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Antagonists of TRL4

Antiinflammatory drugsAutoimmune inflammationscovid-19Drug developmentSARS-CoV2

Introduction

The search for molecules capable of blocking inflammation at its root and in its molecular causes currently has two major objectives: the first is related to lung infections of some viruses including SARS-CoV2, which result in a violent inflammatory response, which is difficult to be controlled with classic anti-inflammatory drugs. The second is autoimmune and chronic inflammations.

Technical features

The invention consists of new synthetic molecules capable of blocking the inflammatory cascade at the root, selectively blocking the TLR4 receptor. These molecules are prototypes for the development of specific anti-inflammatories for some chronic inflammatory diseases, including those of autoimmune origin, such as Inflammatory Bowel Diseases (IBDs) such as Chron’s disease and ulcerative colitis. Furthermore, the molecules that block TLR4 have enormous potential as therapeutics against violent inflammations induced by some viruses that infect the respiratory tract, including SARS-CoV2. The mechanism of action of the molecules described in the patent has been investigated in vitro with experiments on cells and in vivo on animal models of IBD and influenza virus inflammatory syndrome. The abundance of biochemical data on the functioning of the molecules and the absence of toxicity on cells and animals makes these molecules valid prototypes for the development of specific anti-inflammatories so far absent from the market.

Possible Applications

  • Anti-inflammatoriy drugs for autoimmune diseases;
  • Anti-inflammatory drugs for IBDs;
  • Specific drugs targeting SARS-CoV inflammations.

Advantages

  • First-in-class drugs against IBDs;
  • Low toxicity;
  • High in vivo activity.