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1. 发明申请

WO2018009544A1 BICYCLIC UREA KINASE INHIBITORS AND USES THEREOF 审中-公开
标题翻译：双环脲激酶抑制剂及其用途
公开(公告)号：WO2018009544A1
公开(公告)日：2018-01-11
申请号：PCT/US2017/040722
申请日：2017-07-05
申请人： THE BROAD INSTITUTE, INC. , DANA-FARBER CANCER INSTITUTE, INC. , THE GENERAL HOSPITAL CORPORATION D/B/A MASSACHUSETTS GENERAL HOSPITAL
发明人： GRAY, Nathanael, S. , LIANG, Yanke , CHOI, Hwan, Geun , SUNDBERG, Thomas , SHAMJI, Alykhan , XAVIER, Ramnik , FISHER, David E.
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00 , A61P7/00 , A61P19/00 , A61P21/00 , A61P25/00 , A61P37/00
摘要： The present disclosure provides compounds of Formula (I), (II), and (III). The provided compounds are able to bind protein kinases ( e.g ., SIK) and may be useful in modulating ( e.g ., inhibiting) the activity of a protein kinase ( e.g. , SIK, ( e.g. , SIK1, SIK2, or SIK3)) in a subject or cell. The provided compounds may be useful in treating or preventing a disease ( e.g ., proliferative disease, musculoskeletal disease, genetic disease, hematological disease, neurological disease, painful condition, psychiatric disorder, or metabolic disorder) in a subject in need thereof. Also provided are pharmaceutical compositions, kits, methods, and uses that include or involve a compound described herein.
摘要翻译：本公开提供了式（I），（II）和（III）的化合物。所提供的化合物能够结合蛋白激酶（例如，SIK），并且可用于调节（例如抑制）蛋白激酶（，例如，抑制）蛋白激酶（例如，SIK，（例如，SIK1，SIK2或SIK3））在受试者或细胞中的表达。所提供的化合物可用于治疗或预防哺乳动物中的疾病（例如，增殖性疾病，肌肉骨骼疾病，遗传疾病，血液病，神经疾病，疼痛病症，精神病症或代谢病症）需要的主题。还提供了包含或涉及本文所述化合物的药物组合物，试剂盒，方法和用途。

2. 发明申请

WO2022087433A8 COVALENT INHIBITORS OF CREATINE KINASE (CK) AND USES THEREOF FOR TREATING AND PREVENTING CANCER 审中-公开
公开(公告)号：WO2022087433A8
公开(公告)日：2022-04-28
申请号：PCT/US2021/056280
申请日：2021-10-22
申请人： DANA-FARBER CANCER INSTITUTE, INC. , GRAY, Nathanael, S. , CHOUCHANI, Edward , ZHANG, Tinghu , DARABEDIAN, Narek , JI, Wenzhi , CHE, Jianwei
发明人： GRAY, Nathanael, S. , CHOUCHANI, Edward , ZHANG, Tinghu , DARABEDIAN, Narek , JI, Wenzhi , CHE, Jianwei
IPC分类号： A61P35/00 , C07D265/36 , C07D413/04 , A61K31/538
摘要： The present disclosure relates to compounds of formula I that are capable of inhibiting creatine kinase. The present disclosure also relates to methods of treating cancer, such as hematological malignancies.

3. 发明申请

WO2020106685A1 MACROCYCLIC INHIBITORS OF DYRK1A 审中-公开
公开(公告)号：WO2020106685A1
公开(公告)日：2020-05-28
申请号：PCT/US2019/062150
申请日：2019-11-19
申请人： DANA-FARBER CANCER INSTITUTE, INC. , VORONOI INC.
发明人： GRAY, Nathanael, S. , HATCHER, John, M. , CHOI, Hwan Geun
IPC分类号： A61K31/4985 , A61P29/00 , A61P35/00
摘要： Disclosed are macrocyclic compounds that possess inhibitory activity against DYRK, TRK, TLK, and/or RET. Also disclosed are pharmaceutical compositions containing the compounds, methods of making the compounds, and methods of using the compounds to treat diseases and disorders that are characterized or mediated by aberrant DYRK, TRK, TLK, and/or RET activity such as cancer, neurodegenerative disorders and genetic disorders.

4. 发明申请

WO2019222349A1 COMPOUNDS FOR TREATING DENGUE VIRUS INFECTIONS AND OTHER INFECTIONS 审中-公开
公开(公告)号：WO2019222349A1
公开(公告)日：2019-11-21
申请号：PCT/US2019/032418
申请日：2019-05-15
申请人： DANA-FARBER CANCER INSTITUTE, INC. , PRESIDENT AND FELLOWS OF HARVARD COLLEGE
发明人： YANG, Priscilla, L. , GRAY, Nathanael, S. , JANG, Jaebong , WANG, Jinhua , KWIATKOWSKI, Nicholas, P. , LIAN, Wenlong , LI, Zhengnian
IPC分类号： A61K31/165 , A61K31/404 , A61P31/12
摘要： Provided herein are compounds, pharmaceutical compositions, methods, and kits for treating viral infections ( e.g., Dengue viral infections). In certain embodiments, compounds useful in the methods described herein are of Formula (I) or (II).

