AU2020263390B2 - Degraders of cyclin-dependent kinase 12 (CDK12) and uses thereof - Google Patents

Degraders of cyclin-dependent kinase 12 (CDK12) and uses thereof

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Publication number
AU2020263390B2
AU2020263390B2 AU2020263390A AU2020263390A AU2020263390B2 AU 2020263390 B2 AU2020263390 B2 AU 2020263390B2 AU 2020263390 A AU2020263390 A AU 2020263390A AU 2020263390 A AU2020263390 A AU 2020263390A AU 2020263390 B2 AU2020263390 B2 AU 2020263390B2
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certain embodiments
optionally substituted
alkyl
formula
instance
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AU2020263390A1 (en
Inventor
Jianwei Che
Yang Gao
Nathanael S. Gray
Baishan JIANG
Nicholas Paul Kwiatkowski
Tinghu Zhang
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Dana Farber Cancer Institute Inc
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Dana Farber Cancer Institute Inc
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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

Landscapes

  • 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)
AU2020263390A 2019-04-23 2020-04-23 Degraders of cyclin-dependent kinase 12 (CDK12) and uses thereof Active AU2020263390B2 (en)

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

Publications (2)

Publication Number Publication Date
AU2020263390A1 AU2020263390A1 (en) 2021-10-07
AU2020263390B2 true AU2020263390B2 (en) 2026-01-08

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
AU2020263390A Active AU2020263390B2 (en) 2019-04-23 2020-04-23 Degraders of cyclin-dependent kinase 12 (CDK12) and uses thereof

Country Status (7)

Country Link
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

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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
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
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
SG11201900328WA (en) * 2016-07-13 2019-02-27 Jason Marineau Inhibitors of cyclin-dependent kinase 7 (cdk7)
JP7258748B2 (ja) 2016-11-22 2023-04-17 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 サイクリン依存性キナーゼ１２（ｃｄｋ１２）の阻害剤およびその使用
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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Also Published As

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
CN113993519B (zh) 2025-11-11
EP3958861A1 (en) 2022-03-02
WO2020219650A1 (en) 2020-10-29
JP2022529700A (ja) 2022-06-23
EP3958861A4 (en) 2023-05-03

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