Triptolide derivatives and preparation method and use thereof
US9809822B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Dec 11, 2013 |
| Grant date | Nov 7, 2017 |
| Priority date | — |
| Expiry date | Dec 11, 2033 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC12N2320/30
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
Tripyolide-nucleic acid aptamer derivatives, a preparation method and use thereof are shown. The structure of the triptolide-nucleic acid aptamer derivatives is as shown by formula I, wherein the definitions of R1-R7, G, A, B, M, Z and X are described. The present invention uses a nucleic acid aptamer and triptolide or modified compounds thereof as the starting materials, and introduces a linking group A at the C-14 hydroxyl group, epoxy groups and five-membered ring lactones in triptolide, then connects it to a nucleic acid aptamer B, and obtains the triptolide-nucleic acid aptamer derivatives. The triptolide-nucleic acid aptamer derivatives of the present invention have the characteristics of good targeting, a high anti-cancer activity, low toxicity and side effects, good water solubility and high bioavailability, and the preparation method of the present invention is scientific and reasonable and has a controllable quality and good repeatability, and is thereby suitable for production.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.