A patent review of galectin-1 and galectin-3 inhibitors and their potential therapeutic applications (2022-present): an update

The patent landscape is dominated by β-D-galactopyranose and thiodigalactoside scaffolds, with limited innovation and unresolved issues in selectivity, drug-likeness, and efficacy, highlighted by GB0139's Phase II failure. Moreover, only a few patents provide structural evidence and strong in vitro/in vivo data, limiting confidence in their therapeutic outcome. By contrast, some diversification has emerged, including spirocyclic sugars, ruthenium-conjugates and non-carbohydrate ligands such as heterocycles and repurposed drugs. These highlight underexploited avenues with promise. Yet, robust biochemical data and structural proof of binding remain scarce. To move the field forward, future patents must diversify chemotypes, substantiate binding modes with crystallography or NMR, and demonstrate translation in relevant disease models.