JP7038712B2 - ブルトン型チロシンキナーゼ（ｂｔｋ）阻害剤のｅ３リガーゼリガンドとのコンジュゲーションによるｂｔｋの分解および使用法 - Google Patents

ブルトン型チロシンキナーゼ（ｂｔｋ）阻害剤のｅ３リガーゼリガンドとのコンジュゲーションによるｂｔｋの分解および使用法 Download PDF

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JP7038712B2
JP7038712B2 JP2019527335A JP2019527335A JP7038712B2 JP 7038712 B2 JP7038712 B2 JP 7038712B2 JP 2019527335 A JP2019527335 A JP 2019527335A JP 2019527335 A JP2019527335 A JP 2019527335A JP 7038712 B2 JP7038712 B2 JP 7038712B2
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ナサナエル エス． グレイ
デニス ドブロボルスキー
ハイ－ツァン ファン
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デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド
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    • 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
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    • 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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JP2019527335A 2016-11-22 2017-11-22 ブルトン型チロシンキナーゼ（ｂｔｋ）阻害剤のｅ３リガーゼリガンドとのコンジュゲーションによるｂｔｋの分解および使用法 Active JP7038712B2 (ja)

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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

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2021512059A (ja) * 2018-01-29 2021-05-13 ダナ−ファーバー キャンサー インスティテュート，インコーポレイテッド ブルトン型チロシンキナーゼ（ｂｔｋ）阻害剤のｅ３リガーゼリガンドとのコンジュゲーションによるｂｔｋの分解および使用方法

Families Citing this family (41)

* Cited by examiner, † Cited by third party
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
CN110087680B (zh) 2016-08-19 2024-03-19 百济神州有限公司 使用包含btk抑制剂的组合产品治疗癌症
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
EP3645569A4 (en) 2017-06-26 2021-03-24 BeiGene, Ltd. IMMUNOTHERAPY FOR LIVER CELL CARCINOMA
US11786529B2 (en) 2017-11-29 2023-10-17 Beigene Switzerland Gmbh Treatment of indolent or aggressive B-cell lymphomas using a combination comprising BTK inhibitors
US12539292B2 (en) 2018-04-01 2026-02-03 Arvinas Operations, Inc. BRM targeting compounds and associated methods of use
EP3820532A4 (en) 2018-07-11 2022-04-06 H. Lee Moffitt Cancer Center & Research Institute, Inc. DIMERE IMMUNOMODULATORY COMPOUNDS AGAINST CEREBLON-BASED MECHANISMS
US11707452B2 (en) 2018-08-20 2023-07-25 Arvinas Operations, Inc. Modulators of alpha-synuclein proteolysis and associated methods of use
EP3867242A1 (en) * 2018-10-15 2021-08-25 Nurix Therapeutics, Inc. Bifunctional compounds for degrading btk via ubiquitin proteosome pathway
AU2019389174A1 (en) * 2018-11-30 2021-07-01 Kymera Therapeutics, Inc. Irak degraders and uses thereof
EP3924350A1 (en) 2019-02-13 2021-12-22 Nurix Therapeutics, Inc. Bifunctional compounds for degrading btk via ubiquitin proteosome pathway
KR20210141554A (ko) 2019-03-21 2021-11-23 코디악 바이오사이언시즈, 인크. 세포외 소포 접합체 및 이의 용도
EP3941607A1 (en) 2019-03-21 2022-01-26 Codiak BioSciences, Inc. Process for preparing extracellular vesicles
KR102922115B1 (ko) 2019-04-09 2026-02-04 누릭스 테라퓨틱스 인코포레이티드 Cbl-b 억제용의 3-치환된 피페리딘 화합물, 및 암 백신 및/또는 종양용해 바이러스와 조합된 cbl-b 억제제의 용도
CA3140873A1 (en) 2019-05-17 2020-11-26 Nurix Therapeutics, Inc. Cyano cyclobutyl compounds for cbl-b inhibition and uses thereof
CA3294689A1 (en) 2019-06-26 2026-03-02 Nurix Therapeutics, Inc. Substituted benzyl-triazole compounds for cbl-b inhibition, and further uses thereof
EP3999182A1 (en) 2019-07-17 2022-05-25 Arvinas Operations, Inc. Tau-protein targeting compounds and associated methods of use
WO2021018018A1 (en) * 2019-07-26 2021-02-04 Beigene, Ltd. Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inidbitors with e3 ligase ligand and methods of use
US12653809B2 (en) 2019-07-30 2026-06-16 Nurix Therapeutics, Inc. Urea, amide, and substituted heteroaryl compounds for CBL-B inhibition
EP4034141A1 (en) 2019-09-24 2022-08-03 Nurix Therapeutics, Inc. Cbl inhibitors and compositions for expansion of immune cells
MX2022004526A (es) 2019-10-17 2022-07-21 Arvinas Operations Inc Moléculas bifuncionales que contienen una porción de unión a la ligasa de ubiquitina e3 unida a una porción de direccionamiento a bcl6.
WO2021091575A1 (en) * 2019-11-08 2021-05-14 Nurix Therapeutics, Inc. Bifunctional compounds for degrading btk via ubiquitin proteosome pathway
CA3160713A1 (en) 2019-12-04 2021-06-10 Nurix Therapeutics, Inc. Bifunctional compounds for degrading btk via ubiquitin proteosome pathway
AU2020414151A1 (en) 2019-12-23 2022-08-25 Jiangxi Jemincare Group Co., Ltd Protein degradation agent compound preparation method and application
AU2021247685A1 (en) * 2020-03-31 2022-10-27 Bristol-Myers Squibb Company Conjugates
WO2021237100A1 (en) 2020-05-21 2021-11-25 Codiak Biosciences, Inc. Methods of targeting extracellular vesicles to lung
KR20230024328A (ko) 2020-06-12 2023-02-20 상하이 제민케어 파마슈티칼스 컴퍼니 리미티드 프탈라지논 화합물, 이의 제조 방법 및 이의 의학적 용도
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
WO2022047145A1 (en) 2020-08-28 2022-03-03 Arvinas Operations, Inc. Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use
WO2022066928A2 (en) 2020-09-23 2022-03-31 Codiak Biosciences, Inc. Process for preparing extracellular vesicles
CN117242060B (zh) 2021-01-13 2026-07-17 蒙特罗莎治疗股份有限公司 异吲哚啉酮化合物
US12016860B2 (en) 2021-04-08 2024-06-25 Nurix Therapeutics, Inc. Combination therapies with Cbl-b inhibitor compounds
CN118388454A (zh) 2021-04-16 2024-07-26 阿尔维纳斯运营股份有限公司 Bcl6蛋白水解的调节剂和其相关使用方法
MX2024004899A (es) 2021-10-26 2024-05-24 Nurix Therapeutics Inc Compuestos de piperidinilpirazina-carboxamida para tratar y prevenir el cancer y para degradar btk.
JP2024540179A (ja) * 2021-11-05 2024-10-31 ユービックス セラピューティクス インコーポレイテッド Ｂｔｋタンパク質分解活性を有する化合物及びその医薬用途
CN119823111B (zh) * 2021-11-18 2026-05-05 正大天晴药业集团股份有限公司 稠合酰亚胺类衍生物
CA3240051A1 (en) * 2021-12-30 2023-07-06 Beigene Switzerland Gmbh Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use
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
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
EP4584258A1 (en) 2022-09-07 2025-07-16 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 (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008533032A (ja) 2005-03-10 2008-08-21 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 或る種の置換アミド、その製造方法及び使用方法
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
JP2011519948A (ja) 2008-05-06 2011-07-14 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、その製造法及びＢｔｋインヒビターとしての使用
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
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
WO2015160845A2 (en) 2014-04-14 2015-10-22 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
WO2016105518A1 (en) 2014-12-23 2016-06-30 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
WO2016149668A1 (en) 2015-03-18 2016-09-22 Arvinas, Inc. Compounds and methods for the enhanced degradation of targeted proteins
WO2016169989A1 (en) 2015-04-22 2016-10-27 Glaxosmithkline Intellectual Property Development Limited Iap e3 ligase directed proteolysis targeting chimeric molecules

