Condensed-Cyclic Compound M1 Receptor Modulation
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Solution Overview
Problem
Current treatments lack effective compounds for addressing constipation associated with neurological diseases, spinal cord injuries, multiple sclerosis, and other conditions by modulating cholinergic muscarinic M1 receptors.
Innovation Solution
Development of a compound represented by formula (I), which acts as a cholinergic muscarinic M1 receptor positive allosteric modulator, binding to a site different from the endogenous activator acetylcholine to potentiate receptor function, potentially serving as a prophylactic or therapeutic agent for constipation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional treatments are used for constipation, then general constipation symptoms may be relieved, but constipation associated with neurological diseases and spinal cord injuries cannot be effectively treated
Solution Approach 1:
The patent develops a compound with specific molecular structure (formula I) that selectively targets M1 muscarinic receptors in the gastrointestinal tract. This local quality approach creates a treatment that is specifically effective for neurological disease-related constipation while maintaining safety for general use, resolving the contradiction between specialized effectiveness and broad adaptability
2Reliability
If M1 receptor agonists are used to promote gastrointestinal motility, then constipation can be treated, but unwanted central nervous system effects occur
Solution Approach 1:
The compound in formula I is designed to selectively activate M1 receptors in the gastrointestinal tract while having minimal effect on central nervous system M1 receptors. This spatial selectivity allows the drug to promote gastrointestinal motility effectively without causing CNS-related side effects such as confusion, hallucinations, or seizures
Solution Approach 2:
The patent uses a positive allosteric modulator mechanism where the compound binds to a distinct site on the M1 receptor and enhances the effect of endogenous acetylcholine rather than directly activating the receptor. This intermediary approach provides more selective and modulated gastrointestinal motility promotion with reduced risk of overstimulation and CNS side effects
Data Source
AI summary
The present invention aims to provide a compound that may be useful for the prophylaxis or treatment of constipation and the like. The present invention provides a compound represented by the formula (I):wherein each symbol is as described in the specification, or a salt thereof.