- Discovery of a flexible triazolylbutanoic acid as a highly potent uric acid transporter 1 (URAT1) inhibitor
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In order to systematically explore and understand the structure-activity relationship (SAR) of a lesinurad-based hit (1c) derived from the replacement of the S atom in lesinurad with CH2, 18 compounds (1a-1r) were designed, synthesized and subjected to in vitro URAT1 inhibitory assay. The SAR exploration led to the discovery of a highly potent flexible URAT1 inhibitor, 1q, which was 31-fold more potent than parent lesinurad (IC50 = 0.23 μM against human URAT1 for 1q vs. 7.18 μM for lesinurad). The present study discovered a flexible molecular scaffold, as represented by 1q, which might serve as a promising prototype scaffold for further development of potent URAT1 inhibitors, and also demonstrated that the S atom in lesinurad was not indispensable for its URAT1 inhibitory activity.
- Tian, He,Liu, Wei,Zhou, Zhixing,Shang, Qian,Liu, Yuqiang,Xie, Yafei,Liu, Changying,Xu, Weiren,Tang, Lida,Wang, Jianwu,Zhao, Guilong
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- DIAMINE COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE INCLUDING THE SAME
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Provided are a diamine compound and an organic light-emitting device including the same. The organic light-emitting device includes: a first electrode; a second electrode; and an organic layer between the first electrode and the second electrode and comprising an emission layer, the organic layer including a diamine compound represented by one selected from Formulae 1-1 to 1-8.
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Paragraph 0465-0467
(2020/01/12)
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- Organic light-emitting device including diamine compound and diamine compound
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The present invention provide a diamine compound and an organic light-emitting device including the same. The organic light-emitting device includes: a first electrode; a second electrode; and an organic layer between the first electrode and the second electrode and comprising an emission layer, the organic layer including a diamine compound represented by one selected from Formulae 1-1 to 1-8.
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Paragraph 0553-0557
(2020/01/08)
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- Thiophene derivatives used as inhibitor of URAT1
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The invention relates to thiophene derivatives used as an inhibitor of urate transporter 1 (URAT1), in particular relates to the thiophene derivatives represented by a general formula (I) shown in thedescription, a pharmaceutically-acceptable salt of the thiophene derivatives, and preparation methods of the thiophene derivatives and the pharmaceutically-acceptable salt, and particularly relates to an application of the thiophene derivatives and the pharmaceutically-acceptable salt used as a therapeutic agent for a disease associated with an abnormal uric acid level.
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Paragraph 0133; 0135; 0136; 0137
(2019/04/26)
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- Composite taken as URAT 1 inhibitor
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The invention provides a series of composite with a formula (I), wherein n is selected from 1, 2 or 3, X is selected from O or S, Q is selected from C or N, and R is selected from H, halogen or -C1-6.The composite can be used as the URAT 1 inhibitor and can be used for treating hyperuricemia and gout.
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Paragraph 0019; 0020
(2018/05/16)
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