# US 12,213,959 B2 · Use of 3-O-sulfamoyloxy-7β-methyl-d-homo-6-oxaestra-1,3,5(10),8(9)-tetraen-17a-one to treat breast cancer

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- Number: US 12,213,959 B2
- Document ID: US12213959B2
- Status: Granted
- Kind: B2
- Application number: 17/292,690
- Filed: 2019-09-19
- Published: 2022-05-26
- Granted: 2025-02-04
- Earliest claimed: 2018-11-08
- Applicants: Natalia Eduardovna Iliasova
- Inventors: Shamil Sionovich Ilyasov; Alexandr Grigorievich Shavva; Svetlana Nikolaevna Morozkina
- Web page: https://patentgrep.com/patent/US12213959B2

## CPC

- A61K 31/566: having an oxo group in position 17, e.g. estrone
- A61K 31/138: Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine (atenolol A61K31/165; pindolol A61K31/404; timolol A61K31/5377)
- A61P 35/00: Antineoplastic agents
- C07D 311/78: Ring systems having three or more relevant rings
- C07J 73/003: {by oxygen as hetero atom}
- 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
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- C07J: STEROIDS (seco-steroids C07C)

## Abstract

The invention relates to the field of medicine and to the chemical and pharmacological industry, and concerns medicaments for the treatment of breast cancer. In particular the invention relates to a use of 3-O-sulfamoyloxy-7β-methyl-D-homo-6-oxaestra-1,3,5 (10),8(9)-tetraen-17a-one as an anti-cancer agent in monotherapy and adjuvant therapy of breast cancer, including the triple negative breast cancer.

## Claims

### Claim 1

A compound, which is 3-O-sulfamoyloxy-7β-methyl-D-homo-6-oxaestra-1,3,5 (10),8 (9)-tetraen-17a-one of formula 2:

### Claim 2

A method of treating cancer, the method comprising administering to a patient in need thereof an effective amount of 3-O-sulfamoyloxy-7β-methyl-D-homo-6-oxaestra-1,3,5 (10),8 (9)-tetraen-17a-one of formula 2:

### Claim 3 (depends on 2)

The method of claim 2, wherein the cancer is a breast cancer.

### Claim 4 (depends on 3)

The method of claim 3, wherein the patient is a female patient with an early stage of the breast cancer.

### Claim 5 (depends on 3)

The method of claim 3, wherein the patient is a female patient with an advanced form of the breast cancer.

### Claim 6 (depends on 5)

The method of claim 5, wherein the patient has been treated with tamoxifen.

### Claim 7 (depends on 3)

The method of claim 3, wherein the breast cancer is a triple negative form of the breast cancer.

### Claim 8 (depends on 4)

The method of claim 4, wherein the female patient is a woman in postmenopause.

### Claim 9 (depends on 5)

The method of claim 5, wherein the female patient is a woman in postmenopause.

### Claim 10 (depends on 3)

The method of claim 3, wherein 3-O-sulfamoyloxy-7β-methyl-D-homo-6-oxaestra-1,3,5 (10),8 (9)-tetraen-17a-one of formula 2 is administered as monotherapy or adjuvant therapy.

### Claim 11 (depends on 4)

The method of claim 4, wherein 3-O-sulfamoyloxy-7β-methyl-D-homo-6-oxaestra-1,3,5 (10),8 (9)-tetraen-17a-one of formula 2 is administered orally.

### Claim 12

A method of preparing 3-O-sulfamoyloxy-7β-methyl-D-homo-6-oxaestra-1,3,5 (10),8 (9)-tetraen-17a-one of formula (2), the method comprising the reactions as follows

### Claim 13 (depends on 12)

The method of claim 12, wherein the compound of formula (4) is obtained by reacting chromanone of formula (3) with vinyl magnesium bromide and carrying out the condensation of the resulting vinyl carbinol with 2-methylcyclohexane-1,3-dione.

### Claim 14 (depends on 12)

The method of claim 12, wherein the cyclodehydratation reaction of the compound of formula (4) is carried out in hydrochloric acid in methanol to give a compound of formula (5).

### Claim 15 (depends on 12)

The method of claim 12, wherein estratetraen of formula (6) is prepared by hydrogenation of the compound of formula (5) over Pd/C in ethanol.