Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Substituted hydroxylamine derivatives with anti-inflammatory activity and preparation method and application thereof

A technology of substituents and representatives, applied in the field of substituted hydroxylamine derivatives with anti-inflammatory activity, their preparation and application, and able to solve problems such as application limitations

Active Publication Date: 2010-08-18
CHINA PHARM UNIV
View PDF0 Cites 4 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the application of NSAIDs is limited due to its side effects on the gastrointestinal tract (GI) and kidneys, especially the "Vanlo incident" that occurred in 2004, which has aroused people's attention to the safety of NSAIDs

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Substituted hydroxylamine derivatives with anti-inflammatory activity and preparation method and application thereof
  • Substituted hydroxylamine derivatives with anti-inflammatory activity and preparation method and application thereof
  • Substituted hydroxylamine derivatives with anti-inflammatory activity and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0070] 1-Phenyl-3-thiosemicarbazide

[0071] Phenylhydrazine hydrochloride (6.0g, 0.042mol) was suspended in 40ml of absolute ethanol, 0.5ml of concentrated hydrochloric acid was added dropwise, the temperature was raised to about 40°C, KSCN (4.9g, 0.050mol) was added in batches for 40min, and the temperature was raised to reflux for 6h. After suction filtration, the filtrate was allowed to stand still, and a large amount of precipitate was precipitated, and then suction filtration gave 4.5 g of white powder, yield: 65.2%, m.p.197-200°C.

Embodiment 2

[0073] p-methylsulfonylbenzoyl chloride

[0074] p-Methanesulfonylbenzoic acid (10 g, 0.05 mol) was suspended in SOCl 2 (25ml, 0.21mol), heated and refluxed for 2.5h, concentrated to dryness under reduced pressure to obtain a white yellowish solid, which was recrystallized from toluene to obtain 8.5g of white solid, yield: 78%, m.p.128-130°C.

Embodiment 3

[0076] 2-(4-Methanesulfonylbenzoyl)-2-phenyl-thiosemicarbazide

[0077] Suspend 1-phenyl-3-thiosemicarbazide (0.6g, 3.6mmol) in 20ml of anhydrous acetone, add triethylamine 5d, stir at room temperature, add p-methylsulfonylbenzoyl chloride (0.79g , 3.6mmol), heated to reflux for 3h, suction filtered, and the filter cake was dried to obtain 1.1g of white solid, yield: 87.8%, m.p.204-206°C.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention relates to the field of pharmaceutical chemistry, in particular to substituted hydroxylamine derivatives. The invention also discloses a preparation method for the substituted hydroxylamine derivatives, a medicinal composition comprising the compounds, and the application of the compounds in treating rheumatoid arthritis and osteoarthritis, and treating other diseases and symptoms through doubly inhibiting cyclooxygenase-2(COX-2) and 5-lipoxygenase (5-LOX).

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a class of substituted hydroxylamine derivatives. The invention also discloses a preparation method of these substituted hydroxylamine derivatives, a pharmaceutical composition containing the compound and the use of the compound in treating rheumatoid arthritis , osteoarthritis and in the treatment of other diseases or conditions by dual inhibition of cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX). Background technique [0002] Non-steroidal anti-inflammatory drugs (NSAIDs) are one of the most widely used drugs in the world. They are the basic symptomatic drugs for the treatment of rheumatic diseases. and soft tissue inflammation. However, the application of NSAIDs is limited due to its side effects on the gastrointestinal tract (GI) and kidneys, especially the "Vanlo incident" in 2004, which aroused people's concern on the safety of NSAIDs. Therefore, the development of...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): C07D249/12A61K31/4196A61P29/00A61P19/02A61P19/08
Inventor 徐进宜吴晓明江波黄晓静蒋婧章朱培清柳军黄婧儿王秋娟蒋斯怡
Owner CHINA PHARM UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com