Compositions comprising enzyme-cleavable phenol-modified tapentadol prodrug
US9238020B2 · kind B2 · utility
5Cited by
9References
24Claims
0Family size
Assignee
Inventors
Key dates
| Filing date | Oct 14, 2010 |
| Grant date | Jan 19, 2016 |
| Priority date | — |
| Expiry date | Mar 24, 2032 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07C279/14
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
A method of providing a patient with controlled release of tapentadol using a prodrug capable, upon enzymatic activation and intramolecular cyclization, of releasing tapentadol is disclosed. The disclosure also provides such prodrug compounds and pharmaceutical compositions comprising such compounds. Such pharmaceutical compositions can optionally include an enzyme inhibitor that interacts with the enzyme(s) to mediate the enzymatically-controlled release of tapentadol from the prodrug so as to modify enzymatic cleavage of the prodrug. Also included are methods to use such compounds and pharmaceutical compositions.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.