JP6789962B2 - ＣＤＫ阻害剤としてのピラゾロ［１，５−ａ］［１，３，５］トリアジンとピラゾロ［１，５−ａ］ピリミジン誘導体 - Google Patents

ＣＤＫ阻害剤としてのピラゾロ［１，５−ａ］［１，３，５］トリアジンとピラゾロ［１，５−ａ］ピリミジン誘導体 Download PDF

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Publication number
JP6789962B2
JP6789962B2 JP2017546949A JP2017546949A JP6789962B2 JP 6789962 B2 JP6789962 B2 JP 6789962B2 JP 2017546949 A JP2017546949 A JP 2017546949A JP 2017546949 A JP2017546949 A JP 2017546949A JP 6789962 B2 JP6789962 B2 JP 6789962B2
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compound
amino
mmol
pyrazolo
triazine
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JP2018507877A (ja
JP2018507877A5 (enExample
Inventor
サマジダール，ササンタ
ポダトーリ，ラマル
マッカジー，サブヘンドゥ
ゴスワミ，ラジーブ
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Aurigene Oncology Ltd
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Aurigene Discovery Technologies Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • 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)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2017546949A 2015-03-09 2016-03-08 ＣＤＫ阻害剤としてのピラゾロ［１，５−ａ］［１，３，５］トリアジンとピラゾロ［１，５−ａ］ピリミジン誘導体 Expired - Fee Related JP6789962B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IN1128CH2015 2015-03-09
IN1128/CHE/2015 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 (3)

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JP2018507877A JP2018507877A (ja) 2018-03-22
JP2018507877A5 JP2018507877A5 (enExample) 2020-04-30
JP6789962B2 true JP6789962B2 (ja) 2020-11-25

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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
CA2784807C (en) 2009-12-29 2021-12-14 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)
JP6491202B2 (ja) 2013-10-18 2019-03-27 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド サイクリン依存性キナーゼ７（ｃｄｋ７）の多環阻害剤
EP3805218A1 (en) * 2014-04-05 2021-04-14 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
WO2016105528A2 (en) 2014-12-23 2016-06-30 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
CA2978518C (en) * 2015-03-27 2023-11-21 Nathanael S. Gray Inhibitors of cyclin-dependent kinases
AU2016319125B2 (en) 2015-09-09 2021-04-08 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
CN111194317A (zh) 2017-07-28 2020-05-22 林伯士拉克许米公司 Tyk2抑制剂与其用途
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
CN111918863B (zh) * 2018-03-29 2024-01-05 武田药品工业株式会社 杂环化合物
EP3774809A1 (en) * 2018-04-11 2021-02-17 Qurient Co. Ltd. Pharmaceutically active pyrazolo-triazine and/or pyrazolo-pyrimidine derivatives
IL277770B2 (en) * 2018-04-11 2024-01-01 Qurient Co Ltd Pyrazolo-triazine and/or pyrazolo-pyrimidine derivatives as selective inhibitor of cyclin dependent kinase
WO2020005807A1 (en) 2018-06-25 2020-01-02 Dana-Farber Cancer Institute, Inc. Taire family kinase inhibitors and uses thereof
PT3710446T (pt) * 2018-07-20 2022-09-20 Lilly Co Eli Compostos úteis para inibir 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
BR112021008176A2 (pt) 2018-10-30 2021-08-03 Kronos Bio, Inc. compostos, composições, e métodos para a modulação da atividade da cdk9.
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
CA3162470A1 (en) * 2019-11-22 2021-05-27 The Regents Of The University Of California Caspase 6 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
US20230115907A1 (en) * 2019-12-20 2023-04-13 Evopoint Biosciences Co., Ltd. Heterocyclic compound and pharmaceutical composition, preparation method, intermediate and use thereof
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
WO2022033552A1 (zh) * 2020-08-12 2022-02-17 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
CN120712267A (zh) * 2023-02-21 2025-09-26 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
WO2025067540A1 (zh) * 2023-09-28 2025-04-03 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

Family Cites Families (19)

* 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
PL353455A1 (en) 1999-08-12 2003-11-17 Pharmacia Italia S.P.A. 3(5)-amino-pyrazole derivatives, process for their preparation and their use as antitumor agents
WO2005026129A1 (en) 2003-09-15 2005-03-24 Gpc Biotech Ag Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases
US20100160324A1 (en) 2004-12-30 2010-06-24 Astex Therapeutics Limited Pyrazole derivatives as that modulate the activity of cdk, gsk and aurora kinases
JP5507049B2 (ja) 2004-12-30 2014-05-28 アステックス、セラピューティックス、リミテッド 医薬品
US20070078136A1 (en) 2005-09-22 2007-04-05 Bristol-Myers Squibb Company Fused heterocyclic compounds useful as kinase modulators
US7517882B2 (en) * 2006-09-18 2009-04-14 Polaris Group Protein kinase inhibitors
CA2688616A1 (en) * 2007-06-05 2008-12-11 Emory University Selective inhibitors for cyclin-dependent kinases
US20110201599A1 (en) 2008-07-03 2011-08-18 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
EP2634190A1 (en) 2012-03-01 2013-09-04 Lead Discovery Center GmbH Pyrazolo-triazine derivatives as selective cyclin-dependent kinase inhinitors
EP2634189A1 (en) 2012-03-01 2013-09-04 Lead Discovery Center GmbH Pyrazolo-triazine derivatives as selective cyclin-dependent kinase inhibitors
US10112927B2 (en) 2012-10-18 2018-10-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
CN110746424A (zh) * 2013-03-15 2020-02-04 西建卡尔有限责任公司 Mk2抑制剂和其用途
EP3805218A1 (en) 2014-04-05 2021-04-14 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
CA2978518C (en) * 2015-03-27 2023-11-21 Nathanael S. Gray Inhibitors of cyclin-dependent kinases
FI3302448T3 (fi) * 2015-06-04 2024-01-24 Aurigene Oncology Ltd Substituoituja heterosyklyylijohdannaisia cdk-inhibiittoreina

Also Published As

Publication number Publication date
CN107530329A (zh) 2018-01-02
JP2018507877A (ja) 2018-03-22
EP3268000B1 (en) 2021-08-04
ES2899196T3 (es) 2022-03-10
CA2978170A1 (en) 2016-09-15
WO2016142855A3 (en) 2016-11-03
EP3268000A4 (en) 2018-08-22
US20180057497A1 (en) 2018-03-01
CA2978170C (en) 2024-02-27
US20180258092A9 (en) 2018-09-13
US11186576B2 (en) 2021-11-30
EP3268000A2 (en) 2018-01-17
CN107530329B (zh) 2021-10-08
WO2016142855A2 (en) 2016-09-15
US20220281871A1 (en) 2022-09-08

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