Novel Azole Derivatives as V1b Receptor Antagonists
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Solution Overview
Problem
Current treatments for mood disorders, anxiety disorders, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorders, hypertension, gastrointestinal diseases, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related diseases, and alopecia lack effective V1b receptor antagonists with novel structures.
Innovation Solution
Development of novel azole derivatives with a specific azole skeleton that act as V1b receptor antagonists, providing a pharmaceutical composition for treating or preventing the mentioned diseases.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing V1b receptor antagonists (1,3-dihydro-2H-indol-2-one compounds and other derivatives) are used, then therapeutic effects for mood disorders and other diseases can be achieved, but structural novelty and potential for improved efficacy are limited
Solution Approach 1:
The patent applies parameter changes by modifying the core chemical structure from existing V1b receptor antagonist frameworks (such as 1,3-dihydro-2H-indol-2-one) to a novel pyrazolo[1,2-a]pyrimidine skeleton. This structural parameter change maintains the essential pharmacophore elements needed for V1b receptor binding while introducing novel molecular architecture that may improve therapeutic efficacy and reduce side effects associated with existing compounds
2Adaptability or versatility
If novel compound structures are developed, then structural diversity and potential therapeutic advantages are improved, but development complexity and validation requirements increase
Solution Approach 1:
The patent applies segmentation by dividing the novel pyrazolo[1,2-a]pyrimidine compound into distinct functional domains: the core heterocyclic scaffold (providing structural novelty), substituent groups at specific positions (providing pharmacological activity), and pharmacophore elements (providing receptor binding). This segmentation allows systematic optimization of each domain while maintaining overall molecular integrity and facilitating structure-activity relationship studies
Solution Approach 2:
The patent uses the pyrazolo[1,2-a]pyrimidine core structure as an intermediary framework that bridges the gap between existing V1b antagonist structures and desired novel therapeutic agents. This intermediary scaffold incorporates essential binding features while allowing diverse substituent modifications, thereby simplifying the development process by providing a validated core structure rather than requiring de novo design of all molecular features
Data Source
AI summary
The present invention provides agents for treating or preventing diseases such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, alopecia, and so forth. Specifically, the invention provides azole derivatives represented by general formula (I), or pharmaceutically acceptable salts thereof that have an antagonistic action against the arginine-vasopressin (AVP) V1b receptor: