CN118019741A - 作为smarca降解剂的新型四氢喹啉和包含它们的蛋白水解靶向嵌合体（protac） - Google Patents

作为smarca降解剂的新型四氢喹啉和包含它们的蛋白水解靶向嵌合体（protac） Download PDF

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Publication number
CN118019741A
CN118019741A CN202280065436.1A CN202280065436A CN118019741A CN 118019741 A CN118019741 A CN 118019741A CN 202280065436 A CN202280065436 A CN 202280065436A CN 118019741 A CN118019741 A CN 118019741A
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alkyl
compound
formula
salt
group
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CN202280065436.1A
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English (en)
Chinese (zh)
Inventor
A·西尤利
E·迪尔斯
W·法纳比
P·格莱布
C·科芬克
S·施特尔
N·特雷纳
H·魏因斯塔布尔
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Boehringer Ingelheim International GmbH
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Boehringer Ingelheim International GmbH
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Publication of CN118019741A publication Critical patent/CN118019741A/zh
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    • 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
    • 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
    • C07D471/14—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
    • 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
    • C07D487/12—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 three hetero rings
    • C07D487/14—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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (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)
  • Medicinal Preparation (AREA)
CN202280065436.1A 2021-09-29 2022-09-27 作为smarca降解剂的新型四氢喹啉和包含它们的蛋白水解靶向嵌合体（protac） Pending CN118019741A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP21199982.6 2021-09-29
EP21199982 2021-09-29
PCT/EP2022/076850 WO2023052363A1 (en) 2021-09-29 2022-09-27 Novel tetrahydroquinolines and proteolysis targeting chimera (protacs) comprising them as degraders of smarca

Publications (1)

Publication Number Publication Date
CN118019741A true CN118019741A (zh) 2024-05-10

Family

ID=78211839

Family Applications (1)

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CN202280065436.1A Pending CN118019741A (zh) 2021-09-29 2022-09-27 作为smarca降解剂的新型四氢喹啉和包含它们的蛋白水解靶向嵌合体（protac）

Country Status (5)

Country Link
US (1) US20250049929A1 (enExample)
EP (1) EP4408846A1 (enExample)
JP (1) JP2024537784A (enExample)
CN (1) CN118019741A (enExample)
WO (1) WO2023052363A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN119330886A (zh) * 2024-09-03 2025-01-21 常州大学 一种苯并咪唑胺类衍生物及其制备方法和作为β2-肾上腺素受体别构拮抗剂的应用

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW202409036A (zh) * 2022-05-17 2024-03-01 美商858療法股份有限公司 Parg抑制劑
CN119403803A (zh) 2022-05-17 2025-02-07 858治疗公司 Parg抑制剂
EP4695250A1 (en) 2023-04-12 2026-02-18 Aurigene Oncology Limited Tetracyclic compounds as smarca2 and/or smarca4 degraders
WO2025106482A1 (en) * 2023-11-13 2025-05-22 Oncopia Therapeutics, Inc. D/B/A Sk Life Science Labs Compounds and compositions as smarca2/4 degraders and uses thereof
AR134429A1 (es) * 2023-11-22 2026-01-14 858 Therapeutics Inc Inhibidores de parg

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MA41598A (fr) 2015-02-25 2018-01-02 Constellation Pharmaceuticals Inc Composés thérapeutiques de pyridazine et leurs utilisations
CN112996800B (zh) 2018-10-16 2024-06-25 勃林格殷格翰国际有限公司 作为smarca2和/或smarca4的降解剂的新型蛋白水解靶向嵌合体（protac）及其衍生物
KR20210097733A (ko) * 2018-11-30 2021-08-09 메르크 파텐트 게엠베하 전자 디바이스용 화합물
WO2020251969A1 (en) * 2019-06-10 2020-12-17 Kymera Therapeutics, Inc. Smarca degraders and uses thereof

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN119330886A (zh) * 2024-09-03 2025-01-21 常州大学 一种苯并咪唑胺类衍生物及其制备方法和作为β2-肾上腺素受体别构拮抗剂的应用

Also Published As

Publication number Publication date
JP2024537784A (ja) 2024-10-16
WO2023052363A1 (en) 2023-04-06
US20250049929A1 (en) 2025-02-13
EP4408846A1 (en) 2024-08-07

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