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. 2025 Aug 13;20(8):e0328559.
doi: 10.1371/journal.pone.0328559. eCollection 2025.

Gout management: Patent analytics and computational drug design explores URAT1 inhibitors landscape

Jiaxin Zhang  1   2   3   4 , Liang Hong  1   2   3   4 , Wenfei Xu  1   2   3   4 , Xin Zhang  1   2   3   4 , Huina Fu  1   2   3   4 , Xinan Song  1   2   3   4 , Jing Zhao  1   2   3   4
Affiliations

Gout management: Patent analytics and computational drug design explores URAT1 inhibitors landscape

Jiaxin Zhang et al. PLoS One. .

Abstract

Gout, caused by hyperuricemia, has a detrimental impact on patients'quality of life. The urate transporter 1 (URAT1) stands out as a key therapeutic target. However, its clinical development remains uncertain. This study aims to explore the landscape of URAT1 inhibitors by combining global patent analytics with computational drug design. We utilized the Derwent Innovation platform to analyze patents (from 2005 to 2024). Molecular docking was performed on 73.96% of novel compounds using AutoDock Vina. Additionally, scaffold diversity was analyzed using the Bemis-Murcko (BM) scaffold approach. A total of 2,195 entries were screened and eventually narrowed down to 1,056 high-value entries. The global research on URAT1 inhibitors is highly active, with China, the US, Japan, and Europe leading. Most patents are new compounds, indicating significant potential for novel drug development. Molecular docking showed ideal binding affinities for most compounds. The top five BM scaffolds were identified and compared with marketed drugs. This study highlights the potential for developing new URAT1 inhibitors. The identified compounds and scaffolds offer promising starting points for further drug development. Future work should focus on experimental validation and exploring clinical potential.

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Conflict of interest statement

The authors have declared that no competing interests exist.

Figures

Fig 1
Fig 1. Patent screening process flow chart.
Fig 2
Fig 2. Annual distribution of patent disclosures related to global URAT1 inhibitors.
Fig 3
Fig 3. Comparison of the number of published patents in each country/regions.
Fig 4
Fig 4. Changes in the number of patents from the top ten published countries/regions over the years.
Fig 5
Fig 5. Sources of patent holders in the top ten countries/regions with the number of published atents.
Fig 6
Fig 6. Changes in technology types by year in the world (A) and in China (B).
Fig 7
Fig 7. The connection mode between compound 1 in Table 3 and URAT1 protein.
Fig 8
Fig 8. Chemical structures of 16 compounds with binding free energies of less than −9 kcal/mol to URAT1 protein.
Fig 9
Fig 9. The chemical structures of the top five BM scaffolds.
Fig 10
Fig 10. Citation relationship diagram between patent families.
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