2-Oxapregnane Agent for Urination Disorders Beyond Prostate Enlargement

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Solution Overview

Problem

Existing urination disorder treatments are ineffective in addressing the condition regardless of prostate enlargement and often require long-term administration with safety concerns.

Innovation Solution

A urination disorder-improving agent containing a 2-oxapregnane compound or its pharmaceutically acceptable salt, specifically with a hydroxyl or oxo group on the steroid skeleton, effectively treats urination disorders by enhancing antiandrogenic activity, irrespective of prostate enlargement.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional urination disorder treatments (5α-reductase inhibitors, plant preparations) are used, then prostate enlargement is addressed, but they are ineffective for patients without significant prostate enlargement and require long-term administration with safety concerns

Engineering Contradiction:

Improvetherapeutic effectivenessVSAvoidapplicability regardless of prostate enlargement

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent changes the chemical structure parameters of the active ingredient from conventional 5α-reductase inhibitors to a specific 2-oxapregnane compound with formula (1), featuring unique structural elements (oxa ring at position 2, specific substituents R1-R6, X, Y) that enable broader mechanism of action beyond just addressing prostate enlargement

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The 2-oxapregnane compound is designed to serve multiple functions: it addresses urination disorders through antiandrogenic activity while also being effective regardless of the degree of prostate enlargement, and maintains safety for long-term administration, making it universally applicable to different patient subgroups

Inventive Principle:

Principle #6Universality (Multi-functionality)

2Duration of action of moving object

If long-term administration of conventional urination disorder drugs is required, then chronic symptom management is achieved, but safety concerns arise from prolonged use

Engineering Contradiction:

Improveduration of treatmentVSAvoidsafety concerns

Core Design Contradiction:

Duration of action of moving objectVSObject-affected harmful factors

Solution Approach 1:

The patent identifies a specific 2-oxapregnane compound structure that demonstrates improved safety profile for long-term use compared to conventional drugs, allowing for extended treatment duration without accumulating harmful effects, effectively replacing long-term conventional medications with a safer alternative

Inventive Principle:

Principle #27Cheap short-living objects (Disposable)

Data Source

PatentUS12458650B2Urination disorder-improving agent

Publication Date: 2025.11.04 ASKA PHARMACEUTICAL CO LTD

AI summary

Provided is a urination disorder-improving agent useful for treating or improving (or alleviating) a urination disorder regardless of the degree or presence of prostatomegaly. The urination disorder-improving agent contains a 2-oxapregnane compound represented by the following formula (1) as an active ingredient. (In the formula, R1 to R3 represent an alkyl group such as methyl group, R4 represents an alkylcarbonyl group such as acetyl group, X represents a halogen atom such as a chlorine atom, Y represents a hydroxyl group or oxo group bonded to the 11-position, 15-position, or 16-position of the steroid skeleton.)