AU2021358596A1 - Heterocyclic inhibitors of egfr and/or her2, for use in the treatment of cancer - Google Patents

Heterocyclic inhibitors of egfr and/or her2, for use in the treatment of cancer Download PDF

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Publication number
AU2021358596A1
AU2021358596A1 AU2021358596A AU2021358596A AU2021358596A1 AU 2021358596 A1 AU2021358596 A1 AU 2021358596A1 AU 2021358596 A AU2021358596 A AU 2021358596A AU 2021358596 A AU2021358596 A AU 2021358596A AU 2021358596 A1 AU2021358596 A1 AU 2021358596A1
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compound
ring
independently selected
optionally substituted
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AU2021358596A
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AU2021358596A9 (en
Inventor
Angel Guzman-Perez
Benjamin C. MILGRAM
JR. David St. Jean
Ryan D. WHITE
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Antares Therapeutics Inc
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Scorpion Therapeutics Inc
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Publication of AU2021358596A1 publication Critical patent/AU2021358596A1/en
Publication of AU2021358596A9 publication Critical patent/AU2021358596A9/en
Assigned to ANTARES THERAPEUTICS, INC. reassignment ANTARES THERAPEUTICS, INC. Request for Assignment Assignors: SCORPION THERAPEUTICS, INC.
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    • 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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/20—Spiro-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
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/575—Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/57515—Immunoassay; Biospecific binding assay; Materials therefor for cancer of the breast
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/475—Assays involving growth factors
    • G01N2333/485—Epidermal growth factor [EGF] (urogastrone)
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2440/00—Post-translational modifications [PTMs] in chemical analysis of biological material
    • G01N2440/14—Post-translational modifications [PTMs] in chemical analysis of biological material phosphorylation

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Physics & Mathematics (AREA)
  • Biotechnology (AREA)
  • Food Science & Technology (AREA)
  • Analytical Chemistry (AREA)
  • Microbiology (AREA)
  • Pathology (AREA)
  • Cell Biology (AREA)
  • Biochemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
AU2021358596A 2020-10-09 2021-10-08 Heterocyclic inhibitors of egfr and/or her2, for use in the treatment of cancer Pending AU2021358596A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US202063089965P 2020-10-09 2020-10-09
US63/089,965 2020-10-09
US202163151468P 2021-02-19 2021-02-19
US63/151,468 2021-02-19
PCT/US2021/054191 WO2022076831A2 (en) 2020-10-09 2021-10-08 Methods for treating cancer

Publications (2)

Publication Number Publication Date
AU2021358596A1 true AU2021358596A1 (en) 2023-05-25
AU2021358596A9 AU2021358596A9 (en) 2024-10-24

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
AU2021358596A Pending AU2021358596A1 (en) 2020-10-09 2021-10-08 Heterocyclic inhibitors of egfr and/or her2, for use in the treatment of cancer

Country Status (13)

Country Link
US (1) US20240101576A1 (enExample)
EP (1) EP4225445A2 (enExample)
JP (1) JP2023548657A (enExample)
KR (1) KR20230107419A (enExample)
AU (1) AU2021358596A1 (enExample)
BR (1) BR112023006531A2 (enExample)
CA (1) CA3198202A1 (enExample)
CL (2) CL2023001012A1 (enExample)
IL (1) IL301929A (enExample)
MX (1) MX2023004085A (enExample)
PH (1) PH12023500010A1 (enExample)
TW (1) TW202227063A (enExample)
WO (1) WO2022076831A2 (enExample)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201905721D0 (en) 2019-04-24 2019-06-05 Univ Dundee Compounds
TW202309022A (zh) 2021-04-13 2023-03-01 美商努法倫特公司 用於治療具egfr突變之癌症之胺基取代雜環
WO2023205595A2 (en) * 2022-04-20 2023-10-26 Celyn Therapeutics, Inc Egfr inhibitors in cancer treatment
CN117946098A (zh) * 2022-10-28 2024-04-30 上海深势唯思科技有限责任公司 一种嘧啶类plk1抑制剂及其制备方法和用途
US20260217701A1 (en) * 2022-12-23 2026-07-30 Tay Therapeutics Limited Selective bet inhibitors and uses thereof
CN115819418B (zh) * 2023-02-14 2023-04-28 山东绿叶制药有限公司 Plk1激酶抑制剂及其制备方法和应用
EP4724150A1 (en) 2023-06-08 2026-04-15 Antares Therapeutics, Inc. A 1,5-dihydro-4h-pyrrolo[3,2-c] pyridin-4-one for use in the treatment of cancer
WO2024254298A1 (en) * 2023-06-08 2024-12-12 Scorpion Therapeutics, Inc. A 1,5-dihydro-4h-pyrrolo[3,2-c] pyridin-4-one for use in the treatment of cancer
CN119528906B (zh) * 2023-08-30 2026-06-12 中国科学院上海药物研究所 氮杂螺环类化合物及其制备方法、药物组合物和应用
EP4534085A1 (en) * 2023-10-03 2025-04-09 Scorpion Therapeutics, Inc. Compounds for use in methods of treating cancer
WO2025251058A1 (en) * 2024-05-31 2025-12-04 Celyn Therapeutics, Inc. Egfr inhibitors in cancer treatment

