Azetidine Estrogen Receptor Modulators for Resistance
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Solution Overview
Problem
Current treatments for estrogen-sensitive and estrogen receptor-mediated diseases, such as breast cancer and other cancers, often face challenges with resistance and limited therapeutic options, particularly in metastatic disease and hormone-dependent cancers.
Innovation Solution
Development of compounds that act as estrogen receptor degraders or antagonists with minimal agonist activity, specifically targeting estrogen receptor alpha (ER-α) to reduce ER activation and concentrations, thereby offering improved therapeutic activity, including complete or longer-lasting tumor regression and reduced resistance.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current treatments for estrogen-sensitive diseases are used, then therapeutic effects are achieved, but resistance develops and therapeutic options are limited
Solution Approach 1:
The patent changes the molecular structure parameters of estrogen receptor modulators by introducing azetidine rings at positions 1, 3, or 7 of the steroid core, creating novel compounds with improved therapeutic profiles that overcome resistance to conventional treatments
Solution Approach 2:
The patent combines the azetidine functional group with the steroid estrogen structure to create composite molecules that exhibit both estrogen receptor modulatory activity and enhanced therapeutic durability, preventing resistance development
2Reliability
If estrogen receptor modulators are used to treat cancer, then tumor regression is achieved, but tumor invasiveness may increase
Solution Approach 1:
The patent introduces azetidine rings at specific local positions (1, 3, or 7) of the steroid molecule to create localized structural modifications that selectively enhance anti-tumor activity while suppressing harmful invasive effects through precise spatial control of molecular interactions
Data Source
AI summary
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.