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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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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JP2018507877A5 (OSRAM
JP2018507877A (ja
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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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    • 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

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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)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (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
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 (3)

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

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JP2017546949A Expired - Fee Related JP6789962B2 (ja) 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

Country Status (7)

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

Families Citing this family (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2519517B1 (en) 2009-12-29 2015-03-25 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
JP6106685B2 (ja) 2011-11-17 2017-04-05 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 C−jun−n−末端キナーゼ(jnk)の阻害剤
AU2014337044A1 (en) 2013-10-18 2016-05-05 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)
EP3805218A1 (en) * 2014-04-05 2021-04-14 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
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
EP3268000B1 (en) * 2015-03-09 2021-08-04 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
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
DK3658557T3 (da) 2017-07-28 2024-07-29 Takeda Pharmaceuticals Co Tyk2-inhibitorer og anvendelser deraf
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
HRP20241119T1 (hr) 2018-03-29 2024-11-22 Takeda Pharmaceutical Company Limited Heterociklički spoj
CA3095880A1 (en) * 2018-04-11 2019-10-17 Qurient Co., Ltd. Pyrazolo-triazine and/or pyrazolo-pyrimidine derivatives as selective inhibitor of cyclin dependent kinase
US11858937B2 (en) * 2018-04-11 2024-01-02 Qurient Co., Ltd. Substituted pyrazolo[1,5-a]pyrimidines and pyrazolo[1,5-a][1,3,5]triazines as CDK inhibitors
EP3810132A4 (en) 2018-06-25 2022-06-22 Dana-Farber Cancer Institute, Inc. TAIRE FAMILY KINASE INHIBITORS AND RELATED USES
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
MD20210033A2 (ro) 2018-10-30 2021-10-31 Kronos Bio, Inc. Compuşi, compoziţii şi metode pentru modularea activităţii CDK9
US20220144841A1 (en) * 2019-03-13 2022-05-12 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
AU2020386639A1 (en) * 2019-11-22 2022-06-02 Shangpharma Innovation Inc. 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
AU2020404326A1 (en) * 2019-12-20 2022-08-11 Evopoint Biosciences Co., Ltd. Heterocyclic compound, and pharmaceutical composition thereof, preparation method therefor, intermediate thereof and application 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
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
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
US20240217960A1 (en) * 2021-04-09 2024-07-04 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
SK1812002A3 (en) 1999-08-12 2003-02-04 Pharmacia Italia Spa 3(5)-Amino-pyrazole derivatives, process for their preparation and their use as antitumor agents
US8084457B2 (en) 2003-09-15 2011-12-27 Lead Discovery Center Gmbh Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases
WO2006070198A1 (en) 2004-12-30 2006-07-06 Astex Therapeutics Limited Pyrazole derivatives as that modulate the activity of cdk, gsk and aurora kinases
TWI427077B (zh) 2004-12-30 2014-02-21 Astex Therapeutics Ltd 吡唑化合物及其用途和含有彼之藥學組成物
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
AU2008261027A1 (en) * 2007-06-05 2008-12-11 Emory University Selective inhibitors for cyclin-dependent kinases
WO2010003133A2 (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
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)
CA2908098A1 (en) * 2013-03-15 2014-09-25 Celgene Avilomics Research, Inc. Mk2 inhibitors and uses thereof
EP3805218A1 (en) 2014-04-05 2021-04-14 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
EP3268000B1 (en) * 2015-03-09 2021-08-04 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

Also Published As

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

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