Mu opioid receptor agonist analogs of the endomorphins
US8716436B2 · kind B2 · utility
4Cited by
4References
8Claims
0Family size
Assignees
Inventors
Key dates
| Filing date | May 22, 2012 |
| Grant date | May 6, 2014 |
| Priority date | — |
| Expiry date | May 22, 2032 |
Classification
- Technology area (CPC G)Physics
- CPC primaryG01N2500/04
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The invention relates to cyclic peptide agonists that bind to the mu (morphine) opioid receptor and their use in the treatment of acute and/or chronic pain. Embodiments of the invention are directed to cyclic pentapeptide and hexapeptide analogs of endomorphin that have (i) a carboxy-terminal extension with an amidated hydrophilic amino acid and (ii) a substitution in amino acid position 2. These peptide analogs exhibit decreased tolerance relative to morphine, increased solubility compared to similar tetrapeptide analogs, while maintaining favorable or improved therapeutic ratios of analgesia to side effects.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.