# US 10,369,159 B2 · Estrogen receptor β partial agonist having estrogen receptor α inhibitory effect, and gynecological disease therapeutic agent using same

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- Number: US 10,369,159 B2
- Document ID: US10369159B2
- Status: Granted
- Kind: B2
- Application number: 16/138,556
- Filed: 2018-09-21
- Published: 2019-01-24
- Granted: 2019-08-06
- Earliest claimed: 2015-07-14
- Assignees: Nobelpharma AB; National University Corporation Tottori University
- Applicants: Nobelpharma Co., Ltd.; National University Corporation Tottori University
- Inventors: Kenichiro Nakao; Tasuku Harada; Fuminori Taniguchi
- Web page: https://patentgrep.com/patent/US10369159B2

## CPC

- A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
- A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives
- C07J 41/0072: {the A ring of the steroid being aromatic}
- 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

[Problem] To provide a therapeutic agent for estrogen-dependent gynecological diseases such as endometriosis, uterine fibroids, and uterus adenomyosis. [Solution] To use an estrogen receptor α-inhibiting β partial agonist represented by the formula (a), a pharmaceutically-acceptable salt thereof, or a hydrate of either of the afore-mentioned, as an active ingredient.

## Claims

### Claim 1

A method of treating a gynecological disease, comprising:
administering an effective amount of a compound represented by following formula (a);
to a patient in need thereof,
wherein the gynecological disease is at least one disease selected from the group consisting of endometriosis, uterine fibroids, and uterus adenomyosis.

### Claim 2 (depends on 1)

The method according to claim 1, wherein the compound is a pharmaceutically acceptable salt of the compound represented by the formula (a).

### Claim 3 (depends on 2)

The method according to claim 2, wherein the pharmaceutically acceptable salts is at least one organic salt selected from the group consisting of citrate, fumarate, succinate, benzoate, and malonate.

### Claim 4 (depends on 1)

The method according to claim 1, wherein the compound is an estrogen receptor β partial agonist having estrogen receptor α inhibitory effect.