CN116669722A - 白细胞介素-1受体相关激酶(irak)降解物及其用途 - Google Patents

白细胞介素-1受体相关激酶(irak)降解物及其用途 Download PDF

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Publication number
CN116669722A
CN116669722A CN202180090865.XA CN202180090865A CN116669722A CN 116669722 A CN116669722 A CN 116669722A CN 202180090865 A CN202180090865 A CN 202180090865A CN 116669722 A CN116669722 A CN 116669722A
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alkyl
ring
optionally substituted
nitrogen
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CN202180090865.XA
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English (en)
Chinese (zh)
Inventor
X·郑
朱潇
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Kemela Medical Co
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Kemela Medical Co
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    • 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
    • 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
    • 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
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • 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)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Liquid Crystal Substances (AREA)
  • Steroid Compounds (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
CN202180090865.XA 2020-12-09 2021-12-09 白细胞介素-1受体相关激酶(irak)降解物及其用途 Pending CN116669722A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202063123330P 2020-12-09 2020-12-09
US63/123,330 2020-12-09
PCT/US2021/062640 WO2022125790A1 (en) 2020-12-09 2021-12-09 Irak degraders and uses thereof

Publications (1)

Publication Number Publication Date
CN116669722A true CN116669722A (zh) 2023-08-29

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Family Applications (1)

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CN202180090865.XA Pending CN116669722A (zh) 2020-12-09 2021-12-09 白细胞介素-1受体相关激酶(irak)降解物及其用途

Country Status (13)

Country Link
US (2) US20230096599A1 (enExample)
EP (1) EP4259128A4 (enExample)
JP (1) JP7832945B2 (enExample)
KR (1) KR20230130179A (enExample)
CN (1) CN116669722A (enExample)
AR (1) AR124294A1 (enExample)
AU (1) AU2021396308A1 (enExample)
CA (1) CA3200608A1 (enExample)
CO (1) CO2023006818A2 (enExample)
IL (1) IL303458A (enExample)
MX (1) MX2023006719A (enExample)
TW (1) TW202237601A (enExample)
WO (1) WO2022125790A1 (enExample)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2025051160A1 (zh) * 2023-09-08 2025-03-13 北京华益健康药物研究中心 用于治疗或预防冠状病毒感染的3cl蛋白酶抑制剂及其用途
WO2025108406A1 (zh) * 2023-11-22 2025-05-30 广东东阳光药业股份有限公司 一种靶向降解雄激素受体的双功能嵌合体的杂环化合物及其用途
WO2025168131A1 (zh) * 2024-02-08 2025-08-14 清华大学 一种多靶降解剂及其用途

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL315310A (en) 2017-12-26 2024-10-01 Kymera Therapeutics Inc Irak degraders and uses thereof
CA3119773A1 (en) 2018-11-30 2020-06-04 Kymera Therapeutics, Inc. Irak degraders and uses thereof
PH12022500002A1 (en) 2019-06-28 2023-04-03 Kymera Therapeutics Inc Irak degraders and uses thereof
WO2021011868A1 (en) 2019-07-17 2021-01-21 Kymera Therapeutics, Inc. Irak degraders and uses thereof
WO2021119159A1 (en) 2019-12-10 2021-06-17 Kymera Therapeutics, Inc. Irak degraders and uses thereof
KR20220145325A (ko) 2019-12-17 2022-10-28 카이메라 쎄라퓨틱스 인코포레이티드 Irak 분해제 및 이의 용도
CN116867758A (zh) * 2020-12-30 2023-10-10 凯麦拉医疗公司 Irak降解剂和其用途
CA3243560A1 (en) 2022-01-31 2023-08-03 Kymera Therapeutics, Inc. Iraqi Degradation Agents and Their Uses
WO2024020084A1 (en) * 2022-07-20 2024-01-25 Bristol-Myers Squibb Company Heteroaryl compounds as ligand directed degraders of irak4
IL325910A (en) * 2023-07-13 2026-03-01 Increland Aromatic compound, pharmaceutical preparation comprising the same, and use thereof
CN121816348A (zh) 2023-08-11 2026-04-07 深圳众格生物科技有限公司 一种降解irak4的蛋白降解靶向嵌合体化合物及其应用

Citations (5)

