EP4 Agonist Morpholine Carboxamides With Low Systemic Exposure
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Solution Overview
Problem
Current treatments for gastrointestinal and pulmonary disorders, such as chronic constipation, inflammatory bowel disease, asthma, and chronic obstructive pulmonary disease, often fail to provide complete and sustainable relief due to systemic side effects, and there is a need for EP4 receptor agonists that can effectively target these conditions without cardiovascular complications.
Innovation Solution
Development of novel morpholine-3-carboxamide derivatives that act as selective EP4 receptor agonists, designed to promote intestinal fluid homeostasis and bronchodilation, with low gastrointestinal permeability to minimize systemic distribution and cardiovascular side effects.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current treatments for gastrointestinal and pulmonary disorders are used, then therapeutic effects are achieved, but systemic side effects occur including cardiovascular complications
Solution Approach 1:
The patent applies local quality by designing compounds with selective EP4 receptor agonist activity that targets specific gastrointestinal and pulmonary tissues. The compounds promote intestinal fluid homeostasis and bronchodilation through localized EP4 receptor activation, minimizing systemic distribution and cardiovascular side effects while maintaining therapeutic efficacy in target organs.
2Reliability
If EP4 receptor agonists are designed to promote intestinal fluid homeostasis and bronchodilation, then therapeutic benefits are achieved, but gastrointestinal permeability may increase leading to systemic distribution
Solution Approach 1:
The patent applies local quality by designing compounds with selective EP4 receptor agonist activity that targets specific gastrointestinal and pulmonary tissues. The compounds promote intestinal fluid homeostasis and bronchodilation through localized EP4 receptor activation, minimizing systemic distribution and cardiovascular side effects while maintaining therapeutic efficacy in target organs.
Data Source
AI summary
The present invention relates to compounds of formula (I) as prostaglandin E2 receptor 4 (EP4) agonists for use in methods of treatment of gastrointestinal and pulmonary diseases or disorders. The present disclosure provides exemplary compounds and pharmacological data.