JP2022529700A - サイクリン依存性キナーゼ１２（ｃｄｋ１２）の分解剤およびその使用 - Google Patents

サイクリン依存性キナーゼ１２（ｃｄｋ１２）の分解剤およびその使用 Download PDF

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JP2022529700A
JP2022529700A JP2021562085A JP2021562085A JP2022529700A JP 2022529700 A JP2022529700 A JP 2022529700A JP 2021562085 A JP2021562085 A JP 2021562085A JP 2021562085 A JP2021562085 A JP 2021562085A JP 2022529700 A JP2022529700 A JP 2022529700A
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JP2022529700A5 (enExample
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チェ，ジャンウェイ
グレイ，ナサナエル，エス．
ジャン，ティンフー
ジャン，バイシャン
ガオ，ヤン
クフャトコフスキ，ニコラス，ポール
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ダナ－ファーバー キャンサー インスティテュート，インコーポレイテッド
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    • 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
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • A61K47/555—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 pre-targeting systems involving an organic compound, other than a peptide, protein or antibody, for targeting specific cells
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
JP2021562085A 2019-04-23 2020-04-23 サイクリン依存性キナーゼ１２（ｃｄｋ１２）の分解剤およびその使用 Pending JP2022529700A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962837331P 2019-04-23 2019-04-23
US62/837,331 2019-04-23
PCT/US2020/029483 WO2020219650A1 (en) 2019-04-23 2020-04-23 Degraders of cyclin-dependent kinase 12 (cdk12) and uses thereof

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JP2022529700A true JP2022529700A (ja) 2022-06-23
JP2022529700A5 JP2022529700A5 (enExample) 2023-05-01

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US (1) US12662464B2 (enExample)
EP (1) EP3958861A4 (enExample)
JP (1) JP2022529700A (enExample)
CN (1) CN113993519B (enExample)
AU (1) AU2020263390B2 (enExample)
CA (1) CA3132387A1 (enExample)
WO (1) WO2020219650A1 (enExample)

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US10357493B2 (en) 2017-03-10 2019-07-23 Selenity Therapeutics (Bermuda), Ltd. Metalloenzyme inhibitor compounds
US11458149B1 (en) 2019-05-31 2022-10-04 Ikena Oncology, Inc. TEAD inhibitors and uses thereof
BR112021024108A2 (pt) 2019-05-31 2022-03-22 Ikena Oncology Inc Inibidores de tead e usos dos mesmos
EP3976621A4 (en) * 2019-06-03 2023-11-15 Regents of the University of Minnesota COMPOUNDS THAT DEGRADE KINASES AND THEIR USES
CN114727974A (zh) 2019-07-30 2022-07-08 艾科尼佐治疗股份有限公司 Hdac6抑制剂及其用途
WO2022120355A1 (en) * 2020-12-02 2022-06-09 Ikena Oncology, Inc. Tead degraders and uses thereof
WO2022169985A1 (en) 2021-02-03 2022-08-11 Eikonizo Therapeutics, Inc. Hdac6 inhibitors and uses thereof
CA3217792A1 (en) 2021-05-07 2022-11-10 Kymera Therapeutics, Inc Cdk2 degraders and uses thereof
AU2022362494A1 (en) * 2021-10-14 2024-05-23 Cullgen (Shanghai), Inc. Modified proteins and protein degraders
TW202329937A (zh) 2021-12-03 2023-08-01 美商英塞特公司 雙環胺ｃｋ１２抑制劑
US12084453B2 (en) 2021-12-10 2024-09-10 Incyte Corporation Bicyclic amines as CDK12 inhibitors
WO2023143482A1 (zh) * 2022-01-29 2023-08-03 上海辉启生物医药科技有限公司 2-氨基嘧啶类化合物或其盐及其制备方法和用途
AU2023250964A1 (en) 2022-04-08 2024-11-07 Eikonizo Therapeutics, Inc. Oxadiazole hdac6 inhibitors and uses thereof
CA3251059A1 (en) 2022-05-02 2023-11-09 The Board Of Trustees Of The Leland Stanford Junior University Compositions, systems and methods for modulating a target gene
CN121358732A (zh) * 2023-03-07 2026-01-16 睿跃生物科技有限公司 治疗癌症的化合物和方法
CN116768860A (zh) * 2023-06-05 2023-09-19 西安交通大学医学院第一附属医院 一类靶向降解cd26的化合物、其制备方法与应用
CN119950745B (zh) * 2025-01-14 2025-10-17 浙江大学 一种药物组合物及其在制备抗肿瘤药物中的应用

Citations (3)

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WO2017185023A1 (en) * 2016-04-22 2017-10-26 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
WO2018013867A1 (en) * 2016-07-13 2018-01-18 Marineau Jason J Inhibitors of cyclin dependnt kinase 7 (cdk7)
WO2018098361A1 (en) * 2016-11-22 2018-05-31 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 12 (cdk12) and uses thereof

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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
WO2015058126A1 (en) * 2013-10-18 2015-04-23 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
WO2015058163A2 (en) * 2013-10-18 2015-04-23 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
MX358346B (es) * 2014-04-04 2018-08-15 Syros Pharmaceuticals Inc Inhibidores de la quinasa dependiente de ciclina 7 (cdk7).
US9694084B2 (en) * 2014-12-23 2017-07-04 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
BR112018008918A8 (pt) 2015-11-02 2019-02-26 Univ Yale compostos de quimera proteólise dirigida e métodos para preparação e uso dos mesmos
WO2017185031A1 (en) * 2016-04-22 2017-10-26 Dana-Farber Cancer Institute, Inc. Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use
AU2019309909A1 (en) 2018-07-23 2021-02-04 Dana-Farber Cancer Institute, Inc. Degradation of cyclin-dependent kinase 4/6 (CDK4/6) by conjugation of CDK4/6 inhibitors with E3 ligase ligand and methods of use

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WO2017185023A1 (en) * 2016-04-22 2017-10-26 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
WO2018013867A1 (en) * 2016-07-13 2018-01-18 Marineau Jason J Inhibitors of cyclin dependnt kinase 7 (cdk7)
WO2018098361A1 (en) * 2016-11-22 2018-05-31 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 12 (cdk12) and uses thereof

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NATURE CHEMICAL BIOLOGY, vol. 14, JPN6024015062, 2017, pages 163 - 170, ISSN: 0005634361 *

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Publication number Publication date
AU2020263390A1 (en) 2021-10-07
CN113993519A (zh) 2022-01-28
US20220227734A1 (en) 2022-07-21
US12662464B2 (en) 2026-06-23
CA3132387A1 (en) 2020-10-29
AU2020263390B2 (en) 2026-01-08
CN113993519B (zh) 2025-11-11
EP3958861A1 (en) 2022-03-02
WO2020219650A1 (en) 2020-10-29
EP3958861A4 (en) 2023-05-03

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