KR102566109B1 - Ｅ3 리가아제 리간드와 브루톤 티로신 키나아제(ｂｔｋ) 억제제의 컨쥬게이션에 의한 ｂｔｋ의 분해 및 사용 방법 - Google Patents
Ｅ3 리가아제 리간드와 브루톤 티로신 키나아제(ｂｔｋ) 억제제의 컨쥬게이션에 의한 ｂｔｋ의 분해 및 사용 방법 Download PDFInfo
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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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, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P35/00—Antineoplastic agents
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
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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
- A61K31/435—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
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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- 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
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- 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
- C07D401/02—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
- 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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- 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
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- 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
- C07D417/02—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 two hetero rings
- C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
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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)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- 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)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662425204P | 2016-11-22 | 2016-11-22 | |
| US62/425,204 | 2016-11-22 | ||
| PCT/US2017/063011 WO2018098275A1 (en) | 2016-11-22 | 2017-11-22 | Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20190077595A KR20190077595A (ko) | 2019-07-03 |
| KR102566109B1 true KR102566109B1 (ko) | 2023-08-10 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020197018105A KR102566109B1 (ko) | 2016-11-22 | 2017-11-22 | Ｅ3 리가아제 리간드와 브루톤 티로신 키나아제(ｂｔｋ) 억제제의 컨쥬게이션에 의한 ｂｔｋ의 분해 및 사용 방법 |
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Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109153644B (zh) | 2016-03-16 | 2022-10-21 | H·李·莫菲特癌症中心研究有限公司 | 用以增强效应t细胞功能的针对cereblon的小分子 |
| ES2971881T3 (es) | 2016-08-19 | 2024-06-10 | Beigene Switzerland Gmbh | Combinación de zanubrutinib con un anticuerpo anti-cd20 o anti-pd-1 para su uso en el tratamiento del cáncer |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
| TW201906866A (zh) | 2017-06-26 | 2019-02-16 | 英屬開曼群島商百濟神州有限公司 | 酸性鞘磷脂酶缺乏症患者中異常骨狀況的治療 |
| CN111801334B (zh) | 2017-11-29 | 2023-06-09 | 百济神州瑞士有限责任公司 | 使用包含btk抑制剂的组合治疗惰性或侵袭性b-细胞淋巴瘤 |
| EP3746426A4 (en) * | 2018-01-29 | 2021-12-29 | Dana Farber Cancer Institute, Inc. | Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use |
| BR112021000395A2 (pt) | 2018-07-11 | 2021-04-06 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Compostos imunomoduladores diméricos contra mecanismos baseados em cereblon |
| CN112912376A (zh) | 2018-08-20 | 2021-06-04 | 阿尔维纳斯运营股份有限公司 | 用于治疗神经变性疾病的具有E3泛素连接酶结合活性并靶向α-突触核蛋白的蛋白水解靶向嵌合(PROTAC)化合物 |
| CA3115526A1 (en) | 2018-10-15 | 2020-04-23 | Nurix Therapeutics, Inc. | Bifunctional compounds for degrading btk via ubiquitin proteosome pathway |
| SG11202109587TA (en) | 2019-03-21 | 2021-10-28 | Codiak Biosciences Inc | Extracellular vesicle conjugates and uses thereof |
| WO2020191369A1 (en) | 2019-03-21 | 2020-09-24 | Codiak Biosciences, Inc. | Process for preparing extracellular vesicles |
| CA3136348A1 (en) | 2019-04-09 | 2020-10-15 | Nurix Therapeutics, Inc. | 3-substituted piperidine compounds for cbl-b inhibition, and use of a cbl-b inhibitor in combination with a cancer vaccine and/or oncolytic virus |
| CA3140873A1 (en) | 2019-05-17 | 2020-11-26 | Nurix Therapeutics, Inc. | Cyano cyclobutyl compounds for cbl-b inhibition and uses thereof |
| MX2021015675A (es) | 2019-06-26 | 2022-02-03 | Nurix Therapeutics Inc | Compuestos de bencil-triazol sustituidos para la inhibicion de cbl-b y otros usos de los mismos. |
| WO2021011913A1 (en) | 2019-07-17 | 2021-01-21 | Arvinas Operations, Inc. | Tau-protein targeting compounds and associated methods of use |
| US20220281876A1 (en) * | 2019-07-26 | 2022-09-08 | Beigene, Ltd. | Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use |
