P2X7 Modulator Pharmaceutical Composition for Oral Administration
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Solution Overview
Problem
Current therapeutic agents fail to effectively modulate P2X7 receptor activity, which is implicated in various inflammatory and neurological disorders, including pain, mood disorders, and Alzheimer's disease, highlighting the need for compounds that can specifically target and regulate P2X7 receptor function.
Innovation Solution
Pharmaceutical compositions comprising specific compounds such as 11-{[2-Chloro-3-(trifluoromethyl)phenyl]carbonyl}-3-pyrimidin-2-yl-5,6,7,8,9,10-hexahydro-6,10-epimino[1,2,4]triazolo[4,3-a]azocine and its stereoisomers, which are formulated for oral administration and include pharmaceutically acceptable excipients to treat diseases mediated by P2X7 receptor activity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current therapeutic agents are used to treat P2X7 receptor-mediated diseases, then treatment is provided, but the agents fail to effectively modulate P2X7 receptor activity
Solution Approach 1:
The patent applies parameter changes by developing new chemical compounds with specific molecular structures (formula 1 and its stereoisomers) that have optimized binding affinity and modulatory efficacy for the P2X7 receptor. These compounds represent a parameter change from existing therapeutic agents in terms of chemical structure, receptor binding characteristics, and pharmacological activity, thereby achieving effective P2X7 modulation where previous agents failed.
2Reliability
If specific P2X7 modulating compounds are developed, then effective receptor modulation is achieved, but the complexity of identifying and developing such compounds increases
Solution Approach 1:
The patent embodies preliminary action by providing a defined set of specific chemical compounds (formula 1 and stereoisomers) that have been pre-identified and characterized for their P2X7 modulatory activity. This preliminary development and characterization of specific compounds with known structures and activities reduces the complexity for subsequent applications, as researchers can directly use these pre-validated compounds rather than conducting de novo screening campaigns.
Data Source
AI summary
The present invention is directed to a compound of Formula (I): wherein: n is an integer from 0-1; • X is CH2 when n is 0, or X is CH2 or oxygen when n is 1; • R1 is phenyl or pyridinyl, wherein the phenyl or pyridinyl is optionally substituted with from 1 to 4 substituents independently selected from halogen and alkyl; and • R2 is phenyl, pyridinyl, pyrazinyl, pyradizinyl, pyrimidinyl, pyrrolyl, pyrazolyl, thiazolyl or thiophenyl, wherein the phenyl, pyridinyl, pyrazinyl, pyradizinyl, pyrimidinyl, pyrrolyl, pyrazolyl, thiazolyl or thiophenyl is optionally substituted with from 1 to 2 substituents independently selected from the group consisting of halogen, alkyl, hydroxy and alkoxy. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). The compounds of formula (I) are useful as P2X7 modulators.