WO2025006902A3 - 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) Download PDF

Info

Publication number
WO2025006902A3
WO2025006902A3 PCT/US2024/036042 US2024036042W WO2025006902A3 WO 2025006902 A3 WO2025006902 A3 WO 2025006902A3 US 2024036042 W US2024036042 W US 2024036042W WO 2025006902 A3 WO2025006902 A3 WO 2025006902A3
Authority
WO
WIPO (PCT)
Prior art keywords
degradation
dnmt1
compounds
protacs
synthesis
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/US2024/036042
Other languages
English (en)
Other versions
WO2025006902A2 (fr
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
Priority to EP24833014.4A priority Critical patent/EP4734989A2/fr
Priority to CN202480042233.XA priority patent/CN121368481A/zh
Publication of WO2025006902A2 publication Critical patent/WO2025006902A2/fr
Publication of WO2025006902A3 publication Critical patent/WO2025006902A3/fr
Anticipated expiration legal-status Critical
Ceased 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)

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.
PCT/US2024/036042 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) Ceased WO2025006902A2 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
EP24833014.4A 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)
CN202480042233.XA CN121368481A (zh) 2023-06-29 2024-06-28 用于降解dna甲基转移酶1 (dnmt1)的蛋白水解靶向嵌合体(protacs)的合成和体外表征

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202363523993P 2023-06-29 2023-06-29
US63/523,993 2023-06-29

Publications (2)

Publication Number Publication Date
WO2025006902A2 WO2025006902A2 (fr) 2025-01-02
WO2025006902A3 true WO2025006902A3 (fr) 2025-06-12

Family

ID=93940010

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2024/036042 Ceased 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)

Country Status (3)

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

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20190194166A1 (en) * 2016-06-13 2019-06-27 Glaxosmithkline Intellectual Property Development Limited Substituted pyridines as inhibitors of dnmt1
US20220017510A1 (en) * 2016-04-22 2022-01-20 Dana-Farber Cancer Institute, Inc. Bifunctional molecules for degradation of egfr and methods of use
US20230024096A1 (en) * 2019-10-29 2023-01-26 Hoffmann-La Roche Inc. Bifunctional compounds for the treatment of cancer

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20220017510A1 (en) * 2016-04-22 2022-01-20 Dana-Farber Cancer Institute, Inc. Bifunctional molecules for degradation of egfr and methods of use
US20190194166A1 (en) * 2016-06-13 2019-06-27 Glaxosmithkline Intellectual Property Development Limited Substituted pyridines as inhibitors of dnmt1
US20230024096A1 (en) * 2019-10-29 2023-01-26 Hoffmann-La Roche Inc. Bifunctional compounds for the treatment of cancer

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
DATABASE Pubchem compound 29 January 2018 (2018-01-29), ANONYMOUS: "2-(3,5-Dicyano-4-ethyl-6-piperidin1-ylpyridin-2-yl)sulfanyl-2- phenylacetamide", XP093327236, retrieved from Pubchem Database accession no. 132248944 *

Also Published As

Publication number Publication date
WO2025006902A2 (fr) 2025-01-02
EP4734989A2 (fr) 2026-05-06
CN121368481A (zh) 2026-01-20

Similar Documents

Publication Publication Date Title
Plyta et al. Inhibition of topoisomerase I by naphthoquinone derivatives
Shoyab et al. Structure and function of human amphiregulin: a member of the epidermal growth factor family
Capranico et al. DNA topoisomerase-trapping antitumour drugs
Barciszewski et al. Kinetin—45 years on
Pflaum et al. Visible light generates oxidative DNA base modifications in high excess of strand breaks in mammalian cells
Hartley et al. DNA alkylation and interstrand cross-linking by treosulfan
Niggli et al. Cyclobutane-type pyrimidine photodimer formation and excision in human skin fibroblasts after irradiation with 313-nm ultraviolet light
Bae et al. A novel synthesized tyrosinase inhibitor:(E)-2-((2, 4-dihydroxyphenyl) diazenyl) phenyl 4-methylbenzenesulfonate as an azo-resveratrol analog
WO1999009000A3 (fr) Nouveaux inhibiteurs de l'aggrecanase et des metalloproteinases matricielles pour le traitement de l'arthrite
Modrzejewska et al. Vitamin C enhances substantially formation of 5-hydroxymethyluracil in cellular DNA
Yu et al. Anticancer drug discovery targeting DNA hypermethylation
MXPA05008688A (es) Derivados tetraciclicos de pirazol como inhibidores de la cinasa, procedimiento para su preparacion y composiciones farmaceuticas que los comprenden.
Yu et al. Antiproliferative and apoptotic activities of sequence-specific histone acetyltransferase inhibitors
CN118785908A (zh) 四环类化合物在治疗肿瘤中的应用
Ratter et al. S-adenosylhomocysteine as a physiological modulator of Apo-1-mediated apoptosis
WO2025006902A3 (fr) Synthèse et caractérisation in vitro de chimères ciblant la protéolyse (protacs) pour la dégradation de l'adn méthyltransférase 1 (dnmt1)
EP0689586B8 (fr) Activite et fonction de la proteine virale r
AU7385398A (en) Novel macrocyclic compounds as metalloprotease inhibitors
Jin et al. Oligosaccharides from Sargassum thunbergii inhibit osteoclast differentiation via regulation of IRF-8 signaling
Feng et al. DNA methyltransferase 3A: a significant target for the discovery of inhibitors as potent anticancer drugs
Yoshimura et al. Interstrand photocrosslinking of DNA via p-carbamoylvinyl phenol nucleoside
Jack et al. The distribution of benzo (a) pyrene DNA adducts in mammalian chromatin
Arabiyat et al. Antilipolytic-Antiproliferative Activity of Novel Antidiabesity Triazolo/Fluoroquinolones.
WO2000020026A3 (fr) Compositions et methodes permettant d'inhiber l'angiogenese
Iyengar et al. Alkylation of DNA by C-10 of 2, 7-diaminomitosene

Legal Events

Date Code Title Description
121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 24833014

Country of ref document: EP

Kind code of ref document: A2

WWE Wipo information: entry into national phase

Ref document number: 2024833014

Country of ref document: EP

NENP Non-entry into the national phase

Ref country code: DE

ENP Entry into the national phase

Ref document number: 2024833014

Country of ref document: EP

Effective date: 20260129

ENP Entry into the national phase

Ref document number: 2024833014

Country of ref document: EP

Effective date: 20260129