# US 10,765,688 B2 · Lipolytic composition containing phosphocholine derivatives

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- Number: US 10,765,688 B2
- Document ID: US10765688B2
- Status: Granted
- Kind: B2
- Application number: 15/906,451
- Filed: 2018-02-27
- Published: 2019-05-09
- Granted: 2020-09-08
- Earliest claimed: 2017-11-03
- Assignees: Penmix Ltd.
- Applicants: Penmix Ltd.
- Inventors: Dongkyu Park; Sang Yun Lee; Young Sub Song; Surin Kim; Joo Hwan Kim; Ji Hyun Moon; Seung Jun Lee; Hana Lee; Seung Ho Ji
- Web page: https://patentgrep.com/patent/US10765688B2

## CPC

- A61K 31/575: substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
- A61K 31/661: Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion {or mevinphos}
- A61K 8/553: {Phospholipids, e.g. lecithin}
- A61K 31/56: Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K 31/685: one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 3/04: Anorexiants; Antiobesity agents
- A61Q 19/06: for countering cellulitis
- A61K 2800/84: Products or compounds obtained by lyophilisation, freeze-drying
- A61K 2800/91: Injection
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61Q: SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS

## Abstract

The present invention provides a composition for lipolysis, for example a pharmaceutical composition for preventing or treating obesity including localized fat deposits (LFD), comprising certain phosphocholine derivatives or pharmaceutically acceptable salt thereof. The pharmaceutical composition of the present invention shows an excellent lipolytic activity as well as a uniform lipolytic activity. And also, the pharmaceutical composition of the present invention can minimize side effects such as inflammation, tissue necrosis, etc., at the administered site. In addition, the pharmaceutical composition of the present invention has excellent storage stability.

## Claims

### Claim 1

A method for treating localized fat deposits in a subject in need thereof, comprising topically administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of a phosphocholine derivative or pharmaceutically acceptable salt thereof,
wherein the phosphocholine derivative is selected from the group consisting of
1,2-dimyristoyl-sn-glycero-3-phosphocholine;
1,2-dipalmitoyl-sn-glycero-3-phosphocholine;
1-stearoyl-2-myristoyl-sn-glycero-3-phosphocholine;
1,2-didecanoyl-sn-glycero-3-phosphocholine; and
1-palmitoyl-2-stearoyl-sn-glycero-3-phosphocholine, and
wherein the pharmaceutical composition is a formulation for topical administration selected from the group consisting of a formulation for transdermal administration, a formulation for subcutaneous administration, a formulation for intramuscular administration, and a formulation for intraperitoneal administration.

### Claim 2 (depends on 1)

The method according to claim 1, wherein the phosphocholine derivative is 1,2-dimyristoyl-sn-glycero-3-phosphocholine.

### Claim 3 (depends on 1)

The method according to claim 1, wherein the pharmaceutical composition further comprises a therapeutically effective amount of bile acid or pharmaceutically acceptable salt thereof.

### Claim 4 (depends on 3)

The method according to claim 3, wherein the bile acid or pharmaceutically acceptable salt thereof is one or more selected from the group consisting of cholic acid, glycocholic acid, glycodeoxycholic acid, deoxycholic acid, taurocholic acid, ursodeoxycholic acid, tauroursodeoxycholic acid, taurodeoxycholic acid, chenodeoxycholic acid, glycoursodeoxycholic acid, sodium deoxycholate, and sodium taurocholate.

### Claim 5 (depends on 3)

The method according to claim 3, wherein the bile acid or pharmaceutically acceptable salt thereof is one or more selected from the group consisting of glycocholic acid, deoxycholic acid, taurocholic acid, tauroursodeoxycholic acid, glycoursodeoxycholic acid, sodium deoxycholate, and sodium taurocholate.

### Claim 6 (depends on 3)

The method according to claim 3, wherein the phosphocholine derivative or pharmaceutically acceptable salt thereof and the bile acid or pharmaceutically acceptable salt thereof are in a weight ratio of from 0.5:1 to 40:1.

### Claim 7 (depends on 1)

The method according to claim 1, wherein the formulation for topical administration is a liquid formulation or a dry powder formulation.

### Claim 8 (depends on 1)

The method according to claim 1, wherein the formulation for topical administration is a solution, an emulsion, or a lyophilized powder.

### Claim 9 (depends on 1)

The method according to claim 1, wherein the formulation for topical administration comprises one or more pharmaceutically acceptable excipient(s) selected from the group consisting of a pH controlling agent, an isotonic agent, a surfactant, a stabilizer, a preservative, a chelating agent, a buffer, and a cryoprotectant; and one or more pharmaceutically acceptable carriers selected from the group consisting of an oil, an organic solvent, and an aqueous solvent.