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

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

Info

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
Authority
AU
Australia
Prior art keywords
certain embodiments
optionally substituted
alkyl
formula
instance
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.)
Active
Application number
AU2020263390A
Other languages
English (en)
Other versions
AU2020263390A1 (en
Inventor
Jianwei Che
Yang Gao
Nathanael S. Gray
Baishan JIANG
Nicholas Paul Kwiatkowski
Tinghu Zhang
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.)
Dana Farber Cancer Institute Inc
Original Assignee
Dana Farber Cancer Institute Inc
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 Dana Farber Cancer Institute Inc filed Critical Dana Farber Cancer Institute Inc
Publication of AU2020263390A1 publication Critical patent/AU2020263390A1/en
Application granted granted Critical
Publication of AU2020263390B2 publication Critical patent/AU2020263390B2/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (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

ID=72941778

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) US20220227734A1 (https=)
EP (1) EP3958861A4 (https=)
JP (1) JP2022529700A (https=)
CN (1) CN113993519B (https=)
AU (1) AU2020263390B2 (https=)
CA (1) CA3132387A1 (https=)
WO (1) WO2020219650A1 (https=)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018165520A1 (en) 2017-03-10 2018-09-13 Vps-3, Inc. Metalloenzyme inhibitor compounds
CA3141826A1 (en) 2019-05-31 2020-12-03 Ikena Oncology, Inc. Tead inhibitors and uses thereof
CA3142351A1 (en) 2019-05-31 2020-12-03 Ikena Oncology, Inc. Tead inhibitors and uses thereof
CA3142713A1 (en) 2019-06-03 2020-12-10 Regents Of The University Of Minnesota Compounds that degrade kinases and uses thereof
AU2020321955A1 (en) 2019-07-30 2022-03-17 Eikonizo Therapapeutics, Inc. HDAC6 inhibitors and uses thereof
WO2022120355A1 (en) * 2020-12-02 2022-06-09 Ikena Oncology, Inc. Tead degraders and uses thereof
KR20240020735A (ko) 2021-05-07 2024-02-15 카이메라 쎄라퓨틱스 인코포레이티드 Cdk2 분해제 및 그 용도
IL312013A (en) * 2021-10-14 2024-06-01 Cullgen Shanghai Inc Modified proteins and protein degraders
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
TW202345813A (zh) 2022-04-08 2023-12-01 美商艾科尼佐療法股份有限公司 㗁二唑ｈｄａｃ６抑制劑及其用途
WO2024183798A1 (en) * 2023-03-07 2024-09-12 Cullgen Inc. Compounds and methods of treating cancers
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

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102668696B1 (ko) * 2012-01-12 2024-05-29 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
CA2927924A1 (en) * 2013-10-18 2015-04-23 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of proliferative diseases
CN110229142A (zh) * 2014-04-04 2019-09-13 希洛斯医药品股份有限公司 细胞周期蛋白依赖性激酶7(cdk7)的抑制剂
US9694084B2 (en) * 2014-12-23 2017-07-04 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
EP3445765A4 (en) * 2016-04-22 2019-09-18 Dana Farber Cancer Institute, Inc. DECREASE OF CYCLINE-DEPENDENT KINASE 4/6 (CDK4 / 6) BY CONJUGATION OF CDK4 / 6 INHIBITORS WITH E3-LIGASE LIGANDS AND METHODS OF USE
CA3018429A1 (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
AU2017295863B2 (en) * 2016-07-13 2022-07-07 Medic Life Sciences, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
AU2017363307B2 (en) * 2016-11-22 2021-07-29 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 12 (CDK12) and uses thereof
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

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
LI TAN; NATHANAEL S. GRAY: "When Kinases Meet PROTACs", CHINESE JOURNAL OF CHEMISTRY, ZHONGGUO KEXUEYUAN, CN, vol. 36, no. 10, 28 August 2018 (2018-08-28), CN, pages 971 - 977, XP071929868, ISSN: 1001-604X, DOI: 10.1002/cjoc.201800293 *

Also Published As

Publication number Publication date
CA3132387A1 (en) 2020-10-29
US20220227734A1 (en) 2022-07-21
JP2022529700A (ja) 2022-06-23
CN113993519B (zh) 2025-11-11
EP3958861A1 (en) 2022-03-02
CN113993519A (zh) 2022-01-28
EP3958861A4 (en) 2023-05-03
WO2020219650A1 (en) 2020-10-29
AU2020263390A1 (en) 2021-10-07

Similar Documents

Publication Publication Date Title
AU2020263390B2 (en) Degraders of cyclin-dependent kinase 12 (CDK12) and uses thereof
EP3544970B1 (en) Inhibitors of interleukin-1 receptor-associated kinases and uses thereof
US20230227433A9 (en) Inhibitors of cyclin-dependent kinase 12 (cdk12) and uses thereof
US12415816B2 (en) Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof
AU2020301399B2 (en) HCK degraders and uses thereof
US20220395509A1 (en) A pyrazolopyrimidine derivative as a hck inhibitor for use in therapy, in particular myd88 mutated diseases
EP3814365B1 (en) Dot1l degrader and uses thereof
US20220242872A1 (en) E3 ligase binders and uses thereof
AU2019318046B2 (en) Histone demethylase 5 inhibitors and uses thereof
AU2020362194B2 (en) A pyrazolopyrimidine derivative as a HCK inhibitor for use in therapy, in particular MYD88 mutated diseases