Estrogen receptor ligands, compositions and methods related thereto

Patent metadata

Field	Value
Publication number	US-11622954-B2
Application number	US-202117203548-A
Country	US
Kind code	B2
Filing date	Mar 16, 2021
Priority date	Sep 9, 2016
Publication date	Apr 11, 2023
Grant date	Apr 11, 2023

Abstract

Provided are compounds and methods for treating neurodegenerative diseases and conditions, such as multiple sclerosis, using an estrogen receptor-β ligand (ERβ ligand).

First claim

The invention claimed is:

1. A compound of represented by Formula (I):

or a pharmaceutically acceptable salt thereof, wherein
R 1 and R 2 are each independently —C(O)—R 3 ; and
each R 3 is independently selected from alkyl, alkoxy, alkoxyalkyl, aryloxyalkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heterocyclyl, heterocyclylalkyl, heteroaryl, and heteroarylalkyl.

2. The compound of claim 1 , wherein R 3 is selected from alkyl, aryl, alkoxyalkyl, and aralkyl.

3. The compound of claim 1 , wherein R 3 is alkyl.

4. The compound of claim 1 , wherein R 3 is selected from methyl, ethyl, isopropyl, t-butyl, phenyl and benzyl.

5. The compound of claim 1 , wherein R 3 is alkoxyalkyl.

6. The compound of claim 1 , wherein each R 3 is selected from alkyl, aryl, alkoxyalkyl, and aralkyl.

7. The compound of claim 1 , wherein each R 3 is alkyl.

8. The compound of claim 1 , wherein each R 3 is selected from methyl, ethyl, isopropyl, t-butyl, phenyl and benzyl.

9. The compound of claim 1 , wherein each R 3 is alkoxyalkyl.

10. The compound of claim 1 , wherein the carbon bearing the CN substituent is in the R-configuration.

11. The compound of claim 1 , wherein the carbon bearing the CN substituent is in the S-configuration.

12. The compound of claim 7 , wherein the carbon bearing the CN substituent is in the R-configuration.

13. The compound of claim 7 , wherein the carbon bearing the CN substituent is in the S-configuration.

14. The compound of claim 9 , wherein the carbon bearing the CN substituent is in the R-configuration.

15. The compound of claim 9 , wherein the carbon bearing the CN substituent is in the S-configuration.

16. The compound of claim 1 , wherein the compound is selected from:

or
a pharmaceutically acceptable salt thereof.

17. The compound of claim 1 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

Assignees

• Univ California

Inventors

• Jung Michael E
• Voskuhl Rhonda R

Classifications

• A61K45/06

  Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · CPC title

• A61P25/28

  for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia · CPC title

• A61K31/277 Primary

  having a ring, e.g. verapamil · CPC title

• A61P25/14

  for treating abnormal movements, e.g. chorea, dyskinesia · CPC title

• A61P25/16

  Anti-Parkinson drugs · CPC title