# US 2019/0169225 A1 · Nuclear Sulfated Oxysterol, Potent Regulator of Lipid Homeostasis, for Therapy of Hypercholesterolemia, Hypertriglycerides, Fatty Liver Diseases, and Atherosclerosis

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- Number: US 2019/0169225 A1
- Document ID: US20190169225A1
- Status: Published application
- Kind: A1
- Application number: 16/154,007
- Filed: 2018-10-08
- Published: 2019-06-06
- Earliest claimed: 2004-10-25
- Assignees: Virginia Commonwealth University
- Applicants: Virginia Commonwealth University
- Inventors: Shunlin Ren; William M. Pandak
- Web page: https://patentgrep.com/patent/US20190169225A1

## CPC

- C07J 31/006: {not covered by C07J31/003}
- A61K 31/575: substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
- C07J 9/00: Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
- C07J: STEROIDS (seco-steroids C07C)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

The sulfated oxysterol 5-cholesten-3β, 25-diol 3-sulphate, a nuclear cholesterol metabolite that decreases lipid biosynthesis and increases cholesterol secretion and degradation, is provided as an agent to lower intracellular and serum cholesterol and/or triglycerides, and to prevent or treat lipid accumulation-associated inflammation and conditions associated with such inflammation. Methods which involve the use of this sulfated oxysterol to treat conditions associated with high cholesterol and/or high triglycerides and/or inflammation (e.g. hypercholesterolemia, hypertriglyceridemia, non-alcoholic fatty liver diseases, atherosclerosis, etc.) are also provided.

## Claims

### Claim at position 1

-11. (canceled)

### Claim 12

A method of decreasing fat accumulation in liver cells of a patient in need thereof, the method comprising administering a salt of 5-cholesten-3β, 25-diol 3-sulphate to the patient in an amount sufficient to decrease fat accumulation in the liver cells of the patient.

### Claim 13 (depends on 12)

The method of claim 12, wherein the salt is selected from a sodium salt, a potassium salt, a calcium salt, a lithium salt, and an ammonium salt.

### Claim 14 (depends on 12)

The method of claim 12, wherein the salt is a sodium salt.

### Claim 15 (depends on 12)

The method of claim 12, wherein the fat comprises triglycerides.

### Claim 16 (depends on 13)

The method of claim 13, wherein the fat comprises triglycerides.

### Claim 17 (depends on 14)

The method of claim 14, wherein the fat comprises triglycerides.

### Claim 18

A method of making a sodium salt of 5-cholesten-3β, 25-diol 3-sulphate, comprising:
sulfating a 3β position of 25-hydroxycholesterol to form 5-cholesten-3β, 25-diol 3-sulphate; and
combining the 5-cholesten-3β, 25-diol 3-sulphate with an alkaline solvent to form a solution comprising the sodium salt of 5-cholesten-3β, 25-diol 3-sulphate.

### Claim 19 (depends on 18)

The method of claim 18, wherein the alkaline solvent is an alcohol.

### Claim 20 (depends on 19)

The method of claim 19, wherein the alcohol is methanol.

### Claim 21 (depends on 18)

The method of claim 18, further comprising forming a solid comprising the sodium salt of 5-cholesten-3β, 25-diol 3-sulphate.

### Claim 22 (depends on 18)

The method of claim 18, further comprising performing flash chromatography on the solution comprising the sodium salt of 5-cholesten-3β, 25-diol 3-sulphate.

### Claim 23 (depends on 19)

The method of claim 19, further comprising performing flash chromatography on the solution comprising the sodium salt of 5-cholesten-3β, 25-diol 3-sulphate.

### Claim 24 (depends on 20)

The method of claim 20, further comprising performing flash chromatography on the solution comprising the sodium salt of formula 5-cholesten-3β, 25-diol 3-sulphate.

### Claim 25 (depends on 21)

The method of claim 21, further comprising performing flash chromatography on the solution comprising the sodium salt of formula 5-cholesten-3β, 25-diol 3-sulphate.

### Claim 26 (depends on 18)

The method of claim 18, wherein the pH of the alkaline solvent is about 8.

### Claim 27 (depends on 19)

The method of claim 19, wherein the pH of the alkaline solvent is about 8.

### Claim 28 (depends on 20)

The method of claim 20, wherein the pH of the alkaline solvent is about 8.

### Claim 29 (depends on 21)

The method of claim 21, wherein the pH of the alkaline solvent is about 8.

### Claim 30 (depends on 18)

A product made by the method of claim 18.

### Claim 31 (depends on 21)

A product made by the method of claim 21.