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1. (WO2018161892) BENZENE SULFONAMIDE IDO1 INHIBITOR, PREPARATION METHOD THEREFOR AND USE THEREOF

Pub. No.:    WO/2018/161892    International Application No.:    PCT/CN2018/078136
Publication Date: Fri Sep 14 01:59:59 CEST 2018 International Filing Date: Wed Mar 07 00:59:59 CET 2018
IPC: C07C 311/46
C07C 303/38
C07C 311/19
C07C 311/39
C07C 311/16
C07C 311/17
A61K 31/18
A61K 31/63
A61P 35/00
A61P 31/12
A61P 25/28
Applicants: CHINA PHARMACEUTICAL UNIVERSITY
中国药科大学
NANJING UNIVERSITY
南京大学
Inventors: LAI, Yisheng
赖宜生
GE, Shushan
葛书山
ZHENG, Yingbo
郑英博
ZOU, Yi
邹毅
WANG, Fang
王芳
XU, Qiang
徐强
GUO, Wenjie
郭文洁
WANG, Yan
王燕
HU, Yue
胡月
Title: BENZENE SULFONAMIDE IDO1 INHIBITOR, PREPARATION METHOD THEREFOR AND USE THEREOF
Abstract:
A benzene sulfonamide compound having structural features of formula (I) or a pharmaceutically acceptable salt thereof, a preparation method therefor, and use thereof as an indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor. Experimental results indicate that the compound has a significant inhibitory effect on activities of IDO1, and can effectively promote the proliferation of T cells, inhibit the differentiation of naïve T cells into regulatory T cells, and reverse IDO1-mediated immunosuppression, being able to be used in the treatment of related diseases having pathological features of IDO1-mediated kynurenine metabolic pathways, including cancers, viral infections, neurodegenerative diseases, cataracts, organ transplant rejection, depression, autoimmune diseases and the like.