JP7471232B2 - Polybromo-1(pbrm1)の小分子分解剤 - Google Patents

Polybromo-1(pbrm1)の小分子分解剤 Download PDF

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JP7471232B2
JP7471232B2 JP2020560316A JP2020560316A JP7471232B2 JP 7471232 B2 JP7471232 B2 JP 7471232B2 JP 2020560316 A JP2020560316 A JP 2020560316A JP 2020560316 A JP2020560316 A JP 2020560316A JP 7471232 B2 JP7471232 B2 JP 7471232B2
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cancer
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JP2021522276A (ja
JP2021522276A5 (enExample
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エリック フィッシャー,
ナサナエル エス. グレイ,
ラドスロー ノワク,
キャサリン ドノヴァン,
ティンフー チャン,
ヤオ リウ,
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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
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    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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)
  • Medicinal Preparation (AREA)
JP2020560316A 2018-04-30 2019-04-30 Polybromo-1(pbrm1)の小分子分解剤 Active JP7471232B2 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2024004034A JP7838004B2 (ja) 2018-04-30 2024-01-15 Polybromo-1(pbrm1)の小分子分解剤

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862664592P 2018-04-30 2018-04-30
US62/664,592 2018-04-30
PCT/US2019/029778 WO2019213005A1 (en) 2018-04-30 2019-04-30 Small molecule degraders of polybromo-1 (pbrm1)

Related Child Applications (1)

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JP2024004034A Division JP7838004B2 (ja) 2018-04-30 2024-01-15 Polybromo-1(pbrm1)の小分子分解剤

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JP2021522276A JP2021522276A (ja) 2021-08-30
JP2021522276A5 JP2021522276A5 (enExample) 2022-05-09
JP7471232B2 true JP7471232B2 (ja) 2024-04-19

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JP2020560316A Active JP7471232B2 (ja) 2018-04-30 2019-04-30 Polybromo-1(pbrm1)の小分子分解剤
JP2024004034A Active JP7838004B2 (ja) 2018-04-30 2024-01-15 Polybromo-1(pbrm1)の小分子分解剤

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US (1) US11771697B2 (enExample)
EP (1) EP3787747A4 (enExample)
JP (2) JP7471232B2 (enExample)
AU (1) AU2019261938B2 (enExample)
CA (1) CA3093405C (enExample)
WO (1) WO2019213005A1 (enExample)

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EP4717317A3 (en) 2017-06-20 2026-06-03 C4 Therapeutics, Inc. N/o-linked degrons and degronimers for protein degradation
EP3710002A4 (en) 2017-11-16 2021-07-07 C4 Therapeutics, Inc. DEGRADER AND DEGRONE FOR TARGETED PROTEIN DEGRADATION
EP3737666A4 (en) 2018-01-12 2022-01-05 Kymera Therapeutics, Inc. PROTEIN DEGRADATION AGENTS AND ASSOCIATED USES
CN111902141A (zh) 2018-03-26 2020-11-06 C4医药公司 用于ikaros降解的羟脑苷脂结合剂
WO2019204354A1 (en) 2018-04-16 2019-10-24 C4 Therapeutics, Inc. Spirocyclic compounds
SG11202104495YA (en) * 2018-04-26 2021-05-28 Aurigene Discovery Tech Ltd Pyridazine derivatives as smarca2/4 degraders
US12454520B2 (en) 2018-07-06 2025-10-28 Kymera Therapeutics, Inc. Protein degraders and uses thereof
CA3121667A1 (en) * 2018-09-30 2020-04-02 Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences Isoindoline compound, preparation method, pharmaceutical composition and use thereof
EP3897631A4 (en) 2018-12-20 2022-11-23 C4 Therapeutics, Inc. TARGETED PROTEIN BREAKDOWN
WO2020251972A1 (en) 2019-06-10 2020-12-17 Kymera Therapeutics, Inc. Smarca degraders and uses thereof
US12624044B2 (en) 2019-06-10 2026-05-12 Kymera Therapeutics, Inc. SMARCA degraders and uses thereof
EP4054724A4 (en) * 2019-10-28 2023-12-27 C4 Therapeutics, Inc. BIFUNCTIONAL CONNECTIONS
CN114728936A (zh) * 2019-10-29 2022-07-08 豪夫迈·罗氏有限公司 用于治疗癌症的双功能化合物
WO2021133917A1 (en) 2019-12-23 2021-07-01 Kymera Therapeutics, Inc. Smarca inhibitors and uses thereof
US11679109B2 (en) 2019-12-23 2023-06-20 Kymera Therapeutics, Inc. SMARCA degraders and uses thereof
CA3167166A1 (en) * 2020-01-10 2021-07-15 Amgen Inc. Smarca2-vhl degraders
EP4192504A4 (en) * 2020-08-07 2025-04-16 Cornell University THERAPEUTIC HARDENING PRO-COMPOUNDS FOR THE TARGETED DEGRADATION OF BET-DOMAIN PROTEINS AND METHODS FOR THEIR PRODUCTION AND USE
WO2022099117A1 (en) * 2020-11-06 2022-05-12 Prelude Therapeutics Incorporated Brm targeting compounds and associated methods of use
US12552775B2 (en) * 2020-11-20 2026-02-17 Foghorn Therapeutics Inc. Compounds and uses thereof
US20240024488A1 (en) * 2020-11-20 2024-01-25 Foghorn Therapeutics Inc. Compounds and uses thereof
US12606568B2 (en) 2020-12-09 2026-04-21 Kymera Therapeutics, Inc. SMARCA degraders and uses thereof
MX2023012981A (es) * 2021-05-03 2024-01-11 Nurix Therapeutics Inc Compuestos para inhibir o degradar proteinas objetivo, composiciones que los comprenden, metodos para su preparacion y metodos para usarlos.
JP2024533990A (ja) 2021-08-09 2024-09-18 ジェネンテック, インコーポレイテッド Brmの調節に使用するためのフェノール誘導体
IL316803A (en) 2022-06-06 2025-01-01 C4 Therapeutics Inc Bicyclic glutarimide-modified cervalon-binding agents
PE20260307A1 (es) 2023-06-14 2026-02-11 Astrazeneca Ab Degradadores de smarca2 y usos de estos
IL325247A (en) 2023-06-14 2026-02-01 Astrazeneca Ab History of 3-[3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl]-8,3-diazabicyclo[3.2.1]octane as a protacs from SMARCA2 joints for cancer treatment
WO2025106472A1 (en) * 2023-11-13 2025-05-22 Regents Of The University Of Michigan Compounds and compositions as smarca2/4 degraders and uses thereof
CN122070278A (zh) * 2024-09-19 2026-05-19 标新生物医药科技(上海)有限公司 含有芳基取代杂芳基的双功能蛋白降解剂及其应用
WO2026120044A1 (en) 2024-12-04 2026-06-11 Astrazeneca Ab Smarca2 degraders and uses thereof

