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1. 发明申请

WO2017117474A1 BIFUNCTIONAL COMPOUNDS FOR HER3 DEGRADATION AND METHODS OF USE 审中-公开
标题翻译： HER3降解的双功能化合物及其使用方法
公开(公告)号：WO2017117474A1
公开(公告)日：2017-07-06
申请号：PCT/US2016/069351
申请日：2016-12-29
申请人： DANA-FARBER CANCER INSTITUTE, INC. , DAEGU-GYEONGBUK MEDICAL INNOVATION FOUNDATION
发明人： GRAY, Nathanael , BRADNER, James , JANNE, Pasi , JANG, Jaebong , CHOI, Hwan, Geun , KO, Eunhwa , CHO, Joong-heui
IPC分类号： C07D487/04 , A61P35/00
CPC分类号： C07D401/14
摘要： The present invention provides bifunctional compounds which act as protein degradation inducing moieties for a HER family protein, such as Her3. The present invention also provides methods for the targeted degradation of a HER family protein through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to the HER family protein which can be utilized in the treatment of disorders modulated by a HER family protein.
摘要翻译：本发明提供了双功能化合物，其充当HER家族蛋白质（例如Her3）的蛋白质降解诱导部分。本发明还提供了通过使用将泛素连接酶结合部分连接至能够结合HER家族蛋白的配体的双功能化合物来靶向降解HER家族蛋白的方法，所述HER家族蛋白可以用于治疗由HER家族蛋白调节的疾病。

2. 发明申请

WO2020117759A1 SMALL MOLECULE DEGRADERS OF HELIOS AND METHODS OF USE 审中-公开
公开(公告)号：WO2020117759A1
公开(公告)日：2020-06-11
申请号：PCT/US2019/064169
申请日：2019-12-03
申请人： DANA-FARBER CANCER INSTITUTE, INC.
发明人： VERANO, Alyssa , WANG, Eric , NOWAK, Radoslaw , YUAN, Christine , GRAY, Nathanael , FISCHER, Eric , ZHANG, Tinghu , LIU, Hu
IPC分类号： A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/496
摘要： Disclosed are compounds and pharmaceutically acceptable salts and stereoisomers thereof that may cause degradation of various proteins e.g., IKZF2 (Helios). Also disclosed are pharmaceutical compositions containing same, and methods of making and using the compounds to treat diseases and disorders characterized or mediated by aberrant protein activity.

3. 发明申请

WO2017185031A1 DEGRADATION OF CYCLIN-DEPENDENT KINASE 4/6 (CDK4/6) BY CONJUGATION OF CDK4/6 INHIBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE 审中-公开
标题翻译： CDK4 / 6抑制剂与E3连接配体结合降解周期蛋白依赖性激酶4/6（CDK4 / 6）的方法和使用方法
公开(公告)号：WO2017185031A1
公开(公告)日：2017-10-26
申请号：PCT/US2017/028941
申请日：2017-04-21
申请人： DANA-FARBER CANCER INSTITUTE, INC.
发明人： GRAY, Nathanael , ZHANG, Tinghu , OLSON, Calla M. , LIANG, Yanke , KWIATKOWSKI, Nicholas
IPC分类号： C07D487/04 , C07D471/04 , C07D401/14 , A61K31/519
摘要： The present application provides bifunctional compounds of Formula (I), or Targeting Ligand, or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which act as protein degradation inducing moieties for cyclin-dependent kinase 4 (CDK4) and/or cyclin-dependent kinase 6 (CDK6). The present application also relates to methods for the targeted degradation of CDK4 and/or CDK6 through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to CDK4 and/or CDK6 which can be utilized in the treatment of disorders modulated by CDK4 and/or CDK6.
摘要翻译：本申请提供了作为蛋白质降解诱导部分起作用的式（I）的双官能化合物或其靶向配体或其药学上可接受的盐，水合物，溶剂化物，前药，立体异构体或互变异构体，细胞周期蛋白依赖性激酶4（CDK4）和/或细胞周期蛋白依赖性激酶6（CDK6）。本申请还涉及通过使用将泛素连接酶结合部分连接至能够结合CDK4和/或CDK6的配体的双功能化合物来靶向降解CDK4和/或CDK6的方法，所述配体可以被利用用于治疗由CDK4和/或CDK6调节的疾病。

