Chinese Academy of Sciences

Tianjin Chase Sun Pharmaceutical Co., Ltd

Chinese Academy of Medical Sciences

Zhiqiang Feng

Yang Yang

Xiaoguang Chen

Fangfang Lai

Ming Ji

Yi Zheng

Ling Li

Ke Fei Wang

Hao Chen

Ke Wang

Nina Xue

Chuan Zhou

Lijing Zhang

Yuchen Wang

Chen Ma

Kaijing Guo

Xiaofeng Jin

The present invention relates to the technical field of medicine, and disclosed a maleate of a nicotinyl alcohol ether derivative, a crystal form thereof, and an application thereof, i.e., (S)-N-(2-(pyridin-3-yl-methoxy)-4-(2-bromo-3-phenylbenzyloxy)-5-chlorobenzyl) serine isopropyl ester maleate and a stereoisomer and a crystal form thereof, a preparation method therefor, a pharmaceutical composition, and a use thereof. Specifically, the present invention relates to the (S)-N-(2-(pyridin-3-yl-methoxy)-4-(2-bromo-3-phenylbenzyloxy)-5-chlorobenzyl) serine isopropyl ester maleate represented by formula I, and a crystal form thereof, a stereoisomer thereof, a preparation method therefor, a composition containing said compound or the crystal form thereof, and a use of said compound or the crystal form thereof in the preparation of a medicine for treating diseases related to a PD-1/PD-L1 signaling pathway, such as cancer, infectious diseases and autoimmune diseases.

Maleate of nicotinyl alcohol ether derivative, crystal form thereof, and application thereof

The present invention discloses a nicotinyl alcohol ether derivative, a preparation method therefor, and a pharmaceutical composition and uses thereof. Specifically, the invention relates to nicotinyl alcohol ether derivatives represented by formula (I), a pharmaceutically-acceptable salt thereof, a stereoisomer thereof, a preparation method therefor, a pharmaceutical composition containing the one or more compounds, and uses of the compounds in treating diseases related to PD-1/PD-L1 signal channels, such as cancers, infectious diseases and autoimmune diseases. 

Nicotinyl alcohol ether derivative, preparation method therefor, and pharmaceutical composition and uses thereof

The present invention discloses a benzyl phenyl ether derivative, a preparation method therefor, and a pharmaceutical composition and uses thereof. Specifically, the invention relates to benzyl phenyl ether derivatives represented by formula (I), a pharmaceutically-acceptable salt thereof, a stereoisomer thereof, a preparation method therefor, a pharmaceutical composition containing the one or more compounds, and uses of the compounds in treating diseases related to PD-1/PD-L1 signal channels, such as cancers, infectious diseases and autoimmune diseases. 

Benzyl phenyl ether derivative, preparation method therefor, and pharmaceutical composition and uses thereof

The present invention discloses a phenylate derivative, a preparation method therefor, and a pharmaceutical composition and uses thereof. Specifically, the invention relates to phenylate derivatives represented by formula (I), a pharmaceutically-acceptable salt thereof, a stereoisomer thereof, a preparation method therefor, a pharmaceutical composition containing the one or more compounds, and uses of the compounds in treating diseases related to PD-1/PD-L1 signal channels, such as cancers, infectious diseases and autoimmune diseases. 

Phenylate derivative, preparation method therefor, and pharmaceutical composition and uses thereof

Provided is a method for preparing 2-hydroxy-4-(2, 3-disubstituted benzyloxy)-5-substituted benzaldehyde derivative represented by formula (I). The method comprises the following steps: (1) preparing 3-aryl-2-substituted toluene derivative 2 by using 3-iodo-2-substituted toluene derivative 1 and aryl boronic acid 5 or aryl boronate as starting materials; (2) preparing a benzyl halide derivative 3 by using 3-aryl-2-substituted toluene derivative 2 as starting materials; and (3) preparing 4-(2, 3-disubstituted benzyloxy)-2-hydroxy-5-substituted benzaldehyde derivative (I) by using benzyl halide derivative 3 and 2,4-dihydroxy-5-substituted benzaldehyde 6. 

Method for preparing 2-hydroxyl-4-(2, 3-disubstituted benzyloxy)-5-substituted benzaldehyde derivative

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Beijing, China

Zhiqiang Feng