JP7631191B2 - Ｅ３リガーゼの共有結合による標的化 - Google Patents

Ｅ３リガーゼの共有結合による標的化 Download PDF

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JP7631191B2
JP7631191B2 JP2021519602A JP2021519602A JP7631191B2 JP 7631191 B2 JP7631191 B2 JP 7631191B2 JP 2021519602 A JP2021519602 A JP 2021519602A JP 2021519602 A JP2021519602 A JP 2021519602A JP 7631191 B2 JP7631191 B2 JP 7631191B2
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rnf114
nimbolide
cells
231mfp
substituted
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JPWO2020076996A5 (enExample
JP2022512643A (ja
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スプラドリン，ジェシカ
ワード，カール・シー
ノムラ，ダニエル・ケイ
シルル，マルクス
タラリコ，ジョン・エイ
マッケナ，ジェフリー
マイモニ，トーマス・ジョン
フー，シールイ
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ザ・リージエンツ・オブ・ザ・ユニバーシテイー・オブ・カリフオルニア
ノバルティス アーゲー
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    • 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, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Other Investigation Or Analysis Of Materials By Electrical Means (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
JP2021519602A 2018-10-09 2019-10-09 Ｅ３リガーゼの共有結合による標的化 Active JP7631191B2 (ja)

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JP2025017433A JP2025072508A (ja) 2018-10-09 2025-02-05 Ｅ３リガーゼの共有結合による標的化

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US201862743337P 2018-10-09 2018-10-09
US62/743,337 2018-10-09
PCT/US2019/055461 WO2020076996A1 (en) 2018-10-09 2019-10-09 Covalent targeting of e3 ligases

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JP2022512643A JP2022512643A (ja) 2022-02-07
JPWO2020076996A5 JPWO2020076996A5 (enExample) 2022-10-18
JP7631191B2 true JP7631191B2 (ja) 2025-02-18

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US (2) US12161648B2 (enExample)
EP (1) EP3863642A4 (enExample)
JP (2) JP7631191B2 (enExample)
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WO (1) WO2020076996A1 (enExample)

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US11666661B2 (en) 2018-03-23 2023-06-06 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
JP7774612B2 (ja) * 2020-07-30 2025-11-21 サノフイ アクリルアミド置換インダン化合物およびその治療的使用
AU2022205670A1 (en) * 2021-01-08 2023-07-13 The Board Of Regents Of The University Of Texas System Nimbolide analogs and methods of use thereof
WO2022187650A1 (en) * 2021-03-04 2022-09-09 The Scripps Research Institute Heterobifunctional compositions for targeted protein degradation and methods for their use
AU2022246282A1 (en) * 2021-03-25 2023-10-12 Technion Research & Development Foundation Limited Rnf4 targeting 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
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
TW202416958A (zh) * 2022-10-13 2024-05-01 南韓商韓美藥品股份有限公司 用於抑制yap-tead交互作用的新穎雜雙環化合物及包含其之藥學組成物
EP4605088A1 (en) * 2022-10-21 2025-08-27 Novartis AG Molecular glue degrader compounds and uses thereof
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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WO2017180417A1 (en) 2016-04-12 2017-10-19 The Regents Of The University Of Michigan Bet protein degraders
WO2018052945A1 (en) 2016-09-13 2018-03-22 The Regents Of The University Of Michigan Fused 1,4-oxazepines as bet protein degraders
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
WO2020146779A1 (en) 2019-01-11 2020-07-16 The Regents Of The University Of California mTORC1 INHIBITORS FOR ACTIVATING AUTOPHAGY

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CA2443370A1 (en) * 2002-10-17 2004-04-17 Mount Sinai Hospital Structures of substrate binding pockets of scf complexes
DK2571503T3 (en) * 2010-05-14 2015-04-20 Dana Farber Cancer Inst Inc COMPOSITIONS AND THEIR USE IN THE TREATMENT OF NEOPLASIA, INFLAMMATORY DISEASE AND OTHER DISORDERS
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
US20150119435A1 (en) * 2012-05-11 2015-04-30 Yale University Compounds useful for promoting protein degradation and methods using 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
KR20240108531A (ko) * 2015-05-29 2024-07-09 더 트러스티스 오브 더 유니버시티 오브 펜실바니아 잘못 접혀진 단백질의 분해를 위한 조성물 및 방법
RU2742035C2 (ru) 2015-11-25 2021-02-01 Дана-Фарбер Кэнсер Инститьют, Инк. Бивалентные ингибиторы бромодоменов и пути их применения

Patent Citations (4)

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US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
WO2017180417A1 (en) 2016-04-12 2017-10-19 The Regents Of The University Of Michigan Bet protein degraders
WO2018052945A1 (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

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US20250120982A1 (en) 2025-04-17
WO2020076996A1 (en) 2020-04-16
EP3863642A1 (en) 2021-08-18
JP2022512643A (ja) 2022-02-07
CN120468320A (zh) 2025-08-12
CN113164495B (zh) 2025-04-22
EP3863642A4 (en) 2022-06-29
US12161648B2 (en) 2024-12-10
JP2025072508A (ja) 2025-05-09
CN113164495A (zh) 2021-07-23
US20210369731A1 (en) 2021-12-02

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