Urate transporter URAT1 inhibitors: a patent review (2012 - 2015)

ABSTRACT

Introduction: Human urate transporter 1 (URAT1, encoded by SLC22A12) has been identified as a key urate transporter expressed at the apical membrane of renal proximal tubule cells for regulating urate homeostasis. Therefore, URAT1 is an attractive target for the development of new uricosurics against hyperuricemia. Discovery of novel inhibitors targeting URAT1 has become a research hotspot in recent years.

Areas covered: In this paper, we reviewed the patent applications and related research published during the years 2012–2015, covering the development of URAT1 inhibitors.

Expert opinion: There are some promising and inspiring patent applications in this area. Several compounds have superior inhibitory activity of URAT1 with the availability of urate-lowering treatment. For new drug development and commercialization, further studies are needed to evaluate the efficacy and safety.

KEYWORDS:

• URAT1 inhibitors
• uricosurics
• urate
• hyperuricemia

Article highlights

• New compounds with URAT1 inhibitory property and their preparation.

• New screening methods based on expanded concept of URAT1 inhibitors.

• Recent development of URAT1 inhibitors.

This box summarizes key points contained in the article.

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Additional information

Funding

This work has been supported by grants from the National Basic Research Program of China 973 Program No. 2012CB617600 [2012CB617602] and the Program for Changjiang Scholars and Innovative Research Team in University [IRT_14R27].