Polycyclic Androgen Receptor Modulators for Prostate Cancer
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Solution Overview
Problem
There is a need for compounds that modulate androgen receptor activity, particularly anti-androgen properties, to treat androgen-dependent conditions such as prostate cancer, which are not adequately addressed by existing treatments.
Innovation Solution
Development of polycyclic compounds, including tetracyclic steroidal compounds with specific alkyl substitutions and bridges, that act as androgen receptor antagonists, potentially offering therapeutic benefits for conditions like prostate cancer and benign prostatic hyperplasia.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing anti-androgen treatments are used, then androgen receptor activity is inhibited, but therapeutic efficacy for prostate cancer and BPH is insufficient
Solution Approach 1:
The patent modifies the chemical structure of anti-androgen compounds by changing parameters such as the steroid core structure, substituent groups at specific positions (e.g., C6, C9, C11, C12), and molecular configuration to create a series of novel compounds with potentially improved therapeutic efficacy and selectivity for androgen-dependent conditions
Solution Approach 2:
The invention develops composite chemical structures combining modified steroid cores with various functional groups and substituent patterns, creating new molecular entities that may offer enhanced binding affinity and selectivity for the androgen receptor compared to existing single-structure agents
2Reliability
If new polycyclic compounds are developed, then androgen receptor modulation is improved, but structural complexity increases
Solution Approach 1:
The patent systematically divides the molecular structure into distinct segments (steroid core, substituent groups at specific positions, bridge structures) that can be independently modified, allowing for structured exploration of structure-activity relationships while maintaining overall molecular framework consistency
Solution Approach 2:
The invention applies local modifications to specific regions of the steroid core (e.g., substituting groups at C6, C9, C11, C12 positions) rather than changing the entire molecular structure, enabling targeted optimization of androgen receptor binding while controlling overall complexity
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
These compounds effectively inhibit androgen receptor activity, providing a potential therapeutic approach for treating androgen-dependent conditions, including prostate cancer and BPH, by administering them orally or in combination with other therapeutic agents.
Implementation Method 1
The AR is activated by androgen binding, which exposes the nuclear localization signal (NLS) thereby initiating translocation of the complex into the nucleus to exert transcriptional activity.
Data Source
AI summary
The present disclosure relates to polycyclic (e.g., tetracyclic) androgen receptor (AR) modulators, synthetic methods for preparing such AR modulators, and methods of using such AR modulators to treat an androgen-dependent condition, such as prostate cancer or BPH. Exemplary compounds have quaternary centers at C10 and C13 and a fused cyclic ring comprising C14 and C15.