Invivogen

Kayla Therapeutics

The Provost, Fellows, Foundation Scholars, & the Other Members of Board, of the College of Holy and Undiv. Trinity of Queen Elizabeth Near Dublin

Invivogen Sas

Thierry Lioux

Fabienne Vernejoul

Gerard Tiraby

Daniel Drocourt

Kingston Mills

Eric Perouzel

Arnaud Debin

Michèle Tiraby

Jean-Gerard Tiraby

Gérard Tiraby

Cédric Boularan

Patrick Kelly

The present invention provides a Pro-cyclic dinucleotide (Pro-CDN) comprising a STING agonist cyclic dinucleotide which is coupled to a linker system. The Pro-CDNs of the present invention can be metabolized at a targeted site into CDNs and exert their full immunomodulatory effects at said targeted site. The present invention also provides conjugates wherein a Pro-CDN is conjugated to a Biologically Active Molecule (BAM) such as e.g. a cytotoxic molecule, a lipid, a protein, a peptide, a nucleic acid, a sugar or a PRR ligand. The invention provides also methods related to the use of such compounds to perform their activities at their targeted sites, to exert cytotoxic, cytostatic or immunomodulatory effects, to treat or to prevent diseases such as cancers, immunological disorders or infections.

Pro-cyclic dinucleotides and pro-cyclic dinucleotide conjugates for cytokine induction

A cyclic dinucleotide compound of Formula (I): wherein Xis H or F; Xis H or F; at least one among Xand Xis a fluorine atom; Z is OH, OR, SH or SR, wherein: Ris Na or NH, or Ris an enzyme-labile group which provides OH or SH in vivo such as pivaloyloxymethyl; Band Bare bases chosen from Adenine, Hypoxanthine or Guanine, and Bis a different base than Band a pharmaceutically acceptable salt thereof. Pharmaceutical compositions including the cyclic dinucleotide, as well as their use in the treatment of a bacterial infection, a viral infection or a cancer are also described.

Cyclic dinucleotides for cytokine induction

A conjugated compound of formula Q-Z&#x2014;Rwherein Q is a TLR7 and/or TLR8 agonist and Z&#x2014;Ris a TLR2 agonist, and the uses thereof in the treatment of infection, cancer or immune disorders or for use in vaccines.

Conjugated TLR7 and/or TLR8 and TLR2 agonists

A conjugated compound of formula Q-Z&#x2014;Rwherein Q is a TLR7 and/or TLR8 agonist and Z&#x2014;Ris a lipid covalently linked to an amino acid or peptide coupled to a polyamine group, and a process for the manufacture of the conjugated compound, as well as a complex formed between the conjugated compound and a polyanionic molecule and a pharmaceutical composition containing the conjugated compound or complex. Also described is the use of the conjugated compound or complex in the treatment of infection, cancer or immune disorders or for use in vaccines.

Compositions of TLR7 and/or TLR8 agonists conjugated to lipids

A conjugated compound of Formula I: Q-Z&#x2014;Rwherein Q is a TLR7 and/or TLR8 agonist and Z&#x2014;Ris a TLR2 agonist, the conjugated compound being chosen among compounds of Formula II: 

Conjugated TLR7 and/or TLR8 and TLR2 polycationic agonists

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Balma, France

Thierry Lioux