Quinoline Derivatives for Selective Protein Kinase Inhibition

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Solution Overview

Problem

Current protein kinase inhibitors face challenges such as side effects, limited efficacy, and the emergence of resistance, as well as compliance issues in treating diseases associated with kinase signaling pathway dysregulation.

Innovation Solution

Development of a compound (C) or its N-oxide, pharmaceutically acceptable salt, solvate, or stereoisomer, which serves as a potent inhibitor targeting specific protein kinases to treat a range of diseases, including cancer, metabolic disorders, inflammatory and autoimmune disorders, neurological disorders, cardiovascular diseases, and others, while minimizing side effects and resistance.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current protein kinase inhibitors are used to treat diseases associated with kinase signaling pathway dysregulation, then therapeutic efficacy is achieved, but side effects and resistance development occur

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoidside effects

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by designing the inhibitor molecule with specific functional groups and structural features that enable selective binding to the target protein kinase. The compound structure includes specific substituents (R1-R6, R11-R22) that can be optimized to enhance selectivity for the target kinase while minimizing off-target effects, thereby reducing side effects while maintaining therapeutic efficacy

Inventive Principle:

Principle #3Local quality

Solution Approach 2:

The patent employs parameter changes by systematically varying the chemical structure parameters of the inhibitor compound (including different substituents, ring structures, and molecular weight) to optimize the balance between efficacy and side effect profile. The invention describes multiple compounds with varying structures that can be selected or optimized based on the desired therapeutic window

Inventive Principle:

Principle #35Parameter changes

2Reliability

If current protein kinase inhibitors are used to treat diseases associated with kinase signaling pathway dysregulation, then therapeutic efficacy is achieved, but resistance emerges

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoidresistance development

Core Design Contradiction:

ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent addresses resistance development by providing a series of compounds with varying chemical parameters and structural features. This structural diversity allows for the selection of inhibitors that can overcome resistance mechanisms, and the invention describes how different substituents and molecular configurations can be used to maintain efficacy against resistant kinase variants

Inventive Principle:

Principle #35Parameter changes

3Reliability

If current protein kinase inhibitors are used to treat diseases associated with kinase signaling pathway dysregulation, then disease treatment is achieved, but compliance issues arise

Engineering Contradiction:

Improvedisease treatmentVSAvoidcompliance

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The patent addresses compliance issues by optimizing the pharmacological parameters of the inhibitor compounds, including potency, selectivity, and pharmacokinetic properties. The invention describes compounds designed to achieve effective inhibition at appropriate dosages with favorable safety profiles, which are critical factors for patient compliance in long-term therapy

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentEP4010330B1Quinoline derivatives as protein kinase inhibitors

Publication Date: 2025.10.01 HIRUNDO BIOSCIENCES

AI summary

The present invention relates to a compound suitable for use as a kinase inhibitor