Small molecule lipid II inhibitors
US10961214B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Dec 20, 2016 |
| Grant date | Mar 30, 2021 |
| Priority date | — |
| Expiry date | Dec 20, 2036 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D471/06
- 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 generic scaffold structure. Synthetic methods and methods of using the compounds also are described. Preferred compound 6jc48-1 ((E)-2,4-bis(4-bromophenyl)-6-(4-(dimethyl-amino)styryl)pyrylium boron tetrafluoride salt) binds to Lipid II with high affinity, has markedly reduced cytotoxicity than BAS00127538, and retains activity against drug-resistant strains of Enterococci. It is stable in plasma, has dramatically improved pharmacokinetic and pharmacodynamics properties, and possesses in vivo efficacy in a mouse model of sepsis.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.