Quinolone Composition for IBS-D With Lower Side-Effect Burden

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Solution Overview

Problem

Current treatments for irritable bowel syndrome (IBS), particularly IBS-D, are not sufficiently effective, leading to a need for a more potent medicament.

Innovation Solution

A quinolone compound, 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methyl-7-(2-amino-3-cyano-5-pyridyl)-4-oxo-3-quinoline-carboxylic acid, or its derivatives, is used as an active ingredient in pharmaceutical compositions for treating and preventing IBS, particularly IBS-D.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing medicaments (tricyclic antidepressants, 5HT antagonists) are used to treat IBS-D, then some therapeutic effect is achieved, but side effects occur (sleep disturbance, constipation, thirst) and complete therapy is not expected

Engineering Contradiction:
Improvetherapeutic effectVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by selecting a quinolone compound with specific chemical structure parameters (1-cyclopropyl-6-fluoro-1,4-dihydro-8-methyl-7-(2-amino-3-cyano-5-pyridyl)-4-oxo-3-quinoline-carboxylic acid) that exhibits different pharmacological properties from existing medicaments. This chemical parameter change results in a compound that addresses IBS-D symptoms without producing the side effects associated with tricyclic antidepressants and 5HT antagonists, thereby improving the therapeutic index.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If more potent medicament is developed to achieve complete therapy of IBS-D, then therapeutic efficacy is improved, but risk of side effects and unknown harmful factors may increase

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidunknown harmful factors
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent employs an intermediary approach by using a quinolone compound that acts through a different mechanism of action compared to existing IBS-D treatments. This intermediary compound (OPS-2071) provides complete therapy for IBS-D while maintaining a favorable safety profile, as evidenced by the lack of significant side effects in clinical studies, thus achieving high efficacy without proportionally increased risk.

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentUS20260027103A1Pharmaceutical compositions comprising a quinolone compound for irritable bowel syndrome
Publication Date: 2026.01.29 OTSUKA PHARM CO LTD
  • US20260027103A1 patent drawing
  • US20260027103A1 patent drawing
  • US20260027103A1 patent drawing

AI summary

Provided herein are pharmaceutical compositions comprising a quinolone compound for irritable bowel syndrome, especially provided is the use of the quinolone compound, in particular 1-cyclopropyl-6-fluoro-1. 4-dihydro-8-methyl-7-(2-amino-3-cyano-5-pyridyl)-4-oxo-3-quinoline-carboxylic acid or a pharmacologically acceptable salt, a hydrate, a solvate or a deuteride thereof for preventing or treating irritable bowel syndrome of a human or an animal.