CA3103185A1 - Bifunctional molecules for targeting rpn11 - Google Patents

Bifunctional molecules for targeting rpn11 Download PDF

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Publication number
CA3103185A1
CA3103185A1 CA3103185A CA3103185A CA3103185A1 CA 3103185 A1 CA3103185 A1 CA 3103185A1 CA 3103185 A CA3103185 A CA 3103185A CA 3103185 A CA3103185 A CA 3103185A CA 3103185 A1 CA3103185 A1 CA 3103185A1
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CA
Canada
Prior art keywords
group
linker
rnh
nhme
sme
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Pending
Application number
CA3103185A
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English (en)
French (fr)
Inventor
Alessio CIULLI
Andrea TESTA
Scott Hughes
Steven Peter Butcher
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Amphista Therapeutics Ltd
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Amphista Therapeutics Ltd
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Publication of CA3103185A1 publication Critical patent/CA3103185A1/en
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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
    • A61K47/56—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
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    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
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    • 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
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    • 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
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 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
    • C07D495/12—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 three hetero rings
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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
CA3103185A 2018-06-13 2019-06-13 Bifunctional molecules for targeting rpn11 Pending CA3103185A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201862684265P 2018-06-13 2018-06-13
US62/684,265 2018-06-13
US201962835953P 2019-04-18 2019-04-18
US62/835,953 2019-04-18
PCT/EP2019/065481 WO2019238817A1 (en) 2018-06-13 2019-06-13 Bifunctional molecules for targeting rpn11

Publications (1)

Publication Number Publication Date
CA3103185A1 true CA3103185A1 (en) 2019-12-19

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CA3103185A Pending CA3103185A1 (en) 2018-06-13 2019-06-13 Bifunctional molecules for targeting rpn11

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US (1) US11925690B2 (enExample)
EP (1) EP3807272A1 (enExample)
JP (1) JP2021527137A (enExample)
KR (1) KR20210021016A (enExample)
CN (1) CN112533918A (enExample)
CA (1) CA3103185A1 (enExample)
WO (1) WO2019238817A1 (enExample)

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PE20240545A1 (es) 2020-12-18 2024-03-19 Amphista Therapeutics Ltd Moleculas bifuncionales novedosas para la degradacion de proteinas dirigidas
MX2024004525A (es) * 2021-10-14 2024-05-24 Cullgen Shanghai Inc Proteinas modificadas y degradadores de proteinas.
CN114959036A (zh) * 2022-06-07 2022-08-30 北京大学 Rpn11标记物在检测骨髓瘤及其患病风险、预后分析及治疗药物中的应用
WO2023242598A1 (en) 2022-06-16 2023-12-21 Amphista Therapeutics Limited Bifunctional molecules for targeted protein degradation
JP2025525347A (ja) 2022-06-16 2025-08-05 アンフィスタ セラピューティクス リミテッド 標的タンパク質分解のための新規の二官能性分子
CA3267147A1 (en) 2022-09-13 2024-03-21 Amphista Therapeutics Limited COMPOUNDS FOR THE TARGETED DEGRADATION OF A PROTEIN
IL319486A (en) 2022-10-07 2025-05-01 Pfizer HSD17B13 Inhibitors and/or Retarders
JP2025541231A (ja) 2022-12-16 2025-12-18 ファイザー・インク ３－フルオロ－４－ヒドロキシベンズアミド含有阻害剤および／または分解剤ならびにそれらの使用
US20250188030A1 (en) 2023-12-07 2025-06-12 Pfizer Inc. Biphenyl and Phenylpyridine Compounds
GB202319256D0 (en) 2023-12-15 2024-01-31 Amphista Therapeutics Ltd Novel compounds for targeted protein degradation
WO2026088071A1 (en) 2024-10-23 2026-04-30 Pfizer Inc. Substituted fused heteroaryl lactam compounds

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JP2021527137A (ja) 2021-10-11
KR20210021016A (ko) 2021-02-24
CN112533918A (zh) 2021-03-19

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