Anti-inflammatory coupling compound drug, and preparation method therefor and use thereof

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Solution Overview

Problem

Existing JAK inhibitors require high doses or have side effects and lack effective skin-selective administration, leading to systemic toxicity.

Innovation Solution

Optimize the structure of known JAK inhibitors by coupling them with specific linkers and small molecules to enhance transdermal penetration and stability, allowing controlled release of active ingredients.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If JAK inhibitors are administered systemically to achieve therapeutic effect, then efficacy is improved, but systemic side effects and toxicity increase

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoidsystemic side effects

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent divides the drug delivery system into two parts: a JAK inhibitor active ingredient and a polymer carrier. The polymer carrier enables localized delivery to skin tissues, segmenting the distribution pattern from systemic to targeted, thereby maintaining efficacy while reducing systemic exposure and side effects

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The polymer carrier acts as an intermediary between the JAK inhibitor and the body's distribution system. This intermediary enables controlled transdermal penetration and localized release at the target site, preventing direct systemic circulation and associated toxicity

Inventive Principle:

Principle #24Intermediary (Mediator)

2Reliability

If high doses of JAK inhibitors are used to overcome resistance or achieve sufficient effect, then therapeutic efficacy is improved, but systemic toxicity increases

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoidsystemic toxicity

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by concentrating the drug delivery at the specific target site (skin tissues) rather than distributing uniformly throughout the body. The polymer carrier facilitates localized accumulation of the JAK inhibitor at therapeutic concentrations where needed, while maintaining lower systemic concentrations to reduce toxicity

Inventive Principle:

Principle #3Local quality

3Speed

If transdermal penetration is enhanced by adding nonfunctional groups to increase compound size, then transdermal potential is improved, but compound stability and controlled release may be compromised

Engineering Contradiction:

Improvetransdermal penetration rateVSAvoidcompound stability

Core Design Contradiction:

SpeedVSStability of the object's composition

Solution Approach 1:

The patent creates a composite material system combining the JAK inhibitor with a polymer carrier. This composite approach allows the small molecule drug to benefit from the polymer's properties including stability, controlled release characteristics, and enhanced transdermal penetration capabilities without modifying the drug's active structure

Inventive Principle:

Principle #40Composite materials

Solution Approach 2:

The JAK inhibitor is nested within or associated with the polymer carrier structure. This nesting arrangement allows the polymer to provide protective and functional properties (stability, controlled release, penetration enhancement) while the core active ingredient maintains its molecular characteristics for biological activity

Inventive Principle:

Principle #7Nested doll (Nesting)

Data Source

PatentUS20250241922A1Anti-inflammatory coupling compound drug, and preparation method therefor and use thereof

Publication Date: 2025.07.31 COVAL BIOPHARMA (SHANGHAI) CO LTD

AI summary

An anti-inflammatory drug compound, and a preparation method therefor and the use thereof. The structural formula of the compound is A-Y—B, wherein A is a group after dehydrogenation of an amine compound having JAK inhibitory activity, Y is a direct connection or —(CH2)-O— or, and B is a group formed by means of dehydroxylation of a carboxy-containing carboxylic acid compound B1, or a group formed by means of dehydrogenation of a hydroxy-containing compound B2. The compound has the special effects of having a strong transdermal property, controlled drug release, high efficacy, etc.