CA2987914C - Inhibitors of egfr and methods of use thereof - Google Patents
Inhibitors of egfr and methods of use thereof Download PDFInfo
- Publication number
- CA2987914C CA2987914C CA2987914A CA2987914A CA2987914C CA 2987914 C CA2987914 C CA 2987914C CA 2987914 A CA2987914 A CA 2987914A CA 2987914 A CA2987914 A CA 2987914A CA 2987914 C CA2987914 C CA 2987914C
- Authority
- CA
- Canada
- Prior art keywords
- oxoisoindolin
- thiazol
- phenyl
- oxo
- yoacetamide
- 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.)
- Active
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/44—Iso-indoles; Hydrogenated iso-indoles
- C07D209/46—Iso-indoles; Hydrogenated iso-indoles with an oxygen atom in position 1
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D277/38—Nitrogen atoms
- C07D277/44—Acylated amino or imino radicals
- C07D277/46—Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Indole Compounds (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562186563P | 2015-06-30 | 2015-06-30 | |
| US62/186,563 | 2015-06-30 | ||
| US201562259895P | 2015-11-25 | 2015-11-25 | |
| US62/259,895 | 2015-11-25 | ||
| PCT/US2016/040421 WO2017004383A1 (en) | 2015-06-30 | 2016-06-30 | Inhibitors of egfr and methods of use thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2987914A1 CA2987914A1 (en) | 2017-01-05 |
| CA2987914C true CA2987914C (en) | 2022-09-13 |
Family
ID=57609152
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2987914A Active CA2987914C (en) | 2015-06-30 | 2016-06-30 | Inhibitors of egfr and methods of use thereof |
Country Status (8)
| Country | Link |
|---|---|
| US (3) | US10385019B2 (https=) |
| EP (1) | EP3317273B1 (https=) |
| JP (1) | JP6845165B2 (https=) |
| CN (1) | CN107849034B (https=) |
| AU (1) | AU2016288204B2 (https=) |
| CA (1) | CA2987914C (https=) |
| HK (1) | HK1252693A1 (https=) |
| WO (1) | WO2017004383A1 (https=) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3365334B1 (en) * | 2015-10-21 | 2024-07-17 | Otsuka Pharmaceutical Co., Ltd. | Benzolactam compounds as protein kinase inhibitors |
| EP3445357B1 (en) * | 2016-04-22 | 2021-05-26 | Dana-Farber Cancer Institute, Inc. | Bifunctional molecules for degradation of egfr and methods of use |
| EP3453392B1 (en) * | 2016-05-17 | 2025-10-22 | Japanese Foundation For Cancer Research | Therapeutic agent for lung cancer that has acquired egfr-tki resistance |
| TW201834651A (zh) | 2016-12-22 | 2018-10-01 | 瑞士商赫孚孟拉羅股份公司 | 化合物 |
| MX2019007646A (es) | 2016-12-23 | 2019-09-06 | Arvinas Operations Inc | Moleculas quimericas dirigidas a la proteolisis del egfr y metodos asociados de uso. |
| JP7191045B2 (ja) * | 2017-06-02 | 2022-12-16 | エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト | 化合物 |
| CN109111439B (zh) * | 2017-06-26 | 2020-09-18 | 深圳市塔吉瑞生物医药有限公司 | 一种酰胺类化合物及包含该化合物的组合物及其用途 |
| EP3700901A1 (en) | 2017-10-24 | 2020-09-02 | Genentech, Inc. | (4-hydroxypyrrolidin-2-yl)-heterocyclic compounds and methods of use thereof |
| TW201945357A (zh) * | 2018-02-05 | 2019-12-01 | 瑞士商赫孚孟拉羅股份公司 | 化合物 |
| US20210077469A1 (en) * | 2018-02-20 | 2021-03-18 | Dana-Farber Cancer Institute, Inc. | Pharmaceutical combinations of egfr inhibitors and methods of use thereof |
| WO2019162323A1 (en) | 2018-02-21 | 2019-08-29 | Boehringer Ingelheim International Gmbh | New benzimidazole compounds and derivatives as egfr inhibitors |
