CN113412259B - 通过泛素蛋白酶体途径降解btk的双官能化合物 - Google Patents

通过泛素蛋白酶体途径降解btk的双官能化合物 Download PDF

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CN113412259B
CN113412259B CN201980082722.7A CN201980082722A CN113412259B CN 113412259 B CN113412259 B CN 113412259B CN 201980082722 A CN201980082722 A CN 201980082722A CN 113412259 B CN113412259 B CN 113412259B
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alkyl
pharmaceutically acceptable
disease
atoms
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CN113412259A (zh
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D·W·罗宾斯
A·T·桑德斯
J·麦金托什
J·米哈利克
J·吴
加藤大辅
D·维斯
G·彭
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Nulex Therapy
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    • 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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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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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    • 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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    • 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
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    • 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
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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    • C07D498/10—Spiro-condensed systems

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  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
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CN201980082722.7A 2018-10-15 2019-10-14 通过泛素蛋白酶体途径降解btk的双官能化合物 Active CN113412259B (zh)

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US201862745786P 2018-10-15 2018-10-15
US62/745786 2018-10-15
US201862767819P 2018-11-15 2018-11-15
US62/767819 2018-11-15
US201962836398P 2019-04-19 2019-04-19
US62/836398 2019-04-19
US201962887812P 2019-08-16 2019-08-16
US62/887812 2019-08-16
US201962901984P 2019-09-18 2019-09-18
US62/901984 2019-09-18
PCT/US2019/056112 WO2020081450A1 (en) 2018-10-15 2019-10-14 Bifunctional compounds for degrading btk via ubiquitin proteosome pathway

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CN202410998099.2A Pending CN118955473A (zh) 2018-10-15 2019-10-14 通过泛素蛋白酶体途径降解btk的双官能化合物

