公开(公告)号：EP4029863A1

公开(公告)日：2022-07-20

申请号：EP20863682.9

申请日：2020-09-09

申请人： INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF MEDICAL SCIENCES

发明人： FENG, Zhiqiang ,  CHEN, Xiaoguang ,  MA, Chen ,  YANG, Yang ,  LAI, FangFang ,  WANG, Yuchen ,  JI, Ming ,  GUO, Kaijing

IPC分类号： C07D405/14 ,  C07D207/16 ,  A61K31/44 ,  A61P35/00 ,  A61P31/04 ,  A61P31/12 ,  A61P37/02

摘要： 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.

公开(公告)号：EP3459926A1

公开(公告)日：2019-03-27

申请号：EP17802122.6

申请日：2017-05-23

申请人： Institute of Materia Medica, Chinese Academy of Medical Sciences

发明人： FENG, Zhiqiang ,  CHEN, Xiaoguang ,  YANG, Yang ,  ZHOU, Chuan ,  LAI, Fangfang ,  JI, Ming ,  JIN, Xiaofeng ,  XUE, Nina ,  ZHENG, Yi ,  CHEN, Hao ,  LI, Ling

IPC分类号： C07C43/174 ,  C07C43/235 ,  C07D319/16 ,  A61K31/03 ,  A61K31/075 ,  A61K31/357 ,  A61P35/00

摘要： 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.

公开(公告)号：EP3466944A1

公开(公告)日：2019-04-10

申请号：EP17802120.0

申请日：2017-05-23

申请人： Institute of Materia Medica, Chinese Academy of Medical Sciences

发明人： FENG, Zhiqiang ,  CHEN, Xiaoguang ,  YANG, Yang ,  ZHENG, Yi ,  LAI, Fangfang ,  JI, Ming ,  ZHOU, Chuan ,  ZHANG, Lijing ,  WANG, Ke ,  XUE, Nina ,  LI, Ling

IPC分类号： C07D405/14 ,  C07D207/16 ,  A61K31/40 ,  A61K31/44 ,  A61P35/00 ,  A61P31/04 ,  A61P31/12 ,  A61P37/02

摘要： 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.

公开(公告)号：EP3450423A1

公开(公告)日：2019-03-06

申请号：EP17802119.2

申请日：2017-05-23

申请人： Institute of Materia Medica, Chinese Academy of Medical Sciences

发明人： FENG, Zhiqiang ,  CHEN, Xiaoguang ,  YANG, Yang ,  LAI, Fangfang ,  JI, Ming ,  ZHANG, Lijing ,  ZHENG, Yi ,  XUE, Nina ,  WANG, Ke ,  LI, Ling

IPC分类号： C07C255/54 ,  C07C233/36 ,  C07C311/05 ,  C07D319/18 ,  C07D405/12 ,  A61K31/277 ,  A61K31/36 ,  A61K31/165 ,  A61P35/00 ,  A61P31/00 ,  A61P37/00

摘要： 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.

公开(公告)号：EP3459925A1

公开(公告)日：2019-03-27

申请号：EP17802123.4

申请日：2017-05-23

申请人： Institute of Materia Medica, Chinese Academy of Medical Sciences

发明人： FENG, Zhiqiang ,  CHEN, Xiaoguang ,  YANG, Yang ,  LAI, Fangfang

IPC分类号： C07C41/09 ,  C07C43/184 ,  C07C17/14 ,  C07C47/565 ,  C07C15/16 ,  C07D319/14

摘要： 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-dihdrox-5-substituted benzaldehyde 6.