Marine Macrocyclic Lactam Anti-Inflammatory Compound

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Solution Overview

Problem

Existing anti-inflammatory drugs have a single structure, which limits their effectiveness and can lead to side effects such as drug dependence and compromised adrenocortical function.

Innovation Solution

A polar marine-derived macrocyclic lactam compound with a novel structure, represented by formula 1 or its pharmaceutically acceptable salt, is developed. This compound is isolated from the fermentation culture of Streptomyces somaliensis and has good inflammation inhibitory activity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If glucocorticoid anti-inflammatory drugs are used, then anti-inflammatory efficacy is improved, but side effects and drug dependence increase

Engineering Contradiction:

Improveanti-inflammatory efficacyVSAvoidside effects and drug dependence

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the chemical structure parameters by introducing a novel macrocyclic lactam framework with specific functional groups (carboxylic acid, hydroxyl, amino) and stereochemical configurations, creating a new class of anti-inflammatory compounds that differ fundamentally from traditional glucocorticoids and NSAIDs

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The compound combines multiple functional groups (carboxylic acid at C1, hydroxyl at C2, amino at C3) within a single macrocyclic lactam structure, creating a multi-functional molecule that may simultaneously provide anti-inflammatory activity while avoiding the harmful effects of single-class drugs

Inventive Principle:

Principle #40Composite materials

2Object-affected harmful factors

If non-steroidal anti-inflammatory drugs are developed, then side effects are reduced, but structural diversity remains limited

Engineering Contradiction:

Improveside effectsVSAvoidstructural diversity

Core Design Contradiction:

Object-affected harmful factorsVSAdaptability or versatility

Solution Approach 1:

The macrocyclic lactam structure is divided into distinct functional segments: a carboxylic acid group at C1, a hydroxyl group at C2, an amino group at C3, and various substitutable R groups (R1-R4, R5-R10) that can be independently modified to create structural diversity

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The patent provides multiple embodiments with variable substituents at different positions (R1-R10 can be hydrogen, hydroxyl, amino, cyano, halogen, or various carbon chains), allowing the structure to be dynamically adjusted to optimize both activity and diversity

Inventive Principle:

Principle #15Dynamics

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The compound demonstrates significant inflammation inhibitory activity, providing a new candidate for developing anti-inflammatory drugs with potentially fewer side effects.

Implementation Method 1

isolating the compound from the fermentation culture of Streptomyces somaliensis

Methodology Applied

Scientific EffectFermentation: Fermentation

Data Source

PatentUS20250114326A1Polar marine-derived macrocyclic lactam compound, and preparation method therefor and use thereof

Publication Date: 2025.04.10 RENJI HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE

AI summary

Provided in the present invention are a polar marine-derived macrocyclic lactam compound, and a preparation method therefor and the use thereof. Provided in the present invention is a macrocyclic lactam compound as represented by formula 1 or a pharmaceutically acceptable salt thereof. The compound has a novel structure and good inflammation inhibitory activity, and provides a new candidate compound for developing an anti-inflammatory drug.