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EP (1) EP3867242A1 (https=)
JP (2) JP7600123B2 (https=)
KR (1) KR102816424B1 (https=)
CN (2) CN113412259B (https=)
AU (2) AU2019360928B2 (https=)
BR (2) BR112021007115A2 (https=)
CA (1) CA3115526A1 (https=)
IL (1) IL281904B2 (https=)
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Families Citing this family (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3710002A4 (en) 2017-11-16 2021-07-07 C4 Therapeutics, Inc. DEGRADER AND DEGRONE FOR TARGETED PROTEIN DEGRADATION
EP3728228A1 (en) 2017-12-22 2020-10-28 Ravenna Pharmaceuticals, Inc. Aminopyridine derivatives as phosphatidylinositol phosphate kinase inhibitors
JP2021519337A (ja) 2018-03-26 2021-08-10 シー４ セラピューティクス， インコーポレイテッド Ｉｋａｒｏｓの分解のためのセレブロン結合剤
CN119751456A (zh) 2018-04-16 2025-04-04 C4医药公司 螺环化合物
JP7600123B2 (ja) 2018-10-15 2024-12-16 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てｂｔｋを分解するための二官能性化合物
EP3877371A4 (en) 2018-11-07 2022-07-27 Dana-Farber Cancer Institute, Inc. IMIDAZOPYRIDINE DERIVATIVES AND AZA-IMIDAZOPYRIDINE DERIVATIVES AS JANUS KINASE 2 INHIBITORS AND USES THEREOF
WO2020097398A1 (en) 2018-11-07 2020-05-14 Dana-Farber Cancer Institute, Inc. Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof
WO2020097396A1 (en) 2018-11-07 2020-05-14 Dana-Farber Cancer Institute, Inc. Benzimidazole derivatives and aza-benzimidazole derivatives as janus kinase 2 inhibitors and uses thereof
WO2020167518A1 (en) 2019-02-13 2020-08-20 Nurix Therapeutics, Inc. Bifunctional compounds for degrading btk via ubiquitin proteosome pathway
EP3953346A1 (en) 2019-04-09 2022-02-16 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
EP3969447A1 (en) 2019-05-17 2022-03-23 Nurix Therapeutics, Inc. Cyano cyclobutyl compounds for cbl-b inhibition and uses thereof
KR20220030222A (ko) 2019-05-31 2022-03-10 이케나 온콜로지, 인코포레이티드 Tead 억제제 및 이의 용도
WO2020243423A1 (en) 2019-05-31 2020-12-03 Ikena Oncology, Inc. Tead inhibitors and uses thereof
TW202112767A (zh) 2019-06-17 2021-04-01 美商佩特拉製藥公司 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物
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.
EP4034141A1 (en) 2019-09-24 2022-08-03 Nurix Therapeutics, Inc. Cbl inhibitors and compositions for expansion of immune cells
US11820781B2 (en) * 2019-12-04 2023-11-21 Nurix Therapeutics, Inc. Bifunctional compounds for degrading BTK via ubiquitin proteosome pathway
CA3181537A1 (en) 2020-05-06 2021-11-11 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors
US11739101B2 (en) * 2020-05-06 2023-08-29 Nurix Therapeutics, Inc. Bifunctional degraders of hematopoietic progenitor kinase and therapeutic uses thereof
WO2022099117A1 (en) 2020-11-06 2022-05-12 Prelude Therapeutics Incorporated Brm targeting compounds and associated methods of use
WO2022120355A1 (en) * 2020-12-02 2022-06-09 Ikena Oncology, Inc. Tead degraders and uses thereof
EP4267574B1 (en) 2020-12-23 2025-04-23 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors
US12016860B2 (en) 2021-04-08 2024-06-25 Nurix Therapeutics, Inc. Combination therapies with Cbl-b inhibitor compounds
CA3217892A1 (en) * 2021-05-03 2022-11-10 Joel Mcintosh Compounds for inhibiting or degrading target proteins, compositions, comprising the same, methods of their making, and methods of their use
BR112023025403A2 (pt) 2021-06-25 2024-02-20 Korea Res Inst Chemical Tech Composto heterocíclico bifuncional tendo função de degradação de btk por meio da via ubiquitina proteassoma e uso do mesmo
KR102637915B1 (ko) * 2021-06-25 2024-02-19 한국화학연구원 유비퀴틴 프로테오좀 경로를 통해 비티케이 분해작용을 가지는 신규한 이작용성 헤테로사이클릭 화합물과 이의 용도
CN115557933B (zh) * 2021-07-01 2024-08-16 杭州和正医药有限公司 布鲁顿酪氨酸激酶及其突变体降解剂、组合物及应用
KR20240035820A (ko) 2021-07-09 2024-03-18 플렉시움 인코포레이티드 Ikzf2를 조절하는 아릴 화합물 및 약학 조성물
IL309796A (en) 2021-07-14 2024-02-01 Nurix Therapeutics Inc Bifunctional compounds for BTK degradation with reduced IMID activity
WO2023004163A1 (en) 2021-07-23 2023-01-26 Nurix Therapeutics, Inc. Bifunctional compounds for degrading btk with enhanced imid activity
WO2023009709A1 (en) * 2021-07-29 2023-02-02 Ajax Therapeutics, Inc. Pyrazolo piperazines as jak2 inhibitors
WO2023059582A1 (en) * 2021-10-04 2023-04-13 Halda Therapeutics Opco, Inc. Heterobifunctional compounds and their use in treating disease
AU2022379494A1 (en) * 2021-10-26 2024-05-30 Nurix Therapeutics, Inc. Piperidinylpyrazine-carboxamide compounds for treating and preventing cancer and for degrading btk
TW202325289A (zh) 2021-11-09 2023-07-01 美商雅捷可斯治療公司 Ｊａｋ２抑制劑之形式及組合物
JP7782035B2 (ja) 2021-11-09 2025-12-08 エイジャックス セラピューティクス， インコーポレイテッド Ｊａｋ２阻害剤としての６－ヘテロアリールオキシベンゾイミダゾール及びアザベンゾイミダゾール
CA3238118A1 (en) * 2021-11-18 2023-05-25 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Fused imide derivative
CN116143757B (zh) * 2021-11-22 2024-07-05 杭州和正医药有限公司 一种可降解btk激酶的多功能化合物、组合物及应用
CN115894450B (zh) * 2021-11-30 2023-09-12 山东如至生物医药科技有限公司 一种新型多环类化合物及其组合物和用途
WO2023143249A1 (zh) * 2022-01-28 2023-08-03 上海齐鲁制药研究中心有限公司 靶向malt1的蛋白降解化合物
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
WO2023227080A1 (zh) * 2022-05-25 2023-11-30 百极弘烨(南通)医药科技有限公司 一种protac化合物、含其的药物组合物及其制备方法和应用
JP2025523393A (ja) 2022-06-06 2025-07-23 シーフォー セラピューティクス， インコーポレイテッド 二環式置換グルタルイミドセレブロンバインダー
CN119816484A (zh) * 2022-08-26 2025-04-11 富士胶片株式会社 新型哌嗪衍生物或其盐及医药组合物
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
CN119451952A (zh) * 2023-06-01 2025-02-14 标新生物医药科技(上海)有限公司 氧代异吲哚啉基取代的四氢嘧啶二酮衍生物及其应用
CN121889391A (zh) 2023-08-03 2026-04-17 海思科医药集团股份有限公司 一种多环并环btk降解剂及其在医药上的应用
WO2025094065A1 (en) 2023-11-01 2025-05-08 Aurigene Oncology Limited Amino-substituted pyridazine compounds as smarca2 and/or smarca4 degraders
CN121335894A (zh) * 2024-02-04 2026-01-13 上海超阳药业有限公司 一种具备降解酪氨酸蛋白激酶btk活性的化合物及其制备方法和用途
WO2025174220A1 (ko) * 2024-02-14 2025-08-21 주식회사 유빅스테라퓨틱스 Shp2 단백질 분해 활성을 갖는 화합물 및 이들의 의약 용도
WO2025193454A1 (en) 2024-03-01 2025-09-18 Prelude Therapeutics Incorporated Brm and brg1 targeting antibody-drug conjugates and methods of use thereof
TW202543650A (zh) 2024-03-08 2025-11-16 美商海爾達醫療運營公司 異雙官能化合物及其在治療疾病中之用途
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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105960404A (zh) * 2013-12-05 2016-09-21 药品循环有限责任公司 布鲁顿氏酪氨酸激酶的抑制剂
WO2018098275A1 (en) * 2016-11-22 2018-05-31 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

