Molecules
Inventors
Holmes, Ian • Zeng, Weiguang • Jackson, David • Demaison, Christophe • McLachlan, Grant
Assignees
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Publication Number
US-12017979-B2
Publication Date
2024-06-25
Expiration Date
Abstract
The present invention relates to TLR2 agonist compounds and their compositions, and the use of such compounds and compositions in the prevention and/or treatment of respiratory infections, or diseases or conditions associated with viral or bacterial infections.
Core Innovation
The invention relates to TLR2 agonist compounds defined by broad structural parameters, including variable chain and substituent parameters denoted by n, m, p, q, and unit counts for L, together with substituent selections such as R1, R2, and R3. The structural definition further specifies sulfur or heteroatom linkage options using variables X and Z1/Z2, and includes multiple formula embodiments such as compounds of formula I, formula VI, formula VII, and formula X.
The invention also relates to stereochemically defined compounds, including Cys analogue configurations at moiety A with specified (S,R; S,S; R,S; R,R) combinations at starred chiral centers and a separate chiral centre in the Y moiety, including L-Y stereoisomers and D-Y stereoisomers. The variable substituents L1, L2, Z1, Z2, Rx, Ry, and R11-R19 are specified to follow Formula (I), and specific named and illustrated compounds are included as examples.
The documents provide biological and therapeutic context for the compounds, stating that they are proposed for treating and/or preventing respiratory infections and for reducing airway inflammation. The compounds are associated with raising innate immune responses, may inhibit viral progression and reduce viral load, and include pharmaceutical compositions comprising the compounds together with pharmaceutically acceptable carriers, diluents, or excipients.
Claims Coverage
The provided independent claims are directed to the compound itself, including pharmaceutically acceptable salt or solvate forms, and to pharmaceutical composition embodiments comprising the compound with pharmaceutically acceptable carrier, diluent, or excipient. Across the provided claim scope, the inventive-feature coverage is limited to these two features.
Tlr2 agonist compound, pharmaceutically acceptable salt or solvate
A compound, or a pharmaceutically acceptable salt or solvate thereof, defined as a TLR2 agonist compound.
Pharmaceutical composition comprising the compound with carrier, diluent, or excipient
A pharmaceutical composition comprising the compound, or a pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable carrier, diluent, or excipient.
The independent claims cover the compound itself and its inclusion in a pharmaceutical composition with pharmaceutically acceptable formulation components. No additional independent inventive features are explicitly stated in the provided claim text.
Stated Advantages
Raises innate immune responses.
Reduces airway inflammation.
Inhibits viral progression.
Reduces viral load.
Solution stability with at least 80% retention after 14 days in pH 7.4 PBS under accelerated conditions.
Documented Applications
Treating and/or preventing respiratory infections, including influenza (Types A/B/C).
Reducing airway inflammation associated with respiratory infections.
Respiratory route.
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