CN114007698B - 作为egfr抑制剂的大环化合物和衍生物 - Google Patents
作为egfr抑制剂的大环化合物和衍生物 Download PDFInfo
- Publication number
- CN114007698B CN114007698B CN202080045795.1A CN202080045795A CN114007698B CN 114007698 B CN114007698 B CN 114007698B CN 202080045795 A CN202080045795 A CN 202080045795A CN 114007698 B CN114007698 B CN 114007698B
- Authority
- CN
- China
- Prior art keywords
- alkyl
- egfr
- cancer
- group
- pharmaceutically acceptable
- 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.)
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/22—Heterocyclic 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
-
- 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
- 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
-
- 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
- C07D487/22—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 four or more hetero rings
Landscapes
- 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)
Applications Claiming Priority (3)
| 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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN114007698A CN114007698A (zh) | 2022-02-01 |
| CN114007698B true CN114007698B (zh) | 2024-01-09 |
Family
ID=67003267
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202080045795.1A Active CN114007698B (zh) | 2019-06-24 | 2020-06-23 | 作为egfr抑制剂的大环化合物和衍生物 |
Country Status (5)
| Country | Link |
|---|---|
| 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)
| 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 (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103159742A (zh) * | 2011-12-16 | 2013-06-19 | 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 |
| CN104379575A (zh) * | 2012-06-06 | 2015-02-25 | Irm责任有限公司 | 用于调节egfr活性的化合物和组合物 |
| CN104520291A (zh) * | 2012-06-06 | 2015-04-15 | Irm责任有限公司 | 用于调节egfr活性的化合物和组合物 |
| CN105008371A (zh) * | 2013-02-07 | 2015-10-28 | 默克专利股份公司 | 大环哒嗪酮衍生物 |
| WO2018005860A1 (en) * | 2016-07-01 | 2018-01-04 | G1 Therapeutics, Inc. | Pyrimidine-based antiproliferative agents |
| WO2018112111A1 (en) * | 2016-12-13 | 2018-06-21 | Health Research, Inc. | Epidermal growth factor receptor (egfr) targeted photosensitizers |
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| 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 |
| 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 |
-
2020
- 2020-06-23 WO PCT/EP2020/067451 patent/WO2020260252A1/en not_active Ceased
- 2020-06-23 JP JP2021576576A patent/JP7590996B2/ja active Active
- 2020-06-23 US US17/621,420 patent/US12522615B2/en active Active
- 2020-06-23 CN CN202080045795.1A patent/CN114007698B/zh active Active
- 2020-06-23 EP EP20734188.4A patent/EP3986564A1/en active Pending
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103159742A (zh) * | 2011-12-16 | 2013-06-19 | 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 |
| CN104379575A (zh) * | 2012-06-06 | 2015-02-25 | Irm责任有限公司 | 用于调节egfr活性的化合物和组合物 |
| CN104520291A (zh) * | 2012-06-06 | 2015-04-15 | Irm责任有限公司 | 用于调节egfr活性的化合物和组合物 |
| CN105008371A (zh) * | 2013-02-07 | 2015-10-28 | 默克专利股份公司 | 大环哒嗪酮衍生物 |
| WO2018005860A1 (en) * | 2016-07-01 | 2018-01-04 | G1 Therapeutics, Inc. | Pyrimidine-based antiproliferative agents |
| WO2018112111A1 (en) * | 2016-12-13 | 2018-06-21 | Health Research, Inc. | Epidermal growth factor receptor (egfr) targeted photosensitizers |
Non-Patent Citations (1)
| Title |
|---|
| TKI耐药后针对T790M突变治疗;王红等;《中国肺癌杂志》;第18卷(第4期);第245-250页 * |
Also Published As
| Publication number | Publication date |
|---|---|
| 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 |
| JP7590996B2 (ja) | 2024-11-27 |
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| 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 |