Compounds for the treatment of Clostridium difficile infection
US11168062B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Sep 12, 2017 |
| Grant date | Nov 9, 2021 |
| Priority date | — |
| Expiry date | Sep 17, 2037 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D413/12
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
Clostridium difficile infection (CDI) is a public health threat that results in 14,000 annual deaths in the United States. Challenges involve the production of CDI spores that can remain dormant for years and the production of toxins that damage the gut. Current therapies for CDI include vancomycin and metronidazole, but neither inhibits spore or toxin production. Thus, recurrence of infection occurs in 25% of patients and there are no antibiotics that are effective for multiple recurrences. We describe oxadiazoles with activity against C. difficile, including the highly virulent NAP1/027 strain with increased production of toxins A and B, as well as the additional binary toxin. Oxadiazole 2 is poorly absorbed, thus advantageously achieving high concentrations in the gut. The compound targets peptidoglycan synthesis and inhibits vegetative cells, spores, and toxin production.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.