# US 8,569,274 B2 · Progesterone antagonist and selective progesterone modulator in the treatment of excessive uterine bleeding

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- Number: US 8,569,274 B2
- Document ID: US8569274B2
- Status: Granted
- Kind: B2
- Application number: 12/596,624
- Filed: 2008-04-18
- Published: 2010-07-29
- Granted: 2013-10-29
- Earliest claimed: 2007-04-20
- Assignees: PregLem SA
- Applicants: Bartholomeus C. J. M. Fauser; Ernest Loumaye
- Inventors: Bartholomeus C. J. M. Fauser; Ernest Loumaye
- Web page: https://patentgrep.com/patent/US8569274B2

## CPC

- A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
- A61K 31/567: substituted in position 17 alpha, e.g. mestranol, norethandrolone
- A61K 31/57: substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
- A61P 5/00: Drugs for disorders of the endocrine system
- A61P 5/36: Antigestagens
- A61P 7/00: Drugs for disorders of the blood or the extracellular fluid
- A61P 7/02: Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
- A61P 7/04: Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
- A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives
- 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

## Abstract

Progesterone antagonists and SPRM are useful to prepare a medication for the treatment or the prophylaxis of excessive uterine bleeding in women with spontaneous or iatrogenic coagulation disorders such as thrombopenia, coagulation factor deficiency or anti-coagulant therapy. Treatment will last from 1 day to 180 days.

## Claims

### Claim 1

A method of treating excessive uterine bleeding resulting from a coagulation disorder comprising administering a therapeutically effective amount of a progesterone antagonist, a selective progesterone receptor modulator (SPRM), or an active metabolite thereof, or a combination of two or more of said progesterone antagonists, SPRMs, or active metabolites, or a combination of two or more of said progesterone antagonists, SPRMs or active metabolites thereof, to a woman in need thereof, wherein
said progesterone antagonist or SPRM is selected from the group consisting of CDB-2914, mifepristone, asoprisnil, CDB-4124, onapristone, org33628, tanaproget, tanaproget-combo, 11 beta-((4-N,N-dimethylamino)-phenyl)-17 beta-hydroxy-18-methyl-17 alpha-propinyl-4,9(10)-estradien-3-one, 11 beta-((4-N,N-dimethylamino)-phenyl)-17 a beta-hydroxy-17a alpha-propinyl-D-homo-4,9(10),16-estradien-3-one, 11 beta-4-methoxyphenyl-17 beta-hydroxy-17 alpha-ethinyl-4,9(10)-estradien-3-one, 11 beta-(4-acetylphenyl)-17 beta-hydroxy-17 alpha-(prop-1-inyl)-4,9(10)estradien-3-one, 11 beta-(4-dimethylaminophenyl)-17 alpha-hydroxy-17 beta-(3-hydroxy-propyl)-13 alpha-methyl-4,9-gonadien-3-one, (Z)-11 beta-[4-(dimethylamino)phenyl]-17beta-hydroxy-17alpha-(3-hydroxy-1-propenyl)-estr-4-en-3-one-5, 11 beta-(4-acetylphenyl)-17 beta-hydroxy-17 alpha-(3-hydroxyprop-1-(Z)-enyl)-4,9(10)-estradien-3-one, 11 beta-(4-cyanophenyl)-17 beta-hydroxy-17 alpha-(3-hydroxyprop-1-(Z)-enyl)-4-androsten-3-one, 11 beta, 19-(4-(3-pyridinyl)-o-phenylene)-17 beta-hydroxy-17 alpha-(3-hydroxyprop-1-(Z)-enyl)-4-androsten-3-one, and an active metabolite of any of said progesterone antagonists or SPRMs.

### Claim 2 (depends on 1)

The method of claim 1, wherein the coagulation disorder is selected from the group consisting of hemophilia, von Willebrand's disease, hepatic function impairment, thrombocytopenia, leukemia, disseminated intravascular coagulation, bone marrow aplasia and inadequate anticoagulation treatment.

### Claim 3 (depends on 1)

The method of claim 1, wherein said active metabolite of asoprisnil is selected from the group consisting of J912, J956 and a combination thereof.

### Claim 4 (depends on 1)

The method of claim 1, wherein said active metabolite of CDB-4124 is CDB-4453.

### Claim 5 (depends on 1)

The method of claim 1, wherein said active metabolite of CDB-2914 is selected from the group consisting of CBD-3877, CDB-3963, CDB-3236, and CDB-4183, and a combination of two or more of said metabolites.

### Claim 6 (depends on 1)

The method of claim 1, wherein said administration is over a period of 1 to 180 days.

### Claim 7 (depends on 1)

The method of claim 1, wherein said administration is during bleeding peaks or during menstruation.

### Claim 8 (depends on 1)

The method of claim 1, wherein said administration is daily, every other day, once a week or once every month.

### Claim 9 (depends on 1)

The method of claim 1, wherein said administration is a one-time administration.

### Claim 10 (depends on 1)

The method of claim 1, wherein said progesterone antagonist, SPRM, or active metabolite thereof is administered at a daily dose between 0.1 to 1000 mg.

### Claim 11 (depends on 10)

The method of claim 10, wherein the SPRM is CDB-2914, or an active metabolite thereof, and is administered at a daily dose between 5 to 15 mg.

### Claim 12 (depends on 1)

The method of claim 1, wherein said progesterone antagonist, SPRM or active metabolite thereof is administered with an oestrogen, either simultaneously or sequentially.

### Claim 13 (depends on 1)

The method of claim 1, wherein said progesterone antagonist, SPRM, or active metabolite thereof is administered by vaginal, rectal, subcutaneous, intravenous, intradermal, intramuscular, intraperitoneal, intra-uterine, intranasal, transdermal, or buccal routes or via an implanted device.

### Claim 14 (depends on 1)

The method of claim 1, wherein said progesterone antagonist, SPRM, or active metabolite thereof is selected from the group consisting of CDB-2914, mifepristone, CDB-4124, onapristone, org33628, 11 beta-((4-N,N-dimethylamino)-phenyl)-17 beta-hydroxy-18-methyl-17 alpha-propinyl-4,9(10)-estradien-3-one, 11 beta-((4-N,N-dimethylamino)-phenyl)-17 a beta-hydroxy-17a alpha-propinyl-D-homo-4,9(10),16-estratrien-3-one, 11 beta-4-methoxyphenyl-17 beta-hydroxy-17 alpha-ethinyl-4,9(10)-estradien-3-one, 11 beta-(4-acetylphenyl)-17 beta-hydroxy-17 alpha-(prop-1-inyl)-4,9(10)estradien-3-one, 11 beta-(4-dimethylaminophenyl)-17 alpha-hydroxy-17 beta-(3-hydroxy-propyl)-13 alpha-methyl-4,9-gonadien-3-one, (Z)-11 beta-[4-(dimethylamino)phenyl]-17beta-hydroxy-17alpha-(3-hydroxy-1-propenyl)-estr-4-en-3-one-5, 11 beta-(4-acetylphenyl)-17 beta-hydroxy-17 alpha-(3-hydroxyprop-1-(Z)-enyl)-4,9(10)-estradien-3-one, 11 beta-(4-cyanophenyl)-17 beta-hydroxy-17 alpha-(3-hydroxyprop-1-(Z)-enyl)-4-androsten-3-one, 11 beta, 19-(4-(3-pyridinyl)-o-phenylene)-17 beta-hydroxy-17 alpha-(3-hydroxyprop-1-(Z)-enyl)-4-androsten-3-one, and an active metabolite of any of said progesterone antagonists or SPRMs.