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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JP2018535293A
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Japanese (ja)
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JP2019504830A5 (enExample
Inventor
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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Publication of JP2019504830A publication Critical patent/JP2019504830A/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94—Nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • 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
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (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

Country Status (7)

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)

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KR20240017986A (ko) * 2017-09-26 2024-02-08 더 리전트 오브 더 유니버시티 오브 캘리포니아 암 치료를 위한 조성물 및 방법
KR102809395B1 (ko) 2019-03-15 2025-05-16 더 리전트 오브 더 유니버시티 오브 캘리포니아 암을 치료하기 위한 조성물 및 방법
CA3129665A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
US12523663B2 (en) 2019-06-04 2026-01-13 Inserm (Institut National De La Santé Et De La Rescherche 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
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
MX2022006691A (es) * 2019-12-04 2022-09-19 Incyte Corp Derivados de un inhibidor de receptores del factor de crecimiento de fibroblastos (fgfr).
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
MX2022015703A (es) 2020-06-09 2023-01-24 Array Biopharma Inc Compuestos para el tratamiento de enfermedades y trastornos asociados a braf.
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
CA3233057A1 (en) 2021-09-23 2023-03-30 Erasca, Inc. Egfr inhibitor polymorph forms
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
CN119241448A (zh) * 2024-08-16 2025-01-03 安润医药科技（苏州）有限公司 一种酪氨酸激酶抑制剂的可药用盐、晶体、制备方法及其用途

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HRP20110958T1 (hr) * 2004-05-06 2012-01-31 Warner-Lambert Company Llc 4-fenilaminokinazolin-6-ilamidi
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
WO2013166952A1 (en) * 2012-05-07 2013-11-14 Teligene Ltd Substituted aminoquinazolines useful as kinases inhibitors
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
WO2016023217A1 (zh) * 2014-08-15 2016-02-18 安润医药科技（苏州）有限公司 喹唑啉衍生物、其制备方法、药物组合物和应用

Also Published As

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

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