SHANGHAI INSTITUTES FOR BIOLOGICAL SCIENCES CHINESE ACADEMY OF SCIENCES;SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES
发明人:
申请号：
EP11741906.9
公开号：
EP2535332B1
申请日:
2011.02.09
申请国别(地区):
EP
年份:
2015
代理人:
摘要：
The invention relates to sinomenine derivatives, methods for their synthesis and their applications. The sinomenine derivatives include oxidation derivatives, and C-10 substituted sinomenine derivatives. Based on the readily oxidizable phenol group on sinomenine structure, using oxidation, oxidative dearomatization, or conjugated addition aromatization, one can introduce C-10 substitutions to synthesize the sinomenine derivatives. The sinomenine derivatives of the invention have the following structures: Using in vitro TNF-± inhibition assay, the activities of the synthetic compounds are assessed. Results from these assays shown that most compounds have anti-inflammatory effects, and some compounds have better activities than that of sinomenine. These compounds may be used in treating immune diseases such as rheumatoid arthritis (RA).
