Heteroconjugated disulfides of 2-mercaptoethane sulfonate sodium
Inventors
Hausheer, Frederick H. • Kochat, Harry • Huang, Qiuli
Assignees
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Publication Number
US-7829539-B2
Publication Date
2010-11-09
Expiration Date
Abstract
Novel compositions and formulations are disclosed that have use as toxicity-reducing agents for various chemotherapeutic agents and as treatment for certain diseases and conditions. The compositions of matter are amino acid and peptide heteroconjugated disulfides of 2-mercaptoethane sulfonate sodium.
Core Innovation
The invention relates to heteroconjugated disulfides derived from 2-mercaptoethane sulfonate sodium (mesna). The disclosed disulfides have a Formula I structure X—S—S—R1—R2, where X is a sulfur-containing amino acid or a 2-10 amino acid peptide and R1 is a lower alkylene. R2 is a sulfonate or phosphonate.
Specific examples identified include L-cysteine-mesna disulfide, DL-homocysteine-mesna disulfide, glutathione-mesna disulfide, cysteinyl glycine-mesna disulfide, and γ-glutamylcysteine-mesna disulfide. A central aspect described is the use of these heteroconjugated disulfides as compounds to reduce toxicity of a chemotherapeutic regimen.
The partial content further identifies the mesna disulfides as pharmaceutical formulations for therapeutic use and discloses a preferred polymer-bound synthetic approach using resin intermediates, including resin-bound mesna intermediates and polystyrene resin. The disclosed framework links defined mesna-derived disulfide structures to pharmaceutical toxicity reduction of chemotherapeutic regimens.
Claims Coverage
The partial claim set provided includes one independent claim. The claim covers one defined compound structure for reducing toxicity of a chemotherapeutic agent, with specific values for the heteroconjugated disulfide component and pharmaceutically acceptable salts.
γ-Glutamyl cysteine mesna-derived disulfide structure for toxicity reduction
A compound to reduce the toxicity of a chemotherapeutic agent, wherein the compound is X—S—S—R1—R2 with X—S being γ-Glutamyl cysteine, R1 being —(CH2)2—, and R2 being —SO3− or —P(O)(OH)2, or a pharmaceutically acceptable salt thereof.
The independent claim focuses on a specifically defined heteroconjugated disulfide structure featuring γ-Glutamyl cysteine and mesna-derived R2 functionality for reducing toxicity of a chemotherapeutic agent, including pharmaceutically acceptable salts.
Stated Advantages
Reduces the toxicity of a chemotherapeutic agent.
Documented Applications
Therapeutic use for reducing toxicity of chemotherapeutic regimens.
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