| Patent(s) and the Corresponding Patented Drug(s) |
Top |
| World Intellectual Property Organization (WIPO) |
| Patent ID |
WO2014152127 |
| Title |
Dipeptide and Tripeptide Epoxy Ketone Protease Inhibitors. |
| Abstract |
Provided herein are dipeptide and tripeptide epoxy ketone protease inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (X): and pharmaceutically acceptable salts and compositions including the same. The compounds and compositions provided herein may be used, for example, in the treatment of proliferative diseases including cancer and autoimmune diseases. |
| Applicant(s) |
Onyx Therapeutics, Inc |
| Representative Drug(s) |
D0R8XD |
Drug Info
|
IC50 = 110 nM |
[1] |
| Patent ID |
WO2006099261 |
| Title |
Potent and Specific Immunoproteasome Inhibitors. |
| Abstract |
Compounds and methods of selectively inhibiting an immunoproteasome are described. Also described are methods of treating a cancer, an inflammation, and/or an autoimmune disease and methods of suppressing endogenous antigenic peptide generation by administering to a subject in need of treatment thereof a therapeutic amount of an immunoproteasome specific inhibitor. |
| Applicant(s) |
The University of North Carolina at Chapel Hill |
| Representative Drug(s) |
D0B0GG |
Drug Info
|
Ki = 1450 nM |
[1] |
| Patent ID |
WO2006045066 |
| Title |
Labeled Compounds for Proteasome Inhibition. |
| Abstract |
Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like and PGPH activities of the 20S proteasome can be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus, such as a detectable label. Along with therapeutic utilities, these peptide based compounds can be used in assays useful for screening, monitoring, diagnostic and/or dosing purposes. |
| Applicant(s) |
PROTEOLIX, INC. BENNETT, Mark, K. BUCHHOLZ, Tonia, J. DEMO, Susan LAIDIG, Guy, J. LEWIS, Evan, R. SMYTH, Mark, S. |
| Representative Drug(s) |
D01OOO |
Drug Info
|
IC50 = 160 nM |
[1] |
