Modified Beta-Agonists for IBS Symptom Relief

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Solution Overview

Problem

Current treatments for irritable bowel syndrome (IBS) are often ineffective and associated with significant adverse side effects, failing to adequately address the chronic pain, fatigue, and societal costs imposed by the condition.

Innovation Solution

Administration of specific compounds, such as those of formulas I, II, III, and IV, or their metabolites, prodrugs, and pharmaceutically acceptable salts, which target the gastrointestinal system to alleviate symptoms of IBS by reducing motor and sensory dysfunction, potentially combined with other drugs like non-steroidal anti-inflammatory agents or probiotics.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If traditional β-adrenergic agonists like terbutaline are used to treat IBS, then motor dysfunction and sensory symptoms may be addressed, but significant adverse side effects occur

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidadverse side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure of β-adrenergic agonists through specific molecular formulas (I, II, III, IV) with defined substituents and stereochemistry. This structural modification changes the pharmacological parameters to achieve selective gastrointestinal smooth muscle relaxation while minimizing systemic side effects, thus resolving the contradiction between treatment effectiveness and adverse effects

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention applies local quality by designing compounds that specifically target gastrointestinal smooth muscle tissue. The modified β-adrenergic agonists exhibit selective action on GI tract receptors, providing localized therapeutic effect in the gastrointestinal system while reducing unwanted systemic effects, thereby improving the ratio of beneficial to harmful effects

Inventive Principle:
Principle #3Local quality

2Reliability

If current IBS treatments are administered, then some symptoms may be alleviated, but they fail to adequately address chronic pain and fatigue

Engineering Contradiction:
Improvesymptom alleviationVSAvoidcomprehensive symptom coverage
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies universality by developing a multi-functional treatment approach. The modified β-adrenergic agonists address multiple IBS symptoms simultaneously including abdominal pain, bloating, constipation, and diarrhea through their mechanism of relaxing gastrointestinal smooth muscle and normalizing motility. This multi-symptom coverage resolves the limitation of current treatments that only partially alleviate symptoms

Inventive Principle:
Principle #6Universality (Multi-functionality)

3Ease of operation

If IBS is treated with conventional methods, then some patients may experience relief, but the condition imposes high societal costs and work absenteeism

Engineering Contradiction:
Improvepatient reliefVSAvoidsocietal cost
Core Design Contradiction:
Ease of operationVSQuantity of substance

Solution Approach 1:

The patent applies self-service by providing a treatment that enables patients to manage their own symptoms effectively with minimal medical intervention. The oral administration of modified β-adrenergic agonists allows patients to control their condition at home, reducing the need for frequent hospital visits and work absenteeism, thereby decreasing societal costs while maintaining ease of operation for the patient

Inventive Principle:
Principle #25Self-service

Data Source

PatentUS8518995B2Methods and compositions for the treatment of irritable bowel syndrome
Publication Date: 2013.08.27 MEDICINOVA INC
  • US8518995B2 patent drawing
  • US8518995B2 patent drawing
  • US8518995B2 patent drawing

AI summary

A method for a prevention and/or treatment of irritable bowel syndrome or amelioration of a symptom thereof in a subject, comprises administering to said subject an effective amount of a compound of formula I: