Anatabine Glutarate Crystal Forms for NFKB and STAT3 Inhibition

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Solution Overview

Problem

There is a need for agents that can reduce inappropriate levels of inflammation and treat disorders associated with NFKB-mediated and STAT3-mediated inflammatory components, as well as substance addiction, as existing treatments are inadequate.

Innovation Solution

The use of 3-(1,2,3,6-tetrahydropyridin-2-yl)pyridine glutarate (anatabine glutarate) or its pharmaceutically acceptable solvates, crystals, and polymorphs, which have MAO inhibitory and STAT3 phosphorylation inhibition effects, to treat inflammation and addiction by administering them in extended release formulations or bottled water products, and in combination with other therapies.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing treatments are used for inflammation, then treatment is provided, but the treatments are inadequate and cannot effectively reduce inappropriate levels of inflammation

Engineering Contradiction:

Improveeffectiveness of inflammation treatmentVSAvoidability to treat NFKB-mediated and STAT3-mediated inflammatory components

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure to create anatabine glutarate, a salt form of anatabine with glutaric acid. This chemical parameter change enhances the compound's ability to inhibit NFKB and STAT3 pathways, providing more effective and targeted anti-inflammatory treatment compared to existing therapies.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent employs composite materials by forming a salt complex between anatabine and glutaric acid. This composite structure combines the pharmacological properties of anatabine with the characteristics of glutaric acid, resulting in a compound with improved stability, solubility, and targeted inhibition of inflammatory pathways including NFKB and STAT3.

Inventive Principle:

Principle #40Composite materials

2Duration of action of moving object

If anatabine glutarate is administered to reduce inflammation, then NFKB and STAT3 pathways are inhibited, but extended release formulations and combination therapies are required for optimal effect

Engineering Contradiction:

Improveduration of anti-inflammatory effectVSAvoidcomplexity of formulation and administration regimen

Core Design Contradiction:

Duration of action of moving objectVSDevice complexity

Solution Approach 1:

The patent applies preliminary action by using extended release formulations that are prepared in advance to provide sustained delivery of anatabine glutarate. This preliminary formulation approach ensures prolonged inhibition of NFKB and STAT3 pathways without requiring frequent dosing, thereby extending the duration of anti-inflammatory effect while managing administration complexity.

Inventive Principle:

Principle #10Preliminary action

Solution Approach 2:

The patent demonstrates universality by developing anatabine glutarate as a multi-functional therapeutic agent that can be used in various formulations (extended release, bottled water products) and in combination with other therapies. This universal approach allows the same active compound to address different inflammatory conditions through NFKB and STAT3 inhibition while adapting to different administration needs.

Inventive Principle:

Principle #6Universality (Multi-functionality)

3Reliability

If high doses of anti-inflammatory agents are used, then inflammation is reduced, but toxicity increases

Engineering Contradiction:

Improveeffectiveness of inflammation reductionVSAvoidtoxicity of treatment

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies the intermediary principle by using anatabine glutarate as a mediator compound that selectively targets and inhibits NFKB and STAT3 pathways. This intermediary approach allows for effective inflammation reduction at lower doses compared to conventional anti-inflammatory agents, thereby minimizing toxicity while maintaining therapeutic efficacy through pathway-specific inhibition.

Inventive Principle:

Principle #24Intermediary (Mediator)

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

Anatabine glutarate effectively reduces inflammation and addiction symptoms by inhibiting NFKB and STAT3 pathways, providing a broad range of therapeutic utilities and minimizing toxicity.

Implementation Method 1

The claimed compound, crystal, polymorph and/or pharmaceutical composition can have a monoamine oxidase (MAO) inhibitory effect.

Methodology Applied

Scientific EffectMAO inhibition: Enzyme

Implementation Method 2

the compound, crystal, polymorph and/or pharmaceutical composition of the invention may have a STAT3 phosphorylation inhibition effect.

Methodology Applied

Scientific EffectSTAT3 phosphorylation inhibition:

Data Source

PatentUS20250243178A13-(1,2,3,6-tetrahydropyridin-2-yl) pyridine glutarate or a pharmaceutically acceptable solvate thereof

Publication Date: 2025.07.31 PHILIP MORRIS PRODUCTS SA

AI summary

The present invention relates to 3-(1,2,3,6-tetrahydropyridin-2-yl)pyridine glutarate or a pharmaceutically acceptable solvate thereof, to a crystal thereof and to a polymorph of this crystal. It further relates to the medicinal use of each of these, in particular in the treatment or prophylaxis of substance addiction or inflammation