CN114007652A - 小分子靶向溴/乙酰蛋白及其用途 - Google Patents

小分子靶向溴/乙酰蛋白及其用途 Download PDF

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Publication number
CN114007652A
CN114007652A CN202080044388.9A CN202080044388A CN114007652A CN 114007652 A CN114007652 A CN 114007652A CN 202080044388 A CN202080044388 A CN 202080044388A CN 114007652 A CN114007652 A CN 114007652A
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China
Prior art keywords
pharmaceutically acceptable
optionally substituted
bispecific compound
stereoisomer
acceptable salt
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CN202080044388.9A
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English (en)
Chinese (zh)
Inventor
祁军
李德耀
维兰吉卡·K·威马拉森纳
保罗·帕克
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Dana Farber Cancer Institute Inc
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Dana Farber Cancer Institute Inc
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Publication of CN114007652A publication Critical patent/CN114007652A/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
    • A61K47/555—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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K47/545—Heterocyclic compounds
    • 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
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D417/14—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 three or more hetero rings
    • 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

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Saccharide Compounds (AREA)
CN202080044388.9A 2019-06-18 2020-06-17 小分子靶向溴/乙酰蛋白及其用途 Pending CN114007652A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962862879P 2019-06-18 2019-06-18
US62/862,879 2019-06-18
PCT/US2020/038130 WO2020257278A2 (en) 2019-06-18 2020-06-17 Small molecule target bromo/acetyl proteins and uses thereof

Publications (1)

Publication Number Publication Date
CN114007652A true CN114007652A (zh) 2022-02-01

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CN202080044388.9A Pending CN114007652A (zh) 2019-06-18 2020-06-17 小分子靶向溴/乙酰蛋白及其用途

Country Status (7)

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US (1) US12496348B2 (https=)
EP (1) EP3986470A4 (https=)
JP (1) JP7626721B2 (https=)
CN (1) CN114007652A (https=)
AU (1) AU2020295399B2 (https=)
CA (1) CA3143507A1 (https=)
WO (1) WO2020257278A2 (https=)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024152943A1 (zh) * 2023-01-17 2024-07-25 中国科学院广州生物医药与健康研究院 一种芳基咪唑基异恶唑类化合物及其制备方法和应用
WO2025242233A1 (zh) * 2024-05-24 2025-11-27 中国科学院广州生物医药与健康研究院 一种酰胺吲嗪类化合物及其制备方法和应用

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7712867B2 (ja) * 2018-11-02 2025-07-24 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 アセチル化ライター阻害剤の開発およびその使用
JP2024504932A (ja) 2021-01-13 2024-02-02 モンテ ローザ セラピューティクス， インコーポレイテッド イソインドリノン化合物
CN114989158A (zh) * 2021-03-02 2022-09-02 复旦大学 组蛋白乙酰转移酶p300溴结构域抑制剂及其药用组合物及其应用
CN117321053A (zh) * 2021-06-07 2023-12-29 贝达药业股份有限公司 P300抑制剂及其在医药上的应用
CN119707936B (zh) * 2025-02-25 2025-07-25 中南大学 一种2,4-二取代-5-氟嘧啶衍生物的盐的制备方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20160176916A1 (en) * 2014-12-23 2016-06-23 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
WO2018237026A1 (en) * 2017-06-20 2018-12-27 C4 Therapeutics, Inc. N / O-LINKED DEGRONS AND DEGRONIMERS FOR DEGRADATION OF PROTEINS
US20190076542A1 (en) * 2016-05-10 2019-03-14 C4 Theraprutics, Inc. C3-carbon linked glutarimide degronimers for target protein degradation

Family Cites Families (6)

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Publication number Priority date Publication date Assignee Title
MX2016004570A (es) 2013-10-11 2016-09-08 Genentech Inc Uso de inhibidores del bromodominio de cbp/ep300 para la inmunoterapia del cáncer.
WO2016055028A1 (en) 2014-10-10 2016-04-14 Genentech, Inc. Therapeutic compounds and uses thereof
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
GB201506658D0 (en) 2015-04-20 2015-06-03 Cellcentric Ltd Pharmaceutical compounds
MX2020003190A (es) 2017-09-22 2020-11-11 Kymera Therapeutics Inc Degradadores de proteinas y usos de los mismos.
JP7712867B2 (ja) * 2018-11-02 2025-07-24 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 アセチル化ライター阻害剤の開発およびその使用

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20160176916A1 (en) * 2014-12-23 2016-06-23 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
US20190076542A1 (en) * 2016-05-10 2019-03-14 C4 Theraprutics, Inc. C3-carbon linked glutarimide degronimers for target protein degradation
WO2018237026A1 (en) * 2017-06-20 2018-12-27 C4 Therapeutics, Inc. N / O-LINKED DEGRONS AND DEGRONIMERS FOR DEGRADATION OF PROTEINS

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024152943A1 (zh) * 2023-01-17 2024-07-25 中国科学院广州生物医药与健康研究院 一种芳基咪唑基异恶唑类化合物及其制备方法和应用
WO2025242233A1 (zh) * 2024-05-24 2025-11-27 中国科学院广州生物医药与健康研究院 一种酰胺吲嗪类化合物及其制备方法和应用

Also Published As

Publication number Publication date
JP2022537521A (ja) 2022-08-26
US12496348B2 (en) 2025-12-16
EP3986470A2 (en) 2022-04-27
WO2020257278A3 (en) 2021-01-28
CA3143507A1 (en) 2020-12-24
JP7626721B2 (ja) 2025-02-04
WO2020257278A2 (en) 2020-12-24
US20220241425A1 (en) 2022-08-04
AU2020295399A1 (en) 2021-12-02
AU2020295399B2 (en) 2025-10-16
EP3986470A4 (en) 2023-10-04

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