JP7590996B2 - Egfr阻害剤としての新たな大環状化合物および誘導体 - Google Patents

Egfr阻害剤としての新たな大環状化合物および誘導体 Download PDF

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JP7590996B2
JP7590996B2 JP2021576576A JP2021576576A JP7590996B2 JP 7590996 B2 JP7590996 B2 JP 7590996B2 JP 2021576576 A JP2021576576 A JP 2021576576A JP 2021576576 A JP2021576576 A JP 2021576576A JP 7590996 B2 JP7590996 B2 JP 7590996B2
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alkylene
cancer
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ハーラルト エンゲルハルト
ディートリッヒ ベーゼ
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ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング
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    • 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
    • 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
    • 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
    • C07D487/22Heterocyclic 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 four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2021576576A 2019-06-24 2020-06-23 Egfr阻害剤としての新たな大環状化合物および誘導体 Active JP7590996B2 (ja)

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Application Number Priority Date Filing Date Title
EP19181952.3 2019-06-24
EP19181952 2019-06-24
PCT/EP2020/067451 WO2020260252A1 (en) 2019-06-24 2020-06-23 New macrocyclic compounds and derivatives as egfr inhibitors

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JP2022538228A JP2022538228A (ja) 2022-09-01
JP2022538228A5 JP2022538228A5 (https=) 2023-06-26
JP7590996B2 true JP7590996B2 (ja) 2024-11-27

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US (1) US12522615B2 (https=)
EP (1) EP3986564A1 (https=)
JP (1) JP7590996B2 (https=)
CN (1) CN114007698B (https=)
WO (1) WO2020260252A1 (https=)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4079735B1 (en) 2019-12-16 2025-08-06 Beijing Tide Pharmaceutical Co., Ltd. Macrocyclic compounds for inhibiting and inducing degradation of egfr kinase in the treatment of cancer
CN113880804A (zh) * 2020-07-01 2022-01-04 微境生物医药科技(上海)有限公司 新型苯并咪唑化合物
CN114163454B (zh) * 2020-09-11 2026-01-02 上海翰森生物医药科技有限公司 含吡啶多环类衍生物抑制剂、其制备方法和应用
WO2022098992A1 (en) * 2020-11-05 2022-05-12 Scorpion Therapeutics, Inc. Use of macrocyclic compounds in methods of treating cancer
CN114057771B (zh) * 2020-12-03 2023-10-03 北京鞍石生物科技有限责任公司 大环化合物及其制备方法和应用
CN114656482B (zh) * 2020-12-23 2025-10-17 南京圣和药业股份有限公司 作为egfr抑制剂的大环杂环类化合物及其应用
CN116761603A (zh) * 2021-02-06 2023-09-15 正大天晴药业集团股份有限公司 含有苯并杂环的作为egfr激酶抑制剂的大环化合物、其药物组合物和用途
CN114907379B (zh) * 2021-02-06 2026-04-17 正大天晴药业集团股份有限公司 作为egfr激酶抑制剂的大环化合物
AU2022230397A1 (en) * 2021-03-02 2023-09-21 Dana-Farber Cancer Institute, Inc. Covalent egfr inhibitors and methods of use thereof
IL306067A (en) * 2021-03-26 2023-11-01 Theseus Pharmaceuticals Inc Macrocyclic egfr inhibitors for the treatment of cancer
TW202309022A (zh) 2021-04-13 2023-03-01 美商努法倫特公司 用於治療具egfr突變之癌症之胺基取代雜環
CN115368378B (zh) * 2021-05-21 2024-11-19 深圳市塔吉瑞生物医药有限公司 取代的大环化合物及包含该化合物的组合物及其用途
IL309040A (en) * 2021-06-30 2024-02-01 Aqilion Ab Macrocyclic TAK1 inhibitors
WO2023001069A1 (zh) * 2021-07-23 2023-01-26 南京明德新药研发有限公司 大环酰胺类化合物及其应用
TW202330550A (zh) * 2021-11-30 2023-08-01 大陸商正大天晴藥業集團股份有限公司 含有環烷基或鹵代烷基的化合物
US20250282795A1 (en) * 2022-04-20 2025-09-11 Celyn Therapeutics, Inc. EGFR Inhibitors in cancer treatment
CN117024443A (zh) * 2022-05-09 2023-11-10 元启(苏州)生物制药有限公司 Egfr抑制剂及其用途
CN119522227A (zh) * 2022-07-21 2025-02-25 贝达药业股份有限公司 大环化合物及其药物组合物和应用
CN119487039A (zh) 2022-07-21 2025-02-18 贝达药业股份有限公司 大环化合物及其药物组合物和应用
TW202416963A (zh) * 2022-09-02 2024-05-01 大陸商迪哲(江蘇)醫藥股份有限公司 Egfr抑制劑及其用途
WO2024078263A1 (zh) * 2022-10-09 2024-04-18 药雅科技(上海)有限公司 大环杂环类化合物作为egfr抑制剂的制备及其应用
CN117229300A (zh) * 2023-03-12 2023-12-15 药雅科技(上海)有限公司 Egfr抑制剂的制备及其应用
WO2024099402A1 (en) * 2022-11-10 2024-05-16 Beigene (Beijing) Co., Ltd. Intermediates and process of compounds for the degradation of egfr kinase
WO2024099400A1 (en) * 2022-11-10 2024-05-16 Beigene (Beijing) Co., Ltd. Intermediates and process of compounds for the degradation of egfr kinase
TW202428267A (zh) * 2022-11-10 2024-07-16 英屬開曼群島商百濟神州有限公司 用於降解egfr激酶之化合物
CN118324778A (zh) * 2023-04-25 2024-07-12 苏州共康医药科技有限公司 第四代egfr抑制剂
EP4720071A1 (en) * 2023-05-31 2026-04-08 Beone Medicines I GmbH Compounds for the degradation of egfr kinase

