GPR132 Modulator Structures for Broader Disease Coverage
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Solution Overview
Problem
There is a need for a new type of GPR132 agonist effective in treating diseases such as atherosclerosis, colorectal inflammation, and leukemia, or in treatment approaches like bone marrow transplantation.
Innovation Solution
A GPR132 modulator with a new structural compound, including specific ring and substituent configurations, is developed to address these conditions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing GPR132 agonists are used, then some therapeutic effects are achieved, but they are insufficient for treating diseases such as atherosclerosis, colorectal inflammation, and leukemia
Solution Approach 1:
The patent modifies the chemical structure parameters of GPR132 agonists by changing the core ring structure (benzofuran, benzothiophene, indole, or benzene) and varying substituent groups (R0-R4, R4′) to create a series of compounds with different biological activities and disease-specific efficacies
Solution Approach 2:
The patent combines multiple structural elements (core ring A, substituent R0 with heteroaryl group, linker L1-L3, and terminal group R4′) to create composite molecular structures that achieve enhanced and diversified therapeutic effects across multiple disease types
2Adaptability or versatility
If a new GPR132 agonist is developed, then broader disease treatment capability is achieved, but the structural complexity increases
Solution Approach 1:
The patent divides the GPR132 agonist molecule into distinct functional segments: core ring A (providing basic structure), substituent R0 (providing heteroaryl group), linker L1-L3 (providing connection), and terminal group R4′ (providing additional functionality), allowing systematic optimization of each segment for different disease indications
Data Source
AI summary
The present invention relates to a GPCR modulator and use thereof, and particularly provides a compound represented by Formula (I), or a stereoisomer, a prodrug, a crystal form, a pharmaceutically acceptable salt, a pharmaceutically acceptable solvate or a pharmaceutically acceptable ester of the compound.