Wuhan Ll Science and Technology Development Co., Ltd.

Xiaodan Guo

Li Liu

Chaodong Wang

Yongkai Chen

Jun Lou

Lina Qian

Junhua Liu

Yihan Zhang

Wei Peng

Certain compounds are lysophosphatidic acid receptor antagonists have high LPAR1 antagonist activity and selectivity, low toxicity, good metabolic stability, promising pharmaceutical development prospects, and may be used for preventing or treating LPAR1-related diseases or illnesses. The IC50 values of some of the compounds may be as low as 300 nM or below, even 50 nM or below. In addition, CC50 value range of the compounds may be as high as 200 μM or above. Furthermore, the compounds have good metabolic stability in humans, mice and rats.

Lysophosphatidic acid receptor antagonist and preparation method therefor

Certain triazole compounds have good LPAR1 antagonistic activity and selectivity, low toxicity, and good metabolic stability, and can be used for preventing or treating the LPAR1-related disease or disorder. The ICvalue of some triazole compounds can be below 300 nM, even 50 nM. The range of CCof the triazole compounds can be greater than 200 μM. They also show good metabolic stability in human, fancy rats, and house mice.

Triazole compounds and preparation method therefor and use thereof

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Hubei, China

Xiaodan Guo