CN120468320A - E3连接酶的共价靶向 - Google Patents

E3连接酶的共价靶向

Info

Publication number
CN120468320A
CN120468320A CN202510552209.7A CN202510552209A CN120468320A CN 120468320 A CN120468320 A CN 120468320A CN 202510552209 A CN202510552209 A CN 202510552209A CN 120468320 A CN120468320 A CN 120468320A
Authority
CN
China
Prior art keywords
substituted
unsubstituted
membered
substituent
nhc
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
CN202510552209.7A
Other languages
English (en)
Chinese (zh)
Inventor
J·斯普拉德林
C·C·沃德
D·K·野村
M·席尔勒
J·A·塔拉里科
J·麦肯纳
T·J·马伊莫内
胡曦睿
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.)
Morphochem GmbH
University of California San Diego UCSD
Original Assignee
Morphochem AG fuer Kombinatorische Chemie
University of California San Diego UCSD
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 Morphochem AG fuer Kombinatorische Chemie, University of California San Diego UCSD filed Critical Morphochem AG fuer Kombinatorische Chemie
Publication of CN120468320A publication Critical patent/CN120468320A/zh
Pending legal-status Critical Current

Links

Classifications

    • 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
    • C07D495/14—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365—Lactones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4535—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
    • 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
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Peptides Or Proteins (AREA)
  • Other Investigation Or Analysis Of Materials By Electrical Means (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
CN202510552209.7A 2018-10-09 2019-10-09 E3连接酶的共价靶向 Pending CN120468320A (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201862743337P 2018-10-09 2018-10-09
US62/743,337 2018-10-09
CN201980079494.8A CN113164495B (zh) 2018-10-09 2019-10-09 E3连接酶的共价靶向
PCT/US2019/055461 WO2020076996A1 (en) 2018-10-09 2019-10-09 Covalent targeting of e3 ligases

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN201980079494.8A Division CN113164495B (zh) 2018-10-09 2019-10-09 E3连接酶的共价靶向

Publications (1)

Publication Number Publication Date
CN120468320A true CN120468320A (zh) 2025-08-12

Family

ID=70164411

Family Applications (2)

Application Number Title Priority Date Filing Date
CN202510552209.7A Pending CN120468320A (zh) 2018-10-09 2019-10-09 E3连接酶的共价靶向
CN201980079494.8A Active CN113164495B (zh) 2018-10-09 2019-10-09 E3连接酶的共价靶向

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN201980079494.8A Active CN113164495B (zh) 2018-10-09 2019-10-09 E3连接酶的共价靶向

Country Status (5)

Country Link
US (2) US12161648B2 (https=)
EP (1) EP3863642A4 (https=)
JP (2) JP7631191B2 (https=)
CN (2) CN120468320A (https=)
WO (1) WO2020076996A1 (https=)

