公开(公告)号：EP2535332A4

公开(公告)日：2013-08-07

申请号：EP11741906

申请日：2011-02-09

申请人： SHANGHAI INST ORGANIC CHEM ,  SHANGHAI INST BIOL SCIENCES

发明人： YAO ZHUJUN ,  SUN BING ,  LOU YANGTONG ,  YANG ZHENYU ,  CHEN AIZHONG ,  MA ZHAO

IPC分类号： C07D221/28 ,  A61K31/485 ,  A61P29/00 ,  A61P37/06

CPC分类号： C07D221/28 ,  A61K31/485

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).