Indolin-2-one derivatives for CNS disorders
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current treatments for schizophrenia and related CNS disorders, such as antipsychotic medications, fail to effectively address negative symptoms and cognitive dysfunction, and there is a need for novel compounds that can treat a wide range of psychiatric and neurological conditions.
Innovation Solution
Development of indolin-2-one or pyrrolo-pyridin/pyrimidin-2-one derivatives with specific heteroaryl groups, which can be used alone or in combination with existing antipsychotics, antidepressants, and anxiolytics to treat positive and negative symptoms of schizophrenia, as well as other CNS disorders.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If antipsychotic medications are used to treat schizophrenia, then positive symptoms can be controlled, but negative symptoms and cognitive dysfunction remain untreated
Solution Approach 1:
The patent develops compounds with dual functionality that can simultaneously address positive symptoms, negative symptoms, and cognitive dysfunction. The indolin-2-one and pyrrolo-pyridin/pyrimidin-2-one derivatives are designed to interact with multiple neurotransmitter systems (dopamine, serotonin, NMDA receptors), enabling a single compound to perform multiple therapeutic functions that were previously requiring separate medications.
2Reliability
If existing antipsychotics are used, then psychotic symptoms can be managed, but functional impairments and quality of life remain significantly reduced
Solution Approach 1:
The patent employs parameter changes by modifying the chemical structure of antipsychotic compounds to alter their pharmacological profile. By changing molecular parameters (adding heteroaryl groups, modifying substitution patterns), the compounds achieve improved binding affinity and selectivity for multiple receptor types, thereby enhancing functional outcomes and quality of life while maintaining psychotic symptom control.
3Adaptability or versatility
If novel compounds with multiple therapeutic functions are developed, then treatment versatility improves, but drug development complexity increases
Solution Approach 1:
The patent applies segmentation by dividing the complex therapeutic target into modular chemical components. The core indolin-2-one or pyrrolo-pyridin/pyrimidin-2-one structure serves as a foundation, to which various heteroaryl groups and substitution patterns can be systematically added or modified. This modular approach allows researchers to tune specific properties (affinity, selectivity, pharmacokinetics) by changing individual modules rather than redesigning the entire molecule.
Data Source
AI summary
The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula (I)wherein Ar, X, X1, R1, R2, R3, m, n and the dotted line are as defined herein which compounds are useful for treating certain central nervous system disorders as described herein.