Compositions and methods for treating estrogen-related medical disorders

Patent metadata

Field	Value
Publication number	US-9895348-B2
Application number	US-201615264407-A
Country	US
Kind code	B2
Filing date	Sep 13, 2016
Priority date	Oct 24, 2012
Publication date	Feb 20, 2018
Grant date	Feb 20, 2018

Abstract

Disclosed herein are methods for treatment of estrogen-related medical disorders. The methods of treatment may comprise administering to a subject in need of such treatment a composition comprising a therapeutically effective amount of at least one compound of formula (I)

or a pharmaceutically acceptable salt thereof.

First claim

What is claimed is:

1. A method for treatment of an estrogen-related medical disorder, the method comprising administering to a subject in need of such treatment a composition comprising a therapeutically effective amount of at least one compound of formula (II)

or a pharmaceutically acceptable salt thereof,
wherein
A 2 is —O— or —C(═O)—,
R 5 and R 6 are each independently selected from the group consisting of hydrogen, alkyl, —SO 3 R x2 , —PO 3 R y2 R z2 , and —C(═O)R c ;
R c is selected from the group consisting of —OH and alkyl;
R x2 , R y2 and R z2 are each independently selected from the group consisting of hydrogen and a pharmaceutically acceptable cation; and
X is halogen or trifluoromethyl;
provided that 2-(4-fluorophenyl)-3-(4-hydroxyphenoxy)benzo[b]thiophen-6-ol is excluded from the compound of formula (II),
wherein the estrogen-related medical disorder is cancer.

2. The method of claim 1 , wherein the cancer is selected from the group consisting of breast cancer, ovarian cancer, prostate cancer, and lung cancer.

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

4. The method of claim 3 , wherein the breast cancer is a tamoxifen resistant breast cancer.

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

6. The method of claim 1 , wherein the at least one compound of formula (II) is 3-(4-fluorophenyl)-2-(4-hydroxyphenoxy)benzo[b]thiophen-6-ol or a pharmaceutically acceptable salt thereof.

Assignees

• Univ Illinois

Inventors

• Thatcher Gregory R
• Tonetti Debra
• Molloy Mary Ellen
• Michalsen Bradley
• Qin Zihui

Classifications

• A61P35/00

  Antineoplastic agents · CPC title

• G01N33/57595

  involving intracellular compounds · CPC title

• G01N2800/52

  Predicting or monitoring the response to treatment, e.g. for selection of therapy based on assay results in personalised medicine; Prognosis · CPC title

• A61K31/381 Primary

  having five-membered rings · CPC title

• C07D333/64

  Oxygen atoms · CPC title