CB2 Receptor Modulators for Selective Anti-Inflammatory Therapy

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Solution Overview

Problem

Current therapeutic applications of cannabinoids are limited by their psychoactive effects, and there is a need for compounds that can selectively modulate the CB2 receptor to treat inflammation and pain without affecting the central nervous system.

Innovation Solution

Development of novel compounds that bind to and modulate the CB2 receptor, specifically designed to administer therapeutic amounts for treating inflammation and pain, with a focus on pharmaceutical compositions and methods for their use.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If cannabinoids are used for therapeutic applications, then anti-inflammatory and analgesic effects are achieved, but psychoactive side effects occur

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidpsychoactive effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent segments the cannabinoid receptor system into two distinct targets: CB1 receptors in the central nervous system and CB2 receptors in the immune system. By designing compounds that selectively target only CB2 receptors, the therapy achieves anti-inflammatory and analgesic effects without activating CB1 receptors, thereby eliminating psychoactive side effects.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention creates compounds with localized specificity for CB2 receptors expressed in immune cells and peripheral tissues. This local quality ensures that therapeutic action is confined to immune-mediated processes while leaving central nervous system functions unaffected, thus providing targeted therapy without systemic psychoactive effects.

Inventive Principle:
Principle #3Local quality

2Adaptability or versatility

If CB1 and CB2 receptors are both activated, then broad therapeutic effects are achieved, but central nervous system side effects occur

Engineering Contradiction:
Improvetherapeutic rangeVSAvoidcentral nervous system effects
Core Design Contradiction:
Adaptability or versatilityVSObject-affected harmful factors

Solution Approach 1:

The patent extracts the CB2 receptor-specific therapeutic function from the broader cannabinoid receptor system. By isolating and targeting only the CB2 receptor pathway, the invention removes the unwanted central nervous system effects associated with CB1 activation while preserving the beneficial anti-inflammatory and analgesic properties.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The invention introduces CB2-selective compounds as intermediaries that mediate therapeutic effects through immune system modulation without bridging to central nervous system effects. These compounds act as selective mediators that translate CB2 receptor activation into anti-inflammatory and analgesic outcomes while blocking the pathway to psychoactive effects.

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentUS9315454B2Compounds which modulate the CB2 receptor
Publication Date: 2016.04.19 BOEHRINGER INGELHEIM INT GMBH
  • US9315454B2 patent drawing
  • US9315454B2 patent drawing
  • US9315454B2 patent drawing

AI summary

Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.