Belactosin derivatives as therapeutic agents/biological probes and their synthesis
US8119653B2 · kind B2 · utility
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2References
32Claims
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Assignee
Inventors
Key dates
| Filing date | Jul 9, 2007 |
| Grant date | Feb 21, 2012 |
| Priority date | — |
| Expiry date | Oct 24, 2029 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D305/12
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Derivatives of belactosin and their synthesis are disclosed. In certain embodiments, compounds of the present invention exhibit anti-cancer, antiviral, antibiotic, and/or auto-immune therapeutic abilities. In general, methods of synthesis disclosed herein allow for introduction of a variety of substituents at numerous positions as well as the facile introduction of a beta-lactone ring moiety. The synthetic steps comprise, in preferred embodiments, a tandem Mukaiyama aldol lactonization reaction. Data demonstrating the utility of some of the derivatives as proteasome inhibitors is also disclosed.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.