CRAC Channel Inhibitor Compositions for Intracellular Calcium Modulation

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Solution Overview

Problem

Current treatments for pancreatitis, viral infections, stroke, traumatic brain injury, fibrosis, and autoimmune diseases do not effectively modulate intracellular calcium levels, which are crucial for cellular function and response.

Innovation Solution

A pharmaceutical composition comprising a CRAC channel inhibitor, specifically N-(5-(6-chloro-2,2-difluorobenzo[d][1,3]dioxol-5-yl)pyrazin-2-yl)-2-fluoro-6-methylbenzamide, formulated as a homogeneous liquid, emulsion, nanosuspension, or powder for reconstitution, is administered to modulate intracellular calcium levels.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments are used for pancreatitis, viral infections, stroke, traumatic brain injury, fibrosis, and autoimmune diseases, then existing therapeutic approaches are maintained, but intracellular calcium levels cannot be effectively modulated

Engineering Contradiction:
Improveeffectiveness of treatmentVSAvoidability to modulate intracellular calcium
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies parameter changes by developing a CRAC channel inhibitor that specifically targets intracellular calcium levels. The compound N-(5-(6-chloro-2,2-difluorobenzo[d][1,3]dioxol-5-yl)pyrazin-2-yl)-2-fluoro-6-methylbenzamide modulates calcium influx through CRAC channels, changing the physiological parameter of intracellular calcium concentration to achieve therapeutic effects for multiple diseases including pancreatitis, viral infections, stroke, traumatic brain injury, fibrosis, and autoimmune diseases.

Inventive Principle:
Principle #35Parameter changes

2Stability of the object's composition

If the CRAC channel inhibitor is formulated as a homogeneous liquid, emulsion, nanosuspension, or powder for reconstitution, then therapeutic stability is improved, but formulation complexity increases

Engineering Contradiction:
Improvetherapeutic stabilityVSAvoidformulation complexity
Core Design Contradiction:
Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The patent applies segmentation by providing the CRAC channel inhibitor in multiple distinct formulation types: homogeneous liquid, emulsion, nanosuspension, and powder for reconstitution. Each formulation type represents a segmented approach to delivering the active compound, allowing selection based on specific therapeutic needs, route of administration, and stability requirements while maintaining the core therapeutic function.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent applies composite materials by formulating the CRAC channel inhibitor as an emulsion or nanosuspension, which are composite systems combining the active pharmaceutical ingredient with excipients, surfactants, and other components. These composite formulations enhance stability, solubility, and deliverability of the inhibitor while managing the complexity through standardized formulation science.

Inventive Principle:
Principle #40Composite materials

3Reliability

If the pharmaceutical composition is designed for injection, then bioavailability is improved, but manufacturing and handling complexity increases

Engineering Contradiction:
ImprovebioavailabilityVSAvoidmanufacturing and handling
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The patent applies parameter changes by designing the pharmaceutical composition for injection, which fundamentally changes the delivery parameter from oral or other routes to parenteral administration. This parameter change achieves superior bioavailability and rapid onset of action for the CRAC channel inhibitor, ensuring reliable therapeutic effects while the formulation is optimized to manage the associated manufacturing and handling requirements.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS20240058332A1CRAC channel inhibitor compositions
Publication Date: 2024.02.22 CALCIMEDICA SUBSIDIARY INC
  • US20240058332A1 patent drawing
  • US20240058332A1 patent drawing
  • US20240058332A1 patent drawing

AI summary

Provided herein are pharmaceutical compositions, such as emulsions and nanosuspensions, comprising a CRAC channel inhibitor. Also provided herein are methods of treating pancreatitis, viral infections, stroke, traumatic brain injury, fibrosis, inflammation, and autoimmune diseases by administering such pharmaceutical compositions.