Androgen Receptor Modulators for Castration-Resistant Prostate Cancer
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Solution Overview
Problem
Current therapies for metastatic prostate cancer, particularly in the castration-resistant state, are ineffective due to biological changes that render them either ineffective or even stimulatory, and there is a need for new treatments that can address hormone-refractory prostate cancer.
Innovation Solution
Development of compounds that act as androgen receptor modulators, capable of binding to or inhibiting the androgen receptor, either as antagonists or agonists, to effectively treat both hormone-sensitive and castration-resistant prostate cancer by modulating androgen receptor activity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current anti-androgen therapies are used to treat hormone-sensitive prostate cancer, then androgen receptor activity is blocked and tumor growth is inhibited, but the therapies become ineffective or stimulatory when the cancer transitions to castration-resistant state
Solution Approach 1:
The patent applies parameter changes by developing compounds with modified chemical structures (formula I and formula II) that alter the binding characteristics and pharmacological properties of androgen receptor modulators. These structural modifications enable the compounds to maintain therapeutic effectiveness in both hormone-sensitive and castration-resistant prostate cancer states, resolving the contradiction between reliability in initial treatment and adaptability to disease progression.
2Quantity of substance
If androgen production is reduced through surgical or chemical castration, then hormone-sensitive prostate cancer growth is inhibited, but the cancer develops resistance and continues to grow in castration-resistant state
Solution Approach 1:
The patent employs the intermediary principle by introducing novel compounds (formula I and formula II) that act as mediators between the androgen receptor and the therapeutic goal of inhibiting prostate cancer growth. These compounds serve as alternative intermediaries that can effectively block androgen receptor signaling even when androgen levels are reduced or when the cancer becomes resistant to conventional anti-androgen therapies, thereby maintaining long-term therapeutic effectiveness.
3Productivity
If conventional anti-androgen drugs are administered, then initial response in hormone-sensitive cancer is positive, but the drugs may become stimulatory to castration-resistant cancer growth
Solution Approach 1:
The patent applies the inversion principle by developing compounds with reversed or modified pharmacological actions compared to conventional anti-androgen drugs. While conventional drugs may become stimulatory to castration-resistant cancer, the novel compounds (formula I and formula II) are designed to maintain inhibitory effects or provide alternative mechanisms of action that prevent the harmful stimulatory effect, effectively inverting the adverse response pattern.
Data Source
AI summary
Substituted phenylcarbamoyl alkylamino arenes; substituted phenylthiocarbamyl alkylamino arenes; substituted phenylcarbamoyl alkylamino heteroarenes; substituted phenylthiocarbamyl alkylamino heteroarenes; N-substituted aryl, N′-substituted aryl urea compounds; N-substituted aryl, N′-substituted heteroaryl urea compounds; N-substituted aryl, N′-substituted aryl thiourea compounds and N-substituted aryl, N′-substituted heteroaryl thiourea compounds are provided and may find use as androgen receptor modulators. The compounds may find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer.