CA3217661A1 - Small molecule cyclin dependent kinase 4/6 (cdk4/6) and ikzf2 (helios) degraders and methods of use thereof - Google Patents

Small molecule cyclin dependent kinase 4/6 (cdk4/6) and ikzf2 (helios) degraders and methods of use thereof Download PDF

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Publication number
CA3217661A1
CA3217661A1 CA3217661A CA3217661A CA3217661A1 CA 3217661 A1 CA3217661 A1 CA 3217661A1 CA 3217661 A CA3217661 A CA 3217661A CA 3217661 A CA3217661 A CA 3217661A CA 3217661 A1 CA3217661 A1 CA 3217661A1
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Canada
Prior art keywords
cancer
bifunctional compound
cell
cdk4
linker
Prior art date
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Pending
Application number
CA3217661A
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English (en)
French (fr)
Inventor
Alyssa VERANO
Eric Wang
Inchul YOU
Nathanael Gray
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
Individual
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 Individual filed Critical Individual
Publication of CA3217661A1 publication Critical patent/CA3217661A1/en
Pending legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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
    • A61K47/545Heterocyclic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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
    • A61K47/55Medicinal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
CA3217661A 2021-07-16 2022-07-15 Small molecule cyclin dependent kinase 4/6 (cdk4/6) and ikzf2 (helios) degraders and methods of use thereof Pending CA3217661A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202163222646P 2021-07-16 2021-07-16
US63/222,646 2021-07-16
PCT/US2022/073782 WO2023288305A1 (en) 2021-07-16 2022-07-15 Small molecule cyclin dependent kinase 4/6 (cdk4/6) and ikzf2 (helios) degraders and methods of use thereof

Publications (1)

Publication Number Publication Date
CA3217661A1 true CA3217661A1 (en) 2023-01-19

Family

ID=84919760

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3217661A Pending CA3217661A1 (en) 2021-07-16 2022-07-15 Small molecule cyclin dependent kinase 4/6 (cdk4/6) and ikzf2 (helios) degraders and methods of use thereof

Country Status (7)

Country Link
US (1) US20240376096A1 (https=)
EP (1) EP4370126A4 (https=)
JP (1) JP2024525740A (https=)
CN (1) CN117396208A (https=)
AU (1) AU2022311961A1 (https=)
CA (1) CA3217661A1 (https=)
WO (1) WO2023288305A1 (https=)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20240020735A (ko) 2021-05-07 2024-02-15 카이메라 쎄라퓨틱스 인코포레이티드 Cdk2 분해제 및 그 용도
US12122764B2 (en) 2021-12-22 2024-10-22 Gilead Sciences, Inc. IKAROS zinc finger family degraders and uses thereof
WO2023178181A1 (en) 2022-03-17 2023-09-21 Gilead Sciences, Inc. Ikaros zinc finger family degraders and uses thereof
CN118420612A (zh) * 2023-02-01 2024-08-02 沈阳药科大学 一种基于cdk4/6抑制剂的靶向蛋白降解化合物及制备方法和用途
WO2025245178A1 (en) * 2024-05-21 2025-11-27 Innovo Therapeutics, Inc. Pak4, cstf2, or cstf2t protein degraders, pharmaceutical compositions, and therapeutic applications

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA04005939A (es) 2002-01-22 2005-01-25 Warner Lambert Co 2-(piridin-2-ilamino)-pirido[2,3-d]pirimidin-7-onas.
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
TWI398252B (zh) 2006-05-26 2013-06-11 諾華公司 吡咯并嘧啶化合物及其用途
US20090030005A1 (en) * 2007-07-19 2009-01-29 Amgen Inc. Combinations for the treatment of cancer
ES2522346T3 (es) 2008-08-22 2014-11-14 Novartis Ag Compuestos de pirrolopirimidina como inhibidores de CDK
TW201014830A (en) 2008-09-30 2010-04-16 Theravance Inc Crystalline form of an alkoxyimidazol-1-ylmethyl biphenyl carboxylic acid
US20120115878A1 (en) 2010-11-10 2012-05-10 John Vincent Calienni Salt(s) of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7h-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and processes of making thereof
WO2013039854A1 (en) 2011-09-15 2013-03-21 Merck Sharp & Dohme Corp. Compositions and methods for treating cancer
MX386473B (es) 2013-02-21 2025-03-18 Pfizer Formas solidas de un inhibidor de cdk4/6 selectivo
CN107530292B (zh) 2015-04-16 2022-11-01 诺华股份有限公司 瑞博西尼片剂
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
AU2018351050B2 (en) * 2017-10-18 2025-09-18 Novartis Ag Compositions and methods for selective protein degradation
WO2019196812A1 (zh) * 2018-04-09 2019-10-17 上海科技大学 蛋白降解靶向化合物、其抗肿瘤应用、其中间体及中间体应用
CA3123519A1 (en) * 2019-02-15 2020-08-20 Novartis Ag Substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof

Also Published As

Publication number Publication date
AU2022311961A1 (en) 2023-11-09
EP4370126A1 (en) 2024-05-22
US20240376096A1 (en) 2024-11-14
EP4370126A4 (en) 2025-05-28
WO2023288305A1 (en) 2023-01-19
JP2024525740A (ja) 2024-07-12
CN117396208A (zh) 2024-01-12

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