China Pharmaceutical University

Jiangsu Hengrui Medicine Company Ltd.

Haopeng Sun

Qidong You

Xiaoke Guo

Xiaoli Xu

Xiaojin Zhang

Zhengyu Jiang

Mengchen Lu

Hongyu Yang

Xingsen Wu

Zhiyun Chen

Yao Chen

Feng Feng

Tingkai Chen

Yonghua Lei

Tianhan Hu

Chenxi Du

The present invention discloses a selective butyrylcholinesterase inhibitor having a general formula (I) or a pharmaceutically acceptable salt thereof, a preparation method and use thereof. The treatment efficacy of Alzheimer's disease, especially moderate to severe Alzheimer's disease, is tested through butyrylcholinesterase inhibitory activity, selectivity screening and toxicity to nerve cells as a carrier, and it is found that it has good target activity in vitro, extremely high selectivity and drug safety, can be used as a lead substance for further development of the treatment of Alzheimer's disease by selectively inhibiting butyrylcholinesterase.

Selective butyrylcholinesterase inhibitor or pharmaceutically acceptable salt thereof, preparation method and use thereof

The present invention relates to the field of pharmaceutical chemistry. In particular, the present invention relates to a class of alkynyl pyridine prolyl hydroxylase inhibitors (I). The experiments show that such a compound has good activity of inhibiting prolyl hydroxylase, and can enhance the generation and secretion of erythropoietin in cell or animal models, and thus can promote the generation of red cells, and can be used for the treatment or prevention of anemia, such as chronic kidney disease anemia, and ischemic diseases, including ischemic strokes, myocardial ischemia and other related diseases. The present invention also discloses a method for preparing such a compound.

Alkynyl pyridine prolyl hydroxylase inhibitor, and preparation method and medical use thereof

Compounds of formula (I) having 1-sulfonamido-4-aryloxy as a basic backbone. A preliminary activity test showed that the compounds provide excellent interference of a binding of Nrf2 by Keap1, thereby activating Nrf2. The compounds have a potential anti-inflammatory activity and can be used to treat a plurality of inflammation-associated diseases, including chronic obstructive pulmonary disease (COPD), Alzheimer's disease, Parkinson's disease, atherosclerosis, chronic kidney disease (CKD), diabetes, gastroenteritis, rheumatoid arthritis, and the like. 

1-sulfonamido-4-aryloxy compounds, and preparation method and medicinal application thereof

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Jiangsu, China

Haopeng Sun