5. 发明申请

WO2018160774A1 USES OF PYRIMIDOPYRIMIDINONES AS SIK INHIBITORS 审中-公开
公开(公告)号：WO2018160774A1
公开(公告)日：2018-09-07
申请号：PCT/US2018/020335
申请日：2018-02-28
申请人： THE GENERAL HOSPITAL CORPORATION , DANA-FARBER CANCER INSTITUTE, INC. , MURAKAMI, Ryo
发明人： MURAKAMI, Ryo , FISHER, David, E. , MUJAHID, Nisma , GRAY, Nathanael, S.
IPC分类号： A61K31/395 , A61K31/505 , A61K31/506
摘要： The present disclosure provides methods of increasing skin pigmentation in a subject in need thereof using salt-inducible kinase (SIK) inhibitors, such as macrocyclic compounds of Formula (I), bicyclic urea compounds of Formula (II), (III), and (IV), and compounds of Formula (V), (VI), (VI-A), or (VII). Also provided are pharmaceutical compositions, methods, and uses that include or involve a compound described herein.

6. 发明申请

WO2018085247A1 COMPOUNDS FOR MALT1 DEGRADATION 审中-公开
标题翻译：用于MALT1降解的化合物
公开(公告)号：WO2018085247A1
公开(公告)日：2018-05-11
申请号：PCT/US2017/059234
申请日：2017-10-31
申请人： CORNELL UNIVERSITY , DANA-FARBER CANCER INSTITUTE, INC. , CHILDREN'S MEDICAL CENTER CORPORATION
发明人： MELNICK, Ari, M. , GABAS, Lorena, Fontan , US, Ilkay , CASALENA, Gabriella , GRAY, Nathanael, S. , SCOTT, David, A. , HATCHER, John , DU, Guangyan , WU, Hao , QIAO, Qi
IPC分类号： C07D401/12 , C07D487/04 , C07D401/14 , C07D209/48 , A61K31/519 , A61K31/4439
摘要： Provided herein are bifunctional compounds that inhibit MALTl and/or promote targeted ubiquitination for the degradation of MALTl. In particular, provided are compounds that can bind MALTl, a protein whose activity is responsible for constitutive NF-KB signaling in certain cancers (e.g., activated B-cell diffuse large B-cell lymphoma (ABC-DLBCL)), and can assist in its degradation by recruiting an E3 ubiquitin ligase (e.g., Cereblon, VHL), which can ubiquitinate MALTl, marking it for proteasome degradation. Also provided are pharmaceutical compositions comprising the bifunctional compounds, methods of treating cancer with the bifunctional compounds, methods of promoting the degradation of MALTl, and methods of binding E3 ubiquitin ligase activity in a subject by administering a compound or composition described herein.
摘要翻译：本文提供了抑制MALT1和/或促进MALT1降解的靶向泛素化的双功能化合物。具体而言，提供了能够结合MALT1的化合物，所述MALT1是在某些癌症（例如活化的B细胞弥漫性大B细胞淋巴瘤（ABC-DLBCL））中其活性负责组成型NF-κB信号传导的蛋白质，并且可以辅助其通过募集泛素化MALT1的E3泛素连接酶（例如，Cereblon，VHL）降解，将其标记为蛋白酶体降解。还提供了包含双功能化合物的药物组合物，用双功能化合物治疗癌症的方法，促进MALT1降解的方法，以及通过施用本文所述的化合物或组合物在受试者中结合E3泛素连接酶活性的方法。 >

7. 发明申请

WO2017177092A1 PYRIMIDO-DIAZEPINONE KINASE SCAFFOLD COMPOUNDS AND METHODS OF TREATING PI3K-MEDIATED DISORDERS 审中-公开
标题翻译：吡嘧啶二氮杂酮激酶支架化合物和治疗PI3K介导的疾病的方法
公开(公告)号：WO2017177092A1
公开(公告)日：2017-10-12
申请号：PCT/US2017/026522
申请日：2017-04-07
申请人： DANA-FARBER CANCER INSTITUTE, INC.
发明人： GRAY, Nathanael, S. , ZHANG, Tinghu , FERGUSON, Fleur, M. , ZHAO, Jean , NI, Jing
IPC分类号： C07D487/14 , C07D495/14 , C07D473/34
摘要： The present invention relates to use of pyrimido-diazepinone compounds that are able to modulate protein kinases such as ΡΙ3Κ-γ and PI3K-δ, which are members of the Class I Type IA and Class I Type IB family of phosphatidylinositol- 4,5-bisphosphate 3-kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.
摘要翻译：本发明涉及能够调节蛋白激酶例如PI3K-γ和PI3K-δ的嘧啶并二氮杂酮化合物的用途，所述蛋白激酶是属于I型IA型和I型IB型的成员磷脂酰肌醇-4,5-二磷酸3-激酶家族，以及这些化合物在治疗各种疾病，障碍或病症中的用途。

