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Title:
ORTHO-CARBONYL AMINO-SUBSTITUTED BENZENE DERIVATIVE, AND PREPARATION METHOD THEREFOR AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2020/199945
Kind Code:
A1
Abstract:
The present invention relates to the technical field of medicine, and discloses a compound as shown in formula (I) and a preparation method therefor, a pharmaceutical composition and the use thereof. In particular, further disclosed in the present invention are a compound as shown in formula (I), a pharmaceutically acceptable salt and a pharmaceutical composition thereof, wherein same can inhibit the enzymatic activity of a human indoleamine 2,3-dioxygenase (IDO) and/or a human tryptophan 2,3-dioxygenase (TDO), and the use of same in the preparation of a drug for treating and/or preventing diseases or conditions related to excessive activity or overexpression of the IDO/TDO, such as a drug for treating tumors. The compound of the present invention has a strong IDO inhibitory activity. (I)

Inventors:
CHEN XIAOGUANG (CN)
CUI HUAQING (CN)
WEN HUI (CN)
LAI FANGFANG (CN)
WANG YUCHEN (CN)
GAO YONGXIN (CN)
YIN DALI (CN)
WANG TING (CN)
HAN JIANYI (CN)
WANG SHUFANG (CN)
JI MING (CN)
LI YAN (CN)
SHENG LI (CN)
MA CHEN (CN)
ZHANG TINGTING (CN)
Application Number:
PCT/CN2020/080517
Publication Date:
October 08, 2020
Filing Date:
March 20, 2020
Export Citation:
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Assignee:
INST MATERIA MEDICA CAMS (CN)
International Classes:
C07C333/08; A61K31/27; A61K31/34; A61K31/381; A61K31/4409; A61K31/473; A61K31/536; A61P35/00; A61P35/02; C07C333/24; C07D213/32; C07D219/02; C07D265/24; C07D307/38; C07D333/28; C07D413/12
Domestic Patent References:
WO2001053278A12001-07-26
Foreign References:
CN105658643A2016-06-08
Other References:
ALLEN KRANTZ ET AL.: "Design and Synthesis of 4H-3, l-benzoxazin-4-ones as Potent Alternate Substrate Inhibitors of Human Leukocyte Elastase", J. MED. CHEM., vol. 33, no. 2, 31 December 1990 (1990-12-31), XP002030653, DOI: 20200619091209X
HANS-GEORG H√ĄCKER ET AL.: "2-Amino- and 2-Alkylthio-4H-3, 1-benzothiazin-4-ones: Synthesis, Interconversion and Enzyme Inhibitory Activities", MOLECULES, vol. 14, no. 1, 14 January 2009 (2009-01-14), XP055739371, DOI: 20200619091345A
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