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Title:
BENZENE SULFONAMIDE IDO1 INHIBITOR, PREPARATION METHOD THEREFOR AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2018/161892
Kind Code:
A1
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.

Inventors:
LAI YISHENG (CN)
GE SHUSHAN (CN)
ZHENG YINGBO (CN)
ZOU YI (CN)
WANG FANG (CN)
XU QIANG (CN)
GUO WENJIE (CN)
WANG YAN (CN)
HU YUE (CN)
Application Number:
PCT/CN2018/078136
Publication Date:
September 13, 2018
Filing Date:
March 06, 2018
Export Citation:
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Assignee:
UNIV CHINA PHARMA (CN)
UNIV NANJING (CN)
International Classes:
C07C311/46; A61K31/18; A61K31/63; A61P25/28; A61P31/12; A61P35/00; C07C303/38; C07C311/16; C07C311/17; C07C311/19; C07C311/39
Foreign References:
CN106928101A2017-07-07
CN101817767A2010-09-01
CN103193691A2013-07-10
Other References:
MCCARROLL ANDREW J.: "Quinols As Novel Therapeutic Agents. 7.1 Synthesis of Antitumor 4-[1-(Arylsulfonyl-lH-indol-2-yl)]-4-hydroxycyclohe- xa-2, 5-dien-l-ones by Sonogashira Reactions", JOURNAL OF MEDICINAL CHEMISTRY, vol. 50, no. 7, 8 March 2007 (2007-03-08), pages 1707 - 1710, XP055605876, ISSN: 1520-4804
MIRIAN MINA F.: "Synthesis and Cytotoxic Evaluation of Some Novel Sulfonamide Derivatives Against a Few Human Cancer Cells", IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH, vol. 10, no. 4, 31 December 2011 (2011-12-31), pages 741 - 748, XP055605879, ISSN: 1735-0328
Attorney, Agent or Firm:
BEIJING TINGLI PATENT FIRM(ORDINARY PARTNERSHIP) (CN)
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