AU2017204973A1 - Novel fluorinated quinazoline derivatives as EGFR inhibitors - Google Patents

Novel fluorinated quinazoline derivatives as EGFR inhibitors Download PDF

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Publication number
AU2017204973A1
AU2017204973A1 AU2017204973A AU2017204973A AU2017204973A1 AU 2017204973 A1 AU2017204973 A1 AU 2017204973A1 AU 2017204973 A AU2017204973 A AU 2017204973A AU 2017204973 A AU2017204973 A AU 2017204973A AU 2017204973 A1 AU2017204973 A1 AU 2017204973A1
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AU
Australia
Prior art keywords
difluoromethoxy
compound
enamide
ethoxy
anilino
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.)
Abandoned
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AU2017204973A
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English (en)
Inventor
Peter Dove
Abdelmalik Slassi
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Trillium Therapeutics ULC
Original Assignee
Trillium Therapeutics ULC
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Trillium Therapeutics ULC filed Critical Trillium Therapeutics ULC
Publication of AU2017204973A1 publication Critical patent/AU2017204973A1/en
Abandoned legal-status Critical Current

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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

Landscapes

  • 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)
AU2017204973A 2016-01-06 2017-01-06 Novel fluorinated quinazoline derivatives as EGFR inhibitors Abandoned AU2017204973A1 (en)

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 (1)

Publication Number Publication Date
AU2017204973A1 true AU2017204973A1 (en) 2018-07-12

Family

ID=59273095

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2017204973A Abandoned AU2017204973A1 (en) 2016-01-06 2017-01-06 Novel fluorinated quinazoline derivatives as EGFR inhibitors

Country Status (7)

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

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111868039A (zh) * 2017-09-26 2020-10-30 加利福尼亚大学董事会 用于治疗癌症的组合物和方法
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
US20220143049A1 (en) 2019-03-21 2022-05-12 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
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
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
EP4054579A1 (en) 2019-11-08 2022-09-14 Institut National de la Santé et de la Recherche Médicale (INSERM) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
BR112022010664A2 (pt) * 2019-12-04 2022-08-16 Incyte Corp Derivados de um inibidor de 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
WO2021250521A1 (en) 2020-06-09 2021-12-16 Array Biopharma Inc. 4-oxo-3,4-dihydroquinazolinon compounds for the treatment of braf-associated diseases and disorders
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
WO2023049312A1 (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
CN1972688B (zh) * 2004-05-06 2012-06-27 沃尼尔·朗伯有限责任公司 4-苯胺基-喹唑啉-6-基-酰胺类化合物
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
CN103874696B (zh) * 2011-10-12 2015-06-03 苏州韬略生物科技有限公司 作为激酶抑制剂的喹唑啉衍生物及其使用方法
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
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
WO2017117680A1 (en) 2017-07-13
US20190016689A1 (en) 2019-01-17
JP2019504830A (ja) 2019-02-21
CN108779079A (zh) 2018-11-09
EP3400216A4 (en) 2019-08-14
CA3008312A1 (en) 2017-07-13

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MK4 Application lapsed section 142(2)(d) - no continuation fee paid for the application