公开(公告)号：EP3154938A4

公开(公告)日：2018-04-18

申请号：EP15806407

申请日：2015-06-05

申请人： GOVERNMENT OF THE UNITED STATES AS REPRESENTED BY THE SECRETARY OF THE ARMY ON BEHALF OF ARMY MEDI C ,  SCRIPPS RESEARCH INST

发明人： SAIKH KAMAL U ,  REBEK JULIUS M ,  GLASS PAMELA J

IPC分类号： C07D207/02 ,  A61K31/401 ,  A61K31/4025 ,  A61P31/12 ,  C07D295/185 ,  C07D403/12

CPC分类号： A61K31/4025 ,  C07D295/185 ,  C07D403/12

摘要： A synthetic molecule 4210 and a therapeutic use of a synthetic small molecule 4210 for treating viral infections, especially encephalitic alphavirus infections. The compound 4210 showed antiviral efficacy by up regulation type 1 interferon (IFN) specifically IFN-β. The compound 4210 was designed and synthesized by a structure-based approach targeting intracellular adaptor protein, myeloid differentiation primary response protein 88 (MyD88). Besides having an antiviral effect, the compound 4210 also demonstrated therapeutic efficacy for treating inflammatory syndrome associated with Gram positive bacterial infections such as exposure to staphylococcal enterotoxin B (SEB) induced toxic shock syndrome (TSS) in mice and can potentially be used in clinical set up for treating sepsis and septic shock. In addition, the application of molecule 4210 can treat sepsis and septic shock triggered by exposure to other biological agents such as Francisella tularensis or Burkholderia mallei known to cause tularemia and glanders, respectively. The molecule 4210 has the potential for a broad-spectrum therapeutic use.