IP Library Granted Patent US 11,406,646
Granted Patent B2
US 11,406,646 · App. 17/094,432 · Granted Aug 9, 2022

Compositions comprising 5-cholesten-3, 25-diol, 3-sulfate (25HC3S) or pharmaceutically acceptable salt thereof and at least one cyclic oligosaccharide

Inventors: Shunlin Ren (Richmond, VA); Leyuan Xu (Richmond, VA); Yanxia Ning (Richmond, VA); Jin Koung Kim (Richmond, VA); WeiQi Lin (Emerald Hills, CA); Andrew R. Miksztal (Palo Alto, CA); Hongwei Wu (Cupertino, CA); Min L. Lee (Saratoga, CA)
Assignees: Virginia Commonwealth University; Durect Corporation; The United States Government as Represented by The Department of Veterans Affairs
A61K31/565A61K8/63A61K8/738A61K9/0019A61K9/19A61K31/575A61K31/724A61K47/10A61K47/40A61P1/16A61P3/06A61P17/06A61P31/04A61Q19/00A61Q19/004A61Q19/007C07J31/006
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Quick Facts
Patent No.
US 11,406,646
App. No.
17/094,432
Granted
Aug 9, 2022
Kind
B2
Abstract

Compositions comprising 5-cholesten-3,25-diol, 3-sulfate (25HC3S) or pharmaceutically acceptable salt thereof and at least one cyclic oligosaccharide, e.g., a cyclodextrin (CD), are provided. The compositions may be used to prevent and/or treat a variety of diseases and conditions, including organ failure (e.g. acute liver failure), high cholesterol/high lipids, and various inflammatory diseases and conditions.

Claims (28)

1. A method of treating alcoholic hepatitis in a subject in need thereof, comprising intravenously administering an effective amount of an aqueous pharmaceutical composition comprising:

5-cholesten-3,25-diol, 3-sulfate (25HC3 S) or pharmaceutically acceptable salt thereof,

at least one buffer, and

at least one cyclic oligosaccharide comprising at least one of hydroxypropyl β-cyclodextrin and sulfobutyl ether β-cyclodextrin.

2. The method of claim 1 , wherein the 25HC3 S or pharmaceutically acceptable salt thereof comprises a pharmaceutically acceptable salt of 25HC3 S.

3. The method of claim 1 , wherein the at least one cyclic oligosaccharide is present in the aqueous pharmaceutical composition at a concentration ranging from 0.1% (w/w) to 90% (w/w).

4. The method of claim 1 , wherein the aqueous pharmaceutical composition has an osmolality ranging from 270 mmol/kg to 340 mmol/kg.

5. The method of claim 1 , wherein the 25HC3S or pharmaceutically acceptable salt thereof is administered at a dose ranging from 0.001 mg/kg to 100 mg/kg.

6. The method of claim 1 , wherein the 25HC3 S or pharmaceutically acceptable salt thereof is administered at a dose ranging from 0.001 mg/kg to 10 mg/kg.

7. The method of claim 1 , wherein the 25HC3 S or pharmaceutically acceptable salt thereof is administered at a dose ranging from 0.1 mg/kg to 10 mg/kg.

8. The method of claim 2 , wherein the 25HC3 S or pharmaceutically acceptable salt thereof is administered at a dose ranging from 0.001 mg/kg to 10 mg/kg.

9. The method of claim 3 , wherein the 25HC3 S or pharmaceutically acceptable salt thereof is administered at a dose ranging from 0.001 mg/kg to 10 mg/kg.

10. The method of claim 1 , wherein the 25HC3 S or pharmaceutically acceptable salt thereof comprises a sodium salt of 25HC3S.

11. The method of claim 1 , wherein the at least one cyclic oligosaccharide comprises hydroxypropyl β-cyclodextrin.

12. The method of claim 1 , wherein the 25HC3 S or pharmaceutically acceptable salt thereof is present in the aqueous pharmaceutical composition at a concentration ranging from 0.01% (w/w) to 3% (w/w).

