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Novel urate transporter 1 (URAT1) inhibitors: a review of recent patent literature (2016-2019).
Expert Opin Ther Pat 2019; 29(11):871-879EO

Abstract

Introduction: Human urate transporter 1 (URAT1), which is an influx transporter protein, is located at the apical surface of renal tubular cells and presumed to be the major transporter responsible for the reabsorption of urate from blood. About 90% of patients develop hyperuricemia due to insufficient urate excretion; thus, it is important to develop URAT1 inhibitors that could enhance renal urate excretion by blocking the reabsorption of urate anion. Areas covered: In this review, the authors addressed the patent applications (2016-2019) about URAT1 inhibitors and some medicinal chemistry strategies employed in these patents. Expert opinion: Substituent decorating, bioisosterism, and scaffold hopping are three common medicinal chemistry strategies used in the discovery of URAT1 inhibitors. Meanwhile, the introduction of sulfonyl group into small molecules has become one of the important strategies for structural optimization of URAT1 inhibitors. Furthermore, developing drug candidates targeting both URAT1 and xanthine oxidase (XOD) has attracted lots of interest and attention.

Authors+Show Affiliations

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University , Jinan , Shandong , PR China.Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University , Jinan , Shandong , PR China.Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University , Jinan , Shandong , PR China.Department of Pharmacy, Faculty of Health Science, American University of Madaba , Amman , Jordan.Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University , Jinan , Shandong , PR China.Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University , Guangzhou , Guangdong , China.Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University , Jinan , Shandong , PR China.Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University , Jinan , Shandong , PR China.

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

31593642

Citation

Dong, Yue, et al. "Novel Urate Transporter 1 (URAT1) Inhibitors: a Review of Recent Patent Literature (2016-2019)." Expert Opinion On Therapeutic Patents, vol. 29, no. 11, 2019, pp. 871-879.
Dong Y, Zhao T, Ai W, et al. Novel urate transporter 1 (URAT1) inhibitors: a review of recent patent literature (2016-2019). Expert Opin Ther Pat. 2019;29(11):871-879.
Dong, Y., Zhao, T., Ai, W., Zalloum, W. A., Kang, D., Wu, T., ... Zhan, P. (2019). Novel urate transporter 1 (URAT1) inhibitors: a review of recent patent literature (2016-2019). Expert Opinion On Therapeutic Patents, 29(11), pp. 871-879. doi:10.1080/13543776.2019.1676727.
Dong Y, et al. Novel Urate Transporter 1 (URAT1) Inhibitors: a Review of Recent Patent Literature (2016-2019). Expert Opin Ther Pat. 2019;29(11):871-879. PubMed PMID: 31593642.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Novel urate transporter 1 (URAT1) inhibitors: a review of recent patent literature (2016-2019). AU - Dong,Yue, AU - Zhao,Tong, AU - Ai,Wei, AU - Zalloum,Waleed A, AU - Kang,Dongwei, AU - Wu,Ting, AU - Liu,Xinyong, AU - Zhan,Peng, Y1 - 2019/10/14/ PY - 2019/10/9/pubmed PY - 2019/11/8/medline PY - 2019/10/9/entrez KW - RDEA3170 KW - SHR4640 KW - URAT1 inhibitors KW - benzbromarone KW - dual inhibitor KW - gout KW - hyperuricemia KW - lesinurad KW - sulfonamide SP - 871 EP - 879 JF - Expert opinion on therapeutic patents JO - Expert Opin Ther Pat VL - 29 IS - 11 N2 - Introduction: Human urate transporter 1 (URAT1), which is an influx transporter protein, is located at the apical surface of renal tubular cells and presumed to be the major transporter responsible for the reabsorption of urate from blood. About 90% of patients develop hyperuricemia due to insufficient urate excretion; thus, it is important to develop URAT1 inhibitors that could enhance renal urate excretion by blocking the reabsorption of urate anion. Areas covered: In this review, the authors addressed the patent applications (2016-2019) about URAT1 inhibitors and some medicinal chemistry strategies employed in these patents. Expert opinion: Substituent decorating, bioisosterism, and scaffold hopping are three common medicinal chemistry strategies used in the discovery of URAT1 inhibitors. Meanwhile, the introduction of sulfonyl group into small molecules has become one of the important strategies for structural optimization of URAT1 inhibitors. Furthermore, developing drug candidates targeting both URAT1 and xanthine oxidase (XOD) has attracted lots of interest and attention. SN - 1744-7674 UR - https://www.unboundmedicine.com/medline/citation/31593642/Novel_urate_transporter_1_(URAT1)_inhibitors:_a_review_of_recent_patent_literature_(2016-2019) L2 - http://www.tandfonline.com/doi/full/10.1080/13543776.2019.1676727 DB - PRIME DP - Unbound Medicine ER -