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

Info

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
Authority
CN
China
Prior art keywords
compound
mmol
pharmaceutically acceptable
formula
acceptable salt
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.)
Pending
Application number
CN202180065971.2A
Other languages
English (en)
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
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.)
AstraZeneca AB
Original Assignee
AstraZeneca AB
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 AstraZeneca AB filed Critical AstraZeneca AB
Publication of CN116249554A publication Critical patent/CN116249554A/zh
Pending legal-status Critical Current

Links

Classifications

    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (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

Publications (1)

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

Family

ID=78085628

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202180065971.2A Pending CN116249554A (zh) 2020-09-30 2021-09-29 化合物以及它们在治疗癌症中的用途

Country Status (17)

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

Cited By (2)

* 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
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

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN119301111A (zh) 2022-03-24 2025-01-10 葛兰素史密斯克莱知识产权发展有限公司 作为protac中的降解决定子的2,4-二氧代四氢嘧啶基衍生物
USD1018676S1 (en) * 2022-04-15 2024-03-19 Puttshack LTD Miniature golf hole
USD1018746S1 (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
USD1018747S1 (en) * 2022-04-15 2024-03-19 Puttshack LTD Miniature golf hole
CN119855812A (zh) * 2022-09-14 2025-04-18 海南先声再明医药股份有限公司 多并环类化合物及其用途
US20240374588A1 (en) 2023-04-07 2024-11-14 Astrazeneca Ab Irak4 protacs
TW202515566A (zh) 2023-06-14 2025-04-16 瑞典商阿斯特捷利康公司 Ｓｍａｒｃａ２降解劑及其用途
MX2025015084A (es) * 2023-06-14 2026-02-03 Astrazeneca Ab Degradadores de smarca2 y usos de estos
WO2025036489A1 (zh) * 2023-08-17 2025-02-20 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
IL326555A (en) 2023-09-22 2026-04-01 Glaxosmithkline Ip Dev Ltd Androgen receptor protax
US20250177539A1 (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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0422263D0 (en) 2004-10-07 2004-11-10 Glaxo Group Ltd Novel compounds
PH12012502079A1 (en) 2010-04-16 2013-02-11 Ac Immune Sa Novel compounds for the treatment of diseases associated with amyloid or amyloid-like proteins
JP6509838B2 (ja) 2013-06-26 2019-05-08 アッヴィ・インコーポレイテッド Ｂｔｋ阻害薬としての一級カルボキサミド類
ES2826443T3 (es) 2014-09-25 2021-05-18 Araxes Pharma Llc Inhibidores de proteínas mutantes KRAS G12C
JP6815318B2 (ja) * 2014-12-23 2021-01-20 ダナ−ファーバー キャンサー インスティテュート，インコーポレイテッド 二官能性分子によって標的化タンパク質分解を誘導する方法
WO2019140387A1 (en) * 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Crbn ligands and uses thereof
CN120698983A (zh) * 2018-12-20 2025-09-26 C4医药公司 靶向蛋白降解

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Also Published As

Publication number Publication date
WO2022069520A1 (en) 2022-04-07
JP2023543299A (ja) 2023-10-13
US20230374007A1 (en) 2023-11-23
CL2023000881A1 (es) 2023-11-17
AU2021353968A9 (en) 2024-10-03
AU2025200137A1 (en) 2025-01-30
EP4221756A1 (en) 2023-08-09
AU2021353968A1 (en) 2023-06-08
MX2023003564A (es) 2023-04-04
CO2023005188A2 (es) 2023-05-19
AU2021353968B2 (en) 2024-10-10
KR20230079408A (ko) 2023-06-07
PE20230782A1 (es) 2023-05-09
DOP2023000062A (es) 2023-05-31
ECSP23030959A (es) 2023-05-31
CR20230185A (es) 2023-06-27
CA3195695A1 (en) 2022-04-07
BR112023005708A2 (pt) 2023-05-02
IL301626A (en) 2023-05-01

Similar Documents

Publication Publication Date Title
CN116249554A (zh) 化合物以及它们在治疗癌症中的用途
JP7687970B2 (ja) Ｉｒａｋ分解剤およびその使用
JP6352571B1 (ja) キナーゼ阻害剤としての複素環式アミド
CN107660205B (zh) 作为lsd1抑制剂的杂环化合物
CN116867758A (zh) Irak降解剂和其用途
CN118561952A (zh) Ras抑制剂
KR102496364B1 (ko) Ｓｍｙｄ 억제제
ES2494718T3 (es) Derivados de tetrahidro-pirido-pirimidina
CN119798279A (zh) Ras抑制剂
AU2014304046B2 (en) Benzimidazolyl-methyl urea derivatives as ALX receptor agonists
ES2956090T3 (es) Inhibidores de bencimidazol de enzimas PAD
JP2023518423A (ja) Ｍｄｍ２分解剤およびそれらの使用
CN121889399A (zh) Kras蛋白水解靶向嵌合体
EA038143B1 (ru) ИНГИБИТОРЫ Mcl-1 НА ОСНОВЕ ЗАМЕЩЕННЫХ ИНДОЛОВ
WO2009124166A1 (en) Hydroxymethyl pyrrolidines as beta 3 adrenergic receptor agonists
JP2017510564A (ja) 新規なヘテロ芳香族誘導体およびそれらの医薬としての使用
US8648074B2 (en) Substituted octahydropyrrolo[1,2-a]pyrazine sulfonamides as calcium channel blockers
WO2009119776A1 (ja) 縮合複素環誘導体およびその用途
CA3236550A1 (en) Spirotricycle ripk1 inhibitors and methods of uses thereof
IL325136A (en) Pyrazolo-pyrimidinone compounds for use in methods for inhibiting kinase week1 a
KR20220052934A (ko) 치환 1,3-페닐 헤테로아릴 유도체 및 질환 치료에서의 이의 용도

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination