Substituted Isoindolinones Selective Protein Modulation

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Solution Overview

Problem

Current treatments for diseases associated with protein malfunction, such as cancer and inflammatory disorders, often face challenges in selectively modulating protein activity without causing toxicity to healthy cells, and existing therapies may have significant side effects due to systemic delivery of cytokines.

Innovation Solution

Development of substituted isoindolinones that selectively modulate protein activity, including cytokines like IL-2, PDE6, and CK1α, to restore protein homeostasis with minimal toxicity to healthy cells, using compounds represented by Formula (I) and their pharmaceutical compositions for local delivery.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments are used to modulate protein activity, then therapeutic effect is achieved, but toxicity to healthy cells occurs

Engineering Contradiction:
Improvetherapeutic effectVSAvoidtoxicity to healthy cells
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by designing substituted isoindolinone compounds with specific molecular structures (Formula I) that enable selective binding to target proteins in diseased cells. The compounds achieve differential toxicity through localized molecular interactions - the core structure with specific substituents (R1-R11 groups) provides selective affinity for malfunctioning proteins in cancer or inflammatory cells while sparing healthy cells, thus achieving therapeutic effect with reduced systemic toxicity

Inventive Principle:
Principle #3Local quality

2Adaptability or versatility

If systemic delivery of cytokines is used, then therapeutic coverage is improved, but side effects increase

Engineering Contradiction:
Improvetherapeutic coverageVSAvoidside effects
Core Design Contradiction:
Adaptability or versatilityVSObject-generated harmful factors

Solution Approach 1:

The patent applies parameter changes by modifying the chemical parameters of cytokine-based therapies through substituted isoindolinone compounds. The molecular structure (Formula I) with variable substituents (R1-R11) allows tuning of pharmacokinetic and pharmacodynamic parameters to achieve targeted protein modulation. This enables broad therapeutic coverage across different diseases (cancer, inflammatory disorders, autoimmune conditions) while minimizing side effects through selective cellular targeting based on protein malfunction rather than systemic cytokine exposure

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS11352338B2Substituted isoindolinones
Publication Date: 2022.06.07 BIOTHERYX INC
  • US11352338B2 patent drawing
  • US11352338B2 patent drawing
  • US11352338B2 patent drawing

AI summary

Substituted isoindolinones of Formula (I), methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat or ameliorate diseases, disorders, or conditions associated with protein malfunction, such as cancer, are provided.