Sulfamide P-CAB Compounds for Fast, Sustained Gastric Acid Suppression
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Solution Overview
Problem
Current proton pump inhibitors (PPIs) face issues such as instability, short half-life, susceptibility to CYP2C19 gene polymorphism, limited dosing time, slow onset of action, and safety risks like hepatotoxicity, necessitating the development of new compounds with faster onset of action, stronger acid inhibition, and longer pH maintenance time.
Innovation Solution
Development of compounds containing a sulfamide structure, including tautomers, mesomers, racemates, enantiomers, or diastereoisomers, or pharmaceutically acceptable salts, which act as potassium-competitive acid blockers (P-CABs) to inhibit H+/K+-ATPase in both resting and activated states, providing faster and more sustained acid suppression.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If conventional PPIs are used to inhibit gastric acid secretion, then acid inhibition efficacy is achieved, but onset of action is slow and dosing time is limited
Solution Approach 1:
The patent changes the chemical structure parameters of acid inhibitors by introducing sulfamide groups and specific substituent patterns (R1-R6 groups) to create P-CAB compounds with improved pharmacokinetic properties, enabling faster onset and extended dosing flexibility compared to conventional PPIs
2Duration of action of stationary object
If PPIs are used for long-term clinical application, then acid-related diseases are treated, but instability and short half-life occur
Solution Approach 1:
The patent employs composite molecular structures combining sulfamide core with various stabilizing substituent groups (R1-R6) to create P-CAB compounds that exhibit both extended half-life and enhanced chemical stability, overcoming the limitations of conventional PPIs
3Speed
If P-CABs are developed to provide faster acid suppression, then onset of action is improved, but tissue distribution and druggability need enhancement
Solution Approach 1:
The patent applies local quality modifications by introducing specific functional groups at different positions (R1-R6 substituents) on the sulfamide core structure to optimize both the rapid onset action and the tissue distribution properties, allowing different regions of the molecule to fulfill different functional requirements
Data Source
AI summary
The present invention relates to the field of pharmaceuticals and discloses a compound containing a sulfamide structure, its preparation method thereof and application thereof, and pharmaceutical composition and application. The compound has the structure shown in formula (I). The compound provided by the present invention can serve as therapeutic agents, particularly as gastric acid secretion inhibitors and potassium-competitive acid blockers (P-CABs).