Preparation and the use of ethoxy combretastatins and their prodrugs
US7838706B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | May 16, 2007 |
| Grant date | Nov 23, 2010 |
| Priority date | — |
| Expiry date | May 16, 2027 |
Classification
- Technology area (CPC Y)Emerging Cross-Sectional Technologies
- CPC primaryY10T137/87885
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The invention disclosed a total synthesis process of novel ethoxy combretastatins and their prodrugs. Combretastatins are chemically modified by ethoxy substituted on the 4′-position of their B aryl ring and are converted to be their soluble prodrugs of phosphate or their inner salt of phosphorylcholine by modifying the hydroxyl on the 3′-position of their B aryl ring. Similarly, 3′-amino combretastatin is 4′-ethoxy chemically modified and further side chain of amino acid can be introduced to the amino to form soluble prodrug of amino acidamide. The structure of the said compound is showed as formula (I). Ethoxy combretastatins possess potent tubulin polymerization inhibitory activity and can be used for the treatment of inhibiting tumor or neovascular.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.