AU2022370021B2 - Crbn e3 ligase ligand compound, protein degrading agent developed on the basis of ligand compound, and their applications - Google Patents

Crbn e3 ligase ligand compound, protein degrading agent developed on the basis of ligand compound, and their applications

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Publication number
AU2022370021B2
AU2022370021B2 AU2022370021A AU2022370021A AU2022370021B2 AU 2022370021 B2 AU2022370021 B2 AU 2022370021B2 AU 2022370021 A AU2022370021 A AU 2022370021A AU 2022370021 A AU2022370021 A AU 2022370021A AU 2022370021 B2 AU2022370021 B2 AU 2022370021B2
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dione
diazabicyclo
dioxopiperidin
heptan
octan
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AU2022370021A1 (en
Inventor
Renhong SUN
Xiaobao Yang
Baoyin ZHAO
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Gluetacs Therapeutics Shanghai Co Ltd
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Gluetacs Therapeutics Shanghai Co Ltd
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • 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
    • A61K31/4995—Pyrazines or piperazines forming part of bridged ring systems
    • 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
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • 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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    • 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
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    • 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
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    • 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
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    • C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
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    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings

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  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
AU2022370021A 2021-10-22 2022-10-20 Crbn e3 ligase ligand compound, protein degrading agent developed on the basis of ligand compound, and their applications Active AU2022370021B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN202111231963 2021-10-22
CN202111231963.9 2021-10-22
PCT/CN2022/126516 WO2023066350A1 (zh) 2021-10-22 2022-10-20 Crbn e3连接酶配体化合物、基于该配体化合物开发的蛋白降解剂及它们的应用

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AU2022370021A1 AU2022370021A1 (en) 2024-05-09
AU2022370021B2 true AU2022370021B2 (en) 2026-04-16

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US (1) US20250243210A1 (https=)
EP (1) EP4421071A4 (https=)
JP (1) JP2024539269A (https=)
KR (1) KR20240110576A (https=)
CN (1) CN116003418A (https=)
AU (1) AU2022370021B2 (https=)
CA (1) CA3235512A1 (https=)
WO (1) WO2023066350A1 (https=)

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JP7805983B2 (ja) 2022-03-22 2026-01-26 アッヴィ・インコーポレイテッド ブルトン型チロシンキナーゼを分解するためのピリミジン
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TW202425989A (zh) * 2022-10-20 2024-07-01 大陸商西藏海思科製藥有限公司 膦醯衍生物的製備方法
WO2024173646A1 (en) * 2023-02-16 2024-08-22 Innovo Therapeutics, Inc. Cyclin-dependent kinase degrading compounds
WO2024240858A1 (en) 2023-05-23 2024-11-28 Valerio Therapeutics Protac molecules directed against dna damage repair system and uses thereof
EP4722207A1 (en) * 2023-06-01 2026-04-08 Gluetacs Therapeutics (Shanghai) Co., Ltd. Oxoisoindolinyl-substituted tetrahydropyrimidinedione derivative and use thereof
CN117126133A (zh) * 2023-08-14 2023-11-28 中国海洋大学 一种化合物及其用途
CN121773112A (zh) 2023-08-17 2026-03-31 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
TW202532055A (zh) * 2023-11-22 2025-08-16 大陸商廣東東陽光藥業股份有限公司 靶向降解雄激素受體的雙功能嵌合體的雜環化合物及其用途
CN117756818B (zh) * 2023-12-12 2025-04-29 北京医院 一种戊二酰亚胺类化合物及其制备方法和应用
CN120548310A (zh) * 2023-12-26 2025-08-26 标新生物医药科技(上海)有限公司 具有双氮杂环取代的异吲哚啉酮骨架的化合物及其应用
CN120787219A (zh) * 2024-02-04 2025-10-14 标新生物医药科技(上海)有限公司 具有取代的戊二酰亚胺基异吲哚啉酮新颖骨架的化合物及其应用
CN120787222A (zh) * 2024-02-04 2025-10-14 标新生物医药科技(上海)有限公司 基于取代的异吲哚啉酮新颖骨架化合物、含有其的双功能蛋白降解剂及它们的应用
WO2025212165A1 (en) * 2024-04-05 2025-10-09 Board Of Regents Of The University Of Nebraska Targeted heterobifunctional small molecule proteolysis targeting chimeras
WO2026061104A1 (zh) * 2024-07-05 2026-03-26 甘李药业股份有限公司 用于雄激素受体靶向降解的化合物和方法
CN118955474A (zh) * 2024-07-29 2024-11-15 浙江爱索拓标记医药科技有限公司 一种放射性同位素碳-14标记的巴德卡鲁胺及其制备方法和应用
CN120004863A (zh) * 2025-02-27 2025-05-16 江苏天士力帝益药业有限公司 一种alk蛋白降解剂及其在抗肿瘤中的应用

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