AU2007261345B2 - Peptide epoxyketones for proteasome inhibition - Google Patents

Peptide epoxyketones for proteasome inhibition Download PDF

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Publication number
AU2007261345B2
AU2007261345B2 AU2007261345A AU2007261345A AU2007261345B2 AU 2007261345 B2 AU2007261345 B2 AU 2007261345B2 AU 2007261345 A AU2007261345 A AU 2007261345A AU 2007261345 A AU2007261345 A AU 2007261345A AU 2007261345 B2 AU2007261345 B2 AU 2007261345B2
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Prior art keywords
alkyl
compound
mmol
hydrogen
absent
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AU2007261345A1 (en
Inventor
Mark K. Bennett
Guy J. Laidig
Francesco Parlati
Kevin D. Shenk
Mark S. Smyth
Catherine Sylvain
Han-Jie Zhou
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Onyx Therapeutics Inc
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Onyx Therapeutics Inc
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Assigned to ONYX THERAPEUTICS, INC. reassignment ONYX THERAPEUTICS, INC. Request to Amend Deed and Register Assignors: PROTEOLIX, INC.
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US20120088762A1 (en) 2012-04-12
US8765745B2 (en) 2014-07-01
CN101506224B (zh) 2016-03-30
RU2450016C2 (ru) 2012-05-10
US8609654B1 (en) 2013-12-17
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UA101303C2 (uk) 2013-03-25
CO6241190A2 (es) 2011-01-20
US20130338057A1 (en) 2013-12-19
EP2041158A2 (en) 2009-04-01
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US8431571B2 (en) 2013-04-30
US9657058B2 (en) 2017-05-23
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US8080545B2 (en) 2011-12-20

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