Fused Ring Pyrimidine Compound for Multi-Kinase Inhibition

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Solution Overview

Problem

Current therapies lack effective inhibitors for Janus kinase (JAK), FGFR kinase, FLT3 kinase, and Src family kinase, which are crucial for addressing various diseases including tumors, immune system disorders, and cardiovascular diseases.

Innovation Solution

A fused ring pyrimidine compound is developed, capable of inhibiting JAK, FGFR kinase, FLT3 kinase, and Src family kinase, offering a strong inhibitory effect on these kinases.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current therapies are used, then treatment options are limited, but effective inhibition of JAK, FGFR kinase, FLT3 kinase, and Src family kinase is not achieved

Engineering Contradiction:
Improveinhibitory effect on kinasesVSAvoidtherapeutic coverage for multiple diseases
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The fused ring pyrimidine compound is designed to simultaneously inhibit multiple kinase families (JAK, FGFR, FLT3, and Src family kinases) through a single molecular structure. This multi-target capability allows the compound to address various diseases including tumors, immune system disorders, and cardiovascular diseases, thereby achieving both strong inhibitory effect and broad therapeutic coverage without requiring multiple separate drugs

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

2Reliability

If specific kinase inhibitors are developed for each disease, then targeted treatment is improved, but drug development complexity and time increase

Engineering Contradiction:
Improvedisease treatment effectivenessVSAvoiddrug development complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The invention merges the functions of multiple disease-specific kinase inhibitors into a single fused ring pyrimidine compound. By combining inhibition capabilities for JAK, FGFR, FLT3, and Src family kinases into one molecular entity, the compound provides targeted treatment for multiple diseases simultaneously, thereby reducing drug development complexity and accelerating the availability of effective therapies

Inventive Principle:
Principle #5Merging (Combining)

Data Source

PatentUS10494378B2Fused ring pyrimidine compound, intermediate, and preparation method, composition and use thereof
Publication Date: 2019.12.03 GUANGZHOU MAXINOVEL PHARMA CO LTD
  • US10494378B2 patent drawing
  • US10494378B2 patent drawing
  • US10494378B2 patent drawing

AI summary

Disclosed area fused ring pyrimidine compound, and an intermediate, a preparation method, a composition and a use thereof. The fused ring pyrimidine compound is a compound as shown in formula I, a tautomer, an enantiomer, a diastereoisomer, a pharmaceutically acceptable salt, a metabolite, a metabolic precursor or a prodrug thereof, wherein the above-mentioned compound is used for the preparation of a medicine for preventing, remitting or treating one or more of immune system diseases, autoimmune diseases, cell proliferative diseases, allergic disorders and cardiovascular diseases, and the compound has a strong inhibitory effect on the Janues kinase, FGFR kinase, FLT3 kinase and Src family kinase.