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WO2019183600A1 (en) 2018-03-23 2019-09-26 The Regents Of The University Of California Methods and compounds for targeted autophagy
GB202005876D0 (en) * 2020-04-22 2020-06-03 Univ Dundee Protein degradation
US12441679B2 (en) 2020-07-30 2025-10-14 Sanofi Acrylamide-substituted indane compounds and therapeutic use thereof
KR20230144008A (ko) * 2021-01-08 2023-10-13 더 보드 오브 리젠츠 오브 더 유니버시티 오브 텍사스 시스템 님볼리드 유사체 및 이의 사용 방법
CN117042765A (zh) * 2021-01-08 2023-11-10 德克萨斯大学系统董事会 印苦楝内酯类似物及其使用方法
WO2022187650A1 (en) * 2021-03-04 2022-09-09 The Scripps Research Institute Heterobifunctional compositions for targeted protein degradation and methods for their use
EP4313979A4 (en) * 2021-03-25 2025-02-19 Technion Research & Development Foundation Limited RNF4-TARGETED COMPOUNDS AND USES THEREOF
CN113527270B (zh) * 2021-07-16 2024-03-01 河南大学 一种靶向单酰基甘油脂肪酶的protac分子的医药中间体、制备方法及应用
CN116676273A (zh) * 2022-02-22 2023-09-01 中国科学院深圳先进技术研究院 一种蛋白水解靶向流感病毒及其制备方法和应用
CN114560908B (zh) * 2022-03-11 2024-10-25 国家纳米科学中心 一种多肽protac分子及其制备方法和应用
EP4514780A4 (en) * 2022-04-29 2026-04-29 Dong A St Co Ltd BICYCLIC COMPOUNDS USED AS TEAD INHIBITORS
CN115417913B (zh) * 2022-08-26 2024-10-29 天津医科大学 靶向雌激素受体的谷胱甘肽响应protac降解剂的制备方法及应用
WO2024080793A1 (en) * 2022-10-13 2024-04-18 Hanmi Pharm. Co., Ltd. Novel heterobicyclic compound for inhibiting yap-tead interaction and pharmaceutical composition comprising same
WO2024086361A1 (en) * 2022-10-21 2024-04-25 Novartis Ag Molecular glue degrader compounds and uses thereof
CN117263865B (zh) * 2023-08-04 2026-03-27 南开大学 以6,6-二甲基双环[3.1.1]-2-甲胺为疏水基团的蛋白降解剂及其制备方法、药物组合物和应用
WO2025226951A1 (en) * 2024-04-24 2025-10-30 Novartis Ag Molecular glue degrader compounds and uses thereof
CN119331047B (zh) * 2024-10-09 2025-09-30 重庆医科大学 一种蛋白水解靶向嵌合体及其制备方法
CN119405823B (zh) * 2024-11-15 2025-10-21 湖南大学 一种基于g四链体rna的蛋白降解靶向嵌合体及其制备方法与应用

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040171074A1 (en) * 2002-10-17 2004-09-02 Mount Sinai Hospital Structures of substrate binding pockets of SCF complexes
PL2902030T3 (pl) 2010-05-14 2017-07-31 Dana-Farber Cancer Institute, Inc. Związki tienotriazolodiazepinowe do leczenia nowotworu
CN101928747B (zh) * 2010-08-31 2012-08-08 中国人民解放军第二军医大学 E3泛素连接酶chip在脑胶质瘤疾病中的应用
WO2013170147A1 (en) 2012-05-11 2013-11-14 Yale University Compounds useful for promoting protein degradation and methods using same
US20180228907A1 (en) * 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
CN104017879A (zh) * 2014-06-16 2014-09-03 山东大学 Fbxo31基因及其相关产物在制备胃癌诊断试剂中的应用
MX2017015373A (es) * 2015-05-29 2018-07-06 Univ Pennsylvania COMPOSICIONES Y Mí‰TODOS PARA LA DEGRADACIí“N DE PROTEíNAS MAL PLEGADAS.
MX2018006499A (es) * 2015-11-25 2018-08-01 Dana Farber Cancer Inst Inc Inhibidores de bromodominio bivalentes y usos de los mismos.
KR20180132861A (ko) * 2016-04-12 2018-12-12 더 리젠츠 오브 더 유니버시티 오브 미시간 Bet 단백질 분해제
CA3036834A1 (en) * 2016-09-13 2018-03-22 The Regents Of The University Of Michigan Fused 1,4-oxazepines as bet protein degraders
WO2020146779A1 (en) 2019-01-11 2020-07-16 The Regents Of The University Of California mTORC1 INHIBITORS FOR ACTIVATING AUTOPHAGY

Also Published As

Publication number Publication date
CN113164495A (zh) 2021-07-23
WO2020076996A1 (en) 2020-04-16
JP2022512643A (ja) 2022-02-07
CN113164495B (zh) 2025-04-22
JP2025072508A (ja) 2025-05-09
EP3863642A4 (en) 2022-06-29
US20210369731A1 (en) 2021-12-02
EP3863642A1 (en) 2021-08-18
US20250120982A1 (en) 2025-04-17
US12161648B2 (en) 2024-12-10
JP7631191B2 (ja) 2025-02-18

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