CN107530329B - 用作CDK抑制剂的吡唑并[1,5-a][1,3,5]三嗪和吡唑并[1,5-a]嘧啶衍生物 - Google Patents

用作CDK抑制剂的吡唑并[1,5-a][1,3,5]三嗪和吡唑并[1,5-a]嘧啶衍生物 Download PDF

Info

Publication number
CN107530329B
CN107530329B CN201680014422.1A CN201680014422A CN107530329B CN 107530329 B CN107530329 B CN 107530329B CN 201680014422 A CN201680014422 A CN 201680014422A CN 107530329 B CN107530329 B CN 107530329B
Authority
CN
China
Prior art keywords
compound
amino
mmol
pyrazolo
isopropyl
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.)
Expired - Fee Related
Application number
CN201680014422.1A
Other languages
English (en)
Chinese (zh)
Other versions
CN107530329A (zh
Inventor
苏姗塔·萨玛吉代尔
拉姆鲁·波杜涂拉
须伯汗杜·慕克吉
拉杰夫·高斯瓦米
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.)
Oregini Oncology Co ltd
Original Assignee
Aurigene Discovery Technologies Ltd
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 Aurigene Discovery Technologies Ltd filed Critical Aurigene Discovery Technologies Ltd
Publication of CN107530329A publication Critical patent/CN107530329A/zh
Application granted granted Critical
Publication of CN107530329B publication Critical patent/CN107530329B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-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
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201680014422.1A 2015-03-09 2016-03-08 用作CDK抑制剂的吡唑并[1,5-a][1,3,5]三嗪和吡唑并[1,5-a]嘧啶衍生物 Expired - Fee Related CN107530329B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IN1128/CHE/2015 2015-03-09
IN1128CH2015 2015-03-09
PCT/IB2016/051302 WO2016142855A2 (en) 2015-03-09 2016-03-08 Pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives as cdk inhibitors

Publications (2)

Publication Number Publication Date
CN107530329A CN107530329A (zh) 2018-01-02
CN107530329B true CN107530329B (zh) 2021-10-08

Family

ID=56879301

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201680014422.1A Expired - Fee Related CN107530329B (zh) 2015-03-09 2016-03-08 用作CDK抑制剂的吡唑并[1,5-a][1,3,5]三嗪和吡唑并[1,5-a]嘧啶衍生物

Country Status (7)

Country Link
US (2) US11186576B2 (enExample)
EP (1) EP3268000B1 (enExample)
JP (1) JP6789962B2 (enExample)
CN (1) CN107530329B (enExample)
CA (1) CA2978170C (enExample)
ES (1) ES2899196T3 (enExample)
WO (1) WO2016142855A2 (enExample)

Families Citing this family (39)