| EP4055019A1 (en) * | 2019-11-08 | 2022-09-14 | Nurix Therapeutics, Inc. | Bifunctional compounds for degrading btk via ubiquitin proteosome pathway |
| JP2023504147A (ja) | 2019-12-04 | 2023-02-01 | ニューリックス セラピューティクス，インコーポレイテッド | ユビキチンプロテオソーム経路を介したｂｔｋの分解のための二官能性化合物 |
| IL294225A (en) * | 2019-12-23 | 2022-08-01 | Shanghai Jemincare Pharmaceuticals Co Ltd | Method of preparation of a protein-degrading agent compound and application |
| CA3172720A1 (en) * | 2020-03-31 | 2021-10-07 | Nathan FISHKIN | Conjugates |
| WO2021237100A1 (en) | 2020-05-21 | 2021-11-25 | Codiak Biosciences, Inc. | Methods of targeting extracellular vesicles to lung |
| CN113801098B (zh) | 2020-06-12 | 2023-05-30 | 上海济煜医药科技有限公司 | 酞嗪酮类化合物及其制备方法和医药用途 |
| CN113943293A (zh) * | 2020-07-16 | 2022-01-18 | 百济神州(北京)生物科技有限公司 | 用于制备作为protac btk降解剂的双官能化合物的方法 |
| US20240241020A1 (en) | 2020-09-23 | 2024-07-18 | Lonza Sales Ag | Process for preparing extracellular vesicles |
| WO2022152821A1 (en) | 2021-01-13 | 2022-07-21 | Monte Rosa Therapeutics Ag | Isoindolinone compounds |
| JP2024514836A (ja) | 2021-04-08 | 2024-04-03 | ニューリックス セラピューティクス，インコーポレイテッド | Ｃｂｌ－ｂ阻害化合物との組み合わせ療法 |
| US11986532B2 (en) | 2021-04-16 | 2024-05-21 | Arvinas Operations, Inc. | Modulators of BCL6 proteolysis and associated methods of use |
| AU2022424178A1 (en) * | 2021-12-30 | 2024-07-11 | Beigene, Ltd. | Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use |
| CN114853735B (zh) * | 2022-07-06 | 2022-10-21 | 北京鑫开元医药科技有限公司 | 靶向泛素化降解trk的化合物及其制备方法、组合物和用途 |
| US11957759B1 (en) | 2022-09-07 | 2024-04-16 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use |
| CN116283929B (zh) * | 2023-01-10 | 2023-11-07 | 暨南大学 | 诱导egfr降解的化合物及其应用 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2010540452A (ja) | 2007-09-20 | 2010-12-24 | シージーアイ ファーマシューティカルズ，インコーポレイティド | 置換アミド、その製造方法、及びその使用方法 |
| JP2015508414A (ja) * | 2012-01-12 | 2015-03-19 | イエール ユニバーシティ | Ｅ３ユビキチンリガーゼによる標的タンパク質および他のポリペプチドの分解増強のための化合物および方法 |
| WO2016105518A1 (en) * | 2014-12-23 | 2016-06-30 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
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|---|---|---|---|---|
| KR101357524B1 (ko) | 2005-03-10 | 2014-02-03 | 질레드 코네티컷 인코포레이티드 | 특정 치환된 아미드, 그의 제조 방법, 및 사용 방법 |
| ES2554615T3 (es) * | 2008-05-06 | 2015-12-22 | Gilead Connecticut, Inc. | Amidas sustituidas, método de preparación y utilización como inhibidores de Btk |
| AU2009265813B2 (en) * | 2008-07-02 | 2014-04-10 | F. Hoffmann-La Roche Ag | Novel phenylpyrazinones as kinase inhibitors |
| JP2013104687A (ja) | 2011-11-10 | 2013-05-30 | Carna Biosciences Inc | 新規な蛍光プローブ及びキナーゼ阻害剤の新規スクリーニング方法 |
| KR20170002446A (ko) | 2014-04-14 | 2017-01-06 | 아비나스 인코포레이티드 | 단백질분해의 이미드-기초된 조절인자 및 연관된 이용 방법 |
| US9694084B2 (en) * | 2014-12-23 | 2017-07-04 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| CA2979070A1 (en) | 2015-03-18 | 2016-09-22 | Arvinas, Inc. | Compounds and methods for the enhanced degradation of targeted proteins |
| GB201506871D0 (en) | 2015-04-22 | 2015-06-03 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
-
2017
- 2017-11-22 WO PCT/US2017/063011 patent/WO2018098275A1/en unknown
- 2017-11-22 AU AU2017363252A patent/AU2017363252B2/en not_active Ceased
- 2017-11-22 CA CA3042297A patent/CA3042297A1/en active Pending
- 2017-11-22 EP EP17873155.0A patent/EP3544975B1/en active Active
- 2017-11-22 JP JP2019527335A patent/JP7038712B2/ja active Active
- 2017-11-22 KR KR1020197018105A patent/KR102566109B1/ko active IP Right Grant
- 2017-11-22 US US16/343,974 patent/US10842878B2/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2010540452A (ja) | 2007-09-20 | 2010-12-24 | シージーアイ ファーマシューティカルズ，インコーポレイティド | 置換アミド、その製造方法、及びその使用方法 |
| JP2015508414A (ja) * | 2012-01-12 | 2015-03-19 | イエール ユニバーシティ | Ｅ３ユビキチンリガーゼによる標的タンパク質および他のポリペプチドの分解増強のための化合物および方法 |
| WO2016105518A1 (en) * | 2014-12-23 | 2016-06-30 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
Also Published As
| Publication number | Publication date |
|---|---|
| EP3544975B1 (en) | 2022-01-05 |
| KR20190077595A (ko) | 2019-07-03 |
| US20190262458A1 (en) | 2019-08-29 |
| EP3544975A4 (en) | 2020-07-01 |
| CA3042297A1 (en) | 2018-05-31 |
| WO2018098275A1 (en) | 2018-05-31 |
| US10842878B2 (en) | 2020-11-24 |
| JP2019535744A (ja) | 2019-12-12 |
| EP3544975A1 (en) | 2019-10-02 |
| AU2017363252B2 (en) | 2021-08-19 |
| JP7038712B2 (ja) | 2022-03-18 |
| AU2017363252A1 (en) | 2019-05-16 |
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