Tetrazole mGluR5 Modulators for Reduced Side Effects
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
There is a need for novel compounds that therapeutically inhibit metabotropic glutamate receptor subtype 5 (mGluR5) with minimal side effects, as existing compounds may have significant adverse effects in treating psychiatric and mood disorders, pain, Parkinson's disease, and other conditions.
Innovation Solution
Development of novel tetrazole compounds substituted directly or by a bridge with a heteroaryl moiety containing N adjacent to the point of connection, and another heteroaryl or aryl ring, which act as mGluR5 modulators, providing a pharmaceutical composition for treating psychiatric and mood disorders, pain, Parkinson's disease, and other conditions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing mGluR5 modulators are used to treat psychiatric and mood disorders, then therapeutic effect is achieved, but significant adverse effects occur
Solution Approach 1:
The patent modifies the chemical structure of mGluR5 modulators by changing molecular parameters - specifically incorporating tetrazole rings with specific substituents (heteroaryl groups, aryl groups, cycloalkyl groups) at defined positions. This structural parameter change creates new compounds with improved pharmacological profiles that maintain therapeutic efficacy while reducing adverse effects.
Solution Approach 2:
The invention creates composite molecular structures by combining tetrazole core compounds with various substituent groups (heteroaryl, aryl, cycloalkyl). These composite structures allow fine-tuning of pharmacological properties to achieve the desired balance between therapeutic effect and reduced side effects.
2Reliability
If existing mGluR5 modulators are used to treat pain conditions, then therapeutic effect is achieved, but significant adverse effects occur
Solution Approach 1:
The patent applies parameter changes by modifying the molecular structure of pain treatment compounds. Specific tetrazole derivatives with customized substituents are designed to optimize analgesic efficacy while minimizing adverse effects associated with existing mGluR5 modulators.
Solution Approach 2:
The invention introduces local quality variations by placing specific functional groups at specific positions within the molecular structure. The tetrazole ring with its electron-withdrawing properties is positioned to interact with the mGluR5 receptor binding site, while substituents are strategically placed to optimize pharmacokinetic properties and reduce side effects.
3Reliability
If existing mGluR5 modulators are used to treat Parkinson's disease, then therapeutic effect is achieved, but significant adverse effects occur
Solution Approach 1:
The patent employs parameter changes to create novel tetrazole compounds with optimized structures for Parkinson's disease treatment. The molecular parameters are adjusted to achieve dopaminergic modulation with reduced adverse effects compared to existing therapies.
Data Source
AI summary
Tetrazole compounds substituted directly, or by a bridge, with i) a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl and ii) another heteroaryl or aryl ring, with at least one of the rings being further substituted with another ring, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, panic, and bipolar disorder, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, drug addiction, drug abuse, drug withdrawal, obesity and other diseases.