SGLT2 Inhibitor Composition for Renal Hyperfiltration

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Solution Overview

Problem

Current methods fail to effectively prevent or treat renal hyperfiltrative injury, which is an early manifestation of renal damage and a risk factor for end-stage renal disease, particularly in patients with diabetes and other metabolic disorders.

Innovation Solution

Administration of a pharmaceutical composition containing the SGLT2 inhibitor 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene or its prodrug to patients with conditions such as diabetes mellitus, chronic kidney disease, and renal transplant recipients, to slow the progression or treat renal hyperfiltrative injury.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional treatments are used for renal hyperfiltrative injury, then general renal protection may be achieved, but effective prevention or treatment of renal hyperfiltrative injury is not achieved

Engineering Contradiction:

Improveeffectiveness in preventing/treating renal hyperfiltrative injuryVSAvoidspecific efficacy for hyperfiltrative stage

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies parameter changes by modifying the SGLT2 inhibitor molecule to create compound (I) with specific structural features (R1, R2, R3 substituents) that enhance its effectiveness specifically for renal hyperfiltrative injury while maintaining general renal protective effects

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent segments the treatment approach by specifically targeting the hyperfiltrative stage of renal damage with a specialized compound formulation, distinguishing it from general renal protection approaches

Inventive Principle:

Principle #1Segmentation

2Reliability

If SGLT2 inhibitor is administered to reduce renal hyperfiltration, then renal damage progression is delayed, but glycemic control mechanism requires glucose excretion through urine

Engineering Contradiction:

Improvedelay of renal damage progressionVSAvoidglucose excretion through urine

Core Design Contradiction:

ReliabilityVSLoss of substance

Solution Approach 1:

The patent converts the potentially harmful effect of glucose loss through urine into a beneficial therapeutic mechanism. By inhibiting SGLT2, the compound promotes glucose excretion which simultaneously achieves glycemic control and reduces renal hyperfiltration, transforming what could be seen as a waste loss into a therapeutic benefit

Inventive Principle:

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

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 SGLT2 inhibitor composition effectively reduces renal hyperfiltration, delaying the progression of renal damage and improving glycemic control by excreting excessive glucose through urine, thereby reducing the risk of further renal complications.

Implementation Method 1

a pharmaceutical composition comprising an SGLT2 inhibitor is administered to the patient, wherein the SGLT2 inhibitor is 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene

Methodology Applied

Scientific EffectSGLT2 inhibition:

Data Source

PatentUS20230405032A1Pharmaceutical composition, methods for treating and uses thereof

Publication Date: 2023.12.21 BOEHRINGER INGELHEIM INT GMBH

AI summary

The invention relates to the treatment or prevention of renal impairment and/or complications using a SGLT-2 inhibitor, for example in patients diagnosed with metabolic disorders and related conditions.