Benzothiophene derivatives as estrogen receptor inhibitors
By developing a compound that binds the estrogen receptor and E3 ubiquitin ligase, the selective degradation of the estrogen receptor is achieved, solving the problem that existing anti-estrogen drugs cannot completely block estrogen-mediated activity, and provides Effective treatment options for estrogen receptor-mediated diseases such as breast cancer.
Patent Information
- Application Number
- CN201480046846.7
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Priority Date
- 2013-07-03
- Filing Date
- 2014-07-01
- Publication Date
- 2016-03-30
- Estimated Expiration
- Not applicable · inactive patent
AI Technical Summary
Existing antiestrogen drugs have partial agonistic effects when blocking estrogen receptors, cannot completely inhibit estrogen-mediated activity, and lack selectivity and pure degradation effects, making it difficult to effectively treat estrogen receptor-mediated diseases. Diseases such as breast cancer.
A compound, formula (I), was developed. This compound can bind to the estrogen receptor and E3 ubiquitin ligase and promote the proteinization and degradation of the estrogen receptor. The specific structure is R1 is OH, OC1-3 alkyl, Halogen, R2 is OH, OC1-3 alkyl , 5-yl or its derivatives, used as selective degraders of estrogen receptors.
The compound is capable of effectively degrading estrogen receptors, providing a purer and selective blocking effect, and is potentially useful in the treatment of estrogen receptor-mediated diseases and conditions, particularly breast cancer.