EP4734989A2 - Synthèse et caractérisation in vitro de chimères ciblant la protéolyse (protacs) pour la dégradation de l'adn méthyltransférase 1 (dnmt1) - Google Patents

Synthèse et caractérisation in vitro de chimères ciblant la protéolyse (protacs) pour la dégradation de l'adn méthyltransférase 1 (dnmt1)

Info

Publication number
EP4734989A2
EP4734989A2 EP24833014.4A EP24833014A EP4734989A2 EP 4734989 A2 EP4734989 A2 EP 4734989A2 EP 24833014 A EP24833014 A EP 24833014A EP 4734989 A2 EP4734989 A2 EP 4734989A2
Authority
EP
European Patent Office
Prior art keywords
compound
amino
formula
mmol
linker
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
EP24833014.4A
Other languages
German (de)
English (en)
Inventor
Jun Qi
Priscilla LIOW
Tingjian WANG
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 EP4734989A2 publication Critical patent/EP4734989A2/fr
Pending legal-status Critical Current

Links

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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

L'invention concerne des composés (agents de dégradation) qui ciblent DNMT1 pour la dégradation. L'invention concerne également des compositions pharmaceutiques contenant les composés et des procédés d'utilisation des composés pour traiter des maladies et troubles caractérisés ou médiés par une activité de DNMT1 aberrante.
EP24833014.4A 2023-06-29 2024-06-28 Synthèse et caractérisation in vitro de chimères ciblant la protéolyse (protacs) pour la dégradation de l'adn méthyltransférase 1 (dnmt1) Pending EP4734989A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202363523993P 2023-06-29 2023-06-29
PCT/US2024/036042 WO2025006902A2 (fr) 2023-06-29 2024-06-28 Synthèse et caractérisation in vitro de chimères ciblant la protéolyse (protacs) pour la dégradation de l'adn méthyltransférase 1 (dnmt1)

Publications (1)

Publication Number Publication Date
EP4734989A2 true EP4734989A2 (fr) 2026-05-06

Family

ID=93940010

Family Applications (1)

Application Number Title Priority Date Filing Date
EP24833014.4A Pending EP4734989A2 (fr) 2023-06-29 2024-06-28 Synthèse et caractérisation in vitro de chimères ciblant la protéolyse (protacs) pour la dégradation de l'adn méthyltransférase 1 (dnmt1)

Country Status (4)

Country Link
EP (1) EP4734989A2 (fr)
JP (1) JP2026523231A (fr)
CN (1) CN121368481A (fr)
WO (1) WO2025006902A2 (fr)

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017185036A1 (fr) * 2016-04-22 2017-10-26 Dana Farber Cancer Institute, Inc. Molécules bifonctionnelles pour la dégradation du egfr et méthodes d'utilisation
SG11201809559UA (en) * 2016-06-13 2018-12-28 Glaxosmithkline Ip Dev Ltd Substituted pyridines as inhibitors of dnmt1
CN114728936A (zh) * 2019-10-29 2022-07-08 豪夫迈·罗氏有限公司 用于治疗癌症的双功能化合物

Also Published As

Publication number Publication date
WO2025006902A3 (fr) 2025-06-12
WO2025006902A2 (fr) 2025-01-02
JP2026523231A (ja) 2026-07-13
CN121368481A (zh) 2026-01-20

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