Controlled release of thioamide moiety-containing therapeutic agents
US6468522B1 · kind B1 · utility
Assignees
Inventors
Key dates
| Filing date | Jul 21, 2000 |
| Grant date | Oct 22, 2002 |
| Priority date | — |
| Expiry date | Jul 21, 2020 |
Classification
- Technology area (CPC Y)Emerging Cross-Sectional Technologies
- CPC primaryY10S424/16
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
This invention pertains to disulfide-linked conjugates of therapeutic agents containing at least one thioamide group with polymer comprising at least one thiol group, so as to provide a controlled release pharmaceutical composition for administration to animals for the prophylaxis or treatment of various conditions or diseases. The therapeutic agent conjugate may comprise an inactive or weakly active prodrug form which may be converted into the original therapeutic compound by the natural action of reducing agents in vivo. The composition may comprise a mixture of polymers each with a different thioamide-containing agent attached, or a polymer conjugated with a mixture of thioamide-containing agents. Modified properties of the therapeutic compound potentially provided by the polymer itself, as well as by other compounds also appended to the polymer, include but are not limited to greater water solubility, longer in-vivo half-life (due to larger size of the conjugate), slower release from a sustained-release depot (due to larger size of the conjugate), better oral bioavailability and tissue-specific targeting.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.