Aryl Pyridine Compounds Modulating Protein Kinase Activity

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Solution Overview

Problem

Current methods for modulating protein kinase activity are ineffective in treating a wide range of diseases, including non-life-threatening conditions and virulent cancers, highlighting a need for more effective compounds and treatment approaches.

Innovation Solution

Development of aryl pyridine compounds and their pharmaceutically acceptable salts and solvates, which can be administered to patients to treat, manage, and prevent various diseases and disorders by modulating protein kinase activity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current methods for modulating protein kinase activity are used, then treatment approaches are available, but they are ineffective in treating a wide range of diseases including cancers

Engineering Contradiction:
Improveeffectiveness of treatmentVSAvoidapplicability across different diseases
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent employs parameter changes by modifying the chemical structure of protein kinase modulators through various substitutions and modifications to the core pyridine ring structure. This allows optimization of binding affinity, selectivity, and pharmacological properties to achieve effective treatment across different diseases including cancers, autoimmune disorders, and inflammatory conditions

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates universal protein kinase modulators that can treat multiple disease types. The compounds are designed to target protein kinases involved in various pathological conditions, enabling a single compound or class of compounds to address diverse diseases including cancers, autoimmune disorders, inflammatory conditions, and viral infections

Inventive Principle:
Principle #6Universality (Multi-functionality)

2Adaptability or versatility

If existing protein kinase modulators are used, then some diseases can be treated, but effective methods still do not exist for a wide range of conditions

Engineering Contradiction:
Improverange of treatable conditionsVSAvoidtherapeutic efficacy
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The patent utilizes parameter changes by systematically varying chemical parameters such as substituent groups, ring structures, and molecular weight to optimize compound efficacy. This includes modifying the pyridine ring with various heterocyclic groups, alkyl chains, and functional groups to enhance binding affinity and selectivity for specific protein kinases, thereby achieving reliable therapeutic effects across multiple disease indications

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS8153804B2Aryl pyridines and methods of their use
Publication Date: 2012.04.10 LEXICON PHARMACEUTICALS INC
  • US8153804B2 patent drawing
  • US8153804B2 patent drawing
  • US8153804B2 patent drawing

AI summary

Aryl pyridines, compositions comprising them, and methods of their use for the treatment, prevention and management of a variety of diseases and disorders are disclosed.