Indolin-2-one derivatives targeting NMDA and ENT1 for CNS disorders
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Solution Overview
Problem
Current treatments for schizophrenia and related CNS diseases, such as antipsychotic medications, fail to significantly alleviate negative symptoms and cognitive dysfunction, and there is a need for more effective therapeutic options that can address a wide range of associated neuropsychiatric syndromes and comorbid conditions.
Innovation Solution
Development of novel indolin-2-one derivatives and their pharmaceutically acceptable salts, which can be used alone or in combination with existing antipsychotics, antidepressants, and anxiolytics, to treat CNS diseases including schizophrenia, substance abuse, depression, anxiety disorders, and neurodegenerative conditions by targeting NMDA glycine sites and acting as ENT1 inhibitors.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current antipsychotic medications are used to treat schizophrenia, then positive symptoms can be controlled, but negative symptoms and cognitive dysfunction are not significantly alleviated
Solution Approach 1:
The patent describes indolin-2-one derivatives that simultaneously target multiple receptors and transporters including NMDA glycine sites, ENT1, and adenosine receptors, enabling a single compound to address positive symptoms, negative symptoms, and cognitive dysfunction of schizophrenia as well as other neuropsychiatric conditions, thereby achieving multi-functionality and improved versatility
2Reliability
If existing treatments are used for CNS diseases, then some symptoms can be managed, but overall therapeutic efficacy is insufficient
Solution Approach 1:
The patent describes combining indolin-2-one derivatives with existing antipsychotics, antidepressants, and anxiolytics in single therapeutic regimens, merging multiple pharmacological actions into a coordinated treatment approach that improves overall efficacy while potentially simplifying management compared to multiple separate medications
Data Source
AI summary
The present invention is concerned with indolin-2-one derivatives of general formula (I) wherein the substituents are defined in claim 1. The compounds may be used in the treatment of CNS diseases related to positive (psychosis) and negative symptoms of schizophrenia, substance abuse, alcohol and drug addiction, obsessive-compulsive disorders, cognitive impairment, bipolar disorders, mood disorders, major depression, treatment resistant depression, anxiety disorders, Alzheimer's disease, autism, Parkinson's disease, chronic pain, borderline personality disorder, neurodegenerative disease, sleep disturbances, chronic fatigue syndrome, stiffness, inflammatory disease, asthma, Huntington's disease, ADHD, amyotrophic lateral sclerosis, effects in arthritis, autoimmune disease, viral and fungal infections, cardiovascular diseases, ophthalmology and inflammatory retinal diseases and balance problems, epilepsy and neurodevelopmental disorders with co-morbid epilepsy.