- Discovery of potent and orally bioavailable inhibitors of Human Uric Acid Transporter 1 (hURAT1) and binding mode prediction using homology model
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This Letter describes the discovery of a series of potent inhibitors of Human Uric Acid Transporter 1 (hURAT1). Lead generation and optimization via 3D pharmacophore analysis resulted in compound 41. With an IC50 of 33.7 nM, 41 also demonstrated good oral bioavailability in rat (74.8%) and displayed a consistent PK profile across all species tested (rat, dog and monkey).
- Peng, Jianbiao,Hu, Qiyue,Gu, Chunyan,Liu, Bonian,Jin, Fangfang,Yuan, Jijun,Feng, Jun,Zhang, Lei,Lan, Jiong,Dong, Qing,Cao, Guoqing
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- THYROID HORMONE RECEPTOR BETA AGONIST COMPOUNDS
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Provided herein are compounds, preferably thyroid hormone receptor beta (THR beta) agonist compounds, compositions thereof, and methods of their preparation, and methods of agonizing THR beta and methods for treating disorders mediated by THR beta.
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Paragraph 0326
(2021/03/05)
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- CYCLOALKYL ACID DERIVATIVE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL APPLICATION THEREOF
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The present invention relates to a cycloalkyl acid derivative, a preparation method thereof, and a pharmaceutical application thereof, and in particular, the present invention relates to a cycloalkyl acid derivative represented by general formula (I) and a medical salt thereof, a preparation method thereof, and an application of the cycloalkyl acid derivative and the medical salt thereof as URAT1 inhibitors, and particularly as therapeutic agents for diseases related to an abnormal uric acid level, wherein definitions of substituent groups in general formula (I) are the same as definitions in the specifications.
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Paragraph 0516; 0519-0522
(2016/11/14)
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- CYCLOALKYL ACID DERIVATIVE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL APPLICATION THEREOF
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Cycloalkyl acid derivatives, a preparation method thereof, and a pharmaceutical application thereof are described. In particular, a cycloalkyl acid derivative represented by general formula (I) and a medical salt thereof, a preparation method thereof, and an application of the cycloalkyl acid derivative and the medical salt thereof as URAT1 inhibitors, and particularly as therapeutic agents for diseases related to an abnormal uric acid level are described, wherein definitions of substituent groups in general formula (I) are the same as the definitions in the specification.
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Paragraph 0286-0287
(2016/05/24)
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- Quinoline derivatives as immunostimulants
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This invention relates to compounds of the formula STR1 wherein R1, R2, R3, R4, R5, R6 and R7 are as defined hereinbelow that exhibit activity as immunostimulants.
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