Estrogen receptor modulators and uses thereof

Patent metadata

Field	Value
Publication number	US-9868704-B2
Application number	US-201615186246-A
Country	US
Kind code	B2
Filing date	Jun 17, 2016
Priority date	Sep 16, 2010
Publication date	Jan 16, 2018
Grant date	Jan 16, 2018

Abstract

Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

First claim

What is claimed is:

1. A method of treating breast cancer comprising administering a therapeutically effective amount of (E)-3-(4-((E)-2-(2-Chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)but-1-en-1-yl)phenyl)acrylic acid, or a pharmaceutically acceptable salt thereof, to a patient.

2. The N-methylglucamine salt of (E)-3-(4-((E)-2-(2-Chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)but-1-en-1-yl)phenyl)acrylic acid.

3. A pharmaceutical composition comprising (E)-3-(4-((E)-2-(2-Chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)but-1-en-1-yl)phenyl)acrylic acid, or a pharmaceutically acceptable salt thereof, and an excipient or carrier.

4. The pharmaceutical composition of claim 3 wherein the pharmaceutically acceptable salt of (E)-3 -(4-((E)-2-(2-Chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)but-1-en-1-yl)phenyl)acrylic acid is the N-methylglucamine salt.

5. The method of claim 1 , wherein the therapeutically effective amount of (E)-3-(4-((E)-2-(2-Chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)but-1-en-1-yl)phenyl)acrylic acid or a pharmaceutically acceptable salt thereof is administered before the patient has received surgery.

6. The method of claim 1 , wherein the therapeutically effective amount of (E)-3-(4-((E)-2-(2-Chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)but-1-en-1-yl)phenyl)acrylic acid or a pharmaceutically acceptable salt thereof is administered after the patient has received surgery.

7. The method of claim 1 , wherein the patient has hormone receptor positive metastatic breast cancer.

8. The method of claim 7 , wherein the patient has disease progression following anti-estrogen therapy before said administration.

9. A method of treating breast cancer, the method comprising administering a therapeutically effective amount of the N-methylglucamine salt of (E)-3-(4-((E)-2-(2-Chloro-4-fluorophenyl)-1-(1H-indazol5 -yl)but-1-en-1-yl)phenyl)acrylic acid to a patient.

10. The method of claim 9 , wherein the therapeutically effective amount of the N-methylglucamine salt of (E)-3-(4((E)-2-(2-Chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)but-1-en-1-yl)phenyl)acrylic acid is administered before the patient has received surgery.

11. The method of claim 9 , wherein the therapeutically effective amount of the N-methylglucamine salt of (E)-3-(4((E)-2-(2-Chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)but-1-en-1-yl)phenyl)acrylic acid is administered after the patient has received surgery.

12. The method of claim 9 , wherein the patient has hormone receptor positive metastatic breast cancer.

13. The method of claim 12 , wherein the patient has disease progression following anti-estrogen therapy before said administration.

14. A method of treating breast cancer comprising administering a therapeutically effective amount of the pharmaceutical composition of claim 3 to a patient having breast cancer.

15. The method of claim 14 , wherein the pharmaceutical composition is administered before the patient has received surgery.

16. The method of claim 14 , wherein the pharmaceutical composition is administered after the patient has received surgery.

17. The method of claim 14 , wherein the patient has hormone receptor positive metastatic breast cancer.

18. The method of claim 17 , wherein the patient has disease progression following anti-estrogen therapy before said administration.

Assignees

• Genentech Inc

Inventors

• Smith Nicholas D
• Kahraman Mehmet
• Govek Steven P
• Nagasawa Johnny Y
• Lai Andiliy G
• Julien Jackaline D
• Herbert Mark R
• Douglas Karensa L

Classifications

• A61P37/06

  Immunosuppressants, e.g. drugs for graft rejection · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P9/10

  for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title

• A61P9/12

  Antihypertensives · CPC title

• A61P35/00

  Antineoplastic agents · CPC title