TW202140489A - 介白素-1受體相關激酶之雙官能降解劑及其治療用途 - Google Patents

介白素-1受體相關激酶之雙官能降解劑及其治療用途 Download PDF

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TW202140489A
TW202140489A TW110105770A TW110105770A TW202140489A TW 202140489 A TW202140489 A TW 202140489A TW 110105770 A TW110105770 A TW 110105770A TW 110105770 A TW110105770 A TW 110105770A TW 202140489 A TW202140489 A TW 202140489A
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TW110105770A
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威利 索朗 帕瑪
傑弗瑞 吳
西拉 力普菲爾
柯然 歐茲博雅
妲里亞 威斯
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美商紐力克斯醫療股份有限公司
美商基利科學股份有限公司
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Publication of TW202140489A publication Critical patent/TW202140489A/zh

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • 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)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Engineering & Computer Science (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicinal Preparation (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
TW110105770A 2020-02-19 2021-02-19 介白素-1受體相關激酶之雙官能降解劑及其治療用途 TW202140489A (zh)

Applications Claiming Priority (2)

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US202062978635P 2020-02-19 2020-02-19
US62/978,635 2020-02-19

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TW202140489A true TW202140489A (zh) 2021-11-01

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US (1) US12528814B2 (https=)
EP (1) EP4107158A1 (https=)
JP (1) JP7815127B2 (https=)
KR (1) KR20220155295A (https=)
CN (1) CN115335381A (https=)
AU (1) AU2021224923A1 (https=)
CA (1) CA3165009A1 (https=)
TW (1) TW202140489A (https=)
WO (1) WO2021168197A1 (https=)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US11739101B2 (en) 2020-05-06 2023-08-29 Nurix Therapeutics, Inc. Bifunctional degraders of hematopoietic progenitor kinase and therapeutic uses thereof
CN117813307A (zh) 2021-08-18 2024-04-02 新锐思生物制药股份有限公司 白介素-1受体相关激酶的双官能降解物及其治疗用途
AR127625A1 (es) 2021-11-10 2024-02-14 Nurix Therapeutics Inc Degradadores bifuncionales inhibidores de la quinasa del progenitor hematopoyético y usos terapeuticos de los mismos
EP4446324A4 (en) * 2021-12-08 2026-05-06 Gluetacs Therapeutics Shanghai Co Ltd Ligand compounds for e3 ubiquitin ligase, protein degraders developed on basis of ligand compounds, and uses thereof
WO2023186069A1 (zh) * 2022-03-31 2023-10-05 石药集团中奇制药技术（石家庄）有限公司 一类白介素-1受体相关激酶4的双功能嵌合体杂环化合物及其制备方法、药用组合物和用途
JP2025513850A (ja) 2022-04-12 2025-04-30 ジェンザイム・コーポレーション 遺伝子治療のためのｉｒａｋ４モジュレーターの使用
CN117164583A (zh) * 2022-05-20 2023-12-05 斯迈旭(苏州)生物科技有限公司 一种靶向irak4蛋白降解的化合物及其应用
WO2024245331A1 (zh) * 2023-05-30 2024-12-05 上海汇伦医药股份有限公司 三并环类化合物、其制备方法和应用
CN120202200A (zh) * 2023-06-01 2025-06-24 标新生物医药科技(上海)有限公司 基于氧代异吲哚啉基取代的四氢嘧啶二酮的化合物及其应用
AU2024325813A1 (en) * 2023-08-15 2026-03-05 Guangzhou Imd Pharmaceutical Co., Ltd. Compound targeting irak protein inhibition or degradation and use thereof
WO2025126115A1 (en) 2023-12-13 2025-06-19 Beigene Switzerland Gmbh Degradation of irak4 by conjugation of irak4 inhibitors with e3 ligase ligands and methods of use
WO2025149070A1 (zh) * 2024-01-10 2025-07-17 甘李药业股份有限公司 一种新型靶向白细胞介素1受体关联激酶4(irak4)的蛋白降解嵌合体化合物的合成及其应用
CN118406019B (zh) * 2024-07-02 2024-09-20 苏州源起材料科技有限公司 一种噻唑化合物生物医药砌块的合成方法
WO2026050190A1 (en) * 2024-08-27 2026-03-05 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Smyd3 protacs for the treatment of hpv-negative squamous cell carcinoma
CN119119080A (zh) * 2024-09-06 2024-12-13 上海信诺维生物医药有限公司 一种irak4的蛋白降解剂
CN120757537B (zh) * 2025-09-09 2026-01-06 广东省科学院动物研究所 Protac降解剂及其应用

Family Cites Families (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6306663B1 (en) 1999-02-12 2001-10-23 Proteinex, Inc. Controlling protein levels in eucaryotic organisms
US7208157B2 (en) 2000-09-08 2007-04-24 California Institute Of Technology Proteolysis targeting chimeric pharmaceutical
WO2002020740A2 (en) 2000-09-08 2002-03-14 California Institute Of Technology Proteolysis targeting chimeric pharmaceutical
US7030112B2 (en) 2003-03-25 2006-04-18 Bristol-Myers Squibb Company Pyrrolopyridazine compounds and methods of use thereof for the treatment of proliferative disorders
CN101594909A (zh) 2006-09-07 2009-12-02 比奥根艾迪克Ma公司 用于治疗炎性病症、细胞增殖性失调、免疫失调的irak调节剂
ES2575604T3 (es) * 2012-01-13 2016-06-29 Bristol-Myers Squibb Company Compuestos de piridilo sustituidos con tiazolilo o tiadiazolilo útiles como inhibidores cinasa
US9464326B2 (en) 2012-03-22 2016-10-11 University Of Maryland, Baltimore Total and phosphorylated IL-1 receptor-associated kinase-1 and IL-1 receptor-associated kinase-4 as a biomarker for cancer progression and chemotherapy resistance
UY35935A (es) 2014-01-03 2015-06-30 Bristol Myers Squibb Company Una Corporación Del Estado De Delaware Compuestos de nicotinamida sustituida con heteroarilo como inhibidores de quinasa y moduladores de irak-4
RU2738833C9 (ru) 2014-04-14 2022-02-28 Арвинас, Оперэйшнз, Инк. Имидные модуляторы протеолиза и способы их применения
WO2016105518A1 (en) 2014-12-23 2016-06-30 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
GB201506871D0 (en) 2015-04-22 2015-06-03 Glaxosmithkline Ip Dev Ltd Novel compounds
EP3313840B1 (en) * 2015-06-24 2019-07-24 Bristol-Myers Squibb Company Heteroaryl substituted aminopyridine compounds
ES2822956T3 (es) 2015-06-24 2021-05-05 Bristol Myers Squibb Co Compuestos de aminopiridina sustituidos con heteroarilo
US10487329B2 (en) 2015-10-29 2019-11-26 Children's Hospital Medical Center Methods and compositions for the treatment of head and neck cancer
CN109641874A (zh) 2016-05-10 2019-04-16 C4医药公司 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体
CN110506039A (zh) 2016-10-11 2019-11-26 阿尔维纳斯股份有限公司 用于雄激素受体靶向降解的化合物和方法
WO2018081738A1 (en) 2016-10-28 2018-05-03 Children's Hospital Medical Center Treatment of diseases associated with activated irak
IL312367A (en) 2017-01-31 2024-06-01 Arvinas Operations Inc Cereblon ligands and bifunctional compounds comprising the same
TW202340194A (zh) 2017-02-16 2023-10-16 美商基利科學股份有限公司 吡咯并[1,2-b]嗒𠯤衍生物
CN110740733A (zh) 2017-06-16 2020-01-31 豪夫迈·罗氏有限公司 Irak4介导的疾患和病症的诊断和治疗方法
EP3710443A1 (en) 2017-11-17 2020-09-23 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of interleukin-1 receptor-associated kinase 4 polypeptides
US11595101B2 (en) 2017-11-24 2023-02-28 Lg Electronics Inc. Method and apparatus for reporting beam in wireless communication system
IL315310A (en) 2017-12-26 2024-10-01 Kymera Therapeutics Inc Irak degraders and uses thereof
US11542251B2 (en) 2018-02-14 2023-01-03 Dana-Farber Cancer Institute, Inc. IRAK degraders and uses thereof
TWI842978B (zh) 2018-07-13 2024-05-21 美商基利科學股份有限公司 衍生物
WO2020023851A1 (en) 2018-07-26 2020-01-30 Yale University Bifunctional substitued pyrimidines as modulators of fak proteolyse
WO2020036830A1 (en) * 2018-08-13 2020-02-20 Gilead Sciences, Inc. Pyrrolo[1,2-b]pyridazine derivatives as irak4 inhibitors
TWI727392B (zh) 2018-08-13 2021-05-11 美商基利科學股份有限公司 噻二唑irak4抑制劑
WO2021011868A1 (en) 2019-07-17 2021-01-21 Kymera Therapeutics, Inc. Irak degraders and uses thereof
JP7502425B2 (ja) 2019-10-01 2024-06-18 アルヴィナス・オペレーションズ・インコーポレイテッド Ｂｒｍ標的化化合物および関連使用方法
WO2021113557A1 (en) 2019-12-04 2021-06-10 Nurix Therapeutics, Inc. Bifunctional compounds for degrading btk via ubiquitin proteosome pathway
US20230322761A1 (en) 2020-03-11 2023-10-12 Beigene, Ltd. Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use
WO2021257914A1 (en) 2020-06-17 2021-12-23 Kymera Therapeutics, Inc. Irak degraders and uses thereof
JP2023530030A (ja) 2020-06-19 2023-07-12 シーフォー セラピューティクス， インコーポレイテッド Ｂｒａｆ分解剤
AU2022270089A1 (en) 2021-05-03 2023-11-16 Nurix Therapeutics, Inc. Compounds for inhibiting or degrading target proteins, compositions, comprising the same, methods of their making, and methods of their use
CN117813307A (zh) 2021-08-18 2024-04-02 新锐思生物制药股份有限公司 白介素-1受体相关激酶的双官能降解物及其治疗用途

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CA3165009A1 (en) 2021-08-26
CN115335381A (zh) 2022-11-11
US12528814B2 (en) 2026-01-20
JP2023514323A (ja) 2023-04-05
AU2021224923A1 (en) 2022-08-11
KR20220155295A (ko) 2022-11-22
WO2021168197A1 (en) 2021-08-26
US20230142629A1 (en) 2023-05-11
EP4107158A1 (en) 2022-12-28
JP7815127B2 (ja) 2026-02-17

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