* 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
CA2856291C (en) 2011-11-17 2020-08-11 Dana-Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
US10047070B2 (en) 2013-10-18 2018-08-14 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)
US10336760B2 (en) * 2014-04-05 2019-07-02 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
EP3236959B1 (en) 2014-12-23 2025-09-24 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
CA2978170C (en) * 2015-03-09 2024-02-27 Aurigene Discovery Technologies Limited Pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives as cdk inhibitors
AU2016243529B2 (en) 2015-03-27 2021-03-25 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
EP4019515A1 (en) 2015-09-09 2022-06-29 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
JP7216705B2 (ja) 2017-07-28 2023-02-02 ニンバス ラクシュミ, インコーポレイテッド Tyk2阻害剤およびその使用方法
TWI703149B (zh) 2017-11-16 2020-09-01 美商美國禮來大藥廠 用於抑制cdk7之化合物
JP7282743B2 (ja) * 2018-03-29 2023-05-29 武田薬品工業株式会社 複素環化合物
CA3095426A1 (en) * 2018-04-11 2019-10-17 Qurient Co., Ltd. Pharmaceutically active pyrazolo-triazine and/or pyrazolo-pyrimidine derivatives
WO2019197549A1 (en) * 2018-04-11 2019-10-17 Qurient Co., Ltd. Pyrazolo-triazine and/or pyrazolo-pyrimidine derivatives as selective inhibitor of cyclin dependent kinase
JP7590185B2 (ja) 2018-06-25 2024-11-26 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 Taireファミリーキナーゼインヒビターおよびそれらの使用
EA039950B1 (ru) * 2018-07-20 2022-03-31 Эли Лилли Энд Компани Соединения, пригодные для ингибирования cdk7
CN110835345A (zh) * 2018-08-17 2020-02-25 中国科学院上海药物研究所 一类细胞周期依赖性激酶的降解剂、其制备方法、药物组合物及其用途
MY210039A (en) 2018-10-30 2025-08-22 Kronos Bio Inc Compounds, compositions, and methods for modulating cdk9 activity
WO2020186196A1 (en) * 2019-03-13 2020-09-17 The Translational Genomics Research Institute Trisubstituted pyrazolo [1,5-a] pyrimidine compounds as cdk7 inhibitors
CN112125908B (zh) * 2019-06-25 2023-11-03 隆泰申医药科技(南京)有限公司 Cdk激酶抑制剂、其制备方法、药物组合物和应用
EP4061341A4 (en) * 2019-11-22 2024-04-10 The Regents of the University of California CASPASE6 INHIBITORS AND USES THEREOF
TW202146416A (zh) * 2019-12-11 2021-12-16 德商拜耳廠股份有限公司 吡唑并三𠯤
WO2021121390A1 (zh) * 2019-12-20 2021-06-24 苏州信诺维医药科技股份有限公司 杂环化合物及其药物组合物、制备方法、中间体和应用
CN110950871B (zh) * 2019-12-25 2022-05-17 陕西师范大学 2-取代-4-芳氨基吡唑并三嗪衍生物及制备抗肿瘤药物的应用
CN111393447B (zh) * 2020-05-14 2021-01-15 苏州信诺维医药科技有限公司 一种嘧啶并吡唑类化合物、其制备方法及应用
TWI783480B (zh) 2020-05-27 2022-11-11 美商美國禮來大藥廠 用於抑制cdk7之化合物
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
CN114075205A (zh) * 2020-08-12 2022-02-22 隆泰申医药科技(南京)有限公司 Cdk激酶抑制剂、其制备方法、药物组合物和应用
EP4320110A1 (en) * 2021-04-09 2024-02-14 Universität Basel Triazine derivative as covalent inhibitors of pi3k
CN115340524B (zh) * 2021-05-14 2024-05-28 重庆博腾制药科技股份有限公司 一种(s)-去甲烟碱甲基化制备(s)-尼古丁的方法
US20250042903A1 (en) * 2021-06-17 2025-02-06 H. Lee Moffitt Cancer Center And Research Institute, Inc. Triazine inhibitors of cyclin-dependent kinases
CN113801119B (zh) * 2021-08-30 2022-09-30 新乡医学院 一种吡唑并[1,3,5]三嗪类化合物的合成方法
WO2023107705A1 (en) 2021-12-10 2023-06-15 Incyte Corporation Bicyclic amines as cdk12 inhibitors
CN114181217B (zh) * 2022-01-10 2022-12-27 陕西师范大学 吡唑并[1,5-a][1,3,5]三嗪衍生物及其盐和在制备抗癌药物中的应用
WO2023227125A1 (zh) * 2022-05-26 2023-11-30 杭州德睿智药科技有限公司 作为CDKs抑制剂的新型并杂环类新化合物及其应用
CN119790056A (zh) * 2022-09-30 2025-04-08 楚浦创制(武汉)医药科技有限公司 三并环类衍生物、药物组合物以及应用
WO2024125532A1 (zh) * 2022-12-12 2024-06-20 杭州德睿智药科技有限公司 作为CDKs抑制剂的新型并杂环类新化合物及其应用
WO2024175024A1 (zh) * 2023-02-21 2024-08-29 杭州德睿智药科技有限公司 作为CDKs抑制剂的新型并杂环类新化合物及其应用
WO2025040170A1 (zh) * 2023-08-24 2025-02-27 杭州德睿智药科技有限公司 作为CDKs抑制剂的新型并杂环类新化合物及其应用
CN119707984A (zh) * 2023-09-28 2025-03-28 中国科学院上海药物研究所 吡唑并三嗪及吡唑并嘧啶衍生物、其制备方法、药物组合物及其用途

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6194410B1 (en) * 1998-03-11 2001-02-27 Hoffman-La Roche Inc. Pyrazolopyrimidine and pyrazolines and process for preparation thereof
WO2008036277A1 (en) * 2006-09-18 2008-03-27 Polaris Group Pyraz0l0(l,5-a) (1, 3, 5) triazine and pyrazolo (1, 5-a) pyrimidine derivatives useful as protein kinase inhibitors
WO2008151304A1 (en) * 2007-06-05 2008-12-11 Emory University Selective inhibitors for cyclin-dependent kinases
CN104350054A (zh) * 2012-03-01 2015-02-11 利德探索中心有限公司 作为选择性细胞周期蛋白依赖性激酶抑制剂的吡唑并-三嗪衍生物

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GEP20053476B (en) 1999-08-12 2005-03-25 Upjohn Co 3(5)-Amino-Pyrazole Derivatives, Process for Their Preparation and Their Use as Antitumor Agents
EP1678147B1 (en) 2003-09-15 2012-08-08 Lead Discovery Center GmbH Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases
EP2395000A1 (en) 2004-12-30 2011-12-14 Astex Therapeutics Limited Benzimidazole compounds that modulate the activity of CDK, GSK and aurora kinases
JP2008526723A (ja) 2004-12-30 2008-07-24 アステックス、セラピューティックス、リミテッド Cdk、gsk及びオーロラキナーゼの活性を調節するピラゾール誘導体
US20070078136A1 (en) 2005-09-22 2007-04-05 Bristol-Myers Squibb Company Fused heterocyclic compounds useful as kinase modulators
AU2009266806A1 (en) 2008-07-03 2010-01-07 Exelixis Inc. CDK modulators
FR2943058B1 (fr) * 2009-03-11 2011-06-03 Centre Nat Rech Scient Derives de pyrazolo°1,5-a!-1,3,5-triazines, leur preparation et leur application en therapeutique.
WO2012045195A1 (en) 2010-10-09 2012-04-12 Abbott Laboratories Pyrrolopyrimidines as fak and alk inhibiters for treatment of cancers and other diseases
EP2634189A1 (en) 2012-03-01 2013-09-04 Lead Discovery Center GmbH Pyrazolo-triazine derivatives as selective cyclin-dependent kinase inhibitors
EP2909194A1 (en) 2012-10-18 2015-08-26 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
CA2908098A1 (en) * 2013-03-15 2014-09-25 Celgene Avilomics Research, Inc. Mk2 inhibitors and uses thereof
US10336760B2 (en) 2014-04-05 2019-07-02 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
CA2978170C (en) * 2015-03-09 2024-02-27 Aurigene Discovery Technologies Limited Pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives as cdk inhibitors
AU2016243529B2 (en) 2015-03-27 2021-03-25 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
EP3302448B1 (en) * 2015-06-04 2023-10-25 Aurigene Oncology Limited Substituted heterocyclyl derivatives as cdk inhibitors

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6194410B1 (en) * 1998-03-11 2001-02-27 Hoffman-La Roche Inc. Pyrazolopyrimidine and pyrazolines and process for preparation thereof
WO2008036277A1 (en) * 2006-09-18 2008-03-27 Polaris Group Pyraz0l0(l,5-a) (1, 3, 5) triazine and pyrazolo (1, 5-a) pyrimidine derivatives useful as protein kinase inhibitors
WO2008151304A1 (en) * 2007-06-05 2008-12-11 Emory University Selective inhibitors for cyclin-dependent kinases
CN104350054A (zh) * 2012-03-01 2015-02-11 利德探索中心有限公司 作为选择性细胞周期蛋白依赖性激酶抑制剂的吡唑并-三嗪衍生物

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Synthesis and Structure-Activity Relationship of a New Series of Potent Angiotensin II Receptor Antagonists: Pyrazolo(1,5-a)pyrimidine Derivatives";SHIOTA, T. et.al.;《CHEMICAL & PHARMACEUTICAL BULLETIN》;19991231;第47卷(第7期);928–938 *

Also Published As

Publication number Publication date
JP6789962B2 (ja) 2020-11-25
ES2899196T3 (es) 2022-03-10
WO2016142855A3 (en) 2016-11-03
CA2978170C (en) 2024-02-27
CA2978170A1 (en) 2016-09-15
CN107530329A (zh) 2018-01-02
EP3268000A2 (en) 2018-01-17
US20180057497A1 (en) 2018-03-01
WO2016142855A2 (en) 2016-09-15
US20220281871A1 (en) 2022-09-08
US11186576B2 (en) 2021-11-30
US20180258092A9 (en) 2018-09-13
JP2018507877A (ja) 2018-03-22
EP3268000A4 (en) 2018-08-22
EP3268000B1 (en) 2021-08-04

Similar Documents

Publication Publication Date Title
CN107530329B (zh) 用作CDK抑制剂的吡唑并[1,5-a][1,3,5]三嗪和吡唑并[1,5-a]嘧啶衍生物
CN108024970B (zh) 用作cdk抑制剂的经过取代的杂环衍生物
CA2927917C (en) Heteroaromatic compounds useful for the treatment of proliferative diseases
AU2021203051A1 (en) Inhibitors of cyclin-dependent kinase 7 (CDK7)
EP3489232A2 (en) Inhibitors of cyclin-dependent kinase 7 (cdk7)
CN111699176B (zh) 作为parp14抑制剂的喹唑啉酮
KR101828187B1 (ko) 신규 축합 피리미딘 화합물 또는 그 염
JP2020125321A (ja) リジン特異的なデメチラーゼ−1の阻害剤
AU2019202838A1 (en) Inhibitors of cyclin-dependent kinase 7 (CDK7)
AU2017250369A1 (en) Amine-substituted aryl or heteroaryl compounds as EHMT1 and EHMT2 inhibitors
EP3555070A1 (en) Amine-substituted heterocyclic compounds as ehmt2 inhibitors and methods of use thereof
WO2014134772A1 (en) Compounds inhibiting leucine-rich repeat kinase enzyme activity
US20220144838A1 (en) Compounds as Inhibitors of Macrophage Migration Inhibitory Factor
JP2024527623A (ja) 癌の治療のためのhpk1阻害剤としての置換ピラジン-2-カルボキサミド阻害剤
WO2024017372A1 (zh) 一种吲哚酮衍生物及其应用
JP7770065B2 (ja) サイクリン依存性キナーゼ阻害剤
CN118510764A (zh) 新颖苯并咪唑吡啶衍生物
HK40065957A (zh) 用作cdk抑制剂的经过取代的杂环衍生物
HK40097285A (zh) Myc家族原癌基因蛋白的调节剂
HK1255239B (zh) 用作cdk抑制剂的经过取代的杂环衍生物
HK1229328A1 (en) Inhibitors of cyclin-dependent kinase 7 (cdk7)
HK1229328B (en) Inhibitors of cyclin-dependent kinase 7 (cdk7)

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant
CP01 Change in the name or title of a patent holder
CP01 Change in the name or title of a patent holder

Address after: Karnataka

Patentee after: Oregini Oncology Co.,Ltd.

Address before: Karnataka

Patentee before: AURIGENE DISCOVERY TECHNOLOGIES Ltd.

CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20211008