Cereblon-Binding Piperidine Diones for Lower-Toxicity AR Treatment

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Solution Overview

Problem

There is a significant need for safe and effective methods to treat androgen receptor (AR) mediated diseases, particularly those that are refractory to standard treatments such as surgery, radiation therapy, chemotherapy, and hormonal therapy, while minimizing toxicities and side effects.

Innovation Solution

Development of compounds with formula I and their pharmaceutically acceptable salts, tautomers, or stereoisomers for treating or preventing AR mediated diseases, administered with suitable carriers or vehicles for oral, parenteral, mucosal, transdermal, or topical delivery.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional therapies (surgery, radiation therapy, chemotherapy, hormonal therapy) are used to treat androgen receptor mediated diseases, then therapeutic effect is achieved, but toxicity and side effects increase

Engineering Contradiction:
Improvetherapeutic effectVSAvoidtoxicity and side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent employs parameter changes by developing novel chemical compounds with specific molecular structures (formula I) that differ from conventional therapies. These compounds are designed to selectively target androgen receptor signaling pathways, changing the chemical and biological parameters of treatment to achieve therapeutic effects with reduced toxicity and side effects compared to standard treatments

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent introduces intermediary compounds that act as selective modulators of androgen receptor signaling. These compounds serve as intermediaries between the treatment goal and the biological system, providing a more selective mechanism of action that spares healthy tissues from the harmful effects of conventional therapies while maintaining therapeutic efficacy

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If standard treatments are used for castration-resistant prostate cancer, then initial response is achieved, but disease progression occurs

Engineering Contradiction:
Improveinitial responseVSAvoiddisease progression time
Core Design Contradiction:
ReliabilityVSDuration of action of stationary object

Solution Approach 1:

The patent applies preliminary action by developing compounds that can be used in combination with or after standard androgen deprivation therapy. These novel compounds are designed to address resistance mechanisms that develop during standard treatment, providing a pre-planned subsequent therapeutic strategy to extend disease control beyond the initial response period

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent employs dynamics by creating a flexible treatment approach where the novel compounds can be adapted for use at different stages of disease progression. The compounds are designed to dynamically address evolving resistance mechanisms, allowing the treatment strategy to evolve with the disease rather than remaining static

Inventive Principle:
Principle #15Dynamics

Data Source

PatentEP4171568B1Cereblon binding compounds, compositions thereof, and methods of treatment therewith
Publication Date: 2025.08.27 CELGENE CORP
  • EP4171568B1 patent drawing
  • EP4171568B1 patent drawing
  • EP4171568B1 patent drawing

AI summary

Provided herein are piperidine dione compounds having the following structure: (I) wherein R1, R2, R3, R4, L,V, X, a and m are as defined herein, compositions comprising an effective amount of a piperidine dione compound, and methods for treating or preventing an androgen receptor mediated disease.