CN114174281B - 细胞周期蛋白依赖性激酶7(cdk7)的降解剂及其用途 - Google Patents

细胞周期蛋白依赖性激酶7(cdk7)的降解剂及其用途 Download PDF

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CN114174281B
CN114174281B CN202080050815.4A CN202080050815A CN114174281B CN 114174281 B CN114174281 B CN 114174281B CN 202080050815 A CN202080050815 A CN 202080050815A CN 114174281 B CN114174281 B CN 114174281B
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compound
pharmaceutically acceptable
bispecific compound
cancer
acceptable salt
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CN114174281A (zh
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杜广艳
纳撒尼尔·S·格雷
张庭湖
何志祥
尼古拉斯·克维亚特科夫斯基
姜杰
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Dana Farber Cancer Institute Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • 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
    • A61K47/545—Heterocyclic compounds
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN202080050815.4A 2019-08-05 2020-08-04 细胞周期蛋白依赖性激酶7(cdk7)的降解剂及其用途 Active CN114174281B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962882958P 2019-08-05 2019-08-05
US62/882,958 2019-08-05
PCT/US2020/044815 WO2021026109A1 (en) 2019-08-05 2020-08-04 Degraders of cyclin-dependent kinase 7 (cdk7) and uses thereof

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CN114174281A CN114174281A (zh) 2022-03-11
CN114174281B true CN114174281B (zh) 2025-02-07

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US (1) US12491251B2 (enExample)
EP (1) EP4010336B1 (enExample)
JP (1) JP7636388B2 (enExample)
CN (1) CN114174281B (enExample)
AU (1) AU2020324408B2 (enExample)
CA (1) CA3149374A1 (enExample)
ES (1) ES3031581T3 (enExample)
WO (1) WO2021026109A1 (enExample)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10870651B2 (en) 2014-12-23 2020-12-22 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
CN107427521B (zh) 2015-03-27 2021-08-03 达纳-法伯癌症研究所股份有限公司 细胞周期蛋白依赖性激酶的抑制剂
EP3810132A4 (en) 2018-06-25 2022-06-22 Dana-Farber Cancer Institute, Inc. TAIRE FAMILY KINASE INHIBITORS AND RELATED USES
CN113164477A (zh) 2018-12-14 2021-07-23 达纳-法伯癌症研究所股份有限公司 C-jun-n-末端激酶的吡唑并吡啶抑制剂及其用途
EP3902542A4 (en) 2018-12-28 2022-09-07 Dana-Farber Cancer Institute, Inc. CYCLIN DEPENDENT KINASE 7 INHIBITORS AND USES THEREOF
CA3166135A1 (en) * 2019-12-24 2021-07-01 Dana-Farber Cancer Institute, Inc. The combination of cyclin dependent kinase 7 inhibitor and immunotherapy for treatment of cancer
CN117242060B (zh) 2021-01-13 2026-07-17 蒙特罗莎治疗股份有限公司 异吲哚啉酮化合物
CA3217792A1 (en) 2021-05-07 2022-11-10 Kymera Therapeutics, Inc Cdk2 degraders and uses thereof
CN113234081A (zh) * 2021-05-27 2021-08-10 东南大学 一种吡咯并吡唑衍生物与dmpeda做脲的制备方法
WO2022248682A1 (en) * 2021-05-28 2022-12-01 Qurient Co., Ltd. Compounds for degradation of cyclin-dependent kinase 7 (cdk7)
CN116396295A (zh) * 2023-04-04 2023-07-07 合肥工业大学 一种基于protac的plk1降解剂的合成方法
WO2025252190A1 (en) * 2024-06-07 2025-12-11 Cullgen Inc. Targeted degraders of werner syndrome recq helicase
CN119119072B (zh) * 2024-08-23 2025-10-03 武汉大学 一种用于检测和降解ERα的诊疗一体化ERαPROTACs化合物及其制备方法与应用

Citations (1)

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CN108366992A (zh) * 2015-11-02 2018-08-03 耶鲁大学 蛋白水解靶向嵌合体化合物及其制备和应用方法

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CA2416527C (en) 2000-08-10 2009-12-22 Pharmacia Italia S.P.A. Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
US7968569B2 (en) 2002-05-17 2011-06-28 Celgene Corporation Methods for treatment of multiple myeloma using 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione
US9345705B2 (en) 2011-09-15 2016-05-24 Merck Sharp & Dohme Corp. Compositions and methods for treating cancer
WO2013070688A1 (en) 2011-11-11 2013-05-16 Yale University Reprogramming urokinase into an antibody-recruiting anticancer agent
KR102438072B1 (ko) 2012-01-12 2022-08-31 예일 유니버시티 E3 유비퀴틴 리가아제에 의한 표적 단백질 및 다른 폴리펩티드의 증진된 분해를 위한 화합물 및 방법
US10870651B2 (en) * 2014-12-23 2020-12-22 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
AU2016232705C1 (en) * 2015-03-18 2021-06-17 Arvinas, Inc. Compounds and methods for the enhanced degradation of targeted proteins
AU2016281225B2 (en) * 2015-06-15 2020-10-15 Ube Corporation Substituted dihydropyrrolopyrazole derivative
AU2017254702B2 (en) 2016-04-22 2020-12-24 Dana-Farber Cancer Institute, Inc. Degradation of cyclin-dependent kinase 9 (CDK9) by conjugation of CDK9 inhibitors with E3 ligase ligand and methods of use
CN121974842A (zh) * 2016-05-10 2026-05-05 C4医药公司 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体
CA3045037A1 (en) * 2016-12-08 2018-06-14 Icahn School Of Medicine At Mount Sinai Compositions and methods for treating cdk4/6-mediated cancer
CN109516989B (zh) 2017-09-17 2021-12-31 上海美志医药科技有限公司 一类抑制并降解cdk的化合物

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Publication number Priority date Publication date Assignee Title
CN108366992A (zh) * 2015-11-02 2018-08-03 耶鲁大学 蛋白水解靶向嵌合体化合物及其制备和应用方法

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Publication number Publication date
US12491251B2 (en) 2025-12-09
US20220280649A1 (en) 2022-09-08
JP2022543231A (ja) 2022-10-11
AU2020324408B2 (en) 2026-03-12
JP7636388B2 (ja) 2025-02-26
CA3149374A1 (en) 2021-02-11
WO2021026109A1 (en) 2021-02-11
CN114174281A (zh) 2022-03-11
EP4010336B1 (en) 2025-04-02
EP4010336A1 (en) 2022-06-15
AU2020324408A1 (en) 2021-12-16
ES3031581T3 (en) 2025-07-09
EP4010336A4 (en) 2023-08-23

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