Small molecule lipid II inhibitors
US10941114B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Dec 23, 2019 |
| Grant date | Mar 9, 2021 |
| Priority date | — |
| Expiry date | Dec 23, 2039 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D213/20
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Newly synthesized derivatives of BAS00127538 have been discovered to possess antibiotic activity and to combat resistant bacterial strains. Compounds and pharmaceutical compositions containing these compounds are described, and are based on a genetic scaffold structure. Synthetic methods and methods of using the compounds also are described. Preferred compounds bind to Lipid II with high affinity, have markedly reduced cytotoxicity compared to BAS00127538, and retain activity against drug-resistant strains of Enterococci. They are stable in plasma, have dramatically improved pharmacokinetic and pharmacodynamics properties, and possess in vivo efficacy in a mouse model of sepsis.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.