# US 8,465,763 B2 · 3-hydroxychlormadinone acetate for the topical treatment of androgen-dependent skin diseases

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- Number: US 8,465,763 B2
- Document ID: US8465763B2
- Status: Granted
- Kind: B2
- Application number: 12/483,869
- Filed: 2009-06-12
- Published: 2009-12-24
- Granted: 2013-06-18
- Earliest claimed: 2006-12-22
- Assignees: Richter Gedeon Nyrt.
- Applicants: Georg Schramm; Christa Kneip
- Inventors: Georg Schramm; Christa Kneip
- Web page: https://patentgrep.com/patent/US8465763B2

## CPC

- A61K 31/57: substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
- A61K 8/63: Steroids; Derivatives thereof
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/08: Antiseborrheics
- A61P 17/10: Anti-acne agents
- A61P 17/14: for baldness or alopecia
- A61Q 7/00: Preparations for affecting hair growth
- A61Q 7/02: Preparations for inhibiting or slowing hair growth
- A61Q 19/00: Preparations for care of the skin
- 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 relates to the use of 3β-hydroxychlormadinone acetate (17α-acetoxychloropregna-4,6-dien-3β-ol-20-one) and/or 3α-hydroxychlormadinone acetate (17α-acetoxychloropregna-4,6-dien-3α-ol-20-one) for producing a medicament for treating skin, preferably human skin by means of topical application, and to a pharmaceutical or cosmetic composition containing 3β-hydroxychlormadinone acetate and/or 3α-hydroxychlormadinone acetate.

## Claims

### Claim 1

A pharmaceutical composition for treating the skin by means of topical application, comprising 0.01 to 20 wt. % of 3β-hydroxychlormadinone acetate (17α-acetoxychloropregna-4,6-dien-3β-ol-20-one) or 3α-hydroxychlormadinone acetate (17α-acetoxychloropregna-4,6-dien-3α-ol-20-one), or mixtures thereof and at least one pharmaceutically acceptable vehicle wherein the composition is formulated as a cream, ointment, lotion, gel, tincture, mask, facial lotion, hair balsam, hair conditioner, hair gel, hair tonic, hair lotion, hair cream or hair shampoo.

### Claim 2

A cosmetic composition for care of the skin by topical application comprising 0.01 to 5 wt. % of 3β-hydroxychlormadinone acetate or 3α-hydroxychlormadinone acetate or mixtures thereof and at least one cosmetic vehicle wherein the composition is formulated as a cream, ointment, lotion, gel, tincture, mask, facial lotion, hair balsam, hair conditioner, hair gel, hair tonic, hair lotion, hair cream or hair shampoo.

### Claim 3 (depends on 1)

A pharmaceutical composition according to claim 1 comprising at least one buffer, at least one preservative, at least one aroma additive or at least one auxiliary substance.

### Claim 4 (depends on 3)

A pharmaceutical composition according to claim 3, wherein the preservative is at least one compound selected from the group consisting of antioxidants, reducing agents and UV absorbers.

### Claim 5 (depends on 3)

A pharmaceutical composition according to claim 3, wherein characterised the 3β-hydroxychlormadinone acetate or 3α-hydroxychlormadinone acetate is distributed in molecularly disperse manner in a hydrophilic component.

### Claim 6 (depends on 3)

A pharmaceutical composition according to claim 3, wherein the active ingredient 3β-hydroxychlormadinone acetate or 3α-hydroxychlormadinone acetate is distributed in molecularly disperse manner in a moisturising base.

### Claim 7 (depends on 3)

A pharmaceutical composition according to claim 3, wherein the composition contains a penetration promoter.

### Claim 8 (depends on 3)

A pharmaceutical composition according to claim 3, wherein the composition contains at least one colorant or one fragrance.

### Claim 9 (depends on 3)

A pharmaceutical composition according to claim 3, suitable for at least once daily topical treatment of human skin.

### Claim 10 (depends on 2)

A cosmetic composition according to claim 2, suitable for at least once daily care of human skin.

### Claim 11 (depends on 6)

A pharmaceutical composition according to claim 6, wherein the 3β-hydroxychlormadinone acetate or 3α-hydroxychlormadinone acetate is distributed in molecularly disperse manner in a moisturizing base in combination with a hydrophilic component.

### Claim 12 (depends on 7)

A pharmaceutical composition according to claim 7, wherein the penetration promoter is a compound selected from the group consisting of acid amides and amines.

### Claim 13 (depends on 9)

A pharmaceutical composition according to claim 9, wherein the composition is applied to the scalp, facial skin, skin of the upper body, skin of the back, skin of the chest or hair.

### Claim 14 (depends on 2)

A cosmetic composition according to claim 2, comprising at least one buffer, at least one preservative, at least one aroma additive or at least one auxiliary substance.

### Claim 15 (depends on 14)

A cosmetic composition according to claim 14, wherein the preservative is at least one compound selected from the group consisting of antioxidants, reducing agents and UV absorbers.

### Claim 16 (depends on 14)

A cosmetic composition according to claim 14, wherein the 3β-hydroxychlormadinone acetate or 3α-hydroxychlormadinone acetate is distributed in molecularly disperse manner in a hydrophilic component.

### Claim 17 (depends on 14)

A cosmetic composition according to claim 14, wherein 3β-hydroxychlormadinone acetate or 3α-hydroxychlormadinone acetate is distributed in molecularly disperse manner in a moisturizing base.

### Claim 18 (depends on 14)

A cosmetic composition according to claim 14, wherein the composition contains a penetration promoter.

### Claim 19 (depends on 14)

A cosmetic composition according to claim 14, wherein the composition contains at least one colorant or one fragrance.

### Claim 20 (depends on 1)

A pharmaceutical composition according to claim 1 wherein the composition is used for the topical treatment of an androgen-dependent disease.

### Claim 21 (depends on 20)

A pharmaceutical composition according to claim 20 wherein the androgen-dependent diseases are selected from acne, seborrhea, hirsuitism, and alopecia.

### Claim 22 (depends on 1)

A pharmaceutical composition according to claim 1 wherein the composition is used for the promotion of hair growth in both female and male patients.

### Claim 23 (depends on 1)

A method for treating androgen-dependent diseases comprising topically applying the composition according to claim 1 to a patient in need thereof.

### Claim 24 (depends on 23)

A method according to claim 23 wherein the androgen-dependent diseases are selected from acne, seborrhea, hirsuitism, and alopecia.

### Claim 25 (depends on 1)

A method for promoting hair growth in a male or female comprising topically applying the composition according to claim 1 to a patient in need thereof.