| WO2019183523A1 (en) * | 2018-03-23 | 2019-09-26 | Genentech, Inc. | Hetero-bifunctional degrader compounds and their use as modulators of targeted ubiquination (vhl) |
| CN110372666B (zh) * | 2018-04-13 | 2022-11-08 | 华东理工大学 | 喹唑啉类化合物作为egfr三突变抑制剂及其应用 |
| SG11202011818YA (en) * | 2018-06-29 | 2020-12-30 | Hoffmann La Roche | Compounds |
| CN108892664A (zh) * | 2018-07-02 | 2018-11-27 | 秦继伟 | 一种酰胺类化合物及其合成方法和治疗癌症的用途 |
| CN108912115A (zh) * | 2018-07-02 | 2018-11-30 | 秦继伟 | 一种用于治疗肺癌的egfr酪氨酸激酶抑制剂 |
| CN108570044A (zh) * | 2018-07-02 | 2018-09-25 | 秦继伟 | 一种酰胺类化合物及其合成方法和治疗癌症的用途 |
| CN108690013A (zh) * | 2018-07-02 | 2018-10-23 | 秦继伟 | 苯并[d]噻唑衍生物及其作为EGFR抑制剂在癌症治疗中的应用 |
| JP7561777B2 (ja) * | 2019-06-21 | 2024-10-04 | エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト | 新規ｅｇｆｒ阻害剤 |
| WO2020257632A1 (en) * | 2019-06-21 | 2020-12-24 | Dana-Farber Cancer Institute, Inc. | Allosteric egfr inhibitors and methods of use thereof |
| US12377080B2 (en) | 2019-06-21 | 2025-08-05 | Dana-Farber Cancer Institute, Inc. | Allosteric EGFR inhibitors and methods of use thereof |
| CN114008049B (zh) | 2019-06-21 | 2024-07-05 | 豪夫迈·罗氏有限公司 | 用于癌症治疗的egfr抑制剂 |
| CN113993591A (zh) * | 2019-06-21 | 2022-01-28 | 豪夫迈·罗氏有限公司 | 新egfr抑制剂 |
| JP7590996B2 (ja) | 2019-06-24 | 2024-11-27 | 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 | Ｅｇｆｒ阻害剤としての新たな大環状化合物および誘導体 |
| IL326879A (en) | 2019-11-11 | 2026-04-01 | Dana Farber Cancer Inst Inc | EGFR allosteric inhibitors and methods of using them |
| KR102267662B1 (ko) * | 2019-11-19 | 2021-06-22 | 한국화학연구원 | 벤즈아미드 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물 |
| AR120800A1 (es) * | 2019-12-20 | 2022-03-16 | Hoffmann La Roche | Derivados de 6,7-dihidro-5h-pirrolo[1,2-c]imidazol como inhibidores de egfr |
| AR120799A1 (es) * | 2019-12-20 | 2022-03-16 | Hoffmann La Roche | 2-[4-cloro-6-[2-[4-[[4-(hidroximetil)-1-piperidil]metil]fenil]etinil]-1-oxoisoindolin-2-il]-2-(6,7-dihidro-5h-pirrolo[1,2-c]imidazol-1-il)-n-tiazol-2-il-acetamida como inhibidor de egfr |
| BR112022011827A2 (pt) * | 2019-12-20 | 2022-08-30 | C4 Therapeutics Inc | Composto, composição farmacêutica, uso de um composto, métodos para tratamento ou profilaxia de câncer e para tratar um paciente com um distúrbio mediado por receptor do fator de crescimento epidérmico, e, invenção |
| CN115811977A (zh) * | 2020-06-09 | 2023-03-17 | 达纳-法伯癌症研究所股份有限公司 | 变构egfr抑制剂及其使用方法 |
| CN111592535B (zh) * | 2020-06-22 | 2021-07-20 | 通化师范学院 | 一种抗egfr突变的抑制剂eai045的制备方法 |
| JP7805363B2 (ja) | 2020-11-02 | 2026-01-23 | 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 | ＥＧＦＲ阻害薬としての置換１Ｈ－ピラゾロ［４，３－ｃ］及び誘導体 |
| PE20240099A1 (es) * | 2020-12-01 | 2024-01-18 | Hoffmann La Roche | Nuevos derivados de indazol acetileno |
| JP7840324B2 (ja) | 2020-12-01 | 2026-04-03 | エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト | 新規インダゾール誘導体 |
| CN116600806A (zh) * | 2020-12-01 | 2023-08-15 | 豪夫迈·罗氏有限公司 | 新的吲唑衍生物 |
| WO2022245061A1 (ko) * | 2021-05-17 | 2022-11-24 | 에이치케이이노엔 주식회사 | 벤즈아미드 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물 |
| AR127064A1 (es) | 2021-09-15 | 2023-12-13 | Hua Medicine Shanghai Ltd | Prodroga de derivados de pirrolidona como activador de glucoquinasa |
| CN117126142B (zh) * | 2023-08-30 | 2026-02-10 | 遵义医科大学珠海校区 | 杂环类egfr突变抑制剂及其应用 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003055482A1 (en) * | 2001-12-21 | 2003-07-10 | Novo Nordisk A/S | Amide derivatives as gk activators |