Citations (3)

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JP2018510851A (ja) 2015-02-25 2018-04-19 ジェネンテック, インコーポレイテッド 治療用ピリダジン化合物およびその使用
JP2021520350A (ja) 2018-04-01 2021-08-19 アルビナス・オペレーションズ・インコーポレイテッドArvinas Operations, Inc. Brm標的化化合物および関連使用方法
JP2021520372A (ja) 2018-04-26 2021-08-19 オーリジーン ディスカバリー テクノロジーズ リミテッドAurigene Discovery Technologies Limited Smarca2/4分解剤としてのピリダジン誘導体

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US9694084B2 (en) 2014-12-23 2017-07-04 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
EP3337476A4 (en) * 2015-08-19 2019-09-04 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
AU2017246452C1 (en) * 2016-04-06 2021-06-03 The Regents Of The University Of Michigan MDM2 protein degraders
CN121974842A (zh) 2016-05-10 2026-05-05 C4医药公司 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体
ES2857743T3 (es) 2016-09-13 2021-09-29 Univ Michigan Regents 1,4-diazepinas fusionadas como degradadores de proteína BET
WO2019023149A1 (en) * 2017-07-24 2019-01-31 Salk Institute For Biological Studies USE OF BROMODOMAIN-CONTAINING PROTEIN-9 ANTAGONISTS IN ASSOCIATION WITH VITAMIN D RECEPTOR AGONISTS IN THE TREATMENT OF DIABETES

Patent Citations (3)

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JP2018510851A (ja) 2015-02-25 2018-04-19 ジェネンテック, インコーポレイテッド 治療用ピリダジン化合物およびその使用
JP2021520350A (ja) 2018-04-01 2021-08-19 アルビナス・オペレーションズ・インコーポレイテッドArvinas Operations, Inc. Brm標的化化合物および関連使用方法
JP2021520372A (ja) 2018-04-26 2021-08-19 オーリジーン ディスカバリー テクノロジーズ リミテッドAurigene Discovery Technologies Limited Smarca2/4分解剤としてのピリダジン誘導体

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US20210038599A1 (en) 2021-02-11
CA3093405C (en) 2025-06-17
EP3787747A4 (en) 2022-01-12
EP3787747A1 (en) 2021-03-10
US11771697B2 (en) 2023-10-03
JP2021522276A (ja) 2021-08-30
WO2019213005A1 (en) 2019-11-07
JP7838004B2 (ja) 2026-03-31
AU2019261938B2 (en) 2024-06-13
CA3093405A1 (en) 2019-11-07
AU2019261938A1 (en) 2020-09-24
JP2024041923A (ja) 2024-03-27

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