Title:
COMPOUND WITH MOTHER NUCLEUS OF 3-PHENYL-1,2,4-OXADIAZOLE, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2022/222730
Kind Code:
A1
Abstract:
Disclosed in the present invention are a compound with mother nucleus of 3-phenyl-1,2,4-oxadiazole, a preparation method therefor and an application thereof. The compound with mother nucleus of 3-phenyl-1,2,4-oxadiazole provided in the present invention is simple in preparation method and novel in structure. The compound specifically inhibits the activation of NLRP3 inflammasome, to reduce the maturation and secretion of IL-1β, thereby reducing inflammatory damage and improving the inflammatory microenvironment. Therefore, the compound has significant anti-inflammatory activity and has no significant toxicity to THP-1 cells. The compound of the present invention can be prepared into anti-inflammatory drugs and are used for the treatment of inflammation-related diseases, including diabetes, atherosclerosis, rheumatic arthritis, rheumatoid arthritis, chronic obstructive pulmonary diseases, gout, chronic kidney diseases, neurodegenerative diseases, cold pyrazoline related periodic syndromes, non-alcoholic fatty liver diseases, inflammatory bowel diseases, etc.
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Inventors:
XU LILI (CN)
DI BIN (CN)
ZHAO NI (CN)
DI BIN (CN)
ZHAO NI (CN)
Application Number:
PCT/CN2022/084705
Publication Date:
October 27, 2022
Filing Date:
April 01, 2022
Export Citation:
Assignee:
UNIV CHINA PHARMA (CN)
International Classes:
C07D417/12; A61K31/4245; A61K31/428; A61K31/433; A61K31/4439; A61P1/00; A61P1/16; A61P3/10; A61P9/10; A61P11/00; A61P13/12; A61P19/02; A61P19/06; A61P25/14; A61P25/16; A61P25/28; A61P29/00; C07D217/06; C07D413/12
Domestic Patent References:
| WO2020211956A1 | 2020-10-22 |
Foreign References:
| CN113214242A | 2021-08-06 | |||
| CN103237795A | 2013-08-07 |
Other References:
DATABASE REGISTRY 07-12-2021, ANONYMOUS : "4(3H)-Quinazolinone, 3-cyclopropyl-6,7-difluoro-2-[[[3-[4- (trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl]methyl]thio]- (CA INDEX NAME)", XP055981376, retrieved from STN Database accession no. 2742018-05-7
DATABASE REGISTRY 09-06-2019, ANONYMOUS : "5H-Pyrimido[5,4-b]indole, 4-[[[3-[4-(trifluoromethoxy)phenyl]-1,2,4- oxadiazol-5-yl]methyl]thio]- (CA INDEX NAME)", XP055981382, retrieved from STN Database accession no. 2326911-32-2
LI YANPING, MING XU: "Research Progress of NLRP3 Inflammasome Activation Mechanism and Small Molecule Inhibitors", GUANGDONG CHEMICAL INDUSTRY, GUANGDONG-SHENG ZHONGHUA GONGYETING,, CN, vol. 47, no. 19, 15 October 2020 (2020-10-15), CN , pages 83 - 86, XP055981392, ISSN: 1007-1865
DATABASE REGISTRY 09-06-2019, ANONYMOUS : "5H-Pyrimido[5,4-b]indole, 4-[[[3-[4-(trifluoromethoxy)phenyl]-1,2,4- oxadiazol-5-yl]methyl]thio]- (CA INDEX NAME)", XP055981382, retrieved from STN Database accession no. 2326911-32-2
LI YANPING, MING XU: "Research Progress of NLRP3 Inflammasome Activation Mechanism and Small Molecule Inhibitors", GUANGDONG CHEMICAL INDUSTRY, GUANGDONG-SHENG ZHONGHUA GONGYETING,, CN, vol. 47, no. 19, 15 October 2020 (2020-10-15), CN , pages 83 - 86, XP055981392, ISSN: 1007-1865
Attorney, Agent or Firm:
NANJING TIANHUA PATENT AGENT CO., LTD. (CN)
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