CB2 Receptor Modulators for Antitumor Immune Response

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Solution Overview

Problem

Current treatments for cancer, particularly those involving the cannabinoid receptor CB2, face challenges in enhancing antitumor immune responses due to immunosuppressive effects caused by endocannabinoids, leading to impaired T, NK, and B cell function.

Innovation Solution

Development of CB2 receptor modulators, including antagonists and inverse agonists, represented by specific compounds of Formula (I) and Formula (X), which modulate CB2 receptor activity to restore immune function and enhance antitumor responses.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Object-affected harmful factors

If endocannabinoids are present to modulate immune responses, then anti-inflammatory effects are achieved, but immunosuppression occurs that impairs T, NK, and B cell function

Engineering Contradiction:
ImproveinflammationVSAvoidimmune function
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent extracts and isolates the harmful immunosuppressive effect from the beneficial anti-inflammatory effect by selectively blocking CB2 receptors. This allows the immune system to maintain anti-inflammatory responses while preventing the suppression of T, NK, and B cell functions that occurs through CB2-mediated pathways.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent introduces CB2 receptor antagonists as intermediary substances that mediate between endocannabinoids and immune cells. These antagonists selectively interfere with the immunosuppressive signaling pathway while permitting other immune regulatory mechanisms to function normally, thus resolving the contradiction between inflammation control and immune responsiveness.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Object-affected harmful factors

If CB2 receptor activity is enhanced to reduce inflammation, then anti-inflammatory response is improved, but antitumor immune response is suppressed

Engineering Contradiction:
ImproveinflammationVSAvoidimmunosuppression in tumor microenvironment
Core Design Contradiction:
Object-affected harmful factorsVSObject-generated harmful factors

Solution Approach 1:

The patent applies inversion by switching from CB2 receptor agonists (which enhance anti-inflammatory effects but suppress immunity) to CB2 receptor antagonists. This inverse approach blocks the immunosuppressive signaling in the tumor microenvironment while still allowing control of inflammation through alternative pathways, thereby converting the harmful effect into a beneficial one for cancer therapy.

Inventive Principle:
Principle #13The other way round (Inversion)

Solution Approach 2:

The patent applies local quality by developing antagonists that specifically target CB2 receptors in the tumor microenvironment and immune cells, rather than systemically suppressing all CB2-mediated effects. This localized blockade preserves anti-inflammatory responses in non-tumor tissues while eliminating immunosuppression where it matters most for cancer treatment.

Inventive Principle:
Principle #3Local quality

3Reliability

If conventional cancer treatments are used, then tumor growth is controlled, but antitumor immune response is not enhanced due to CB2-mediated immunosuppression

Engineering Contradiction:
Improvetumor controlVSAvoidantitumor immune response
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent merges conventional cancer therapies with CB2 receptor antagonism into a combined treatment approach. By integrating the tumor control effects of conventional treatments with the immune-enhancing effects of CB2 blockade, the synergistic combination achieves both reliable tumor control and enhanced antitumor immune response, overcoming the limitations of either approach alone.

Inventive Principle:
Principle #5Merging (Combining)

Data Source

PatentUS20240252504A1Cannabinoid receptor type 2 (CB2) modulators and uses thereof
Publication Date: 2024.08.01 TEON THERAPEUTICS INC
  • US20240252504A1 patent drawing
  • US20240252504A1 patent drawing
  • US20240252504A1 patent drawing

AI summary

Disclosed herein are compounds, compositions, and methods for modulating the Cannabinoid receptor 2 (CB2) with the compounds and compositions disclosed herein. Also described are methods of treating diseases or conditions that are mediated by the action of Cannabinoid receptor 2 (CB2) or that we benefit from modulating the Cannabinoid receptor 2 (CB2).