JP2019504830A - Egfr阻害剤としての新規フッ素化キナゾリン誘導体 - Google Patents

Egfr阻害剤としての新規フッ素化キナゾリン誘導体 Download PDF

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Publication number
JP2019504830A
JP2019504830A JP2018535293A JP2018535293A JP2019504830A JP 2019504830 A JP2019504830 A JP 2019504830A JP 2018535293 A JP2018535293 A JP 2018535293A JP 2018535293 A JP2018535293 A JP 2018535293A JP 2019504830 A JP2019504830 A JP 2019504830A
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Prior art keywords
difluoromethoxy
quinazolin
enamide
cancer
ethoxy
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Japanese (ja)
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JP2019504830A5 (enExample
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スラッシー、アブデルマリック
ダブ、ピーター
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Trillium Therapeutics ULC
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Trillium Therapeutics ULC
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94Nitrogen atoms
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (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)
  • Plural Heterocyclic Compounds (AREA)
JP2018535293A 2016-01-06 2017-01-06 Egfr阻害剤としての新規フッ素化キナゾリン誘導体 Withdrawn JP2019504830A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662275376P 2016-01-06 2016-01-06
US62/275,376 2016-01-06
PCT/CA2017/050015 WO2017117680A1 (en) 2016-01-06 2017-01-06 Novel fluorinated quinazoline derivatives as egfr inhibitors

Publications (2)

Publication Number Publication Date
JP2019504830A true JP2019504830A (ja) 2019-02-21
JP2019504830A5 JP2019504830A5 (enExample) 2020-02-20

Family

ID=59273095

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2018535293A Withdrawn JP2019504830A (ja) 2016-01-06 2017-01-06 Egfr阻害剤としての新規フッ素化キナゾリン誘導体

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Country Link
US (1) US20190016689A1 (enExample)
EP (1) EP3400216A4 (enExample)
JP (1) JP2019504830A (enExample)
CN (1) CN108779079A (enExample)
AU (1) AU2017204973A1 (enExample)
CA (1) CA3008312A1 (enExample)
WO (1) WO2017117680A1 (enExample)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3687981A4 (en) * 2017-09-26 2021-03-31 The Regents of the University of California COMPOSITIONS AND METHODS OF TREATMENT OF CANCER
CN113811528A (zh) 2019-03-15 2021-12-17 加利福尼亚大学董事会 用于治疗癌症的组合物和方法
KR20210142154A (ko) 2019-03-21 2021-11-24 옹쎄오 암 치료를 위한 키나제 억제제와 조합된 dbait 분자
US20220229072A1 (en) 2019-06-04 2022-07-21 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of cd9 as a biomarker and as a biotarget in glomerulonephritis or glomerulosclerosis
TWI817018B (zh) 2019-06-28 2023-10-01 美商艾瑞生藥股份有限公司 用於治療braf相關的疾病和失調症之化合物
JP2023500906A (ja) 2019-11-08 2023-01-11 インサーム(インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル) キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法
AU2020395185A1 (en) * 2019-12-04 2022-06-02 Incyte Corporation Derivatives of an FGFR inhibitor
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN111548314B (zh) * 2020-05-22 2021-09-03 上海万巷制药有限公司 一种n-(3-氯-4-氟苯基)-7-氟-6-硝基-4-喹唑啉胺的生产方法
CN116096710B (zh) 2020-06-09 2025-07-25 阿雷生物药品公司 用于治疗braf相关疾病和障碍的4-氧代-3,4-二氢喹唑啉酮化合物
CN113264888A (zh) * 2021-03-04 2021-08-17 江苏康可得生物技术股份有限公司 酪氨酸激酶抑制剂及其药物应用
TWI825637B (zh) 2021-03-31 2023-12-11 美商輝瑞股份有限公司 啶-1,6(2h,7h)-二酮
WO2023128350A1 (ko) * 2021-12-30 2023-07-06 주식회사 비투에스바이오 헤테로아릴 유도체 및 이를 유효성분으로 포함하는 암의 예방 또는 치료용 약학적 조성물
WO2024218632A1 (en) 2023-04-17 2024-10-24 Array Biopharma Inc. Erk protein kinase inhibitors

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1746999B1 (en) * 2004-05-06 2011-11-16 Warner-Lambert Company LLC 4-phenylamino-quinazolin-6-yl-amides
CN102731485B (zh) * 2011-04-02 2016-06-15 齐鲁制药有限公司 4-(取代苯氨基)喹唑啉衍生物及其制备方法、药物组合物和用途
CN102838590B (zh) * 2011-06-21 2014-07-09 苏州迈泰生物技术有限公司 氨基喹唑啉衍生物及其在制备抗恶性肿瘤药物中的用途
JP2014532063A (ja) * 2011-10-12 2014-12-04 テリジェン リミテッドTeligene Ltd キナーゼ阻害剤としてのキナゾリン誘導体およびその使用方法
CN104350049B (zh) * 2012-05-07 2016-07-13 苏州韬略生物科技有限公司 作为激酶抑制剂的取代氨基喹唑啉
CN104910140A (zh) * 2014-03-14 2015-09-16 齐鲁制药有限公司 喹唑啉类化合物、其制备方法及应用
US10196365B2 (en) * 2014-08-15 2019-02-05 Arromax Pharmatech Co., Ltd. Quinazoline derivative, preparation method therefor, and pharmaceutical composition and application thereof

Also Published As

Publication number Publication date
US20190016689A1 (en) 2019-01-17
CN108779079A (zh) 2018-11-09
EP3400216A1 (en) 2018-11-14
WO2017117680A1 (en) 2017-07-13
EP3400216A4 (en) 2019-08-14
AU2017204973A1 (en) 2018-07-12
CA3008312A1 (en) 2017-07-13

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