Hitgen, Inc.

Jin Li

Dengfeng Dou

Jinqiao Wan

Jingchao Feng

Dengyou Zhang

Wei Jun Zhang

Hongmei Song

Guoqing Zhong

Yan Zhang

Wei Chen

Fei Pan

Jing Hu

Linli Li

Rong Ma

Wei Zhang

Wenji Zhu

Xin Chen

Yang Chen

Xing Wang

Xiao Hu

Zhi Wang

Wei Liao

Lina Zhong

Kai Xu

Xueming Li

Peng Lv

Jingming Li

Yan Lan

Leichang Pan

Li Lin

Si Li

Xiaohu Ge

Benyanzi Yang

Guansai Liu

Shaojun Liu

Yun Mu

Xincheng Liu

Caikui Li

Jian Gao

Yanshan Xu

Barry A Morgan

Yong Chang

Dongyan Hu

Jian Liu

Xuemin Cheng

Weiping Liu

Qiuxia Chen

Xinfu Hong

Xiaoguang Bai

Xiansi Zhou

Qingran Li

Disclosed is a macrocyclic kinase inhibitor, wherein the compound, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof is as shown in formula I. Experiments show that the new compound as shown in formula I disclosed in the present invention exhibits an excellent TRK inhibitory activity, has a significant inhibitory effect on TRKA-mutant cell growth, and exhibits an excellent inhibitory effect on in vivo tumor growth, thus providing a new choice for the clinical treatment of diseases associated with abnormal TRK activity.

Macrocyclic kinase inhibitor

The present invention discloses a compound shown in formula I or a stereoisomer, pharmaceutically acceptable salt, crystal form, solvate or isotopologue thereof. The compound of the present invention shows excellent inhibition activity against histone deacetylases, has remarkable inhibition effects on cancer cells, and provides a new choice of drugs used for the clinic treatment and diseases related to the abnormal activity of histone deacetylases. 

Sulfamide derivatives and preparation method and use thereof

Disclosed herein are a compound of formula (I) and a preparation method and uses thereof. The compound shows a good inhibitory activity against ROCK, providing a new medicinal strategy to clinically treat the diseases associated with abnormal ROCK activity. 

Rock-inhibiting compound and uses thereof

The present invention provides a method of solid-phase synthesis of DNA-encoded compound library. The method includes following steps: a) reacting solid carrier G-1 with linker molecule L-1 to prepare L-G-1; b) reacting DNA with linker molecule L-0 to prepare L-2; c) reacting L-G-1 with L-2 to prepare L-G-2; d) removing protection group of the L-G-2 and obtaining L-G-2-1; e) reacting the L-G-2-1 with synthetic building block and performing DNA encoding; and f) removing the solid carrier and obtaining the DNA-encoded compound library. Compared with the prior art, the present invention can complete post-treatment purification of the reaction only by filtration and irrigation processes for several times. The present invention is simple to operate, can shorten the production cycle of DNA encoded compound library with more than 50%, significantly increases the production efficiency and the unicity as well as the purity of the final products.

Method for solid-phase synthesis of DNA encoded compound library

The present invention discloses a pyrrolic amide compound shown as a formula I, or crystal forms thereof, and pharmaceutically acceptable salts, hydrates or solvates, wherein Ris selected from hydrogen, hydroxyl, cyano, halogen, carboxyl, C-Calkyl and the like; Ris selected from hydrogen, hydroxyl, cyano, halogen and the like; Ris selected from hydroxyl and the like; X is selected from group, m is equal to 0, 1, 2 or 3, and n is equal to 0, 1 or 2. The novel compound shown as the formular I provided by the present invention has high deacetylase inhibitory viability; and meanwhile, a method for preparing the novel compound in the present invention has the advantages of fewer steps, simple and convenient operation, safety, environment friendliness, high yield and the like and is very suitable for industrial application. 

Pyrrolic amide compound and preparation method and application thereof

The present invention discloses a method for capturing drug targets, comprising the following steps of: (1) preparing row materials, i.e., compounds and DNA or RNA or one party of other specific affinity materials; (2) linking: covalently linking the compounds to the DNA or RNA or the one party of other specific affinity materials, to obtain labeled compounds; (3) transferring: transferring the labeled compounds obtained in the step (2) into cells by a specific gene transfer method; (4) capturing targets: disrupting the cells in the step (3), and then capturing the DNA or RNA in the step (1) by immobilized complementary DNA or RNA, or capturing the one party of affinity materials in the step (1) by the other party of immobilized specific affinity materials, thus to enrich the targets through the covalently linked labeled compounds and the affinity of the targets; (5) identifying targets: dissociating the enriched targets from a stationary phase, deploying the targets by a gel electrophoresis method or by an equivalent separation method, and comparing differential proteins by proteomics thus to identify the potential targets; and (6) determining targets: expressing or purchasing the targets identified in the step (5) by priority, and comparing by interaction of the compounds with those targets one by one to determine the targets for the compounds. By the method of the present invention, compounds with low membrane permeability may be transferred into cells to be bound with the targets in the cells, to realize the target identification closer to the real physiological environment and thus provide more conclusive evidences for the acting mechanism of the compounds to diseases. Additionally, the method for capturing drug targets of the present invention is novel, easy, efficient, and low in cost, and has good application prospects.

Drug target capturing method

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Sichuan, China

Jin Li