AU2019224089B2 - Small molecules that block proteasome-associated ubiquitin receptor RPN13 function and uses thereof - Google Patents

Small molecules that block proteasome-associated ubiquitin receptor RPN13 function and uses thereof Download PDF

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Publication number
AU2019224089B2
AU2019224089B2 AU2019224089A AU2019224089A AU2019224089B2 AU 2019224089 B2 AU2019224089 B2 AU 2019224089B2 AU 2019224089 A AU2019224089 A AU 2019224089A AU 2019224089 A AU2019224089 A AU 2019224089A AU 2019224089 B2 AU2019224089 B2 AU 2019224089B2
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certain embodiments
alkyl
compound
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pharmaceutically acceptable
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AU2019224089A1 (en
Inventor
Kenneth C. Anderson
Dharminder Chauhan
Jun Qi
Yan SONG
Lei Wu
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Dana Farber Cancer Institute Inc
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Dana Farber Cancer Institute Inc
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug
    • A61K47/551—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug one of the codrug's components being a vitamin, e.g. niacinamide, vitamin B3, cobalamin, vitamin B12, folate, vitamin A or retinoic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicinal Preparation (AREA)
AU2019224089A 2018-02-23 2019-02-22 Small molecules that block proteasome-associated ubiquitin receptor RPN13 function and uses thereof Active AU2019224089B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862634632P 2018-02-23 2018-02-23
US62/634,632 2018-02-23
PCT/US2019/019162 WO2019165216A1 (en) 2018-02-23 2019-02-22 Small molecules that block proteasome-associated ubiquitin receptor rpn13 function and uses thereof

Publications (2)

Publication Number Publication Date
AU2019224089A1 AU2019224089A1 (en) 2020-08-13
AU2019224089B2 true AU2019224089B2 (en) 2024-10-10

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AU2019224089A Active AU2019224089B2 (en) 2018-02-23 2019-02-22 Small molecules that block proteasome-associated ubiquitin receptor RPN13 function and uses thereof

Country Status (6)

Country Link
US (1) US11702402B2 (https=)
EP (1) EP3755377A1 (https=)
JP (1) JP7389749B2 (https=)
AU (1) AU2019224089B2 (https=)
CA (1) CA3090414A1 (https=)
WO (1) WO2019165216A1 (https=)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3807272A1 (en) 2018-06-13 2021-04-21 Amphista Therapeutics Ltd Bifunctional molecules for targeting rpn11
NZ793813A (en) * 2020-04-29 2025-12-19 Onegene Biotechnology Inc Novel protein conjugate, and use thereof for preventing or treating nonalcoholic steatohepatitis, obesity and diabetes
US20240245787A1 (en) 2021-04-13 2024-07-25 President And Fellows Of Harvard College E3 ligase binders and uses thereof
CN115260212B (zh) * 2022-08-01 2023-05-23 桂林医学院 3,5-双(亚苄基)-4-哌啶酮衍生物及其制备方法和应用
US20250137057A1 (en) * 2023-10-26 2025-05-01 The Chinese University Of Hong Kong Adrm1/rpn13 spliced variant in the prognosis and treatment of hepatocellular carcinoma
WO2025207482A1 (en) * 2024-03-25 2025-10-02 Augusta University Research Institute, Inc. Diarylpiperidone hybrid conjugates and methods of use thereof

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20150291562A1 (en) * 2014-04-14 2015-10-15 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
US20160106725A1 (en) * 2013-05-08 2016-04-21 The Johns Hopkins University Novel bis-Benzylidine Piperidone Proteasome Inhibitor with Anticancer Activity

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20160106725A1 (en) * 2013-05-08 2016-04-21 The Johns Hopkins University Novel bis-Benzylidine Piperidone Proteasome Inhibitor with Anticancer Activity
US20150291562A1 (en) * 2014-04-14 2015-10-15 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use

Also Published As

Publication number Publication date
JP2021514955A (ja) 2021-06-17
AU2019224089A1 (en) 2020-08-13
WO2019165216A1 (en) 2019-08-29
JP7389749B2 (ja) 2023-11-30
US11702402B2 (en) 2023-07-18
US20210130324A1 (en) 2021-05-06
EP3755377A1 (en) 2020-12-30
CA3090414A1 (en) 2019-08-29

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