AU2016214923A1 - Novel fluorinated derivatives as EGFR inhibitors useful for treating cancers - Google Patents

Novel fluorinated derivatives as EGFR inhibitors useful for treating cancers Download PDF

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Publication number
AU2016214923A1
AU2016214923A1 AU2016214923A AU2016214923A AU2016214923A1 AU 2016214923 A1 AU2016214923 A1 AU 2016214923A1 AU 2016214923 A AU2016214923 A AU 2016214923A AU 2016214923 A AU2016214923 A AU 2016214923A AU 2016214923 A1 AU2016214923 A1 AU 2016214923A1
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AU
Australia
Prior art keywords
6alkyl
substituted
nr4r5
compound
independently selected
Prior art date
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Abandoned
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AU2016214923A
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English (en)
Inventor
Peter Dove
Abdelmalik Slassi
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Trillium Therapeutics ULC
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Trillium Therapeutics ULC
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Application filed by Trillium Therapeutics ULC filed Critical Trillium Therapeutics ULC
Publication of AU2016214923A1 publication Critical patent/AU2016214923A1/en
Abandoned legal-status Critical Current

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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
    • 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
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C22/00Cyclic compounds containing halogen atoms bound to an acyclic carbon atom
    • C07C22/02Cyclic compounds containing halogen atoms bound to an acyclic carbon atom having unsaturation in the rings
    • C07C22/04Cyclic compounds containing halogen atoms bound to an acyclic carbon atom having unsaturation in the rings containing six-membered aromatic rings
    • C07C22/08Cyclic compounds containing halogen atoms bound to an acyclic carbon atom having unsaturation in the rings containing six-membered aromatic rings containing fluorine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C25/00Compounds containing at least one halogen atom bound to a six-membered aromatic ring
    • C07C25/02Monocyclic aromatic halogenated hydrocarbons
    • C07C25/13Monocyclic aromatic halogenated hydrocarbons containing fluorine
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • 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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2016214923A 2015-02-03 2016-02-03 Novel fluorinated derivatives as EGFR inhibitors useful for treating cancers Abandoned AU2016214923A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562111240P 2015-02-03 2015-02-03
US62/111,240 2015-02-03
PCT/CA2016/050094 WO2016123706A1 (en) 2015-02-03 2016-02-03 Novel fluorinated derivatives as egfr inhibitors useful for treating cancers

Publications (1)

Publication Number Publication Date
AU2016214923A1 true AU2016214923A1 (en) 2017-08-24

Family

ID=56563262

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2016214923A Abandoned AU2016214923A1 (en) 2015-02-03 2016-02-03 Novel fluorinated derivatives as EGFR inhibitors useful for treating cancers

Country Status (6)

Country Link
US (1) US20180050993A1 (enExample)
EP (1) EP3253739A4 (enExample)
JP (1) JP2018504441A (enExample)
AU (1) AU2016214923A1 (enExample)
CA (1) CA2974442A1 (enExample)
WO (1) WO2016123706A1 (enExample)

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* Cited by examiner, † Cited by third party
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CN108069913B (zh) * 2016-11-18 2022-03-01 陕西师范大学 双(吗啉基烷氧基)喹唑啉衍生物及其在抗肿瘤方面的用途
CN118459413A (zh) * 2017-09-26 2024-08-09 加利福尼亚大学董事会 用于治疗癌症的组合物和方法
WO2019071351A1 (en) * 2017-10-12 2019-04-18 Trillium Therapeutics Inc. NOVEL 4-ARYLOXYQUINAZOLINE FLUORIN DERIVATIVES AS EGFR INHIBITORS USEFUL FOR THE TREATMENT OF CANCERS
CN108329276A (zh) * 2018-04-23 2018-07-27 江苏兢业制药有限公司 杂环衍生物及其制备和用途
US12336995B2 (en) 2018-09-10 2025-06-24 Mirati Therapeutics, Inc. Combination therapies
EP3670501A1 (en) 2018-12-17 2020-06-24 Basf Se Substituted [1,2,4]triazole compounds as fungicides
JP2022526713A (ja) 2019-03-21 2022-05-26 オンクセオ がんの処置のための、キナーゼ阻害剤と組み合わせたDbait分子
WO2020245208A1 (en) 2019-06-04 2020-12-10 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
WO2021023209A1 (zh) 2019-08-05 2021-02-11 北京志健金瑞生物医药科技有限公司 含氮多环稠环类化合物,其药物组合物、制备方法和用途
US20220408745A1 (en) * 2019-09-13 2022-12-29 Meiji Co., Ltd. Solid food and solid milk having hole penetrating first face and second face
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
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN112125890B (zh) * 2020-09-25 2022-12-06 华东理工大学 一种含异吲哚酮基喹唑啉基羧酸酯类衍生物及其应用

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5747498A (en) * 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US6251912B1 (en) * 1997-08-01 2001-06-26 American Cyanamid Company Substituted quinazoline derivatives
GB9800569D0 (en) * 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
JP4703183B2 (ja) * 2002-07-15 2011-06-15 シンフォニー エボルーション, インク. 受容体型キナーゼモジュレーターおよびその使用方法
KR20050122199A (ko) * 2003-01-23 2005-12-28 티.케이. 시그널 리미티드 표피성장인자 수용체 티로신 키나제의 비가역성 억제제 및 그의 용도
WO2006071079A1 (en) * 2004-12-29 2006-07-06 Hanmi Pharm. Co., Ltd. Quinazoline derivatives for inhibiting cancer cell growth and method for the preparation thereof
MX2007010399A (es) * 2005-02-26 2007-09-25 Astrazeneca Ab Derivados de quinazolina en la forma de inhibidores de cinasa de tirosina.
WO2007029251A2 (en) * 2005-09-06 2007-03-15 T.K. Signal Ltd. Polyalkylene glycol derivatives of 4- (phenylamino)quinazolines useful as irreversible inhibitors of epidermal gr0wth fact0r receptor tyrosine kinase
JP2012501991A (ja) * 2008-09-03 2012-01-26 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 ウイルス性疾患の治療のためのキナゾリン誘導体の使用
TWI577671B (zh) * 2011-11-14 2017-04-11 Sunshine Lake Pharma Co Ltd Aminoquinazoline derivatives and salts thereof and methods of use thereof
CN104119351A (zh) * 2013-04-27 2014-10-29 复旦大学 4-(3-氯-4-氟苯基氨基)-7-甲氧基-喹唑啉化合物及其制备方法和用途

Also Published As

Publication number Publication date
JP2018504441A (ja) 2018-02-15
WO2016123706A1 (en) 2016-08-11
EP3253739A1 (en) 2017-12-13
US20180050993A1 (en) 2018-02-22
EP3253739A4 (en) 2018-07-18
CA2974442A1 (en) 2016-08-11

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MK1 Application lapsed section 142(2)(a) - no request for examination in relevant period