CA3041563C - Pyrimidin-2-amine derivatives and pharmaceutical compositions thereof useful as inhibitors of cyclin-dependent kinase 12 (cdk12) - Google Patents

Pyrimidin-2-amine derivatives and pharmaceutical compositions thereof useful as inhibitors of cyclin-dependent kinase 12 (cdk12) Download PDF

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Publication number
CA3041563C
CA3041563C CA3041563A CA3041563A CA3041563C CA 3041563 C CA3041563 C CA 3041563C CA 3041563 A CA3041563 A CA 3041563A CA 3041563 A CA3041563 A CA 3041563A CA 3041563 C CA3041563 C CA 3041563C
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French (fr)
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CA3041563A1 (en
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Nathanael S. Gray
Tinghu Zhang
Baishan JIANG
Nicholas Paul Kwiatkowski
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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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA3041563A 2016-11-22 2017-11-22 Pyrimidin-2-amine derivatives and pharmaceutical compositions thereof useful as inhibitors of cyclin-dependent kinase 12 (cdk12) Active CA3041563C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662425519P 2016-11-22 2016-11-22
US62/425,519 2016-11-22
PCT/US2017/063132 WO2018098361A1 (en) 2016-11-22 2017-11-22 Inhibitors of cyclin-dependent kinase 12 (cdk12) and uses thereof

Publications (2)

Publication Number Publication Date
CA3041563A1 CA3041563A1 (en) 2018-05-31
CA3041563C true CA3041563C (en) 2023-10-31

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CA3041563A Active CA3041563C (en) 2016-11-22 2017-11-22 Pyrimidin-2-amine derivatives and pharmaceutical compositions thereof useful as inhibitors of cyclin-dependent kinase 12 (cdk12)

Country Status (6)

Country Link
US (2) US11306070B2 (https=)
EP (1) EP3544971B1 (https=)
JP (1) JP7258748B2 (https=)
AU (1) AU2017363307B2 (https=)
CA (1) CA3041563C (https=)
WO (1) WO2018098361A1 (https=)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011090738A2 (en) 2009-12-29 2011-07-28 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
JP6854762B2 (ja) 2014-12-23 2021-04-07 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７（ｃｄｋ７）の阻害剤
USRE50776E1 (en) 2015-03-27 2026-02-03 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
AU2017363307B2 (en) 2016-11-22 2021-07-29 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 12 (CDK12) and uses thereof
EP3810132A4 (en) 2018-06-25 2022-06-22 Dana-Farber Cancer Institute, Inc. TAIRE FAMILY KINASE INHIBITORS AND RELATED USES
EP3813819A4 (en) * 2018-06-29 2022-08-17 Kinnate Biopharma Inc. CYCLIN-DEPENDENT KINASE INHIBITORS
CN109111376B (zh) * 2018-09-18 2021-09-14 四川医立特生物医药有限公司 一种2,5-双脱氧链霉胺衍生物及其应用
US12281126B2 (en) 2018-12-28 2025-04-22 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
WO2020219650A1 (en) * 2019-04-23 2020-10-29 Dana-Farber Cancer Institute, Inc. Degraders of cyclin-dependent kinase 12 (cdk12) and uses thereof
WO2020219926A1 (en) * 2019-04-24 2020-10-29 The Trustees Of The University Of Pennsylvania Treatment of cancer with cdk inhibitors
WO2021087138A1 (en) * 2019-10-29 2021-05-06 Syros Pharmaceuticals, Inc. Methods of treating cancer in biomarker-identified patients with inhibitors of cyclin-dependent kinase 7 (cdk7)
CN111269217B (zh) * 2020-04-07 2021-01-08 苏州信诺维医药科技有限公司 一种嘧啶胺类化合物、其制备方法及应用
CN111393415B (zh) * 2020-04-30 2020-11-20 苏州信诺维医药科技有限公司 一种杂芳腈类化合物及其应用
CN114133394B (zh) * 2020-08-12 2023-12-08 赛诺哈勃药业（成都）有限公司 一种选择性针对细胞周期依赖性激酶12活性的化合物、制备方法及医药用途
US20230303512A1 (en) * 2020-08-26 2023-09-28 Massachusetts Institute Of Technology Modulators of myb-mediated transcription and uses thereof
AU2022328634A1 (en) 2021-08-18 2024-02-22 Chemocentryx, Inc. Aryl sulfonyl compounds as ccr6 inhibitors
WO2023023532A2 (en) 2021-08-18 2023-02-23 Chemocentryx, Inc. Aryl sulfonyl (hydroxy) piperidines as ccr6 inhibitors
WO2023091726A1 (en) * 2021-11-18 2023-05-25 Syros Pharmaceuticals, Inc. Inhibitors of cyclin‑dependent kinase 12 (cdk12)
WO2023102184A1 (en) * 2021-12-03 2023-06-08 Incyte Corporation Bicyclic amine compounds as cdk12 inhibitors
US12084453B2 (en) 2021-12-10 2024-09-10 Incyte Corporation Bicyclic amines as CDK12 inhibitors
CN114452391B (zh) * 2022-01-28 2023-08-25 深圳市泰尔康生物医药科技有限公司 Cdk16作为靶标在制备用于治疗三阴性乳腺癌的药物中的应用
US12357645B2 (en) 2023-03-09 2025-07-15 Minneamrita Therapeutics Llc Drug combination for treatment of gastric cancer