13. The method of claim 8 , wherein the 25HC3 S or pharmaceutically acceptable salt thereof is present in the aqueous pharmaceutical composition at a concentration ranging from 0.01% (w/w) to 3% (w/w).

14. The method of claim 1 , wherein the 25HC3 S or pharmaceutically acceptable salt thereof is present in the aqueous pharmaceutical composition at a concentration ranging from 0.1 mg/mL to 50 mg/mL.

15. The method of claim 8 , wherein the 25HC3 S or pharmaceutically acceptable salt thereof is present in the aqueous pharmaceutical composition at a concentration ranging from 0.1 mg/mL to 50 mg/mL.

16. The method of claim 1 , wherein the at least one cyclic oligosaccharide is present in the aqueous pharmaceutical composition at a concentration ranging from 0.1% (w/w) to 40% (w/w).

17. The method of claim 8 , wherein the at least one cyclic oligosaccharide is present in the aqueous pharmaceutical composition at a concentration ranging from 0.1% (w/w) to 40% (w/w).

18. The method of claim 1 , wherein the at least one buffer is present in the aqueous pharmaceutical composition at a concentration ranging from 0.1 mM to 50 mM.

19. The method of claim 8 , wherein the at least one buffer is present in the aqueous pharmaceutical composition at a concentration ranging from 0.1 mM to 50 mM.

20. The method of claim 1 , wherein

the 25HC3 S or pharmaceutically acceptable salt thereof comprises a sodium salt of 25HC3 S,

the at least one cyclic oligosaccharide comprises hydroxypropyl β-cyclodextrin,

the 25HC3 S or pharmaceutically acceptable salt thereof is present in the aqueous pharmaceutical composition at a concentration ranging from 0.01% (w/w) to 3% (w/w),

the at least one cyclic oligosaccharide is present in the aqueous pharmaceutical composition at a concentration ranging from 0.1% (w/w) to 40% (w/w), and

the at least one buffer is present in the aqueous pharmaceutical composition at a concentration ranging from 0.1 mM to 50 mM.

Assignments (6)
SECURITY INTEREST Recorded Mar 30, 2026
From: BAUSCH HEALTH IRELAND LIMITED; MEDICIS PHARMACEUTICAL CORPORATION; SALIX PHARMACEUTICALS, INC.; SOLTA MEDICAL IRELAND LIMITED
To: THE BANK OF NEW YORK MELLON
Reel/Frame 074223/0753 →
SECURITY INTEREST Recorded Mar 30, 2026
From: MEDICIS PHARMACEUTICAL CORPORATION
To: JPMORGAN CHASE BANK, N.A.
Reel/Frame 074227/0509 →
MERGER Recorded Feb 25, 2026
From: DURECT CORPORATION
To: MEDICIS PHARMACEUTICAL CORPORATION
Reel/Frame 073889/0196 →
MERGER Recorded Feb 19, 2026
From: DURECT CORPORATION
To: MEDICIS PHARMACEUTICAL CORPORATION
Reel/Frame 073837/0231 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 30, 2022
From: VIRGINIA COMMONWEALTH UNIVERSITY
To: VIRGINIA COMMONWEALTH UNIVERSITY; THE UNITED STATES GOVERNMENT AS REPRESENTED BY THE DEPARTMENT OF VETERANS AFFAIRS
Reel/Frame 060376/0928 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 9, 2021
From: REN, SHUNLIN; XU, LEYUAN; NING, YANXIA; KIM, JIN KOUNG; LIN, WEIQI; KIM, MEE JEAN; MIKSZTAL, ANDREW R.; WU, HONGWEI; LEE, MIN L.; TAMRAZ, WILMA
To: VIRGINIA COMMONWEALTH UNIVERSITY; DURECT CORPORATION
Reel/Frame 055531/0983 →