Method of converting a drug to an orally available form by covalently bonding a lipid to the drug
US5411947A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Dec 16, 1992 |
| Grant date | May 2, 1995 |
| Priority date | — |
| Expiry date | Dec 16, 2012 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07H19/16
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The oral delivery of many classes of drugs is facilitated by converting drugs having suitable functional groups to 1-O-alkyl-, 1-O-acyl-, 1-S-acyl, and 1-S-alkyl-sn-glycero-3-phosphate derivatives. The method confers the ability to be absorbed through the digestive tract to drugs that are not orally bioavailable in the non-derivatized state, and enhances the effectiveness of drugs that are poorly absorbed or rapidly eliminated. The method provides orally bioavailable lipid prodrugs of pharmaceutical compounds having diverse physiological activities, including anticancer and antiviral agents, anti-inflammatory agents, antihypertensives and antibiotics. Potency of the lipid prodrugs is comparable to that of the corresponding non-derivatized drugs.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.