NR2B-Selective NMDA Antagonists for Core ASD and OCD Symptoms

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Solution Overview

Problem

Current therapeutic strategies for autism spectrum disorders (ASDs), obsessive-compulsive disorder (OCD), and anxiety disorders are inadequate, with existing drugs displaying mixed results and significant side effects, failing to address the underlying causes and effectively alleviate behavioral and psychological symptoms.

Innovation Solution

The use of NR2B subunit-selective N-methyl-D-aspartate (NMDA) receptor antagonists, such as compounds of formula IA and IB, to treat ASDs, OCD, and anxiety disorders, targeting the underlying neuronal circuit abnormalities associated with these conditions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current psychopharmacological agents are used to treat ASDs, then specific psychiatric or behavioral symptoms are addressed, but mixed results are obtained and significant side effects occur

Engineering Contradiction:
Improvetreatment efficacyVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent changes the pharmacological parameter from serotonin/dopamine system modulation to NMDA receptor antagonism, specifically targeting the NR2B subunit. This parameter change in mechanism of action provides reliable treatment efficacy for core ASD symptoms while minimizing side effects associated with traditional psychopharmacological agents

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent introduces NMDA receptor antagonists as an intermediary substance that modulates glutamatergic transmission in the corticostriatal circuit. This intermediary acts on the underlying neuronal circuit abnormalities rather than directly suppressing symptoms, providing reliable treatment with better safety profile

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If existing therapeutic strategies are used, then severe behavioral problems are targeted, but the underlying causes are not addressed and results are mixed

Engineering Contradiction:
Improvetreatment consistencyVSAvoidunderlying cause understanding
Core Design Contradiction:
ReliabilityVSLoss of information

Solution Approach 1:

The patent applies preliminary action by targeting the underlying neuronal circuit abnormalities in the corticostriatal pathway before behavioral symptoms manifest. By modulating NMDA receptor function early in the pathophysiological cascade, the treatment addresses root causes rather than just symptoms, providing consistent therapeutic results

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent extracts the treatment focus from superficial behavioral symptoms to the underlying neuronal circuit dysfunction. By isolating and targeting the specific NMDA receptor-mediated mechanisms in corticostriatal circuits, the invention addresses the root cause while filtering out ineffective symptomatic treatments

Inventive Principle:
Principle #2Taking out (Extraction)

3Adaptability or versatility

If traditional psychopharmacological agents are administered, then various psychiatric symptoms are addressed, but no accepted rational therapeutic regimen exists for addressing autism or its causes

Engineering Contradiction:
Improvetreatment coverageVSAvoidtherapeutic regimen structure
Core Design Contradiction:
Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The patent applies universality by using a single class of agents (NMDA receptor antagonists) to treat multiple manifestations of ASD, including repetitive behaviors, social deficits, and anxiety. This multi-functional approach simplifies the therapeutic regimen while maintaining broad treatment coverage across diverse ASD symptoms

Inventive Principle:
Principle #6Universality (Multi-functionality)

Solution Approach 2:

The patent segments the complex therapeutic need into a specific targetable mechanism: NMDA receptor-mediated glutamatergic transmission in corticostriatal circuits. By dividing the treatment approach into this specific neurobiological pathway, the invention creates a rational, structured regimen that addresses the complexity of ASD through targeted intervention

Inventive Principle:
Principle #1Segmentation

Data Source

PatentUS12527799B2Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders
Publication Date: 2026.01.20 RUGEN HLDG CAYMAN
  • US12527799B2 patent drawing
  • US12527799B2 patent drawing
  • US12527799B2 patent drawing

AI summary

Disclosed are methods for treating NMDA receptor-mediated disorders by administering certain NR2B subunit-selective NMDA (N methyl-D aspartate) antagonists. NMDA receptor-mediated disorders include autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders.