CN116249554A - 化合物以及它们在治疗癌症中的用途 - Google Patents

化合物以及它们在治疗癌症中的用途 Download PDF

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Publication number
CN116249554A
CN116249554A CN202180065971.2A CN202180065971A CN116249554A CN 116249554 A CN116249554 A CN 116249554A CN 202180065971 A CN202180065971 A CN 202180065971A CN 116249554 A CN116249554 A CN 116249554A
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compound
mmol
pharmaceutically acceptable
formula
acceptable salt
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Chinese (zh)
Inventor
U·布杰森
M·W·D·佩里
C·格雷布纳
I·N·迈克尔德斯
T·G·C·海豪
J·G·凯特尔
G·W·柯利
R·I·斯托勒
S·K·巴加尔
C·法伦
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AstraZeneca AB
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AstraZeneca AB
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Publication of CN116249554A publication Critical patent/CN116249554A/zh
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    • 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
    • C07D495/12—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 three hetero rings
    • C07D495/14—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal 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
    • A61K47/51—Medicinal 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
    • A61K47/54—Medicinal 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
    • A61K47/55—Medicinal 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal 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
    • A61K47/51—Medicinal 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
    • A61K47/54—Medicinal 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
    • A61K47/555—Medicinal 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
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic 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
    • 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/04—Heterocyclic 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
    • 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
    • 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
    • C07D491/02—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 two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic 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
    • C07D498/04—Ortho-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)
CN202180065971.2A 2020-09-30 2021-09-29 化合物以及它们在治疗癌症中的用途 Pending CN116249554A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202063085384P 2020-09-30 2020-09-30
US63/085384 2020-09-30
PCT/EP2021/076752 WO2022069520A1 (en) 2020-09-30 2021-09-29 Compounds and their use in treating cancer

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Publication Number Publication Date
CN116249554A true CN116249554A (zh) 2023-06-09

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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)

Cited By (2)

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CN115141179A (zh) * 2021-03-31 2022-10-04 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
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

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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
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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CN111344293A (zh) * 2017-09-20 2020-06-26 阿斯利康(瑞典)有限公司 1，3-二氢咪唑并[4，5-c]噌啉-2-酮化合物及其在治疗癌症中的用途

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WO2018144649A1 (en) * 2017-01-31 2018-08-09 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
CN111344293A (zh) * 2017-09-20 2020-06-26 阿斯利康(瑞典)有限公司 1，3-二氢咪唑并[4，5-c]噌啉-2-酮化合物及其在治疗癌症中的用途

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115141179A (zh) * 2021-03-31 2022-10-04 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
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
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

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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
KR20230079408A (ko) 2023-06-07
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
EP4221756A1 (en) 2023-08-09

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