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公开(公告)号:US11878019B2
公开(公告)日:2024-01-23
申请号:US17532215
申请日:2021-11-22
发明人: David E. Fisher , Nisma Mujahid , Ryo Murakami , Nathanael S. Gray , Yanke Liang , Hwan Geun Choi
IPC分类号: A61K31/519 , A61K31/5377 , A61P17/00 , A61P35/00
CPC分类号: A61K31/5377 , A61K31/519 , A61P17/00 , A61P35/00
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.
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公开(公告)号:US11826365B2
公开(公告)日:2023-11-28
申请号:US16893289
申请日:2020-06-04
IPC分类号: A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/517 , A61K45/06 , C07D239/88 , C07D403/12 , C07D401/14 , C07D401/12 , C07D239/42 , C07D417/12 , C07D471/04 , C07D487/04 , A61K31/437 , A61K31/519 , C07D213/81 , C07D241/20 , C07D473/30
CPC分类号: A61K31/496 , A61K31/437 , A61K31/497 , A61K31/4965 , A61K31/517 , A61K31/519 , A61K45/06 , C07D213/81 , C07D239/42 , C07D239/88 , C07D241/20 , C07D401/12 , C07D401/14 , C07D403/12 , C07D417/12 , C07D471/04 , C07D473/30 , C07D487/04
摘要: The present invention relates to novel compounds which are able to modulate b-raf kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.
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公开(公告)号:US20210147388A1
公开(公告)日:2021-05-20
申请号:US17155244
申请日:2021-01-22
发明人: Nathanael S. Gray , Hwan Geun Choi , Yanke Liang
IPC分类号: C07D403/04 , C07D403/14
摘要: The present disclosure provides imidazolyl compounds of Formula (I) and methods of preparing the compounds. The provided compounds are able to bind protein kinases and may be useful in modulating (e.g., inhibiting) the activity of a protein kinase in a subject or cell and/or in treating or preventing a disease (e.g., proliferative 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.
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公开(公告)号:US20200253981A1
公开(公告)日:2020-08-13
申请号:US16489462
申请日:2018-02-28
发明人: David E. Fisher , Nisma Mujahid , Ryo Murakami , Nathanael S. Gray , Yanke Liang , Hwan Geun Choi
IPC分类号: A61K31/5377 , A61K31/519 , A61P17/00 , A61P35/00
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.
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公开(公告)号:US10457691B2
公开(公告)日:2019-10-29
申请号:US15327690
申请日:2015-07-21
发明人: Nathanael S. Gray , Hwan Geun Choi , Yanke Liang
IPC分类号: C07D498/08 , C07D498/18
摘要: The present disclosure provides macrocyclic compounds of Formula (I). The provided compounds are able to bind protein kinases and may be useful in modulating (e.g., inhibiting) the activity of a protein kinase in a subject or cell and/or in treating or preventing a disease (e.g., proliferative 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.
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公开(公告)号:US10316002B2
公开(公告)日:2019-06-11
申请号:US15696309
申请日:2017-09-06
发明人: Nathanael Gray , Hwan Geun Choi , Li Tan
IPC分类号: C07D239/48 , C07D471/04 , C07D409/14 , C07D409/12 , C07D405/14 , C07D405/12 , C07D401/12 , C07D403/12 , C07D487/04 , A61K31/505 , A61K45/06 , A61K31/5377 , A61K31/519 , A61K31/517 , A61K31/506
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.
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公开(公告)号:US20180170912A1
公开(公告)日:2018-06-21
申请号:US15554753
申请日:2016-03-04
发明人: Nathanael Gray , Tinghu Zhang , Hai-Tsang Huang , Yubao Wang , Jean Zhao , Hwan Geun Choi
IPC分类号: C07D403/12 , A61K31/337 , A61K31/55 , C07D223/16 , C07D401/14 , C07D403/14 , A61P35/00
CPC分类号: C07D403/12 , A61K31/337 , A61K31/55 , A61P35/00 , C07D223/16 , C07D231/12 , C07D401/12 , C07D401/14 , C07D403/14 , C07D413/12
摘要: Provided herein are small molecule inhibitors of maternal embryonic leucine zipper kinase (MELK) having the structure of formula (I), wherein X and R1-R3 are defined in the specification. The compounds are useful for treating cancer and other conditions or diseases associated with aberrant MELK expression. Also provided herein are pharmaceutical compositions comprising a compound of formula (I) and a pharmaceutically acceptable carrier. The invention also provides methods of treating cancers associated with over-expression of MELK.
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公开(公告)号:US20160046661A1
公开(公告)日:2016-02-18
申请号:US14775162
申请日:2014-03-13
IPC分类号: C07H19/16 , C07F9/6561 , C07H19/20
摘要: Described herein are compounds of Formulae (I)-(II), and pharmaceutically acceptable salts, and pharmaceutical compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating or preventing proliferative diseases such as cancers (e.g., lung cancer, large bowel cancer, pancreas cancer, biliary tract cancer, or endometrial cancer), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases in a subject.
摘要翻译: 本文描述了式(I) - (II)的化合物及其药学上可接受的盐及其药物组合物。 还提供了涉及用于治疗或预防增殖性疾病如癌症(例如肺癌,大肠癌,胰腺癌,胆道癌或子宫内膜癌),良性肿瘤,血管生成,炎性疾病的本发明化合物或组合物的方法和试剂盒 ,自身炎症性疾病和自身免疫性疾病。
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公开(公告)号:US20150094315A1
公开(公告)日:2015-04-02
申请号:US14321242
申请日:2014-07-01
发明人: Hwan Geun Choi , Taebo Sim , Nathanael Gray , Wenjun Zhou , Jae Won Chang , Jianming Zhang , Ellen Weisberg
IPC分类号: C07D513/04
CPC分类号: C07D513/04 , A61K31/437 , A61K31/496 , A61K31/4985 , A61K31/506 , A61K31/5377
摘要: The present application relates to therapeutic organic compounds, compositions comprising an effective amount of a therapeutic organic compound; and methods for treating and preventing disease comprising administering and effective amount of a therapeutic organic compound to a subject in need thereof.
摘要翻译: 本申请涉及治疗性有机化合物,包含有效量的治疗性有机化合物的组合物; 以及治疗和预防疾病的方法,包括向有需要的受试者施用和有效量的治疗性有机化合物。
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公开(公告)号:US20230348434A1
公开(公告)日:2023-11-02
申请号:US18309164
申请日:2023-04-28
发明人: Nathanael S. Gray , Pasi Janne , Hwan Geun Choi , Jaebong Jang
IPC分类号: C07D403/04 , C07D471/04 , C07D403/14 , C07D487/04
CPC分类号: C07D403/04 , C07D471/04 , C07D403/14 , C07D487/04
摘要: The application relates to a compound having Formula (I):
which modulates the activity of EGFR, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which EGFR plays a role.
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