GPR146 Small-Molecule Modulators for Simpler Lipid-Lowering Therapy
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current drug candidates for GPR146, such as antibodies, oligonucleotides, and proteins, involve complex and costly synthesis and purification steps, necessitating a need for small molecule drug compounds to treat cardio-metabolic diseases associated with GPR146.
Innovation Solution
Development of small molecule compounds, specifically those of Formula (I) or its pharmaceutically acceptable forms, to inhibit GPR146 activity, thereby treating diseases like hyperlipidedia, coronary artery disease, liver inflammation, obesity, and hypertension.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If antibodies, oligonucleotides, or proteins are used as GPR146 drug candidates, then therapeutic effect is achieved, but synthesis and purification steps become complicated and costly
Solution Approach 1:
The patent employs small molecule compounds as GPR146 inhibitors, replacing complex biological therapeutics (antibodies, oligonucleotides, proteins) with simpler, more cost-effective chemical entities. These small molecules require straightforward synthesis procedures and do not demand elaborate purification processes, thereby reducing manufacturing complexity and cost while maintaining therapeutic efficacy through direct GPR146 inhibition
Solution Approach 2:
The invention transitions from macromolecular therapeutics to small molecule inhibitors, fundamentally changing the molecular size and structural complexity parameters. This parameter change enables the use of conventional organic synthesis methods rather than complex biotechnological processes, simplifying production while achieving the same therapeutic outcome through GPR146 inhibition
2Ease of manufacture
If small molecule compounds are developed to inhibit GPR146, then synthesis and purification steps are simplified and cost is reduced, but therapeutic efficacy must be maintained
Solution Approach 1:
The patent designs small molecule compounds that mimic the binding and inhibitory characteristics of natural GPR146 ligands or antibodies. By copying the essential pharmacological function of macromolecular therapeutics into a small molecule format, the invention maintains therapeutic efficacy while achieving simplified manufacturing. The small molecules are structured to specifically target and inhibit GPR146, reproducing the therapeutic effect of complex biologics through a much simpler chemical framework
Data Source
AI summary
The present disclosure concerns a method of treating a disease and/or condition associated with GPR146 in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt, solvate, stereoisomer or prodrug thereof:wherein R1 is selected from H, halo, cyano, optionally substituted alkyl, and optionally substituted alkenyl; R2 is selected from H, halo, cyano, optionally substituted alkyl, and optionally substituted alkenyl; R3 is selected from optionally substituted aryl and optionally substituted heteroaryl; R4 is selected from optionally substituted alkyl and optionally substituted alkenyl; R5 is selected from optionally substituted cycloalkyl and optionally substituted heterocyclyl. The present disclosure also concerns a pharmaceutical composition comprising a compound of Formula (I).