Acid Pump Antagonist for Gastrointestinal Motility

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Solution Overview

Problem

Current medications for gastrointestinal motility disorders in the hungry condition take several days to take effect and do not improve motility cooperatively with physiological contractions, leading to unmet needs in alleviating symptoms such as abdominal distension and discomfort.

Innovation Solution

An acid pump antagonist, represented by compounds like (-)-1-(2-methoxyethyl)-N,N,2-trimethyl-8-phenyl-1,6,7,8-tetrahydrochromeno[7,8-d]imidazole-5-carboxamide, is administered to inhibit gastric acid secretion, thereby enhancing and normalizing gastrointestinal motility, addressing the relationship between gastric acid secretion and motility.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Speed

If conventional drugs are used to treat gastrointestinal motility disorders, then the treatment covers a broad range of conditions, but the onset of effect takes several days and does not improve motility cooperatively with physiological contractions

Engineering Contradiction:
Improveonset of effectVSAvoidcooperative contraction with physiological motility
Core Design Contradiction:
SpeedVSReliability

Solution Approach 1:

The patent applies parameter changes by switching from conventional slow-acting motility drugs to acid pump antagonists that work through a different physiological mechanism. The acid pump antagonist rapidly reduces gastric acid secretion, which immediately removes the inhibitory effect on gastrointestinal motility, enabling rapid onset of action that coordinates with natural physiological contractions rather than forcing artificial stimulation.

Inventive Principle:
Principle #35Parameter changes

2Speed

If compounds forcibly stimulate gastrointestinal motility, then immediate effect is achieved, but the contraction is not cooperative with physiological gastrointestinal motility

Engineering Contradiction:
Improveonset of effectVSAvoidphysiological coordination of contraction
Core Design Contradiction:
SpeedVSStability of the object's composition

Solution Approach 1:

The patent converts the harmful effect of excessive gastric acid secretion into a beneficial therapeutic mechanism. By blocking the acid pump, the drug transforms the pathological high-acid state into a normal-acid state, which naturally restores coordinated gastrointestinal motility. The acid reduction itself becomes the therapeutic action that enables physiological contraction patterns rather than forcing artificial stimulation.

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

3Object-affected harmful factors

If gastric acid secretion is increased in hungry condition, then duodenal ulcer symptoms occur, but gastrointestinal motility decreases causing abdominal distension and discomfort

Engineering Contradiction:
Improveduodenal ulcer protectionVSAvoidabdominal distension and discomfort
Core Design Contradiction:
Object-affected harmful factorsVSObject-generated harmful factors

Solution Approach 1:

The patent applies inversion by treating the root cause (excessive gastric acid secretion) rather than the symptom (decreased motility). Conventional approaches tried to stimulate motility directly, but this patent inverts the approach by reducing gastric acid, which paradoxically restores normal motility. The acid reduction removes the pathological inhibition on gastrointestinal movement, simultaneously protecting against duodenal ulcers and eliminating abdominal distension.

Inventive Principle:
Principle #13The other way round (Inversion)

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The acid pump antagonist effectively alleviates or prevents symptoms of abnormal gastrointestinal motility by enhancing gastrointestinal motility, providing immediate relief and normalizing contractions in the gastric antrum and duodenum, making it a novel treatment for gastrointestinal function adjustment and motility activation.

Implementation Method 1

a reversible inhibitory activity of a gastric proton pump activity

Methodology Applied
Scientific EffectAcid pump antagonism:

Data Source

PatentEP2452680B1Acid pump antagonist for the treatment of diseases involved in abnormal gastrointestinal motility
Publication Date: 2019.12.18 RAQUALIA PHARMA INC
  • EP2452680B1 patent drawingFigure 1~3
  • EP2452680B1 patent drawingFigure 4
  • EP2452680B1 patent drawing

AI summary

The present invention relates to a use of a compound having an acid pump antagonistic activity, a pharmaceutically acceptable salt thereof or a pharmaceutical composition thereof for the manufacture of a medicament for prevention or treatment of diseases in which abnormal gastrointestinal motility is involved. In addition, the present invention relates to the method of prevention or treatment including administering to a human or animal. The compound, the pharmaceutically acceptable salt thereof, or pharmaceutical compositions containing them, may be used in combination with one or more second active agent. Further, the present invention relates to pharmaceutical compositions and kits comprising a compound having an acid pump antagonistic activity or a pharmaceutically acceptable salt thereof for the prevention or treatment of said diseases.