8. 发明申请

WO2016210291A1 FUSED BICYCLIC PYRIMIDINE DERIVATIVES AND USES THEREOF 审中-公开
标题翻译：熔融双相吡啶衍生物及其用途
公开(公告)号：WO2016210291A1
公开(公告)日：2016-12-29
申请号：PCT/US2016/039302
申请日：2016-06-24
申请人： DANA-FARBER CANCER INSTITUTE, INC.
发明人： GRAY, Nathanael, S. , ZHANG, Tinghu
IPC分类号： A61P35/02 , C07D401/14 , A61K31/506
CPC分类号： A61K31/519 , A61K31/166 , A61K31/167 , A61K31/34 , A61K31/381 , A61K31/437 , A61K45/06 , C07D491/048 , C07D495/04 , C07D519/00 , A61K2300/00
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 inventive compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., lung cancer, breast cancer, leukemia, lymphoma, melanoma, multiple myeloma, Ewing's sarcoma, osteosarcoma, brain cancer, neuroblastoma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase (e.g. a protein kinase (e.g. a cyclin-dependent kinase (CDK) (e.g. CDK7, CDK12, or CDK13) or a lipid kinase such as a phosphatidylinositol- 5 -phosphate 4- kinase (PIP4K) (e.g., ΡΙ5Ρ4Κα, ΡΙ5Ρ4Κβ, or ΡΙ5Ρ4Κγ)) in the subject.
摘要翻译：本发明提供新的式（I）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，前药及其组合物。还提供涉及用于治疗或预防增殖性疾病（例如癌症（例如，肺癌，乳腺癌，白血病，淋巴瘤，黑素瘤，多发性骨髓瘤，尤因氏肉瘤，骨肉瘤，脑癌，神经母细胞瘤）的本发明化合物或组合物的方法和试剂盒，，良性肿瘤，血管生成，炎性疾病，自身炎性疾病和自身免疫性疾病）。使用本发明的化合物或组合物治疗具有增殖性疾病的受试者可以抑制激酶（例如蛋白激酶（例如细胞周期蛋白依赖性激酶（CDK）（例如CDK7，CDK12或CDK13））的异常活性或脂质激酶，例如磷脂酰肌醇-5-磷酸4-激酶（PIP4K）（例如，PIP5P4Kα，PI5P4Kβ或PIP5P4Kγ））。

9. 发明申请

WO2021257660A1 SMALL MOLECULE COVALENT ACTIVATORS OF UCP1 审中-公开
公开(公告)号：WO2021257660A1
公开(公告)日：2021-12-23
申请号：PCT/US2021/037566
申请日：2021-06-16
申请人： DANA-FARBER CANCER INSTITUTE, INC. , GRAY, Nathanael, S. , FAN, Mengyang , ORDONEZ, Martha , CHOUCHANI, Edward , ZHANG, Tinghu , LI, Zhengnian , CHE, Jianwei
发明人： GRAY, Nathanael, S. , FAN, Mengyang , ORDONEZ, Martha , CHOUCHANI, Edward , ZHANG, Tinghu , LI, Zhengnian , CHE, Jianwei
IPC分类号： A61K31/713 , C12N15/113
摘要： Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof. The compounds of Formula (I) are useful for activating uncoupling protein 1 (UCP1) dependent thermogenesis. Also disclosed herein are methods of treating obesity or metabolic disorders such as diabetes using a compound of Formula (I).

10. 发明申请

WO2021133896A8 TRANSCRIPTIONAL ENHANCED ASSOCIATE DOMAIN (TEAD) TRANSCRIPTION FACTOR INHIBITORS AND USES THEREOF 审中-公开
公开(公告)号：WO2021133896A8
公开(公告)日：2021-07-01
申请号：PCT/US2020/066811
申请日：2020-12-23
申请人： DANA-FARBER CANCER INSTITUTE, INC.
发明人： GRAY, Nathanael, S. , ZHANG, Tinghu , CHE, Jianwei , KWIATKOWSKI, Nicholas, Paul , FAN, Mengyang , LU, Wenchao
IPC分类号： A61K31/18 , C07C311/37 , A61P29/00 , A61P35/00 , C07C233/27 , C07C233/44 , C07C233/55 , C07C235/46 , C07C237/30 , C07C237/38 , C07C311/29 , C07C311/51
摘要： Provided herein are compounds of (I-A), (I-B), or (II), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. Also provided are methods, uses, and kits involving the inventive compounds and pharmaceutical compositions thereof for treating and/or preventing diseases (e.g., proliferative diseases (e.g., cancers), inflammatory diseases (e.g., fibrosis), autoimmune diseases (e.g., sclerosis)) in a subject. Provided are methods of inhibiting the activity of a transcription factor (e.g., TEAD, such as TEAD1, TEAD2, TEAD3, TEAD4) and/or inhibiting the transcription of a gene (e.g., a gene controlled or regulated by a transcription factor (e.g., TEAD)) in a subject.

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