4. 发明申请

WO2015196072A2 USES OF KINASE INHIBITORS FOR INDUCING AND MAINTAINING PLURIPOTENCY 审中-公开
标题翻译：使用激酶抑制剂诱导和维持群体性
公开(公告)号：WO2015196072A2
公开(公告)日：2015-12-23
申请号：PCT/US2015/036692
申请日：2015-06-19
申请人： WHITEHEAD INSTITUTE FOR BIOMEDICAL RESEARCH , DANA-FARBER CANCER INSTITUTE, INC.
发明人： THEUNISSEN, Thorold, W. , GRAY, Nathanael , JAENISCH, Rudolf
IPC分类号： C12N5/0735
CPC分类号： C12N5/0606 , C12N5/0696 , C12N2501/11 , C12N2501/115 , C12N2501/165 , C12N2501/727 , C12N2501/999
摘要： The present disclosure provides compounds of any one of Formulae (A) to (L). The present disclosure also provides compositions, uses, and methods that include or involve a compound described herein, a serine/threonine-protein kinase B-Raf (BRAF) inhibitor, an epidermal growth factor receptor (EGFR) inhibitor, a vascular endothelial growth factor 1 (VEGFR1) inhibitor, a fibroblast growth factor receptor 1 (FGFR1) inhibitor, or a combination thereof. The compounds, compositions, uses, and methods are useful in changing the pluripotency state of a vertebrate cell to a more naive state.
摘要翻译：本公开内容提供式（A）至（L）中任一项的化合物。本公开还提供组合物，用途和方法，其包括或涉及本文所述的化合物，丝氨酸/苏氨酸 - 蛋白激酶B-Raf（BRAF）抑制剂，表皮生长因子受体（EGFR）抑制剂，血管内皮生长因子 1（VEGFR1）抑制剂，成纤维细胞生长因子受体1（FGFR1）抑制剂或其组合。化合物，组合物，用途和方法可用于将脊椎动物细胞的多能性状态改变为更幼稚的状态。

5. 发明申请

WO2015164614A1 JANUS KINASE INHIBITORS AND USES THEREOF 审中-公开
标题翻译： JANUS激酶抑制剂及其用途
公开(公告)号：WO2015164614A1
公开(公告)日：2015-10-29
申请号：PCT/US2015/027312
申请日：2015-04-23
申请人： DANA-FARBER CANCER INSTITUTE, INC.
发明人： GRAY, Nathanael , TAN, Li
IPC分类号： A61K31/505 , A61K31/506 , C07D403/12
CPC分类号： C07D239/48 , C07D239/47 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D487/04 , C07D495/04
摘要： The present invention provides kinase inhibitors, such as compounds of Formula (I) and Formula (II). The compounds may covalently or non-covalently bind a kinase (e.g., Janus kinase 3 (JAK3)). Also provided are pharmaceutical compositions, kits, methods, and uses that involve the compounds for reducing the activity of a kinase and/or treating and/or preventing a condition associated with aberrant activity of a kinase (e.g., a proliferative disease, inflammatory disorder, autoimmune disorder, painful condition, and/or viral infection). (I) (II)
摘要翻译：本发明提供激酶抑制剂，例如式（I）和式（II）的化合物。所述化合物可以共价或非共价结合激酶（例如，Janus激酶3（JAK3））。还提供了涉及用于降低激酶活性和/或治疗和/或预防与激酶异常活性相关的病症的化合物的药物组合物，试剂盒，方法和用途（例如，增殖性疾病，炎症性疾病，自身免疫性疾病，疼痛状况和/或病毒感染）。（一）（二）

