China Pharmaceutical University

Jiangsu Hengrui Medicine Company Ltd.

China Tobacco Yunnan Industrial Co., Ltd

Xiaoli Xu

Qidong You

Xiaoke Guo

Zhengyu Jiang

Mengchen Lu

Jing Zhao

Haopeng Sun

Xiaojin Zhang

Lei Wang

Yongkuan Chen

Shanzhai Shang

Ping Lei

Jingmei Han

Zhiqiang Li

Chengya Wang

Ru Wang

Yang Su

Xudong Zheng

Jianguo Tang

Yan Wang

Zhihua Liu

Jun Wu

Liu Hong

Dongdong Li

Xin Chen

Weilin Chen

Yifan Wang

Pei He

Weimin Gong

Xian Zhang

Lingxuan Liu

Deshou Mao

Yuting Liu

Jing Gu

Hongli Shao

Jun Xu

Yuhui Jin

Yuanchun Dou

Zhiyun Chen

Xingsen Wu

Tianhan Hu

Yonghua Lei

Dongye Cao

Wen Yang

Jinghui Cheng

Xiaolong Ma

The present disclosure discloses a WDR5 protein-protein interaction inhibitor, including a compound having a structure represented by general formula (I). Experiments show that the inhibitor acts on a WDR5 protein and an interacting protein thereof including, but not limited to, MLL, selectively inhibits the proliferation of leukemia cells, and inhibits the methylation of H3K4 and the expression of downstream Hox/Meis-1 gene at the cellular level. The present disclosure also discloses a method for preparing the inhibitor and use thereof in the preparation of a drug for treating acute leukemia and other related diseases.

Aniline-based WDR5 protein-protein interaction inhibitor, and preparation method and use thereof

The present application relates to a hydrogen peroxide-responsive Keap1-Nrf2 PPI inhibitor prodrug, and a preparation method therefor. The hydrogen peroxide-responsive Keap1-Nrf2 PPI inhibitor prodrug pro2 has a chemical structure as shown below. By modifying a key carboxyl pharmacophore in a Keap1-Nrf2 inhibitor with a HO-responsive thiazolidinone moiety, a novel ROS-responsive antioxidant prodrug pro2 is synthesized. The HOactivated prodrug pro2 can simultaneously achieve targeted activation of Nrf2 and enhancement of therapeutic efficacy in the body. The prodrug is based on the concept of ROS activation-ROS clearance therapy, is the first example of a HO-responsive prodrug suitable for oral administration, and is expected to be used clinically by virtue of the characteristics of druggability and high targeting ability.

Hydrogen peroxide-responsive KEAP1-NRF2 ppi inhibitor prodrug, and preparation method therefor

Disclosed in the present invention are a naphthalenesulfonamide compound, a preparation method, and an application. The naphthalenesulfonamide compound provided by the present invention can interfere with Keap1-Nrf2 binding and activate Nrf2 to relieve inflammatory damage and improve an inflammatory microenvironment, has a potential anti-inflammatory activity, and can be used for preparing an anti-inflammatory drug for inflammatory damage of various inflammation-related diseases, including chronic obstructive pulmonary disease (COPD), Alzheimer's disease, Parkinson's disease, atherosclerosis, chronic kidney disease (CKD), diabetes, intestinal Inflammations, rheumatoid arthritis, etc.

Naphthalenesulfonamide compound, preparation method, and application

It discloses a proteolysis targeting chimeric molecule, a preparation method and an application thereof. The proteolysis targeting chimeric molecule provided by the disclosure can inhibit the expression of BCR-ABL and/or CRBN protein in BCR-ABL and/or CRBN positive leukemia K562 cells to varying degrees, and thus can be used to prepare drugs for treating BCR-ABL and/or CRBN positive leukemia, wherein the proteolysis targeting chimeric molecule with n=3 has excellent photo-isomerization activity, and can be used in preparation of the reagents or drugs for light-regulated degradation of BCR-ABL and/or CRBN protein. The disclosure also provides a method for synthesizing the series of proteolysis targeting chimeric molecules.

Proteolysis targeting chimeric molecule, preparation method, and application

A modified carbon material, including a carbonaceous material and a water-insoluble modifier combined with the carbonaceous material, wherein the water-insoluble modifier is CuO, the carbonaceous material is one of or a mixture of biomass carbon or carbon black, a mass of the water-insoluble modifier is being 0.1-10 wt % of the carbonaceous material. The method for preparing the modified carbon material includes: (1) soaking the carbonaceous material in a copper sulfate solution for 5 to 36 hours, and (2) adding an alkali solution into a solution obtained in step (1) to provide a pH value &#x2265;12, and after keeping the pH value for 0.5 to 2 hours, filtering and drying to obtain a solid. (3) using the carbonaceous material as a combustion heat source to reduce the ignition temperature, increase or reduce the peak thermal power temperature.

Modified carbon material and method for reducing carbonaceous material ignition temperature

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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Nanjing, China

Xiaoli Xu