# US 2014/0154306 A1 · 17alfa, 21-dihydroxypregnene esters as antiandrogenic agents

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- Number: US 2014/0154306 A1
- Document ID: US20140154306A1
- Status: Published application
- Kind: A1
- Application number: 14/103,707
- Filed: 2013-12-11
- Published: 2014-06-05
- Earliest claimed: 2001-08-10
- Assignees: Cosmo S.p.A.
- Applicants: Cosmo S.P.A.
- Inventors: Mauro AJANI; Luigi MORO
- Web page: https://patentgrep.com/patent/US20140154306A1

## CPC

- A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
- A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)}
- A61K 9/06: Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)}
- A61K 9/127: Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
- A61K 47/06: Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/12: Carboxylic acids; Salts or anhydrides thereof
- A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
- A61K 47/20: containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
- A61P 5/24: of the sex hormones
- A61P 5/28: Antiandrogens
- A61P 13/08: of the prostate
- A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives
- A61P 15/16: Masculine contraceptives
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/08: Antiseborrheics
- A61P 17/10: Anti-acne agents
- A61P 17/14: for baldness or alopecia
- A61P 35/00: Antineoplastic agents
- C07J 5/0053: {not substituted in position 16}
- C07J 9/005: {containing a carboxylic function directly attached or attached by a chain containing only carbon atoms to the cyclopenta[a]hydrophenanthrene skeleton}
- 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
- C07J: STEROIDS (seco-steroids C07C)

## Abstract

17α,21-Dihydroxypregna-4,9-diene-3,20-dione and 17α,21-dihydroxypregna-4-ene-3,20-dione 17 and/or 21 esters of having remarkable antiandrogenic activity, and the processes for the preparation thereof.

## Claims

### Claim 1

A method of treating a patient suffering from acne or alopecia comprising administering to said patient topically an effective amount of 17α-propionyloxy-21-hydroxy-pregna-4-ene-3,20-dione.

### Claim 2 (depends on 1)

The method of claim 1, wherein the patient suffers from acne.

### Claim 3 (depends on 1)

The method of claim 1, wherein the patient suffers from alopecia.

### Claim 4

A method of treating a patient suffering from acne or alopecia comprising administering to said patient topically an effective amount of a pharmaceutical composition comprising 17α-propionyloxy-21-hydroxy-pregna-4-ene-3,20-dione.

### Claim 5 (depends on 4)

The method of claim 4, wherein the 17α-propionyloxy-21-hydroxy-pregna-4-ene-3,20-dione is present in the composition at a concentration of about 2 μg/μL to about 8 μg/μL.

### Claim 6 (depends on 4)

The method of claim 4, wherein the patient suffers from acne.

### Claim 7 (depends on 4)

The method of claim 4, wherein the patient suffers from alopecia.

### Claim 8 (depends on 4)

The method of claim 4, wherein the pharmaceutical composition is selected from the group consisting of a liposomal emulsion or suspension, a cream, and a gel.

### Claim 9 (depends on 8)

The method of claim 8, wherein the pharmaceutical composition is a cream.

### Claim 10 (depends on 9)

The method of claim 9, wherein the cream comprises cetyl alcohol, glycerol monostearate, liquid paraffin, propylene glycol, disodium mono-oleo-amido sulfosuccinate, citric acid monohydrate, and purified water.