WO2006099261A3 - Potent and specific immunoproteasome inhibitors - Google Patents

Potent and specific immunoproteasome inhibitors Download PDF

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Publication number
WO2006099261A3
WO2006099261A3 PCT/US2006/008835 US2006008835W WO2006099261A3 WO 2006099261 A3 WO2006099261 A3 WO 2006099261A3 US 2006008835 W US2006008835 W US 2006008835W WO 2006099261 A3 WO2006099261 A3 WO 2006099261A3
Authority
WO
WIPO (PCT)
Prior art keywords
potent
methods
immunoproteasome inhibitors
immunoproteasome
specific
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/US2006/008835
Other languages
French (fr)
Other versions
WO2006099261A2 (en
Inventor
Robert Z Orlowski
Marian Orlowski
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
University of North Carolina at Chapel Hill
Icahn School of Medicine at Mount Sinai
Original Assignee
University of North Carolina at Chapel Hill
Mount Sinai School of Medicine
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by University of North Carolina at Chapel Hill, Mount Sinai School of Medicine filed Critical University of North Carolina at Chapel Hill
Priority to EP06748358A priority Critical patent/EP1863513A2/en
Publication of WO2006099261A2 publication Critical patent/WO2006099261A2/en
Publication of WO2006099261A3 publication Critical patent/WO2006099261A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0827—Tripeptides containing heteroatoms different from O, S, or N
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1016—Tetrapeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1027—Tetrapeptides containing heteroatoms different from O, S, or N
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • General Health & Medical Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)

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.
PCT/US2006/008835 2005-03-11 2006-03-13 Potent and specific immunoproteasome inhibitors Ceased WO2006099261A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP06748358A EP1863513A2 (en) 2005-03-11 2006-03-13 Potent and specific immunoproteasome inhibitors

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US66059605P 2005-03-11 2005-03-11
US60/660,596 2005-03-11

Publications (2)

Publication Number Publication Date
WO2006099261A2 WO2006099261A2 (en) 2006-09-21
WO2006099261A3 true WO2006099261A3 (en) 2007-05-18

Family

ID=36992315

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2006/008835 Ceased WO2006099261A2 (en) 2005-03-11 2006-03-13 Potent and specific immunoproteasome inhibitors

Country Status (3)

Country Link
US (1) US7589066B2 (en)
EP (1) EP1863513A2 (en)
WO (1) WO2006099261A2 (en)

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8541581B2 (en) 2009-04-07 2013-09-24 Infinity Pharmaceuticals, Inc. Inhibitors of fatty acid amide hydrolase
US8546564B2 (en) 2009-04-07 2013-10-01 Infinity Pharmaceuticals, Inc. Inhibitors of fatty acid amide hydrolase
US8853147B2 (en) 2009-11-13 2014-10-07 Onyx Therapeutics, Inc. Use of peptide epoxyketones for metastasis suppression
US8921583B2 (en) 2007-10-04 2014-12-30 Onyx Therapeutics, Inc. Crystalline peptide epoxy ketone protease inhibitors and the synthesis of amino acid keto-epoxides
US8957049B2 (en) 2008-04-09 2015-02-17 Infinity Pharmaceuticals, Inc. Inhibitors of fatty acid amide hydrolase
US9034849B2 (en) 2010-02-03 2015-05-19 Infinity Pharmaceuticals, Inc. Fatty acid amide hydrolase inhibitors
US9108989B2 (en) 2006-10-10 2015-08-18 Infinity Pharmaceuticals, Inc. Inhibitors of fatty acid amide hydrolase
US9205124B2 (en) 2005-11-09 2015-12-08 Onyx Therapeutics, Inc. Compounds for enzyme inhibition
US9309283B2 (en) 2012-07-09 2016-04-12 Onyx Therapeutics, Inc. Prodrugs of peptide epoxy ketone protease inhibitors