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015518894A (ja) 2012-06-06 2015-07-06 アイアールエム・リミテッド・ライアビリティ・カンパニーIrm,Llc Egfr活性を調節するための化合物および組成物
JP2015518895A (ja) 2012-06-06 2015-07-06 アイアールエム・リミテッド・ライアビリティ・カンパニーIrm,Llc Egfr活性を調節するための化合物および組成物
JP2016507539A (ja) 2013-02-07 2016-03-10 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung 大環状ピリダジノン誘導体

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7132438B2 (en) 2001-10-09 2006-11-07 Amgen Inc. Benzimidazole derivatives
JP2005509003A (ja) 2001-11-09 2005-04-07 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド タンパク質キナーゼインヒビターとして有用なベンゾイミダゾール化合物
EP1388341A1 (en) 2002-08-07 2004-02-11 Aventis Pharma Deutschland GmbH Acylamino-substituted heteroaromatic compounds and their use as pharmaceuticals
AU2003257094A1 (en) 2002-08-08 2004-02-25 Boehringer Ingelheim Pharmaceuticals, Inc. Substituted benzimidazole compounds
WO2005070420A1 (en) 2004-01-14 2005-08-04 Boehringer Ingelheim Pharmaceuticals, Inc. 1h-benzimidazol-2-yl-benzamide derivatives and related compounds as itk inhibitors (interleukin-2-inducible t cell kinase) for the treatment of inflammation, immunological and allergic disorders
WO2005079791A1 (en) 2004-02-12 2005-09-01 Boehringer Ingelheim Pharmaceuticals, Inc. Thiophene -2- carboxylic acid - (1h - benzimidazol - 2 yl) - amide derivatives and related compounds as inhibitors of the tec kinase itk (interleukin -2- inducible t cell kinase) for the treatment of inflammation, immunological and allergic disorders
WO2007133983A2 (en) 2006-05-08 2007-11-22 Pharmacopeia, Inc. 2-aminobenzimidazoles for treating neurodegenerative diseases
SG10201505997TA (en) 2010-08-05 2015-09-29 Amgen Inc Benzimidazole And Azabenzimidazole Compounds That Inhibit Anaplastic Lymphoma Kinase
CN103159742B (zh) * 2011-12-16 2015-08-12 北京韩美药品有限公司 5-氯嘧啶类化合物及其作为egfr酪氨酸激酶抑制剂的应用
US9573958B2 (en) * 2012-08-31 2017-02-21 Principia Biopharma, Inc. Benzimidazole derivatives as ITK inhibitors
WO2014081718A1 (en) 2012-11-20 2014-05-30 Genentech, Inc. Aminopyrimidine compounds as inhibitors of t790m containing egfr mutants
WO2014210354A1 (en) 2013-06-28 2014-12-31 Genentech, Inc. Azaindazole compounds as inhibitors of t790m containing egfr mutants
CN104513253A (zh) 2013-10-01 2015-04-15 南京波尔泰药业科技有限公司 用于治疗增殖性疾病的大环化合物
CA2943220C (en) 2014-03-20 2024-01-16 Capella Therapeutics, Inc. Benzimidazole derivatives as erbb tyrosine kinase inhibitors for the treatment of cancer
JP6568926B2 (ja) 2014-03-20 2019-08-28 カペラ セラピューティクス,インコーポレーテッド 癌の治療のためのerbbチロシンキナーゼ阻害剤としてのベンゾイミダゾール誘導体
WO2016176473A1 (en) 2015-04-28 2016-11-03 Sanford-Burnham Medical Researc Institute Apelin receptor agonists and methods of use thereof
CN108012529A (zh) 2015-05-15 2018-05-08 诺华股份有限公司 治疗egfr突变的癌症的方法
JP6845165B2 (ja) 2015-06-30 2021-03-17 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 Egfr阻害剤およびその使用方法
EP3328418A1 (en) 2015-07-29 2018-06-06 Novartis AG Combination therapies comprising antibody molecules to pd-1
BR112018003812B1 (pt) 2015-09-18 2024-04-30 Merck Patent Gmbh Compostos de heteroarila como inibidores de irak, seu uso, composição farmacêutica, e kit
CN108602776B (zh) 2015-09-18 2021-12-03 默克专利有限公司 用作irak抑制剂的杂芳基化合物及其用途
RU2019102647A (ru) 2016-07-01 2020-08-03 Г1 Терапьютикс, Инк. Антипролиферационные средства на основе пиримидина
US11083793B2 (en) 2016-12-13 2021-08-10 Health Research, Inc. Epidermal growth factor receptor (EGFR) targeted photosensitizers

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015518894A (ja) 2012-06-06 2015-07-06 アイアールエム・リミテッド・ライアビリティ・カンパニーIrm,Llc Egfr活性を調節するための化合物および組成物
JP2015518895A (ja) 2012-06-06 2015-07-06 アイアールエム・リミテッド・ライアビリティ・カンパニーIrm,Llc Egfr活性を調節するための化合物および組成物
JP2016507539A (ja) 2013-02-07 2016-03-10 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung 大環状ピリダジノン誘導体

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CN114007698B (zh) 2024-01-09
US12522615B2 (en) 2026-01-13
CN114007698A (zh) 2022-02-01
EP3986564A1 (en) 2022-04-27
US20220380382A1 (en) 2022-12-01
JP2022538228A (ja) 2022-09-01
WO2020260252A1 (en) 2020-12-30

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