69/24C07C69/28C07C69/34C07C69/608C07C69/612C07C69/618C07C69/738C07C69/74C07C69/76C07C69/96C07C229/08C07C229/34C07C229/36C07C233/47C07C255/57C07C271/22C07C271/34C07C317/14C07C317/44C07D207/12C07D207/16C07D211/44C07D211/46C07D213/79C07D213/80C07D277/30C07D277/56C07D307/68C07D309/12C07D317/64C07D333/38C07C2601/06C07C2601/08C07C2601/14C07C2601/16
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Quick Facts
Patent No.
US 10,774,031
App. No.
16/831,086
Granted
Sep 15, 2020
Kind
B2
Abstract

The present disclosure discloses prodrugs of gamma-hydroxybutyric acid as well as compositions and uses thereof.

Claims (53)

1. A method of treating a disease in a patient, wherein the disease is selected from excessive daytime sleepiness in a patient with Parkinson's disease or chronic fatigue in a patient with Parkinson's disease, comprising administering to a patient in need thereof a therapeutically effective amount of a compound of Formula (IA):

or a pharmaceutically acceptable salt thereof, wherein,

R g is selected from hydrogen and C 1-6 alkyl; and

each of R h and R f is independently selected from hydrogen, C 1-6 alkyl, C 1-6 alkoxylcarbonyl, and C 3-6 cycloalkoxylcarbonyl.

2. The method of claim 1 , wherein R g is selected from hydrogen and C 1-3 alkyl.

3. The method of claim 1 , wherein at least one of R h and R f is selected from hydrogen and C 1-3 alkyl.

4. The method of claim 1 , wherein each of R h and R f is selected from hydrogen and C 1-3 alkyl.

5. The method of claim 1 , wherein,

R h is selected from hydrogen and C 1-3 alkyl; and

R f is —COR 5 , wherein R 5 is selected from C 1-3 alkoxyl and C 54 cycloalkyloxyl.

6. The method of claim 1 , wherein,

each of R h and R f is hydrogen; and

R g is selected from hydrogen and C 1-3 alkyl.

7. The method of claim 1 , wherein the carbon atom to which R g is bonded is in the (R)-configuration.

8. The method of claim 1 , wherein the carbon atom to which R g is bonded is in the (S)-configuration.

9. The method of claim 1 , wherein the compound is selected from:

4-(((tert-butoxycarbonyl)glycyl)oxy)butanoic acid;

4-(glycyloxy)butanoic acid;

4-((D-valyl)oxy)butanoic acid;

4-((L-alanyl)oxy)butanoic acid;

4-(((ethoxycarbonyl)glycyl)oxy)butanoic acid;

4-(((isopropoxycarbonyl)glycyl)oxy)butanoic acid;

4-((((cyclohexyloxy)carbonyl)glycyl)oxy)butanoic acid;

4-(((ethoxycarbonyl)-D-valyl)oxy)butanoic acid;

4-((L-valyl)oxy)butanoic acid;

a pharmaceutically acceptable salt of any of the foregoing;

and a combination of any of the foregoing.

10. The method of claim 1 , wherein the compound is 4-((L-valyl)oxy)butanoic acid (IIA) or a pharmaceutically acceptable salt thereof:

11. The method of claim 1 , wherein the compound is 4-(glycyloxy)buatanoic acid (IIB) or a pharmaceutically acceptable salt thereof:

12. The method of claim 1 , wherein the compound is 4-((L-alanyl)oxy)butanoic acid (IIC) or a pharmaceutically acceptable salt thereof:

13. The method of claim 1 , wherein administering comprises orally administering.

14. The method of claim 1 , wherein administering comprises administering a pharmaceutical composition comprising the compound of Formula (IA) or a pharmaceutically acceptable salt thereof.

15. The method of claim 1 , wherein the pharmaceutical composition comprises an oral formulation.

16. The method of claim 1 , wherein the pharmaceutical composition comprises an oral dosage form.

17. The method of claim 1 , wherein the pharmaceutical composition comprises a sustained release oral formulation.

18. The method of claim 1 , wherein the pharmaceutical composition comprises a quick release oral formulation.

19. The method of claim 1 , wherein the pharmaceutical composition comprises a delayed release oral formulation.

20. The method of claim 1 , wherein the disease is excessive daytime sleepiness in a patient with Parkinson's disease.

21. The method of claim 1 , wherein the disease is chronic fatigue in a patient with Parkinson's disease.

22. A method of treating excessive daytime sleepiness in a patient with Parkinson's disease, comprising administering to a patient in need thereof a therapeutically effective amount of a compound of Formula (IA):

or a pharmaceutically acceptable salt thereof, wherein,

each of R h and R f is hydrogen; and

R g is selected from hydrogen and C 1-3 alkyl.

23. The method of claim 22 , wherein the compound is 4-((L-valyl)oxy)butanoic acid (IIA) or a pharmaceutically acceptable salt thereof:

24. The method of claim 22 , wherein the compound is 4-(glycyloxy)buatanoic acid (IIB) or a pharmaceutically acceptable salt thereof:

25. The method of claim 22 , wherein the compound is 4-((L-alanyl)oxy)butanoic acid (IIC) or a pharmaceutically acceptable salt thereof:

26. A method of treating chronic fatigue in a patient with Parkinson's disease, comprising administering to a patient in need thereof a therapeutically effective amount of a compound of Formula (IA):

or a pharmaceutically acceptable salt thereof, wherein,

each of R h and R f is hydrogen; and

R g is selected from hydrogen and C 1-3 alkyl.

27. The method of claim 26 , wherein the compound is 4-((L-valyl)oxy)butanoic acid (IIA) or a pharmaceutically acceptable salt thereof:

28. The method of claim 26 , wherein the compound is 4-(glycyloxy)buatanoic acid (IIB) or a pharmaceutically acceptable salt thereof:

29. The method of claim 26 , wherein the compound is 4-((L-alanyl)oxy)butanoic acid (IIC) or a pharmaceutically acceptable salt thereof:

Assignments (2)
CHANGE OF NAME Recorded May 4, 2021
From: XW LABORATORIES INC.
To: XWPHARMA LTD.
Reel/Frame 056177/0619 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 26, 2020
From: XIANG, JIA-NING; XU, XUESONG; ZHANG, XUAN
To: XW LABORATORIES INC.
Reel/Frame 052241/0597 →
Priority Claims (2)
CN PCT/CN2015/090326 · Sep 23, 2015 · national
CN 2016 1 0782104 · Aug 31, 2016 · national
Continuity (4)
Continuation 16601908 · Oct 15, 2019
Continuation 16275165 · Feb 13, 2019
Continuation 15762559
Related Publication 20200223783A1 · Jul 16, 2020
Cited By (17)
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