6. 发明申请

WO2015089481A2 METHODS TO TREAT LYMPHOPLASMACYTIC LYMPHOMA 审中-公开
标题翻译：治疗淋巴细胞淋巴瘤的方法
公开(公告)号：WO2015089481A2
公开(公告)日：2015-06-18
申请号：PCT/US2014/070167
申请日：2014-12-12
申请人： DANA-FARBER CANCER INSTITUTE, INC.
发明人： TREON, Steven, P. , BUHRLAGE, Sara, Jean , GRAY, Nathanael , TAN, Li , YANG, Guang
IPC分类号： A61K31/4436 , C07D409/04
CPC分类号： C07D409/04 , A61K31/44 , A61K31/4436 , A61K31/4439 , A61K31/4745 , A61K31/496 , A61K45/06 , C07D401/04 , C07D409/14 , C07D413/04 , A61K2300/00
摘要： The present invention provides compounds of any one of Formulae (I) to (V) (e.g. , compounds of any one of Formulae (I-l) to (1-9)), and methods for treating Waldenstrom' s macroglobulinemia (WM) and other B cell neoplams in a subject using the compounds. The methods comprise administering to a subject in need thereof an effective amount of the compounds. Also provided are methods to treat B cell neoplasms using the compounds in combination with inhibitors of Bruton's tyrosine kinase (BTK), interleukin- 1 receptor- associated kinase 1 (IRAKI), interleukin- 1 receptor-associated kinase 4 (IRAK4), bone marrow on X chromosome kinase (BMX), phosphoinositide 3-kinase (PI3K), transforming growth factor b-activated kinase- 1 (TAK1), and/or a Src family kinase.
摘要翻译：本发明提供式（I）至（V）中任一项的化合物（例如，式（II）至（1-9）中任一项的化合物）和用于治疗瓦尔登斯特伦的巨球蛋白血症（WM）等的方法使用该化合物的受试者中的B细胞肿瘤。所述方法包括向有需要的受试者施用有效量的化合物。还提供了使用与Bruton酪氨酸激酶（BTK），白细胞介素-1受体相关激酶1（IRAKI），白细胞介素-1受体相关激酶4（IRAK4），骨髓抑制剂 X染色体激酶（BMX），磷酸肌醇3-激酶（PI3K），转化生长因子b激活激酶-1（TAK1）和/或Src家族激酶。

7. 发明申请

WO2015089479A1 METHODS TO TREAT LYMPHOPLASMACYTIC LYMPHOMA 审中-公开
标题翻译：治疗淋巴细胞淋巴瘤的方法
公开(公告)号：WO2015089479A1
公开(公告)日：2015-06-18
申请号：PCT/US2014/070162
申请日：2014-12-12
申请人： DANA-FARBER CANCER INSTITUTE, INC.
发明人： TREON, Steven, P. , BUHRLAGE, Sara, Jean , GRAY, Nathanael , TAN, Li , YANG, Guang
IPC分类号： A61K31/165
CPC分类号： C07D239/47 , A61K31/506 , A61K45/06 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/04 , C07D487/04
摘要： The present invention provides compounds of any one of Formulae (A), (I-11), (II), and (V) ( e.g. , compounds of Formula (A-1)-(A-18)), and methods for treating Waldenström's macroglobulinemia (WM) and other B cell neoplams in a subject using the compounds. The methods comprise administering to a subject in need thereof an effective amount of the compounds. Also provided are methods to treat B cell neoplasms using the compounds in combination with inhibitors of Bruton's tyrosine kinase (BTK), interleukin-1 receptor-associated kinase 1 (IRAK1), interleukin-1 receptor-associated kinase 4 (IRAK4), bone marrow on X chromosome kinase (BMX), phosphoinositide 3-kinase (PI3K), transforming growth factor b-activated kinase-1 (TAK1), and/or a Src family kinase.
摘要翻译：本发明提供式（A），（I-11），（II）和（V）中任一项的化合物（例如式（A-1） - （A-18）的化合物）使用该化合物治疗受试者中的Waldenström的巨球蛋白血症（WM）和其他B细胞肿瘤。所述方法包括向有需要的受试者施用有效量的化合物。还提供了使用与Bruton酪氨酸激酶（BTK），白细胞介素-1受体相关激酶1（IRAK1），白细胞介素-1受体相关激酶4（IRAK4），骨髓抑制剂 X染色体激酶（BMX），磷酸肌醇3-激酶（PI3K），转化生长因子b激活激酶-1（TAK1）和/或Src家族激酶。

