GPCR Modulator Compounds With Improved Solubility and Delivery

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Solution Overview

Problem

Existing GPCR ligands face challenges with high lipophilicity and low water solubility, limiting their clinical development and efficacy in treating various medical conditions.

Innovation Solution

Development of compounds, such as those in Formula IA and Formula IB, which modulate G-Protein-Coupled Receptors, along with their salts, prodrugs, and metabolites, formulated in pharmaceutical compositions to improve solubility, stability, and delivery systems for targeted tissue concentration and safety, including formulations like nanoparticles and liposomes.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing GPCR ligands are used, then GPCR modulation activity is achieved, but water solubility is poor and clinical development is limited

Engineering Contradiction:

ImproveGPCR modulation activityVSAvoidwater solubility

Core Design Contradiction:

ReliabilityVSQuantity of substance

Solution Approach 1:

The patent modifies the chemical structure of GPCR ligands by introducing polar functional groups (hydroxyl, carboxyl, amino groups) and adjusting molecular weight parameters. These parameter changes increase water solubility while maintaining GPCR binding affinity, directly resolving the contradiction between activity and solubility

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent creates composite pharmaceutical formulations combining GPCR ligands with solubility-enhancing excipients, surfactants, and delivery vehicle components. This composite approach maintains the pharmacological activity of the active ingredient while improving overall water solubility and clinical developability

Inventive Principle:

Principle #40Composite materials

2Strength

If lipophilic GPCR ligands are used, then receptor binding affinity is improved, but delivery to target tissues and safety are compromised

Engineering Contradiction:

Improvereceptor binding affinityVSAvoiddelivery to target tissues

Core Design Contradiction:

StrengthVSEase of operation

Solution Approach 1:

The patent introduces amphipathic molecular structures with localized hydrophobic regions for receptor binding and hydrophilic regions for aqueous solubility and tissue delivery. This local differentiation of properties allows the molecule to maintain high binding affinity while improving delivery characteristics

Inventive Principle:

Principle #3Local quality

Solution Approach 2:

The patent employs delivery vehicles (liposomes, nanoparticles, micelles) as intermediary systems that carry lipophilic GPCR ligands through aqueous biological environments to target tissues. The intermediary protects the ligand's lipophilic nature while enabling improved delivery and safety profiles

Inventive Principle:

Principle #24Intermediary (Mediator)

Data Source

PatentUS20260001881A1Compounds and methods for modulation of g-protein-coupled receptors

Publication Date: 2026.01.01 PRIMETIME LIFE SCIENCES LLC

AI summary

The present invention relates to compounds that modulate G-Protein-Coupled Receptors, to process of preparing these compounds, their salts, prodrugs, and metabolites, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of medical conditions, diseases or disorders.