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6906194B2 (en) 2003-10-08 2005-06-14 Massachusetts Instititue Of Technology Fluorescence assay for kinase activity
US7964729B2 (en) 2006-08-28 2011-06-21 Massachusetts Institute Of Technology Sox-based kinase sensor
EP3045457B1 (en) * 2009-06-15 2018-05-09 Nerviano Medical Sciences S.r.l. Substituted pyrimidinylpyrrolopyridinone derivatives, process for their preparation and their use as kinase inhibitors
JP5825932B2 (ja) 2011-08-26 2015-12-02 キヤノン株式会社 撮像装置及びその制御方法、プログラム、及び記録媒体
CN104125957B (zh) 2011-12-21 2016-05-25 拜耳知识产权有限责任公司 取代的苄基吡唑
EP2847180B1 (en) 2012-05-11 2017-01-04 Bayer Pharma Aktiengesellschaft Substituted cycloalkenopyrazoles as bub1 inhibitors for the treatment of cancer
US20160046604A1 (en) 2013-03-21 2016-02-18 Bayer Pharma Aktiengesellschaft Heteroaryl substituted indazoles
EP2976336A1 (en) 2013-03-21 2016-01-27 Bayer Pharma Aktiengesellschaft 3-heteroaryl substituted indazoles
WO2014202590A1 (en) 2013-06-21 2014-12-24 Bayer Pharma Aktiengesellschaft Substituted benzylpyrazoles
WO2014202583A1 (en) 2013-06-21 2014-12-24 Bayer Pharma Aktiengesellschaft Substituted benzylpyrazoles
US9745285B2 (en) 2013-06-21 2017-08-29 Bayer Pharma Aktiengesellschaft Heteroaryl substituted pyrazoles
EP3010911A1 (en) 2013-06-21 2016-04-27 Bayer Pharma Aktiengesellschaft Heteroaryl substituted pyrazoles
CN105764893A (zh) 2013-10-30 2016-07-13 拜耳制药股份公司 杂芳基取代的吡唑
US20170166598A1 (en) 2014-05-13 2017-06-15 Ariad Pharmaceuticals, Inc. Heteroaryl compounds for kinase inhibition
TW201613886A (en) 2014-06-17 2016-04-16 Bayer Pharma AG 3-amino-1,5,6,7-tetrahydro-4h-indol-4-ones
CN107406417B (zh) * 2015-01-28 2020-06-09 拜耳制药股份公司 4H-吡咯并[3,2-c]吡啶-4-酮衍生物
CN107922389A (zh) 2015-06-17 2018-04-17 拜耳制药股份公司 3‑氨基‑1,5,6,7‑四氢‑4h‑吲哚‑4‑酮
US10308629B2 (en) 2015-08-05 2019-06-04 Bayer Pharma Aktiengesellschaft 1H-pyrrol-3-amines
KR102075886B1 (ko) 2015-09-01 2020-02-11 다이호야쿠힌고교 가부시키가이샤 신규한 피라졸로[3,4-d]피리미딘 화합물 또는 그 염
WO2019081486A1 (en) * 2017-10-24 2019-05-02 Bayer Aktiengesellschaft 4h-pyrrolo[3,2-c]pyridin-4-one derivatives
AU2019223168B2 (en) 2018-02-23 2024-09-12 The Regents Of The University Of Michigan EGFR dimer disruptors and use of the same
JP2021527088A (ja) 2018-06-14 2021-10-11 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド Ｈｅｒ２阻害剤としてのシアノキノリンアミド化合物及び使用方法
US12161649B2 (en) 2018-06-21 2024-12-10 Dana-Farber Cancer Institute, Inc. Inhibitors of EGFR and methods of use thereof
EP3921317B1 (en) * 2019-02-07 2023-08-02 Bayer Aktiengesellschaft 3-amino-2-[2-(acylamino)pyridin-4-yl]-1,5,6,7-tetrahydro-4h-pyrrolo[3,2-c]pyridin-4-one as csnk1 inhibitors

Also Published As

Publication number Publication date
MX2023004085A (es) 2023-06-29
JP2023548657A (ja) 2023-11-20
AU2021358596A9 (en) 2024-10-24
PH12023500010A1 (en) 2024-03-11
KR20230107419A (ko) 2023-07-14
WO2022076831A3 (en) 2022-07-07
EP4225445A2 (en) 2023-08-16
CL2025004052A1 (es) 2026-03-20
TW202227063A (zh) 2022-07-16
CA3198202A1 (en) 2022-04-14
WO2022076831A2 (en) 2022-04-14
US20240101576A1 (en) 2024-03-28
IL301929A (en) 2023-06-01
BR112023006531A2 (pt) 2023-10-03
CL2023001012A1 (es) 2023-12-22

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