Biaryl Piperidine Amide Compounds Modulating CRAC Channels
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Solution Overview
Problem
Current methods fail to effectively modulate calcium levels in cells, leading to adverse effects on cell function and structure, particularly in immune, inflammatory, and allergic disorders, where dysregulation of calcium plays a significant role in disease pathogenesis.
Innovation Solution
Development of novel biaryl piperidine amide compounds that target store-operated calcium (SOC) channels, specifically the calcium-release activated calcium (CRAC) channels, to modulate calcium entry and regulate cellular responses.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current methods are used to modulate calcium levels in cells, then cell function and structure are maintained, but they fail to effectively treat immune, inflammatory, and allergic disorders caused by calcium dysregulation
Solution Approach 1:
The patent employs parameter changes by developing novel biaryl piperidine amide compounds with specific molecular structures and substitutions that modify calcium channel activity. The compounds feature variable parameters including different substituents (R1-R5), ring structures (X1-X4), and stereochemical configurations that fine-tune the modulation of store-operated calcium channels to achieve therapeutic effects while minimizing adverse effects on cell function.
Solution Approach 2:
The biaryl piperidine amide compounds act as intermediary molecules that mediate the modulation of calcium entry through store-operated calcium channels. These compounds bind to and regulate CRAC channel activity, serving as a bridge between therapeutic intervention and calcium homeostasis control, thereby treating immune and inflammatory disorders without directly disrupting cell structure.
2Productivity
If calcium levels are modulated to treat immune and inflammatory disorders, then therapeutic benefits are achieved, but precise control of calcium entry through SOC channels is required to avoid cellular dysfunction
Solution Approach 1:
The patent applies local quality by designing compounds with specific functional groups and substitution patterns at different positions of the biaryl piperidine amide core structure. Different substituents (R1-R5) and ring configurations (X1-X4) provide localized modifications that fine-tune the compound's affinity and selectivity for store-operated calcium channels, enabling precise control of calcium entry while achieving therapeutic effects.
Solution Approach 2:
The patent incorporates dynamics by developing compounds with variable stereochemical configurations and conformational flexibility. The biaryl piperidine amide structure allows for dynamic interactions with CRAC channels, where different isomers and conformers can modulate channel activity with varying degrees of potency and selectivity, enabling precise therapeutic control.
Data Source
AI summary
The present application is directed to biaryl piperidine amide compounds, or pharmaceutically acceptable salts, solvates, and prodrugs thereof, and methods of use thereof.