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公开(公告)号：WO2018195321A1
公开(公告)日：2018-10-25
申请号：PCT/US2018/028382
申请日：2018-04-19
发明人： AKTOUDIANAKIS, Evangelos , APPLEBY, Todd , CHO, Aesop , DU, Zhimin , GRAUPE, Michael , GUERRERO, Juan A. , JABRI, Salman Y. , LAD, Lateshkumar Thakorlal , MACHICAO TELLO, Paulo A. , MEDLEY, Jonathan William , METOBO, Samuel E. , MUKHERJEE, Prasenjit Kumar , NADUTHAMBI, Devan , NOTTE, Gregory , PARKHILL, Eric Q. , PHILLIPS, Barton W. , SIMONOVICH, Scott Preston , SQUIRES, Neil H. , VENKATARAMANI, Chandrasekar , WANG, Peiyuan , WATKINS, William J. , XU, Jie , YANG, Kin Shing , ZIEBENHAUS, Christopher Allen
IPC分类号： C07D405/14 , A61K31/497 , C07D403/14 , C07D241/18 , C07D241/20 , C07D487/08 , C07D487/10 , C07D491/107 , C07D519/00 , A61P35/00 , C07D401/14 , C07D401/04 , C07D498/04 , C07D213/61 , C07D213/64
摘要： Compounds according to formula (I), methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are disclosed.
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公开(公告)号：WO2020264081A1
公开(公告)日：2020-12-30
申请号：PCT/US2020/039501
申请日：2020-06-25
发明人： AKTOUDIANAKIS, Evangelos , AMBROSI, Andrea , ASSELIN, Sylvie M. , BACHRACH, Florence J. , BADALOV, Pavel R. , CHIN, Gregory F. , LATHROP, Stephen P. , LEW, Willard , MACKMAN, Richard L. , MERIT, Jeffrey E. , METOBO, Samuel E. , MISH, Michael R. , PRITCHETT, Beau P. , PYUN, Hyung-Jung , REGENS, Christopher S. , VIEIRA, Tiago , WANG, Xianghong , WEINSTEIN, Adam B. , WENDERSKI, Todd A. , ZHENG, Zehua
IPC分类号： C07D471/04 , C07D413/04 , C07D213/81
摘要： The present disclosure provides methods for preparing (7?)-2-((2-amino-7- fluoropyrido[3,2-d]pyrimidin-4-yl)amino)-2-methylhexan-l-ol or a salt thereof and related key intermediates.
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公开(公告)号：WO2020014643A1
公开(公告)日：2020-01-16
申请号：PCT/US2019/041657
申请日：2019-07-12
发明人： AKTOUDIANAKIS, Evangelos , CHO, Aesop , GRAUPE, Michael , LAD, Lateshkumar Thakorlal , MACHICAO TELLO, Paulo A. , MEDLEY, Jonathan William , METOBO, Samuel E. , NADUTHAMBI, Devan , PHILLIPS, Barton W. , SIMONOVICH, Scott Preston , WANG, Peiyuan , WATKINS, William J. , XU, Jie , YANG, Kin Shing , ZIEBENHAUS, Christopher Allen
IPC分类号： A61P35/00 , C07D213/74 , C07D241/20 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D471/08 , C07D487/10 , A61K31/4439 , A61K31/444 , A61K31/497
摘要： Compounds and methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are disclosed.
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公开(公告)号：WO2020237025A1
公开(公告)日：2020-11-26
申请号：PCT/US2020/033955
申请日：2020-05-21
发明人： AKTOUDIANAKIS, Evangelos , CHANDRASEKHAR, Jayaraman , CODELLI, Julian A. , CONWAY, John H. , ELBEL, Kristyna M. , KALLA, Rao V. , METOBO, Samuel E. , MITCHELL, Scott A. , PERRY, Thao , SIMONOVICH, Scott P. , ZIEBENHAUS, Christopher A.
IPC分类号： A61P35/00 , C07D413/14 , C07D498/04 , A61K31/538 , A61K31/5383
摘要： The present disclosure relates generally to certain ene-oxindole compounds, pharmaceutical compositions comprising thereof. Also disclosed are methods of making and using said compounds and pharmaceutical compositions. The compounds and compositions disclosed herein may be used for the treatment or prevention of diseases, disorders, or infections modifiable by hematopoietic progenitor kinase 1 (HPK1) inhibitors, such as HBV, HIV, cancer, and/or a hyper-proliferative disease.
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公开(公告)号：WO2014182929A1
公开(公告)日：2014-11-13
申请号：PCT/US2014/037344
申请日：2014-05-08
发明人： AKTOUDIANAKIS, Evangelos , CHIN, Gregory , CORKEY, Britton Kenneth , DU, Jinfa , ELBEL, Kristyna , JIANG, Robert H. , KOBAYASHI, Tetsuya , LEE, Rick , MARTINEZ, Ruben , METOBO, Samuel E. , MISH, Michael , MUNOZ, Manuel , SHEVICK, Sophie , SPERANDIO, David , YANG, Hai , ZABLOCKI, Jeff
IPC分类号： C07D413/04 , C07D413/14 , C07D417/14 , A61K31/422 , A61P35/00
CPC分类号： C07D413/04 , C07D413/14 , C07D417/14 , C07D453/02 , C07D471/04
摘要： This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I) wherein R 1a , R 1b , R 2a , R 2b , R 3 , R 4a , R 4b , and R 5 are described herein.
