Phosphate ROR Modulators for Improved Pulmonary Absorption
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Solution Overview
Problem
There is a need for new ROR modulators with improved pharmacokinetic properties to provide more efficient treatment for respiratory diseases such as asthma and COPD.
Innovation Solution
Development of phosphate derivatives of ROR modulators with enhanced solubility, stability, and metabolization in the organism, facilitating absorption in the lungs, particularly in the form of compounds with specific structural formulas and stereoisomers, along with pharmaceutical compositions for administration via nasal inhalation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If new ROR modulators are developed for treating respiratory diseases, then therapeutic efficacy is improved, but pharmacokinetic properties (solubility, stability, absorption) are insufficient
Solution Approach 1:
The patent applies parameter changes by modifying the chemical structure of ROR modulators through phosphate derivative formation. This chemical modification transforms the original compounds into phosphate esters, which fundamentally changes their physicochemical parameters including solubility, stability, and metabolic properties, thereby resolving the pharmacokinetic deficiencies while maintaining therapeutic efficacy
Solution Approach 2:
The invention creates composite molecular structures by combining the ROR modulator core structure with phosphate groups. This composite approach integrates the therapeutic activity of the original modulator with the enhanced pharmacokinetic properties of phosphate derivatives, achieving both improved efficacy and better absorption/stability characteristics
2Ease of operation
If phosphate derivatives are developed to improve solubility and stability, then absorption in lungs is enhanced, but molecular complexity increases
Solution Approach 1:
The phosphate derivative modification changes key physicochemical parameters of the ROR modulators, specifically enhancing water solubility and metabolic stability. These parameter changes directly improve pulmonary absorption characteristics without requiring complex delivery systems or formulation approaches
Data Source
Figure 1
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Figure 3B~3C
AI summary
The present invention relates to phosphate derivatives of formula (I), and their therapeutic uses, preferably for treating a respiratory disease. The present invention further relates to pharmaceutical compositions and devices comprising such compounds.