Family Cites Families (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0860433B1 (en) 1995-11-07 2002-07-03 Kirin Beer Kabushiki Kaisha Quinoline derivatives and quinazoline derivatives inhibiting autophosphorylation of growth factor receptor originating in platelet and pharmaceutical compositions containing the same
PT1154774E (pt) 1999-02-10 2005-10-31 Astrazeneca Ab Derivados de quinazolina como inibidores de angiogenese
EP1206260A4 (en) 1999-06-30 2002-10-30 Merck & Co Inc SRC-KINASE INHIBITING COMPOUNDS
WO2006038001A1 (en) * 2004-10-06 2006-04-13 Celltech R & D Limited Aminopyrimidine derivatives as jnk inhibitors
EP2258704A1 (en) * 2004-10-19 2010-12-08 ArQule, Inc. Synthesis of imidazooxazole and imidazothiazole inhibitors of p38 map kinase
AU2005323797B2 (en) 2005-01-10 2009-07-09 Pfizer Inc. Pyrrolopyrazoles, potent kinase inhibitors
WO2007123892A2 (en) * 2006-04-17 2007-11-01 Arqule Inc. Raf inhibitors and their uses
WO2007129195A2 (en) 2006-05-04 2007-11-15 Pfizer Products Inc. 4-pyrimidine-5-amino-pyrazole compounds
US20090054392A1 (en) 2007-08-20 2009-02-26 Wyeth Naphthylpyrimidine, naphthylpyrazine and naphthylpyridazine analogs and their use as agonists of the wnt-beta-catenin cellular messaging system
WO2009115572A2 (en) 2008-03-21 2009-09-24 Novartis Ag Novel heterocyclic compounds and uses therof
EP2361254A1 (en) 2008-12-05 2011-08-31 ArQule, Inc. Raf inhibitors and their uses
JPWO2010092962A1 (ja) 2009-02-12 2012-08-16 アステラス製薬株式会社 へテロ環誘導体
WO2010144416A1 (en) 2009-06-08 2010-12-16 Gaeta Federico C A SUBSTITUTED PYRAZOLO [1,5-a] PYRIDINE COMPOUNDS HAVING MULTI-TARGET ACTIVITY
BR112013011520A2 (pt) 2010-11-19 2019-09-24 Hoffmann La Roche pirazolo piridinas e pirazolo piridinas e seu uso como inibidores de tyk2
US9382239B2 (en) 2011-11-17 2016-07-05 Dana-Farber Cancer Institute, Inc. Inhibitors of c-Jun-N-terminal kinase (JNK)
EP2909194A1 (en) 2012-10-18 2015-08-26 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
TWI621618B (zh) 2013-03-13 2018-04-21 比利時商健生藥品公司 經取代２－氮雜雙環類及其作為食慾素受體調控劑之用途
TW201444821A (zh) 2013-03-13 2014-12-01 Janssen Pharmaceutica Nv 經取代之哌啶化合物及其作為食慾素受體調節劑之用途
EP3057956B1 (en) 2013-10-18 2021-05-05 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)
CA2927924A1 (en) * 2013-10-18 2015-04-23 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of proliferative diseases
WO2015058126A1 (en) 2013-10-18 2015-04-23 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative 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
WO2016058544A1 (en) 2014-10-16 2016-04-21 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
USRE50776E1 (en) * 2015-03-27 2026-02-03 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
WO2016201370A1 (en) * 2015-06-12 2016-12-15 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
AU2016319125B2 (en) 2015-09-09 2021-04-08 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
AU2017363307B2 (en) 2016-11-22 2021-07-29 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 12 (CDK12) and uses thereof
CA3043222A1 (en) 2016-11-28 2018-05-31 Dana-Farber Cancer Institute, Inc. Reagents and methods for analysis of proteins and metabolites targeted by covalent probes
EP3810132A4 (en) 2018-06-25 2022-06-22 Dana-Farber Cancer Institute, Inc. TAIRE FAMILY KINASE INHIBITORS AND RELATED USES
US20220073512A1 (en) 2018-12-14 2022-03-10 Dana-Farber Cancer Institute, Inc. Pyrazolopyridine inhibitors of c-jun-n-terminal kinases and uses thereof
US12281126B2 (en) 2018-12-28 2025-04-22 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
WO2021133601A1 (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

Also Published As

Publication number Publication date
EP3544971B1 (en) 2022-07-06
US11306070B2 (en) 2022-04-19
US20220213067A1 (en) 2022-07-07
US20200361906A1 (en) 2020-11-19
WO2018098361A1 (en) 2018-05-31
AU2017363307B2 (en) 2021-07-29
US11932625B2 (en) 2024-03-19
CA3041563A1 (en) 2018-05-31
JP2019535749A (ja) 2019-12-12
JP7258748B2 (ja) 2023-04-17
US20210317105A9 (en) 2021-10-14
US20230227433A9 (en) 2023-07-20
AU2017363307A1 (en) 2019-05-02
EP3544971A1 (en) 2019-10-02

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