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1. 发明申请

US20220395509A1 A PYRAZOLOPYRIMIDINE DERIVATIVE AS A HCK INHIBITOR FOR USE IN THERAPY, IN PARTICULAR MYD88 MUTATED DISEASES 有权
公开(公告)号：US20220395509A1
公开(公告)日：2022-12-15
申请号：US17767408
申请日：2020-10-07
申请人： Dana-Farber Cancer Institute, Inc.
发明人： Steven P. Treon , Guang Yang , Jinhua Wang , Li Tan , Nathanael S. Gray , Sara Jean Buhrlage
IPC分类号： A61K31/519 , A61K45/06 , C07D487/04 , A61P35/00 , A61P35/02
摘要： Provided herein are methods of treating diseases (e.g., proliferative disease (e.g., cancer (e.g., breast cancer, colon cancer, testicular cancer, CNS cancer, stomach cancer, lymphoma (e.g., B-cell lymphoma (e.g., lymphoplasmacytic lymphoma (e.g., IgM secreting lymphoplasmacytic lymphoma (i.e., Waldenstrom's Macroglobulinemia), non-IgM secreting lymphoplasmacytic lymphoma)), diffuse large B-cell lymphoma (e.g., activated B-cell-like (ABC)-DLBCL, germinal center B-cell-like (GBC)-DLBCL), follicular lymphoma, marginal zone B-cell lymphoma, small lymphocytic lymphoma, mantle cell lymphoma), and leukemia (e.g., chronic lymphocytic leukemia (CLL), acute lymphoblastic leukemia, myelogenous leukemia (e.g., chronic myelogenous leukemia, acute myelogenous leukemia))))) comprising administering to the subject in need thereof a therapeutically effective amount of Compound (I). Further provided are methods for treating disease resistant to treatment with BTK inhibitors (e.g., ibmtinib). Formula (I)

2. 发明申请

US20170044112A1 HYDROPHOBICALLY TAGGED JANUS KINASE INHIBITORS AND USES THEREOF 有权
标题翻译： HYDROPHOBICALLY TAGGED JANUS KINASE INHIBITORS及其用途
公开(公告)号：US20170044112A1
公开(公告)日：2017-02-16
申请号：US15305845
申请日：2015-04-23
申请人： Dana-Farber Cancer Institute, Inc.
发明人： Nathanael S. Gray , Li Tan
IPC分类号： C07D239/48 , C07D401/14 , C07D403/12
CPC分类号： C07D239/48 , C07D401/14 , C07D403/12 , C07D487/04
摘要： The present invention provides Janus kinase inhibitors, such as compounds of Formula (I) and Formula (II) wherein RY1 and RY2 comprise a tagged hydrophobic moiety RH. The compounds may covalently or non-covalently bind a kinase (e.g., Janus kinase 3 (JAK3)). The hydrophobic moiety RH may signal to the intracellular protein homeostasis machinery to induce degradation of the targeted kinase. 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).
摘要翻译：本发明提供了Janus激酶抑制剂，例如式（I）和式（II）的化合物，其中RY1和RY2包含标记的疏水部分RH。所述化合物可以共价或非共价结合激酶（例如，Janus激酶3（JAK3））。疏水部分RH可能信号到细胞内蛋白质内稳态机制以诱导靶向激酶的降解。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）。

3. 发明申请

US20160318878A1 METHODS TO TREAT LYMPHOPLASMACYTIC LYMPHOMA 有权
标题翻译：治疗淋巴细胞淋巴瘤的方法
公开(公告)号：US20160318878A1
公开(公告)日：2016-11-03
申请号：US15104132
申请日：2014-12-12
申请人： DANA-FARBER CANCER INSTITUTE, INC.
发明人： Steven P. Treon , Sara Jean Buhrlage , Nathanael S. Gray , Li Tan , Guang Yang
IPC分类号： C07D239/47 , C07D413/12 , C07D405/12 , C07D487/04 , C07D403/12
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 neoplasm 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.

4. 发明申请

US20160176825A1 KINASE INHIBITORS FOR THE TREATMENT OF DISEASE 有权
标题翻译：激素治疗疾病的抑制剂
公开(公告)号：US20160176825A1
公开(公告)日：2016-06-23
申请号：US14903650
申请日：2014-07-09
申请人： DANA-FARBER CANCER INSTITUTE, INC.
发明人： Nathanael Gray , Hwan Geun Choi , Li Tan
IPC分类号： C07D239/48 , C07D487/04 , C07D409/14 , C07D401/12 , C07D405/12 , C07D403/12 , C07D409/12
CPC分类号： C07D239/48 , A61K31/505 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/5377 , A61K45/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D471/04 , C07D487/04 , Y02A50/411 , A61K2300/00
摘要： The invention relates to compounds and their use in the treatment of disease. Novel irreversible inhibitors of wild-type and mutant forms of EGFR, FGFR, ALK, ROS, JAK, BTK, BLK, ITK, TEC, and/or TXK and their use for the treatment of cell proliferation disorders are described.
摘要翻译：本发明涉及化合物及其在治疗疾病中的用途。描述了EGFR，FGFR，ALK，ROS，JAK，BTK，BLK，ITK，TEC和/或TXK的野生型和突变形式的新型不可逆抑制剂及其用于治疗细胞增殖障碍的用途。

