Nicotinic Acid Derivative B Anti-Inflammatory Selectivity

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Solution Overview

Problem

Current treatments for autoimmune diseases like rheumatoid arthritis, such as those involving Tripterygium plants, face limitations in effectively managing inflammation and immune regulation, with existing compounds having toxicity and limited structural diversity for targeted therapeutic applications.

Innovation Solution

A nicotinic acid derivative B with anti-inflammatory and immunosuppressive activity is developed, characterized by a specific molecular structure, which is derived from Tripterygium plants and used in medicaments for treating rheumatoid arthritis, psoriasis, and other autoimmune diseases, exhibiting strong selectivity and clinical application value.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If Tripterygium plants are used for treating autoimmune diseases, then immunosuppressive effects are achieved, but toxicity increases

Engineering Contradiction:

Improveimmunosuppressive effectsVSAvoidtoxicity

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent extracts and isolates the active immunosuppressive components (sesquiterpene alkaloids like triptolide and tripteroid) from the Tripterygium plant material. By separating these specific active ingredients from the complex plant matrix, the invention achieves potent immunosuppressive effects while eliminating or reducing the toxicity associated with other plant constituents.

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The invention focuses on specific chemical structures and functional groups within the sesquiterpene alkaloids that are responsible for immunosuppressive activity. By identifying and optimizing these local structural features (such as the tripteroid core structure and specific substituent patterns), the patent enhances therapeutic efficacy while minimizing toxic effects through structure-activity relationship optimization.

Inventive Principle:

Principle #3Local quality

2Reliability

If existing compounds from Tripterygium plants are used, then immunosuppression is achieved, but structural diversity for targeted therapy is limited

Engineering Contradiction:

ImproveimmunosuppressionVSAvoidstructural diversity

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent systematically varies key structural parameters of the sesquiterpene alkaloid core structure, including substituent types (R1-R6 groups), positions, and configurations. This includes modifying the tripteroid skeleton with different ester groups, hydroxyl positions, and side chain variations to create a library of analogs with diversified structures that maintain immunosuppressive activity while exploring structure-activity relationships for targeted therapies.

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentUS20230373921A1Nicotinic Acid Derivative B Having Anti-Inflammatory and Immunosuppressive Activity and Use Thereof

Publication Date: 2023.11.23 CHONGQING ACAD OF CHINESE MATERIA MEDICA

AI summary

Provided in the present invention is a nicotinic acid derivative B having an anti-inflammatory and immunosuppressive activity, and the structural general formula thereof is I, wherein, R1 and R2 are different substitution sites on a main chain, and R11′, R21′, R31′, R12′, R22′, and R32′ are different substitution sites on a side chain. The nicotinic acid derivative B compound provided in the present invention has a good anti-inflammatory and anti-autoimmune disease activity, and a high selectivity.