Thiosemicarbazates and Uses Thereof - US12600699B2
Summary
The USPTO granted Patent US12600699B2 to The Feinstein Institutes for Medical Research covering thiosemicarbazates, thiocarbamates, thiocarbazates, semithiocarbazates, peptides, aza-amino acid conjugates, and azapeptides. The patent also protects a chemoselective functionalization protocol using Mitsunobu reaction for site-specific alkylation. Methods for preparing and using these compounds in drug discovery, diagnosis, inhibition, prevention and treatment of diseases are included in the 17 granted claims.
What changed
The USPTO issued Patent US12600699B2 to The Feinstein Institutes for Medical Research, granting exclusive rights to thiosemicarbazate compounds, their preparation methods, and applications in drug discovery and disease treatment. The patent covers novel synthesis protocols including chemoselective Mitsunobu reactions for functionalizing protected thiocarbazates.
Pharmaceutical and biotechnology companies developing compounds in related therapeutic areas should assess potential freedom-to-operate concerns. The patent's broad claim scope covering peptides, aza-amino acid conjugates, and azapeptides may affect research programs in similar chemical space. Companies should consult patent counsel for infringement risk assessments and explore potential licensing opportunities with the Feinstein Institutes.
What to do next
- Monitor patent portfolio for freedom-to-operate implications
- Review compound families for potential licensing opportunities
- Consult patent counsel regarding infringement risk assessment
Archived snapshot
Apr 14, 2026GovPing captured this document from the original source. If the source has since changed or been removed, this is the text as it existed at that time.
Thiosemicarbazates and uses thereof
Grant US12600699B2 Kind: B2 Apr 14, 2026
Assignee
THE FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
Inventors
Yousef Al-Abed, Ahmad Altiti
Abstract
Thioesters, thiocarbamates, thiocarbazates, semithiocarbazates, peptides, aza-amino acid conjugates, and azapeptides; and a chemoselective and site-specific functionalization protocol of protected thiocarbazates and semithiocarbazates are described. The protocol features the use of Mitsunobu reaction to alkylate specifically the nitrogen atom close to the acylthiol moiety with alcohols to produce protected mono-substituted thiocarbazates that can be stored for months, activated under mild conditions at low temperature using halonium reagents and integrated orthogonally to make substituted semicarbazides that can be used, e.g., as synthons in synthesis of aza-amino acid conjugates, azapeptides and other peptidomimetics. Methods for preparing and using ureases, carbazides, semicarbazides, beta-peptides, azapeptides, and other peptidomimetics and azapeptide conjugates, and uses of ureases, carbazides, semicarbazides, beta-peptides, azapeptides in drug discovery, diagnosis, inhibition, prevention and treatment of diseases are also described.
CPC Classifications
C07D 209/48 C07D 403/12
Filing Date
2022-12-02
Application No.
18073689
Claims
17
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