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

Info

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
Authority
CA
Canada
Prior art keywords
optionally substituted
certain embodiments
ring
alkyl
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
CA3041563A
Other languages
English (en)
French (fr)
Other versions
CA3041563A1 (en
Inventor
Nathanael S. Gray
Tinghu Zhang
Baishan JIANG
Nicholas Paul Kwiatkowski
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 CA3041563A1 publication Critical patent/CA3041563A1/en
Application granted granted Critical
Publication of CA3041563C publication Critical patent/CA3041563C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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

Landscapes

  • 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

Family

ID=60703092

Family Applications (1)

Application Number Title Priority Date Filing Date
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 (OSRAM)
EP (1) EP3544971B1 (OSRAM)
JP (1) JP7258748B2 (OSRAM)
AU (1) AU2017363307B2 (OSRAM)
CA (1) CA3041563C (OSRAM)
WO (1) WO2018098361A1 (OSRAM)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2010343102B2 (en) 2009-12-29 2016-03-24 Dana-Farber Cancer Institute, Inc. Type II Raf kinase inhibitors
US10870651B2 (en) 2014-12-23 2020-12-22 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
AU2016243529B2 (en) 2015-03-27 2021-03-25 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
US11306070B2 (en) 2016-11-22 2022-04-19 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 12 (CDK12) and uses thereof
AU2019295632B2 (en) 2018-06-25 2025-03-06 Dana-Farber Cancer Institute, Inc. Taire family kinase inhibitors and uses thereof
AU2019291935A1 (en) * 2018-06-29 2021-02-04 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
CA3132387A1 (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
WO2023023534A2 (en) 2021-08-18 2023-02-23 Chemocentryx, Inc. Aryl sulfonyl compounds as ccr6 inhibitors
CR20240136A (es) 2021-08-18 2024-05-07 Chemocentryx Inc Arilsulfonil(hidroxi)piperidinas como inhibidores de ccr6
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
AU2024204522B1 (en) 2023-03-09 2024-08-22 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
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
EE05345B1 (et) 1999-02-10 2010-10-15 Astrazeneca Ab Kinasoliini derivaadid angiogeneesi inhibiitoritena
CA2376957A1 (en) * 1999-06-30 2001-01-04 Merck & Co., Inc. Src kinase inhibitor 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
AP2007004061A0 (en) 2005-01-10 2007-08-31 Galloway & Company Pyrrolopyrazoles, potent kinase inhibitors
US7501430B2 (en) * 2006-04-17 2009-03-10 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
KR101408517B1 (ko) 2008-03-21 2014-06-17 노파르티스 아게 신규한 헤테로시클릭 화합물 및 그의 용도
AU2009322158A1 (en) 2008-12-05 2010-06-10 Arqule, Inc. RAF inhibitors and their uses
AU2010214440A1 (en) 2009-02-12 2011-09-01 Astellas Pharma Inc. Hetero ring derivative
WO2010144416A1 (en) 2009-06-08 2010-12-16 Gaeta Federico C A SUBSTITUTED PYRAZOLO [1,5-a] PYRIDINE COMPOUNDS HAVING MULTI-TARGET ACTIVITY
WO2012066061A1 (en) 2010-11-19 2012-05-24 F. Hoffmann-La Roche Ag Pyrazolopyridines and pyrazolopyridines and their use as tyk2 inhibitors
EP2822935B1 (en) 2011-11-17 2019-05-15 Dana-Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
US10112927B2 (en) 2012-10-18 2018-10-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
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
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
EP3057956B1 (en) 2013-10-18 2021-05-05 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)
AU2014337067B2 (en) * 2013-10-18 2019-01-24 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of proliferative diseases
ES2676734T3 (es) 2013-10-18 2018-07-24 Syros Pharmaceuticals, Inc. Compuestos heteroatómicos útiles para el tratamiento de enfermedades proliferativas
CA2944669A1 (en) 2014-04-04 2015-10-08 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
WO2016058544A1 (en) * 2014-10-16 2016-04-21 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
AU2016243529B2 (en) 2015-03-27 2021-03-25 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
US10702527B2 (en) * 2015-06-12 2020-07-07 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
JP7028766B2 (ja) 2015-09-09 2022-03-02 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の阻害剤
US11306070B2 (en) 2016-11-22 2022-04-19 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 12 (CDK12) and uses thereof
EP3545314A4 (en) 2016-11-28 2020-10-07 Dana-Farber Cancer Institute, Inc. REAGENTS AND METHODS OF ANALYSIS OF PROTEINS AND METABOLITES TARGETED BY COVALENT PROBES
AU2019295632B2 (en) 2018-06-25 2025-03-06 Dana-Farber Cancer Institute, Inc. Taire family kinase inhibitors and uses thereof
WO2020123925A1 (en) * 2018-12-14 2020-06-18 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
EP3544971B1 (en) 2022-07-06
US20220213067A1 (en) 2022-07-07
EP3544971A1 (en) 2019-10-02
US20210317105A9 (en) 2021-10-14
JP7258748B2 (ja) 2023-04-17
US20200361906A1 (en) 2020-11-19
AU2017363307B2 (en) 2021-07-29
US11306070B2 (en) 2022-04-19
CA3041563A1 (en) 2018-05-31
US20230227433A9 (en) 2023-07-20
JP2019535749A (ja) 2019-12-12
WO2018098361A1 (en) 2018-05-31
AU2017363307A1 (en) 2019-05-02
US11932625B2 (en) 2024-03-19

Similar Documents

Publication Publication Date Title
CA3041563C (en) Pyrimidin-2-amine derivatives and pharmaceutical compositions thereof useful as inhibitors of cyclin-dependent kinase 12 (cdk12)
AU2016319125B2 (en) Inhibitors of cyclin-dependent kinases
AU2016283105C1 (en) 4,6-pyrimidinylene derivatives and uses thereof
AU2017363313B2 (en) Inhibitors of interleukin-1 receptor-associated kinases and uses thereof
CA2978518C (en) Inhibitors of cyclin-dependent kinases
AU2019413694B2 (en) Inhibitors of cyclin-dependent kinase 7 and uses thereof
WO2016210291A1 (en) Fused bicyclic pyrimidine derivatives and uses thereof
WO2020097398A1 (en) Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof
CA3132387A1 (en) Degraders of cyclin-dependent kinase 12 (cdk12) and uses thereof
WO2020097400A1 (en) Imidazopyridine derivatives and aza-imidazopyridine derivatives as janus kinase 2 inhibitors and uses thereof
WO2020097396A1 (en) Benzimidazole derivatives and aza-benzimidazole derivatives as janus kinase 2 inhibitors and uses thereof
AU2020357983B2 (en) Tricyclic kinase inhibitors and uses thereof
CA3157331A1 (en) A pyrazolopyrimidine derivative as a hck inhibitor for use in therapy, in particular myd88 mutated diseases
CA3106548A1 (en) Histone demethylase 5 inhibitors and uses thereof
CA2988330C (en) 4,6-pyrimidinylene derivatives and uses thereof

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20220429

EEER Examination request

Effective date: 20220429

EEER Examination request

Effective date: 20220429

EEER Examination request

Effective date: 20220429

EEER Examination request

Effective date: 20220429

EEER Examination request

Effective date: 20220429

EEER Examination request

Effective date: 20220429

EEER Examination request

Effective date: 20220429

EEER Examination request

Effective date: 20220429

EEER Examination request

Effective date: 20220429