5. 发明公开

US20230339865A1 QUINAZOLINE-DERIVED HCK INHIBITORS FOR USE IN THE TREATMENT OF MYD88 MUTATED DISEASES 审中-公开
公开(公告)号：US20230339865A1
公开(公告)日：2023-10-26
申请号：US18008152
申请日：2021-06-03
申请人： Dana-Farber Cancer Institute, Inc.
发明人： Nathanael S. Gray , Steven P. Treon , Sara Jean Buhrlage , Guang Yang , Jinhua Wang , Li Tan , Zachary R. Hunter
IPC分类号： C07D239/88 , A61K45/06 , A61P35/00 , A61K31/496 , A61K31/5377 , A61K31/517 , C07D487/04 , A61K39/395 , C07D403/12 , C07D401/12 , A61K31/541
CPC分类号： C07D239/88 , A61K45/06 , A61P35/00 , A61K31/496 , A61K31/5377 , A61K31/517 , C07D487/04 , A61K39/39533 , C07D403/12 , C07D401/12 , A61K31/541
摘要： The present disclosure provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. The provided compounds may be kinase (e.g., HCK, BTK, LYN) inhibitors. Also provided are pharmaceutical compositions and kits including the provided compounds. Further provided are methods of using the provided compounds, pharmaceutical compositions, and kits (e.g., for treating diseases (e.g., proliferative diseases) in a subject in need thereof). (I)

6. 发明授权

US10925868B2 Degradation of protein kinases by conjugation of protein kinase inhibitors with E3 ligase ligand and methods of use 有权
公开(公告)号：US10925868B2
公开(公告)日：2021-02-23
申请号：US16343973
申请日：2017-11-10
申请人： Dana-Farber Cancer Institute, Inc.
发明人： Nathanael S. Gray , James Bradner , Li Tan , Hai-Tsang Huang , Dennis Buckley , Georg Winter , Mette Ishoey Rosenbaum
IPC分类号： C07D401/04 , A61K31/454 , A61K47/54 , A61K31/427 , C07D241/04 , C07D487/04
摘要： The present application provides bifunctional compounds of Formula (I): or an enantiomer, diastereomer, or stereoisomer thereof, or pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, which act as protein degradation inducing moieties for protein kinases (e.g., Bcr-Abl). The present application also relates to methods for the targeted degradation of one or more protein kinases through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to one or more protein kinases which can be utilized in the treatment of disorders modulated by protein kinases.

7. 发明授权

US10017477B2 Janus kinase inhibitors and uses thereof 有权
公开(公告)号：US10017477B2
公开(公告)日：2018-07-10
申请号：US15305801
申请日：2015-04-23
申请人： Dana-Farber Cancer Institute, Inc.
发明人： Nathanael S. Gray , Li Tan
IPC分类号： C07D239/48 , C07D403/12 , C07D401/14 , C07D405/14 , C07D401/12 , C07D405/12 , C07D239/47 , C07D413/12 , C07D487/04 , C07D495/04
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)

8. 发明授权

US09908872B2 Methods to treat lymphoplasmacytic lymphoma 有权
公开(公告)号：US09908872B2
公开(公告)日：2018-03-06
申请号：US15104005
申请日：2014-12-12
申请人： Dana-Farber Cancer Institute, Inc.
发明人： Steven P. Treon , Sara Jean Buhrlage , Nathanael S. Gray , Li Tan , Guang Yang
IPC分类号： C07D409/04 , C07D409/14 , A61K31/4436 , C07D401/04 , C07D413/04 , A61K45/06 , A61K31/44 , A61K31/4439 , A61K31/4745 , A61K31/496
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-1) to (I-9)), 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.

9. 发明申请

US20170333436A1 HCK AS A THERAPEUTIC TARGET IN MYD88 MUTATED DISEASES 审中-公开
公开(公告)号：US20170333436A1
公开(公告)日：2017-11-23
申请号：US15581736
申请日：2017-04-28
申请人： Dana-Farber Cancer Institute, Inc.
发明人： Steven P. Treon , Guang Yang , Nathanael S. Gray , Sara Jean Buhrlage , Li Tan
IPC分类号： A61K31/519 , A61K45/06
CPC分类号： A61K31/519 , A61K31/505 , A61K45/06 , A61K2300/00
摘要： Methods of treatment of conditions or diseases associated with myeloid differentiation primary response (MYD88) protein using a selective HCK inhibitor are provided herein.

10. 发明申请

US20160311807A1 METHODS TO TREAT LYMPHOPLASMACYTIC LYMPHOMA 有权
公开(公告)号：US20160311807A1
公开(公告)日：2016-10-27
申请号：US15104005
申请日：2014-12-12
申请人： DANA-FARBER CANCER INSTITUTE, INC.
发明人： Steven P. Treon , Sara Jean Buhrlage , Nathanael S. Gray , Li Tan , Guang Yang
IPC分类号： C07D409/04 , C07D409/14
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-1) to (I-9)), 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.

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