JP7815127B2 - インターロイキン-1受容体関連キナーゼの二機能性分解剤およびその治療的使用 - Google Patents
インターロイキン-1受容体関連キナーゼの二機能性分解剤およびその治療的使用Info
- Publication number
- JP7815127B2 JP7815127B2 JP2022549454A JP2022549454A JP7815127B2 JP 7815127 B2 JP7815127 B2 JP 7815127B2 JP 2022549454 A JP2022549454 A JP 2022549454A JP 2022549454 A JP2022549454 A JP 2022549454A JP 7815127 B2 JP7815127 B2 JP 7815127B2
- Authority
- JP
- Japan
- Prior art keywords
- mmol
- methyl
- tert
- equiv
- butyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Classifications
-
- 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
Landscapes
- 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)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202062978635P | 2020-02-19 | 2020-02-19 | |
| US62/978,635 | 2020-02-19 | ||
| PCT/US2021/018710 WO2021168197A1 (en) | 2020-02-19 | 2021-02-19 | Bifunctional degraders of interleukin-1 receptor-associated kinases and therapeutic use thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2026016996A Division JP2026074171A (ja) | 2020-02-19 | 2026-02-04 | インターロイキン-1受容体関連キナーゼの二機能性分解剤およびその治療的使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2023514323A JP2023514323A (ja) | 2023-04-05 |
| JP2023514323A5 JP2023514323A5 (https=) | 2024-02-27 |
| JP7815127B2 true JP7815127B2 (ja) | 2026-02-17 |
Family
ID=74870905
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022549454A Active JP7815127B2 (ja) | 2020-02-19 | 2021-02-19 | インターロイキン-1受容体関連キナーゼの二機能性分解剤およびその治療的使用 |
Country Status (9)
| Country | Link |
|---|---|
| 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)
| 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 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019099926A1 (en) | 2017-11-17 | 2019-05-23 | Arvinas, Inc. | Compounds and methods for the targeted degradation of interleukin-1 receptor-associated kinase 4 polypeptides |
| WO2019133531A1 (en) | 2017-12-26 | 2019-07-04 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| US20200048261A1 (en) | 2018-08-13 | 2020-02-13 | Gilead Sciences, Inc. | PYRROLO[1,2-b]PYRIDAZINE DERIVATIVES |
| JP2021535089A (ja) | 2018-08-13 | 2021-12-16 | ギリアード サイエンシーズ, インコーポレイテッド | チアジアゾールirak4阻害剤 |
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| 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 |
| US11595101B2 (en) | 2017-11-24 | 2023-02-28 | Lg Electronics Inc. | Method and apparatus for reporting beam in wireless communication system |
| 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 |
| 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 |
-
2021
- 2021-02-19 WO PCT/US2021/018710 patent/WO2021168197A1/en not_active Ceased
- 2021-02-19 JP JP2022549454A patent/JP7815127B2/ja active Active
- 2021-02-19 CA CA3165009A patent/CA3165009A1/en active Pending
- 2021-02-19 KR KR1020227031406A patent/KR20220155295A/ko active Pending
- 2021-02-19 TW TW110105770A patent/TW202140489A/zh unknown
- 2021-02-19 US US17/904,592 patent/US12528814B2/en active Active
- 2021-02-19 CN CN202180015953.3A patent/CN115335381A/zh active Pending
- 2021-02-19 EP EP21711431.3A patent/EP4107158A1/en active Pending
- 2021-02-19 AU AU2021224923A patent/AU2021224923A1/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019099926A1 (en) | 2017-11-17 | 2019-05-23 | Arvinas, Inc. | Compounds and methods for the targeted degradation of interleukin-1 receptor-associated kinase 4 polypeptides |
| WO2019133531A1 (en) | 2017-12-26 | 2019-07-04 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| US20200048261A1 (en) | 2018-08-13 | 2020-02-13 | Gilead Sciences, Inc. | PYRROLO[1,2-b]PYRIDAZINE DERIVATIVES |
| JP2021535089A (ja) | 2018-08-13 | 2021-12-16 | ギリアード サイエンシーズ, インコーポレイテッド | チアジアゾールirak4阻害剤 |
Non-Patent Citations (1)
| Title |
|---|
| ACS Medicinal Chemistry Letters,2019年,Vol.10,pp.1081-1085 |
Also Published As
| Publication number | Publication date |
|---|---|
| CA3165009A1 (en) | 2021-08-26 |
| TW202140489A (zh) | 2021-11-01 |
| 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 |
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