SOC Channel Modulation via Specific Compound Structures

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Solution Overview

Problem

Current technologies fail to effectively modulate store-operated calcium (SOC) channel activity, which is crucial for regulating various cellular functions, including cell proliferation, gene transcription, and cytokine release, as existing methods do not adequately inhibit SOC channels, leading to uncontrolled calcium influx and associated cellular responses.

Innovation Solution

Development of compounds of specific formulas (I, IA, II, IIA, III, IIIA, IV, IVA, V, VA, VIA, VII, VIIA) that inhibit SOC channel activity by preventing the activation of store-operated calcium channels, including calcium-release activated calcium channels, thereby modulating intracellular calcium levels and interactions with proteins like STIM and Orai.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing methods are used to modulate SOC channel activity, then general calcium regulation is maintained, but effective inhibition of SOC channels is not achieved, leading to uncontrolled calcium influx

Engineering Contradiction:
ImproveSOC channel inhibition effectivenessVSAvoiduncontrolled calcium influx
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure of compounds to achieve effective SOC channel inhibition. Specifically, the patent describes compounds with specific molecular structures (including various substituted benzodiazepine and related compounds) that have been designed to interact with SOC channels. By changing the chemical parameters (molecular structure, functional groups, substituents) of the compounds, the patent achieves reliable inhibition of SOC channels, thereby controlling calcium influx that was previously uncontrolled with existing methods.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If SOC channel activity is not inhibited, then normal cellular calcium signaling is maintained, but pathological conditions such as autoimmune diseases and inflammatory disorders persist

Engineering Contradiction:
Improvedisease treatment effectivenessVSAvoidcytokine release and inflammatory response
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent applies parameter changes by using compounds with specific chemical structures to modulate SOC channel activity, thereby controlling calcium-dependent cellular processes. The described compounds (including substituted benzodiazepines and related structures) are designed to inhibit SOC channels, which prevents excessive calcium influx that triggers pathological cytokine release and inflammatory responses. This chemical parameter modification approach enables effective treatment of autoimmune diseases and inflammatory disorders while maintaining normal physiological calcium signaling.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS9353099B2Compounds that modulate intracellular calcium
Publication Date: 2016.05.31 CALCIMEDICA SUBSIDIARY INC
  • US9353099B2 patent drawing
  • US9353099B2 patent drawing
  • US9353099B2 patent drawing

AI summary

Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.