| WO2004072102A2 (en) * | 2003-02-11 | 2004-08-26 | Bristol-Myers Squibb Company | Benzene acetamide compounds useful as serine protease inhibitors |
| GB0320197D0 (en) * | 2003-08-28 | 2003-10-01 | Novartis Ag | Organic compounds |
| WO2007002313A2 (en) * | 2005-06-24 | 2007-01-04 | Bristol-Myers Squibb Company | Phenylglycinamide and pyridylglycinamide derivatives useful as anticoagulants |
| GB0517740D0 (en) * | 2005-08-31 | 2005-10-12 | Novartis Ag | Organic compounds |
| US8034822B2 (en) * | 2006-03-08 | 2011-10-11 | Takeda San Diego, Inc. | Glucokinase activators |
| EP2049518B1 (en) * | 2006-05-31 | 2011-08-31 | Takeda San Diego, Inc. | Indazole and isoindole derivatives as glucokinase activating agents. |
| KR20190126460A (ko) * | 2007-02-09 | 2019-11-11 | 메타베이시스 테라퓨틱스, 인크. | 글루카곤 수용체의 길항제 |
| EP2240475B1 (en) * | 2007-12-20 | 2013-09-25 | Novartis AG | Thiazole derivatives used as pi 3 kinase inhibitors |
| WO2010021882A2 (en) * | 2008-08-19 | 2010-02-25 | Janssen Pharmaceutica Nv | Cold menthol receptor antagonists |
| WO2010039534A2 (en) * | 2008-09-23 | 2010-04-08 | Georgetown University | Viral and fungal inhibitors |
| US20120142705A1 (en) * | 2010-12-06 | 2012-06-07 | Robert Francis Kester | Isatin and oxindole compounds |
| WO2012129562A2 (en) | 2011-03-24 | 2012-09-27 | The Scripps Research Institute | Compounds and methods for inducing chondrogenesis |
| US8470866B2 (en) * | 2011-05-03 | 2013-06-25 | Hoffmann-La Roche Inc. | Isoindolinone derivatives |
| JO3300B1 (ar) * | 2012-06-06 | 2018-09-16 | Novartis Ag | مركبات وتركيبات لتعديل نشاط egfr |
| WO2014106800A2 (en) * | 2013-01-04 | 2014-07-10 | Aurigene Discovery Technologies Limited | Substituted 2-amino pyrimidine derivatives as kinase inhibitors |
-
2016
- 2016-06-30 CA CA2987914A patent/CA2987914C/en active Active
- 2016-06-30 WO PCT/US2016/040421 patent/WO2017004383A1/en not_active Ceased
- 2016-06-30 EP EP16818796.1A patent/EP3317273B1/en active Active
- 2016-06-30 CN CN201680043974.5A patent/CN107849034B/zh active Active
- 2016-06-30 US US15/580,088 patent/US10385019B2/en active Active
- 2016-06-30 HK HK18112001.2A patent/HK1252693A1/zh unknown
- 2016-06-30 AU AU2016288204A patent/AU2016288204B2/en not_active Ceased
- 2016-06-30 JP JP2017568230A patent/JP6845165B2/ja active Active
-
2019
- 2019-06-13 US US16/440,803 patent/US10836722B2/en active Active
-
2020
- 2020-09-28 US US17/035,164 patent/US20210094913A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| US10385019B2 (en) | 2019-08-20 |
| CN107849034B (zh) | 2021-09-03 |
| CN107849034A (zh) | 2018-03-27 |
| US20200002279A1 (en) | 2020-01-02 |
| CA2987914A1 (en) | 2017-01-05 |
| HK1252693A1 (zh) | 2019-05-31 |
| US20180290975A1 (en) | 2018-10-11 |
| EP3317273A1 (en) | 2018-05-09 |
| WO2017004383A1 (en) | 2017-01-05 |
| JP2018522879A (ja) | 2018-08-16 |
| US10836722B2 (en) | 2020-11-17 |
| JP6845165B2 (ja) | 2021-03-17 |
| EP3317273B1 (en) | 2021-12-29 |
| EP3317273A4 (en) | 2019-03-20 |
| AU2016288204B2 (en) | 2020-11-05 |
| AU2016288204A1 (en) | 2017-12-21 |
| US20210094913A1 (en) | 2021-04-01 |
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Free format text: ST27 STATUS EVENT CODE: N-6-6-H10-H13-H100 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE AND LATE FEE NOT PAID BY DEADLINE OF NOTICE Effective date: 20260325 Free format text: ST27 STATUS EVENT CODE: N-4-6-H10-H13-H100 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE AND LATE FEE NOT PAID BY DEADLINE OF NOTICE Effective date: 20260325 |