Family Cites Families (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004099388A2 (en) 2003-03-05 2004-11-18 Proteologics, Inc. Cbl-b polypeptides, complexes and related methods
CN101365806B (zh) 2005-12-01 2016-11-16 医学预后研究所 用于鉴定治疗反应的生物标记的方法和装置及其预测疗效的用途
ES2566502T3 (es) 2006-09-13 2016-04-13 The Trustees Of Columbia University In The City Of New York Agentes y métodos para provocar una respuesta inmune antitumoral
AT506041A1 (de) 2007-12-10 2009-05-15 Univ Innsbruck Verfahren zur erhöhung der immunreaktivität
CA2710462C (en) 2008-02-05 2015-11-24 F. Hoffmann-La Roche Ag Pyridinones and pyridazinones
EP2440204B1 (en) * 2009-06-12 2013-12-18 Bristol-Myers Squibb Company Nicotinamide compounds useful as kinase modulators
KR101862327B1 (ko) 2010-05-07 2018-05-29 질레드 코네티컷 인코포레이티드 피리돈 및 아자-피리돈 화합물 및 사용 방법
AR082590A1 (es) 2010-08-12 2012-12-19 Hoffmann La Roche Inhibidores de la tirosina-quinasa de bruton
EP2471548A1 (de) 2010-12-28 2012-07-04 Apeiron Biologics AG siRNA gegen Cbl-b und optional IL2 und IL12 zur Verwendung in der Behandlung von Krebs
US20130110678A1 (en) 2011-11-02 2013-05-02 Apple Inc. Purchasing a product in a store using a mobile device
UA111756C2 (uk) 2011-11-03 2016-06-10 Ф. Хоффманн-Ля Рош Аг Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона
WO2013067264A1 (en) 2011-11-03 2013-05-10 Genentech, Inc. 8-fluorophthalazin-1 (2h) - one compounds as inhibitors of btk activity
CA2861066C (en) 2012-01-12 2024-01-02 Yale University Compounds and methods for the enhanced degradation of targeted proteins and other polypeptides by an e3 ubiquitin ligase
KR20150054994A (ko) 2012-09-13 2015-05-20 에프. 호프만-라 로슈 아게 브루톤 티로신 키나아제의 억제제
US10308707B2 (en) 2013-12-02 2019-06-04 Aaron Diamond Aids Research Center Bispecific HIV-1-neutralizing antibodies
GB201506871D0 (en) 2015-04-22 2015-06-03 Glaxosmithkline Ip Dev Ltd Novel compounds
BR112017025986A2 (pt) 2015-06-02 2018-08-14 Pharmacyclics Llc inibidores de tirosina quinase de bruton.
EP3325475B1 (en) 2015-07-17 2020-03-18 Takeda Pharmaceutical Company Limited Oxadiazole derivatives useful as hdac inhibitors
GB201610147D0 (en) * 2016-06-10 2016-07-27 Glaxosmithkline Ip Dev Ltd Novel compounds
MX2019004707A (es) 2016-10-26 2019-08-12 Iovance Biotherapeutics Inc Reestimulacion de linfocitos infiltrantes de tumor crioconservados.
TWI788307B (zh) 2016-10-31 2023-01-01 美商艾歐凡斯生物治療公司 用於擴增腫瘤浸潤性淋巴細胞之工程化人造抗原呈現細胞
JP2020514252A (ja) 2016-12-08 2020-05-21 アイカーン スクール オブ メディスン アット マウント シナイ Ｃｄｋ４／６媒介性がんを治療するための組成物および方法
JOP20190224A1 (ar) 2017-03-29 2019-09-26 Iovance Biotherapeutics Inc عمليات من أجل إنتاج الخلايا اللمفاوية المرتشحة للأورام واستخداماتها في العلاج المناعي
WO2019148005A1 (en) 2018-01-26 2019-08-01 Nurix Therapeutics, Inc. Inhibitors of cbl-b and methods of use thereof
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
KR20210040355A (ko) 2018-06-19 2021-04-13 바이오엔테크 유에스 인크. 네오항원 및 이의 용도
JP7600123B2 (ja) 2018-10-15 2024-12-16 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てｂｔｋを分解するための二官能性化合物
WO2020167518A1 (en) 2019-02-13 2020-08-20 Nurix Therapeutics, Inc. Bifunctional compounds for degrading btk via ubiquitin proteosome pathway
EP3953346A1 (en) 2019-04-09 2022-02-16 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
EP3969447A1 (en) 2019-05-17 2022-03-23 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.
WO2021021761A1 (en) 2019-07-30 2021-02-04 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
US20230024442A1 (en) 2019-11-08 2023-01-26 Nurix Therapeutics, Inc. Bifunctional compounds for grading btk via ubiquitin proteosome pathway
CN112812109B (zh) 2019-11-18 2022-06-21 中国科学院微生物研究所 化合物DaP-01及其制备方法和应用
US11820781B2 (en) 2019-12-04 2023-11-21 Nurix Therapeutics, Inc. Bifunctional compounds for degrading BTK via ubiquitin proteosome pathway
WO2022093742A1 (en) 2020-10-26 2022-05-05 Dana-Farber Cancer Institute, Inc. Compounds for targeted protein degradation of kinases
IL309796A (en) 2021-07-14 2024-02-01 Nurix Therapeutics Inc Bifunctional compounds for BTK degradation with reduced IMID activity
WO2023004163A1 (en) 2021-07-23 2023-01-26 Nurix Therapeutics, Inc. Bifunctional compounds for degrading btk with enhanced imid activity
AU2022379494A1 (en) 2021-10-26 2024-05-30 Nurix Therapeutics, Inc. Piperidinylpyrazine-carboxamide compounds for treating and preventing cancer and for degrading btk
EP4702014A1 (en) 2023-04-28 2026-03-04 Nurix Therapeutics, Inc. Bifunctional compounds for degrading braf via ubiquitin proteosome pathway
US20250136579A1 (en) 2023-10-23 2025-05-01 Nurix Therapeutics, Inc. Salts and free bases of bifunctional compound and polymorph forms thereof

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105960404A (zh) * 2013-12-05 2016-09-21 药品循环有限责任公司 布鲁顿氏酪氨酸激酶的抑制剂
WO2018098275A1 (en) * 2016-11-22 2018-05-31 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

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