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CN104582705A (zh) * 2012-01-10 2015-04-29 林伯士艾瑞斯公司 白介素-1受体相关激酶(irak)抑制剂和其用途
US20180153894A1 (en) * 2015-06-26 2018-06-07 Dana-Farber Cancer Institute, Inc. Fused bicyclic pyrimidine derivatives and uses thereof
CN109071552A (zh) * 2016-04-22 2018-12-21 达纳－法伯癌症研究所公司 细胞周期蛋白依赖性激酶4/6(cdk4/6)通过cdk4/6抑制剂与e3连接酶配体的缀合的降解及使用方法
US20190151295A1 (en) * 2017-11-17 2019-05-23 Arvinas, Inc. Compounds and methods for the targeted degradation of interleukin-1 receptor-associated kinase 4 polypeptides
WO2020010227A1 (en) * 2018-07-06 2020-01-09 Kymera Therapeutics, Inc. Protein degraders and uses thereof

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WO2017007612A1 (en) * 2015-07-07 2017-01-12 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
IL315310A (en) * 2017-12-26 2024-10-01 Kymera Therapeutics Inc Irak degraders and uses thereof
CA3119773A1 (en) * 2018-11-30 2020-06-04 Kymera Therapeutics, Inc. Irak degraders and uses thereof
WO2021053555A1 (en) * 2019-09-16 2021-03-25 Novartis Ag Glue degraders and methods of use thereof
KR20230005160A (ko) * 2020-03-19 2023-01-09 카이메라 쎄라퓨틱스 인코포레이티드 Mdm2 분해제 및 이의 용도

Patent Citations (5)

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CN104582705A (zh) * 2012-01-10 2015-04-29 林伯士艾瑞斯公司 白介素-1受体相关激酶(irak)抑制剂和其用途
US20180153894A1 (en) * 2015-06-26 2018-06-07 Dana-Farber Cancer Institute, Inc. Fused bicyclic pyrimidine derivatives and uses thereof
CN109071552A (zh) * 2016-04-22 2018-12-21 达纳－法伯癌症研究所公司 细胞周期蛋白依赖性激酶4/6(cdk4/6)通过cdk4/6抑制剂与e3连接酶配体的缀合的降解及使用方法
US20190151295A1 (en) * 2017-11-17 2019-05-23 Arvinas, Inc. Compounds and methods for the targeted degradation of interleukin-1 receptor-associated kinase 4 polypeptides
WO2020010227A1 (en) * 2018-07-06 2020-01-09 Kymera Therapeutics, Inc. Protein degraders and uses thereof

Non-Patent Citations (1)

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Title
DEGORCE, SÉBASTIEN L ET AL.: "Optimization of permeability in a series of pyrrolotriazine inhibitors of IRAK4", 《BIOORGANIC & MEDICINAL CHEMISTRY》, vol. 26, no. 4, 15 February 2018 (2018-02-15), pages 913 - 924, XP085350870, DOI: 10.1016/j.bmc.2018.01.008 *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2025051160A1 (zh) * 2023-09-08 2025-03-13 北京华益健康药物研究中心 用于治疗或预防冠状病毒感染的3cl蛋白酶抑制剂及其用途
WO2025108406A1 (zh) * 2023-11-22 2025-05-30 广东东阳光药业股份有限公司 一种靶向降解雄激素受体的双功能嵌合体的杂环化合物及其用途
WO2025168131A1 (zh) * 2024-02-08 2025-08-14 清华大学 一种多靶降解剂及其用途

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EP4259128A4 (en) 2025-04-30
AR124294A1 (es) 2023-03-15
US20250375526A1 (en) 2025-12-11
CO2023006818A2 (es) 2023-07-10
AU2021396308A1 (en) 2023-06-22
MX2023006719A (es) 2023-06-23
TW202237601A (zh) 2022-10-01
IL303458A (en) 2023-08-01
JP7832945B2 (ja) 2026-03-18
JP2023552827A (ja) 2023-12-19
EP4259128A1 (en) 2023-10-18
WO2022125790A1 (en) 2022-06-16
US20230096599A1 (en) 2023-03-30
CA3200608A1 (en) 2022-06-16
KR20230130179A (ko) 2023-09-11
AU2021396308A9 (en) 2025-03-20

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