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL2300459T3 (pl) * 2008-07-02 2013-10-31 Hoffmann La Roche Nowe fenylopirazynony jako inhibitory kinazy
US9694084B2 (en) * 2014-12-23 2017-07-04 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008533032A (ja) 2005-03-10 2008-08-21 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 或る種の置換アミド、その製造方法及び使用方法
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
JP2011519948A (ja) 2008-05-06 2011-07-14 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、その製造法及びＢｔｋインヒビターとしての使用
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
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
WO2015160845A2 (en) 2014-04-14 2015-10-22 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
WO2016105518A1 (en) 2014-12-23 2016-06-30 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
WO2016149668A1 (en) 2015-03-18 2016-09-22 Arvinas, Inc. Compounds and methods for the enhanced degradation of targeted proteins
WO2016169989A1 (en) 2015-04-22 2016-10-27 Glaxosmithkline Intellectual Property Development Limited Iap e3 ligase directed proteolysis targeting chimeric molecules

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2021512059A (ja) * 2018-01-29 2021-05-13 ダナ−ファーバー キャンサー インスティテュート，インコーポレイテッド ブルトン型チロシンキナーゼ（ｂｔｋ）阻害剤のｅ３リガーゼリガンドとのコンジュゲーションによるｂｔｋの分解および使用方法

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AU2017363252A1 (en) 2019-05-16
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KR102566109B1 (ko) 2023-08-10
US20190262458A1 (en) 2019-08-29
EP3544975B1 (en) 2022-01-05
CA3042297A1 (en) 2018-05-31
US10842878B2 (en) 2020-11-24
JP2019535744A (ja) 2019-12-12
EP3544975A1 (en) 2019-10-02
WO2018098275A1 (en) 2018-05-31
AU2017363252B2 (en) 2021-08-19

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