| Patent(s) and the Corresponding Patented Drug(s) |
Top |
| World Intellectual Property Organization (WIPO) |
| Patent ID |
WO2017156471 |
| Title |
Immunoproteasome Inhibitor Analogs. |
| Abstract |
The disclosure provides for compounds having immunoproteasome inhibitory activity, and pharmaceutical compositions made thereof. The disclosure further provides for the use of the compounds and compositions in treating various diseases and disorders in a subject that are associated with immunoproteasome activity, including inflammatory disorders, autoimmune disorders, hematological disorders, and neurodegenerative disorders. |
| Applicant(s) |
The Regents of the University of California |
| Representative Drug(s) |
D00GGB |
Drug Info
|
Ki = 920 nM |
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[1] |
|
2
|
D01GON
|
Drug Info
|
Ki = 1070 nM
|
[1] |
|
3
|
D0DY3A
|
Drug Info
|
Ki = 1760 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 = 141 nM |
[1] |
