COMPOUNDS FOR ENZYME INHIBITION

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United States of America Patent

SERIAL NO

12434185

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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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.

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Patent Owner(s)

Patent OwnerAddress
ONYX THERAPEUTICS INC2100 POWELL STREET C/O ONYX PHARMAECUTICALS INC EMERYVILLE CA 94608

International Classification(s)

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  • 2009 Application Filing Year
  • C12N Class
  • 4329 Applications Filed
  • 2065 Patents Issued To-Date
  • 47.71 % Issued To-Date
Click to zoom InYear of Issuance% of Matters IssuedCumulative IssuancesYearly Issuances20092010201120122013201420152016201720182019202020212022202320240255075100

Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Bennett, Mark K Moraga , US 53 621
Buchholz, Tonia J Ann Arbor , US 14 122
Demo, Susan D San Francisco , US 8 124
Laidig, Guy J Menlo Park , US 51 1416
Lewis, Evan R Pacifica , US 3 181
Smyth, Mark S San Mateo , US 75 1296

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Patent Citation Ranking

  • 38 Citation Count
  • C12N Class
  • 88.19 % this patent is cited more than
  • 16 Age
Citation count rangeNumber of patents cited in rangeNumber of patents cited in various citation count ranges1568362451155445231210372701 - 1011 - 2021 - 3031 - 4041 - 5051 - 6061 - 7071 - 8081 - 9091 - 100100 +050100150200250300350400450500550600650700750800850900

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