8. 发明申请

WO2014063054A1 BONE MARROW ON X CHROMOSOME KINASE (BMX) INHIBITORS AND USES THEREOF 审中-公开
标题翻译： X染色体激酶（BMX）抑制剂及其用途的骨髓
公开(公告)号：WO2014063054A1
公开(公告)日：2014-04-24
申请号：PCT/US2013/065689
申请日：2013-10-18
申请人： DANA-FARBER CANCER INSTITUTE, INC. , BETH ISRAEL DEACONESS MEDICAL CENTER, INC.
发明人： GRAY, Nathanael , BALK, Steven , LIU, Qingson , CHEN, Sen
IPC分类号： C07D471/04 , A61K31/473 , A61P35/00
CPC分类号： C07D471/04
摘要： The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the compounds of Formula (I) or (II), or compositions thereof, for treating or preventing a wide range of diseases (e.g., proliferative diseases (e.g., cancers, benign neoplasms, angiogenesis, inflammatory diseases, autoimmune diseases) and metabolic diseases (e.g., diabetes (e.g., type 2 diabetes, gestational diabetes)) in a subject. Treatment of a subject with a disease using a compound of Formula (I) or (II), or compositions thereof, may downregulate the expression and/or inhibit the activity of a kinase (e.g., a tyrosine kinase, such as a Tec kinase, in particular, bone marrow on X chromosome kinase (BMX)), and therefore, suppress tyrosine kinase singling in the subject.
摘要翻译：本发明提供了式（I）的新型化合物及其药学上可接受的盐，溶剂合物，水合物，多晶型物，共晶体，互变异构体，立体异构体，同位素标记的衍生物，前药和组合物。还提供了涉及式（I）或（II）化合物或其组合物的方法和试剂盒用于治疗或预防多种疾病（例如增殖性疾病（例如癌症，良性肿瘤，血管生成，炎性疾病，（I）或（II）化合物或其组合物治疗患有疾病的受试者，可以使用式（I）或（II）化合物或其组合物治疗患有疾病的受试者（例如酪氨酸激酶，例如Tec激酶，特别是X染色体激酶（BMX）上的骨髓）的表达和/或抑制活性，并且因此抑制受试者中的酪氨酸激酶单选。

9. 发明申请

WO2023288305A1 SMALL MOLECULE CYCLIN DEPENDENT KINASE 4/6 (CDK4/6) AND IKZF2 (HELIOS) DEGRADERS AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：WO2023288305A1
公开(公告)日：2023-01-19
申请号：PCT/US2022/073782
申请日：2022-07-15
申请人： DANA-FARBER CANCER INSTITUTE, INC. , VERANO, Alyssa , WANG, Eric , YOU, Inchul , GRAY, Nathanael
发明人： VERANO, Alyssa , WANG, Eric , YOU, Inchul , GRAY, Nathanael
IPC分类号： A61K31/519 , C07D471/04 , C07D487/04
摘要： The present application provides bifunctional compounds that act as protein degradation inducing moieties for cyclin-dependent kinase 4 (CDK4), cyclin-dependent kinase 6 (CDK6) and Ikaros Family Zinc Finger 2 (IKZF2), also known as Helios. Also disclosed are methods for the treatment of disorders modulated by CDK4, CDK6, and IKZF2.

10. 发明申请

WO2020006262A1 NEW CRBN MODULATORS 审中-公开
公开(公告)号：WO2020006262A1
公开(公告)日：2020-01-02
申请号：PCT/US2019/039553
申请日：2019-06-27
申请人： DANA-FARBER CANCER INSTITUTE, INC.
发明人： GRAY, Nathanael , ZHANG, Tinghu , FISCHER, Eric , VERANO, Alyssa , HE, Zhixiang , DU, Guangyan , DONOVAN, Katherine , NOWAK, Radoslaw , YUAN, Christine
IPC分类号： A61K31/4545 , A61K47/54 , C07D401/14
摘要： Disclosed are degraders, pharmaceutical compositions containing them, and methods of making and using the degraders to treat diseases and disorders characterized by dysregulated or dysfunctional protein activity that can be targeted by cereblon.

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