KR20230079408A - 화합물 및 암의 치료에서의 이의 용도 - Google Patents

화합물 및 암의 치료에서의 이의 용도 Download PDF

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Publication number
KR20230079408A
KR20230079408A KR1020237014514A KR20237014514A KR20230079408A KR 20230079408 A KR20230079408 A KR 20230079408A KR 1020237014514 A KR1020237014514 A KR 1020237014514A KR 20237014514 A KR20237014514 A KR 20237014514A KR 20230079408 A KR20230079408 A KR 20230079408A
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South Korea
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formula
compound
pharmaceutically acceptable
acceptable salt
mmol
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Korean (ko)
Inventor
울프 뵈르예쏜
매튜 윌리엄 댐피어 페리
크리스토프 그레브너
이아코보스 닐 미카엘리데스
토마스 조지 크리스토퍼 헤이하우
제이슨 그랜트 케틀
개빈 윌리엄 콜리
로버트 이언 스토러
샤란지트 카우르 바갈
샤를린 팰런
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아스트라제네카 아베
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Publication of KR20230079408A publication Critical patent/KR20230079408A/ko
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12Heterocyclic 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 three hetero rings
    • C07D495/14Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/555Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound pre-targeting systems involving an organic compound, other than a peptide, protein or antibody, for targeting specific cells
    • 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • 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
    • C07D403/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D413/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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 two hetero rings
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Molecular Biology (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)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicinal Preparation (AREA)
KR1020237014514A 2020-09-30 2021-09-29 화합물 및 암의 치료에서의 이의 용도 Pending KR20230079408A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202063085384P 2020-09-30 2020-09-30
US63/085,384 2020-09-30
PCT/EP2021/076752 WO2022069520A1 (en) 2020-09-30 2021-09-29 Compounds and their use in treating cancer

Publications (1)

Publication Number Publication Date
KR20230079408A true KR20230079408A (ko) 2023-06-07

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Country Link
US (1) US20230374007A1 (enExample)
EP (1) EP4221756A1 (enExample)
JP (1) JP2023543299A (enExample)
KR (1) KR20230079408A (enExample)
CN (1) CN116249554A (enExample)
AU (2) AU2021353968B2 (enExample)
BR (1) BR112023005708A2 (enExample)
CA (1) CA3195695A1 (enExample)
CL (1) CL2023000881A1 (enExample)
CO (1) CO2023005188A2 (enExample)
CR (1) CR20230185A (enExample)
DO (1) DOP2023000062A (enExample)
EC (1) ECSP23030959A (enExample)
IL (1) IL301626A (enExample)
MX (1) MX2023003564A (enExample)
PE (1) PE20230782A1 (enExample)
WO (1) WO2022069520A1 (enExample)

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CN115141179B (zh) * 2021-03-31 2024-09-13 江苏恒瑞医药股份有限公司 一种新型苯并杂环基类衍生物、其制备方法及其在医药上的应用
US20250205344A1 (en) 2022-03-24 2025-06-26 Glaxosmithkline Intellectual Property Development Limited 2,4-dioxotetrahydropyrimidinyl deratives as degrons in protacs
USD1018747S1 (en) * 2022-04-15 2024-03-19 Puttshack LTD Miniature golf hole
USD1020957S1 (en) * 2022-04-15 2024-04-02 Puttshack LTD Miniature golf hole
USD1018746S1 (en) * 2022-04-15 2024-03-19 Puttshack LTD Miniature golf hole
USD1018676S1 (en) * 2022-04-15 2024-03-19 Puttshack LTD Miniature golf hole
US20260098043A1 (en) * 2022-09-14 2026-04-09 Hainan Simcere Zaiming Pharmeceutical Co., Ltd. Polycyclic compound and use thereof
TW202508568A (zh) 2023-04-07 2025-03-01 瑞典商阿斯特捷利康公司 Irak4蛋白水解靶向嵌合體
PE20260301A1 (es) 2023-06-14 2026-02-10 Astrazeneca Ab Derivados de 3-[3-amino-6-(2-hidroxifenil)piridazin-4-il]-3,8-diazabiciclo[3.2.1]octano como protacs degradantes de smarca2 para el tratamiento del cancer
PE20260307A1 (es) * 2023-06-14 2026-02-11 Astrazeneca Ab Degradadores de smarca2 y usos de estos
CN121773112A (zh) * 2023-08-17 2026-03-31 海思科医药集团股份有限公司 一种氰基芳香环衍生物及其在医药上的应用
TW202530192A (zh) 2023-09-22 2025-08-01 英商葛蘭素史密斯克藍智慧財產發展有限公司 新穎化合物
CN117430605A (zh) * 2023-10-26 2024-01-23 广西天铭药业有限公司 一种kras g12c抑制剂amg-510中间体的合成方法
WO2025114875A1 (en) * 2023-12-01 2025-06-05 Astrazeneca Ab Er degraders and uses thereof
WO2025125575A1 (en) 2023-12-14 2025-06-19 Astrazeneca Ab Irak4 protacs

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GB0422263D0 (en) 2004-10-07 2004-11-10 Glaxo Group Ltd Novel compounds
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JP2017528498A (ja) 2014-09-25 2017-09-28 アラクセス ファーマ エルエルシー Kras g12c変異体タンパク質のインヒビター
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CN120698983A (zh) * 2018-12-20 2025-09-26 C4医药公司 靶向蛋白降解

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AU2021353968B2 (en) 2024-10-10
BR112023005708A2 (pt) 2023-05-02
WO2022069520A1 (en) 2022-04-07
AU2025200137A1 (en) 2025-01-30
MX2023003564A (es) 2023-04-04
DOP2023000062A (es) 2023-05-31
AU2021353968A1 (en) 2023-06-08
CR20230185A (es) 2023-06-27
AU2021353968A9 (en) 2024-10-03
ECSP23030959A (es) 2023-05-31
CO2023005188A2 (es) 2023-05-19
CA3195695A1 (en) 2022-04-07
CL2023000881A1 (es) 2023-11-17
US20230374007A1 (en) 2023-11-23
PE20230782A1 (es) 2023-05-09
IL301626A (en) 2023-05-01
JP2023543299A (ja) 2023-10-13
CN116249554A (zh) 2023-06-09
EP4221756A1 (en) 2023-08-09

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