Modified peptides as potent inhibitors of the PSD-95/NMDA receptor interaction
US9902754B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Dec 16, 2015 |
| Grant date | Feb 27, 2018 |
| Priority date | — |
| Expiry date | Jan 11, 2036 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61K38/00
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The present invention is directed to the provision of small molecule inhibitors of the PSD-95/NMDA receptor interaction, employing an undecapeptide corresponding to the C-terminal of the NMDA as a template for finding lead candidates. A compound (NMDAR/PSD-95 inhibitor) of the invention includes a peptide or peptide analog comprising at least four peptide bonded residues having the sequence YTXV or YSXV, wherein Y is selected from among E, Q, and A, or an analog thereof, and X is selected from among A, Q, D, N, N-Me-A, N-Me-Q, N-Me-D, and N-Me-N or an analog thereof, wherein an amino-terminal residue of the peptide is N-alkylated. Alternatively the compound of the invention comprises a first peptide or peptide analog linked to a second peptide or peptide analog by a linker, where the first and second peptide or peptide analog each comprise at least four peptide bonded residues having the sequence YTXV or YSXV, wherein Y is selected from among E, Q, and A, or an analog thereof, and X is selected from among A, Q, D, N, N-Me-A, N-Me-Q, N-Me-D, and N-Me-N or an analog thereof.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.