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Powerful broad-spectrum antivirals with action against emerging viruses

covid-19covid-19drug-resistanceemerging virusesviral envelope destabilization

Introduction

Compounds of formula I, their use as medicaments, their combination with a further antiviral agent and related pharmaceutical compositions. In particular, the compounds of the invention are useful in the treatment of a disease caused by an envelope virus.

Technical features

Current antiviral approaches require high efficacy and the absence of toxicity as they act within cells and are often virus-specific. The latter often develops resistance to the used drugs. The present compounds act directly on the extracellular virus, destabilizing the viral envelope through radical oxidation of the lipid component promoted by light and preventing the virus from entering the cell. The selectivity of the compounds is linked to the repair mechanisms of eukaryotic membranes which are not present in viruses. Good in vitro characteristics of permeability, solubility and metabolic stability of the compounds would allow their use through various administration routes. They can be formulated as vaginal microbicides to prevent disease and sexual transmission and as a nasal spray to prevent and treat respiratory infections. They represent an innovative tool to combat emerging viruses for which there is no time to develop specific antiviral molecules or vaccines, as active towards all enveloped viruses (ZIKV, DENV, SARS-CoV-2).

Possible Applications

  • Pharmaceutical formulation as anti-viral medicament;
  • Treatment of Zika, HIV-1, HIV-2, HCMV, RSV, VSV, H1N1 among others;
  • Can be used in combination with other antiviral agent(s);
  • Potential activity against SARS-CoV-2;
  • Intranasal, parenteral, oral, vaginal or rectal administration.

Advantages

  • Potent activity against 9 emerging viruses causing recent outbreaks;
  • Potentially active against all envelope viruses;
  • Active against resistant strains;
  • Alone or combinatory therapy;
  • Safety (good in vitro ADME properties).