AU2016288204B2 - Inhibitors of EGFR and methods of use thereof - Google Patents

Inhibitors of EGFR and methods of use thereof Download PDF

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Publication number
AU2016288204B2
AU2016288204B2 AU2016288204A AU2016288204A AU2016288204B2 AU 2016288204 B2 AU2016288204 B2 AU 2016288204B2 AU 2016288204 A AU2016288204 A AU 2016288204A AU 2016288204 A AU2016288204 A AU 2016288204A AU 2016288204 B2 AU2016288204 B2 AU 2016288204B2
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Australia
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alkyl
formula
egfr
optionally substituted
compound
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AU2016288204A1 (en
Inventor
Hwan Geun Choi
Michael Eck
Nathanael Gray
Jaebong Jang
Pasi Janne
Kwok-Kin Wong
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Dana Farber Cancer Institute Inc
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Dana Farber Cancer Institute Inc
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    • 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

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  • 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)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (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)
AU2016288204A 2015-06-30 2016-06-30 Inhibitors of EGFR and methods of use thereof Ceased AU2016288204B2 (en)

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
AU2016288204A1 AU2016288204A1 (en) 2017-12-21
AU2016288204B2 true AU2016288204B2 (en) 2020-11-05

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AU2016288204A Ceased AU2016288204B2 (en) 2015-06-30 2016-06-30 Inhibitors of EGFR and methods of use thereof

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US (3) US10385019B2 (enExample)
EP (1) EP3317273B1 (enExample)
JP (1) JP6845165B2 (enExample)
CN (1) CN107849034B (enExample)
AU (1) AU2016288204B2 (enExample)
CA (1) CA2987914C (enExample)
HK (1) HK1252693A1 (enExample)
WO (1) WO2017004383A1 (enExample)

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WO2017200016A1 (ja) * 2016-05-17 2017-11-23 公益財団法人がん研究会 Ｅｇｆｒ－ｔｋｉ耐性を獲得した肺癌の治療薬
TW201834651A (zh) 2016-12-22 2018-10-01 瑞士商赫孚孟拉羅股份公司 化合物
CN110753693A (zh) 2016-12-23 2020-02-04 阿尔维纳斯运营股份有限公司 Egfr蛋白水解靶向嵌合分子和相关使用方法
ES2927480T3 (es) * 2017-06-02 2022-11-07 Hoffmann La Roche Compuestos de isoindolina-acetileno para el tratamiento del cáncer
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
WO2019084026A1 (en) 2017-10-24 2019-05-02 Genentech, Inc. (4-HYDROXYPYRROLIDIN-2-YL) -HETEROCYCLIC COMPOUNDS AND METHODS OF USE
TW201945357A (zh) * 2018-02-05 2019-12-01 瑞士商赫孚孟拉羅股份公司 化合物
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JP7313364B2 (ja) 2018-02-21 2023-07-24 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ベンズイミダゾール化合物および誘導体
WO2019183523A1 (en) * 2018-03-23 2019-09-26 Genentech, Inc. Hetero-bifunctional degrader compounds and their use as modulators of targeted ubiquination (vhl)
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IL279800B2 (en) * 2018-06-29 2024-02-01 Hoffmann La Roche Selective allosteric inhibitors of epidermal growth factor receptor mutants, pharmaceutical preparations containing them and their use
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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
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TW202115073A (zh) * 2019-06-21 2021-04-16 瑞士商赫孚孟拉羅股份公司 新穎的egfr抑制劑
ES2961187T3 (es) 2019-06-21 2024-03-08 Hoffmann La Roche Inhibidor de EGFR para el tratamiento del cáncer
US12522615B2 (en) 2019-06-24 2026-01-13 Boehringer Ingelheim International Gmbh Macrocyclic compounds and derivatives as EGFR inhibitors
AU2020383423B2 (en) 2019-11-11 2026-06-18 Dana-Farber Cancer Institute, Inc. Allosteric EGFR inhibitors and methods of use thereof
KR102267662B1 (ko) 2019-11-19 2021-06-22 한국화학연구원 벤즈아미드 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물
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
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
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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
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JP7798887B2 (ja) * 2020-12-01 2026-01-14 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
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CN107849034B (zh) 2021-09-03
US20200002279A1 (en) 2020-01-02
CN107849034A (zh) 2018-03-27
US10385019B2 (en) 2019-08-20
AU2016288204A1 (en) 2017-12-21
CA2987914C (en) 2022-09-13
JP2018522879A (ja) 2018-08-16
EP3317273B1 (en) 2021-12-29
EP3317273A4 (en) 2019-03-20
US20210094913A1 (en) 2021-04-01
CA2987914A1 (en) 2017-01-05
JP6845165B2 (ja) 2021-03-17
WO2017004383A1 (en) 2017-01-05
US10836722B2 (en) 2020-11-17
HK1252693A1 (zh) 2019-05-31
EP3317273A1 (en) 2018-05-09
US20180290975A1 (en) 2018-10-11

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