7-Azaindazole Compounds Inhibit Wnt Pathway Signaling

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Solution Overview

Problem

Current treatments for disorders associated with aberrant Wnt signaling, such as cancer and other diseases, lack effective inhibitors to modulate cellular events and correct genetic disorders caused by mutations in Wnt signaling components.

Innovation Solution

Development of 7-azaindazole compounds and their salts or analogs as Wnt pathway inhibitors, which can be used to antagonize Wnt activity and treat diseases by reversing aberrant growth states or correcting genetic disorders.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments are used for disorders associated with aberrant Wnt signaling, then existing therapeutic options are limited, but effective inhibition of Wnt pathway activity is not achieved

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoidavailability of treatment options
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent employs parameter changes by modifying the chemical structure of Wnt inhibitors through the 7-azaindazole core with various substituents (R1-R6 groups). This structural parameter modification enables the compounds to effectively antagonize Wnt pathway activity, thereby achieving reliable therapeutic effectiveness for disorders caused by aberrant Wnt signaling

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent segments the Wnt pathway inhibition problem into specific molecular targets and addresses them with designed compounds. The 7-azaindazole core structure with variable substituents allows targeted inhibition of Wnt pathway components, providing effective treatment options for specific disorders while maintaining versatility across different Wnt-related conditions

Inventive Principle:
Principle #1Segmentation

2Reliability

If 7-azaindazole compounds are developed as Wnt pathway inhibitors, then effective inhibition of Wnt activity is achieved, but the complexity of drug development increases

Engineering Contradiction:
ImproveWnt pathway inhibition efficacyVSAvoidcompound structure complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent uses parameter changes by systematically varying substituents (R1-R6) on the 7-azaindazole core to optimize Wnt pathway inhibition efficacy. This structured approach to modifying chemical parameters enables effective inhibition while managing compound complexity through rational design

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The 7-azaindazole core structure serves as a universal scaffold that can accommodate multiple substituent patterns (R1-R6 groups) to address different aspects of Wnt pathway inhibition. This multi-functional design allows a single core structure to provide effective inhibition across various Wnt-related disorders without requiring entirely different molecular frameworks

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

Data Source

PatentUS10285983B23-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[3,4-B] pyridines and therapeutic uses thereof
Publication Date: 2019.05.14 BIOSPLICE THERAPEUTICS INC
  • US10285983B2 patent drawing
  • US10285983B2 patent drawing
  • US10285983B2 patent drawing

AI summary

7-Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a 7-azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.