C-Kit Kinase Inhibitor Compounds for Autoimmune Disease Treatment

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Solution Overview

Problem

Current compounds that inhibit KIT, CSF1R, and PDGFR kinases are not approved for treating autoimmune diseases or disorders involving abnormal activation of these kinases.

Innovation Solution

A compound of Formula (I) or its pharmaceutically acceptable salt, which inhibits KIT, CSF1R, and PDGFR kinases, is developed to address the abnormal activation of these kinases in various diseases.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current compounds that inhibit KIT, CSF1R, and PDGFR kinases are used, then kinase inhibition activity is achieved, but approval for treating autoimmune diseases is not obtained

Engineering Contradiction:
Improvetherapeutic efficacy for autoimmune diseasesVSAvoidindication approval scope
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent modifies the chemical structure of existing kinase inhibitors by introducing specific substituent groups (R1, R2, R3, R4, R5, R9) and structural variations (m, n values) to optimize the compound's properties for autoimmune disease treatment, thereby expanding its therapeutic indication scope while maintaining kinase inhibition activity

Inventive Principle:
Principle #35Parameter changes

2Reliability

If existing kinase inhibitors are developed, then cancer treatment approval is achieved, but autoimmune disease treatment approval is not achieved

Engineering Contradiction:
Improvecancer treatment efficacyVSAvoiddisease indication scope
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent designs kinase inhibitors with broad-spectrum activity targeting multiple kinase families (KIT, CSF1R, PDGFR) to enable single compounds to treat multiple disease types including both cancer and autoimmune diseases, thereby expanding the versatility and indication scope of the therapeutic agents

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

Data Source

PatentUS20250034138A1Compounds and Compositions as C-Kit Kinase Inhibitors
Publication Date: 2025.01.30 ENANTA PHARM INC
  • US20250034138A1 patent drawing
  • US20250034138A1 patent drawing
  • US20250034138A1 patent drawing

AI summary

The invention provides compounds of formula (I), or pharmaceutically acceptable salts and pharmaceutical compositions thereof,which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit, CSF1R and PDGFR (PDGFRα, PDGFRβ) kinases.