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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cell
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JP2021522276A5 (https=
JP2021522276A (ja
JPWO2019213005A5 (https=
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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)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • 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)

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

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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)

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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 (https=) 2022-05-09
JPWO2019213005A5 JPWO2019213005A5 (https=) 2022-05-09
JP7471232B2 true JP7471232B2 (ja) 2024-04-19

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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 (https=)
EP (1) EP3787747A4 (https=)
JP (2) JP7471232B2 (https=)
AU (1) AU2019261938B2 (https=)
CA (1) CA3093405C (https=)
WO (1) WO2019213005A1 (https=)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4717317A2 (en) 2017-06-20 2026-04-01 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
WO2019140380A1 (en) 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Protein degraders and uses thereof
JP2021519337A (ja) 2018-03-26 2021-08-10 シー４ セラピューティクス， インコーポレイテッド Ｉｋａｒｏｓの分解のためのセレブロン結合剤
CN119751456A (zh) 2018-04-16 2025-04-04 C4医药公司 螺环化合物
US12371426B2 (en) * 2018-04-26 2025-07-29 Aurigene Discovery Technologies Limited Pyridazine derivatives as SMARCA2/4 degraders
WO2020010227A1 (en) 2018-07-06 2020-01-09 Kymera Therapeutics, Inc. Protein degraders and uses thereof
KR102672549B1 (ko) * 2018-09-30 2024-06-10 상하이 인스티튜트 오브 마테리아 메디카 차이니즈 아카데미 오브 싸이언시즈 이소인돌린계 화합물, 이의 제조 방법, 약학 조성물 및 용도
CN120698983A (zh) 2018-12-20 2025-09-26 C4医药公司 靶向蛋白降解
WO2020251972A1 (en) 2019-06-10 2020-12-17 Kymera Therapeutics, Inc. Smarca degraders and uses thereof
JP2023511471A (ja) * 2019-10-28 2023-03-20 エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト 二官能性化合物
EP4051674A1 (en) * 2019-10-29 2022-09-07 F. Hoffmann-La Roche AG Bifunctional compounds for the treatment of cancer
WO2021133917A1 (en) 2019-12-23 2021-07-01 Kymera Therapeutics, Inc. Smarca inhibitors and uses thereof
BR112022012410A2 (pt) * 2019-12-23 2022-08-30 Kymera Therapeutics Inc Degradadores smarca e usos dos mesmos
AU2021205326A1 (en) * 2020-01-10 2022-07-21 Amgen Inc. SMARCA2-VHL degraders
US20240000950A1 (en) * 2020-08-07 2024-01-04 Cornell University Therapeutic cure-pro compounds for targeted degradation of bet domain proteins, and methods of making and using them
WO2022099117A1 (en) * 2020-11-06 2022-05-12 Prelude Therapeutics Incorporated Brm targeting compounds and associated methods of use
CA3199652A1 (en) * 2020-11-20 2022-05-27 Matthew Netherton Compounds and uses thereof
CA3196965A1 (en) * 2020-11-20 2022-05-27 Foghorn Therapeutics Inc. Compounds and uses thereof
EP4259144A4 (en) 2020-12-09 2025-08-20 Kymera Therapeutics Inc SMARCA DEGRADING AGENTS AND THEIR USES
CA3217892A1 (en) * 2021-05-03 2022-11-10 Joel Mcintosh Compounds for inhibiting or degrading target proteins, compositions, comprising the same, methods of their making, and methods of their use
US11993599B2 (en) 2021-08-09 2024-05-28 Genentech, Inc. Therapeutic compounds
JP2025523393A (ja) 2022-06-06 2025-07-23 シーフォー セラピューティクス， インコーポレイテッド 二環式置換グルタルイミドセレブロンバインダー
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
WO2025106472A1 (en) * 2023-11-13 2025-05-22 Regents Of The University Of Michigan Compounds and compositions as smarca2/4 degraders and uses thereof
WO2026061475A1 (zh) * 2024-09-19 2026-03-26 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

Citations (3)

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

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CN109790143A (zh) * 2016-05-10 2019-05-21 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
CA3036841A1 (en) * 2016-09-13 2018-03-22 The Regents Of The University Of Michigan Fused 1,4-diazepines as bet protein degraders
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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2019213005A1 (en) 2019-11-07
AU2019261938B2 (en) 2024-06-13
US11771697B2 (en) 2023-10-03
JP2021522276A (ja) 2021-08-30
EP3787747A1 (en) 2021-03-10
JP7838004B2 (ja) 2026-03-31
CA3093405A1 (en) 2019-11-07
JP2024041923A (ja) 2024-03-27
EP3787747A4 (en) 2022-01-12
AU2019261938A1 (en) 2020-09-24

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