Aryl (ethanoic) propanoic acid ascorbyl ester, preparation method thereof and medicament containing the same
US8703975B2 · kind B2 · utility
Assignees
Inventors
Key dates
| Filing date | Dec 24, 2009 |
| Grant date | Apr 22, 2014 |
| Priority date | — |
| Expiry date | Dec 24, 2029 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC12Y301/01003
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The present invention designs and synthesizes the ascorbyl ester derivatives of the aryl (ethanoic) propanoic acid non-steroidal anti-inflammatory medicaments, such as ibuprofen, ketoprofen and naproxen, and addition salt of the derivatives with pharmaceutical acid or pharmaceutical alkaline. The non-steroidal anti-inflammatory medicament which takes the ibuprofen as the representative is a common antipyretic analgesic medicament. The invention has remarkable antipyretic and analgesic effects and good safety except for anti-inflammatory effect, thus being not only suitable for adults, but also suitable for the elderly people, infants and children. The aryl (ethanoic) propanoic acid ascorbyl ester can be converted into ascorbyl ester derivatives and the addition salts of the derivatives with pharmaceutical acid or pharmaceutical alkaline, which can improve the water solubility thereof, facilitate intravenously administration, reduce the onset time, improve the bioavailability, reduce the stimulation effect to gastrointestinal tract, and enhance the penetrating capacity to hemato encephalic barrier, and can be used as a novel medicament to be applied for antiphlogistic, antipyresis, …
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.