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5616569B2 (en) 2004-04-15 2014-10-29 オニキス セラピューティクス， インク．Ｏｎｙｘ Ｔｈｅｒａｐｅｕｔｉｃｓ， Ｉｎｃ． Compounds for enzyme inhibition
US8198270B2 (en) * 2004-04-15 2012-06-12 Onyx Therapeutics, Inc. Compounds for proteasome enzyme inhibition
BRPI0510802A (en) * 2004-05-10 2007-11-06 Proteolix Inc enzyme inhibiting compounds
AU2012200797B2 (en) * 2006-06-19 2015-04-16 Onyx Therapeutics, Inc. Peptide epoxyketones for proteasome inhibition
NZ573759A (en) 2006-06-19 2012-03-30 Proteolix Inc Peptide epoxyketones for proteasome inhibition
US7838673B2 (en) 2007-10-16 2010-11-23 Millennium Pharmaceuticals, Inc. Proteasome inhibitors
JP5600595B2 (en) * 2007-10-16 2014-10-01 ミレニアム ファーマシューティカルズ， インコーポレイテッド Proteasome inhibitor
US20090110688A1 (en) * 2007-10-24 2009-04-30 Georg Fertig Combination therapy of type ii anti-cd20 antibody with a proteasome inhibitor
EP2088205A1 (en) 2008-02-11 2009-08-12 Institut National De La Sante Et De La Recherche Medicale (Inserm) PSMB10: A diagnosis marker and therapeutic target of chronic rejection.
DK2288615T3 (en) 2008-05-21 2017-09-04 Genesis Tech Ltd SELECTIVE CASPASE INHIBITORS AND APPLICATIONS THEREOF
BRPI0919668A2 (en) 2008-10-21 2018-05-29 Onyx Therapeutics, Inc. peptide epoxy ketone combination therapy
AR075899A1 (en) 2009-03-20 2011-05-04 Onyx Therapeutics Inc PROTEASA INHIBITING CRYSTALLINE EPOXYCETON TRIPEPTIDES
US9045524B2 (en) 2009-05-21 2015-06-02 Novagenesis Foundation Selective caspase inhibitors and uses thereof
CN101928329B (en) * 2009-06-19 2013-07-17 北京大学 Tripeptide boric acid (ester) compound and preparation method and application thereof
PH12012501719A1 (en) * 2010-03-01 2012-11-12 Onyx Therapeutics Inc Compounds for immunoproteasome inhibition
US8697646B2 (en) 2010-04-07 2014-04-15 Onyx Therapeutics, Inc. Crystalline peptide epoxyketone immunoproteasome inhibitor
EP2697246B1 (en) 2011-04-15 2018-03-07 Genesis Technologies Limited Selective cysteine protease inhibitors and uses thereof
AR095426A1 (en) 2013-03-14 2015-10-14 Onyx Therapeutics Inc TRIPEPTIDE INHIBITORS OF PROTEASA EPOXYCETONE
EA030957B1 (en) * 2013-03-14 2018-10-31 Оникс Терапьютикс, Инк. Dipeptide and tripeptide epoxy ketone protease inhibitors
WO2015106200A2 (en) * 2014-01-10 2015-07-16 Cornell University Dipeptides as inhibitors of human immunoproteasomes
US11202817B2 (en) 2014-08-18 2021-12-21 Cornell University Dipeptidomimetics as inhibitors of human immunoproteasomes
WO2016050356A1 (en) * 2014-10-01 2016-04-07 Merck Patent Gmbh Boronic acid derivatives
EP3362754B1 (en) 2015-10-15 2021-12-22 Cornell University Proteasome inhibitors and uses thereof
EP3413977A1 (en) * 2016-02-10 2018-12-19 Axiava Pharma UG Dipeptidyl aldehydes for the treatment and/or prevention of parasitic diseases
US20210128667A1 (en) * 2017-08-23 2021-05-06 Kezar Life Sciences Immunoproteasome inhibitors and immunosuppressive agent in the treatment of autoimmune disorders
US11203613B2 (en) 2017-10-11 2021-12-21 Cornell University Peptidomimetic proteasome inhibitors
IL277402B1 (en) 2018-03-20 2026-04-01 Abraxis Bioscience Llc Methods of treating central nervous system disorders via administration of nanoparticles of an mtor inhibitor and an albumin
WO2022259049A1 (en) * 2021-06-08 2022-12-15 Alessio Fasano Antiviral larazotide derivatives
WO2023003882A2 (en) * 2021-07-19 2023-01-26 University Of North Carolina At Wilmington Compounds having selective inactivation activity

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5780454A (en) * 1994-10-28 1998-07-14 Proscript, Inc. Boronic ester and acid compounds

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2701932B2 (en) 1989-04-10 1998-01-21 サントリー株式会社 Protease inhibitor
EP0839155B1 (en) * 1995-07-17 2004-10-13 Medivir UK Ltd CYSTEINE PROTEASE INHIBITORS FOR USE IN TREATMENT OF IgE MEDIATED ALLERGIC DISEASES

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5780454A (en) * 1994-10-28 1998-07-14 Proscript, Inc. Boronic ester and acid compounds

Cited By (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9205126B2 (en) 2005-11-09 2015-12-08 Onyx Therapeutics, Inc. Compounds for enzyme inhibition
US9205125B2 (en) 2005-11-09 2015-12-08 Onyx Therapeutics, Inc. Compounds for enzyme inhibition
US9205124B2 (en) 2005-11-09 2015-12-08 Onyx Therapeutics, Inc. Compounds for enzyme inhibition
US9108989B2 (en) 2006-10-10 2015-08-18 Infinity Pharmaceuticals, Inc. Inhibitors of fatty acid amide hydrolase
US8921583B2 (en) 2007-10-04 2014-12-30 Onyx Therapeutics, Inc. Crystalline peptide epoxy ketone protease inhibitors and the synthesis of amino acid keto-epoxides
US8921324B2 (en) 2007-10-04 2014-12-30 Onyx Therapeutics, Inc. Crystalline peptide epoxy ketone protease inhibitors and the synthesis of amino acid keto-epoxides
US8957049B2 (en) 2008-04-09 2015-02-17 Infinity Pharmaceuticals, Inc. Inhibitors of fatty acid amide hydrolase
US8541581B2 (en) 2009-04-07 2013-09-24 Infinity Pharmaceuticals, Inc. Inhibitors of fatty acid amide hydrolase
US8546564B2 (en) 2009-04-07 2013-10-01 Infinity Pharmaceuticals, Inc. Inhibitors of fatty acid amide hydrolase
US8853147B2 (en) 2009-11-13 2014-10-07 Onyx Therapeutics, Inc. Use of peptide epoxyketones for metastasis suppression
US9034849B2 (en) 2010-02-03 2015-05-19 Infinity Pharmaceuticals, Inc. Fatty acid amide hydrolase inhibitors
US9309283B2 (en) 2012-07-09 2016-04-12 Onyx Therapeutics, Inc. Prodrugs of peptide epoxy ketone protease inhibitors
US9315542B2 (en) 2012-07-09 2016-04-19 Onyx Therapeutics, Inc. Prodrugs of peptide epoxy ketone protease inhibitors

Also Published As

Publication number Publication date
EP1863513A2 (en) 2007-12-12
WO2006099261A2 (en) 2006-09-21
US7589066B2 (en) 2009-09-15
US20060241056A1 (en) 2006-10-26

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