摘要翻译： 本申请涉及可用作含溴结构域的蛋白质（包括含溴结构域蛋白质的蛋白质4（BRD4））的抑制剂或其它调节活性的化合物，以及含有这些化合物的组合物和制剂，以及 使用和制造这些化合物。 化合物包括其中R1a，R1b，R2a，R2b，R3，R4a，R4b和R5如本文所述的式（I）化合物。
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公开(公告)号：WO2019204609A1
公开(公告)日：2019-10-24
申请号：PCT/US2019/028129
申请日：2019-04-18
发明人： AKTOUDIANAKIS, Evangelos , CHO, Aesop , DU, Zhimin , GRAUPE, Michael , LAD, Lateshkumar Thakorlal , MACHICAO TELLO, Paulo A. , MEDLEY, Jonathan William , METOBO, Samuel E. , MUKHERJEE, Prasenjit Kumar , NADUTHAMBI, Devan , PARKHILL, Eric Q. , PHILLIPS, Barton W. , SIMONOVICH, Scott Preston , SQUIRES, Neil H. , WANG, Peiyuan , WATKINS, William J. , XU, Jie , YANG, Kin Shing , ZIEBENHAUS, Christopher Allen
IPC分类号： C07D401/14 , C07D401/04 , C07D401/06 , C07D401/12 , A61K31/4427 , A61P35/00 , C07D487/10 , C07D491/10
摘要： Compounds and methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are disclosed Formula (I)
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公开(公告)号：WO2018144605A1
公开(公告)日：2018-08-09
申请号：PCT/US2018/016243
申请日：2018-01-31
发明人： AKTOUDIANAKIS, Evangelos , CANALES, Eda , CURRIE, Kevin S. , KATO, Darryl , LI, Jiayao , LINK, John O. , METOBO, Samuel E. , SAITO, Roland D. , SCHROEDER, Scott D. , SHAPIRO, Nathan , TSE, Winston C. , WU, Qiaoyin
IPC分类号： C07D471/14 , C07D491/22 , C07D498/14 , C07D519/00 , A61K31/5025 , A61K31/503 , A61P31/12
摘要： The present disclosure generally relates to compounds and pharmaceutical compositions which may be used in methods of treating a hepatitis B virus infection.
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公开(公告)号：WO2020086556A1
公开(公告)日：2020-04-30
申请号：PCT/US2019/057407
申请日：2019-10-22
发明人： DU, Zhimin , GRAUPE, Michael , MACHICAO TELLO, Paulo A. , MEDLEY, Jonathan William , METOBO, Samuel E. , PARKHILL, Eric Q. , PHILLIPS, Barton W. , SIMONOVICH, Scott P. , WANG, Peiyuan , XU, Jie , ZIEBENHAUS, Christopher A.
IPC分类号： C07D217/04 , C07D401/12 , C07D401/14 , C07D413/04 , C07D417/14 , C07D471/04 , C07D471/08 , C07D487/04 , C07D495/04 , C07D513/04 , C07D519/00 , A61P35/00 , A61K31/444
摘要： Compounds and methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are disclosed. (I)
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公开(公告)号：WO2019160882A1
公开(公告)日：2019-08-22
申请号：PCT/US2019/017721
申请日：2019-02-12
发明人： AKTOUDIANAKIS, Evangelos , CHO, Aesop , DU, Zhimin , GRAUPE, Michael , LAD, Lateshkumar Thakorlal , MACHICAO TELLO, Paulo A. , MEDLEY, Jonathan William , METOBO, Samuel E. , MUKHERJEE, Prasenjit Kumar , NADUTHAMBI, Devan , PARKHILL, Eric Q. , PHILLIPS, Barton W. , SIMONOVICH, Scott Preston , SQUIRES, Neil H. , WANG, Peiyuan , WATKINS, William J. , XU, Jie , YANG, Kin Shing , ZIEBENHAUS, Christopher Allen
IPC分类号： C07D405/14 , A61K31/497 , C07D403/14 , C07D241/18 , C07D241/20 , C07D487/08 , C07D487/10 , C07D491/107 , C07D519/00 , A61P35/00
摘要： Compounds of Formula (I), methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are disclosed.
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公开(公告)号：WO2014160873A1
公开(公告)日：2014-10-02
申请号：PCT/US2014/032031
申请日：2014-03-27
发明人： AKTOUDIANAKIS, Evangelos , CHIN, Gregory , CORKEY, Britton Kenneth , DU, Jinfa , ELBEL, Kristyna , JIANG, Robert H. , KOBAYASHI, Tetsuya , MARTINEZ, Ruben , METOBO, Samuel E. , MISH, Michael , SHEVICK, Sophie , SPERANDIO, David , YANG, Hai , ZABLOCKI, Jeff
IPC分类号： C07D413/14 , C07D413/04 , C07D417/14 , A61K31/42 , A61P35/00
CPC分类号： C07D413/14 , C07D413/04 , C07D417/14
摘要： This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I) wherein R 1a , R 1b , R 2a , R 2b , R 3 , and X are described herein.
摘要翻译： 本申请涉及可用作含溴结构域的蛋白质（包括含有溴结构域的蛋白质4（BRD4））的抑制剂或可以调节其中含有溴结构域的蛋白质的活性的化合物，以及含有这些化合物的组合物和制剂，以及 使用和制造这些化合物。 化合物包括其中R1a，R1b，R2a，R2b，R3和X在本文中描述的式（I）的化合物。
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