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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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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    • 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
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (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)

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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
US9180127B2 (en) 2009-12-29 2015-11-10 Dana-Farber Cancer Institute, Inc. Type II Raf kinase inhibitors
AU2015371251B2 (en) 2014-12-23 2020-06-11 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
HK1246645A1 (zh) 2015-03-27 2018-09-14 达纳-法伯癌症研究所股份有限公司 细胞周期蛋白依赖性激酶的抑制剂
WO2018098361A1 (en) 2016-11-22 2018-05-31 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 12 (cdk12) and uses thereof
US12187701B2 (en) 2018-06-25 2025-01-07 Dana-Farber Cancer Institute, Inc. Taire family kinase inhibitors and uses thereof
SG11202013175SA (en) * 2018-06-29 2021-01-28 Kinnate Biopharma Inc Inhibitors of cyclin-dependent kinases
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
JP7660063B2 (ja) 2018-12-28 2025-04-10 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のインヒビターおよびそれらの使用
AU2020263390B2 (en) * 2019-04-23 2026-01-08 Dana-Farber Cancer Institute, Inc. Degraders of cyclin-dependent kinase 12 (CDK12) and uses thereof
US20220288067A1 (en) * 2019-04-24 2022-09-15 The Trustees Of The University Of Pennsylvania Treatment of cancer with cdk inhibitors
CN114901284A (zh) * 2019-10-29 2022-08-12 希洛斯医药品股份有限公司 用细胞周期蛋白依赖性激酶7(cdk7)抑制剂治疗生物标志物鉴定的患者的癌症的方法
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
US12018016B2 (en) 2021-08-18 2024-06-25 Amgen Inc. Aryl sulfonyl (hydroxy) piperidines as CCR6 inhibitors
WO2023023534A2 (en) 2021-08-18 2023-02-23 Chemocentryx, Inc. Aryl sulfonyl compounds as ccr6 inhibitors
WO2023091726A1 (en) * 2021-11-18 2023-05-25 Syros Pharmaceuticals, Inc. Inhibitors of cyclin‑dependent kinase 12 (cdk12)
TW202329937A (zh) * 2021-12-03 2023-08-01 美商英塞特公司 雙環胺ck12抑制劑
WO2023107705A1 (en) 2021-12-10 2023-06-15 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
KR102821060B1 (ko) 2023-03-09 2025-06-16 미네암리타 테라퓨틱스, 엘엘씨 위암의 치료를 위한 약물 조합

Family Cites Families (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6143764A (en) 1995-11-07 2000-11-07 Kirin Beer Kabushiki Kaisha Quinoline and quinazoline derivatives inhibiting platelet-derived growth factor receptor autophosphorylation and pharmaceutical compositions containing the same
SK288365B6 (sk) 1999-02-10 2016-07-01 Astrazeneca Ab Medziprodukty pre chinazolínové deriváty ako inhibítory angiogenézy
JP2003503351A (ja) 1999-06-30 2003-01-28 メルク エンド カムパニー インコーポレーテッド Srcキナーゼ阻害化合物
WO2006038001A1 (en) * 2004-10-06 2006-04-13 Celltech R & D Limited Aminopyrimidine derivatives as jnk inhibitors
JP2008517064A (ja) * 2004-10-19 2008-05-22 アークル インコーポレイテッド P38mapキナーゼのイミダゾオキサゾールおよびイミダゾチアゾール阻害剤の合成
AU2005323797B2 (en) 2005-01-10 2009-07-09 Pfizer Inc. Pyrrolopyrazoles, potent kinase inhibitors
EP2013218A2 (en) * 2006-04-17 2009-01-14 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
AU2009227013B2 (en) 2008-03-21 2013-01-10 Novartis Ag Novel heterocyclic compounds and uses therof
CN102317293A (zh) 2008-12-05 2012-01-11 艾科尔公司 Raf抑制剂及其用途
US20120165309A1 (en) 2009-02-12 2012-06-28 Astellas Pharma Inc. Hetero ring derivative
TW201102387A (en) 2009-06-08 2011-01-16 Medicinova Inc Substituted pyrazolo[1,5-a]pyridine compounds having multi-target activity
MX2013005445A (es) 2010-11-19 2013-07-29 Hoffmann La Roche Pirazolopiridinas y el uso de pirazolopiridinas como inhibidores de tirosina cinasa 2 (tyk2).
CA2856291C (en) 2011-11-17 2020-08-11 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
EP3057955B1 (en) 2013-10-18 2018-04-11 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
AU2014337067B2 (en) * 2013-10-18 2019-01-24 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of proliferative diseases
US10047070B2 (en) 2013-10-18 2018-08-14 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)
CN106458990B (zh) 2014-04-04 2019-06-07 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)
HK1246645A1 (zh) * 2015-03-27 2018-09-14 达纳-法伯癌症研究所股份有限公司 细胞周期蛋白依赖性激酶的抑制剂
US10702527B2 (en) 2015-06-12 2020-07-07 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
EP3347018B1 (en) 2015-09-09 2021-09-01 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
WO2018098361A1 (en) 2016-11-22 2018-05-31 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 12 (cdk12) and uses thereof
US10969394B2 (en) 2016-11-28 2021-04-06 Dana-Farber Cancer Institute, Inc. Reagents and methods for analysis of proteins and metabolites targeted by covalent probes
US12187701B2 (en) 2018-06-25 2025-01-07 Dana-Farber Cancer Institute, Inc. Taire family kinase inhibitors and uses thereof
AU2019395255B2 (en) * 2018-12-14 2025-02-27 Dana-Farber Cancer Institute, Inc. Pyrazolopyridine inhibitors of c-Jun-N-terminal kinases and uses thereof
JP7660063B2 (ja) 2018-12-28 2025-04-10 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のインヒビターおよびそれらの使用
US20230114207A1 (en) * 2019-12-24 2023-04-13 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
JP2019535749A (ja) 2019-12-12
US11932625B2 (en) 2024-03-19
CA3041563A1 (en) 2018-05-31
AU2017363307A1 (en) 2019-05-02
US20210317105A9 (en) 2021-10-14
AU2017363307B2 (en) 2021-07-29
US20230227433A9 (en) 2023-07-20
WO2018098361A1 (en) 2018-05-31
JP7258748B2 (ja) 2023-04-17
EP3544971A1 (en) 2019-10-02
EP3544971B1 (en) 2022-07-06
US20200361906A1 (en) 2020-11-19
US20220213067A1 (en) 2022-07-07
US11306070B2 (en) 2022-04-19

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