CA3090414A1 - 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
CA3090414A1
CA3090414A1 CA3090414A CA3090414A CA3090414A1 CA 3090414 A1 CA3090414 A1 CA 3090414A1 CA 3090414 A CA3090414 A CA 3090414A CA 3090414 A CA3090414 A CA 3090414A CA 3090414 A1 CA3090414 A1 CA 3090414A1
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CA
Canada
Prior art keywords
compound
certain embodiments
pharmaceutically acceptable
alkyl
acceptable salt
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.)
Pending
Application number
CA3090414A
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English (en)
French (fr)
Inventor
Lei Wu
Kenneth C. Anderson
Jun Qi
Yan SONG
Dharminder Chauhan
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.)
Dana Farber Cancer Institute Inc
Original Assignee
Dana Farber Cancer Institute Inc
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 Dana Farber Cancer Institute Inc filed Critical Dana Farber Cancer Institute Inc
Publication of CA3090414A1 publication Critical patent/CA3090414A1/en
Pending legal-status Critical Current

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Classifications

    • 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
    • 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
    • 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)
CA3090414A 2018-02-23 2019-02-22 Small molecules that block proteasome-associated ubiquitin receptor rpn13 function and uses thereof Pending CA3090414A1 (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 (1)

Publication Number Publication Date
CA3090414A1 true CA3090414A1 (en) 2019-08-29

Family

ID=65724533

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3090414A Pending CA3090414A1 (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

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014182744A1 (en) * 2013-05-08 2014-11-13 The Johns Hopkins University Novel bis-benzylidine piperidone proteasome inhibitor with anticancer activity
RU2738833C9 (ru) * 2014-04-14 2022-02-28 Арвинас, Оперэйшнз, Инк. Имидные модуляторы протеолиза и способы их применения

Also Published As

Publication number Publication date
JP2021514955A (ja) 2021-06-17
AU2019224089A1 (en) 2020-08-13
WO2019165216A1 (en) 2019-08-29
AU2019224089B2 (en) 2024-10-10
JP7389749B2 (ja) 2023-11-30
US11702402B2 (en) 2023-07-18
US20210130324A1 (en) 2021-05-06
EP3755377A1 (en) 2020-12-30

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